A Phase 3, Multicenter, Randomized, Double-Blind
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Dexamethasone sodium phosphate ( 0.339 ) Melengestrol acetate ( 0.282 ) 17beta−Trenbolone ( 0.252 ) 17alpha−Estradiol ( 0.24 ) 17alpha−Hydroxyprogesterone ( 0.238 ) Triamcinolone ( 0.233 ) Zearalenone ( 0.216 ) CP−634384 ( 0.21 ) 17alpha−Ethinylestradiol ( 0.203 ) Raloxifene hydrochloride ( 0.203 ) Volinanserin ( 0.2 ) Tiratricol ( 0.197 ) trans−Retinoic acid ( 0.192 ) Chlorpromazine hydrochloride ( 0.191 ) PharmaGSID_47315 ( 0.185 ) Apigenin ( 0.183 ) Diethylstilbestrol ( 0.178 ) 4−Dodecylphenol ( 0.161 ) 2,2',6,6'−Tetrachlorobisphenol A ( 0.156 ) o,p'−DDD ( 0.155 ) Progesterone ( 0.152 ) 4−Hydroxytamoxifen ( 0.151 ) SSR150106 ( 0.149 ) Equilin ( 0.3 ) 3,5,3'−Triiodothyronine ( 0.256 ) 17−Methyltestosterone ( 0.242 ) 17beta−Estradiol ( 0.24 ) 5alpha−Dihydrotestosterone ( 0.235 ) Mifepristone ( 0.218 ) Norethindrone ( 0.214 ) Spironolactone ( 0.204 ) Farglitazar ( 0.203 ) Testosterone propionate ( 0.202 ) meso−Hexestrol ( 0.199 ) Mestranol ( 0.196 ) Estriol ( 0.191 ) 2,2',4,4'−Tetrahydroxybenzophenone ( 0.185 ) 3,3,5,5−Tetraiodothyroacetic acid ( 0.183 ) Norgestrel ( 0.181 ) Cyproterone acetate ( 0.164 ) GSK232420A ( 0.161 ) N−Dodecanoyl−N−methylglycine ( 0.155 ) Pentachloroanisole ( 0.154 ) HPTE ( 0.151 ) Biochanin A ( 0.15 ) Dehydroepiandrosterone ( 0.149 ) PharmaCode_333941 ( 0.148 ) Prednisone ( 0.146 ) Nordihydroguaiaretic acid ( 0.145 ) p,p'−DDD ( 0.144 ) Diphenhydramine hydrochloride ( 0.142 ) Forskolin ( 0.141 ) Perfluorooctanoic acid ( 0.14 ) Oleyl sarcosine ( 0.139 ) Cyclohexylphenylketone ( 0.138 ) Pirinixic acid ( 0.137 ) -
(12) Patent Application Publication (10) Pub. No.: US 2010/0179214 A1 Dubé Et Al
US 20100179214A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2010/0179214 A1 Dubé et al. (43) Pub. Date: Jul. 15, 2010 (54) DOXEPIN TRANS ISOMERS AND SOMERC continuation-in-part of application No. 1 1/804,720, MIXTURES AND METHODS OF USING THE filed on May 18, 2007. SAME TO TREAT SLEEP DSORDERS (60) Provisional application No. 60/898,378, filed on Jan. (75) Inventors: Susan E. Dubé, Carlsbad, CA (US); 30, 2007, provisional application No. 60/801,824, Neil B. Kavey, Chappaqua, NY filed on May 19, 2006, provisional application No. (US) 60/833,319, filed on Jul 25, 2006. Correspondence Address: KNOBBE MARTENS OLSON & BEAR LLP Publication Classification 2040 MAINSTREET, FOURTEENTH FLOOR (51) Int. Cl. IRVINE, CA 92.614 (US) A63L/335 (2006.01) A6IP 25/20 (2006.01) (73) Assignee: SOMAXON PHARMACEUTICALS, INC., (52) U.S. Cl. ........................................................ S14/450 San Diego, CA (US) (21) Appl. No.: 12/535,623 (57) ABSTRACT The invention relates to use of the trans-(E) isomer or iso (22) Filed: Aug. 4, 2009 meric mixtures containing specified ratios of the trans-(E) and cis-(Z) isomers of doxepin, metabolites of doxepin, phar Related U.S. Application Data maceutically-acceptable salts of doxepin and prodrugs of the (63) Continuation-in-part of application No. 12/022,788, same; compositions containing the same, for the treatment of filed on Jan. 30, 2008, now abandoned, which is a sleep disorders US 2010/0179214 A1 Jul. 15, 2010 DOXEPIN TRANS ISOMERS AND SOMERC brings scrutiny from the Drug Enforcement Administration MIXTURES AND METHODS OF USING THE and other regulatory bodies, and requires registration and SAME TO TREAT SLEEP DSORDERS administrative controls in physicians offices. -
