CZ299151B6 - N-Substituované 2-kyanopyrrolidiny, farmaceutickýprostredek, který je obsahuje a jejich použití jako lécivo - Google Patents

N-Substituované 2-kyanopyrrolidiny, farmaceutickýprostredek, který je obsahuje a jejich použití jako lécivo Download PDF

Info

Publication number
CZ299151B6
CZ299151B6 CZ20012028A CZ20012028A CZ299151B6 CZ 299151 B6 CZ299151 B6 CZ 299151B6 CZ 20012028 A CZ20012028 A CZ 20012028A CZ 20012028 A CZ20012028 A CZ 20012028A CZ 299151 B6 CZ299151 B6 CZ 299151B6
Authority
CZ
Czechia
Prior art keywords
cyanopyrrolidine
amino
acetyl
adamantyl
pharmaceutically acceptable
Prior art date
Application number
CZ20012028A
Other languages
Czech (cs)
English (en)
Other versions
CZ20012028A3 (cs
Inventor
Bernard Villhauer@Edwin
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22777194&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CZ299151(B6) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of CZ20012028A3 publication Critical patent/CZ20012028A3/cs
Publication of CZ299151B6 publication Critical patent/CZ299151B6/cs

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/10Heterocyclic 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (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)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CZ20012028A 1998-12-10 1999-12-09 N-Substituované 2-kyanopyrrolidiny, farmaceutickýprostredek, který je obsahuje a jejich použití jako lécivo CZ299151B6 (cs)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US20906898A 1998-12-10 1998-12-10

Publications (2)

Publication Number Publication Date
CZ20012028A3 CZ20012028A3 (cs) 2001-09-12
CZ299151B6 true CZ299151B6 (cs) 2008-05-07

Family

ID=22777194

Family Applications (1)

Application Number Title Priority Date Filing Date
CZ20012028A CZ299151B6 (cs) 1998-12-10 1999-12-09 N-Substituované 2-kyanopyrrolidiny, farmaceutickýprostredek, který je obsahuje a jejich použití jako lécivo

Country Status (34)

Country Link
US (1) US6166063A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EP (1) EP1137635B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
JP (2) JP3681110B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
KR (2) KR100509311B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CN (1) CN1160330C (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AR (1) AR023719A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AT (1) ATE307112T1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
BR (1) BRPI9915985B8 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CA (1) CA2350609C (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CO (1) CO5150173A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CY (3) CY1105355T1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CZ (1) CZ299151B6 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
DE (3) DE69927844T2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
DK (1) DK1137635T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ES (1) ES2251847T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
FR (1) FR08C0005I2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
HK (1) HK1040394B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
HU (1) HU226769B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ID (1) ID28796A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IL (2) IL143091A0 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
LU (2) LU91409I2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MY (1) MY123244A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
NL (2) NL300333I2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
NO (3) NO318741B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
NZ (1) NZ511935A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
PE (1) PE20001317A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
PL (1) PL199443B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
RU (1) RU2251544C2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
SK (1) SK286635B6 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
TR (1) TR200101478T2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
TW (1) TW509674B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
UY (1) UY25843A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
WO (1) WO2000034241A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ZA (1) ZA200104581B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)

