JP5284272B2 - ２−［６−（３−アミノ−ピペリジン−１−イル）−３−メチル−２，４−ジオキソ−３，４−ジヒドロ−２ｈ−ピリミジン−１−イルメチル］−４−フルオロ−ベンゾニトリルのコハク酸塩の多形及びこれらの使用方法 - Google Patents

２−［６−（３−アミノ−ピペリジン−１−イル）−３−メチル−２，４−ジオキソ−３，４−ジヒドロ−２ｈ−ピリミジン−１−イルメチル］−４−フルオロ−ベンゾニトリルのコハク酸塩の多形及びこれらの使用方法 Download PDF

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JP5284272B2
JP5284272B2 JP2009539485A JP2009539485A JP5284272B2 JP 5284272 B2 JP5284272 B2 JP 5284272B2 JP 2009539485 A JP2009539485 A JP 2009539485A JP 2009539485 A JP2009539485 A JP 2009539485A JP 5284272 B2 JP5284272 B2 JP 5284272B2
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JP2010511063A5 (enExample
JP2010511063A (ja
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シー． ケリー、ロン
エイチ． コズテッキ、リアン
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Molecular Biology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2009539485A 2006-11-29 2007-11-29 ２−［６−（３−アミノ−ピペリジン−１−イル）−３−メチル−２，４−ジオキソ−３，４−ジヒドロ−２ｈ−ピリミジン−１−イルメチル］−４−フルオロ−ベンゾニトリルのコハク酸塩の多形及びこれらの使用方法 Active JP5284272B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US86776406P 2006-11-29 2006-11-29
US60/867,764 2006-11-29
PCT/US2007/085933 WO2008067465A1 (en) 2006-11-29 2007-11-29 Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2h-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor

Publications (3)

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JP2010511063A JP2010511063A (ja) 2010-04-08
JP2010511063A5 JP2010511063A5 (enExample) 2011-01-20
JP5284272B2 true JP5284272B2 (ja) 2013-09-11

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US (3) US20080227798A1 (enExample)
EP (1) EP2102185B1 (enExample)
JP (1) JP5284272B2 (enExample)
KR (1) KR20090086619A (enExample)
CN (1) CN101573351B (enExample)
AR (1) AR064035A1 (enExample)
AU (1) AU2007325107A1 (enExample)
BR (1) BRPI0719365A2 (enExample)
CA (1) CA2670776A1 (enExample)
CL (1) CL2007003427A1 (enExample)
CR (1) CR10874A (enExample)
EA (1) EA200970519A1 (enExample)
EC (1) ECSP099465A (enExample)
IL (1) IL198866A0 (enExample)
MA (1) MA31140B1 (enExample)
MX (1) MX2009005588A (enExample)
NO (1) NO20092249L (enExample)
PE (1) PE20081394A1 (enExample)
TN (1) TN2009000215A1 (enExample)
TW (1) TW200838536A (enExample)
WO (1) WO2008067465A1 (enExample)
ZA (1) ZA200903870B (enExample)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200838536A (en) * 2006-11-29 2008-10-01 Takeda Pharmaceutical Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
WO2008114800A2 (en) * 2007-03-13 2008-09-25 Takeda Pharmaceutical Company Limited Solid preparation comprising 2- [ [6- [ (3r) -3-amino-1-piperidinyl] -3, 4-dihydro-3-methyl-2, 4-dioxo-1 (2h) -pyrimidinyl] methyl] -4-fluorobenzonitrile
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
MX370599B (es) 2008-08-15 2019-12-18 Boehringer Ingelheim Int Derivados de purina para su uso en el tratamiento de enfermedades relacionadas con fab.
AR074990A1 (es) 2009-01-07 2011-03-02 Boehringer Ingelheim Int Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina
TWI466672B (zh) 2009-01-29 2015-01-01 Boehringer Ingelheim Int 小兒科病人糖尿病之治療
NZ619520A (en) 2009-02-13 2015-06-26 Boehringer Ingelheim Int Antidiabetic medications comprising a dpp-4 inhibitor (linagliptin) optionally in combination with other antidiabetics
CN102361557A (zh) 2009-03-26 2012-02-22 Mapi医药公司 制备阿格列汀的方法
NZ599298A (en) 2009-11-27 2014-11-28 Boehringer Ingelheim Int Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin
CA2784799C (en) 2009-12-30 2014-06-10 Shanghai Fochon Pharmaceutical Co Ltd Certain dipeptidyl peptidase inhibtors
EP2547339A1 (en) 2010-03-18 2013-01-23 Boehringer Ingelheim International GmbH Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions
MX2012011631A (es) 2010-04-06 2013-01-18 Arena Pharm Inc Moduladores del receptor gpr119 y el tratamiento de trastornos relacionados con el mismo.
WO2011138421A1 (en) 2010-05-05 2011-11-10 Boehringer Ingelheim International Gmbh Combination therapy
BR112012028906A2 (pt) * 2010-05-12 2016-07-26 Mapi Pharma Ltd polimorfos de benzoato de alogliptina
NZ603319A (en) 2010-06-24 2015-04-24 Boehringer Ingelheim Int Diabetes therapy
MX2013003184A (es) 2010-09-22 2013-06-07 Arena Pharm Inc Moduladores del receptor gpr119 y el tratamiento de transtornos relacionados con el mismo.
EP2680851B1 (en) 2011-03-03 2016-08-17 Merck Sharp & Dohme Corp. Fused bicyclic heterocycles useful as dipeptidyl peptidase-iv inhibitors
WO2012135570A1 (en) 2011-04-01 2012-10-04 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145361A1 (en) 2011-04-19 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20140038889A1 (en) 2011-04-22 2014-02-06 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
US20140051714A1 (en) 2011-04-22 2014-02-20 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2012170702A1 (en) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
JP6122879B2 (ja) 2012-06-05 2017-04-26 武田薬品工業株式会社 固形製剤
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
CN104003975A (zh) * 2013-02-22 2014-08-27 四川海思科制药有限公司 曲格列汀新的固态形式及其制备方法和用途
EP3083580A4 (en) * 2013-12-18 2017-06-28 Harman Finochem Limited A process for preparation of trelagliptin succinate
CN104803971B (zh) * 2014-01-24 2021-11-30 深圳信立泰药业股份有限公司 化合物A单苯甲酸盐的晶型α及其制备方法和含有该晶型的药物组合物
CN105228988B (zh) * 2014-04-01 2017-06-27 杭州普晒医药科技有限公司 曲格列汀半琥珀酸盐的晶体及其制备方法和药物组合物
CN105315256B (zh) * 2014-07-07 2018-02-06 广州朗圣药业有限公司 一种适合工业化的高纯度琥珀酸曲格列汀的制备方法
WO2016024224A1 (en) * 2014-08-11 2016-02-18 Sun Pharmaceutical Industries Limited A process for the preparation of 4-fluoro-2-methylbenzonitrile
CN105384724A (zh) * 2014-09-01 2016-03-09 广东东阳光药业有限公司 一种氟代物的晶型及其制备方法
CN105524042B (zh) * 2014-10-22 2019-09-13 重庆医药工业研究院有限责任公司 一种制备曲格列汀的方法
CN105646446B (zh) * 2014-11-14 2018-09-28 瀚晖制药有限公司 一种纯化阿格列汀的方法
CN104829590B (zh) * 2015-04-08 2020-04-24 重庆医药工业研究院有限责任公司 一种纯化曲格列汀的方法
CN105622575A (zh) * 2015-06-16 2016-06-01 上海元智生物医药科技有限公司 曲格列汀的制备方法
CN105399725B (zh) * 2015-11-06 2018-09-07 杭州华东医药集团新药研究院有限公司 曲格列汀化合物其盐、晶体、药物组合物和用途
CN105669645B (zh) * 2016-02-18 2019-12-31 南京正大天晴制药有限公司 曲格列汀及其琥珀酸盐的制备方法
CN107434800A (zh) * 2016-05-27 2017-12-05 威海迪素制药有限公司 一种琥珀酸曲格列汀晶型a的制备方法
CN105949175A (zh) * 2016-05-31 2016-09-21 威海迪素制药有限公司 一种琥珀酸曲格列汀杂质c对照品的制备方法
CN106117179B (zh) * 2016-06-23 2019-03-15 江苏万川医疗健康产业集团有限公司 一种琥珀酸曲格列汀的精制方法
CN106074422A (zh) * 2016-07-27 2016-11-09 上海海虹实业(集团)巢湖今辰药业有限公司 一种琥珀酸曲格列汀口服固体制剂及其制备方法
CN106279104B (zh) * 2016-08-16 2019-04-26 杭州新博思生物医药有限公司 一种制备琥珀酸曲格列汀的工艺改进方法
CN108072709B (zh) * 2016-11-18 2020-11-24 广东东阳光药业有限公司 测定琥珀酸曲格列汀原料药中对映异构体含量的方法
CN106749176A (zh) * 2016-12-08 2017-05-31 郑州明泽医药科技有限公司 一种曲格列汀琥珀酸盐的纯化方法
CN109970706A (zh) * 2017-12-27 2019-07-05 徐州万邦金桥制药有限公司 一种琥珀酸曲格列汀a晶型的制备和精制方法
CN107963991A (zh) * 2017-12-29 2018-04-27 成都百裕制药股份有限公司 一种无定形托伐普坦的生产方法
CN109503551A (zh) * 2018-11-21 2019-03-22 安阳师范学院 一种曲格列汀的制备方法
CN110156750A (zh) * 2019-05-13 2019-08-23 无锡贝塔医药科技有限公司 嘧啶环14c标记的琥珀酸曲格列汀的制备方法
CN114105889B (zh) * 2021-12-16 2023-06-13 山东创新药物研发有限公司 一种dpp-iv抑制剂关键中间体的制备方法及其应用
CN115785066B (zh) * 2022-12-08 2024-05-31 广东工业大学 曲格列汀晶型f及其制备方法

Family Cites Families (421)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB699812A (en) 1950-11-29 1953-11-18 British Ind Solvents Ltd Manufacture of substituted pyrimidones
DE1249281B (enExample) * 1963-05-18
DE1670912C3 (de) 1967-08-18 1981-06-11 Bayer Ag, 5090 Leverkusen Herbizide Mittel auf Basis von 1,2,4-Triazin-5-onen
GB1377642A (en) 1971-01-14 1974-12-18 Koninklijke Gist Spiritus Penicillanic and cephalosporanic acid derivatives