(12) United States Patent (10) Patent No.: US 8.598,119 B2 Mates Et Al
US008598119B2 (12) United States Patent (10) Patent No.: US 8.598,119 B2 Mates et al. (45) Date of Patent: Dec. 3, 2013 (54) METHODS AND COMPOSITIONS FOR AOIN 43/00 (2006.01) SLEEP DSORDERS AND OTHER AOIN 43/46 (2006.01) DSORDERS AOIN 43/62 (2006.01) AOIN 43/58 (2006.01) (75) Inventors: Sharon Mates, New York, NY (US); AOIN 43/60 (2006.01) Allen Fienberg, New York, NY (US); (52) U.S. Cl. Lawrence Wennogle, New York, NY USPC .......... 514/114: 514/171; 514/217: 514/220; (US) 514/229.5: 514/250 (58) Field of Classification Search (73) Assignee: Intra-Cellular Therapies, Inc. NY (US) None See application file for complete search history. (*) Notice: Subject to any disclaimer, the term of this patent is extended or adjusted under 35 (56) References Cited U.S.C. 154(b) by 215 days. U.S. PATENT DOCUMENTS (21) Appl. No.: 12/994,560 6,552,017 B1 4/2003 Robichaud et al. 2007/0203120 A1 8, 2007 McDevitt et al. (22) PCT Filed: May 27, 2009 FOREIGN PATENT DOCUMENTS (86). PCT No.: PCT/US2O09/OO3261 S371 (c)(1), WO WOOOf77OO2 * 6, 2000 (2), (4) Date: Nov. 24, 2010 OTHER PUBLICATIONS (87) PCT Pub. No.: WO2009/145900 Rye (Sleep Disorders and Parkinson's Disease, 2000, accessed online http://www.waparkinsons.org/edu research/articles/Sleep PCT Pub. Date: Dec. 3, 2009 Disorders.html), 2 pages.* Alvir et al. Clozapine-Induced Agranulocytosis. The New England (65) Prior Publication Data Journal of Medicine, 1993, vol. 329, No. 3, pp. 162-167.* US 2011/0071080 A1 Mar. -
List of Vital Essential and Necessary Drugs and Medical Sundries For
LIST OF VITAL ESSENTIAL AND NECESSARY DRUGS AND 2015 MEDICAL SUNDRIES FOR PUBLIC HEALTH INSTITUTIONS Sixth Edition STANDARDS & REGULATION DIVISION JAMAICA List of Vital Essential and Necessary List of Drugs and Medical Sundries for Public Institutions List of Vital Essential and Necessary List of Drugs and Medical Sundries for Public Institutions CONTENTS CONTENTS Contd. Page Preface 5-6 Page Information on Hospitals and Health Centres 7 Explanatory Notes 8 Medical Sundries 69-73 Prescription Writing 9-10 Dental Supplies 74 Algorithm for Treatment of Hypertension 11-12 Radiotherapy – Diagnostic Agents 75 Algorithm for Management of Type 2 Diabetes 13-14 Raw Materials 76 List of Drugs Designated for NHF 15-17 List of Drugs Designated for JADEP 18 VOLUME11 – SPECIALIST LIST 77 VOLUME 1 – GENERAL LIST 19 CLASSIFICATION OF DRUGS SECTION 1. Cardiovascular System 78 CLASSIFICATION OF DRUGS SECTION 2. Central Nervous System 79 SECTION 1. Cardiovascular System 20-24 SECTION 3. Dermatology 80 SECTION 2. Central Nervous System 25-30 SECTION 4. Endocrine System 80 SECTION 3. Dermatology 31-33 SECTION 5. Gastro-intestinal System 81 SECTION 4. Ear, Nose and Oropharynx 34-35 SECTION 6. Infections 81 SECTION 5. Endocrine System 36-38 SECTION 7. Malignant Disease and SECTION 6. Gastro-intestinal System 39-40 Immunosuppression 82 SECTION 7. Infections 41-46 SECTION 8. Musculoskeletal and Joint Diseases 83 SECTION 8. Malignant Disease and SECTION 9. Ophthalmology 83 Immunosuppression 47-49 SECTION 10. Genito-Urinary Tract Disorders 84 SECTION 9. Musculoskeletal and Joint Diseases 50-51 SECTION 11. Respiratory System 84 SECTION 10. Nutrition and Blood 52-54 SECTION 12. -
Novel Cyclodextrin Derivatives Presented at the 3Rd European Conference on Cyclodextrins