Families Citing this family (309)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6376549B1 (en) * 1998-09-17 2002-04-23 Akesis Pharmaceuticals, Inc. Metforimin-containing compositions for the treatment of diabetes
IL141967A0 (en) * 1998-09-17 2002-03-10 Akesis Pharm Inc Combinations of chromium or vanadium with antidiabetics for glucose metabolism disorders
DE19940130A1 (de) * 1999-08-24 2001-03-01 Probiodrug Ges Fuer Arzneim Neue Effektoren der Dipeptidyl Peptidase IV zur topischen Anwendung
EP1228061A4 (en) * 1999-11-12 2004-12-15 Guilford Pharm Inc DIPEPTIDYL PEPTIDASE IV INHIBITORS; METHODS OF MANUFACTURE AND USE OF SAID INHIBITORS
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
GB9928330D0 (en) * 1999-11-30 2000-01-26 Ferring Bv Novel antidiabetic agents
KR20100130651A (ko) * 1999-12-23 2010-12-13 노파르티스 아게 당 대사 장애를 치료하기 위한 혈당강하제의 용도
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
ES2433476T3 (es) 2000-01-21 2013-12-11 Novartis Ag Combinaciones que contienen inhibidores de la dipeptidilpeptidasa-IV y agentes 5 antidiabéticos
US20080076811A1 (en) * 2000-01-21 2008-03-27 Bork Balkan Combinations comprising depeptidypeptidase-iv inhibitors and antidiabetic agents
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
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
WO2002002560A2 (en) 2000-07-04 2002-01-10 Novo Nordisk A/S Purine-2,6-diones which are inhibitors of the enzyme dipeptidyl peptidase iv (dpp-iv)
US20060089389A1 (en) * 2000-08-22 2006-04-27 Malcolm Allison Combination
PE20020617A1 (es) * 2000-08-22 2002-08-05 Novartis Ag Composicion que comprende un antagonista del receptor at1 y un potenciador de la secrecion de insulina o un sensibilizante a la insulina
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
US20080249016A1 (en) * 2000-09-18 2008-10-09 Sanos Bioscience A/S Use of GLP-2 in a combination treatment for bone-related disorders
US20070135345A1 (en) * 2000-09-18 2007-06-14 Henriksen Dennis B Use of GLP-2 for the treatment or prevention, of bone-related disorders
WO2002022151A2 (en) 2000-09-18 2002-03-21 Osteometer Bio Tech A/S Use of glp-1 and flp-2 peptides for treatment of bone disorders
NZ524974A (en) * 2000-10-06 2005-10-28 Tanabe Seiyaku Co Aliphatic nitrogen-containing 5-membered ring compound
UA74023C2 (en) * 2000-11-10 2005-10-17 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
TWI243162B (en) * 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
US20040180925A1 (en) * 2000-12-27 2004-09-16 Kenji Matsuno Dipeptidylpeptidase-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
CA2450579A1 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
ATE318139T1 (de) 2001-06-20 2006-03-15 Merck & Co Inc Dipeptidylpeptidase-hemmer zur behandlung von diabetes
MXPA03011907A (es) * 2001-06-27 2004-03-26 Smithkline Beecham Corp Fluoropirrolidinas como inhibidores de dipeptidil peptidasa.
WO2003002530A2 (en) * 2001-06-27 2003-01-09 Smithkline Beecham Corporation Pyrrolidines as dipeptidyl peptidase inhibitors
JP4357293B2 (ja) 2001-06-27 2009-11-04 スミスクライン ビーチャム コーポレーション ジペプチジルペプチダーゼ阻害剤としてのフルオロピロリジン類
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
CA2464995A1 (en) * 2001-10-31 2003-05-08 Novartis Ag Methods to treat diabetes and related conditions based on polymorphisms in the tcf1 gene
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
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
MXPA04007744A (es) 2002-02-13 2004-10-15 Hoffmann La Roche Nuevos derivados de piridina y pirimidina.
EP1338595B1 (en) 2002-02-25 2006-05-03 Eisai Co., Ltd. Xanthine derivatives as DPP-IV inhibitors
EP1490335B1 (en) * 2002-03-25 2007-09-19 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
SI1513519T1 (sl) * 2002-06-03 2009-06-30 Novartis Ag Uporaba substituiranih cianopirolidinov za zdravljenje hiperlipidemije
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
EP1554256B1 (en) 2002-07-15 2009-12-09 Merck & Co., Inc. Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of 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
BR0314582A (pt) * 2002-09-19 2005-08-09 Abbott Laboratoires Composições farmacêuticas como inibidoras da dipeptidil peptidase - iv (dpp-iv)
DE60315687T2 (de) * 2002-10-07 2008-06-05 Merck & Co., Inc. Antidiabetische heterocyclische beta-aminoverbindungen als inhibitoren von dipeptidylpeptidase
AU2003298596B2 (en) * 2002-10-18 2008-12-18 Merck Sharp & Dohme Corp. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
JP4413863B2 (ja) 2002-11-07 2010-02-10 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チジルペプチダーゼ阻害剤としてのフェニルアラニン誘導体
AU2003297564A1 (en) * 2002-12-04 2004-06-23 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US20060052382A1 (en) * 2002-12-20 2006-03-09 Duffy Joseph L 3-Amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
GEP20084540B (en) 2003-01-14 2008-11-25 Arena Pharm Inc 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prpphylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
