CN1310915C - 作为DPP-IV抑制剂的吡啶并(2,1-a)异喹啉衍生物 - Google Patents

作为DPP-IV抑制剂的吡啶并(2,1-a)异喹啉衍生物 Download PDF

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Publication number
CN1310915C
CN1310915C CNB02826360XA CN02826360A CN1310915C CN 1310915 C CN1310915 C CN 1310915C CN B02826360X A CNB02826360X A CN B02826360XA CN 02826360 A CN02826360 A CN 02826360A CN 1310915 C CN1310915 C CN 1310915C
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China
Prior art keywords
pyrido
dimethoxy
rac
hydrogen
isoquinoline
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
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CNB02826360XA
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English (en)
Chinese (zh)
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CN1639162A (zh
Inventor
罗卡·克劳蒂安·戈比
托马斯·吕贝斯
帕特里奥·马太
罗伯特·纳尔基齐昂
皮尔·查尔斯·维斯
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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Publication of CN1639162A publication Critical patent/CN1639162A/zh
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Anticipated expiration legal-status Critical
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D455/00—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/03—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/04—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine
    • C07D455/06—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CNB02826360XA 2001-12-27 2002-12-20 作为DPP-IV抑制剂的吡啶并(2,1-a)异喹啉衍生物 Expired - Fee Related CN1310915C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP01130882 2001-12-27
EP01130882.2 2001-12-27

Publications (2)

Publication Number Publication Date
CN1639162A CN1639162A (zh) 2005-07-13
CN1310915C true CN1310915C (zh) 2007-04-18

Family

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Family Applications (1)

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CNB02826360XA Expired - Fee Related CN1310915C (zh) 2001-12-27 2002-12-20 作为DPP-IV抑制剂的吡啶并(2,1-a)异喹啉衍生物

Country Status (27)

Country Link
US (2) US6727261B2 (cg-RX-API-DMAC10.html)
EP (1) EP1461337B1 (cg-RX-API-DMAC10.html)
JP (1) JP4197650B2 (cg-RX-API-DMAC10.html)
KR (1) KR100608428B1 (cg-RX-API-DMAC10.html)
CN (1) CN1310915C (cg-RX-API-DMAC10.html)
AR (1) AR037983A1 (cg-RX-API-DMAC10.html)
AT (1) ATE445615T1 (cg-RX-API-DMAC10.html)
AU (1) AU2002360074B2 (cg-RX-API-DMAC10.html)
BR (1) BR0215396A (cg-RX-API-DMAC10.html)
CA (1) CA2471262C (cg-RX-API-DMAC10.html)
DE (1) DE60234050D1 (cg-RX-API-DMAC10.html)
ES (1) ES2331354T3 (cg-RX-API-DMAC10.html)
GT (1) GT200200286A (cg-RX-API-DMAC10.html)
HR (1) HRP20040556A2 (cg-RX-API-DMAC10.html)
HU (1) HUP0600068A3 (cg-RX-API-DMAC10.html)
IL (2) IL162516A0 (cg-RX-API-DMAC10.html)
MX (1) MXPA04006241A (cg-RX-API-DMAC10.html)
NO (1) NO20043174L (cg-RX-API-DMAC10.html)
NZ (1) NZ533629A (cg-RX-API-DMAC10.html)
PA (1) PA8562801A1 (cg-RX-API-DMAC10.html)
PE (1) PE20030746A1 (cg-RX-API-DMAC10.html)
PL (1) PL371185A1 (cg-RX-API-DMAC10.html)
RU (1) RU2297417C2 (cg-RX-API-DMAC10.html)
TW (1) TWI265163B (cg-RX-API-DMAC10.html)
UY (1) UY27605A1 (cg-RX-API-DMAC10.html)
WO (1) WO2003055881A1 (cg-RX-API-DMAC10.html)
ZA (1) ZA200404926B (cg-RX-API-DMAC10.html)

