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(12) United States Patent (10) Patent No.: US 6,218,409 B1 Ikeda Et Al

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USOO6218409B1 (12) United States Patent (10) Patent No.: US 6,218,409 B1 Ikeda et al. (45) Date of Patent: Apr. 17, 2001 (54) PHARMACEUTICAL COMPOSITION Akanuma et al., J. Clinical Therapeutics & Medicines, 9 Suppl. 3, p. 19-37, 36-60 (1993) (English translation). (75) Inventors: Hitoshi Ikeda, Higashiosaka; Takashi M. Tominaga et al. “Thiazolidinediones (AD-4833 and Sohda, Takatsuki; Hiroyuki Odaka, CS-045) Improve Hepatic Insulin Resistance in Streptozo Kobe, all of (JP) ticin-Induced Diabetic Rats', Endocrine Journal, vol. 40, No. 3, pp. 345–349, 1993. (73) Assignee: Takeda Chemical Industries, Ltd., C. Hofmann et al., “Glucose Transport Deficiency in Dia Osaka (JP) betic Animals is Corrected by Treatment with the Oral Antihyperglycemic Agent PioglitaZone', Endocrinology, (*) Notice: Subject to any disclaimer, the term of this vol. 129, No. 4, pp. 1915–1925, 1991. patent is extended or adjusted under 35 J. Karam, “Type II Diabetes and Syndrome X,Endocrinol U.S.C. 154(b) by 0 days. ogy and Metabolism Clinics of North America, vol. 21, No. 2, pp. 329-350, 1992. (21) Appl. No.: 09/610,994 S. Suter et al., “Metabolic Effects of New Oral Hypoglyce (22) Filed: Jul. 6, 2000 mic Agent CS-045 in NIDDM Subjects”, Diabetes Care, vol. 15, No. 2, pp. 193-203, 1992. Related U.S. Application Data T. Toyoda, Iyaku Journal, vol. 30, No. 4, pp. 1130-1134, 1994. (62) Division of application No. 09/303,497, filed on Apr. 30, Y. Sugiyama et al., “Effects of Pioglitazone on Glucose and 1999, now Pat. No. 6,156,773, which is a division of application No. 09/057.465, filed on Apr. 9, 1998, now Pat. Lipid Metabolism in Wistar Fatty Rats', Arzneim-Forsch/ No. 5,965,584, which is a division of application No. Drug Res., vol. 40, No. 1, pp. 263-267, 1990. 08/667,979, filed on Jun. 19, 1996, now Pat. No. 5,952,356. Ishida et al., “Oral Hypoglycemic Agents-New Oral Drugs (30) Foreign Application Priority Data and New Strategy of Treatment, Clinic All-round, vol. 43, pp. 2615-2621, 1994 (and English translation). Jun. 20, 1995 (JP) ................................................... 7-1535OO Medicine and Drug Journal, vol. 30, No. 4 (Japanese) with partial English translation, 1990. (51) Int. Cl." ........................ C07D 401/02; A61K 31/42; Therapeutic Research, 14 (No. 10), 4122 to 4126 (1993) A61K 31/49; A61K 31/425 (and English translation). Clinic and Medicine, 9 (Suppl. 3), 19 to 37 (1993). (52) U.S. Cl. .......................... 514/342; 514/369; 514/376; Clinic and Medicine, 9 (Suppl. 3), 39 to 60 (1993). 514/340; 546/269.7; 546/271.4; 548/183; Recent Medicine, 33 197 (1982). 548/227 J. Sturis et al., “Prevention of Diabetes Does Not Com pletely Prevent Insulin Secretory Defects in the ZDF rat', (58) Field of Search .............................. 546/260.7, 271.4; vol. 169, No. 4, pp. 786–792, Oct., 1995. 514/340, 342, 369,376; 548/183, 227 Z. Bloomgarden, "American Diabetes ASSociation Scientific Sessions, 1995, The Journal of Clinical and Applied (56) References Cited Research and Education”, vol. 18, No. 8, pp. 1215-1219, U.S. PATENT DOCUMENTS Aug., 1995. R. Whitcomb et al., “Thiazolidinediones”, Expert Opinion 4,895,862 1/1990 Alessi et al. ......................... 