EA201190280A1 - Производные l-(пиперидин-4-ил)пиразола в качестве модуляторов gpr 119 - Google Patents

Производные l-(пиперидин-4-ил)пиразола в качестве модуляторов gpr 119

Info

Publication number
EA201190280A1
EA201190280A1 EA201190280A EA201190280A EA201190280A1 EA 201190280 A1 EA201190280 A1 EA 201190280A1 EA 201190280 A EA201190280 A EA 201190280A EA 201190280 A EA201190280 A EA 201190280A EA 201190280 A1 EA201190280 A1 EA 201190280A1
Authority
EA
Eurasian Patent Office
Prior art keywords
gpr
pyrazol
piperidin
modulators
derivatives
Prior art date
Application number
EA201190280A
Other languages
English (en)
Other versions
EA020106B1 (ru
Inventor
Винсент Масситти
Ким Фрэнсис Макклюр
Майкл Джон Манчхоф
Ральф Пелтон мл. Робинсон
Майкл Пол Денинно
Кентаро Футацуги
Кун Дэниел Вей-Шун
Брюс Аллен Лефкер
Original Assignee
Пфайзер Инк.
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 Пфайзер Инк. filed Critical Пфайзер Инк.
Publication of EA201190280A1 publication Critical patent/EA201190280A1/ru
Publication of EA020106B1 publication Critical patent/EA020106B1/ru

Links

Classifications

    • 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
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/12Ophthalmic agents for cataracts
    • 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
    • A61P3/06Antihyperlipidemics
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Reproductive Health (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Immunology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

В данной заявке описаны соединения формулы I, которые модулируют активность G-белоксопряженного рецептора GPR119, и их применения в лечении заболеваний, связанных с модуляцией G-белоксопряженного рецептора GPR119 у животных.
EA201190280A 2009-06-05 2010-05-27 Производные l-(пиперидин-4-ил)пиразола в качестве модуляторов gpr119 EA020106B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US18435509P 2009-06-05 2009-06-05
US25762109P 2009-11-03 2009-11-03
PCT/IB2010/052377 WO2010140092A1 (en) 2009-06-05 2010-05-27 L- ( piperidin-4-yl) -pyrazole derivatives as gpr 119 modulators

Publications (2)

Publication Number Publication Date
EA201190280A1 true EA201190280A1 (ru) 2012-09-28
EA020106B1 EA020106B1 (ru) 2014-08-29

Family

ID=42358441

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201190280A EA020106B1 (ru) 2009-06-05 2010-05-27 Производные l-(пиперидин-4-ил)пиразола в качестве модуляторов gpr119

Country Status (33)

Country Link
US (1) US20110020460A1 (ru)
EP (1) EP2438051A1 (ru)
JP (1) JP2012528847A (ru)
KR (1) KR20120061063A (ru)
CN (1) CN102459222B (ru)
AP (1) AP2799A (ru)
AR (1) AR076985A1 (ru)
AU (1) AU2010255422B2 (ru)
BR (1) BRPI1014636A2 (ru)
CA (1) CA2764021C (ru)
CL (1) CL2011003085A1 (ru)
CO (1) CO6470897A2 (ru)
CR (1) CR20110623A (ru)
CU (1) CU20110225A7 (ru)
DO (1) DOP2011000371A (ru)
EA (1) EA020106B1 (ru)
EC (1) ECSP11011493A (ru)
GE (1) GEP20135907B (ru)
GT (1) GT201100308A (ru)
HN (1) HN2011003195A (ru)
IL (1) IL216772A0 (ru)
MA (1) MA33334B1 (ru)
MX (1) MX2011013034A (ru)
NI (1) NI201100204A (ru)
NZ (1) NZ596467A (ru)
PE (1) PE20120399A1 (ru)
SG (1) SG175995A1 (ru)
SV (1) SV2011004063A (ru)
TN (1) TN2012000073A1 (ru)
TW (1) TWI411611B (ru)
UY (1) UY32683A (ru)
WO (1) WO2010140092A1 (ru)
ZA (1) ZA201108481B (ru)

