CN102574841A - 调节硬脂酰-coa去饱和酶的吡唑衍生物 - Google Patents

调节硬脂酰-coa去饱和酶的吡唑衍生物 Download PDF

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Publication number
CN102574841A
CN102574841A CN201080044452XA CN201080044452A CN102574841A CN 102574841 A CN102574841 A CN 102574841A CN 201080044452X A CN201080044452X A CN 201080044452XA CN 201080044452 A CN201080044452 A CN 201080044452A CN 102574841 A CN102574841 A CN 102574841A
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CN
China
Prior art keywords
alkyl
aryl
optionally substituted
cycloalkyl
heteroaryl
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Pending
Application number
CN201080044452XA
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English (en)
Chinese (zh)
Inventor
N·戴斯
付健民
Q·贾
N·波克罗夫斯伽叶
孙绍毅
张载辉
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.)
Xenon Pharmaceuticals Inc
Novartis AG
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Xenon Pharmaceuticals Inc
Novartis AG
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43066810&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN102574841(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Xenon Pharmaceuticals Inc, Novartis AG filed Critical Xenon Pharmaceuticals Inc
Publication of CN102574841A publication Critical patent/CN102574841A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric 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
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Nutrition Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201080044452XA 2009-10-01 2010-10-01 调节硬脂酰-coa去饱和酶的吡唑衍生物 Pending CN102574841A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US24763409P 2009-10-01 2009-10-01
US61/247,634 2009-10-01
PCT/EP2010/064672 WO2011039358A1 (en) 2009-10-01 2010-10-01 Pyrazole derivatives which modulate stearoyl-coa desaturase

Publications (1)

Publication Number Publication Date
CN102574841A true CN102574841A (zh) 2012-07-11

Family

ID=43066810

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201080044452XA Pending CN102574841A (zh) 2009-10-01 2010-10-01 调节硬脂酰-coa去饱和酶的吡唑衍生物

Country Status (23)

Country Link
US (1) US20130011361A1 (enExample)
EP (1) EP2483264A1 (enExample)
JP (1) JP2013506638A (enExample)
KR (1) KR20120080226A (enExample)
CN (1) CN102574841A (enExample)
AU (1) AU2010302577A1 (enExample)
BR (1) BR112012007509A2 (enExample)
CA (1) CA2776294A1 (enExample)
CL (1) CL2012000797A1 (enExample)
CO (1) CO6761294A2 (enExample)
CR (1) CR20120134A (enExample)
EA (1) EA201200545A1 (enExample)
EC (1) ECSP12011837A (enExample)
IL (1) IL218294A0 (enExample)
IN (1) IN2012DN01913A (enExample)
MA (1) MA33693B1 (enExample)
MX (1) MX2012003938A (enExample)
PE (1) PE20121439A1 (enExample)
PH (1) PH12012500648A1 (enExample)
SG (1) SG178869A1 (enExample)
TN (1) TN2012000085A1 (enExample)
WO (1) WO2011039358A1 (enExample)
ZA (1) ZA201201390B (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9358250B2 (en) 2011-10-15 2016-06-07 Genentech, Inc. Methods of using SCD1 antagonists
EP3529245A4 (en) 2016-10-24 2020-12-23 Yumanity Therapeutics, Inc. COMPOUNDS AND USES OF THE LATEST
MA47212A (fr) 2017-01-06 2019-11-13 Yumanity Therapeutics Inc Méthodes de traitement de troubles neurologiques
WO2019084157A1 (en) 2017-10-24 2019-05-02 Yumanity Therapeutics, Inc. COMPOUNDS AND USES THEREOF
ES3043183T3 (en) * 2018-03-23 2025-11-25 Janssen Pharmaceutica Nv Compounds and uses thereof
MA54829A (fr) 2019-01-24 2021-12-01 Yumanity Therapeutics Inc Composés et leurs utilisations
EA202192047A1 (ru) 2019-11-13 2021-12-08 Юманити Терапьютикс, Инк. Соединения и их применение
GB202012969D0 (en) * 2020-08-19 2020-09-30 Univ Of Oxford Inhibitor compounds