JP4564952B2 (ja) 2003-01-17 2010-10-20 メルク・シャープ・エンド・ドーム・コーポレイション 糖尿病の治療および予防のためのジペプチジルペプチダーゼ阻害薬としての3−アミノ−4−フェニルブタン酸誘導体
EP1592689A4 (en) * 2003-01-31 2008-12-24 Merck & Co Inc 3-AMINO-4-PHENYLBUTANOIC ACID DERIVATIVES AS INHIBITORS OF DIPEPTIDYL PEPTIDASE FOR THE TREATMENT OR PREVENTION OF DIABETES
KR20050122220A (ko) 2003-03-25 2005-12-28 다케다 샌디에고, 인코포레이티드 디펩티딜 펩티다제 억제제
PE20050021A1 (es) * 2003-04-16 2005-03-15 Novartis Ag Procedimiento para la preparacion de 2-cianopirrolidina n-sustituida
GB0308854D0 (en) * 2003-04-16 2003-05-21 Novartis Ag Organic compounds
CA2524531A1 (en) 2003-05-14 2004-12-02 Merck And Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004103993A1 (en) 2003-05-14 2004-12-02 Syrrx, Inc. Dipeptidyl peptidase inhibitors
WO2004110436A1 (en) * 2003-06-06 2004-12-23 Merck & Co., Inc. Fused indoles as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004112701A2 (en) * 2003-06-17 2004-12-29 Merck & Co., Inc. Cyclohexylglycine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
DE602004022294D1 (en) 2003-06-20 2009-09-10 Hoffmann La Roche Hexahydropyridoisochinoline als dpp-iv-inhibitoren
HRP20110018T1 (hr) 2003-06-20 2011-02-28 F. Hoffmann - La Roche Ag Derivati pirido(2,1-a)-izokinolina kao inhibitori dpp-iv
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
DE602004018503D1 (de) 2003-07-31 2009-01-29 Merck & Co Inc Hexahydrodiazepinone als inhibitoren des dipeptidylpeptidase-iv zur behandlung bzw. prävention von diabetes
US6995183B2 (en) 2003-08-01 2006-02-07 Bristol Myers Squibb Company Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods
US7678909B1 (en) 2003-08-13 2010-03-16 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
BRPI0413452A (pt) 2003-08-13 2006-10-17 Takeda Pharmaceutical composto, composição farmacêutica, kit, artigo de fabricação, e, métodos de inibir dpp-iv, terapêutico e de tratar um estado de doença, cáncer, distúrbios autoimunes, uma condição einfecção por hiv
US7169926B1 (en) 2003-08-13 2007-01-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
EP1699777B1 (en) 2003-09-08 2012-12-12 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
AR046330A1 (es) * 2003-09-09 2005-12-07 Japan Tobacco Inc Inhibidor de dipeptidilpeptidasa iv
WO2005033099A2 (en) * 2003-10-03 2005-04-14 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
CA2544573A1 (en) * 2003-11-03 2005-06-02 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
WO2005044195A2 (en) * 2003-11-04 2005-05-19 Merck & Co., Inc. Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
US7317109B2 (en) 2003-11-12 2008-01-08 Phenomix Corporation Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
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
NZ547752A (en) * 2003-11-12 2009-12-24 Phenomix Corp Heterocyclic boronic acid compounds for inhibiting dipeptidyl peptidase-IV
US7576121B2 (en) 2003-11-12 2009-08-18 Phenomix Corporation Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
RU2385723C2 (ru) * 2003-11-17 2010-04-10 Новартис Аг Применение ингибиторов дипептидилпептидазы iv
KR20170104639A (ko) * 2003-11-17 2017-09-15 노파르티스 아게 디펩티딜 펩티다제 ⅳ 억제제의 용도
SI3023095T1 (sl) * 2004-01-20 2018-09-28 Novartis Ag Formulacija in postopek za direktno stiskanje
SI1712547T1 (sl) * 2004-02-05 2012-04-30 Kyorin Seiyaku Kk Bicikloestrski derivat
EP1717225A4 (en) * 2004-02-18 2009-10-21 Kyorin Seiyaku Kk BICYCLIC AMIDE DERIVATIVES
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
BRPI0507905A (pt) * 2004-02-20 2007-07-10 Novartis Ag uso de compostos orgánicos
CA2557275C (en) * 2004-02-27 2012-06-05 Kyorin Pharmaceutical Co., Ltd. Bicyclo derivative
WO2005087235A1 (en) * 2004-03-09 2005-09-22 National Health Research Institutes Pyrrolidine compounds
US7732446B1 (en) 2004-03-11 2010-06-08 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
CN102134231B (zh) 2004-03-15 2020-08-04 武田药品工业株式会社 二肽基肽酶抑制剂
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
US7687492B2 (en) * 2004-05-04 2010-03-30 Merck Sharp & Dohme Corp. 1,2,4-Oxadiazole derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
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
WO2005118555A1 (en) 2004-06-04 2005-12-15 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7935723B2 (en) * 2004-06-04 2011-05-03 Novartis Pharma Ag Use of organic compounds
US7786163B2 (en) 2004-07-12 2010-08-31 Forest Laboratories Holdings Limited (BM) 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
PE20060652A1 (es) * 2004-08-27 2006-08-11 Novartis Ag Composiciones farmaceuticas de liberacion inmediata que comprenden granulos de fusion
MX2007004305A (es) 2004-10-12 2007-06-18 Glenmark Pharmaceuticals Sa Inhibidores novedosos de dipeptidil peptidasa iv, composiciones farmaceuticas que los contienen y procedimientos para su preparacion.
BRPI0518409A2 (pt) * 2004-10-25 2008-11-18 Novartis Ag combinaÇço de inibidor dpp-iv, antidiabÉtico ppar e metformina
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
US7411093B2 (en) * 2004-12-20 2008-08-12 Hoffman-La Roche Inc. Aminocycloalkanes as DPP-IV inhibitors
