RU2251544C2 - N-замещенные 2-цианпирролидины - Google Patents

N-замещенные 2-цианпирролидины Download PDF

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Publication number
RU2251544C2
RU2251544C2 RU2001118826/04A RU2001118826A RU2251544C2 RU 2251544 C2 RU2251544 C2 RU 2251544C2 RU 2001118826/04 A RU2001118826/04 A RU 2001118826/04A RU 2001118826 A RU2001118826 A RU 2001118826A RU 2251544 C2 RU2251544 C2 RU 2251544C2
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RU
Russia
Prior art keywords
amino
adamantyl
acetyl
alkyl
formula
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RU2001118826/04A
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English (en)
Russian (ru)
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RU2001118826A (ru
Inventor
Эдуин Бернард ВИЛЛХОЕР (US)
Эдуин Бернард ВИЛЛХОЕР
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Новартис Аг
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Application filed by Новартис Аг filed Critical Новартис Аг
Publication of RU2001118826A publication Critical patent/RU2001118826A/ru
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • A61P3/08—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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
RU2001118826/04A 1998-12-10 1999-12-09 N-замещенные 2-цианпирролидины RU2251544C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US20906898A 1998-12-10 1998-12-10
US09/209068 1998-12-10
US09/209,068 1998-12-10

Publications (2)

Publication Number Publication Date
RU2001118826A RU2001118826A (ru) 2003-06-10
RU2251544C2 true RU2251544C2 (ru) 2005-05-10

Family

ID=22777194

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2001118826/04A RU2251544C2 (ru) 1998-12-10 1999-12-09 N-замещенные 2-цианпирролидины

Country Status (34)

Country Link
US (1) US6166063A (enExample)
EP (1) EP1137635B1 (enExample)
JP (2) JP3681110B2 (enExample)
KR (2) KR100509311B1 (enExample)
CN (1) CN1160330C (enExample)
AR (1) AR023719A1 (enExample)
AT (1) ATE307112T1 (enExample)
BR (1) BRPI9915985B8 (enExample)
CA (1) CA2350609C (enExample)
CO (1) CO5150173A1 (enExample)
CY (3) CY1105355T1 (enExample)
CZ (1) CZ299151B6 (enExample)
DE (3) DE69927844T2 (enExample)
DK (1) DK1137635T3 (enExample)
ES (1) ES2251847T3 (enExample)
FR (1) FR08C0005I2 (enExample)
HK (1) HK1040394B (enExample)
HU (1) HU226769B1 (enExample)
ID (1) ID28796A (enExample)
IL (2) IL143091A0 (enExample)
LU (2) LU91409I2 (enExample)
MY (1) MY123244A (enExample)
NL (2) NL300333I2 (enExample)
NO (3) NO318741B1 (enExample)
NZ (1) NZ511935A (enExample)
PE (1) PE20001317A1 (enExample)
PL (1) PL199443B1 (enExample)
RU (1) RU2251544C2 (enExample)
SK (1) SK286635B6 (enExample)
TR (1) TR200101478T2 (enExample)
TW (1) TW509674B (enExample)
UY (1) UY25843A1 (enExample)
WO (1) WO2000034241A1 (enExample)
ZA (1) ZA200104581B (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2443687C2 (ru) * 2006-04-03 2012-02-27 Матрикс Лэборетериз Лтд. Новые ингибиторы дипептидилпептидазы iv, способы их получения и содержащие их фармацевтические композиции
RU2628573C2 (ru) * 2015-11-27 2017-08-21 Общество с ограниченной ответственностью "Аллель Центр Инновационных Биотехнологий" Ингибитор дипептидилпептидазы-4 для лечения сахарного диабета 2-го типа

