DOCSLIB.ORG

United States Patent (19) 11 Patent Number: 5,565,485 Bagley Et Al

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
United States Patent (19) 11 Patent Number: 5,565,485 Bagley Et Al US005565485A United States Patent (19) 11 Patent Number: 5,565,485 Bagley et al. (45) Date of Patent: Oct. 15, 1996 (54) BLPHENYL COMPOUNDS USEFUL OR "BQ123, An ET(A) Receptor Antagonist, Attenuates ENDOTHELIN ANTAGONSTS Hypoxic Pulmonary-Hypertension in Rats' Bonvallet, S.T., et al. American Journal of Physiology, vol. 266, No. 4, (Apr. (75) Inventors: Scott W. Bagley, Groton, Conn.; 1994), pp. H1327-1331. Theodore P. Broten, Ambler, Pa.; "Endothelin-A Receptor Antagonist Prevents Acute Prasun K. Chakravarty, Edison, N.J.; Hypoxia-Induced Pulmonary-Hypertension in the Rat' Daljit S. Dhanoa, Secaucus, N.J.; Oparil, S., et al. American Journal of Physiology-Lung Kenneth J. Fitch, Scotch Plains, N.J.; Cellular and Molecular Physiology, vol. 12, No. 1, (Jan. William J. Greenlee, Teaneck, N.J.; Nancy J. Kevin, Clifton, N.J.; Douglas 1995), pp. L95-L100. J. Pettibone, Chalfont, Pa.; Ralph A. "Protection from Pulmonary Hypertension with an Orally Rivero, Tinton Falls, N.J.; Thomas F. Active Endothelin Receptor Antagonist in Hypoxic Rats' Walsh, Westfield, N.J.; David L. American Journal of Physiology-Heart and Circulatory Williams, Jr., Telford, Pa.; Richard B. Physiology, vol. 37, No. 2, (Feb. 1995), pp. H828-H835. Toupence, Cranford, N.J.; Jay M. "Endothelial Dysfunction and Remodeling of the Pulmonary Matthews, Fords, N.J. Ciculation in Chronic Hypoxic Pulmonary-Hypertension' Dinhxuan, A. T., et al. ACP-Applied Cardiopulmonary 73 Assignee: Merck & Co., Inc., Rahway, N.J. Pathophysiology, vol. 5, No. 2, (1994), pp. 93-99. "Cyclosporine-induced Elevation in Circulating Endothe 21 Appl. No.: 294,232 lin-1 in Patients with Solid-Organ Transplants' Grieff, M., et al. Transplantation vol. 54, No. 4, (Oct. 1993), pp. 22 Filed: Aug. 22, 1994 880-884. “Cyclosporine-Induced Hypertension After Transplanta Related U.S. Application Data tion' Textor, S.C., et al. Mayo Clinical Proceedings, vol. 69, 63) Continuation-in-part of Ser. No. 287,374, Aug. 8, 1994, (1994), pp. 1182-1193. abandoned, which is a continuation-in-part of Ser. No. "A Role of Endogenous Endothelin-1 in Neointimal For 197,467, Feb. 24, 1994, abandoned, which is a continuation mation. After Rat Carotid Artery Balloon Angioplasty' Dou in-part of Ser. No. 34,455, Mar. 19, 1993, abandoned. glas S. A., et al. Circulation Research, vol. 75, (1994), pp. (51) Int. Cl. A61K 31/335; A61K 31/535; 190-197. C07D 319/08; CO7D 265/30 52 U.S. Cl. .......................... 514/452, 514/146; 514/231; (List continued on next page.) 514/312; 514/347; 514/231.5; 514/381; 514/461; 514/464; 514/465; 514/469; 514/470; Primary Examiner Yogendra N. Gupta 514/869; 544/146; 54.6/153; 546/293; 548/253; Attorney, Agent, or Firm-Valerie J. Camara; Mark R. 548/254; 549/220; 549/362; 549/434; 549/469 Daniel (58) Field of Search .................................. 