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5467151B2 (ja) 2009-06-24 2014-04-09 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 新規化合物、医薬組成物及びそれに関する方法
AR077214A1 (es) 2009-06-24 2011-08-10 Neurocrine Biosciences Inc Heterociclos nitrogenados y composiciones farmaceuticas que los contienen
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
HUE025774T2 (en) 2010-03-19 2016-05-30 Pfizer 2,3-Dihydro-1H-inden-1-yl-2,7-diazaspiro [3.6] nonane derivatives and their use as antagonists or inverse agonists of the ghrelin receptor
RU2540337C2 (ru) 2010-10-29 2015-02-10 Пфайзер Инк. N1/N2-ЛАКТАМНЫЕ ИНГИБИТОРЫ АЦЕТИЛ-КоА-КАРБОКСИЛАЗ
KR20130083915A (ko) * 2010-11-23 2013-07-23 화이자 인코포레이티드 Gpr119 조절제로서의 4-(5-시아노-피라졸-1-일)-피페리딘 유도체
PL2699576T3 (pl) 2011-04-22 2016-05-31 Pfizer Pochodne pirazolospiroketonu do zastosowania jako inhibitory karboksylazy acetylo-COA
AU2012267556B9 (en) 2011-06-09 2017-05-11 Rhizen Pharmaceuticals Sa Novel compounds as modulators of GPR-119
JP2014520879A (ja) 2011-07-15 2014-08-25 ファイザー・インク Gpr119調節因子
US8927577B2 (en) 2011-07-22 2015-01-06 Pfizer Inc. Quinolinyl glucagon receptor modulators
EP2751116B1 (en) 2011-08-31 2016-10-12 Pfizer Inc Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds
UA108713C2 (xx) 2011-11-11 2015-05-25 2-тіопіримідинони
MA37385B1 (fr) 2012-04-06 2019-09-30 Pfizer Inc Etat De Delaware Inhibiteurs de diacylglycérol-acyltransférase 2
US8889730B2 (en) 2012-04-10 2014-11-18 Pfizer Inc. Indole and indazole compounds that activate AMPK
US9309232B2 (en) * 2012-04-24 2016-04-12 Board Of Trustees Of Northern Illinois University Synthesis of novel inhibitors of isoprenoid biosynthesis
ES2585262T3 (es) 2012-05-04 2016-10-04 Pfizer Inc Compuestos heterocíclicos de hexahidropiran[3,4-d][1,3]tiazin-2-amina sustituidos como inhibidores de PPA, BACE1 y BACE2
JP2015522080A (ja) 2012-07-11 2015-08-03 エルセリクス セラピューティクス インコーポレイテッド スタチン、ビグアナイド、およびさらなる薬剤を含む心血管代謝性リスクを減少させるための組成物
EP2897964A1 (en) 2012-09-20 2015-07-29 Pfizer Inc. Alkyl-substituted hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds
CA2893256A1 (en) 2012-12-11 2014-06-19 Pfizer Inc. Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds as inhibitors of bace1
EP2935282A1 (en) 2012-12-19 2015-10-28 Pfizer Inc. CARBOCYCLIC- AND HETEROCYCLIC-SUBSTITUTED HEXAHYDROPYRANO[3,4-d][1,3]THIAZIN-2-AMINE COMPOUNDS
EP2956458B1 (en) 2013-02-13 2017-08-09 Pfizer Inc Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
US9233981B1 (en) 2013-02-15 2016-01-12 Pfizer Inc. Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
WO2015052610A1 (en) 2013-10-09 2015-04-16 Pfizer Inc. Antagonists of prostaglandin ep3 receptor
AP2016009407A0 (en) 2014-03-17 2016-08-31 Pfizer Diacylglycerol acyltransferase 2 inhibitors for use in the treatment of metabolic and related disorders
SG11201608110WA (en) 2014-04-04 2016-10-28 Pfizer Bicyclic-fused heteroaryl or aryl compounds and their use as irak4 inhibitors
EA030085B1 (ru) 2014-04-10 2018-06-29 Пфайзер Инк. 2-АМИНО-6-МЕТИЛ-4,4a,5,6-ТЕТРАГИДРОПИРАНО[3,4-d][1,3]ТИАЗИН-8a(8H)-ИЛ-1,3-ТИАЗОЛ-4-ИЛ АМИДЫ
JP2017119628A (ja) * 2014-05-09 2017-07-06 日産化学工業株式会社 置換アゾール化合物及び糖尿病治療薬
WO2016092413A1 (en) 2014-12-10 2016-06-16 Pfizer Inc. Indole and indazole compounds that activate ampk
WO2016103097A1 (en) 2014-12-22 2016-06-30 Pfizer Inc. Antagonists of prostaglandin ep3 receptor