VOLUME 27. No. 11. NOVEMBER 2013 ISSN 0951-256X October 2-4, 2013, Antalya, Turkey Novel cyclodextrin derivatives presented at the 3rd European Conference on Cyclodextrins This year’s European Conference on Cyclodextrins organized by Prof. Erem Bilensoy, Hacettepe University, Ankara brought 50 oral presentations and 65 posters. Most of the presented works covered the main theme of the congress: ”multifunctional excipient potential of cyclodextrins in pharmaceutical, cosmetic and biomedical industries”. The large number of the presented works dealing with novel cyclodextrin derivatives clearly shows that recently there has been a renewed interest in functionalization of cyclodextrins in order to extend the utilization of these derivatives as tools in catalysis, drug delivery, formulation and stabilization of active molecules and cosmetic ingredients. This short paper gives a brief review of the presented novel cyclodextrin derivatives, summarizes their synthetic methodologies and the field of their applications. Extended abstracts will be published in the Journal of Inclusion Phenomena and Macrocyclic Chemistry after peer review. The references given here are the papers of the cited authors on similar topics presented at the conference. NOVEL CYCLODEXTRIN POLYMERS AND NANOSPONGES Phosphorus-containing cyclodextrin polymers presented by Prof. Catherine Amiel A very attractive new cyclodextrin (CD) based polymeric system presented by Prof. Amiel combines the advantages of cyclodextrin polymers (formation of inclusion complexes with apolar guests) and phosphorus-containing polymers (biocompatibility, calcium affinity). These VOLUME 27. No 11. polymeric systems are promising candidates to be used in biomedical applications that jointly require calcium delivery and transport of lipophilic bioactive molecules. A non-toxic cyclic sodium trimetaphosphate (STMP) was used as a cross-linking agent under basic conditions. -
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Index Note: page numbers in italics refer to figures; those in bold to tables or boxes. abacavir 686 tolerability 536–537 children and adolescents 461 acamprosate vascular dementia 549 haematological 798, 805–807 alcohol dependence 397, 397, 402–403 see also donepezil; galantamine; hepatic impairment 636 eating disorders 669 rivastigmine HIV infection 680 re‐starting after non‐adherence 795 acetylcysteine (N‐acetylcysteine) learning disability 700 ACE inhibitors see angiotensin‐converting autism spectrum disorders 505 medication adherence and 788, 790 enzyme inhibitors obsessive compulsive disorder 364 Naranjo probability scale 811, 812 acetaldehyde 753 refractory schizophrenia 163 older people 525 acetaminophen, in dementia 564, 571 acetyl‐L‐carnitine 159 psychiatric see psychiatric adverse effects acetylcholinesterase (AChE) 529 activated partial thromboplastin time 805 renal impairment 647 acetylcholinesterase (AChE) acute intoxication see intoxication, acute see also teratogenicity inhibitors 529–543, 530–531 acute kidney injury 647 affective disorders adverse effects 537–538, 539 acutely disturbed behaviour 54–64 caffeine consumption 762 Alzheimer’s disease 529–543, 544, 576 intoxication with street drugs 56, 450 non‐psychotropics causing 808, atrial fibrillation 720 rapid tranquillisation 54–59 809, 810 clinical guidelines 544, 551, 551 acute mania see mania, acute stupor 107, 108, 109 combination therapy 536 addictions 385–457 see also bipolar disorder; depression; delirium 675 S‐adenosyl‐l‐methionine 275 mania dosing 535 ADHD -
Datasheet Inhibitors / Agonists / Screening Libraries a DRUG SCREENING EXPERT