514/146, 231, 514/312, 347, 381, 452, 461, 464, 465, 57 ABSTRACT 466, 469, 470, 869; 549/220, 221, 362, 434, 436, 437, 438, 439, 440, 441, 443, Phenoxyphenylacetic acids and derivatives of the general 444, 445, 446, 447, 448, 469, 470, 471; structural formula I 548/253,254; 54.4/146; 54.6/153,293 R12 I (56) References Cited PUBLICATIONS R9 R10 Naim et al., Indian J. Chem. Vol. 19B, pp. 622-623 1980. Crenshaw et al., J. Org. Chem. vol. 47, pp. 101-104 1982. X Z Michael E. Jung et al., Heterocycles, vol.30(2) pp. 839-853, R8 1990. Saraiva et al., CA114(19): 185076t, 1990. R3b R1 "Antihypertensive Effects of the Endothelin Receptor Antagonist BQ-123 in Conscious Spontaneously Hypeten sive Rats' E. H. Ohlstein, et al. Journal of Cardiovascular R3a R2 Pharmacology, vol. 22, (Suppl. 8), 1993, pp. S321-S324. have endothelin antagonist activity and are useful in treating "Direct and Sympathetically Mediated Vasoconstriction in cardiovascular disorders, such as hypertension, postis Essential Hypertension” W. G. Haynes, et al.J. Clin. Invest., chemic renal failure, vasospasm, cerebral and cardiac vol. 94, Oct. 1994, pp. 1359–1364. ischemia, myocardial infarction, endotoxic shock, benign "Role of Endothelin in Hypertension” B. K. Krämer, et al. prostatic hyperplasia, inflammatory diseases including Clin. Investig., vol. 72, (1994), pp. 88-93. Raynaud's disease and asthma. "Potential Role of Endothelin in Hypertension' T. F. Lis cher, et al. Hypertension, vol. 21, No. 6, Part 1, Jun. 1993, pp. 752-757. 23 Claims, No Drawings 5,565,485 Page 2 PUBLICATIONS - "Raynaud-Phenomenon' Coffman, J. D., et al. Current "125I-Endothelin-1 Binding to Vasa Vasorum and Opinion in Cardiology, vol. 8, No. 5, (Sep. 1993), pp. Regions of Neovascularization in Human and Por 821-828. cine-Blood Wessels: A Possible Role for Endothelin in "Parameters of Vascular Function in Idiopathic and Silic Intimal Hyperplasia and Atheroscelerosis' Dashwood, M. a-Induced Systemic-Sclerosis' Haustein, U. F., et al. Hau R., et al. Journal of Cardiovascular Pharmacology, vol. 22, tarzt, vol. 44, No. 11, (Nov. 1993), pp. 717–722. (Suppl. 8), (1993), pp. S343–347. "The Endothelin-1 Receptor Antagonist BQ-123 Reduces "Circulating Endothelin-1 Levels in Systemic-Sclerosis Infarct Size in a Canine Model of Coronary Occlusion and Subsets-A Marker of Fibrosis or Vascular Dysfunction' Reperfusion' Grover, G. J., et al. Cardiovascular Research, Vancheeswaran, R., et al. Journal of Rheumatology, vol. 21, vol. 75, No. 9, (Sep. 1993), pp. 1613–1618. No. 10, (Oct. 1994), pp. 1838-1844. "The Effects of the Endothelin ETa Receptor Antagonist, "Endothelin and Collagen Vascular Disease: A Review with FR139317, on Infarct Size in a Rabbit Model of Acute Special Reference to Raynauds-Phenomenon and Myocardial Ischemia and Reperfusion" McMurdo, L., et al. Systemic-Sclerosis'Yamane, K. Internal Medicine, vol. 33, British Journal of Pharmacology, (1994), vol. 112, pp. No. 10, (Oct. 1994), pp. 579–582. 75-80. "A Pathogenic Role for Endothelin in Raynauds-Phenom "Vasodilator Effects of the Endothelin-1 Receptor Antago enon' Bottomley, W., et al. Acta Dermato-Venereologica, nist Bosentan in Patients with Severe Chronic Heart Failure' vol. 74, No. 6, (Nov. 1994), pp. 433-434. Kiowski, W., et al. Journal Am. College of Cardiology, Feb. "BQ 123, A Peptidic Endothelin ETA Receptor Antagonist, 1995, pp. 296A, abstract No. 779-1. Prevents the Early Cerebral Vasospasm Following Sub "Nonpeptide Endothelin Receptor Antagonists. III, Effect of arachnoid Hemorrhage. After Interacisternal but not Intrave SB 2.09670 and BQ123 on Acute Renal Failure in Anesthe nous-Injection” Clozel, M., et al. Life Sciences, vol. 52, No. tized Dogs' Brooks, D. P., et al. Journal of Pharmacology 9, (1993), pp. 825–834. and Experimental