DK3265126T3 (da) 2015-03-03 2021-09-13 Saniona As Kombinationsformulering af tesofensin og metoprolol
MX2017014128A (es) 2015-05-05 2018-03-15 Pfizer 2-tiopirimidinonas.
JP2018516254A (ja) 2015-05-29 2018-06-21 ファイザー・インク バニン1酵素の阻害薬としての新規なヘテロ環化合物
EP3310784B1 (en) 2015-06-17 2020-10-07 Pfizer Inc Tricyclic compounds and their use as phosphodiesterase inhibitors.
WO2016203335A1 (en) 2015-06-18 2016-12-22 Pfizer Inc. Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors
BR112018002071A2 (pt) 2015-08-13 2018-09-18 Pfizer compostos heteroarílicos ou arílicos fundidos bicíclicos
KR102029124B1 (ko) 2015-08-27 2019-10-07 화이자 인코포레이티드 Irak4 조정제로서의 비시클릭-융합된 헤테로아릴 또는 아릴 화합물
WO2017037567A1 (en) 2015-09-03 2017-03-09 Pfizer Inc. Regulators of frataxin
WO2017051276A1 (en) 2015-09-24 2017-03-30 Pfizer Inc. N-[2-(2-amino-6,6-disubstituted-4, 4a, 5, 6-tetrahydropyrano [3,4-d][1,3] thiazin-8a (8h)-yl) -1, 3-thiazol-4-yl] amides
JP2018534251A (ja) 2015-09-24 2018-11-22 ファイザー・インク Bace阻害剤として有用なn−[2−(3−アミノ−2,5−ジメチル−1,1−ジオキシド−5,6−ジヒドロ−2h−1,2,4−チアジアジン−5−イル)−1,3−チアゾール−4−イル]アミド
JP2018531924A (ja) 2015-09-24 2018-11-01 ファイザー・インク テトラヒドロピラノ[3,4−d][1,3]オキサジン誘導体、およびbace阻害剤としてのその使用
TN2018000198A1 (en) 2015-12-29 2019-10-04 Pfizer Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors
US10155766B2 (en) 2016-06-14 2018-12-18 Board Of Trustees Of Northern Illinois University Pyrazolopyrimidine antibacterial agents
JP2019524716A (ja) 2016-07-14 2019-09-05 ファイザー・インク バニン1酵素の阻害薬としての新規のピリミジンカルボキサミド
AR109179A1 (es) 2016-08-19 2018-11-07 Pfizer Inhibidores de diacilglicerol aciltransferasa 2
WO2019133445A1 (en) 2017-12-28 2019-07-04 Inception Ibd, Inc. Aminothiazoles as inhibitors of vanin-1
MX2021002428A (es) 2018-08-31 2023-01-02 Pfizer Combinaciones para tratamiento de ehna/ehgna y enfermedades relacionadas.
WO2020102575A1 (en) 2018-11-16 2020-05-22 Inception Ibd, Inc. Heterocyclic aminothiazoles and uses thereof
CA3140972A1 (en) 2019-05-20 2020-11-26 Pfizer Inc. Combinations comprising benzodioxol as glp-1r agonists for use in the treatment of nash/nafld and related diseases
TW202115086A (zh) 2019-06-28 2021-04-16 美商輝瑞大藥廠 Bckdk抑制劑
WO2020261144A1 (en) 2019-06-28 2020-12-30 Pfizer Inc. 5-(thiophen-2-yl)-1h-tetrazole derivatives as bckdk inhibitors useful for treating various diseases
TWI771766B (zh) 2019-10-04 2022-07-21 美商輝瑞股份有限公司 二醯基甘油醯基轉移酶2 抑制劑
JP2022058085A (ja) 2020-02-24 2022-04-11 ファイザー・インク ジアシルグリセロールアシルトランスフェラーゼ2阻害剤とアセチル-CoAカルボキシラーゼ阻害剤との組合せ
CR20220632A (es) 2020-06-09 2023-01-23 Pfizer Antagonistas del receptor de melanocortina 4 y usos de estos
WO2023026180A1 (en) 2021-08-26 2023-03-02 Pfizer Inc. Amorphous form of (s)-2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-n-(tetrahydrofuran-3- yl)pyrimidine-5-carboxamide
WO2023100061A1 (en) 2021-12-01 2023-06-08 Pfizer Inc. 3-phenyl-1-benzothiophene-2-carboxylic acid derivatives as branched-chain alpha keto acid dehydrogenase kinase inhibitors for the treatment of diabetes, kidney diseases, nash and heart failure
WO2023105387A1 (en) 2021-12-06 2023-06-15 Pfizer Inc. Melanocortin 4 receptor antagonists and uses thereof
WO2023169456A1 (en) 2022-03-09 2023-09-14 Gasherbrum Bio , Inc. Heterocyclic glp-1 agonists
WO2023198140A1 (en) 2022-04-14 2023-10-19 Gasherbrum Bio, Inc. Heterocyclic glp-1 agonists
WO2024075051A1 (en) 2022-10-07 2024-04-11 Pfizer Inc. Hsd17b13 inhibitors and/or degraders