US3960949A (en) 1971-04-02 1976-06-01 Schering Aktiengesellschaft 1,2-Biguanides
DE2150686A1 (de) 1971-10-12 1973-04-19 Basf Ag 6-amino-uracil-5-carbonsaeurethioamide
BE792206A (enExample) 1971-12-02 1973-06-01 Byk Gulden Lomberg Chem Fab
GB1429184A (en) 1972-04-20 1976-03-24 Allen & Hanburys Ltd Physically anti-inflammatory steroids for use in aerosols
US4044126A (en) 1972-04-20 1977-08-23 Allen & Hanburys Limited Steroidal aerosol compositions and process for the preparation thereof
AU5996573A (en) 1972-09-11 1975-03-06 Commonwealth Scientific And Industrial Research Organisation Pyridinium salts
US3823135A (en) 1972-12-26 1974-07-09 Shell Oil Co Pyrimidone herbicides
GB1464248A (en) 1973-11-01 1977-02-09 Ici Ltd Substituted triazinediones their preparation and use as herbicides
DE2361551A1 (de) 1973-12-11 1975-06-19 Basf Ag Wasserloesliche azofarbstoffe
DE2500024A1 (de) 1975-01-02 1976-07-08 Basf Ag Wasserloesliche azofarbstoffe
DE2720085A1 (de) 1977-05-05 1978-11-16 Hoechst Ag Pyrimido(6,1-a)isochinolin-2-on- derivate
US4494978A (en) * 1976-12-30 1985-01-22 Chevron Research Company Herbicidal N-(N'-hydrocarbyloxycarbamylalkyl)-2,6-dialkyl-alpha-haloacetanilides
CH657851A5 (de) 1983-06-28 1986-09-30 Ciba Geigy Ag Chromogene chinazolonverbindungen.
AR240698A1 (es) 1985-01-19 1990-09-28 Takeda Chemical Industries Ltd Procedimiento para preparar compuestos de 5-(4-(2-(5-etil-2-piridil)-etoxi)benzil)-2,4-tiazolidindiona y sus sales
US5614492A (en) 1986-05-05 1997-03-25 The General Hospital Corporation Insulinotropic hormone GLP-1 (7-36) and uses thereof
ATE186724T1 (de) * 1987-09-04 1999-12-15 Beecham Group Plc Substituierte thiazolidindionderivate
US4935493A (en) 1987-10-06 1990-06-19 E. I. Du Pont De Nemours And Company Protease inhibitors
EP0422011A1 (de) 1988-05-05 1991-04-17 BASF Aktiengesellschaft Mittel auf der basis von uracil-derivaten zur wachstumsförderung und fettreduktion bei tieren
JPH0251150A (ja) 1988-08-12 1990-02-21 Konica Corp 新規なシアンカプラーを含有するハロゲン化銀写真感光材料
IL92915A0 (en) 1989-01-05 1990-09-17 Ciba Geigy Ag Certain pyrrolylphenyl-substituted hydroxamic acid derivatives
GB8900382D0 (en) 1989-01-09 1989-03-08 Janssen Pharmaceutica Nv 2-aminopyrimidinone derivatives
US5433955A (en) 1989-01-23 1995-07-18 Akzo N.V. Site specific in vivo activation of therapeutic drugs
IE63502B1 (en) 1989-04-21 1995-05-03 Zeneca Ltd Aminopyrimidine derivatives useful for treating cardiovascular disorders
ATE164852T1 (de) 1990-01-24 1998-04-15 Douglas I Buckley Glp-1-analoga verwendbar in der diabetesbehandlung
JPH05504969A (ja) 1990-02-13 1993-07-29 メルク・エンド・カムパニー・インコーポレーテツド 置換ベンジル要素を含有するアンギオテンシン２アンタゴニスト類
US5366862A (en) 1990-02-14 1994-11-22 Receptor Laboratories, Inc. Method for generating and screening useful peptides
US5814460A (en) 1990-02-14 1998-09-29 Diatide, Inc. Method for generating and screening useful peptides
US5162326A (en) 1990-02-15 1992-11-10 Takeda Chemical Industries, Ltd. Pyrimidinedione derivatives, their production and use
US5462928A (en) 1990-04-14 1995-10-31 New England Medical Center Hospitals, Inc. Inhibitors of dipeptidyl-aminopeptidase type IV
DE4110019C2 (de) 1991-03-27 2000-04-13 Merck Patent Gmbh Imidazopyridine, Verfahren zu ihrer Herstellung und diese enthaltende pharmazeutische Zubereitungen
US5387512A (en) * 1991-06-07 1995-02-07 Merck & Co. Inc. Preparation of 3-[z-benzoxazol-2-yl)ethyl]-5-(1-hydroxyethyl)-6-methyl-2-(1H)-pyridinone by biotransformation
US6825169B1 (en) 1991-10-22 2004-11-30 Trustees Of Tufts College Inhibitors of dipeptidyl-aminopeptidase type IV
DK0610317T3 (da) 1991-10-22 2001-02-19 New England Medical Center Inc Inhibitorer af dipeptidyl-aminopeptidase type IV
EP0570594B1 (en) 1991-12-10 1997-07-30 Shionogi & Co., Ltd. Hydroxamic acid derivative based on aromatic sulfonamide
US5350752A (en) 1991-12-16 1994-09-27 E. R. Squibb & Sons, Inc. Dihydropyrimidine derivatives
DE4141788A1 (de) 1991-12-18 1993-06-24 Merck Patent Gmbh Imidazopyridine
US5602102A (en) 1992-05-29 1997-02-11 Board Of Regents, The Univ. Of Tx System Dipeptidyl peptidase-I inhibitors and uses thereof
DE4305602A1 (de) 1992-06-17 1993-12-23 Merck Patent Gmbh Imidazopyridine
AU4794393A (en) 1992-07-31 1994-03-03 Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services, The Producing increased numbers of hematopoietic cells by administering inhibitors of dipeptidyl peptidase iv
CZ181493A3 (en) 1992-09-10 1994-03-16 Lilly Co Eli The use of rhodanine derivative for the preparation of a pharmaceutical composition reducing level of sugar in blood and for treating alzheimer's disease
IL106998A0 (en) 1992-09-17 1993-12-28 Univ Florida Brain-enhanced delivery of neuroactive peptides by sequential metabolism
US5811281A (en) 1993-07-12 1998-09-22 Cornell Research Foundation, Inc. Immortalized intestinal epithelial cell lines
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
DE4341453A1 (de) 1993-12-06 1995-06-08 Merck Patent Gmbh Imidazopyridine
CA2184891C (en) 1994-03-08 2000-09-26 Otsuka Pharmaceutical Factory, Inc. Phosphonic diester derivative
US5580979A (en) 1994-03-15 1996-12-03 Trustees Of Tufts University Phosphotyrosine peptidomimetics for inhibiting SH2 domain interactions
US5543396A (en) 1994-04-28 1996-08-06 Georgia Tech Research Corp. Proline phosphonate derivatives
AU2790895A (en) 1994-06-10 1996-01-05 Universitaire Instelling Antwerpen Purification of serine protease and synthetic inhibitors thereof
CN1074900C (zh) 1994-06-17 2001-11-21 拉·特罗比大学 昆虫的生物控制
US5601986A (en) 1994-07-14 1997-02-11 Amgen Inc. Assays and devices for the detection of extrahepatic biliary atresia
DE4432860A1 (de) 1994-09-15 1996-03-21 Merck Patent Gmbh Imidazopyridine
US5512549A (en) 1994-10-18 1996-04-30 Eli Lilly And Company Glucagon-like insulinotropic peptide analogs, compositions, and methods of use
DE69624437T2 (de) 1995-04-13 2003-08-07 Taiho Pharmaceutical Co. Ltd., Tokio/Tokyo 4,6-diarylpyrimidin-derivate und deren salze
US5614379A (en) 1995-04-26 1997-03-25 Eli Lilly And Company Process for preparing anti-obesity protein
JP2002515724A (ja) 1995-06-01 2002-05-28 ダナ−ファーバー キャンサー インスティテュート インコーポレイテッド ヒト血清中に見出されたジペプチジルペプチダーゼｉｖ（ｃｄ２６）の新規形態、その抗体および利用法
US6325989B1 (en) 1995-06-01 2001-12-04 Dana-Farber Cancer Institute, Inc. Form of dipeptidylpeptidase IV (CD26) found in human serum
ATE201016T1 (de) 1995-06-09 2001-05-15 Hoffmann La Roche Pyrimidindion-, pyrimidintrion-, triazindion- derivate als alpha-1-adrenergische rezeptorantagonisten
JPH0928376A (ja) 1995-07-21 1997-02-04 Ajinomoto Co Inc 新規ジペプチジルペプチダーゼｉｖとその製造方法
DE69709069T2 (de) 1996-02-13 2002-07-04 G.D. Searle & Co., Chicago Zusammensetzungen mit immunosuppressiven wirkungen, welche 5-lipoxygenase-inhibitoren und cyclooxygenase-2-inhibitoren enthalten
DE122010000020I1 (de) 1996-04-25 2010-07-08 Prosidion Ltd Verfahren zur Senkung des Blutglukosespiegels in Säugern
US20020006899A1 (en) 1998-10-06 2002-01-17 Pospisilik Andrew J. Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals
US5965532A (en) 1996-06-28 1999-10-12 Trustees Of Tufts College Multivalent compounds for crosslinking receptors and uses thereof
BR9711098B1 (pt) 1996-07-01 2011-10-04 compostos heterocìclicos, processo para sua preparação e composições farmacêuticas contendo os mesmos e seu uso no tratamento de diabetes e doenças relacionadas.