Therapeutics, vol. 271, (1994), pp. 769-775. “An Endothelin ET(A) Receptor Antagonist, FR139317, "Reversal of Postischemic Acute Renal Failure with a Selec Ameliorates Cerebral Vasospasm in Dogs' Nirei, H., et al. tive Endothelina Receptor Antagonist in the Rat' Gellai, M., Life Sciences, vol. 52, No. 23, (1993), pp. 1869-1874. et al. Journal of Clinical Investigator, vol. 93, (1994), pp. "Reversal of Subarachnoid Hemorrhage-Induced Vasocon 900-906. striction with an Endothelin Receptor Antagonist' Foley, P. "Effects of BQ-123 on Renal-Function and Acute L. et al. Neurosurgery, vol. 34, No. 1, (Jan. 1994), pp. Cyclosporine Induced Renal Dysfunction', Kivlighn, S. D. 108-113. et al., Kidney International, vol. 45, No. 1, (Jan. 1994), pp. "Endothelin Levels Increase in Rat Focal and Global-Is 131-136. chemia' Barone, F. C., et al. Journal of Cerebral Blood Flow "Endotoxin-Mediated Changes In Plasma Endothelin Con and Metabolism, vol. 14, No. 2, (Mar. 1994), pp. 337-342. centrations, Renal Endothelin Receptor And Renal-Func "Endothelin ET(A) and ETOB) Receptors in Subarachnoid tion', Nambi, P. et al., vol. 48, No. 3, (Mar. 1994), pp. Hemorrhage-Induced Cerebral Vasospasm' Zuccarello, M., 147-156. et al. European Journal of Pharmacology, vol. 259, No. 1, "Effect of Total-Body Cold-Exposure on Plasma-Concen (Jun. 23 1994), pp. R1-R2. trations of Vonwillebrand-Factor, Endothelin-1 Thrombo modulin in Systemic Lupus-Erythematosus Patients with or "Changes of Endothelin Concentration in Cerebrospi without Raynauds-Phenomeon', Matsuda, J.,et al. Acta nal-Fluid and Plasma of Patients with Aneurysmal Sub Haematologica, vol. 88, No. 4, (1992), pp. 189-193. arachnoid Hemorrhage' Shirakami, G., et al. Acta Anaes "Localization of Endothelin-1 and Its Binding-Sites in thesiologica Scandinavica, vol. 38, No. 5, (Jul. 1994), pp. Scleroderma Skin' Vancheeswaran, R., et al. Journal of 457-461. Rheumatology, vol. 21, No. 7, (Jul. 1994), pp. 1268-1276. "Prevention of Delayed Vasospasm by an Endothelin ET(A) "Increased Endothelin-1 Production in Fibroblasts Derived Receptor Antagonist, BQ-123-Change of ET(A) Receptor from Patients with Systemic-Sclerosis' Kawaguchi, Y., et Messenger-RNA Expression in a Canine Subarachnoid al. Annals of the Rheumatic Diseases, vol. 53, No. 8, (Aug. Hemorrhage Model'Itoh, S., et al., Journal of Neurosurgery, 1994), pp. 506-510. vol. 81, No. 5, (Nov. 1994), pp. 759-764. "Characterization of Endothelin-Binding Sites in Human "Endothelin Concentrations in Patients with Aneurysmal Skin and Their Regulation in Primary Raynauds-Phenom Subarachnoid Hemorrhage-Correlation with Cerebral enon and Systemic-Sclerosis' Knock G. A., et al. Journal of Vasospasm, Delayed Ischemic Neurological Deficits, and Investigative Dermatology, vol. 101, No. 1, (Jul. 1993), pp. Volume of Hematoma' Seifert V., et al. Journal of Neuro 73-78. surgery, vol. 82, No. 1, (Jan. 1995), pp.55-62. 5,565,485 1 2 BPHENYL COMPOUNDS USEFUL OR muscle cells which would suggest a possible relevance to ENDOTHELIN ANTAGONSTS arterial hypertrophy.' Endothelin receptors are present in high concentration in RELATED APPLICATIONS the peripheral tissues and also in the central nervous system, 5 and cerebral administration of endothelin has been shown to The present application is a continuation in part applica induce behavioral changes in animals, suggesting that endot tion of Case 18893IB, U.S.