Families Citing this family (308)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1113804A2 (en) * 1998-09-17 2001-07-11 Akesis Pharmaceuticals, Inc. Combinations of chromium or vanadium with antidiabetics for glucose metabolism disorders
US6376549B1 (en) * 1998-09-17 2002-04-23 Akesis Pharmaceuticals, Inc. Metforimin-containing compositions for the treatment of diabetes
DE19940130A1 (de) * 1999-08-24 2001-03-01 Probiodrug Ges Fuer Arzneim Neue Effektoren der Dipeptidyl Peptidase IV zur topischen Anwendung
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
CA2390231A1 (en) * 1999-11-12 2001-05-17 Paul Jackson 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
BR0016631A (pt) * 1999-12-23 2003-01-07 Novartis Ag Uso de agentes hipoglicêmico para tratar metabolismo de glicose depreciada
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
EP1741445B1 (en) 2000-01-21 2013-08-14 Novartis AG Combinations comprising dipeptidylpeptidase-IV inhibitors and antidiabetic agents
US20080076811A1 (en) * 2000-01-21 2008-03-27 Bork Balkan Combinations comprising depeptidypeptidase-iv inhibitors and antidiabetic agents
JP2003520849A (ja) * 2000-01-24 2003-07-08 ノボ ノルディスク アクティーゼルスカブ 酵素ｄｐｐ−ｉｖの阻害剤であるｎ−置換２−シアノピロールおよび−ピロリン
US6395767B2 (en) 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
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
EP1301187B1 (en) 2000-07-04 2005-07-06 Novo Nordisk A/S Purine-2,6-diones which are inhibitors of the enzyme dipeptidyl peptidase iv (dpp-iv)
AR033390A1 (es) * 2000-08-22 2003-12-17 Novartis Ag Una composicion farmaceutica que comprende un antagonista del receptor at1 y un potenciador de la secrecion de insulina, el uso de dicha composicion para la fabricacion de un medicamento y un kit de partes
US20060089389A1 (en) 2000-08-22 2006-04-27 Malcolm Allison Combination
US20070135345A1 (en) * 2000-09-18 2007-06-14 Henriksen Dennis B Use of GLP-2 for the treatment or prevention, of bone-related disorders
PT1326630E (pt) 2000-09-18 2008-09-02 Sanos Bioscience As Utilização de péptidos glp-2
US20080249016A1 (en) * 2000-09-18 2008-10-09 Sanos Bioscience A/S Use of GLP-2 in a combination treatment for bone-related disorders
US7371721B2 (en) * 2000-09-18 2008-05-13 Sanos Bioscience A/S Use of GLP-2 and related compounds for the treatment, prevention, diagnosis, and prognosis of bone-related disorders and calcium homeostasis related syndromes
PT1325910E (pt) * 2000-10-06 2008-10-27 Mitsubishi Tanabe Pharma Corp Compostos de anel alifático de cinco membros contendo azoto
TWI243162B (en) * 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
UA74023C2 (en) * 2000-11-10 2005-10-17 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
CA2433090A1 (en) * 2000-12-27 2002-07-04 Kyowa Hakko Kogyo Co., Ltd. Dipeptidyl peptidase iv inhibitor
GB0109146D0 (en) * 2001-04-11 2001-05-30 Ferring Bv Treatment of type 2 diabetes
US20030060494A1 (en) * 2001-05-18 2003-03-27 Nobuyuki Yasuda Pharmaceutical use of N-carbamoylazole derivatives
CA2450475A1 (en) 2001-06-20 2003-01-03 Linda Brockunier Dipeptidyl peptidase inhibitors for the treatment of diabetes
JP2004535433A (ja) 2001-06-20 2004-11-25 メルク　エンド　カムパニー　インコーポレーテッド 糖尿病治療用のジペプチジルペプチダーゼ阻害薬
ES2296962T3 (es) 2001-06-27 2008-05-01 Smithkline Beecham Corporation Pirrolidinas como inhibidores de dipeptidil peptidasa.
CN1990469A (zh) 2001-06-27 2007-07-04 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
DE60221983T2 (de) * 2001-06-27 2008-05-15 Smithkline Beecham Corp. Fluorpyrrolidine als dipeptidyl-peptidase inhibitoren
US6709651B2 (en) * 2001-07-03 2004-03-23 B.M.R.A. Corporation B.V. Treatment of substance P-related disorders
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
US6861440B2 (en) 2001-10-26 2005-03-01 Hoffmann-La Roche Inc. DPP IV inhibitors
JP2005507261A (ja) * 2001-10-31 2005-03-17 ノバルティス アクチエンゲゼルシャフト Ｔｃｆ１遺伝子における多型に基づく糖尿病および関連状態の治療方法
US20050101638A1 (en) * 2002-11-08 2005-05-12 Webb Randy L. Combination of organic compounds
US20030135663A1 (en) * 2002-01-16 2003-07-17 Sun Microsystems, Inc. Method, system, and program for including device parameters from a device driver in a configuration file
DE60333166D1 (de) 2002-02-13 2010-08-12 Hoffmann La Roche Pyridin- und pyrimidin-derivate
CA2474460C (en) 2002-02-13 2009-12-22 F. Hoffmann-La Roche Ag Pyridine- and quinoline-derivatives
EP1338595B1 (en) 2002-02-25 2006-05-03 Eisai Co., Ltd. Xanthine derivatives as DPP-IV inhibitors
US7307164B2 (en) * 2002-03-25 2007-12-11 Merck & Co., Inc. β-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
SG154333A1 (en) * 2002-06-03 2009-08-28 Novartis Ag The use of substituted cyanopyrrolidines and combination preparations containing them for treating hyperlipidemia and associated diseases
US6710040B1 (en) 2002-06-04 2004-03-23 Pfizer Inc. Fluorinated cyclic amides as dipeptidyl peptidase IV inhibitors
JP2004026678A (ja) * 2002-06-24 2004-01-29 Microbial Chem Res Found ２型糖尿病治療剤
AU2003248259A1 (en) * 2002-07-10 2004-02-02 Yamanouchi Pharmaceutical Co., Ltd. Novel azetidine derivative or salt thereof
DE60330485D1 (de) 2002-07-15 2010-01-21 Merck & Co Inc Zur behandlung von diabetes
TW200401635A (en) * 2002-07-23 2004-02-01 Yamanouchi Pharma Co Ltd 2-Cyano-4-fluoropyrrolidine derivative or salt thereof
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
WO2004026822A2 (en) * 2002-09-19 2004-04-01 Abbott Laboratories Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
EP1554280B1 (en) * 2002-10-07 2007-08-15 Merck & Co., Inc. Antidiabetic beta-amino heterocyclic dipeptidyl peptidase inhibitors
PL216527B1 (pl) 2002-10-18 2014-04-30 Merck & Co Inc Związki ß-aminoheterocykliczne i kompozycja farmaceutyczna
