BR112015010649A2 - moduladores de gpr40 à base de pirrolidina - Google Patents

moduladores de gpr40 à base de pirrolidina

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Publication number
BR112015010649A2
BR112015010649A2 BR112015010649A BR112015010649A BR112015010649A2 BR 112015010649 A2 BR112015010649 A2 BR 112015010649A2 BR 112015010649 A BR112015010649 A BR 112015010649A BR 112015010649 A BR112015010649 A BR 112015010649A BR 112015010649 A2 BR112015010649 A2 BR 112015010649A2
Authority
BR
Brazil
Prior art keywords
pyrrolidine
gpr40
modulators
gpr40 modulators
compounds
Prior art date
Application number
BR112015010649A
Other languages
English (en)
Inventor
a ellsworth Bruce
Sun Chongqing
A Jurica Elizabeth
Shi Jun
R Ewing William
Ye Xiang-Yang
Wu Ximao
Zhu Yeheng
Original Assignee
Bristol Myers Squibb Co
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
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of BR112015010649A2 publication Critical patent/BR112015010649A2/pt

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • AHUMAN NECESSITIES
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    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
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    • A61P9/00Drugs for disorders of the cardiovascular system
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/12Antihypertensives
    • 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
    • C07D207/08Heterocyclic 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 hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • 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
    • C07D207/12Oxygen or sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

resumo patente de invenção: "moduladores de gpr40 à base de pirrolidina". a presente invenção refere-se a compostos de fórmula (i): (i) ou um estereoisômero, ou um sal farmaceuticamente aceitável do mesmo, onde todas as variáveis têm as definições dadas neste relatório. estes compostos são moduladores do receptor acoplado à proteína g gpr40 que podem ser usados como medicamentos.
BR112015010649A 2012-11-16 2013-11-15 moduladores de gpr40 à base de pirrolidina BR112015010649A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261727253P 2012-11-16 2012-11-16
PCT/US2013/070213 WO2014078609A1 (en) 2012-11-16 2013-11-15 Pyrrolidine gpr40 modulators

Publications (1)

Publication Number Publication Date
BR112015010649A2 true BR112015010649A2 (pt) 2017-07-11

Family

ID=49667626

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015010649A BR112015010649A2 (pt) 2012-11-16 2013-11-15 moduladores de gpr40 à base de pirrolidina

Country Status (14)

Country Link
US (1) US9714231B2 (pt)
EP (1) EP2925741B1 (pt)
JP (1) JP6322202B2 (pt)
KR (1) KR20150082615A (pt)
CN (1) CN105121426B (pt)
AU (1) AU2013344603B2 (pt)
BR (1) BR112015010649A2 (pt)
CA (1) CA2891569A1 (pt)
EA (1) EA201590953A1 (pt)
ES (1) ES2606197T3 (pt)
IL (1) IL238742A0 (pt)
MX (1) MX2015006038A (pt)
SG (1) SG11201503559TA (pt)
WO (1) WO2014078609A1 (pt)