CA2590957A1 (en) 2004-12-20 2006-06-29 Markus Boehringer 4-aminopiperidine derivatives
EP2805953B1 (en) 2004-12-21 2016-03-09 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
EA200702208A1 (ru) * 2005-04-22 2008-04-28 Алантос Фармасьютиклз Холдинг, Инк. Ингибиторы дипептидилпептидазы-iv
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
MX2008000468A (es) * 2005-07-12 2008-03-11 Novartis Ag Combinacion de un inhibidor de dipeptidil-peptidasa-iv y un antagonista del receptor canabinoide cb1.
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
RU2008107873A (ru) * 2005-08-04 2009-09-10 Новартис АГ (CH) Новые соединения
GT200600381A (es) 2005-08-25 2007-03-28 Compuestos organicos
JP5027137B2 (ja) 2005-09-14 2012-09-19 武田薬品工業株式会社 ジペプチジルペプチダーゼ阻害剤の投与
CN102675221A (zh) 2005-09-16 2012-09-19 武田药品工业株式会社 用于制备嘧啶二酮衍生物的方法中的中间体
JOP20180109A1 (ar) * 2005-09-29 2019-01-30 Novartis Ag تركيبة جديدة
TW200738266A (en) * 2005-09-29 2007-10-16 Sankyo Co Pharmaceutical agent containing insulin resistance improving agent
WO2007041833A1 (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
AU2007224066B2 (en) * 2006-03-08 2011-10-27 Kyorin Pharmaceutical Co., Ltd. Method for producing aminoacetylpyrrolidinecarbonitrile derivative and production intermediate thereof
CA2646598C (en) 2006-03-21 2014-08-19 Amylin Pharmaceuticals, Inc. Peptide-peptidase inhibitor conjugates and methods of using same
WO2007112347A1 (en) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
DE602007012845D1 (de) * 2006-04-03 2011-04-14 Matrix Lab Ltd Neue dipeptidylpeptidase-iv-inhibitoren und verfahren zur ihrer herstellung und pharmazeutische zusammensetzung, die diese enthalten
MX2008012756A (es) * 2006-04-03 2009-03-05 Matrix Lab Ltd Inhibidores de dipeptidil peptidasa iv novedosos y procesos para su preparacion y composiciones farmaceuticas que los contienen.
KR101281962B1 (ko) 2006-04-11 2013-07-08 아레나 파마슈티칼스, 인크. 특정 개체에게서 골 질량을 증가시키는 데에 유용한 화합물을 확인하기 위해 gpr119 수용체를 사용하는 방법
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
PE20110235A1 (es) 2006-05-04 2011-04-14 Boehringer Ingelheim Int Combinaciones farmaceuticas que comprenden linagliptina y metmorfina
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
BRPI0711558A2 (pt) 2006-05-04 2011-11-08 Boeringer Ingelheim Internat Gmbh polimorfos
CN101454342A (zh) 2006-05-26 2009-06-10 安米林药品公司 用于治疗充血性心力衰竭的组合物及方法
NZ574710A (en) 2006-09-07 2012-02-24 Nycomed Gmbh Combination treatment comprising the PDE4 inhibitor Compound A ((2R,4aR, 10bR)6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1 ,2,3,4,4a,10b-hexahydrophenanthridin-2-ol) for diabetes mellitus
GEP20125701B (en) * 2006-09-13 2012-12-10 Takeda Pharmaceuticals Co Application of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-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
US20080167479A1 (en) * 2007-01-10 2008-07-10 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
US8143427B2 (en) * 2007-03-22 2012-03-27 Kyorin Pharmaceutical Co., Ltd. Method for producing aminoacetylpyrrolidinecarbonitrile derivative
KR20120030570A (ko) 2007-04-03 2012-03-28 미쓰비시 타나베 파마 코퍼레이션 디펩티딜 펩티다아제 4 저해 화합물과 감미료와의 병용
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
DK2152663T3 (da) 2007-06-04 2014-06-23 Univ Ben Gurion Tri-aryl-forbindelser og sammensætninger, der omfatter dem
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.
JP5769966B2 (ja) * 2007-08-17 2015-08-26 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Fab関連疾患治療用プリン誘導体
US8338450B2 (en) * 2007-09-21 2012-12-25 Lupin Limited Compounds as dipeptidyl peptidase IV (DPP IV) inhibitors
US20090082420A1 (en) * 2007-09-25 2009-03-26 Protia, Llc Deuterium-enriched vildagliptin
US8598314B2 (en) * 2007-09-27 2013-12-03 Amylin Pharmaceuticals, Llc Peptide-peptidase-inhibitor conjugates and methods of making and using same
JP5401465B2 (ja) * 2007-11-30 2014-01-29 ノバルティス アーゲー 有機化合物
MX2010006110A (es) * 2007-12-12 2010-06-25 Astrazeneca Ab Peptidil-nitrilos y usos de los mismos como inhibidores de la dipeptidil-peptidasa i.
CA2710109C (en) 2007-12-21 2016-07-19 Lg Life Sciences Ltd. Dipeptidyl peptidase-iv inhibiting compounds, methods of preparing the same, and pharmaceutical compositions containing the same as active agent
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
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
KR20200118243A (ko) 2008-08-06 2020-10-14 베링거 인겔하임 인터내셔날 게엠베하 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료
EP2322499A4 (en) * 2008-08-07 2011-12-21 Kyorin Seiyaku Kk PROCESS FOR PREPARING A BICYCLO [2,2,2] OCTYLAMINE DERIVATIVE
EP2327406A4 (en) * 2008-08-14 2014-04-09 Kyorin Seiyaku Kk STABILIZED PHARMACEUTICAL COMPOSITION
EA031225B1 (ru) * 2008-08-15 2018-12-28 Бёрингер Ингельхайм Интернациональ Гмбх Ингибиторы дпп-4 для заживления ран
CZ2008512A3 (cs) * 2008-08-26 2010-03-10 Zentiva, A. S Zpusob prípravy vysoce cistého vildagliptinu
US8513264B2 (en) 2008-09-10 2013-08-20 Boehringer Ingelheim International Gmbh Combination therapy for the treatment of diabetes and related conditions