514/360 on Investigational Drugs, vol. 4, No. 12, pp. 1299–1309, 5,068.342 11/1991 Zasket al. ........................... 548/183 Dec., 1995. FOREIGN PATENT DOCUMENTS K, Nihalani et al., “Newer Oral Hypoglyceamic (Antidia 0 008 203 2/1980 (EP). betic) Agents”, Journal of the Diabetic Association of India, O 193 256 9/1986 (EP). vol. 34, Nos. 3 & 4, 1994. 0 710 659 5/1996 (EP). Sugiyama et al., “Effects of PioglitaZone on Hepatic and 4-66579 3/1992 (JP). Peripheral Insulin Resistance in Wistar Fatty Rats, Arzne 4-69383 3/1992 (JP). im.-Forsch., vol. 40, pp. 436-440 (Apr. 1990). 5-202042 8/1993 (JP). 93/03724 3/1993 (WO). (List continued on next page.) OTHER PUBLICATIONS Primary Examiner-Zinna Northington Davis N. Hotta, Diabetes Uptake, No. 10, Kashikojima Seminar, (74) Attorney, Agent, or Firm Wenderoth, Lind & Ponack, pp. 68-77 (1994), with English translation. LLP. H. Lebovitz, Diabetes Care, vol. 17, No. 12, pp. 1542–1544 (57) ABSTRACT (1994). N. Hotta, Chronic Diabetes, vol. 6, No. 1, pp. 98-102 Pharmaceutical composition which comprises an insulin (1995). Sensitivity enhancer in combination with other antidiabetics G. Williams, The Lancet, vol. 343, pp. 95-100 (1994). differing from the enhancer in the mechanism of action, J. Lehman et al., The Journal of Biological Chemistry, vol. which shows a potent depressive effect on diabetic hyperg 270, No. 22, p. 12953–12956 (1995). lycemia and is useful for prophylaxis and treatment of R. Jackson et al., Diabetes, vol. 36, pp. 632-639 (1987). diabetes. R. Donnelly et al., Br. J. Clin. Pharmac., vol. 37, pp. 311-320 (1994). 16 Claims, No Drawings US 6,218,409 B1 Page 2 OTHER PUBLICATIONS Suter et al., “Metabolic Effects of New Oral Hypoglycemic Agent CS-045 in NIDDM Subjects,” Diabetes Care, vol. 15, Ikeda et al., “Effects of Pioglitazone on Glucose and Lipid pp. 193–203 (Feb. 1992). Metabolism in Normal and Insulin Resistant Animals,” Iwamoto et al., “Effect of New Oral Antidiabetic Agent Arzneim-Forsch., vol. 40, pp. 156-162 (Feb. 1990). CS-045 on Glucose Tolerance and Insulin Secretion in Hofmann et al., “New Oral Thiazolidinedione Antidiabetic Agents Act as Insulin Sensitizers, Diabetes Care, Vol. 15, Patients with NIDDM,” Diabetes Care, vol. 14, pp. pp. 1075–1078 (Aug. 1992). 1083–1086 (Nov. 1991). Hofmann et al., “Treatment of Insulin-Resistant Mice with Norris et al. Comparison of Troglitazone (C1991) Dosing the Oral Antidiabetic Agent Pioglitazone: Evaluation of Regimens and Placebo in the Treatment of Patients with Liver GLUT2 and Phosphoenolpyruvate Carboxykinase NIDDM, Diabetes, vol. 42, Supp. 1, Abstract 188 (Jun. Expression,” Endocrinology, vol. 130, pp. 735-740 (Feb. 1993). 1992). Fukuda et al., “Results of a Pilot Study in which Troglita Iwanishi et al., “Effect of Pioglitazone on Insulin Receptors Zone and Insulin were Jointly Administered to NIDDM of Skeletal Muscles from High Fat-Fed Rats,” Metabolism, Patients,” Journal of Clinical Therapeutics & Medicines, vol. 42, pp. 1017-1021 (Aug. 1993). vol. 11, pp. 2055-2062 (Oct. 1995) (with translation, based Iwanishi et al., “New Oral Agent to Increase Insulin Sensi on abstract published at 15th Diabetes Fed. Cong., Nov. tivity by Activating Kinase Activity of Insulin Receptors.” 