EP1562925B1 (en) 2002-11-07 2007-01-03 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
CA2508487A1 (en) * 2002-12-04 2004-06-17 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
EP1583534A4 (en) * 2002-12-20 2007-08-29 Merck & Co Inc 3-AMINO-4-PHENYLBUTANIC ACID DERIVATIVES AS DIPEPTIDYL-PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
KR101078098B1 (ko) 2003-01-14 2011-10-28 아레나 파마슈티칼스, 인크. 대사 조절제로서의 １,２,３-삼치환된 아릴 및 헤테로아릴유도체, 및 당뇨병 및 고혈당증을 비롯한 이에 관련된장애의 예방 및 치료
CA2512546A1 (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
CA2513684A1 (en) * 2003-01-31 2004-08-19 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US20040242568A1 (en) 2003-03-25 2004-12-02 Syrrx, Inc. Dipeptidyl peptidase inhibitors
GB0308854D0 (en) * 2003-04-16 2003-05-21 Novartis Ag Organic compounds
PE20081293A1 (es) * 2003-04-16 2008-11-04 Novartis Ag Procedimiento de preparacion de compuestos 2(s)-cianopirrolidina n-(n'-glicilo sustituida)
WO2004103993A1 (en) 2003-05-14 2004-12-02 Syrrx, Inc. Dipeptidyl peptidase inhibitors
CN1787823A (zh) * 2003-05-14 2006-06-14 麦克公司 作为二肽基肽酶抑制剂用于治疗或预防糖尿病的3－氨基－4－苯基丁酸衍生物
CN1798556A (zh) 2003-06-06 2006-07-05 麦克公司 作为治疗或者预防糖尿病的二肽基肽酶抑制剂的稠合吲哚
WO2004112701A2 (en) 2003-06-17 2004-12-29 Merck & Co., Inc. Cyclohexylglycine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
HRP20110018T1 (hr) 2003-06-20 2011-02-28 F. Hoffmann - La Roche Ag Derivati pirido(2,1-a)-izokinolina kao inhibitori dpp-iv
AU2004251829B2 (en) 2003-06-20 2009-12-17 F. Hoffmann-La Roche Ag Hexahydropyridoisoqinolines as DPP-IV inhibitors
AR045047A1 (es) 2003-07-11 2005-10-12 Arena Pharm Inc Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos
CA2533893A1 (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
US7169926B1 (en) 2003-08-13 2007-01-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
EP1506967B1 (en) 2003-08-13 2007-11-21 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7678909B1 (en) 2003-08-13 2010-03-16 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
EP1699777B1 (en) 2003-09-08 2012-12-12 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
TW200530157A (en) * 2003-09-09 2005-09-16 Japan Tobacco Inc Dipeptidyl peptidase iv inhibitor
WO2005033099A2 (en) * 2003-10-03 2005-04-14 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
JP2007509898A (ja) * 2003-11-03 2007-04-19 プロビオドルグ エージー 神経障害治療に有用な組合せ
JP2007510651A (ja) * 2003-11-04 2007-04-26 メルク　エンド　カムパニー　インコーポレーテッド 糖尿病の治療又は予防のためのジペプチジルペプチダーゼ−ｉｖ阻害剤としての縮合フェニルアラニン誘導体
US7576121B2 (en) * 2003-11-12 2009-08-18 Phenomix Corporation Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
US7674913B2 (en) * 2003-11-12 2010-03-09 Phenomix Corporation Heterocyclic boronic acid compounds
US7767828B2 (en) * 2003-11-12 2010-08-03 Phenomix Corporation Methyl and ethyl substituted pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
US7317109B2 (en) * 2003-11-12 2008-01-08 Phenomix Corporation Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
CA2545641A1 (en) * 2003-11-17 2005-06-02 Novartis Ag Use of organic compounds
RU2385723C2 (ru) * 2003-11-17 2010-04-10 Новартис Аг Применение ингибиторов дипептидилпептидазы iv
DK3366283T3 (da) 2004-01-20 2021-11-22 Novartis Ag Direkte sammenpresningsformulering og fremgangsmåde
ES2375625T3 (es) * 2004-02-05 2012-03-02 Kyorin Pharmaceutical Co., Ltd. Derivados de biciclo éster.
CA2554378A1 (en) * 2004-02-18 2005-08-25 Kyorin Pharmaceutical Co., Ltd. Bicycloamide derivative
US7501426B2 (en) 2004-02-18 2009-03-10 Boehringer Ingelheim International Gmbh 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
WO2005079795A2 (en) * 2004-02-20 2005-09-01 Novartis Ag Dpp-iv inhibitors for treating neurodegeneration and cognitive disorders
WO2005082847A1 (ja) * 2004-02-27 2005-09-09 Kyorin Pharmaceutical Co., Ltd. ビシクロ誘導体
CN1942186B (zh) * 2004-03-09 2010-10-06 国家卫生研究院 吡咯烷化合物
US7732446B1 (en) 2004-03-11 2010-06-08 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
MXPA06010571A (es) 2004-03-15 2007-02-16 Takeda Pharmaceutical Inhibidores de dipeptidil peptidasa.
US7741082B2 (en) * 2004-04-14 2010-06-22 Bristol-Myers Squibb Company Process for preparing dipeptidyl peptidase IV inhibitors and intermediates therefor
TW200604167A (en) * 2004-04-27 2006-02-01 Astellas Pharma Inc Pyrrolidine derivatives
CN1950349A (zh) 2004-05-04 2007-04-18 默克公司 作为用于治疗或预防糖尿病的二肽基肽酶－ⅳ抑制剂的1,2,4－噁二唑衍生物
JP2007538079A (ja) 2004-05-18 2007-12-27 メルク　エンド　カムパニー　インコーポレーテッド 糖尿病の治療又は予防のためのジペプチジルペプチダーゼ−ｉｖ阻害剤としてのシクロヘキシルアラニン誘導体
US7935723B2 (en) * 2004-06-04 2011-05-03 Novartis Pharma Ag Use of organic compounds
US7687638B2 (en) 2004-06-04 2010-03-30 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
WO2006017292A1 (en) 2004-07-12 2006-02-16 Phenomix Corporation Constrained cyano compounds
WO2006019965A2 (en) 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
AU2005267093B2 (en) 2004-07-23 2009-10-01 Nuada Llc Peptidase inhibitors
TW200608967A (en) 2004-07-29 2006-03-16 Sankyo Co Pharmaceutical compositions containing with diabetic agent
AR050615A1 (es) * 2004-08-27 2006-11-08 Novartis Ag Composiciones farmaceuticas para la administracion oral
AP2007003973A0 (en) 2004-10-12 2007-07-30 Glenmark Pharmaceuticals Sa Novel dideptidyl peptidase IV inhibitors, pharmaceutical compositions containing them, and proces for their preparation
WO2006047248A1 (en) * 2004-10-25 2006-05-04 Novartis Ag Combination of dpp-iv inhibitor, ppar antidiabetic and metformin
DE102004054054A1 (de) 2004-11-05 2006-05-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine
MX2007007434A (es) 2004-12-20 2007-07-17 Hoffmann La Roche Derivados de 4-aminopiperidina.