US5885997A (en) * 1996-07-01 1999-03-23 Dr. Reddy's Research Foundation Heterocyclic compounds, process for their preparation and pharmaceutical compositions containing them and their use in the treatment of diabetes and related diseases
US6006753A (en) 1996-08-30 1999-12-28 Eli Lilly And Company Use of GLP-1 or analogs to abolish catabolic changes after surgery
US7235627B2 (en) 1996-08-30 2007-06-26 Novo Nordisk A/S Derivatives of GLP-1 analogs
US6458924B2 (en) 1996-08-30 2002-10-01 Novo Nordisk A/S Derivatives of GLP-1 analogs
US6174905B1 (en) 1996-09-30 2001-01-16 Mitsui Chemicals, Inc. Cell differentiation inducer
WO1998018763A1 (en) 1996-10-25 1998-05-07 Tanabe Seiyaku Co., Ltd. Tetrahydroisoquinoline derivatives
US6011155A (en) 1996-11-07 2000-01-04 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
HUP0001140A3 (en) 1996-12-05 2002-05-28 Amgen Inc Thousand Oaks Substituted pyrimidinone and pyridone compounds and methods of use
GB9702701D0 (en) 1997-02-01 1997-04-02 Univ Newcastle Ventures Ltd Quinazolinone compounds
US20030060434A1 (en) 1997-02-18 2003-03-27 Loretta Nielsen Combined tumor suppressor gene therapy and chemotherapy in the treatment of neoplasms
US6100234A (en) 1997-05-07 2000-08-08 Tufts University Treatment of HIV
WO1998051803A1 (en) 1997-05-16 1998-11-19 Novo Nordisk Biotech, Inc. Polypeptides having prolyl pipeptidyl aminopeptidase activity and nucleic acids encoding same
EP0897012A1 (en) 1997-07-05 1999-02-17 Societe Des Produits Nestle S.A. Cloning of the prolyl-dipeptidyl-peptidase from aspergillus oryzae
US6235493B1 (en) 1997-08-06 2001-05-22 The Regents Of The University Of California Amino acid substituted-cresyl violet, synthetic fluorogenic substrates for the analysis of agents in individual in vivo cells or tissue
IL125950A0 (en) 1997-09-05 1999-04-11 Pfizer Prod Inc Methods of administering ampa receptor antagonists to treat dyskinesias associated with dopamine agonist therapy
CA2304206A1 (en) 1997-09-29 1999-04-08 Point Therapeutics, Inc. Stimulation of hematopoietic cells in vitro
AU9602198A (en) 1997-10-06 1999-04-27 Trustees Of Tufts College Cytoplasmic dipeptidylpeptidase iv from human t-cells
US6485955B1 (en) 1997-10-06 2002-11-26 The Trustees Of Tufts University Quiescent cell dipeptidyl peptidase: a novel cytoplasmic serine protease
US6342611B1 (en) 1997-10-10 2002-01-29 Cytovia, Inc. Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for capsases and other enzymes and the use thereof
PL341661A1 (en) 1997-10-10 2001-04-23 Cytovia Novel fluorescent reporter particles and their application in combination with testing capsizes
WO1999025719A1 (en) 1997-11-18 1999-05-27 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Novel physiologically active substance sulphostin, process for producing the same, and use thereof
FR2771004B1 (fr) 1997-11-19 2000-02-18 Inst Curie Utilisation de derives de benzhydryl sulfinyle pour la fabrication de medicaments ayant un effet eveillant dans des situations de troubles de la vigilance d'origine medicamenteuse
AU1616499A (en) 1997-12-01 1999-06-16 Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services, The Chemokine variants and methods of use
DE69833784T2 (de) * 1997-12-16 2006-10-19 Novozymes A/S Polypeptide mit aminopeptidase-aktivität und für diese codierende nukleinsäuren
US6380357B2 (en) 1997-12-16 2002-04-30 Eli Lilly And Company Glucagon-like peptide-1 crystals
EP2823812A1 (en) 1998-02-02 2015-01-14 Trustees Of Tufts College Dipeptidylpeptidase IV inhibitors for use in the treatment of Type II diabetes
EP1062222A1 (en) 1998-03-09 2000-12-27 Fondatech Benelux N.V. Serine peptidase modulators
US20020061839A1 (en) 1998-03-09 2002-05-23 Scharpe Simon Lodewijk Serine peptidase modulators
WO1999050249A2 (en) 1998-04-01 1999-10-07 Du Pont Pharmaceuticals Company Pyrimidines and triazines as integrin antagonists
FR2777283B1 (fr) 1998-04-10 2000-11-24 Adir Nouveaux composes peptidiques analogues du glucagon-peptide- 1 (7-37), leur procede de preparation et les compositions pharmaceutiques qui les contiennent
DE19823831A1 (de) 1998-05-28 1999-12-02 Probiodrug Ges Fuer Arzneim Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen
WO1999062914A1 (en) * 1998-06-05 1999-12-09 Point Therapeutics, Inc. Cyclic boroproline compounds
DE19828113A1 (de) 1998-06-24 2000-01-05 Probiodrug Ges Fuer Arzneim Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV
DE19828114A1 (de) 1998-06-24 2000-01-27 Probiodrug Ges Fuer Arzneim Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV
US6129911A (en) 1998-07-10 2000-10-10 Rhode Island Hospital, A Lifespan Partner Liver stem cell
AU5027299A (en) 1998-07-31 2000-02-28 Novo Nordisk A/S Use of glp-1 and analogues for preventing type ii diabetes
DE19834591A1 (de) 1998-07-31 2000-02-03 Probiodrug Ges Fuer Arzneim Verfahren zur Steigerung des Blutglukosespiegels in Säugern
JP4624558B2 (ja) 1998-08-10 2011-02-02 ザ ガバメント オブ ザ ユナイテッド ステイツ オブ アメリカ， アズ レプレゼンテッド バイ ザ セクレタリー， デパートメント オブ ヘルス アンド ヒューマン サービシーズ ＧＬＰ−１またはＥｘｅｎｄｉｎ−４による、非インスリン産生細胞のインスリン産生細胞への分化、およびその使用
CA2339537A1 (en) 1998-08-21 2000-03-02 Barbara Wallner Regulation of substrate activity
AU6044699A (en) 1998-09-17 2000-04-03 Akesis Pharmaceuticals, Inc. Compositions and methods for treatment of glucose metabolism disorders
DE19845153A1 (de) 1998-10-01 2000-04-06 Merck Patent Gmbh Imidazo[4,5]-pyridin-4-on-derivate
US20030176357A1 (en) 1998-10-06 2003-09-18 Pospisilik Andrew J. Dipeptidyl peptidase IV inhibitors and their uses for lowering blood pressure levels
CO5150173A1 (es) 1998-12-10 2002-04-29 Novartis Ag Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv
DE19900471A1 (de) 1999-01-08 2000-07-13 Merck Patent Gmbh Imidazo[4,5c]-pyridin-4-on-derivate
CA2361057C (en) 1999-01-22 2010-04-06 Kazuo Kubo Quinoline derivatives and quinazoline derivatives
ES2353728T3 (es) 1999-02-10 2011-03-04 Curis, Inc. Péptido yy (pyy) para tratar trastornos metabólicos de la glucosa.