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
AU2009331471B2 (en) 2008-12-23 2015-09-03 Boehringer Ingelheim International Gmbh Salt forms of organic compound
TW201036975A (en) 2009-01-07 2010-10-16 Boehringer Ingelheim Int Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy
CN105384726A (zh) 2009-01-09 2016-03-09 幽兰化学医药有限公司 二肽基肽酶iv抑制剂
AR075204A1 (es) 2009-01-29 2011-03-16 Boehringer Ingelheim Int Inhibidores de dpp-4 y composiciones farmaceuticas que los comprenden, utiles para tratar enfermedades metabolicas en pacientes pediatricos, particularmente diabetes mellitus tipo 2
CN102387795A (zh) 2009-02-13 2012-03-21 贝林格尔.英格海姆国际有限公司 包含dpp-4抑制剂(利拉列汀)任选地组合其它抗糖尿病药的抗糖尿病药物
KR101694136B1 (ko) 2009-02-13 2017-01-09 베링거 인겔하임 인터내셔날 게엠베하 Sglt2 억제제, dpp-iv 억제제 및 임의로 추가의 당뇨병 치료제를 포함하는 약제학적 조성물 및 이의 용도
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
JP2012526093A (ja) 2009-05-07 2012-10-25 アストラゼネカ・アクチエボラーグ 置換1−シアノエチルヘテロシクリルカルボキサミド化合物750
PL2429995T3 (pl) 2009-05-15 2014-07-31 Novartis Ag Arylopirydyny jako inhibitory syntazy aldosteronu
ES2430088T3 (es) 2009-05-15 2013-11-18 Novartis Ag Derivados de benzoxazolona como inhibidores de aldosterona sintasa
KR20120041702A (ko) 2009-05-28 2012-05-02 노파르티스 아게 네프릴리신 억제제로서의 치환된 아미노부티르산 유도체
SG176009A1 (en) 2009-05-28 2011-12-29 Novartis Ag Substituted aminopropionic derivatives as neprilysin inhibitors
US8748457B2 (en) 2009-06-18 2014-06-10 Lupin Limited 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
EP2459531B1 (en) * 2009-07-31 2019-09-11 KRKA, D.D., Novo Mesto Granulate comprising vildagliptin and process for its preparation
EP2473047B1 (en) 2009-09-02 2014-08-13 Merck Sharp & Dohme Corp. Aminotetrahydropyrans as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
NZ598294A (en) 2009-09-03 2013-07-26 Bioenergenix Heterocyclic compounds for the inhibition of pask
EP2295083A1 (de) 2009-09-15 2011-03-16 Ratiopharm GmbH Pharmazeutische Zusammensetzung mit den Wirkstoffen Metformin und Sitagliptin oder Vildagliptin
JP5855568B2 (ja) 2009-09-15 2016-02-09 セルリアン・ファーマ・インコーポレイテッド 癌の治療法
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
JP2013507366A (ja) 2009-10-09 2013-03-04 アイアールエム・リミテッド・ライアビリティ・カンパニー Gpr119活性モジュレーターとしての化合物および組成物
JP5654608B2 (ja) 2009-11-17 2015-01-14 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−ピリジン誘導体
JO2967B1 (en) 2009-11-20 2016-03-15 نوفارتس ايه جي Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors
MX2012005987A (es) 2009-11-23 2012-06-25 Cerulean Pharma Inc Polimeros a base de ciclodextrina para administracion terapeutica.
KR20240090632A (ko) 2009-11-27 2024-06-21 베링거 인겔하임 인터내셔날 게엠베하 리나글립틴과 같은 dpp-iv 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료
JP5575913B2 (ja) 2009-11-30 2014-08-20 ノバルティス アーゲー アルドステロン合成酵素阻害剤としてのイミダゾール誘導体
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
US8853212B2 (en) 2010-02-22 2014-10-07 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
US20130109703A1 (en) 2010-03-18 2013-05-02 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
CA2795513A1 (en) 2010-04-06 2011-10-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
PH12012502162A1 (en) 2010-05-05 2013-02-04 Boehringer Ingelheim Int Combination therapy
WO2011146358A1 (en) 2010-05-21 2011-11-24 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
WO2011161161A1 (en) 2010-06-24 2011-12-29 Boehringer Ingelheim International Gmbh Diabetes therapy
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
KR101519280B1 (ko) 2010-08-09 2015-05-11 시오노기세이야쿠가부시키가이샤 아미노아다만탄카르바메이트 유도체의 제조 방법
HU231050B1 (hu) 2010-08-19 2020-02-28 Egis Gyógyszergyár Nyrt. Eljárás gyógyszerhatóanyag előállítására
BR112013008100A2 (pt) 2010-09-22 2016-08-09 Arena Pharm Inc "moduladores do receptor de gpr19 e o tratamento de distúrbios relacionados a eles."
US9034883B2 (en) 2010-11-15 2015-05-19 Boehringer Ingelheim International Gmbh Vasoprotective and cardioprotective antidiabetic therapy
US8673974B2 (en) 2010-11-16 2014-03-18 Novartis Ag Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors
US8877815B2 (en) 2010-11-16 2014-11-04 Novartis Ag Substituted carbamoylcycloalkyl acetic acid derivatives as NEP
TR201010683A1 (tr) 2010-12-21 2012-07-23 Sanovel İlaç San. Ve Ti̇c. A.Ş. Vildagliptin formülasyonları.
TR201101809A1 (tr) 2010-12-21 2012-07-23 Sanovel İlaç Sanayi̇ Ve Ti̇caret Anoni̇m Şi̇rketi̇ Vildagliptin ve glimepirid kombinasyonları.
EP2468268B1 (en) 2010-12-21 2017-12-13 Sanovel Ilaç Sanayi Ve Ticaret Anonim Sirketi Combination composition of vildagliptin and gliclazide
TR201107482A1 (tr) 2010-12-21 2012-07-23 Sanovel İlaç San.Ve Ti̇c.A.Ş. Vildagliptin ve gliklazidin iki tabakalı kombinasyon kompozisyonu.
WO2012104869A1 (en) 2011-01-31 2012-08-09 Cadila Healthcare Limited Treatment for lipodystrophy
CN103459382B (zh) 2011-03-02 2016-06-29 拜奥埃内杰尼克斯公司 用于抑制pask的杂环化合物
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
US20140051714A1 (en) 2011-04-22 2014-02-20 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2012145603A1 (en) 2011-04-22 2012-10-26 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