US7411093B2 (en) 2004-12-20 2008-08-12 Hoffman-La Roche Inc. Aminocycloalkanes as DPP-IV inhibitors
EP1828192B1 (en) 2004-12-21 2014-12-03 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
DOP2006000008A (es) 2005-01-10 2006-08-31 Arena Pharm Inc Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1
GT200600008A (es) * 2005-01-18 2006-08-09 Formulacion de compresion directa y proceso
JP2008024592A (ja) * 2005-01-28 2008-02-07 Taisho Pharmaceut Co Ltd シアノピロリジン誘導体含有固形製剤用組成物、それを含有する固形製剤及びその製造方法
WO2006090244A1 (en) * 2005-02-22 2006-08-31 Glenmark Pharmaceuticals S.A. New adamantane derivatives as dipeptidyl, peptidase iv inhibitors, processes for their preparation, and pharmaceutical compositions containing them
TWI357902B (en) 2005-04-01 2012-02-11 Lg Life Science Ltd Dipeptidyl peptidase-iv inhibiting compounds, meth
EP1888562B1 (en) 2005-04-22 2014-06-18 Alantos Pharmaceuticals Holding, Inc. Dipeptidyl peptidase-iv inhibitors
US7825139B2 (en) 2005-05-25 2010-11-02 Forest Laboratories Holdings Limited (BM) Compounds and methods for selective inhibition of dipeptidyl peptidase-IV
CA2610022A1 (en) 2005-06-06 2006-12-14 Georgetown University Compositions and methods for lipo modeling
MY152185A (en) 2005-06-10 2014-08-29 Novartis Ag Modified release 1-[(3-hydroxy-adamant-1-ylamino)-acetyl]-pyrrolidine-2(s)-carbonitrile formulation
US20090149504A1 (en) * 2005-06-17 2009-06-11 Aurigene Discovery Technologies Limited Novel 5-Substituted Indole Derivatives As Dipeptidyl Peptidase IV (DPP-IV) Inhibitors
KR20080028422A (ko) * 2005-07-12 2008-03-31 노파르티스 아게 Ｄｐｐ-ｉｖ 억제제 및 칸나비노이드 ｃｂ1 수용체길항제의 배합물
DE102005035891A1 (de) 2005-07-30 2007-02-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
US20080279932A1 (en) * 2005-08-04 2008-11-13 Jean-Louis Reber Compounds
GT200600381A (es) 2005-08-25 2007-03-28 Compuestos organicos
ME02005B (me) 2005-09-14 2012-08-31 Takeda Pharmaceuticals Co Inhibitori dipeptidil peptidaze za lečenje dijabetesa
CN101360723A (zh) 2005-09-16 2009-02-04 武田药品工业株式会社 制备嘧啶二酮衍生物的方法
TW200738266A (en) * 2005-09-29 2007-10-16 Sankyo Co Pharmaceutical agent containing insulin resistance improving agent
BRPI0616694B8 (pt) * 2005-09-29 2021-05-25 Novartis Ag processo para preparar comprimido farmacêutico com 80 e 96% em peso com base no peso seco de vildagliptina e metformina ou seus sais farmaceuticamente aceitáveis
AU2006301892A1 (en) * 2005-10-07 2007-04-19 Waratah Pharmaceuticals, Inc. Combined use of DPP IV inhibitors and gastrin compounds
GB0526291D0 (en) 2005-12-23 2006-02-01 Prosidion Ltd Therapeutic method
AU2007238522A1 (en) * 2006-01-06 2007-10-25 Novartis Ag Use of vildagliptin for the treatment of diabetes
CN101395131B (zh) 2006-03-08 2012-11-14 杏林制药株式会社 氨基乙酰基吡咯烷甲腈衍生物的制备方法及其制备中间体
CN101432025B (zh) 2006-03-21 2012-04-04 安米林药品公司 肽-肽酶抑制剂结合物及其使用方法
WO2007112347A1 (en) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
CA2682846C (en) * 2006-04-03 2015-05-12 Matrix Laboratories Ltd. Novel dipeptidyl peptidase iv inhibitors and processes for their preparation and pharmaceutical compositions containing them
BRPI0710597A2 (pt) 2006-04-11 2012-06-19 Arena Pharm Inc método de uso do receptor gpr119 para identificar compostos úteis para aumento da massa óssea em um indivìduo
PE20071221A1 (es) 2006-04-11 2007-12-14 Arena Pharm Inc Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
MX2008014024A (es) 2006-05-04 2008-11-14 Boehringer Ingelheim Int Formas poliformas.
PE20110235A1 (es) 2006-05-04 2011-04-14 Boehringer Ingelheim Int Combinaciones farmaceuticas que comprenden linagliptina y metmorfina
KR20090031368A (ko) 2006-05-26 2009-03-25 아밀린 파마슈티칼스, 인크. 울혈성 심부전 치료용 조성물 및 방법
CA2662084A1 (en) 2006-09-07 2008-03-13 Nycomed Gmbh Combination treatment for diabetes mellitus
MY145447A (en) * 2006-09-13 2012-02-15 Takeda Pharmaceutical Use of 2-6(3-amino-piperidin-1-yl)-3-methyl-2, 4-dioxo-3, 4-dihydrp-2h-pyrimidin-1-ylmethyl-4-fluoro-benzonitrile
US8324383B2 (en) 2006-09-13 2012-12-04 Takeda Pharmaceutical Company Limited Methods of making 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
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
WO2008084383A2 (en) * 2007-01-10 2008-07-17 Medichem, S.A. Process for preparing vildagliptin
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
US20080064701A1 (en) * 2007-04-24 2008-03-13 Ramesh Sesha Anti-diabetic combinations
ATE550319T1 (de) 2007-03-22 2012-04-15 Kyorin Seiyaku Kk Verfahren zur herstellung eines aminoacetylpyrrolidincarbonitrilderivats
CN103330939A (zh) 2007-04-03 2013-10-02 田边三菱制药株式会社 二肽基肽酶iv抑制化合物和甜味剂的并用
DE102007022007A1 (de) * 2007-05-08 2008-11-13 Schebo Biotech Ag Neuartike Pharmazeutika, Verfahren zu ihrer Herstellung und ihre Verwendung in der Prophylaxe und Therapie von ZNS-Erkrankungen und Diabetes
AU2008259342B2 (en) 2007-06-04 2014-07-10 Ben-Gurion University Of The Negev Research And Development Authority Tri-aryl compounds and compositions comprising the same
CL2008002427A1 (es) 2007-08-16 2009-09-11 Boehringer Ingelheim Int Composicion farmaceutica que comprende 1-cloro-4-(b-d-glucopiranos-1-il)-2-[4-((s)-tetrahidrofurano-3-iloxi)bencil]-benceno combinado con 1-[(4-metilquinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-(r)-aminopiperidin-1-il)xantina; y su uso para tratar diabetes mellitus tipo 2.
EP3542801A1 (en) * 2007-08-17 2019-09-25 Boehringer Ingelheim International GmbH Purin derivatives for use in the treatment of fap-related diseases
GB2465132B (en) * 2007-09-21 2012-06-06 Lupin Ltd Compounds as dipeptidyl peptidase IV (DPP IV) inhibitors
US20090082420A1 (en) * 2007-09-25 2009-03-26 Protia, Llc Deuterium-enriched vildagliptin