Load more

Recommended publications
  • A2) United States Patent (10) Patent No.: US 8,940,711 B2 Olsonet Al
    US008940711B2 a2) United States Patent (10) Patent No.: US 8,940,711 B2 Olsonet al. (45) Date of Patent: Jan. 27, 2015 (54) MICRO-RNA FAMILY THAT MODULATES C1I2N 2310/321 (2013.01); C12N 2310/346 FIBROSIS AND USES THEREOF (2013.01); CI2N 2310/3515 (2013.01); C12N (71) Applicant: The Board of Regents, The University 2320/31 (2013.01); CI2N 2330/10 (2013.01) of Texas System, Austin, TX (US) USPC iececcsesseeseeesenensceesensessecsenesenscnseeee 514/444 (58) Field of Classification Search (72) Inventors: Erie N. Olson, Dallas, TX (US); Eva USPC iececcsesseeseeesenensceesensessecsenesenscnseeee 514/44A van Rooij, Utrecht (NL) See application file for complete search history. (56) References Cited (73) Assignee: The Board of Regents, The University of Texas System, Austin, TX (US) U.S. PATENT DOCUMENTS Notice: Subject to any disclaimer, the term of this 7,232,806 B2 6/2007 Tuschletal. (*) 7,674,617 B2 3/2010 Kim etal. patent is extended or adjusted under 35 2005/0059005 Al 3/2005 Tuschletal. U.S.C. 154(b) by 1 day. 2005/0222399 Al 10/2005 Bentwich 2005/0261218 Al 11/2005 Esau etal. (21) Appl. No.: 13/840,242 2006/0019286 Al 1/2006 Horvitz et al. 2006/0105360 Al 5/2006 Croceet al. Filed: Mar.15, 2013 2006/0185027 Al 8/2006 Bartel etal. (22) 2006/0247193 Al 11/2006 Taira etal. 2007/0087335 Al 4/2007 Brahmacharietal. (65) Prior Publication Data 2007/0092882 Al 4/2007 Wangetal. US 2013/0261169 Al Oct. 3, 2013 2008/0050722 Al 2/2008 Kim etal. 2008/0176766 Al 7/2008 Brown etal.
    [Show full text]
  • Deliverable 5.A Interim Report on the Study Results APPENDIX 2
    Deliverable 5.a Interim report on the study results APPENDIX 2: Algorithms used to identify study variables for service contract EMA/2011/38/CN ‐ PIOGLITAZONE November 28th 2012 D5.a Interim report on the study results (Appendix 2) for Service Contract EMA/2011/38/CN PIOGLITAZONE Author(s): Vera Ehrenstein (AUH‐AS) APPENDIX 2. ALGORITHMS USED TO IDENTIFY STUDY VARIABLES Algorithms for AU Database DISEASE/CONDITION ICD-8 CODE (1977-1993) ICD-10 CODE (1994-) Diabetes type 2 250.00; 250.06; 250.07; 250.09 E11.0; E11.1; E11.9 Cancer of bladder 188 C67 Haematuria N/A R31 Haematuria, unspecified B18, K70.0–K70.3, K70.9, K71, K73, Mild hepatic impairment 571, 573.01, 573.04 K74, K76.0 Moderate to severe hepatic 070.00, 070.02, 070.04, 070.06, B15.0, B16.0, B16.2, B19.0, K70.4, impairment 070.08, 573.00, 456.00–456.09 K72, K76.6, I85 Acute myocardial infarction 410 I21-I23 Acute coronary syndrome 410, 413 I20-I24 Ischemic heart disease 410-414 I20-I25 427.09, 427.10, 427.11, 427.19, Congestive heart failure I50, I11.0, I13.0,I13.2 428.99, 782.49; Acute renal failure N/A N17 Diabetic coma N/A E10.0, E11.0, E12.0,E13.0, E14.0 Diabetic acidosis N/A E10.1, E11.1, E12.1,E13.1, E14.1 F10.1-F10.9, G31.2, G62.1, G72.1, Alcoholism 291, 303, 577.10, 571.09, 571.10 I42.6, K29.2, K86.0, Z72.1 Obesity 277.99 E65-E66 D5.a Interim report on the study results (Appendix 2) for Service Contract EMA/2011/38/CN PIOGLITAZONE Author(s): Vera Ehrenstein (AUH‐AS) Algorithms for defining acute events in Denmark, ICD-10 code Event ICD-10 code I21.x, I23.x http://apps.who.int/classifications/icd10/browse/2010/en#/I21
    [Show full text]
  • Title 16. Crimes and Offenses Chapter 13. Controlled Substances Article 1
    TITLE 16. CRIMES AND OFFENSES CHAPTER 13. CONTROLLED SUBSTANCES ARTICLE 1. GENERAL PROVISIONS § 16-13-1. Drug related objects (a) As used in this Code section, the term: (1) "Controlled substance" shall have the same meaning as defined in Article 2 of this chapter, relating to controlled substances. For the purposes of this Code section, the term "controlled substance" shall include marijuana as defined by paragraph (16) of Code Section 16-13-21. (2) "Dangerous drug" shall have the same meaning as defined in Article 3 of this chapter, relating to dangerous drugs. (3) "Drug related object" means any machine, instrument, tool, equipment, contrivance, or device which an average person would reasonably conclude is intended to be used for one or more of the following purposes: (A) To introduce into the human body any dangerous drug or controlled substance