Datasheet Inhibitors / Agonists / Screening Libraries A DRUG SCREENING EXPERT Product Name : Volinanserin Catalog Number : T5389 CAS Number : 139290-65-6 Molecular Formula : C22H28FNO3 Molecular Weight : 373.46 Description: Volinanserin (MDL 100907) is a potent and selective antagonist of the serotonin receptor 5-HT2 (Ki: 0.36 nM) and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 adrenergic and sigma receptors. Storage: 2 years -80°C in solvent; 3 years -20°C powder; DMSO 100 mg/mL (267.8 mM) Solubility Ethanol 18 mg/mL (48.2 mM) ( < 1 mg/ml refers to the product slightly soluble or insoluble ) Receptor (IC50) 5-HT2 receptor 0.36 nM (Ki) In vitro Activity MDL 100,907 demonstrated low nanomolar or subnanomolar binding in vitro at the 5-HT2A receptor and showed a > 100-fold separation from all other receptors measured. MDL 100,907 had subnanomolar potency as a 5-HT2A antagonist in vitro in reversing 5-HT-stimulated inositol phosphate accumulation in NIH 3T3 cells transfected with the rat 5-HT2A receptor [2]. In vivo Activity In mice, MDL 100,907 blocked amphetamine-stimulated locomotion at doses that did not significantly affect apomorphine- stimulated climbing behavior. When administered chronically, MDL 100,907 selectively reduced the number of spontaneously active A10 neurons [1]. In vivo, MDL 100,907 potently inhibited 5-methoxy-N, N-dimethyltryptamine-induced head twitches in mice or 5-hydroxytryptophan-induced head twitches in rats. In vivo, functional tests in mice revealed a > 500-fold separation between doses that produced 5-HT2A antagonism and doses that produced alpha 1-adrenergic or striatal D2 antagonism [2]. -
Emerging Anti-Insomnia Drugs: Tackling Sleeplessness and the Quality of Wake Time
REVIEWS Emerging anti-insomnia drugs: tackling sleeplessness and the quality of wake time Keith A. Wafford* and Bjarke Ebert‡ Abstract | Sleep is essential for our physical and mental well being. However, when novel hypnotic drugs are developed, the focus tends to be on the marginal and statistically significant increase in minutes slept during the night instead of the effects on the quality of wakefulness. Recent research on the mechanisms underlying sleep and the control of the sleep–wake cycle has the potential to aid the development of novel hypnotic drugs; however, this potential has not yet been realized. Here, we review the current understanding of how hypnotic drugs act, and discuss how new, more effective drugs and treatment strategies for insomnia might be achieved by taking into consideration the daytime consequences of disrupted sleep. Primary insomnia Humans spend approximately one-third of their lifetime Insomnia is defined as difficulty in initiating and/or Patients who suffer from sleeping, but we still know relatively little about why this maintaining sleep. The incidence of insomnia in the gen- sleeplessness for at least process is so critical for every living animal. Current eral population is between 10–30%, and approximately 1 month that cannot be thinking suggests that waking activity is relatively 50% of the cases complain of serious daytime conse- attributed to a medical, dynamic in terms of using the body’s resources: breaking quences, such as inability to concentrate, reduced energy psychiatric or an environmental cause (such as drug abuse or down proteins, gathering information and expending and memory problems. When this persists for more medications). -
(12) Patent Application Publication (10) Pub. No.: US 2015/0072964 A1 Mates Et Al