WO2009042922A2 (en) * 2007-09-27 2009-04-02 Amylin Pharmaceuticals, Inc. Peptide-peptidase inhibitor conjugates and methods of making and using same
CA2704493A1 (en) 2007-11-30 2009-06-04 Novartis Ag Organic compounds
BRPI0820665A2 (pt) * 2007-12-12 2018-05-29 Astrazeneca Ab compostos de peptidil nitrilas, processos para fabricação dos mesmos, composição farmacêutica, combinação e uso de ditos compostos
CN101903386B (zh) 2007-12-21 2015-04-22 株式会社Lg生命科学 抑制二肽基肽酶-ⅳ的化合物、其制备方法以及含所述化合物作为活性剂的药物组合物
CL2008003653A1 (es) 2008-01-17 2010-03-05 Mitsubishi Tanabe Pharma Corp Uso de un inhibidor de sglt derivado de glucopiranosilo y un inhibidor de dppiv seleccionado para tratar la diabetes; y composicion farmaceutica.
US8551524B2 (en) 2008-03-14 2013-10-08 Iycus, Llc Anti-diabetic combinations
PE20140960A1 (es) * 2008-04-03 2014-08-15 Boehringer Ingelheim Int Formulaciones que comprenden un inhibidor de dpp4
EP2108960A1 (en) 2008-04-07 2009-10-14 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY
PE20100156A1 (es) * 2008-06-03 2010-02-23 Boehringer Ingelheim Int Tratamiento de nafld
WO2009155309A1 (en) * 2008-06-19 2009-12-23 Concert Pharmaceuticals, Inc. Substituted cyanopyrrolidine derivatives
KR20200118243A (ko) 2008-08-06 2020-10-14 베링거 인겔하임 인터내셔날 게엠베하 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
WO2010016584A1 (ja) * 2008-08-07 2010-02-11 杏林製薬株式会社 ビシクロ[２．２．２]オクチルアミン誘導体の製造方法
EP2327406A4 (en) * 2008-08-14 2014-04-09 Kyorin Seiyaku Kk STABILIZED PHARMACEUTICAL COMPOSITION
CN103816158A (zh) * 2008-08-15 2014-05-28 勃林格殷格翰国际有限公司 用于治疗fab-相关疾病的嘌呤衍生物
CZ2008512A3 (cs) 2008-08-26 2010-03-10 Zentiva, A. S Zpusob prípravy vysoce cistého vildagliptinu
CN102149407A (zh) 2008-09-10 2011-08-10 贝林格尔.英格海姆国际有限公司 治疗糖尿病和相关病症的组合疗法
CN102850330B (zh) * 2008-09-23 2014-10-15 成都地奥制药集团有限公司 经溴代的制备n取代的吡咯烷衍生物的方法
US20200155558A1 (en) 2018-11-20 2020-05-21 Boehringer Ingelheim International Gmbh Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug
JO2870B1 (en) 2008-11-13 2015-03-15 ميرك شارب اند دوهم كورب Amino Tetra Hydro Pirans as Inhibitors of Peptide Dipeptide IV for the Treatment or Prevention of Diabetes
CN107011345A (zh) 2008-12-23 2017-08-04 勃林格殷格翰国际有限公司 有机化合物的盐形式
TW201036975A (en) 2009-01-07 2010-10-16 Boehringer Ingelheim Int Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy
EP2376447B1 (en) 2009-01-09 2017-08-09 Orchid Pharma Limited Dipeptidyl peptidase iv inhibitors
TWI466672B (zh) 2009-01-29 2015-01-01 Boehringer Ingelheim Int 小兒科病人糖尿病之治療
HUE050287T2 (hu) 2009-02-13 2020-11-30 Boehringer Ingelheim Int SGLT2-inhibitort, DPP-IV-inhibitort és adott esetben egy további antidiabetikus hatóanyagot tartalmazó gyógyászati készítmény és alkalmazásai
AU2010212823B2 (en) 2009-02-13 2016-01-28 Boehringer Ingelheim International Gmbh Antidiabetic medications comprising a DPP-4 inhibitor (linagliptin) optionally in combination with other antidiabetics
WO2010110436A1 (ja) 2009-03-27 2010-09-30 杏林製薬株式会社 塩基性添加剤を含有するマトリックス型徐放性製剤
AU2010244218B2 (en) 2009-05-07 2012-07-19 Astrazeneca Ab Substituted 1-cyanoethylheterocyclylcarboxamide compounds 750
JP5659224B2 (ja) 2009-05-15 2015-01-28 ノバルティス アーゲー アルドステロンシンターゼ阻害剤としてのアリールピリジン
US8455522B2 (en) 2009-05-15 2013-06-04 Novartis Ag Benzoxazolone derivatives as aldosterone synthase inhibitors
MX2011012628A (es) 2009-05-28 2011-12-14 Novartis Ag Derivados amino-propionicos sustituidos como inhibidores de neprilisina.
ES2582395T3 (es) 2009-05-28 2016-09-12 Novartis Ag Derivados aminobutíricos sustituidos como inhibidores de neprilisina
GB2483614B (en) 2009-06-18 2014-12-03 Lupin Ltd 2-Amino-2- [8-(dimethyl carbamoyl)- 8-aza- bicyclo [3.2.1] oct-3-yl]-exo- ethanoyl derivatives as potent dpp-iv inhibitors
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
WO2011014520A2 (en) 2009-07-29 2011-02-03 Irm Llc Compounds and compositions as modulators of gpr119 activity
EA034049B1 (ru) 2009-07-31 2019-12-23 КРКА, д.д., НОВО МЕСТО Гранулят, включающий вилдаглиптин, способ его получения и фармацевтическая композиция
KR20120092096A (ko) 2009-09-02 2012-08-20 머크 샤프 앤드 돔 코포레이션 당뇨병의 치료 또는 예방을 위한 디펩티딜 펩티다제-ｉｖ 억제제로서의 아미노테트라히드로피란
CN102656163B (zh) 2009-09-03 2016-01-13 拜奥埃内杰尼克斯公司 抑制pask的杂环化合物
EP2295083A1 (de) 2009-09-15 2011-03-16 Ratiopharm GmbH Pharmazeutische Zusammensetzung mit den Wirkstoffen Metformin und Sitagliptin oder Vildagliptin
WO2011034954A1 (en) 2009-09-15 2011-03-24 Cerulean Pharma Inc. Treatment of cancer
HUP0900638A2 (en) 2009-10-07 2011-05-30 Egyt Gyogyszervegyeszeti Gyar Adducts of inorganic salts basea on vildaelitpin applicable for preparation of pharmaceutical compositions
EP2308847B1 (en) 2009-10-09 2014-04-02 EMC microcollections GmbH Substituted pyridines as inhibitors of dipeptidyl peptidase IV and their application for the treatment of diabetes and related diseases
AU2010303780B2 (en) 2009-10-09 2014-02-20 Irm Llc Compounds and compositions as modulators of GPR119 activity
CN102712589B (zh) 2009-11-17 2015-05-13 诺华股份有限公司 作为醛固酮合酶抑制剂的芳基-吡啶衍生物
JO2967B1 (en) 2009-11-20 2016-03-15 نوفارتس ايه جي Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors
CN102781237A (zh) 2009-11-23 2012-11-14 天蓝制药公司 用于传递治疗剂的基于环糊精的聚合物
EP2504002B1 (en) 2009-11-27 2019-10-09 Boehringer Ingelheim International GmbH Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin
CN102666535B (zh) 2009-11-30 2015-02-25 诺华股份有限公司 作为醛固酮合酶抑制剂的咪唑衍生物
US8394858B2 (en) 2009-12-03 2013-03-12 Novartis Ag Cyclohexane derivatives and uses thereof
CN102762531B (zh) 2009-12-22 2015-12-02 盐野义制药株式会社 金刚烷胺衍生物
WO2011090940A1 (en) 2010-01-19 2011-07-28 Cerulean Pharma Inc. Cyclodextrin-based polymers for therapeutic delivery