EP2729468A4 (en) 2011-07-05 2015-03-18 Merck Sharp & Dohme Tricyclic heterocycles useful as dipeptidyl peptidase-iv inhibitors
DK3517539T3 (en) 2011-07-15 2023-01-16 Boehringer Ingelheim Int Farmaceutiske sammensætninger til behandling af type i og type ii diabetes
WO2013036213A1 (en) 2011-09-07 2013-03-14 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi Dpp-iv inhibitor formulations
EP2572704A1 (en) 2011-09-22 2013-03-27 Sanovel Ilac Sanayi ve Ticaret A.S. Orally-Disintegrating Formulations of Vildagliptin
ES2487271T3 (es) 2011-10-06 2014-08-20 Sanovel Ilac Sanayi Ve Ticaret A.S. Formulaciones de dosificación sólidas inhibidoras de 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
WO2013171166A1 (en) 2012-05-14 2013-11-21 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp-4 inhibitor for use in the treatment of sirs and/or sepsis
EP3685839A1 (en) 2012-05-14 2020-07-29 Boehringer Ingelheim International GmbH Linagliptin for use in the treatment of albuminuria and kidney related diseases
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
KR20150119109A (ko) 2013-02-14 2015-10-23 노파르티스 아게 Nep (중성 엔도펩티다제) 억제제로서의 치환된 비스페닐 부타노익 포스폰산 유도체
UA114360C2 (uk) 2013-04-22 2017-05-25 Каділа Хелткере Лімітед Спосіб лікування та/або зменшення інтенсивності неалкогольної жирової хвороби печінки (нжхп)
WO2014195967A2 (en) 2013-05-30 2014-12-11 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
TW201513857A (zh) 2013-07-05 2015-04-16 Cadila Healthcare Ltd 協同性組成物
US9266925B2 (en) 2013-07-25 2016-02-23 Novartis Ag Cyclic polypeptides for the treatment of heart failure
KR20160031552A (ko) 2013-07-25 2016-03-22 노파르티스 아게 합성 아펠린 폴리펩티드의 생체접합체
IN2013MU02470A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2013-07-25 2015-06-26 Cadila Healthcare Ltd
WO2015033357A2 (en) 2013-09-06 2015-03-12 Cadila Healthcare Limited An improved process for the preparation of pyrrole derivatives
AU2014347668A1 (en) 2013-11-05 2016-05-19 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
US9526728B2 (en) 2014-02-28 2016-12-27 Boehringer Ingelheim International Gmbh Medical use of a DPP-4 inhibitor
US20170014380A1 (en) 2014-03-06 2017-01-19 Sanovell IIac Sanayi Ve Ticaret Anonim Sirketi 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
JP6895378B2 (ja) 2015-01-06 2021-06-30 アリーナ ファーマシューティカルズ, インコーポレイテッド S1p1受容体に関連する状態の処置方法
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
CN107406490A (zh) 2015-01-23 2017-11-28 诺华股份有限公司 具有改善的半衰期的合成apelin脂肪酸缀合物
BR112017019170A2 (pt) 2015-03-09 2018-07-10 Intekrin Therapeutics, Inc. métodos para o tratamento de doença do fígado gorduroso não alcoólico e / ou 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
CA3002551A1 (en) 2015-06-22 2016-12-29 Arena Pharmaceuticals, Inc. Crystalline l-arginine salt of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid(com pound 1)for use in s1p1 receptor-associated disorders
US10385017B2 (en) 2015-10-14 2019-08-20 Cadila Healthcare Limited Pyrrole compound, compositions and process for preparation thereof
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
MX2018007681A (es) 2015-12-28 2018-11-14 Wockhardt Ltd Composicion farmaceutica osmotica oral de vildagliptin.
EP3468562A1 (en) 2016-06-10 2019-04-17 Boehringer Ingelheim International GmbH Combinations of linagliptin and metformin
DE102016116130A1 (de) 2016-08-30 2018-03-01 Universität Bielefeld Verfahren zur Herstellung chiraler Aminonitrile
EP3512505B1 (en) 2016-09-16 2023-03-15 Galenicum Health S.L.U. Vildagliptin pharmaceutical compositions
JOP20190086A1 (ar) 2016-10-21 2019-04-18 Novartis Ag مشتقات نافثيريدينون جديدة واستخدامها في معالجة عدم انتظام ضربات القلب
US20180243263A1 (en) 2016-12-09 2018-08-30 Cadila Healthcare Ltd. 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
AU2018249822A1 (en) 2017-04-03 2019-10-31 Coherus Biosciences Inc. PPArgamma 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
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
ES2987794T3 (es) 2018-06-06 2024-11-18 Arena Pharm Inc Procedimientos de tratamiento de afecciones relacionadas con el receptor S1P1
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
EP3887363A1 (en) 2018-11-27 2021-10-06 Novartis AG Cyclic pentamer compounds as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorder
WO2020110011A1 (en) 2018-11-27 2020-06-04 Novartis Ag Cyclic peptides as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorders
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
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
US20230285576A1 (en) 2020-08-05 2023-09-14 Ellipses Pharma Ltd Treatment of cancer using a cyclodextrin-containing polymer-topoisomerase inhibitor conjugate and a parp inhibitor
JP2024504328A (ja) * 2021-01-21 2024-01-31 ザ スクリプス リサーチ インスティテュート 肺疾患の治療のための肺胞2型細胞増殖の小分子調節因子
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
WO2024241229A1 (en) 2023-05-24 2024-11-28 Novartis Ag Naphthyridinone derivatives for the treatment of a disease or disorder