WO2000053171A1 (en) 1999-03-05 2000-09-14 Molteni L. E C. Dei Fratelli Alitti Societa' Di Esercizio S.P.A. Use of metformin in the preparation of pharmaceutical compositions capable of inhibiting the enzyme dipeptidyl peptidase iv
GB9906715D0 (en) 1999-03-23 1999-05-19 Ferring Bv Compositions for promoting growth
GB9906714D0 (en) 1999-03-23 1999-05-19 Ferring Bv Compositions for improving fertility
WO2000057721A2 (en) 1999-03-26 2000-10-05 Akesis Pharmaceuticals, Inc. Edible solids for treatment of glucose metabolism disorders
US6548529B1 (en) 1999-04-05 2003-04-15 Bristol-Myers Squibb Company Heterocyclic containing biphenyl aP2 inhibitors and method
EP1171438A1 (en) 1999-04-20 2002-01-16 Novo Nordisk A/S Compounds, their preparation and use
SI1180121T1 (en) 1999-05-17 2004-04-30 Conjuchem, Inc. Long lasting insulinotropic peptides
DE19926233C1 (de) 1999-06-10 2000-10-19 Probiodrug Ges Fuer Arzneim Verfahren zur Herstellung von Thiazolidin
US6172081B1 (en) 1999-06-24 2001-01-09 Novartis Ag Tetrahydroisoquinoline 3-carboxamide derivatives
US6107317A (en) 1999-06-24 2000-08-22 Novartis Ag N-(substituted glycyl)-thiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
US6110949A (en) 1999-06-24 2000-08-29 Novartis Ag N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
US6528486B1 (en) 1999-07-12 2003-03-04 Zealand Pharma A/S Peptide agonists of GLP-1 activity
US6617340B1 (en) 1999-07-29 2003-09-09 Novartis Ag N-(substituted glycyl)-pyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
DE19940130A1 (de) 1999-08-24 2001-03-01 Probiodrug Ges Fuer Arzneim Neue Effektoren der Dipeptidyl Peptidase IV zur topischen Anwendung
JP4748908B2 (ja) 1999-09-10 2011-08-17 ザ・ユニバーシティ・オブ・シドニー ジペプチジルペプチダーゼ
US6559188B1 (en) 1999-09-17 2003-05-06 Novartis Ag Method of treating metabolic disorders especially diabetes, or a disease or condition associated with diabetes
US6414002B1 (en) 1999-09-22 2002-07-02 Bristol-Myers Squibb Company Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
BR0014311A (pt) 1999-09-28 2002-05-21 Merck Patent Gmbh Quinazolinonas
US6447772B1 (en) 1999-10-01 2002-09-10 Klaire Laboratories, Inc. Compositions and methods relating to reduction of symptoms of autism
US6251391B1 (en) 1999-10-01 2001-06-26 Klaire Laboratories, Inc. Compositions containing dipepitidyl peptidase IV and tyrosinase or phenylalaninase for reducing opioid-related symptons
AU7559900A (en) 1999-10-08 2001-04-23 Meiji Seika Kaisha Ltd. M-substituted benzoic acid derivatives exhibiting integrinalphavbeta3 antagonism
US6261794B1 (en) 1999-10-14 2001-07-17 Saint Louis University Methods for identifying inhibitors of methionine aminopeptidases
US7230000B1 (en) 1999-10-27 2007-06-12 Cytokinetics, Incorporated Methods and compositions utilizing quinazolinones
US20040152745A1 (en) 1999-11-12 2004-08-05 Guilford Pharmaceuticals, Inc. Dipeptidyl peptidase IV inhibitors and methods of making and using dipeptidyl peptidase IV inhibitors
AU1916401A (en) 1999-11-12 2001-06-06 Guilford Pharmaceuticals Inc. Dipeptidyl peptidase iv inhibitors and methods of making and using dipeptidyl peptidase iv inhibitors
GB9928330D0 (en) 1999-11-30 2000-01-26 Ferring Bv Novel antidiabetic agents
WO2001041779A2 (en) 1999-12-08 2001-06-14 1149336 Ontario Inc. Combined use of glp-2 receptor agonist and chemotherapeutic agent in treatment
US6380398B2 (en) 2000-01-04 2002-04-30 Novo Nordisk A/S Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV
DK1248604T4 (da) 2000-01-21 2012-05-21 Novartis Ag Kombinationer indeholdende dipeptidylpeptidase-IV-inhibitorer og antidiabetiske midler
AU2001228309A1 (en) 2000-01-24 2001-08-07 Novo-Nordisk A/S N-substituted 2-cyanopyroles and -pyrrolines which are inhibitors of the enzyme dpp-iv
CA2398018C (en) 2000-01-25 2011-10-18 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
HUP0204281A3 (en) * 2000-01-27 2007-03-28 Lilly Co Eli Process for sulubilizing glucagon-like peptide 1 (glp-1) compounds
US6569901B2 (en) 2000-01-28 2003-05-27 Novo Nordisk A/S Alkynyl-substituted propionic acid derivatives, their preparation and use
US7217722B2 (en) 2000-02-01 2007-05-15 Kirin Beer Kabushiki Kaisha Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same
JP2003523396A (ja) 2000-02-25 2003-08-05 ノボ ノルディスク アクティーゼルスカブ ベータ細胞変性の抑制
US6395767B2 (en) 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
US6448045B1 (en) 2000-03-10 2002-09-10 The Regents Of The University Of California Inducing insulin gene expression in pancreas cells expressing recombinant PDX-1
US6608038B2 (en) 2000-03-15 2003-08-19 Novartis Ag Methods and compositions for treatment of diabetes and related conditions via gene therapy
EP1136482A1 (en) 2000-03-23 2001-09-26 Sanofi-Synthelabo 2-Amino-3-(alkyl)-pyrimidone derivatives as GSK3beta inhibitors
AU2001248701A1 (en) 2000-03-24 2001-10-03 Methylgene, Inc. Inhibitors of histone deacetylase
US6555519B2 (en) 2000-03-30 2003-04-29 Bristol-Myers Squibb Company O-glucosylated benzamide SGLT2 inhibitors and method
AU2001254763A1 (en) 2000-03-31 2001-10-08 Prosidion Limited Method for the improvement of islet signaling in diabetes mellitus and for its prevention
US6573096B1 (en) 2000-04-01 2003-06-03 The Research Foundation At State University Of New York Compositions and methods for inhibition of cancer invasion and angiogenesis
US6545170B2 (en) 2000-04-13 2003-04-08 Pharmacia Corporation 2-amino-5, 6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors
WO2001079206A1 (en) 2000-04-18 2001-10-25 Sumitomo Pharmaceuticals Company, Limited Tricyclic quinazolinediones
DK2223922T3 (en) * 2000-04-25 2016-06-06 Icos Corp Inhibitors of HUMANPHOSPHATIDYL-inositol 3-KINASEDELTA
GB0010188D0 (en) * 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
GB0010183D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
DE10025464A1 (de) 2000-05-23 2001-12-06 Inst Medizintechnologie Magdeb Kombinierte Verwendung von Enzyminhibitoren zur Therapie von Autoimmunerkrankungen, bei Transplantationen und Tumorerkrankungen sowie Kombinationen von Enzyminhibitoren umfassende pharmazeutische Zubereitungen
US6783757B2 (en) * 2000-06-01 2004-08-31 Kirkman Group, Inc. Composition and method for increasing exorphin catabolism to treat autism
AU2001263786A1 (en) 2000-06-09 2001-12-17 Prozymex A/S Purified proenzyme of dipeptidyl peptidase i (pro-dppi)
TW583185B (en) 2000-06-13 2004-04-11 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines and pharmaceutical composition for inhibiting dipeptidyl peptidase-IV (DPP-IV) or for the prevention or treatment of diseases or conditions associated with elevated levels of DPP-IV comprising the same
US6432969B1 (en) 2000-06-13 2002-08-13 Novartis Ag N-(substituted glycyl)-2 cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
US6627636B2 (en) 2000-06-15 2003-09-30 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
US6620821B2 (en) 2000-06-15 2003-09-16 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
US7078397B2 (en) 2000-06-19 2006-07-18 Smithkline Beecham Corporation Combinations of dipeptidyl peptidase IV inhibitors and other antidiabetic agents for the treatment of diabetes mellitus
GB0014969D0 (en) 2000-06-19 2000-08-09 Smithkline Beecham Plc Novel method of treatment
AU6895801A (en) 2000-07-04 2002-01-14 Novo Nordisk As Heterocyclic compounds, which are inhibitors of the enzyme dpp-iv
AU2001269123A1 (en) 2000-07-10 2002-01-21 Bayer Aktiengesellschaft Regulation of human dipeptidyl-peptidase iv-like enzyme
TW535080B (en) 2000-07-24 2003-06-01 Ten Square Co Ltd Method and apparatus for optimal fitting activities into customer idle time
JP2002042960A (ja) 2000-07-25 2002-02-08 Yazaki Corp コネクタ支持機構
US6518269B1 (en) 2000-07-28 2003-02-11 University Of Arizona Foundation Cancer treatment
EP1305293A1 (en) 2000-08-01 2003-05-02 Pharmacia Corporation Hexahydro-7-imino-1h-azepin-2-yl-hexanoic acid derivatives as inhibitors of inducible nitric oxide synthase
JP2004519422A (ja) 2000-08-04 2004-07-02 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー ２−（４−ピリジル）アミノ−６−ジアルコキシフェニルピリド〔２，３−ｄ〕ピリミジン−７−オン
DK1308439T3 (da) 2000-08-10 2009-01-12 Mitsubishi Tanabe Pharma Corp Prolinderivater og anvendelse af disse som lægemidler
US20020165237A1 (en) 2000-08-11 2002-11-07 Fryburg David Albert Treatment of the insulin resistance syndrome
US20020037829A1 (en) * 2000-08-23 2002-03-28 Aronson Peter S. Use of DPPIV inhibitors as diuretic and anti-hypertensive agents
US6900226B2 (en) 2000-09-06 2005-05-31 Hoffman-La Roche Inc. Neuropeptide Y antagonists
WO2002020804A1 (en) 2000-09-08 2002-03-14 Prozymex A/S Rat cathepsin, dipeptidyl peptidase i (dppi): crystal structure, inhibitors and its uses
US20020064736A1 (en) 2000-09-27 2002-05-30 Fuji Photo Film Co., Ltd. Dye-forming coupler, silver halide photographic light-sensitive material, and method for producing an azomethine dye
AU2001292874B2 (en) 2000-09-27 2006-06-15 Merck & Co., Inc. Benzopyrancarboxylic acid derivatives for the treatment of diabetes and lipid disorders
GB0023983D0 (en) 2000-09-29 2000-11-15 Prolifix Ltd Therapeutic compounds
SE0003599D0 (sv) 2000-10-05 2000-10-05 Thomas Johansson Anordning för fuktabsorption
ATE407924T1 (de) 2000-10-06 2008-09-15 Mitsubishi Tanabe Pharma Corp Stickstoffhaltige, fünfgliedrige ringverbindungen
CN101270362A (zh) 2000-10-12 2008-09-24 凡林有限公司 与dppiv相关的新丝氨酸蛋白酶基因
ZA200302394B (en) 2000-10-27 2004-03-29 Probiodrug Ag Method for the treatment of neurological and neuropsychological disorders.