WO2011103256A1 (en) 2010-02-22 2011-08-25 Merck Sharp & Dohme Corp. Substituted aminotetrahydrothiopyrans and derivatives thereof as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
CN101798270B (zh) * 2010-02-25 2013-04-17 东华大学 一种3-氨基-1-金刚烷醇的制备方法
WO2011113947A1 (en) 2010-03-18 2011-09-22 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
WO2011127051A1 (en) 2010-04-06 2011-10-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
KR101927068B1 (ko) 2010-05-05 2018-12-10 베링거 인겔하임 인터내셔날 게엠베하 체중 감소 치료에 후속하는 dpp-4 억제제에 의한 순차적 병용 요법
US8980929B2 (en) 2010-05-21 2015-03-17 Merck Sharp & Dohme Corp. Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
CN102260265B (zh) 2010-05-24 2015-09-02 上海阳帆医药科技有限公司 六氢吡咯[3,4-b]吡咯衍生物、其制备方法及其用途
CN101870671B (zh) * 2010-06-11 2012-06-27 漆又毛 金刚烷基吡咯烷衍生物及制备和应用
KR20200028498A (ko) 2010-06-24 2020-03-16 베링거 인겔하임 인터내셔날 게엠베하 당뇨병 요법
IT1400714B1 (it) 2010-07-06 2013-06-28 Chemelectiva S R L Processo ed intermedi per la preparazione di un principio attivo.
US8697739B2 (en) 2010-07-29 2014-04-15 Novartis Ag Bicyclic acetyl-CoA carboxylase inhibitors and uses thereof
WO2012020724A1 (ja) * 2010-08-09 2012-02-16 塩野義製薬株式会社 アミノアダマンタンカルバメート誘導体の製造方法
HU231050B1 (hu) 2010-08-19 2020-02-28 Egis Gyógyszergyár Nyrt. Eljárás gyógyszerhatóanyag előállítására
SG188548A1 (en) 2010-09-22 2013-04-30 Arena Pharm Inc Modulators of the gpr119 receptor and the treatment of disorders related thereto
AR083878A1 (es) 2010-11-15 2013-03-27 Boehringer Ingelheim Int Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento
US8877815B2 (en) 2010-11-16 2014-11-04 Novartis Ag Substituted carbamoylcycloalkyl acetic acid derivatives as NEP
US8673974B2 (en) 2010-11-16 2014-03-18 Novartis Ag Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors
TR201107482A1 (tr) 2010-12-21 2012-07-23 Sanovel İlaç San.Ve Ti̇c.A.Ş. Vildagliptin ve gliklazidin iki tabakalı kombinasyon kompozisyonu.
EP2468268B1 (en) 2010-12-21 2017-12-13 Sanovel Ilaç Sanayi Ve Ticaret Anonim Sirketi Combination composition of vildagliptin and gliclazide
TR201101809A1 (tr) 2010-12-21 2012-07-23 Sanovel İlaç Sanayi̇ Ve Ti̇caret Anoni̇m Şi̇rketi̇ Vildagliptin ve glimepirid kombinasyonları.
TR201010683A1 (tr) 2010-12-21 2012-07-23 Sanovel İlaç San. Ve Ti̇c. A.Ş. Vildagliptin formülasyonları.
CN103354757A (zh) 2011-01-31 2013-10-16 卡迪拉保健有限公司 脂肪代谢障碍的治疗
WO2012119046A2 (en) 2011-03-02 2012-09-07 Bioenergenix Heterocyclic compounds for the inhibition of pask
WO2012135570A1 (en) 2011-04-01 2012-10-04 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20140066369A1 (en) 2011-04-19 2014-03-06 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
US9051329B2 (en) 2011-07-05 2015-06-09 Merck Sharp & Dohme Corp. Tricyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors
HUE061596T2 (hu) 2011-07-15 2023-07-28 Boehringer Ingelheim Int Szubsztituált dimer kinazolin származék, annak elõállítása és alkalmazása az I. és II. típusú cukorbetegség kezelésére szolgáló gyógyszerkészítményekben
EA201490556A1 (ru) 2011-09-07 2014-08-29 Сановел Илач Санайи Ве Тиджарет Аноним Ширкети Составы ингибитора дпп-4
EP2572704A1 (en) 2011-09-22 2013-03-27 Sanovel Ilac Sanayi ve Ticaret A.S. Orally-Disintegrating Formulations of Vildagliptin
PL2578208T3 (pl) 2011-10-06 2014-10-31 Sanovel Ilac Sanayi Ve Ticaret As Stałe formulacje dawkowane inhibitora DPP-IV
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
ITMI20112224A1 (it) 2011-12-06 2013-06-07 Chemelectiva S R L Nuovo processo ed intermedi per la sintesi di vildagliptin
CN102491928A (zh) * 2011-12-13 2012-06-13 临海天宇药业有限公司 一种制备(2s)-n-氯乙酰基-2-氰基四氢吡咯的方法
US9115082B2 (en) 2012-01-18 2015-08-25 Catherine Yang Dipeptidyl-peptidase-IV inhibitors for treatment of type 2 diabetes complex with hypertension
US9073930B2 (en) 2012-02-17 2015-07-07 Merck Sharp & Dohme Dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
CN102617434B (zh) * 2012-03-29 2014-07-23 中国科学院上海有机化学研究所 一锅法制备维达列汀
WO2013179300A2 (en) * 2012-05-04 2013-12-05 Megafine Pharma (P) Ltd. A process for the preparation of vildagliptin and its intermediate thereof
ES2929025T3 (es) 2012-05-14 2022-11-24 Boehringer Ingelheim Int Linagliptina, un derivado de xantina como inhibidor de dpp-4, para su uso en el tratamiento del SRIS y/o de la septicemia
US20130303462A1 (en) 2012-05-14 2013-11-14 Boehringer Ingelheim International Gmbh Use of a dpp-4 inhibitor in podocytes related disorders and/or nephrotic syndrome
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
WO2014018350A1 (en) 2012-07-23 2014-01-30 Merck Sharp & Dohme Corp. Treating diabetes with dipeptidyl peptidase-iv inhibitors
WO2014020462A1 (en) * 2012-08-01 2014-02-06 Alembic Pharmaceuticals Limited Improved process for preparation of vildagliptin intermediate
WO2014052619A1 (en) 2012-09-27 2014-04-03 Irm Llc Piperidine derivatives and compositions as modulators of gpr119 activity
TWI500613B (zh) 2012-10-17 2015-09-21 Cadila Healthcare Ltd 新穎之雜環化合物
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
UY35144A (es) 2012-11-20 2014-06-30 Novartis Ag Miméticos lineales sintéticos de apelina para el tratamiento de insuficiencia cardiaca
CN103922986B (zh) * 2013-01-16 2017-02-15 上海彩迩文生化科技有限公司 维大列汀及其类似物、中间体及其制备方法和应用
JP6295277B2 (ja) 2013-02-14 2018-03-14 ノバルティス アーゲー Ｎｅｐ（中性エンドペプチダーゼ）阻害剤としての置換ビスフェニルブタン酸ホスホン酸誘導体
EP2988736A1 (en) 2013-04-22 2016-03-02 Cadila Healthcare Limited A novel composition for nonalcoholic fatty liver disease (nafld)
US20160107989A1 (en) 2013-05-30 2016-04-21 Cadila Healthcare Limited A process for preparation of pyrroles having hypolipidemic hypocholesteremic activities
CN103304502B (zh) * 2013-06-02 2015-03-04 张远强 一类抗糖尿病化合物、其制备方法和用途