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995015309A1 (en) * 1993-12-03 1995-06-08 Ferring B.V. Dp-iv-serine protease inhibitors
WO1999000008A1 (en) * 1997-06-27 1999-01-07 The Penn State Research Foundation Agrobacterium-mediated transformation and efficient regeneration of cacao

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE296075C (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) *
DE158109C (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) *
FR2572399B1 (fr) * 1984-10-31 1987-01-16 Panmedica Sa Nouveaux derives de l'adamantanamine, leurs procedes de preparation et medicaments les contenant
JPH0662671B2 (ja) * 1986-01-17 1994-08-17 株式会社大塚製薬工場 プロリン誘導体
WO1990012005A1 (en) * 1989-04-13 1990-10-18 Japan Tobacco Inc. New amino acid derivatives having prolylendopeptidase inhibitor activity
EP0528858B1 (en) * 1990-04-14 1997-01-22 New England Medical Center Hospitals, Inc. 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
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
CZ134296A3 (en) * 1993-11-09 1996-12-11 Merck & Co Inc Piperidine, pyrrolidine and hexahydro-1h-azepine derivatives, process of their preparation and pharmaceutical compositions containing thereof
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
US6090786A (en) * 1994-06-10 2000-07-18 Fondatech Benelux N.V. Serine proteases, their activity and their synthetic inhibitors
TW492957B (en) * 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
EP2574336A1 (en) * 1998-02-02 2013-04-03 Trustees Of Tufts College Use of dipeptidylpeptidase 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
EP1511449A2 (en) * 2002-06-08 2005-03-09 Ian Robert Thomson Delivery system for a medicament or well-being enhancing composition