US 20150.072964A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2015/0072964 A1 Mates et al. (43) Pub. Date: Mar. 12, 2015 (54) NOVELMETHODS filed on Apr. 14, 2012, provisional application No. 61/624.293, filed on Apr. 14, 2012, provisional appli (71) Applicant: INTRA-CELLULAR THERAPIES, cation No. 61/671,713, filed on Jul. 14, 2012, provi INC., New York, NY (US) sional application No. 61/671,723, filed on Jul. 14, 2012. (72) Inventors: Sharon Mates, New York, NY (US); Robert Davis, New York, NY (US); Publication Classification Kimberly Vanover, New York, NY (US); Lawrence Wennogle, New York, (51) Int. Cl. NY (US) C07D 47L/6 (2006.01) A613 L/4985 (2006.01) (21) Appl. No.: 14/394,469 A6II 45/06 (2006.01) (52) U.S. Cl. (22) PCT Fled: Apr. 14, 2013 CPC .............. C07D 471/16 (2013.01); A61K 45/06 (2013.01); A61 K3I/4985 (2013.01) (86) PCT NO.: PCT/US13A36512 USPC ...... 514/171; 514/250; 514/211.13: 514/217; S371 (c)(1), 514/214.02: 514/220 (2) Date: Oct. 14, 2014 (57) ABSTRACT Use of particular substituted heterocycle fused gamma-car Related U.S. Application Data boline compounds as pharmaceuticals for the treatment of (60) Provisional application No. 61/624.291, filed on Apr. agitation, aggressive behaviors, posttraumatic stress disorder 14, 2012, provisional application No. 61/624,292, or impulse control disorders. US 2015/0072964 A1 Mar. 12, 2015 NOVEL METHODS One type of ICD is Intermittent Explosive Disorder (IED) which involves violence or rage. There is a loss of control CROSS REFERENCE TO RELATED grossly out of proportion to any precipitating psychosocial APPLICATIONS stresses. -
United States Patent (10 ) Patent No.: US 10,660,887 B2 Javitt (45 ) Date of Patent: *May 26 , 2020
US010660887B2 United States Patent (10 ) Patent No.: US 10,660,887 B2 Javitt (45 ) Date of Patent : *May 26 , 2020 (54 ) COMPOSITION AND METHOD FOR (56 ) References Cited TREATMENT OF DEPRESSION AND PSYCHOSIS IN HUMANS U.S. PATENT DOCUMENTS 6,228,875 B1 5/2001 Tsai et al. ( 71 ) Applicant : Glytech , LLC , Ft. Lee , NJ (US ) 2004/0157926 A1 * 8/2004 Heresco - Levy A61K 31/198 514/561 (72 ) Inventor: Daniel C. Javitt , Ft. Lee , NJ (US ) 2005/0261340 Al 11/2005 Weiner 2006/0204486 Al 9/2006 Pyke et al . 2008/0194631 Al 8/2008 Trovero et al. ( 73 ) Assignee : GLYTECH , LLC , Ft. Lee , NJ (US ) 2008/0194698 A1 8/2008 Hermanussen et al . 2010/0069399 A1 * 3/2010 Gant CO7D 401/12 ( * ) Notice : Subject to any disclaimer, the term of this 514 / 253.07 patent is extended or adjusted under 35 2010/0216805 Al 8/2010 Barlow 2011/0207776 Al 8/2011 Buntinx U.S.C. 154 ( b ) by 95 days . 2011/0237602 A1 9/2011 Meltzer This patent is subject to a terminal dis 2011/0306586 Al 12/2011 Khan claimer . 2012/0041026 A1 2/2012 Waizumi ( 21 ) Appl. No.: 15 /650,912 FOREIGN PATENT DOCUMENTS CN 101090721 12/2007 ( 22 ) Filed : Jul. 16 , 17 KR 2007 0017136 2/2007 WO 2005/065308 7/2005 (65 ) Prior Publication Data WO 2005/079756 9/2005 WO 2011044089 4/2011 US 2017/0312275 A1 Nov. 2 , 2017 WO 2012/104852 8/2012 WO 2005/000216 9/2013 WO 2013138322 9/2013 Related U.S. Application Data (63 ) Continuation of application No. -
Molecular and Functional Imaging Studies of Psychedelic Drug Action in Animals and Humans