TW201636015A (zh) 2013-07-05 2016-10-16 卡地拉保健有限公司 協同性組成物
TW201536814A (zh) 2013-07-25 2015-10-01 Novartis Ag 用於治療心臟衰竭之合成環狀多肽
PE20160991A1 (es) 2013-07-25 2016-10-15 Novartis Ag Bioconjugados de polipeptidos de apelina sintetica
IN2013MU02470A (enExample) 2013-07-25 2015-06-26 Cadila Healthcare Ltd
IN2013MU02905A (enExample) 2013-09-06 2015-07-03 Cadila Healthcare Ltd
WO2015068156A1 (en) 2013-11-05 2015-05-14 Ben-Gurion University Of The Negev Research And Development Authority Compounds for the treatment of diabetes and disease complications arising from same
CN103641761A (zh) * 2013-11-22 2014-03-19 沈阳化工大学 一种维格利汀的制备方法
EP3110449B1 (en) 2014-02-28 2023-06-28 Boehringer Ingelheim International GmbH Medical use of a dpp-4 inhibitor
WO2015132359A1 (en) 2014-03-06 2015-09-11 Sanovel Ilac Sanayi Ve Ticaret A.S. Vildagliptin formulation process under inert gas atmosphere
CN103992257B (zh) * 2014-05-16 2016-03-30 苏州天马精细化学品股份有限公司 一种维格列汀粗品的纯化方法
CN105439873A (zh) * 2014-08-20 2016-03-30 天津药物研究院 3-羟基-1-金刚烷胺的制备方法
GB201415598D0 (en) 2014-09-03 2014-10-15 Univ Birmingham Elavated Itercranial Pressure Treatment
CN105884669B (zh) * 2014-09-15 2020-05-15 深圳翰宇药业股份有限公司 制备取代的(s)-吡咯烷-2-甲腈及维格列汀的方法
PL3242666T3 (pl) 2015-01-06 2025-02-17 Arena Pharmaceuticals, Inc. Związek do zastosowania w leczeniu dolegliwości związanych z receptorem s1p1
CN104529857B (zh) * 2015-01-13 2016-03-30 佛山市赛维斯医药科技有限公司 卤代金刚烷酰胺类衍生物、其制备方法和用途
WO2016116842A1 (en) 2015-01-23 2016-07-28 Novartis Ag Synthetic apelin fatty acid conjugates with improved half-life
MX386778B (es) 2015-03-09 2025-03-19 Intekrin Therapeutics Inc Métodos para el tratamiento de enfermedad de hígado graso no alcohólico y/o lipodistrofia.
CN104761456B (zh) * 2015-03-10 2020-04-10 上海威智医药科技有限公司 3-氨基-1-金刚烷醇的制备方法
CN104817482B (zh) * 2015-03-17 2017-05-10 宁波百思佳医药科技有限公司 2‑取代吡咯烷类化合物、制备方法及其在制备维格列汀中的应用
HUE060476T2 (hu) 2015-06-22 2023-03-28 Arena Pharm Inc (R)-2-(7-(4-ciklopentil-3-(trifluormetil)benziloxi)-1,2,3,4- tetrahidrociklopenta[B]indol-3-il)ecetsav kristályos L-arginin-sója S1P1 receptorral kapcsolatos rendellenességek esetén való alkalmazásra
US10385017B2 (en) 2015-10-14 2019-08-20 Cadila Healthcare Limited Pyrrole compound, compositions and process for preparation thereof
KR20180092981A (ko) 2015-12-28 2018-08-20 욱크하르트 리미티드 빌다글립틴의 경구 삼투압성 약제학적 조성물
BR112018072401A2 (pt) 2016-06-10 2019-02-19 Boehringer Ingelheim International Gmbh combinações de linagliptina e metformina
DE102016116130A1 (de) 2016-08-30 2018-03-01 Universität Bielefeld Verfahren zur Herstellung chiraler Aminonitrile
PL3512505T3 (pl) 2016-09-16 2023-08-07 Galenicum Health S.L.U. Farmaceutyczne kompozycje wildagliptyny
JOP20190086A1 (ar) 2016-10-21 2019-04-18 Novartis Ag مشتقات نافثيريدينون جديدة واستخدامها في معالجة عدم انتظام ضربات القلب
WO2018104916A1 (en) 2016-12-09 2018-06-14 Cadila Healthcare Limited Treatment for primary biliary cholangitis
WO2018162722A1 (en) 2017-03-09 2018-09-13 Deutsches Institut Für Ernährungsforschung Potsdam-Rehbrücke Dpp-4 inhibitors for use in treating bone fractures
WO2018187350A1 (en) 2017-04-03 2018-10-11 Coherus Biosciences Inc. PPARγ AGONIST FOR TREATMENT OF PROGRESSIVE SUPRANUCLEAR PALSY
GR1009406B (el) 2017-10-03 2018-11-26 Φαρματεν Αβεε Φαρμακευτικο σκευασμα που περιλαμβανει βιλνταγλιπτινη και μεθοδος για την παρασκευη αυτου
EP3737361A4 (en) 2018-01-11 2021-08-25 Centaurus Therapeutics INHIBITORS OF DIHYDROCERAMIDE DESATURASE FOR THE TREATMENT OF DISEASES
UY38072A (es) 2018-02-07 2019-10-01 Novartis Ag Compuestos derivados de éster butanoico sustituido con bisfenilo como inhibidores de nep, composiciones y combinaciones de los mismos
KR102622198B1 (ko) 2018-03-30 2024-01-09 한미약품 주식회사 빌다글립틴을 함유하는 경구용 고형제제 및 그의 제조 방법
US12156866B2 (en) 2018-06-06 2024-12-03 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
GR1009644B (el) 2018-09-25 2019-11-12 Φαρματεν Α.Β.Ε.Ε. Φαρμακευτικο σκευασμα που περιλαμβανει βιλνταγλιπτινη και μετφορμινη και μεθοδος για την παρασκευη αυτου
UY38485A (es) 2018-11-27 2020-06-30 Novartis Ag Compuestos tetrámeros cíclicos como inhibidores de proproteína convertasa subtilisina/kexina tipo 9 (pcsk9), método de tratamiento, uso y su preparación
US20230089867A1 (en) 2018-11-27 2023-03-23 Novartis Ag Cyclic pentamer compounds as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorder
JP7657151B2 (ja) 2018-11-27 2025-04-04 ノバルティス アーゲー 代謝性障害の処置のためのプロタンパク質コンバターゼスブチリシン／ケキシン９型（ｐｃｓｋ９）阻害剤としての環状ペプチド
JP7461735B2 (ja) * 2019-12-02 2024-04-04 日本ジェネリック株式会社 ビルダグリプチン含有錠剤
CN113527167B (zh) * 2020-04-14 2024-01-19 威智医药股份有限公司 一种维格列汀的生产方法
WO2021234430A1 (en) 2020-05-17 2021-11-25 Lotus International Pte. Ltd. Modified release dosage form comprising vildagliptin and process for manufacturing the same
WO2022003405A1 (en) 2020-07-03 2022-01-06 Savoi Guilherme One-pot process to obtain a pyrrolidine-2-carbonitrile intermediate compound and industrial scale telescopic process to prepare (2s)-1-[n-(3-hydroxyadamantan-1-yl)glycyl]-2-pyrrolidinecarbonitrile (vildagliptin) using same
EP4192509A1 (en) 2020-08-05 2023-06-14 Ellipses Pharma Ltd Treatment of cancer using a cyclodextrin-containing polymer-topoisomerase inhibitor conjugate and a parp inhibitor
EP4281439A1 (en) * 2021-01-21 2023-11-29 The Scripps Research Institute Small molecule regulators of alveolar type 2 cell proliferation for the treatment of pulmonary diseases
TW202333563A (zh) 2021-11-12 2023-09-01 瑞士商諾華公司 用於治療疾病或障礙之二胺基環戊基吡啶衍生物
AR127698A1 (es) 2021-11-23 2024-02-21 Novartis Ag Derivados de naftiridinona para el tratamiento de una enfermedad o un trastorno
KR20260015867A (ko) 2023-05-24 2026-02-03 노파르티스 아게 질환 또는 장애 치료용 나프티리디논 유도체