under circumstances in violation of the laws of this state; (B) To enhance the effect on the human body of any dangerous drug or controlled substance under circumstances in violation of the laws of this state; (C) To conceal any quantity of any dangerous drug or controlled substance under circumstances in violation of the laws of this state; or (D) To test the strength, effectiveness, or purity of any dangerous drug or controlled substance under circumstances in violation of the laws of this state. (4) "Knowingly" means having general knowledge that a machine, instrument, tool, item of equipment, contrivance, or device is a drug related object or having reasonable grounds to believe that any such object is or may, to an average person, appear to be a drug related object.
    [Show full text]
  • Guidance for the Format and Content of the Protocol of Non-Interventional
    PASS information Title Metformin use in renal impairment Protocol version identifier Version 2 Date of last version of 30 October 2013 protocol EU PAS register number Study not registered Active substance A10BA02 metformin Medicinal product Metformin Product reference N/A Procedure number N/A Marketing authorisation 1A Farma, Actavis, Aurobindo, Biochemie, Bluefish, holder(s) Hexal, Mylan, Orifarm, Pfizer, Sandoz, Stada, Teva Joint PASS No Research question and To assess the use and safety of metformin in patients objectives with and without renal insufficiency in current clinical practice in at least two EU Member States. Country(-ies) of study Denmark, United Kingdom Author Christian Fynbo Christiansen, MD, PhD Page 1/214 Marketing authorisation holder(s) Marketing authorisation N/A holder(s) MAH contact person N/A Page 2/214 1. Table of Contents PASS information .......................................................................................................... 1 Marketing authorisation holder(s) .................................................................................... 2 1. Table of Contents ...................................................................................................... 3 2. List of abbreviations ................................................................................................... 4 3. Responsible parties .................................................................................................... 5 4. Abstract ..................................................................................................................
    [Show full text]
  • Association of Oral Anticoagulants and Proton Pump Inhibitor Cotherapy with Hospitalization for Upper Gastrointestinal Tract Bleeding
    Supplementary Online Content Ray WA, Chung CP, Murray KT, et al. Association of oral anticoagulants and proton pump inhibitor cotherapy with hospitalization for upper gastrointestinal tract bleeding. JAMA. doi:10.1001/jama.2018.17242 eAppendix. PPI Co-therapy and Anticoagulant-Related UGI Bleeds This supplementary material has been provided by the authors to give readers additional information about their work. Downloaded From: https://jamanetwork.com/ on 10/02/2021 Appendix: PPI Co-therapy and Anticoagulant-Related UGI Bleeds Table 1A Exclusions: end-stage renal disease Diagnosis or procedure code for dialysis or end-stage renal disease outside of the hospital 28521 – anemia in ckd 5855 – Stage V , ckd 5856 – end stage renal disease V451 – Renal dialysis status V560 – Extracorporeal dialysis V561 – fitting & adjustment of extracorporeal dialysis catheter 99673 – complications due to renal dialysis CPT-4 Procedure Codes 36825 arteriovenous fistula autogenous gr 36830 creation of arteriovenous fistula; 36831 thrombectomy, arteriovenous fistula without revision, autogenous or 36832 revision of an arteriovenous fistula, with or without thrombectomy, 36833 revision, arteriovenous fistula; with thrombectomy, autogenous or nonaut 36834 plastic repair of arteriovenous aneurysm (separate procedure) 36835 insertion of thomas shunt 36838 distal revascularization & interval ligation, upper extremity 36840 insertion mandril 36845 anastomosis mandril 36860 cannula declotting; 36861 cannula declotting; 36870 thrombectomy, percutaneous, arteriovenous
    [Show full text]
  • Pharmaceuticals As Environmental Contaminants