AUPR107800A0 (en) 2000-10-27 2000-11-23 University Of Sydney, The Peptide and nucleic acid molecule ii
NZ537490A (en) * 2000-10-30 2006-11-30 Ortho Mcneil Pharm Inc Treatment of diabetes and syndrome X using a sulfamate derivate such as topiramate and metformin
US6586198B2 (en) 2000-10-31 2003-07-01 Vanderbilt University Method of identifying susceptibility to angiotensin converting enzyme inhibto- and vasopeptidase-inhibitor-associated angioedema
CA2427610A1 (en) 2000-10-31 2002-08-08 Merck & Co., Inc. Benzopyrancarboxylic acid derivatives for the treatment of diabetes and lipid disorders
US6864363B2 (en) 2000-11-08 2005-03-08 University Of Georgia Research Foundation, Inc. Dipeptidylpeptidases and methods of use
US20030055052A1 (en) 2000-11-10 2003-03-20 Stefan Peters FAP-activated anti-tumor compounds
US20020155565A1 (en) 2000-11-10 2002-10-24 Pilar Garin-Chesa FAP-activated anti-tumor compounds
TWI243162B (en) 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
US20030203946A1 (en) 2000-11-17 2003-10-30 Carsten Behrens Glucagon antagonists/inverse agonists
HUP0500543A2 (hu) 2000-11-20 2005-09-28 Bristol-Myers Squibb Company Piridonszármazékok mint aP2 inhibitorok és a vegyületeket tartalmazó gyógyszerkészítmények
NZ526622A (en) 2000-12-11 2006-07-28 Amgen Sf Llc CXCR3 antagonists
JPWO2002051836A1 (ja) 2000-12-27 2004-04-22 協和醗酵工業株式会社 ジペプチジルペプチダーゼ−ｉｖ阻害剤
DE10100053A1 (de) 2001-01-02 2002-08-22 Keyneurotek Ag I G Verwendung von Enzyminhibitoren der Dipeptidylpeptidase IV sowie der Aminopeptidase N und pharmazeutischen Zubereitungen daraus zur Prävention und/oder Therapie Ischämie-bedingter akuter und chronischer neurodegenerativer Prozesse und Erkrankungen
JP2004520330A (ja) 2001-01-02 2004-07-08 インスティテュート ヒューア メディツィンテクノロギー マグデブルク ゲーエムベーハー イーエムテーエム 動脈硬化症の治療と予防的治療、ゲル−クームズ分類ｉ型のアレルギー反応の治療と予防、ならびに、毛包性および表皮性の過角化症とケラチノサイトの促進された増殖を伴う皮膚病の治療と予防のための、酵素阻害因子およびその薬剤化合物の併用
WO2002059301A1 (en) 2001-01-27 2002-08-01 K.U. Leuven Research And Development Chemokines
PE20021002A1 (es) * 2001-02-02 2002-12-06 Takeda Chemical Industries Ltd Compuestos heterociclicos condensados
TWI255817B (en) 2001-02-14 2006-06-01 Kissei Pharmaceutical Glucopyranosyloxybenzylbenzene derivatives and medicinal use thereof
WO2002066627A1 (en) 2001-02-16 2002-08-29 Bayer Aktiengesellschaft Regulation of human dipeptidyl peptidase 8
EE05643B1 (et) 2001-02-24 2013-04-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Ksantiini derivaadid, nende valmistamine ja kasutamine ravimina
US6337069B1 (en) * 2001-02-28 2002-01-08 B.M.R.A. Corporation B.V. Method of treating rhinitis or sinusitis by intranasally administering a peptidase
JP4178816B2 (ja) 2001-03-15 2008-11-12 田辺三菱製薬株式会社 医薬組成物
SI1372650T1 (sl) 2001-03-19 2009-04-30 Novartis Ag Kombinacije, ki obsegajo antidiaroično sredstvo in epotilon ali epotilonski derivat
EP1385508B1 (en) 2001-03-27 2008-05-21 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
FR2822826B1 (fr) 2001-03-28 2003-05-09 Servier Lab Nouveaux derives sulfonyles d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
DE10115921A1 (de) 2001-03-30 2002-10-02 Boehringer Ingelheim Pharma Verfahren zur Herstellung von 4,6-Diaminopyrimido[5,4-d]pyrimidinen
US6890905B2 (en) 2001-04-02 2005-05-10 Prosidion Limited Methods for improving islet signaling in diabetes mellitus and for its prevention
GB0109146D0 (en) 2001-04-11 2001-05-30 Ferring Bv Treatment of type 2 diabetes
US6573287B2 (en) 2001-04-12 2003-06-03 Bristo-Myers Squibb Company 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method
PE20021080A1 (es) 2001-04-12 2003-02-12 Boehringer Ingelheim Int Un anticuerpo especifico fapo bibh1 en el tratamiento del cancer
WO2002092127A1 (en) 2001-05-11 2002-11-21 Board Of Regents, The University Of Texas System Anti-cd26 monoclonal antibodies as therapy for diseases associated with cells expressing cd26
FR2824825B1 (fr) 2001-05-15 2005-05-06 Servier Lab Nouveaux derives d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US20030060494A1 (en) 2001-05-18 2003-03-27 Nobuyuki Yasuda Pharmaceutical use of N-carbamoylazole derivatives
IL143366A0 (en) 2001-05-24 2002-04-21 Harasit Medical Res Services & Treatment of renal fibrosis
US7105556B2 (en) 2001-05-30 2006-09-12 Bristol-Myers Squibb Company Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method
US6794379B2 (en) * 2001-06-06 2004-09-21 Tularik Inc. CXCR3 antagonists
DE60209348T2 (de) 2001-06-20 2006-10-12 Merck & Co., Inc. Dipeptidylpeptidase-hemmer zur behandlung von diabetes
EP1406872B1 (en) 2001-06-20 2007-12-19 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
GB0115517D0 (en) 2001-06-25 2001-08-15 Ferring Bv Novel antidiabetic agents
DE10150203A1 (de) 2001-10-12 2003-04-17 Probiodrug Ag Peptidylketone als Inhibitoren der DPIV
US20030130199A1 (en) 2001-06-27 2003-07-10 Von Hoersten Stephan Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
ATE385238T1 (de) 2001-06-27 2008-02-15 Probiodrug Ag Verwendung von dpiv-inhibitoren als therapeutika für krankhafte neurologische zustände
US20030135023A1 (en) 2001-06-27 2003-07-17 Hans-Ulrich Demuth Peptide structures useful for competitive modulation of dipeptidyl peptidase IV catalysis
ATE370943T1 (de) 2001-06-27 2007-09-15 Smithkline Beecham Corp Fluoropyrrolidine als dipeptidyl-peptidase inhibitoren
CN1723196A (zh) 2001-06-27 2006-01-18 史密丝克莱恩比彻姆公司 作为二肽酶抑制剂的氟代吡咯烷
WO2003002530A2 (en) 2001-06-27 2003-01-09 Smithkline Beecham Corporation Pyrrolidines as dipeptidyl peptidase inhibitors
US7368421B2 (en) 2001-06-27 2008-05-06 Probiodrug Ag Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis
DE10154689A1 (de) 2001-11-09 2003-05-22 Probiodrug Ag Substituierte Aminoketonverbindungen
EP1404675B1 (en) 2001-07-03 2008-03-12 Novo Nordisk A/S Dpp-iv-inhibiting purine derivatives for the treatment of diabetes
US6869947B2 (en) 2001-07-03 2005-03-22 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme DPP-IV
UA74912C2 (en) 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
AU2002322585A1 (en) 2001-07-20 2003-03-03 Adipogenix, Inc. Fat accumulation-modulating compounds
WO2003010197A2 (en) 2001-07-25 2003-02-06 Genset S.A. Gmg-1 polynucleotides and polypeptides and uses thereof
CA2453653A1 (en) 2001-07-26 2003-02-06 Genset S.A. Gmg-2 polynucleotides and polypeptides and uses thereof
CZ2004133A3 (cs) 2001-07-30 2004-06-16 Novo Nordisk A/S Deriváty vinylkarboxylové kyseliny, farmaceutický prostředek ho obsahující a jeho použití
JP2004536152A (ja) 2001-07-30 2004-12-02 ノボ　ノルディスク　アクティーゼルスカブ 新規ビニルｎ−（２−ベンゾイルフェニル）−ｌ−チロシン誘導体及び抗糖尿病剤等へのそれらの使用
JP2005501058A (ja) 2001-07-31 2005-01-13 ザ ガバメント オブ ザ ユナイテッドステイツ オブ アメリカ アズ リプレゼンテッド バイ ザ セクレタリー デパートメント オブ ヘルス アンド ヒューマン サービシーズ ザ ナショナル インステ Ｇｌｐ−１、ｅｘｅｎｄｉｎ−４、そのペプチド・アナログ及びその使用
AU2002327430A1 (en) 2001-08-08 2003-02-24 Genzyme Corporation Methods for treating diabetes and other blood sugar disorders
JP2005508891A (ja) 2001-08-13 2005-04-07 プロバイオドラッグ アーゲー レグマインの不可逆性システインプロテアーゼ阻害剤
EP1285922A1 (en) 2001-08-13 2003-02-26 Warner-Lambert Company 1-Alkyl or 1-cycloalkyltriazolo[4,3-a]quinazolin-5-ones as phosphodiesterase inhibitors
JP2003128551A (ja) 2001-08-15 2003-05-08 Sankyo Co Ltd 新規抗糖尿病医薬組成物
US6844316B2 (en) 2001-09-06 2005-01-18 Probiodrug Ag Inhibitors of dipeptidyl peptidase I
DE10143840A1 (de) 2001-09-06 2003-03-27 Probiodrug Ag Neue Inhibitoren der Dipeptidylpeptidase I
EP1426366A4 (en) 2001-09-14 2004-12-08 Mitsubishi Pharma Corp THIAZOLIDE DERIVATIVES AND THEIR MEDICAL USE
US20030186963A1 (en) 2001-09-14 2003-10-02 Dorwald Florencio Zaragoza Substituted piperidines
US6673829B2 (en) 2001-09-14 2004-01-06 Novo Nordisk A/S Aminoazetidine,-pyrrolidine and -piperidine derivatives
EP1463727A2 (en) 2001-09-19 2004-10-06 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme dpp-iv
MXPA04002661A (es) 2001-09-21 2004-11-22 Sanofi Aventis Derivados de pirimidona 4, 3-sustituida.
EP1427415B1 (en) 2001-09-21 2009-08-12 Brystol-Myers Squibb Company Lactam-containing compounds and derivatives thereof as factor xa inhibitors
ES2323576T3 (es) 2001-09-21 2009-07-21 Mitsubishi Tanabe Pharma Corporation Derivados de 4-pirimidona 3-sustituida.
US7019010B2 (en) 2001-09-27 2006-03-28 Novertis Ag Combinations
IL160990A0 (en) 2001-10-01 2004-08-31 Bristol Myers Squibb Co Spiro-hydantoin compounds useful as anti-inflammatory agents
WO2003030946A1 (en) 2001-10-09 2003-04-17 Novartis Ag Regulation of insulin production
US7064135B2 (en) 2001-10-12 2006-06-20 Novo Nordisk Inc. Substituted piperidines
KR20040054729A (ko) 2001-10-18 2004-06-25 브리스톨-마이어스 스큅 컴퍼니 인간 글루카곤-유사-펩티드-1 모방체, 및 당뇨병 및 이와관련된 증상의 치료에 있어서 이의 용도
TWI301834B (en) 2001-10-22 2008-10-11 Eisai R&D Man Co Ltd Pyrimidone compound and pharmaceutical composition including the same
GB0125445D0 (en) 2001-10-23 2001-12-12 Ferring Bv Protease Inhibitors
GB0125446D0 (en) 2001-10-23 2001-12-12 Ferring Bv Novel anti-diabetic agents
US6861440B2 (en) * 2001-10-26 2005-03-01 Hoffmann-La Roche Inc. DPP IV inhibitors
WO2003038123A2 (en) 2001-10-31 2003-05-08 Novartis Ag Methods to treat diabetes and related conditions based on polymorphisms in the tcf1 gene
EP1442028A4 (en) * 2001-11-06 2009-11-04 Bristol Myers Squibb Co SUBSTITUTED ACID DERIVATIVES, WHICH APPRECIATE AS ANTIDIBILICS AND AGENTS AGAINST OBESITAS, AND METHODS
US20030125304A1 (en) 2001-11-09 2003-07-03 Hans-Ulrich Demuth Substituted amino ketone compounds
US20030089935A1 (en) * 2001-11-13 2003-05-15 Macronix International Co., Ltd. Non-volatile semiconductor memory device with multi-layer gate insulating structure
AR037429A1 (es) 2001-11-26 2004-11-10 Schering Corp Derivados de piperidina antagonistas de la mch, composiciones farmaceuticas, un proceso para su elaboracion y el uso de dichos derivados, solos o en combinacion, para la fabricacion de un medicamento para tratamiento de la obesidad y de trastornos del snc
EP1487471A4 (en) 2001-11-26 2010-03-10 Tufts College METHOD FOR TREATING AUTOIMMUNE DISEASES AND ASSOCIATED REAGENTS
EP2316470A3 (en) 2001-11-26 2011-08-24 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
WO2003048081A2 (en) 2001-12-04 2003-06-12 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
GB0129988D0 (en) 2001-12-14 2002-02-06 Ferring Bv Imidazolidineacetic acid derivatives
CA2468413A1 (en) 2001-12-14 2003-06-26 Novo Nordisk A/S Compounds and uses thereof for decreasing activity of hormone-sensitive lipase
SE0104340D0 (sv) 2001-12-20 2001-12-20 Astrazeneca Ab New compounds
TW200301698A (en) 2001-12-21 2003-07-16 Bristol Myers Squibb Co Acridone inhibitors of IMPDH enzyme
WO2003055482A1 (en) 2001-12-21 2003-07-10 Novo Nordisk A/S Amide derivatives as gk activators
AU2002360732A1 (en) 2001-12-26 2003-07-24 Guilford Pharmaceuticals Change inhibitors of dipeptidyl peptidase iv
US6727261B2 (en) 2001-12-27 2004-04-27 Hoffman-La Roche Inc. Pyrido[2,1-A]Isoquinoline derivatives
WO2003059372A2 (en) 2001-12-29 2003-07-24 Novo Nordisk A/S Combined use of a glp-1 compound and a modulator of diabetic late complications
WO2003057200A2 (en) 2002-01-11 2003-07-17 Novo Nordisk A/S Compositions comprising inhibitors of dpp-iv and nep enzymes for the treatment of diabetes
AU2003218969A1 (en) 2002-02-01 2003-09-02 Probiodrug Ag Modulation of t lymphocytes using dp iv inhibitors
US7101898B2 (en) 2002-02-01 2006-09-05 Novo Nordisk A/S Amides of aminoalkyl-substituted azetidines, pyrrolidines, piperidines and azepanes
AU2003207717B9 (en) 2002-02-01 2009-05-07 Merck & Co., Inc. 11-beta-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia
ATE472536T1 (de) 2002-02-13 2010-07-15 Hoffmann La Roche Pyridin- und pyrimidin-derivate
CN1308311C (zh) 2002-02-13 2007-04-04 霍夫曼-拉罗奇有限公司 新型吡啶－和喹啉－衍生物
NZ534582A (en) 2002-02-27 2006-03-31 Pfizer Prod Inc ACC inhibitors
SK3622004A3 (sk) 2002-02-28 2005-02-04 Prosidion Limited Inhibítory DPIV na báze glutaminylu
HUP0200849A2 (hu) 2002-03-06 2004-08-30 Sanofi-Synthelabo N-aminoacetil-2-ciano-pirrolidin-származékok, e vegyületeket tartalmazó gyógyszerkészítmények és eljárás előállításukra
EP1521746B1 (en) 2002-03-07 2011-04-27 X-Ceptor Therapeutics, Inc. Quinazolinone modulators of nuclear receptors
JP2005519949A (ja) 2002-03-11 2005-07-07 ノバルティス アクチエンゲゼルシャフト ナテグリニドの塩
EA200401120A1 (ru) 2002-03-13 2005-02-24 Еуро-Селтик С. А. Арилзамещенные пиримидины и их применение
DE10211555A1 (de) 2002-03-15 2003-10-02 Imtm Inst Fuer Medizintechnolo Verwendung der Inhibitoren von Enzymen mit Aktivitäten der Aminopeptidase N und/oder der Dipeptidylpeptidase IV und pharmazeutischen Zubereitungen daraus zur Therapie und Prävention dermatologischer Erkrankungen mit sebozytärer Hyperproliferation und veränderten Differenzierungszuständen
PE20040291A1 (es) 2002-03-22 2004-07-02 Novartis Ag COMBINACION QUE COMPRENDE UN INHIBIDOR DE HMG-CoA-REDUCTASA Y UN POTENCIADOR DE LA SECRECION DE INSULINA Y/O UN SENSIBILIZANTE DE INSULINA
ES2307916T3 (es) 2002-03-25 2008-12-01 Nippon Kayaku Kabushiki Kaisha Nuevo derivado de alfa-amino-n-(diaminofosfinil)lactama.
EP1490335B1 (en) 2002-03-25 2007-09-19 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US20030232761A1 (en) 2002-03-28 2003-12-18 Hinke Simon A. Novel analogues of glucose-dependent insulinotropic polypeptide
PE20040079A1 (es) 2002-04-03 2004-04-19 Novartis Ag Derivados de indolilmaleimida
US20040106802A1 (en) 2002-04-08 2004-06-03 Torrent Pharmaceuticals Ltd. Novel compounds and therapeutic uses thereof
KR20040105853A (ko) 2002-04-08 2004-12-16 토렌트 파마슈티칼스 리미티드 티아졸리딘-4-카르보니트릴 및 유사체와디펩티딜-펩티다아제 억제제로서의 용도
CA2484551A1 (en) 2002-04-30 2003-11-13 Trustees Of Tufts College Smart pro-drugs of serine protease inhibitors
TW200307667A (en) * 2002-05-06 2003-12-16 Bristol Myers Squibb Co Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
US7057046B2 (en) * 2002-05-20 2006-06-06 Bristol-Myers Squibb Company Lactam glycogen phosphorylase inhibitors and method of use
TW200407143A (en) 2002-05-21 2004-05-16 Bristol Myers Squibb Co Pyrrolotriazinone compounds and their use to treat diseases
JP4141864B2 (ja) * 2002-05-23 2008-08-27 株式会社オーエス 自立式手動昇降スクリーン
DE60333937D1 (de) 2002-05-23 2010-10-07 Novartis Vaccines & Diagnostic Substituierte quinazolinone verbindungen
GB0212412D0 (en) 2002-05-29 2002-07-10 Novartis Ag Combination of organic compounds
US6710040B1 (en) 2002-06-04 2004-03-23 Pfizer Inc. Fluorinated cyclic amides as dipeptidyl peptidase IV inhibitors
MXPA04011958A (es) 2002-06-04 2005-03-31 Pfizer Prod Inc Amidas ciclicas fluoradas como inhibidores de la dipeptidil peptidasa iv.
AU2003233010A1 (en) 2002-06-04 2003-12-19 Pfizer Products Inc. Process for the preparation of 3,3,4,4-tetrafluoropyrrolidine and derivatives thereof
US20060100199A1 (en) 2002-06-06 2006-05-11 Seiji Yoshikawa Novel condensed imidazole derivatives
AR040241A1 (es) 2002-06-10 2005-03-23 Merck & Co Inc Inhibidores de la 11-beta-hidroxiesteroide deshidrogrenasa 1 para el tratamiento de la diabetes obesidad y dislipidemia
HUP0202001A2 (hu) 2002-06-14 2005-08-29 Sanofi-Aventis DDP-IV gátló hatású azabiciklooktán- és nonánszármazékok
CN1688553A (zh) 2002-06-17 2005-10-26 史密丝克莱恩比彻姆公司 化学方法
WO2003106628A2 (en) * 2002-06-17 2003-12-24 Bristol-Myers Squibb Company Benzodiazepine inhibitors of mitochondial f1f0 atp hydrolase and methods of inhibiting f1f0 atp hydrolase
US20040006004A1 (en) 2002-06-27 2004-01-08 Markku Koulu Method for prevention and treatment of diseases or disorders related to excessive formation of vascular tissue or blood vessels
US7105526B2 (en) 2002-06-28 2006-09-12 Banyu Pharmaceuticals Co., Ltd. Benzimidazole derivatives
US20040054171A1 (en) * 2002-07-04 2004-03-18 Jensen Anette Frost Polymorphic forms of a 4H-thieno[3,2-E]-1,2,4-thiadiazine 1,1-dioxide derivative
AU2003248921A1 (en) 2002-07-09 2004-01-23 Point Therapeutics, Inc. Boroproline compound combination therapy
ATE543497T1 (de) 2002-07-09 2012-02-15 Bristol Myers Squibb Co Substituierte heterozyklische derivate als mittel gegen diabetes und adipositas und verfahren
AU2003259131A1 (en) 2002-07-09 2004-01-23 Bristol-Myers Squibb Company Substituted heterocyclic derivatives useful as antidiabetic and antiobesity agents and method
JP2004099600A (ja) 2002-07-19 2004-04-02 Sankyo Co Ltd 二環性アミノ基置換化合物を含有する医薬組成物
AU2003254852A1 (en) 2002-08-08 2004-02-25 Takeda Pharmaceutical Company Limited Fused heterocyclic compounds as peptidase inhibitors
PT1528931E (pt) 2002-08-09 2008-08-13 Prosidion Ltd Inibidores da dipeptidilpeptidase iv para a diminuição da taxa de aumento de peso crónico
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
CN102964347B (zh) 2002-08-21 2015-11-18 勃林格殷格翰制药两合公司 8-[3-氨基-哌啶-1-基]-黄嘌呤化合物，其制备方法及作为药物制剂的用途
DE10238477A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Purinderivate, deren Herstellung und deren Verwendung als Arzneimittel
DE10238470A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
US7495005B2 (en) 2002-08-22 2009-02-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, their preparation and their use in pharmaceutical compositions
UA78104C2 (en) 2002-08-29 2007-02-15 Taisho Pharmaceutical Co Ltd Benzenesulfonate salts of 4-fluoro-2-cyanopyrrolidine derivatives
US6998502B1 (en) 2002-09-05 2006-02-14 Sabinsa Corporation Convenient process of manufacture for difluoromethylornithine and related compounds
EP1398032A1 (en) 2002-09-10 2004-03-17 PheneX Pharmaceuticals AG 4-Oxo-quinazolines as LXR nuclear receptor binding compounds
JP2004123738A (ja) 2002-09-11 2004-04-22 Takeda Chem Ind Ltd 徐放性製剤
WO2004024184A1 (ja) 2002-09-11 2004-03-25 Takeda Pharmaceutical Company Limited 徐放性製剤
EP1543023B1 (en) 2002-09-18 2010-03-17 Prosidion Limited Secondary binding site of dipeptidyl peptidase iv (dp iv)
US20040058876A1 (en) * 2002-09-18 2004-03-25 Torsten Hoffmann Secondary binding site of dipeptidyl peptidase IV (DP IV)
AU2003282800B2 (en) 2002-09-19 2009-10-29 Abbvie Inc. Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
US7262207B2 (en) 2002-09-19 2007-08-28 Abbott Laboratories Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
EP1557165A4 (en) 2002-09-26 2008-12-03 Eisai R&D Man Co Ltd COMBINED MEDICINE
US6869966B2 (en) 2002-09-30 2005-03-22 Banyu Pharmaceutical Co., Ltd. N-substituted-2-oxodihydropyridine derivatives
ATE370141T1 (de) 2002-10-07 2007-09-15 Merck & Co Inc Antidiabetische heterocyclische beta- aminoverbindungen als inhibitoren von dipeptidylpeptidase
AU2003269850A1 (en) 2002-10-08 2004-05-04 Novo Nordisk A/S Hemisuccinate salts of heterocyclic dpp-iv inhibitors
WO2004032861A2 (en) 2002-10-11 2004-04-22 Bristol-Myers Squibb Company Hexahydro-benzimidazolone compounds useful as anti-inflammatory agents
DK1556362T3 (da) 2002-10-18 2008-06-09 Merck & Co Inc Heterocykliske beta-aminodipeptidylpeptidaseinhibitorer til behandling eller forebyggelse af diabetes
US20040132732A1 (en) 2002-10-21 2004-07-08 Wei Han Quinazolinones and derivatives thereof as factor Xa inhibitors
ATE469645T1 (de) 2002-10-23 2010-06-15 Bristol Myers Squibb Co Auf glycinnitril basierende hemmer der dipeptidylpeptidase iv
AU2003286776A1 (en) 2002-10-30 2004-06-07 Guilford Pharmaceuticals Inc. Novel inhibitors of dipeptidyl peptidase iv
MXPA05004890A (es) 2002-11-07 2005-07-22 Merck & Co Inc Derivados de fenilalanina como inhibidores de dipeptidilpeptidasa para el tratamiento o prevencion de diabetes.
US7482337B2 (en) 2002-11-08 2009-01-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
AU2003274601A1 (en) 2002-11-18 2004-06-15 Pfizer Products Inc. Dipeptidyl peptidase iv inhibiting fluorinated cyclic amides
DE10254304A1 (de) 2002-11-21 2004-06-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
AU2002952946A0 (en) 2002-11-27 2002-12-12 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
US7109192B2 (en) 2002-12-03 2006-09-19 Boehringer Ingelheim Pharma Gmbh & Co Kg Substituted imidazo-pyridinones and imidazo-pyridazinones, the preparation thereof and their use as pharmaceutical compositions
UY28103A1 (es) 2002-12-03 2004-06-30 Boehringer Ingelheim Pharma Nuevas imidazo-piridinonas sustituidas, su preparación y su empleo como medicacmentos
AU2003297564A1 (en) 2002-12-04 2004-06-23 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
MXPA05005983A (es) 2002-12-04 2005-08-18 Eisai Co Ltd Compuestos de anillo fusionado 1,3-dihidroimidazol.