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995015309A1 (en) * 1993-12-03 1995-06-08 Ferring B.V. Dp-iv-serine protease inhibitors
WO1999000008A1 (en) * 1997-06-27 1999-01-07 The Penn State Research Foundation Agrobacterium-mediated transformation and efficient regeneration of cacao

Also Published As

Publication number Publication date
KR20050047561A (ko) 2005-05-20
JP3681110B2 (ja) 2005-08-10
DE69927844D1 (de) 2006-03-02
CA2350609C (en) 2008-09-02
ATE307112T1 (de) 2005-11-15
DE122008000017I1 (de) 2008-08-07
SK7892001A3 (en) 2001-11-06
CY2008011I2 (el) 2012-01-25
UY25843A1 (es) 2001-08-27
NO20012853L (no) 2001-08-07
CN1160330C (zh) 2004-08-04
HUP0104495A3 (en) 2002-11-28
NL300345I1 (nl) 2008-07-01
TW509674B (en) 2002-11-11
NO318741B1 (no) 2005-05-02
NL300333I1 (nl) 2008-03-03
AU759773B2 (en) 2003-05-01
NL300333I2 (nl) 2008-05-01
ES2251847T3 (es) 2006-05-01
LU91409I9 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2019-01-02
AR023719A1 (es) 2002-09-04
FR08C0005I1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2008-03-21
DE122008000007I1 (de) 2008-04-17
DE69927844T2 (de) 2006-07-27
SK286635B6 (sk) 2009-02-05
PE20001317A1 (es) 2000-12-13
WO2000034241A1 (en) 2000-06-15
HUP0104495A2 (hu) 2002-04-29
ID28796A (id) 2001-07-05
EP1137635B1 (en) 2005-10-19
JP2002531547A (ja) 2002-09-24
LU91409I2 (fr) 2008-03-17
PL199443B1 (pl) 2008-09-30
FR08C0005I2 (fr) 2009-01-15
MY123244A (en) 2006-05-31
JP2005112864A (ja) 2005-04-28
NO2008001I1 (no) 2008-02-18
US6166063A (en) 2000-12-26
ZA200104581B (en) 2002-05-22
KR20010080740A (ko) 2001-08-22
BRPI9915985B8 (pt) 2021-05-25
EP1137635A1 (en) 2001-10-04
LU91435I2 (fr) 2008-07-09
NO2008001I2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2010-09-27
PL348043A1 (en) 2002-05-06
CY1105355T1 (el) 2010-03-03
BR9915985A (pt) 2001-09-04
NZ511935A (en) 2003-11-28
TR200101478T2 (tr) 2001-10-22
AU1658000A (en) 2000-06-26
CN1329593A (zh) 2002-01-02
CO5150173A1 (es) 2002-04-29
NO20012853D0 (no) 2001-06-08
RU2251544C2 (ru) 2005-05-10
CA2350609A1 (en) 2000-06-15
HU226769B1 (en) 2009-09-28
BR9915985B1 (pt) 2014-03-18
IL143091A0 (en) 2002-04-21
HK1040394B (en) 2006-09-15
KR100509311B1 (ko) 2005-08-23
CY2008002I2 (el) 2009-11-04
CY2008002I1 (el) 2009-11-04
HK1040394A1 (en) 2002-06-07
IL143091A (en) 2006-07-05
CZ20012028A3 (cs) 2001-09-12
DK1137635T3 (da) 2006-02-13
NO2008004I1 (no) 2008-06-02
CY2008011I1 (el) 2012-01-25

Similar Documents

Publication Publication Date Title
CZ299151B6 (cs) N-Substituované 2-kyanopyrrolidiny, farmaceutickýprostredek, který je obsahuje a jejich použití jako lécivo
JP3217380B2 (ja) N―置換2―シアノピロリジン
US6946480B2 (en) Glutaminyl based DPIV inhibitors
US6617340B1 (en) N-(substituted glycyl)-pyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
MXPA05005260A (es) Amidas ciclicas fluoradas que inhiben la dipeptidil peptidasa iv.
CZ120398A3 (cs) Použití 2-alkylpyrrolidinových derivátů pro přípravu léčiva pro léčbu diabetu, 2-alkylpyrrolidiné deriváty
MXPA04011958A (es) Amidas ciclicas fluoradas como inhibidores de la dipeptidil peptidasa iv.
JP2009190971A (ja) 2−シアノピロリジン誘導体
MXPA06012521A (es) Derivado de pirrolidina.
MXPA01005817A (en) N-substituted 2-cyanopyrrolidines
MXPA99004281A (en) N-substituted 2-cyanopyrrolidines
HK1022149B (en) N-substituted 2-cyanopyrrolidines

Legal Events

Date Code Title Description
MK4A Patent expired

Effective date: 20220928