Families Citing this family (109)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI1953162T1 (sl) * 2001-02-24 2012-09-28 Boehringer Ingelheim Pharma Ksantinski derivati, njihova priprava in njihova uporaba kot zdravila
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
US20040242568A1 (en) * 2003-03-25 2004-12-02 Syrrx, Inc. Dipeptidyl peptidase inhibitors
EP1620091B1 (en) 2003-05-05 2010-03-31 Probiodrug AG Inhibitors of glutaminyl cyclase
JP2007511467A (ja) 2003-05-14 2007-05-10 タケダ サン ディエゴ インコーポレイテッド ジペプチジルペプチダーゼインヒビター
MXPA05013904A (es) * 2003-06-20 2006-02-24 Hoffmann La Roche Derivados de pirido[2,1-a] isoquinolinas como inhibidores de dipeptidil-peptidasa iv(dpp-iv).
ATE437876T1 (de) * 2003-06-20 2009-08-15 Hoffmann La Roche Hexahydropyridoisochinoline als dpp-iv- inhibitoren
US7678909B1 (en) 2003-08-13 2010-03-16 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
MXPA06001601A (es) 2003-08-13 2006-08-25 Takeda Pharmaceutical Derivados de 4-pirimidona y su uso como inhibidores de dipeptidilpeptidasa.
US7169926B1 (en) 2003-08-13 2007-01-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2005026148A1 (en) 2003-09-08 2005-03-24 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
US20050065144A1 (en) * 2003-09-08 2005-03-24 Syrrx, Inc. Dipeptidyl peptidase inhibitors
AU2004290499C1 (en) 2003-11-03 2011-02-24 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
WO2005075436A2 (en) 2004-02-05 2005-08-18 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
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
US7732446B1 (en) 2004-03-11 2010-06-08 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
CN102079743B (zh) 2004-03-15 2020-08-25 武田药品工业株式会社 二肽基肽酶抑制剂
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
US7687638B2 (en) 2004-06-04 2010-03-30 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
WO2006019965A2 (en) 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
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
CN101107247B (zh) * 2004-11-30 2011-10-19 霍夫曼-拉罗奇有限公司 作为用于治疗糖尿病的dpp-iv抑制剂的取代的苯并喹嗪衍生物
BRPI0519585A2 (pt) * 2004-12-20 2009-02-25 Hoffmann La Roche compostos de fàrmula i; processo para a fabricaÇço de compostos de fàrmula i; composiÇÕes farmacÊuticas; mÉtodo para o tratamento e/ou profilaxia de doenÇas que estço associadas com a dpp-iv e usos destes compostos
JP2008524331A (ja) 2004-12-21 2008-07-10 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
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
DE602006017997D1 (de) 2005-04-26 2010-12-16 Mitsubishi Tanabe Pharma Corp Prophylaktisches/therapeutisches mittel für abweichungen im fettstoffwechsel
MY152185A (en) 2005-06-10 2014-08-29 Novartis Ag Modified release 1-[(3-hydroxy-adamant-1-ylamino)-acetyl]-pyrrolidine-2(s)-carbonitrile formulation
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
WO2007017423A2 (en) * 2005-08-11 2007-02-15 F. Hoffmann-La Roche Ag Pharmaceutical composition comprising a dpp-iv inhibitor
GEP20135791B (en) * 2005-09-14 2013-03-25 Takeda Pharmaceutical Use of dipeptidyl peptidase inhibitors
NZ566799A (en) * 2005-09-14 2011-04-29 Takeda Pharmaceutical Dipeptidyl peptidase inhibitors for treating diabetes
TW200745080A (en) * 2005-09-16 2007-12-16 Takeda Pharmaceuticals Co Polymorphs of tartrate salt of 2-[2-(3-(R)-amino-piperidin-1-yl)-5-fluoro-6-oxo-6H-pyrimidin-1-ylmethyl]-benzonitrile and methods of use therefor
TW200745079A (en) * 2005-09-16 2007-12-16 Takeda Pharmaceuticals Co Polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and methods of use therefor
WO2007035629A2 (en) 2005-09-16 2007-03-29 Takeda Pharmaceutical Company Limited Process for the preparation of pyrimidinedione derivatives
GB0526291D0 (en) 2005-12-23 2006-02-01 Prosidion Ltd Therapeutic method
WO2007112347A1 (en) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
EP1999108A1 (en) * 2006-03-28 2008-12-10 Takeda Pharmaceutical Company Limited Preparation of (r)-3-aminopiperidine dihydrochloride