molecules Review Molecular and Functional Imaging Studies of Psychedelic Drug Action in Animals and Humans Paul Cumming 1,2,* , Milan Scheidegger 3 , Dario Dornbierer 3, Mikael Palner 4,5,6 , Boris B. Quednow 3,7 and Chantal Martin-Soelch 8 1 Department of Nuclear Medicine, Bern University Hospital, CH-3010 Bern, Switzerland 2 School of Psychology and Counselling, Queensland University of Technology, Brisbane 4059, Australia 3 Department of Psychiatry, Psychotherapy and Psychosomatics, Psychiatric Hospital of the University of Zurich, CH-8032 Zurich, Switzerland; [email protected] (M.S.); [email protected] (D.D.); [email protected] (B.B.Q.) 4 Odense Department of Clinical Research, University of Southern Denmark, DK-5000 Odense, Denmark; [email protected] 5 Department of Nuclear Medicine, Odense University Hospital, DK-5000 Odense, Denmark 6 Neurobiology Research Unit, Copenhagen University Hospital, DK-2100 Copenhagen, Denmark 7 Neuroscience Center Zurich, University of Zurich and Swiss Federal Institute of Technology Zurich, CH-8058 Zurich, Switzerland 8 Department of Psychology, University of Fribourg, CH-1700 Fribourg, Switzerland; [email protected] * Correspondence: [email protected] or [email protected] Abstract: Hallucinogens are a loosely defined group of compounds including LSD, N,N- dimethyltryptamines, mescaline, psilocybin/psilocin, and 2,5-dimethoxy-4-methamphetamine (DOM), Citation: Cumming, P.; Scheidegger, which can evoke intense visual and emotional experiences. We are witnessing a renaissance of re- M.; Dornbierer, D.; Palner, M.; search interest in hallucinogens, driven by increasing awareness of their psychotherapeutic potential. Quednow, B.B.; Martin-Soelch, C. As such, we now present a narrative review of the literature on hallucinogen binding in vitro and Molecular and Functional Imaging ex vivo, and the various molecular imaging studies with positron emission tomography (PET) or Studies of Psychedelic Drug Action in single photon emission computer tomography (SPECT). -
Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor
pharmaceuticals Review Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor Qing Wang 1,2 , Yu Zhou 2 , Jianhui Huang 1 and Niu Huang 2,3,* 1 School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China; [email protected] (Q.W.); [email protected] (J.H.) 2 National Institute of Biological Sciences, No. 7 Science Park Road, Zhongguancun Life Science Park, Beijing 102206, China; [email protected] 3 Tsinghua Institute of Multidisciplinary Biomedical Research, Tsinghua University, Beijing 102206, China * Correspondence: [email protected]; Tel.: +86-10-80720645 Abstract: Since the first characterization of the 5-hydroxytryptamine 2B receptor (5-HT2BR) in 1992, significant progress has been made in 5-HT2BR research. Herein, we summarize the biological function, structure, and small-molecule pharmaceutical ligands of the 5-HT2BR. Emerging evidence has suggested that the 5-HT2BR is implicated in the regulation of the cardiovascular system, fibrosis disorders, cancer, the gastrointestinal (GI) tract, and the nervous system. Eight crystal complex structures of the 5-HT2BR bound with different ligands provided great insights into ligand recognition, activation mechanism, and biased signaling. Numerous 5-HT2BR antagonists have been discovered and developed, and several of them have advanced to clinical trials. It is expected that the novel 5-HT2BR antagonists with high potency and selectivity will lead to the development of first-in-class drugs in various therapeutic areas. Keywords: GPCR; 5-HT2BR; biased signaling; agonist; antagonist Citation: Wang, Q.; Zhou, Y.; Huang, J.; Huang, N. Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor. 1. Introduction Pharmaceuticals 2021, 14, 76.