    PharmaceuticalsPharmaceuticals asas EnvironmentalEnvironmental Contaminants:Contaminants: anan OverviewOverview ofof thethe ScienceScience Christian G. Daughton, Ph.D. Chief, Environmental Chemistry Branch Environmental Sciences Division National Exposure Research Laboratory Office of Research and Development Environmental Protection Agency Las Vegas, Nevada 89119 [email protected] Office of Research and Development National Exposure Research Laboratory, Environmental Sciences Division, Las Vegas, Nevada Why and how do drugs contaminate the environment? What might it all mean? How do we prevent it? Office of Research and Development National Exposure Research Laboratory, Environmental Sciences Division, Las Vegas, Nevada This talk presents only a cursory overview of some of the many science issues surrounding the topic of pharmaceuticals as environmental contaminants Office of Research and Development National Exposure Research Laboratory, Environmental Sciences Division, Las Vegas, Nevada A Clarification We sometimes loosely (but incorrectly) refer to drugs, medicines, medications, or pharmaceuticals as being the substances that contaminant the environment. The actual environmental contaminants, however, are the active pharmaceutical ingredients – APIs. These terms are all often used interchangeably Office of Research and Development National Exposure Research Laboratory, Environmental Sciences Division, Las Vegas, Nevada Office of Research and Development Available: http://www.epa.gov/nerlesd1/chemistry/pharma/image/drawing.pdfNational
    [Show full text]
  • Association of Oral Anticoagulants and Proton Pump Inhibitor Cotherapy with Hospitalization for Upper Gastrointestinal Tract Bleeding
    Supplementary Online Content Ray WA, Chung CP, Murray KT, et al. Association of oral anticoagulants and proton pump inhibitor cotherapy with hospitalization for upper gastrointestinal tract bleeding. JAMA. doi:10.1001/jama.2018.17242 eAppendix. PPI Co-therapy and Anticoagulant-Related UGI Bleeds This supplementary material has been provided by the authors to give readers additional information about their work. Downloaded From: https://edhub.ama-assn.org/ on 09/24/2021 Appendix: PPI Co-therapy and Anticoagulant-Related UGI Bleeds Table 1A Exclusions: end-stage renal disease Diagnosis or procedure code for dialysis or end-stage renal disease outside of the hospital 28521 – anemia in ckd 5855 – Stage V , ckd 5856 – end stage renal disease V451 – Renal dialysis status V560 – Extracorporeal dialysis V561 – fitting & adjustment of extracorporeal dialysis catheter 99673 – complications due to renal dialysis CPT-4 Procedure Codes 36825 arteriovenous fistula autogenous gr 36830 creation of arteriovenous fistula; 36831 thrombectomy, arteriovenous fistula without revision, autogenous or 36832 revision of an arteriovenous fistula, with or without thrombectomy, 36833 revision, arteriovenous fistula; with thrombectomy, autogenous or nonaut 36834 plastic repair of arteriovenous aneurysm (separate procedure) 36835 insertion of thomas shunt 36838 distal revascularization & interval ligation, upper extremity 36840 insertion mandril 36845 anastomosis mandril 36860 cannula declotting; 36861 cannula declotting; 36870 thrombectomy, percutaneous, arteriovenous
    [Show full text]
  • |||||IIIUSOO57673 10A United States Patent (19) 11 Patent Number: 5,767,310 Bagley Et Al
    |||||IIIUSOO57673 10A United States Patent (19) 11 Patent Number: 5,767,310 Bagley et al. 45 Date of Patent: Jun. 16, 1998 (54) PHENOXYPHENYLACETIC ACD 2259 540 3/993 United Kingdom. DERVATIVES WO 92 O0952 1/992 WIPO WO 92 12991 6/992 WIPO (75) Inventors: Scott W. Bagley, Groten. Conn.; WO 92/15321 9/1992 WIPO Theodore P. Broten, Ambler, Pa.; WO 92/2O706 11|1992 WIPO WO 93 08799 5/1993 WIPO : Prasun K. Chakravarty. Edison, N.J.; WO 93 O144 5/1993 WIPO Daljit S. Dhanoa, La Jolla, Calif.; WO 93 13052 7/1993 WIPO Kenneth J. Fitch, Cranford, N.J.; WO 93 13069 7/1993 WIPO William J. Greenlee, Teaneck, N.J.; WO 93 23.404 11/1993 WIPO Nancy Jo Kevin, Clifton, N.J.; Douglas WO 94 14796 12/1993 WIPO J. Pettibone. Chalfont, Pa.; Ralph A. WO 94 O2474 2/1994 WIPO Rivero, North Wales, Pa.; James R. WO 94. 14434 7/1994 WIPO. Tata, Westfield; Thomas F. Walsh. Watchung, both of N.J.; David L. OTHER PUBLICATIONS Williams, Jr., Telford, Pa, "Endothelin: A New Challenge", Doherty, A.M., J. Med. Chem. vol. 35. No. 9, (1992), pp. 1493-1508. 73) Assignee: Merck & Co., Inc.. Rahway, N.J. "Studies on the Chemical Constituents of Rutaceous 21 Appl. No.: 507,492 Plants. ''). Development of a Versatile Method for the Synthesis of Antitumor-Active Benzoic phenanthridine (22 PCT Filled: Mar 17, 1994 Alkaloids. (2)' Preparation of 2-Aryl-1-tetralone Deriva 86) PCT No.: PCT/US94/02871 tives', Ishii, H. et al. Chem. Pharm. Bulletin, vol.