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60219295T2 (de) 2001-02-28 2008-01-03 Merck & Co., Inc. Acylierte piperidinderivate als melanocortin-4-rezeptoragonisten
WO2003072547A1 (en) 2002-02-27 2003-09-04 Pfizer Products Inc. PROCESSES AND INTERMEDIATES USEFUL IN PREPARING β3-ADRENERGIC RECEPTOR AGONISTS
US20040220170A1 (en) 2003-05-01 2004-11-04 Atkinson Robert N. Pyrazole-amides and sulfonamides as sodium channel modulators
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
EP2287165A3 (en) * 2003-07-14 2011-06-22 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
EP2210607B1 (en) 2003-09-26 2011-08-17 Exelixis Inc. N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide for the treatment of cancer
CA2568056A1 (en) 2004-05-25 2005-12-08 Pfizer Products Inc. Tetraazabenzo[e]azulene derivatives and analogs thereof
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
DOP2006000009A (es) * 2005-01-13 2006-08-15 Arena Pharm Inc Procedimiento para preparar eteres de pirazolo [3,4-d] pirimidina
PA8660701A1 (es) 2005-02-04 2006-09-22 Pfizer Prod Inc Agonistas de pyy y sus usos
EP1931337B1 (en) * 2005-09-29 2013-10-23 Sanofi Phenyl- and pyridinyl- 1, 2 , 4 - oxadiazolone derivatives, processes for their preparation and their use as pharmaceuticals
GB0522846D0 (en) 2005-11-09 2005-12-21 Peakdale Molecular Ltd Process
US20100022457A1 (en) * 2006-05-26 2010-01-28 Bristol-Myers Squibb Company Sustained release glp-1 receptor modulators
CN101679422A (zh) 2007-03-28 2010-03-24 阵列生物制药公司 作为受体酪氨酸激酶抑制剂的咪唑并[1,2-a]吡啶化合物
US8093257B2 (en) 2007-05-04 2012-01-10 Bristol-Myers Squibb Company [6,5]-bicyclic GPR119 G protein-coupled receptor agonists
BRPI0814294A2 (pt) * 2007-07-19 2015-02-03 Metabolex Inc Agonistas de receptor heterocíclico ligado a n para o tratamento do diabetes e de desordens metabólicas.
MX2010009205A (es) 2008-02-22 2010-11-10 Irm Llc Compuestos y composiciones como moduladores de la actividad de gpr119.
PL2280704T3 (pl) * 2008-03-31 2015-10-30 Cymabay Therapeutics Inc Związki oksymetylenoarylowe i ich zastosowania
US8536176B2 (en) * 2008-08-01 2013-09-17 Nippon Chemiphar Co., Ltd. GPR119 agonist