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4977179A (en) * 1986-01-17 1990-12-11 Otsuka Pharmaceutical Factory, Inc. Proline derivatives
WO1998019998A2 (en) * 1996-11-07 1998-05-14 Novartis Ag N-substituted 2-cyanopyrrolidines

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE158109C (enExample) *
DE296075C (enExample) *
FR2572399B1 (fr) * 1984-10-31 1987-01-16 Panmedica Sa Nouveaux derives de l'adamantanamine, leurs procedes de preparation et medicaments les contenant
WO1990012005A1 (fr) * 1989-04-13 1990-10-18 Japan Tobacco Inc. Nouveaux derives aminoacides possedant une activite d'inhibiteur de la prolylendopeptidase
CA2080474A1 (en) * 1990-04-14 1991-10-15 William W. Bachovchin Inhibitors of dipeptidyl-aminopeptidase type iv
EP0610317B1 (en) * 1991-10-22 2001-01-31 New England Medical Center Hospitals, Inc. Inhibitors of dipeptidyl-aminopeptidase type iv
PH31294A (en) * 1992-02-13 1998-07-06 Thomae Gmbh Dr K Benzimidazolyl derivatives, pharmaceutical compositions containing these compounds and process for preparing them.
WO1995011689A1 (en) * 1993-10-29 1995-05-04 Trustees Of Tufts College Use of inhibitors of dipeptidyl-aminopeptidase to block entry of hiv into cells
WO1995013069A1 (en) * 1993-11-09 1995-05-18 Merck & Co., Inc. Piperidines, pyrrolidines and hexahydro-1h-azepines promote release of growth hormone
IL111785A0 (en) * 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
FR2719049B1 (fr) * 1994-04-22 1996-06-14 Pasteur Institut Multireprésentation d'un analogue peptidique du substrat de la DPPIV, notamment de type KPR, afin d'inhiber l'entrée du HIV dans les cellules.
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
AU8174398A (en) * 1997-06-27 1999-01-19 Penn State Research Foundation, The Agrobacterium-mediated transformation and efficient regeneration of cacao
EP1520582A3 (en) * 1998-02-02 2009-07-01 Trustees Of Tufts College Use of dipeptidylpetidase inhibitors to regulate glucose metabolism
JP2003190202A (ja) * 2001-12-28 2003-07-08 Yoshinobu Sekizawa 使い捨てカイロ目的別貼付位置及び禁止位置表示付き下着
JP2005528955A (ja) * 2002-06-08 2005-09-29 トムソン，イアン，ロバート 薬剤・健康増進剤投与装置

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4977179A (en) * 1986-01-17 1990-12-11 Otsuka Pharmaceutical Factory, Inc. Proline derivatives
WO1998019998A2 (en) * 1996-11-07 1998-05-14 Novartis Ag N-substituted 2-cyanopyrrolidines

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
J.Med Chem. 1996, 39, 2087-2094. *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2443687C2 (ru) * 2006-04-03 2012-02-27 Матрикс Лэборетериз Лтд. Новые ингибиторы дипептидилпептидазы iv, способы их получения и содержащие их фармацевтические композиции
RU2628573C2 (ru) * 2015-11-27 2017-08-21 Общество с ограниченной ответственностью "Аллель Центр Инновационных Биотехнологий" Ингибитор дипептидилпептидазы-4 для лечения сахарного диабета 2-го типа

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