    [Show full text]
  • Table of Antihypertensive Drugs
    Chapter 14 Table of Antihypertensive Drugs F. GROSS and J. B. LUTH The following tables give information about the most important drugs used today in the treatment of high blood pressure. These lists do not in any way aim for completeness, in particular with respect to brand names, which are much more numerous for several of the mentioned products. The usual forms of adminis­ tration and average dosages are included, but various other schemes are also recommended for some drugs in some countries. What is said for the single entities with respect to completeness holds true even more for the fixed combinations, of which only a fraction of those marketed in a number or'countries has been included. Some examples of the combinations that make sense to the authors have been mentioned; many have been omitted; however, deletion does not mean in all cases - but it does in some - that the combi­ nation is considered useless. If a barbiturate is added to reserpine and a diuretic, it is difficult to ascribe to the new combination an improved effect on the high blood pressure. Quite a few more examples could be given, where the addition of a further ingredient to the basic combination of reserpine and a diuretic is nothing but the mixing in of a special flavor, and not of an antihypertensive component. Some of the readers may also feel that too many drugs and combinations have been listed, and they may never have heard the names of quite a few of them. Despite the incompleteness of the list, it gives an impression of the huge variety of pre­ parations, which will further increase with the growing number of /J-adrenergic blockers and their combinations with other drugs.
    [Show full text]
  • Anatomical Classification Guidelines V2020 EPHMRA ANATOMICAL
    EPHMRA ANATOMICAL CLASSIFICATION GUIDELINES 2020 Anatomical Classification Guidelines V2020 "The Anatomical Classification of Pharmaceutical Products has been developed and maintained by the European Pharmaceutical Marketing Research Association (EphMRA) and is therefore the intellectual property of this Association. EphMRA's Classification Committee prepares the guidelines for this classification system and takes care for new entries, changes and improvements in consultation with the product's manufacturer. The contents of the Anatomical Classification of Pharmaceutical Products remain the copyright to EphMRA. Permission for use need not be sought and no fee is required. We would appreciate, however, the acknowledgement of EphMRA Copyright in publications etc. Users of this classification system should keep in mind that Pharmaceutical markets can be segmented according to numerous criteria." © EphMRA 2020 Anatomical Classification Guidelines V2020 CONTENTS PAGE INTRODUCTION A ALIMENTARY TRACT AND METABOLISM 1 B BLOOD AND BLOOD FORMING ORGANS 28 C CARDIOVASCULAR SYSTEM 35 D DERMATOLOGICALS 50 G GENITO-URINARY SYSTEM AND SEX HORMONES 57 H SYSTEMIC HORMONAL PREPARATIONS (EXCLUDING SEX HORMONES) 65 J GENERAL ANTI-INFECTIVES SYSTEMIC 69 K HOSPITAL SOLUTIONS 84 L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS 92 M MUSCULO-SKELETAL SYSTEM 102 N NERVOUS SYSTEM 107 P PARASITOLOGY 118 R RESPIRATORY SYSTEM 120 S SENSORY ORGANS 132 T DIAGNOSTIC AGENTS 139 V VARIOUS 141 Anatomical Classification Guidelines V2020 INTRODUCTION The Anatomical Classification was initiated in 1971 by EphMRA. It has been developed jointly by Intellus/PBIRG and EphMRA. It is a subjective method of grouping certain pharmaceutical products and does not represent any particular market, as would be the case with any other classification system.
