CA2814231A1 - 4- (5-cyano-pyrazol-1-yl) -piperidine derivatives as gpr 119 modulators - Google Patents

4- (5-cyano-pyrazol-1-yl) -piperidine derivatives as gpr 119 modulators Download PDF

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Publication number
CA2814231A1
CA2814231A1 CA2814231A CA2814231A CA2814231A1 CA 2814231 A1 CA2814231 A1 CA 2814231A1 CA 2814231 A CA2814231 A CA 2814231A CA 2814231 A CA2814231 A CA 2814231A CA 2814231 A1 CA2814231 A1 CA 2814231A1
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CA
Canada
Prior art keywords
methyl
cyano
carboxylate
pyrazol
piperidine
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.)
Abandoned
Application number
CA2814231A
Other languages
English (en)
French (fr)
Inventor
Vincent Mascitti
Kim Francis Mcclure
Michael John Munchhof
Ralph Pelton Robinson, Jr.
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pfizer Inc
Original Assignee
Pfizer Inc
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=45418722&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2814231(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer Inc filed Critical Pfizer Inc
Publication of CA2814231A1 publication Critical patent/CA2814231A1/en
Abandoned legal-status Critical Current

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    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Hospice & Palliative Care (AREA)
  • Gynecology & Obstetrics (AREA)
  • Immunology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CA2814231A 2010-11-23 2011-11-09 4- (5-cyano-pyrazol-1-yl) -piperidine derivatives as gpr 119 modulators Abandoned CA2814231A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41644110P 2010-11-23 2010-11-23
US61/416,441 2010-11-23
PCT/IB2011/054996 WO2012069948A1 (en) 2010-11-23 2011-11-09 4- (5-cyano-pyrazol-1-yl) -piperidine derivatives as gpr 119 modulators

Publications (1)

Publication Number Publication Date
CA2814231A1 true CA2814231A1 (en) 2012-05-31

Family

ID=45418722

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2814231A Abandoned CA2814231A1 (en) 2010-11-23 2011-11-09 4- (5-cyano-pyrazol-1-yl) -piperidine derivatives as gpr 119 modulators

Country Status (26)

Country Link
EP (1) EP2643310A1 (es)
JP (1) JP2013543885A (es)
KR (1) KR20130083915A (es)
CN (1) CN103298801A (es)
AP (1) AP2013006809A0 (es)
AR (1) AR088121A1 (es)
AU (1) AU2011333427A1 (es)
BR (1) BR112013011865A2 (es)
CA (1) CA2814231A1 (es)
CL (1) CL2013001054A1 (es)
CO (1) CO6801716A2 (es)
CR (1) CR20130139A (es)
CU (1) CU20130059A7 (es)
DO (1) DOP2013000102A (es)
EA (1) EA201370118A1 (es)
EC (1) ECSP13012630A (es)
GT (1) GT201300135A (es)
MA (1) MA34805B1 (es)
MX (1) MX2013004083A (es)
NI (1) NI201300044A (es)
PE (1) PE20140409A1 (es)
SG (1) SG189830A1 (es)
TW (1) TWI433843B (es)
UY (1) UY33742A (es)
WO (1) WO2012069948A1 (es)
ZA (1) ZA201302362B (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6463631B2 (ja) 2011-06-09 2019-02-06 ライゼン・ファーマシューティカルズ・エスアー Gpr−119のモジュレータとしての新規化合物
CN104780915A (zh) 2012-07-11 2015-07-15 埃尔舍利克斯治疗公司 包含他汀、双胍和用于减小心脏代谢风险的其它药剂的组合物
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
CN104892517A (zh) * 2015-02-13 2015-09-09 佛山市赛维斯医药科技有限公司 酰肼类化合物、其制备方法及用途
CN104610151A (zh) * 2015-02-13 2015-05-13 佛山市赛维斯医药科技有限公司 含酰肼和烷氧苯类结构的化合物、其制备方法及用途
CN104592120A (zh) * 2015-02-13 2015-05-06 佛山市赛维斯医药科技有限公司 一种环丙基酰肼和甲氧苯类gpr119激动剂、制备方法及其用途
EP3416959B1 (en) 2016-02-18 2021-05-12 Syngenta Participations AG Pesticidally active pyrazole derivatives
CN106631992B (zh) * 2017-01-05 2019-01-18 桑迪亚医药技术(上海)有限责任公司 一种4-氧-3,4-二氢-2h-吡啶-1-甲酸叔丁酯的合成方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2185544B1 (en) * 2007-07-19 2014-11-26 Cymabay Therapeutics, Inc. N-azacyclic substituted pyrrole, pyrazole, imidazole, triazole and tetrazole derivatives as agonists of the rup3 or gpr119 for the treatment of diabetes and metabolic disorders
TW201002705A (en) * 2008-03-31 2010-01-16 Metabolex Inc Oxymethylene aryl compounds and uses thereof
NZ596467A (en) * 2009-06-05 2014-01-31 Pfizer L- ( piperidin-4-yl) -pyrazole derivatives as gpr 119 modulators

Also Published As

Publication number Publication date
MA34805B1 (fr) 2014-01-02
NI201300044A (es) 2013-08-01
SG189830A1 (en) 2013-06-28
PE20140409A1 (es) 2014-03-23
UY33742A (es) 2012-06-29
AU2011333427A1 (en) 2013-04-11
CR20130139A (es) 2013-06-28
EP2643310A1 (en) 2013-10-02
DOP2013000102A (es) 2013-07-15
KR20130083915A (ko) 2013-07-23
CU20130059A7 (es) 2013-06-28
GT201300135A (es) 2015-02-19
MX2013004083A (es) 2013-06-13
WO2012069948A1 (en) 2012-05-31
TWI433843B (zh) 2014-04-11
AP2013006809A0 (en) 2013-04-30
CO6801716A2 (es) 2013-11-29
BR112013011865A2 (pt) 2016-08-23
AR088121A1 (es) 2014-05-14
TW201300373A (zh) 2013-01-01
EA201370118A1 (ru) 2013-12-30
CN103298801A (zh) 2013-09-11
ZA201302362B (en) 2014-06-25
CL2013001054A1 (es) 2013-09-27
JP2013543885A (ja) 2013-12-09
ECSP13012630A (es) 2013-07-31

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Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20130410

FZDE Discontinued

Effective date: 20151015