6–11, 1994, Kobe). Diabetes, vol.39, abstract 474 (Jun. 1990). Kanazawa, “Agent for Lowering Insulin Resistance Kobayashi et al., “Pioglitazone Increases Insulin Sensitivity CS-045,” Diabetes Frontier, vol. 3, pp. 570–574 (1992). by Activating Insulin Receptor Kinase,” Diabetes, vol. 41, Onuma et al., “The Effect of a New Oral Hypoglycemic pp. 476–483 (Apr. 1992). Drug, CS-045, on Glucose Tolerance and Serum Lipids in Hofmann et al., “Insulin Sensitization in Diabetic Rat Liver Nonobese Japanese Patients with Non-Insulin-Dependent by an Antihyperglycemic Agent,” Metabolism, Vol. 44, pp. Diabetes Mellitus: A Pilot Study,” Current Therapeutic 384-389 (Mar. 1995). Research, vol. 55, pp. 416–421 (Apr. 1994). de Souza et al., “Insulin Secretory Defect in Zucker fa/fa Kuzuya et al., “A Pilot Clinical Trial of a New Oral Rats is Improved by Ameliorating Insulin Resistance,” Dia Hypoglycemic Agent, CS-045, in Patients with Non-Insulin betes, vol. 44, pp. 984–991 (Aug. 1995). Dependent Diabetes Mellitus.” Diabetes Research and Clini Hofmann et al., “Glucose Transport Deficiency in Diabetic cal Practice, vol. 11, pp. 147-154 (1991). Animals is Corrected by Treatment with the Oral Antihy Takino et al., “Increased Insulin Responsiveness After perglycemic Agent PioglitaZone, Endocrinology, Vol. 129, CS-045 Treatment in Diabetes Associated with Werner's pp. 1915–1925 (Mar. 1991), Syndrome,” Diabetes Research and Clinical Practice, vol. Colca et al., “Antihyperglycaemic Thiazolidinediones: 24, pp. 167–172 (Jul. 1994). CiglitaZone and its Analogues, New Antidiabetic Drugs, Fujiwara et al., “Characterization of a New Oral Antidiabetic pp. 255-261 (1990). Agent CS-045,” Diabetes, vol. 37, pp. 1549-1558 (Sep. Tominaga et al., “Thiazolidinediones (AD-4833 and 1988). CS-045) Improve Hepatic Insulin Resistance in Streptozo Lee et al., “Metabolic Effects of Troglitazone on Fruc tocin-Induced Diabetic Rats,” Endocrine Journal, Vol. 40, tose-Induced Insulin Resistance in the Rat, Diabetes, vol. pp. 343–349 (Jun. 1993). 43, pp. 1435–1439 (Dec. 1994). Weinstock et al., “Pioglitazone: In Vitro Effects on Rat Khoursheed et al., “Metabolic Effects of Troglitazone on Hepatoma Cells and in vivo Liver Hypertrophy in KKAY Fat-Induced Insulin Resistance in the Rat,” Metabolism, Mice,” Pharmacology, vol. 54, pp. 169-178 (Apr. 1997). vol. 44, pp. 1489–1494 (Nov. 1995). El-Kebbiet al., “Regulation of Glucose Transport by Piogli Valiquett et al., “Troglitazone Dose-Response Study in tazone in BC3H-1 Myocytes,” Clinical Resarch, vol.39, p. Patients with Noninsulin Dependent Diabetes,” Clinical 837A (Dec. 1991). Resarch, vol. 42, p. 400A (Oct. 1994). Kemnitz et al., “PioglitaZone Increases Insulin Sensitivity, Nolan et al., “Improvement in Glucose Tolerance and Insulin Reduces Blood Glucose, Insulin, and Lipid Levels, and Resistance in Obese Subjects Treated with Troglitazone.” Lowers Blood Pressue in Obese, Insulin-Resistant Rhesus The New England Journal of Medicine, vol. 331, pp. Monkeys,” Diabetes, vol. 43, pp. 204–211 (Feb. 1994). 1188–1193 (Nov. 1994). Meehan et al., “Pioglitazone Reduces Blood Pressure and Ciaraldi et al., “In Vitro Studies on the Action of CS-045, a Improves Insulin Sensitivity in Fructose-Fed Rats,” Clinical New Antidiabetic Agent,” Metabolism, vol. 39, pp. Research, vol. 41, p. 21A (Feb. 1993). 1056–1062 (Oct. 1990). Colca et al., “Pioglitazone Hydrochloride Inhibits Choles Oakes et al., A New Antidiabetic Agent, BRL 49653, terol Absorption and Lowers Plasma Cholesterol Concen Reduces Lipid Availability and Improves Insulin Action and trations in Cholesterol-Fed Rats,” Diabetes, vol.