NZ571110A (en) * 2006-04-11 2011-03-31 Arena Pharm Inc Methods of using GPR119 receptor to identify Glucose-dependent Insulinotropic Peptide (GIP) secretagogue compounds useful for increasing bone mass in an individual
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
AU2007235876A1 (en) 2006-04-12 2007-10-18 Probiodrug Ag Enzyme inhibitors
PE20080251A1 (es) * 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
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
WO2007140191A2 (en) 2006-05-23 2007-12-06 Theracos, Inc. Glucose transport inhibitors and methods of use
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
WO2008031750A2 (en) * 2006-09-15 2008-03-20 F. Hoffmann-La Roche Ag Process for the preparation of pyrido[2,1-a]isoquinoline derivatives by catalytic asymmetric hydrogenation of an enamine
EP2066667B1 (en) * 2006-09-15 2011-08-31 F. Hoffmann-La Roche AG Process for the preparation of pyrido[2,1-a]isoquinoline derivatives comprising optical resolution of an enamine
US8278345B2 (en) 2006-11-09 2012-10-02 Probiodrug Ag Inhibitors of glutaminyl cyclase
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
ATE554085T1 (de) 2006-11-30 2012-05-15 Probiodrug Ag Neue inhibitoren von glutaminylcyclase
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
WO2008128985A1 (en) 2007-04-18 2008-10-30 Probiodrug Ag Thiourea derivatives as glutaminyl cyclase inhibitors
NZ600126A (en) * 2007-08-17 2013-12-20 Boehringer Ingelheim Int Purine derivatives for use in the treatment of fap-related diseases
AU2008288770B2 (en) 2007-08-23 2014-06-12 Theracosbio, Llc Benzylbenzene derivatives and methods of use
US20090163718A1 (en) * 2007-12-19 2009-06-25 Stefan Abrecht PROCESS FOR THE PREPARATION OF PYRIDO[2,1-a] ISOQUINOLINE DERIVATIVES
PE20140960A1 (es) 2008-04-03 2014-08-15 Boehringer Ingelheim Int Formulaciones que comprenden un inhibidor de dpp4
EP2146210A1 (en) 2008-04-07 2010-01-20 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY
PE20100156A1 (es) * 2008-06-03 2010-02-23 Boehringer Ingelheim Int Tratamiento de nafld
WO2010009243A1 (en) 2008-07-15 2010-01-21 Theracos, Inc. Deuterated benzylbenzene derivatives and methods of use
BRPI0916997A2 (pt) 2008-08-06 2020-12-15 Boehringer Ingelheim International Gmbh Inibidor de dpp-4 e seu uso
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
KR101657960B1 (ko) * 2008-08-15 2016-09-20 베링거 인겔하임 인터내셔날 게엠베하 Fab-관련 질환의 치료에 사용하기 위한 푸린 유도체
AU2009290911A1 (en) 2008-09-10 2010-03-18 Boehringer Ingelheim International Gmbh Combination therapy for the treatment of diabetes and related conditions
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
US8410284B2 (en) 2008-10-22 2013-04-02 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
WO2010051206A1 (en) 2008-10-31 2010-05-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
EP2382216A1 (en) 2008-12-23 2011-11-02 Boehringer Ingelheim International GmbH Salt forms of organic compound
AR074990A1 (es) 2009-01-07 2011-03-02 Boehringer Ingelheim Int Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
PL2475428T3 (pl) 2009-09-11 2015-12-31 Probiodrug Ag Pochodne heterocykliczne jako inhibitory cyklazy glutaminowej
EA034869B1 (ru) 2009-11-27 2020-03-31 Бёрингер Ингельхайм Интернациональ Гмбх Лечение генотипированных пациентов с диабетом ингибиторами дпп-4, такими как линаглиптин
JP2013520502A (ja) 2010-02-25 2013-06-06 メルク・シャープ・エンド・ドーム・コーポレイション 有用な抗糖尿病薬である新規な環状ベンズイミダゾール誘導体
ES2586231T3 (es) 2010-03-03 2016-10-13 Probiodrug Ag Inhibidores de glutaminil ciclasa
MX2012010470A (es) 2010-03-10 2012-10-09 Probiodrug Ag Inhibidores heterociclicos d ciclasa de glutaminilo (qc, ec .3 2. 5).
JP2013523819A (ja) 2010-04-06 2013-06-17 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 Gpr119レセプターのモジュレーターおよびそれに関連する障害の処置
US8541596B2 (en) 2010-04-21 2013-09-24 Probiodrug Ag Inhibitors