Also Published As

Publication number Publication date
EA020106B1 (ru) 2014-08-29
CL2011003085A1 (es) 2012-09-07
US20110020460A1 (en) 2011-01-27
CR20110623A (es) 2012-01-04
SV2011004063A (es) 2012-01-04
CN102459222A (zh) 2012-05-16
HN2011003195A (es) 2013-03-11
WO2010140092A1 (en) 2010-12-09
CA2764021A1 (en) 2010-12-09
GT201100308A (es) 2013-11-11
CO6470897A2 (es) 2012-06-29
IL216772A0 (en) 2012-03-01
KR20120061063A (ko) 2012-06-12
GEP20135907B (en) 2013-08-12
NZ596467A (en) 2014-01-31
EP2438051A1 (en) 2012-04-11
TN2012000073A1 (fr) 2013-09-19
DOP2011000371A (es) 2012-04-30
PE20120399A1 (es) 2012-04-24
JP2012528847A (ja) 2012-11-15
AU2010255422A1 (en) 2011-12-22
NI201100204A (es) 2012-05-22
UY32683A (es) 2011-01-31
CN102459222B (zh) 2014-06-04
CA2764021C (en) 2014-04-22
CU20110225A7 (es) 2013-01-30
AR076985A1 (es) 2011-07-20
MX2011013034A (es) 2012-02-08
ZA201108481B (en) 2013-02-27
SG175995A1 (en) 2011-12-29
AU2010255422B2 (en) 2014-04-10
AP2011006020A0 (en) 2011-12-31
MA33334B1 (fr) 2012-06-01
TWI411611B (zh) 2013-10-11
BRPI1014636A2 (pt) 2016-04-05
TW201109314A (en) 2011-03-16
ECSP11011493A (es) 2011-12-30
AP2799A (en) 2013-11-30

Similar Documents

Publication Publication Date Title
EA201190280A1 (ru) Производные l-(пиперидин-4-ил)пиразола в качестве модуляторов gpr 119
ECSP13012611A (es) Derivados de pirazol-aminopirimidina como moduladores de la lrrk2
CR20120591A (es) Derivados de aminopirimidina como moduladores de la lrrk2
EA200971084A1 (ru) 5-членные гетероциклические амиды и родственные соединения
EA201001329A1 (ru) Соединения и композиции в качестве модуляторов активности gpr119
IL199972A (en) Tricyclic compounds and their use as modulators of glucocorticoid receptor
EA200901166A1 (ru) Соединения и композиции в качестве модуляторов активности gpr 119
EA201491607A1 (ru) Модуляторы толлподобных рецепторов
EA201001332A1 (ru) Соединения и композиции в качестве модуляторов активности gpr119
EA201170276A1 (ru) Модуляторы рецептора tgr5 и способы их применения
UY30572A1 (es) N-(1-ftalazin-1-il-piperidin-4-il)-amidas como moduladores del receptor ep2
HN2010002774A (es) DERIVADOS DE 2-(1,5-DIHIDRO-5-OXO-1,2,4-TRIAZOL-4-IL/2-OXOIMIDAZOLIDIN-1-IL)PIRIDIN-4-CARBOXAMIDA ACTIVOS COMO MODULADORES DE ESTEAROIL-CoA
EA200602243A1 (ru) 3-аминоциклопентанкарбоксамиды в качестве модуляторов хемокиновых рецепторов
EA201370118A1 (ru) Производные 4-(5-цианопиразол-1-ил)пиперидина в качестве модуляторов gpr 119
EA201590881A1 (ru) Терапевтические соединения и композиции и их использование в качестве модуляторов пк-m2
MX2010003949A (es) N-fenil-bipirrolidina carboxamidas sustituidas y uso terapeutico de las mismas.
EA201001330A1 (ru) Соединения и композиции в качестве модуляторов активности gpr119
MX2010003948A (es) N-fenil-birrolidin ureas sustituidas y uso terapeutico de las mismas.
ATE467632T1 (de) Pyrroloä2,3-büpyridinderivate als modulatoren des h3-rezeptors
MX2010004003A (es) N-fenil-pirrolidinilmetlipirrolidin amidas sustituidas y uso terapeutico de las mismas.
ATE466854T1 (de) 1h-indol-6-ylpiperazin-1-ylmethanonderivate zur verwendung als h3-rezeptormodulatoren
EA201300436A8 (ru) Совместные кристаллы и соли ингибиторов ccr3
EA201000439A1 (ru) Бензотиазолы в качестве модуляторов рецептора грелина
MX2009008286A (es) Compuestos triciclicos y su uso como moduladores del receptor de glucocorticosteroides.
ATE479691T1 (de) 4,5,6,7-tetrahydrothienoä2,3-cüpyridine als h3- modulatoren

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU