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 PDFInfo
- 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
- Authority
- CN
- China
- Prior art keywords
- alkyl
- aryl
- optionally substituted
- cycloalkyl
- heteroaryl
- 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.)
- Pending
Links
- 0 *C(N1**=C)=NN(*)C1=O Chemical compound *C(N1**=C)=NN(*)C1=O 0.000 description 9
- DMWDZKMQGXHKAB-UHFFFAOYSA-N CC(C)CC(C1)C1(F)F Chemical compound CC(C)CC(C1)C1(F)F DMWDZKMQGXHKAB-UHFFFAOYSA-N 0.000 description 1
- RECTWDFRONTKHG-UHFFFAOYSA-N CN(CCN1C)C1O Chemical compound CN(CCN1C)C1O RECTWDFRONTKHG-UHFFFAOYSA-N 0.000 description 1
- LEMNNWHYKOYDMZ-UHFFFAOYSA-N COc1ccc(C[n](c(C(NCc(cc2F)ccc2F)=O)c2)nc2N(C=NN2Cc(cc3)ccc3F)C2=O)cc1 Chemical compound COc1ccc(C[n](c(C(NCc(cc2F)ccc2F)=O)c2)nc2N(C=NN2Cc(cc3)ccc3F)C2=O)cc1 LEMNNWHYKOYDMZ-UHFFFAOYSA-N 0.000 description 1
- JZCLAEDJPSTYEQ-UHFFFAOYSA-N O=C(c1cc(N(CCN2Cc(cc3)ccc3F)C2=O)n[nH]1)NCc1ccccn1 Chemical compound O=C(c1cc(N(CCN2Cc(cc3)ccc3F)C2=O)n[nH]1)NCc1ccccn1 JZCLAEDJPSTYEQ-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (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)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Vascular Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Nutrition Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
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)
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2850836A1 (en) | 2011-10-15 | 2013-04-18 | Genentech, Inc. | Methods of using scd1 antagonists |
| CN117777121A (zh) | 2016-10-24 | 2024-03-29 | 詹森药业有限公司 | 化合物及其用途 |
| MA47212A (fr) | 2017-01-06 | 2019-11-13 | Yumanity Therapeutics Inc | Méthodes de traitement de troubles neurologiques |
| EP3700934A4 (en) | 2017-10-24 | 2021-10-27 | Yumanity Therapeutics, Inc. | COMPOUNDS AND USES OF THESE COMPOUNDS |
| CN112312913B (zh) * | 2018-03-23 | 2024-03-08 | 詹森药业有限公司 | 化合物和其用途 |
| SG11202108079RA (en) | 2019-01-24 | 2021-08-30 | Yumanity Therapeutics Inc | Compounds and uses thereof |
| 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)
| 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU3441400A (en) | 1999-03-29 | 2000-10-16 | Uutech Limited | Peptide |
| ES2307534T3 (es) | 1999-09-28 | 2008-12-01 | Bayer Corporation | Agonistas de receptores 3 (r3) del peptido activador de la adenilato ciclasa hipofisiaria (pacap) y sus metodos de uso farmacologicos. |
| AU2001247228B2 (en) | 2000-02-24 | 2007-01-18 | Wisconsin Alumni Research Foundation | Stearoyl-CoA desaturase to identify triglyceride reducing therapeutic agents |
| CA2430987A1 (en) | 2000-09-26 | 2002-04-04 | Xenon Genetics, Inc. | Methods and compositions employing a novel stearoyl-coa desaturase-hscd5 |
| AR051026A1 (es) * | 2004-09-20 | 2006-12-13 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa |
| WO2007046867A2 (en) * | 2005-05-19 | 2007-04-26 | Xenon Pharmaceuticals Inc. | Piperidine derivatives and their uses as therapeutic agents |
| WO2008036715A1 (en) * | 2006-09-22 | 2008-03-27 | Novartis Ag | Heterocyclic organic compounds |
| US8068738B2 (en) * | 2007-02-21 | 2011-11-29 | Tte Technology, Inc. | System and method for decoding infra-red (IR) signals |