MX341025B (es) 2010-05-05 2016-08-04 Boehringer Ingelheim Int Gmbh * Terapia de combinacion.
WO2011153712A1 (en) 2010-06-12 2011-12-15 Theracos, Inc. Crystalline form of benzylbenzene sglt2 inhibitor
PH12012502524A1 (en) 2010-06-24 2014-02-10 Boehringer Ingelheim Int Diabetes therapy
EP2600716A4 (en) 2010-08-03 2014-02-19 Beth Israel Hospital METHOD AND COMPOSITIONS FOR THE TREATMENT OF METABOLISM DISEASES
CN103221410B (zh) 2010-09-22 2017-09-15 艾尼纳制药公司 Gpr119受体调节剂和对与其相关的障碍的治疗
US9034883B2 (en) 2010-11-15 2015-05-19 Boehringer Ingelheim International Gmbh Vasoprotective and cardioprotective antidiabetic therapy
CA2826649C (en) 2011-02-25 2016-07-26 Merck Sharp & Dohme Corp. Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents
EP2686313B1 (en) 2011-03-16 2016-02-03 Probiodrug AG Benzimidazole derivatives as inhibitors of glutaminyl cyclase
US20140018371A1 (en) 2011-04-01 2014-01-16 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
WO2012145604A1 (en) 2011-04-22 2012-10-26 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
EP3517539B1 (en) 2011-07-15 2022-12-14 Boehringer Ingelheim International GmbH Substituted dimeric quinazoline derivative, its preparation and its use in pharmaceutical compositions for the treatment of type i and ii diabetes
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
US20130303554A1 (en) 2012-05-14 2013-11-14 Boehringer Ingelheim International Gmbh Use of a dpp-4 inhibitor in sirs and/or sepsis
JP6224084B2 (ja) 2012-05-14 2017-11-01 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 糸球体上皮細胞関連障害及び/又はネフローゼ症候群の治療に用いるdpp−4阻害薬としてのキサンチン誘導体
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
US20140045746A1 (en) 2012-08-02 2014-02-13 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
JP2016516004A (ja) 2013-02-22 2016-06-02 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. 抗糖尿病二環式化合物
WO2014139388A1 (en) 2013-03-14 2014-09-18 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
US9526728B2 (en) 2014-02-28 2016-12-27 Boehringer Ingelheim International Gmbh Medical use of a DPP-4 inhibitor
CN107683135A (zh) 2015-03-09 2018-02-09 因特克林医疗有限公司 用于治疗非酒精性脂肪肝疾病和/或脂肪营养不良的方法
JP6506880B2 (ja) * 2015-07-27 2019-04-24 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft B型肝炎ウィルス感染症の治療および予防のための新規な四環式4−オキソ−ピリジン−3−カルボン酸誘導体
CN105412096A (zh) * 2015-12-15 2016-03-23 上海壹志医药科技有限公司 药根碱的药物用途
CN109310697A (zh) 2016-06-10 2019-02-05 勃林格殷格翰国际有限公司 利格列汀和二甲双胍的组合
WO2018106518A1 (en) 2016-12-06 2018-06-14 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
WO2018118670A1 (en) 2016-12-20 2018-06-28 Merck Sharp & Dohme Corp. Antidiabetic spirochroman compounds
AU2018249822A1 (en) 2017-04-03 2019-10-31 Coherus Biosciences Inc. PPArgamma agonist for treatment of progressive supranuclear palsy
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH11230910A (ja) * 1998-02-16 1999-08-27 Shionogi & Co Ltd ベンゾキノリジジン誘導体を含有するカルボン酸のルテニウム錯体化学発光検出用試薬

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9322828D0 (en) * 1993-11-05 1993-12-22 Sandoz Ltd Organic compounds
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
EP1372650B1 (en) 2001-03-19 2008-11-19 Novartis AG Combinations comprising an antidiarrheal agent and an epothilone or an epothilone derivative

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH11230910A (ja) * 1998-02-16 1999-08-27 Shionogi & Co Ltd ベンゾキノリジジン誘導体を含有するカルボン酸のルテニウム錯体化学発光検出用試薬

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
AMINO AND AMI DO TETRABENAZINE DERVATIVES D J CANNEY ET AL,NUCL MED BIOL VOL,Vol.4 1995 *
HYDROPHOBCITY OF THE TETRABENAZINE BINDINGSITE D SCHERMAN ET AL,MOL PHARMACOL,Vol.33 No.1 1988 *
PHOTOA FFINITY LABELING OFTHE TERFRABENAZINEBINDI NG SITES OF M F ISAMBERT J P HENRY,BIOXHEMIDSTRY,Vol.24 No.14 1985 *
STEREOCHE MISTRY OF EMETINE A R BATTERSBY ET AL,CHEM&IND LONDO N 1957 *
SYNTHESIS OF A BUZAS ET AL,CHIM THER,Vol.7 No.5 1972 *

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