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US8962660B2 (en) 2013-03-14 2015-02-24 Bristol-Myers Squibb Company Oxabicyclo [2.2.2] acid GPR120 modulators
KR20160077213A (ko) 2013-11-14 2016-07-01 카딜라 핼쓰캐어 리미티드 새로운 헤테로시클릭 화합물
DK3140296T3 (en) * 2014-05-07 2018-07-23 Bristol Myers Squibb Co PYRROLIDIN GPR40 MODULATORS FOR TREATMENT OF DISEASES SUCH AS DIABETES
US10301260B2 (en) 2014-05-07 2019-05-28 Bristol-Myers Squibb Company Pyrrolidine GPR40 modulators
CA2948175A1 (en) * 2014-05-07 2015-11-12 Bristol-Myers Squibb Company Pyrrolidine gpr40 modulators for the treatment of diseases such as diabetes
US10662171B2 (en) 2014-08-08 2020-05-26 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
EP3177285B1 (en) 2014-08-08 2020-09-23 Merck Sharp & Dohme Corp. [5,6]-fused bicyclic antidiabetic compounds
WO2016019587A1 (en) 2014-08-08 2016-02-11 Merck Sharp & Dohme Corp. [7, 6]-fused bicyclic antidiabetic compounds
US10968193B2 (en) 2014-08-08 2021-04-06 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
AR105889A1 (es) 2015-09-03 2017-11-22 Actelion Pharmaceuticals Ltd Compuestos antibacterianos 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona sustituidos
WO2018027892A1 (en) * 2016-08-12 2018-02-15 Eli Lilly And Company Amino pyrimidine ssao inhibitors
WO2018148856A1 (en) 2017-02-14 2018-08-23 Eli Lilly And Company Diazaspirodecanyl-pyrimidine compounds useful as ssao inhibitors
US10336737B2 (en) 2017-06-20 2019-07-02 The Board Of Trustees Of The University Of Illinois Metal catalyzed dearomative 1,2-carboamination
AU2019222644B2 (en) 2018-02-13 2021-04-01 Gilead Sciences, Inc. PD-1/PD-L1 inhibitors
US10899735B2 (en) 2018-04-19 2021-01-26 Gilead Sciences, Inc. PD-1/PD-L1 inhibitors
JP7105359B2 (ja) 2018-07-13 2022-07-22 ギリアード サイエンシーズ, インコーポレイテッド Pd-1/pd-l1阻害剤
AU2019366355B2 (en) 2018-10-24 2022-10-13 Gilead Sciences, Inc. PD-1/PD-L1 inhibitors
US11034669B2 (en) 2018-11-30 2021-06-15 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
JP2023539639A (ja) 2020-08-25 2023-09-15 イーライ リリー アンド カンパニー Ssao阻害剤の多形
AU2022291768A1 (en) 2021-06-16 2023-11-30 Celgene Corporation Azetidinyl compounds comprising a carboxylic acid group for the treatment of neurodegenerative diseases

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US5614492A (en) 1986-05-05 1997-03-25 The General Hospital Corporation Insulinotropic hormone GLP-1 (7-36) and uses thereof
WO2004099192A2 (en) 2003-04-30 2004-11-18 The Institutes Of Pharmaceutical Discovery, Llc Heterocycle substituted carboxylic acids as inhibitors of protein tyrosine phosphatase-1b
US6995183B2 (en) 2003-08-01 2006-02-07 Bristol Myers Squibb Company Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods
AU2010303670A1 (en) * 2009-10-06 2012-03-29 Bristol-Myers Squibb Company Pyrrolidine GPR40 modulators
MX2012004078A (es) * 2009-10-09 2012-07-25 Irm Llc Compuestos y composiciones como moduladores de la actividad de gpr119.
AR083904A1 (es) 2010-11-18 2013-04-10 Prosidion Ltd Derivados de 1,4-pirrolidinas disustituidos y 3-il-aminas y sus usos en el tratamiento de desordenes metabolicos
CA2818050A1 (en) * 2010-11-26 2012-05-31 Lupin Limited Bicyclic gpr119 modulators
US8791091B2 (en) 2011-12-02 2014-07-29 Bristol-Myers Squibb Company Aryl dihydropyridinone and piperidinone MGAT2 inhibitors
GB2498976A (en) 2012-02-01 2013-08-07 Prosidion Ltd GPR119 agonists useful in the treatment of type II diabetes

Also Published As

Publication number Publication date
ES2606197T3 (es) 2017-03-23
US9714231B2 (en) 2017-07-25
EP2925741B1 (en) 2016-10-26
WO2014078609A1 (en) 2014-05-22
CA2891569A1 (en) 2014-05-22
EA201590953A1 (ru) 2015-08-31
MX2015006038A (es) 2015-08-07
IL238742A0 (en) 2015-06-30
AU2013344603A1 (en) 2015-07-02
AU2013344603B2 (en) 2017-07-06
SG11201503559TA (en) 2015-06-29
CN105121426A (zh) 2015-12-02
EP2925741A1 (en) 2015-10-07
KR20150082615A (ko) 2015-07-15
JP2016500062A (ja) 2016-01-07
JP6322202B2 (ja) 2018-05-09
US20160280680A1 (en) 2016-09-29
CN105121426B (zh) 2017-03-29

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