-
2010
- 2010-10-01 CA CA2776294A patent/CA2776294A1/en not_active Abandoned
- 2010-10-01 JP JP2012531447A patent/JP2013506638A/ja active Pending
- 2010-10-01 CN CN201080044452XA patent/CN102574841A/zh active Pending
- 2010-10-01 EP EP10761003A patent/EP2483264A1/en not_active Withdrawn
- 2010-10-01 WO PCT/EP2010/064672 patent/WO2011039358A1/en not_active Ceased
- 2010-10-01 BR BR112012007509A patent/BR112012007509A2/pt not_active IP Right Cessation
- 2010-10-01 KR KR1020127011127A patent/KR20120080226A/ko not_active Ceased
- 2010-10-01 AU AU2010302577A patent/AU2010302577A1/en not_active Abandoned
- 2010-10-01 MX MX2012003938A patent/MX2012003938A/es not_active Application Discontinuation
- 2010-10-01 EA EA201200545A patent/EA201200545A1/ru unknown
- 2010-10-01 PE PE2012000427A patent/PE20121439A1/es not_active Application Discontinuation
- 2010-10-01 PH PH1/2012/500648A patent/PH12012500648A1/en unknown
- 2010-10-01 IN IN1913DEN2012 patent/IN2012DN01913A/en unknown
- 2010-10-01 US US13/391,900 patent/US20130011361A1/en not_active Abandoned
- 2010-10-01 SG SG2012013066A patent/SG178869A1/en unknown
-
2012
- 2012-02-21 TN TNP2012000085A patent/TN2012000085A1/en unknown
- 2012-02-23 IL IL218294A patent/IL218294A0/en unknown
- 2012-02-24 ZA ZA2012/01390A patent/ZA201201390B/en unknown
- 2012-03-20 CR CR20120134A patent/CR20120134A/es unknown
- 2012-03-30 CL CL2012000797A patent/CL2012000797A1/es unknown
- 2012-04-03 CO CO12056222A patent/CO6761294A2/es not_active Application Discontinuation
- 2012-04-26 MA MA34807A patent/MA33693B1/fr unknown
- 2012-04-27 EC ECSP12011837 patent/ECSP12011837A/es unknown
Patent Citations (4)
| 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 |
| BR112012007509A2 (pt) | 2016-11-22 |
| AU2010302577A1 (en) | 2012-03-15 |
| ECSP12011837A (es) | 2012-06-29 |
| CL2012000797A1 (es) | 2013-08-09 |
| US20130011361A1 (en) | 2013-01-10 |
| MX2012003938A (es) | 2012-08-03 |
| PE20121439A1 (es) | 2012-11-06 |
| IN2012DN01913A (cg-RX-API-DMAC7.html) | 2015-07-24 |
| SG178869A1 (en) | 2012-04-27 |
| CR20120134A (es) | 2012-05-17 |
| IL218294A0 (en) | 2012-04-30 |
| WO2011039358A1 (en) | 2011-04-07 |
| TN2012000085A1 (en) | 2013-09-19 |
| ZA201201390B (en) | 2012-10-31 |
| PH12012500648A1 (en) | 2012-11-12 |
| KR20120080226A (ko) | 2012-07-16 |
| CA2776294A1 (en) | 2011-04-07 |
| CO6761294A2 (es) | 2013-09-30 |
| JP2013506638A (ja) | 2013-02-28 |
| EP2483264A1 (en) | 2012-08-08 |
| EA201200545A1 (ru) | 2012-12-28 |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C53 | Correction of patent of invention or patent application | ||
| CB02 | Change of applicant information |
Address after: Basel Applicant after: Novartis Ag Applicant after: Xenon Pharmaceuticals Inc. Address before: Basel Applicant before: Novartis AG Applicant before: Xenon Pharmaceuticals Inc. |
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| COR | Change of bibliographic data |
Free format text: CORRECT: APPLICANT; FROM: NOVARTIS AG TO: NOVARTIS CO., LTD. |
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20120711 |