US7420079B2 (en) 2002-12-09 2008-09-02 Bristol-Myers Squibb Company Methods and compounds for producing dipeptidyl peptidase IV inhibitors and intermediates thereof
CA2508947A1 (en) 2002-12-20 2004-07-15 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7135467B2 (en) 2003-01-13 2006-11-14 Bristol-Myers Squibb Company HIV integrase inhibitors
WO2004064778A2 (en) 2003-01-17 2004-08-05 Merck & Co. Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7388019B2 (en) 2003-01-31 2008-06-17 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004067509A1 (ja) 2003-01-31 2004-08-12 Sanwa Kagaku Kenkyusho Co., Ltd. ジペプチジルペプチダーゼivを阻害する化合物
WO2004071454A2 (en) 2003-02-13 2004-08-26 Guilford Pharmaceuticals Inc. Substituted azetidine compounds as inhibitors of dipeptidyl peptidase iv
DE10308353A1 (de) 2003-02-27 2004-12-02 Aventis Pharma Deutschland Gmbh Diarylcycloalkylderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
DE10308351A1 (de) 2003-02-27 2004-11-25 Aventis Pharma Deutschland Gmbh 1,3-substituierte Cycloalkylderivate mit sauren, meist heterocyclischen Gruppen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US7148246B2 (en) 2003-02-27 2006-12-12 Sanofi-Aventis Deutschland Gmbh Cycloalkyl derivatives having bioisosteric carboxylic acid groups, processes for their preparation and their use as pharmaceuticals
DE10308356A1 (de) 2003-02-27 2004-09-09 Aventis Pharma Deutschland Gmbh Cycloalkyl substituierte Alkansäurederivate, Verfahren zu ihrer Herstellung und ihre Anwendung als Arzneimittel
AU2003207881A1 (en) 2003-02-28 2004-09-17 Aic Dipeptidyl peptidase inhibitors
WO2004076434A1 (en) 2003-02-28 2004-09-10 Aic Dipeptidyl peptidase inhibitors
WO2004078777A2 (en) 2003-03-04 2004-09-16 Biorexis Pharmaceutical Corporation Dipeptidyl-peptidase protected proteins
AR043443A1 (es) 2003-03-07 2005-07-27 Merck & Co Inc Procedimiento de preparacion de tetrahidrotriazolopirazinas y productos intermedios
US20050014732A1 (en) 2003-03-14 2005-01-20 Pharmacia Corporation Combination of an aldosterone receptor antagonist and an anti-diabetic agent
AR043505A1 (es) 2003-03-18 2005-08-03 Merck & Co Inc Preparacion de beta-cetoamidas e intermediarios de reaccion
WO2004085661A2 (en) 2003-03-24 2004-10-07 Merck & Co., Inc Process to chiral beta-amino acid derivatives
CA2518465A1 (en) 2003-03-25 2004-10-14 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
TWI357408B (en) 2003-03-26 2012-02-01 Mitsubishi Tanabe Pharma Corp 3-substituted-4-pyrimidone derivatives
WO2004087880A2 (en) 2003-03-26 2004-10-14 Bayer Pharmaceuticals Corporation Compounds and their use to treat diabetes and related disorders
WO2004087650A2 (en) 2003-03-27 2004-10-14 Merck & Co. Inc. Process and intermediates for the preparation of beta-amino acid amide dipeptidyl peptidase-iv inhibitors
WO2004089362A1 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S 2-cyanopyrroles and their analogues as ddp-iv inhibitors
JPWO2004096806A1 (ja) 2003-04-30 2006-07-13 大日本住友製薬株式会社 縮合イミダゾール誘導体
NZ568459A (en) 2003-05-05 2009-06-26 Probiodrug Ag Use of effectors of glutaminyl and glutamate cyclases
JP4806628B2 (ja) 2003-05-05 2011-11-02 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤
MXPA05011861A (es) 2003-05-05 2006-02-17 Probiodrug Ag Uso de efectores de ciclasas de glutamato y glutaminil.
US20040229848A1 (en) 2003-05-05 2004-11-18 Hans-Ulrich Demuth Glutaminyl based DP IV-inhibitors
AU2003902260A0 (en) 2003-05-09 2003-05-29 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
US7638638B2 (en) 2003-05-14 2009-12-29 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
ATE447574T1 (de) 2003-05-14 2009-11-15 Merck & Co Inc 3-amino-4-phenylbutansäurederivate als dipeptidylpeptidase-hemmer zur behandlung oder vorbeugung von diabetes
EP1627870A1 (en) 2003-05-15 2006-02-22 Taisho Pharmaceutical Co., Ltd Cyanofluoropyrrolidine derivative
WO2004104215A2 (en) 2003-05-21 2004-12-02 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with dipeptidylpeptidase 7 (dpp7)
WO2004104216A2 (en) 2003-05-21 2004-12-02 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with dipeptidylpeptidase iv (dpp4)
US7332520B2 (en) 2003-06-06 2008-02-19 Merck & Co., Inc. Fused indoles as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
AU2003902946A0 (en) 2003-06-12 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
AU2004249163A1 (en) 2003-06-17 2004-12-29 Merck & Co., Inc. Cyclohexylglycine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
DE10327439A1 (de) 2003-06-18 2005-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Imidazopyridazinon- und Imidazopyridonderivate, deren Herstellung und deren Verwendung als Arzneimittel
US7566707B2 (en) * 2003-06-18 2009-07-28 Boehringer Ingelheim International Gmbh Imidazopyridazinone and imidazopyridone derivatives, the preparation thereof and their use as pharmaceutical compositions
BRPI0411713B8 (pt) 2003-06-20 2021-05-25 Hoffmann La Roche compostos, processo para a sua manufatura, composições farmacêuticas que compreendem os mesmos, método para tratamento e/ou profilaxia de enfermidades que estão associadas com dpp-iv e sua utilização
BRPI0411509A (pt) 2003-06-20 2006-07-25 Hoffmann La Roche compostos, processo para a sua manufatura, composições farmacêuticas que compreendem os mesmos, método para tratamento e/ou profilaxia de enfermidades que estão associadas com dpp-iv e sua utilização
JO2625B1 (en) 2003-06-24 2011-11-01 ميرك شارب اند دوم كوربوريشن Phosphoric acid salts of dipeptidyl betidase inhibitor 4
DE10330842A1 (de) 2003-07-08 2005-02-10 Institut für Medizintechnologie Magdeburg GmbH, IMTM Verwendung der Inhibitoren von Enzymen mit Aktivitäten der Aminopeptidase N und/oder der Dipeptidylpeptidase IV und pharmazeutischen Zubereitungen daraus zur Therapie und Prävention dermatologischer Erkrankungen mit Hyperproliferation und veränderten Differenzierungszuständen von Fibroblasten
AU2004261186A1 (en) 2003-07-31 2005-02-10 Merck & Co., Inc. Hexahydrodiazepinones as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
US6995183B2 (en) 2003-08-01 2006-02-07 Bristol Myers Squibb Company Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods
KR20060041309A (ko) 2003-08-13 2006-05-11 다케다 야쿠힌 고교 가부시키가이샤 ４-피리미돈 유도체 및 펩티딜 펩티다제 저해제로서의 그의용도
WO2005019168A2 (en) * 2003-08-20 2005-03-03 Pfizer Products Inc. Fluorinated lysine derivatives as dipeptidyl peptidase iv inhibitors
WO2005030751A2 (en) 2003-09-08 2005-04-07 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
JP2007505121A (ja) 2003-09-08 2007-03-08 武田薬品工業株式会社 ジペプチジルぺプチダーゼ阻害剤
EP1532980A1 (en) 2003-11-24 2005-05-25 Novo Nordisk A/S N-heteroaryl indole carboxamides and analogues thereof, for use as glucokinase activators in the treatment of diabetes
KR101099206B1 (ko) 2004-02-05 2011-12-27 프로비오드룩 아게 신규한 글루타미닐 시클라제 저해제
EA013427B1 (ru) * 2004-03-15 2010-04-30 Такеда Фармасьютикал Компани Лимитед Ингибиторы дипептидилпептидазы
EP1828192B1 (en) 2004-12-21 2014-12-03 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
AU2006290205B2 (en) 2005-09-14 2012-12-13 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors for treating diabetes
EP2073810B1 (en) * 2006-09-13 2011-08-31 Takeda Pharmaceutical Company Limited Use of 2-6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2h-pyrimidin-1-ylmethyl-4-fluoro-benzonitrile for treating diabetes, cancer, autoimmune disorders and hiv infection
PL1931350T5 (pl) 2005-09-14 2021-11-15 Takeda Pharmaceutical Company Limited Podanie inhibitorów dipeptydylo-peptydazy
US20070060529A1 (en) 2005-09-14 2007-03-15 Christopher Ronald J Administration of dipeptidyl peptidase inhibitors
TW200745079A (en) 2005-09-16 2007-12-16 Takeda Pharmaceuticals Co Polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and methods of use therefor
CA2622642C (en) * 2005-09-16 2013-12-31 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US20100029941A1 (en) * 2006-03-28 2010-02-04 Takeda Pharmaceutical Company Limited Preparation of (r)-3-aminopiperidine dihydrochloride
TW200838536A (en) * 2006-11-29 2008-10-01 Takeda Pharmaceutical Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor

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EA200970519A1 (ru) 2009-12-30
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CN101573351B (zh) 2014-06-18
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CR10874A (es) 2009-07-23
TW200838536A (en) 2008-10-01
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