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101083994A (zh) * 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其用作硬脂酰CoA去饱和酶抑制剂的用途
CN101506203A (zh) * 2006-08-24 2009-08-12 诺瓦提斯公司 治疗代谢病、心血管病和其他病症的作为硬脂酰辅酶a脱饱和酶(scd)抑制剂的2-(吡嗪-2-基)-噻唑和2-(1h-吡唑-3-基)-噻唑衍生物及相关化合物
WO2009103739A1 (en) * 2008-02-20 2009-08-27 Novartis Ag Heterocyclic inhibitors of stearoyl-coa desaturase
CN101535303A (zh) * 2006-08-15 2009-09-16 诺瓦提斯公司 适合用于治疗与升高的脂质水平有关的疾病的杂环化合物

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE272650T1 (de) 1999-03-29 2004-08-15 Uutech Ltd Analoge des magensaft inhibierenden peptides und ihre verwendung für die behandlung von diabetes
DE60039111D1 (de) 1999-09-28 2008-07-17 Bayer Corp Agonisten des rezeptors 3 (r3) von pituitary adenylate cyclase aktivierendem peptid (pacap) und ihre pharmakologische verwendung
EP1315831B8 (en) 2000-02-24 2010-09-01 Xenon Pharmaceuticals Inc. Stearoyl-coa desaturase to identify triglyceride reducing therapeutic agents
EP1322767B1 (en) 2000-09-26 2008-07-23 Xenon Pharmaceuticals Inc. Methods and compositions employing a stearoyl-coa desaturase-hscd5
EP2289510A1 (en) * 2004-09-20 2011-03-02 Xenon Pharmaceuticals Inc. Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-coa desaturase enzymes
WO2007046867A2 (en) * 2005-05-19 2007-04-26 Xenon Pharmaceuticals Inc. Piperidine derivatives and their uses as therapeutic agents
MX2009003080A (es) * 2006-09-22 2009-04-02 Novartis Ag Compuestos organicos heterociclicos.
US8068738B2 (en) * 2007-02-21 2011-11-29 Tte Technology, Inc. System and method for decoding infra-red (IR) signals

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101083994A (zh) * 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其用作硬脂酰CoA去饱和酶抑制剂的用途
CN101535303A (zh) * 2006-08-15 2009-09-16 诺瓦提斯公司 适合用于治疗与升高的脂质水平有关的疾病的杂环化合物
CN101506203A (zh) * 2006-08-24 2009-08-12 诺瓦提斯公司 治疗代谢病、心血管病和其他病症的作为硬脂酰辅酶a脱饱和酶(scd)抑制剂的2-(吡嗪-2-基)-噻唑和2-(1h-吡唑-3-基)-噻唑衍生物及相关化合物
WO2009103739A1 (en) * 2008-02-20 2009-08-27 Novartis Ag Heterocyclic inhibitors of stearoyl-coa desaturase

Also Published As

Publication number Publication date
MA33693B1 (fr) 2012-10-01
IL218294A0 (en) 2012-04-30
CR20120134A (es) 2012-05-17
PH12012500648A1 (en) 2012-11-12
ZA201201390B (en) 2012-10-31
SG178869A1 (en) 2012-04-27
CL2012000797A1 (es) 2013-08-09
BR112012007509A2 (pt) 2016-11-22
TN2012000085A1 (en) 2013-09-19
IN2012DN01913A (enExample) 2015-07-24
AU2010302577A1 (en) 2012-03-15
CO6761294A2 (es) 2013-09-30
KR20120080226A (ko) 2012-07-16
MX2012003938A (es) 2012-08-03
WO2011039358A1 (en) 2011-04-07
CA2776294A1 (en) 2011-04-07
EP2483264A1 (en) 2012-08-08
ECSP12011837A (es) 2012-06-29
JP2013506638A (ja) 2013-02-28
US20130011361A1 (en) 2013-01-10
EA201200545A1 (ru) 2012-12-28
PE20121439A1 (es) 2012-11-06

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Address after: Basel

Applicant after: Novartis Ag

Applicant after: Xenon Pharmaceuticals Inc.

Address before: Basel

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Application publication date: 20120711