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    USOO8846695B2 (12) United States Patent (10) Patent No.: US 8,846,695 B2 Dugi (45) Date of Patent: Sep. 30, 2014 (54) TREATMENT FOR DIABETES IN PATIENTS 5,084,460 A 1/1992 Munson, Jr. et al. 5,130,244 A 7, 1992 Nishimaki et al. WITH INADEQUATE GLYCEMIC CONTROL 5,219,870 A 6, 1993 Kim DESPTE METFORMIN THERAPY 5,223,499 A 6/1993 Greenlee et al. COMPRISINGADPP-IV INHIBITOR 5,234,897 A 8, 1993 Findeisen et al. 5,258,380 A 11/1993 Janssens et al. 5,266,555 A 11/1993 Findeisen et al. (75) Inventor: Klaus Dugi. Dresden (DE) 5,273,995 A 12, 1993 Roth 5,284.967 A 2f1994 Macher (73) Assignee: Boehringer Ingelheim International 5,300,298 A 4, 1994 LaNoue GmbH, Ingelheim am Rhein (DE) 5,329,025 A 7/1994 Wong et al. 5,332,744 A 7/1994 Chakravarty et al. (*) Notice: Subject to any disclaimer, the term of this 5,389,642 A 2f1995 Dorsch et al. 5,399,578 A 3/1995 Buhlmayer et al. patent is extended or adjusted under 35 5,407,929 A 4/1995 Takahashi et al. U.S.C. 154(b) by 148 days. 5,470,579 A 11/1995 Bonte et al. 5,591,762 A 1/1997 Hauel et al. (21) Appl. No.: 13/143,370 5,594,003 A 1/1997 Hauel et al. 5,602,127 A 2f1997 Hauel et al. 5,614,519 A 3, 1997 Hauel et al. (22) PCT Filed: Jan. 7, 2010 5,719,279 A 2f1998 Kufner-Muhl et al.
  • (12) Patent Application Publication (10) Pub. No.: US 2004/0058896 A1 Dietrich Et Al

    (12) Patent Application Publication (10) Pub. No.: US 2004/0058896 A1 Dietrich Et Al

    US 200400.58896A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2004/0058896 A1 Dietrich et al. (43) Pub. Date: Mar. 25, 2004 (54) PHARMACEUTICAL PREPARATION (30) Foreign Application Priority Data COMPRISING AN ACTIVE DISPERSED ON A MATRIX Dec. 7, 2000 (EP)........................................ OO126847.3 (76) Inventors: Rango Dietrich, Konstanz (DE); Publication Classification Rudolf Linder, Kontanz (DE); Hartmut Ney, Konstanz (DE) (51) Int. Cl." ...................... A61K 31156; A61K 31/4439 (52) U.S. Cl. ........................... 514/171; 514/179; 514/338 Correspondence Address: (57) ABSTRACT NATH & ASSOCATES PLLC 1030 FIFTEENTH STREET, N.W. The present invention relates to the field of pharmaceutical SIXTH FLOOR technology and describes a novel advantageous preparation WASHINGTON, DC 20005 (US) for an active ingredient. The novel preparation is Suitable for 9 producing a large number of pharmaceutical dosage forms. (21) Appl. No.: 10/433,398 In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix com (22) PCT Filed: Dec. 6, 2001 posed of one or more excipients Selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid (86) PCT No.: PCT/EPO1/14307 eSter. US 2004/0058896 A1 Mar. 25, 2004 PHARMACEUTICAL PREPARATION 0008 Further subject matters are evident from the claims. COMPRISING AN ACTIVE DISPERSED ON A MATRIX 0009. The preparations for the purpose of the invention preferably comprise numerous individual units in which at least one active ingredient particle, preferably a large num TECHNICAL FIELD ber of active ingredient particles, is present in an excipient 0001. The present invention relates to the field of phar matrix composed of the excipients of the invention (also maceutical technology and describes a novel advantageous referred to as active ingredient units hereinafter).