    [Show full text]
  • Blood Pressure-Lowering Efficacy of Reserpine for Primary Hypertension (Review)
    Cochrane Database of Systematic Reviews Blood pressure-lowering efficacy of reserpine for primary hypertension (Review) Shamon SD, Perez MI Shamon SD, Perez MI. Blood pressure-lowering efficacy of reserpine for primary hypertension. Cochrane Database of Systematic Reviews 2016, Issue 12. Art. No.: CD007655. DOI: 10.1002/14651858.CD007655.pub3. www.cochranelibrary.com Blood pressure-lowering efficacy of reserpine for primary hypertension (Review) Copyright © 2016 The Cochrane Collaboration. Published by John Wiley & Sons, Ltd. TABLE OF CONTENTS HEADER....................................... 1 ABSTRACT ...................................... 1 PLAINLANGUAGESUMMARY . 2 BACKGROUND .................................... 2 OBJECTIVES ..................................... 3 METHODS ...................................... 3 RESULTS....................................... 5 Figure1. ..................................... 6 Figure2. ..................................... 8 Figure3. ..................................... 10 Figure4. ..................................... 11 Figure5. ..................................... 12 Figure6. ..................................... 13 DISCUSSION ..................................... 13 AUTHORS’CONCLUSIONS . 14 ACKNOWLEDGEMENTS . 14 REFERENCES ..................................... 15 CHARACTERISTICSOFSTUDIES . 18 DATAANDANALYSES. 26 Analysis 1.1. Comparison 1 Reserpine versus placebo, Outcome 1 Weighted mean change in systolic blood pressure. 27 Analysis 1.2. Comparison 1 Reserpine versus placebo, Outcome 2 Weighted mean
    [Show full text]
  • (12) United States Patent (10) Patent No.: US 9,456,997 B2 Stauffer Et Al
    USOO9456997B2 (12) United States Patent (10) Patent No.: US 9,456,997 B2 Stauffer et al. (45) Date of Patent: Oct. 4, 2016 (54) SELECTIVE INHIBITION OF (52) U.S. Cl. B1-ADRENERGIC RECEPTORS FOR THE CPC ........... A61K 31/137 (2013.01); A61K 3 1/138 TREATMENT OF PEDIATRC HEART (2013.01); A61K 31/165 (2013.01); A61 K FAILURE 3 1/35 (2013.01); A61K 31/352 (2013.01); (75) Inventors: Brian Stauffer, Aurora, CO (US); A61K 45/06 (2013.01) Carmen Sucharov, Aurora, CO (US); (58) Field of Classification Search Shelley Miyamoto, Aurora, CO (US) CPC ............. A61K 31/137; A61K 31/138: A61 K (73) Assignee: THE REGENTS OF THE 3 1/165; A61K 31/35; A61K 31/352: A61 K UNIVERSITY OF COLORADO, A 45/06 BODY CORPORATE, Denver, CO See application file for complete search history. (US) (56) References Cited (*) Notice: Subject to any disclaimer, the term of this patent is extended or adjusted under 35 U.S. PATENT DOCUMENTS U.S.C. 154(b) by 215 days. 6,545,040 B1 4/2003 Xhonneux et al. 2007/OO 14733 A1 1/2007 O'Donnell et al. (21) Appl. No.: 13/817,969 (Continued) (22) PCT Filed: Aug. 25, 2011 FOREIGN PATENT DOCUMENTS (86). PCT No.: PCT/US2O11AO49123 WO WO2006130174 * 12/2006 ........... A61K 31,352 S 371 (c)(1), WO WO 2009,1384.51 11/2009 (2), (4) Date: Jun. 6, 2013 OTHER PUBLICATIONS (87) PCT Pub. No.: WO2012/027557 Ahmet et al., “Beneficial effects of chronic pharmacological PCT Pub. Date: Mar. 1, 2012 manipulation of beta-adrenoreceptor Subtype signaling in rodent (65) Prior Publication Data dilated ischemic cardiomyopathy'.
    [Show full text]