CN102388052A - 调节硬脂酰基-CoA去饱和酶的螺环衍生物 - Google Patents
调节硬脂酰基-CoA去饱和酶的螺环衍生物 Download PDFInfo
- Publication number
- CN102388052A CN102388052A CN2010800149196A CN201080014919A CN102388052A CN 102388052 A CN102388052 A CN 102388052A CN 2010800149196 A CN2010800149196 A CN 2010800149196A CN 201080014919 A CN201080014919 A CN 201080014919A CN 102388052 A CN102388052 A CN 102388052A
- Authority
- CN
- China
- Prior art keywords
- alkyl
- compound
- piperidine
- cycloalkyl
- pharmaceutically acceptable
- 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*c(nc(C)[s]1)c1I(C)C Chemical compound C*c(nc(C)[s]1)c1I(C)C 0.000 description 1
- XDTMQSROBMDMFD-UHFFFAOYSA-N C1CCCCC1 Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 description 1
- UWSHCXKRJOYEOD-UHFFFAOYSA-N CC(N(CC1)CCC11Oc2cc(F)ccc2CC1)=C Chemical compound CC(N(CC1)CCC11Oc2cc(F)ccc2CC1)=C UWSHCXKRJOYEOD-UHFFFAOYSA-N 0.000 description 1
- MGMHILKONGEISP-UHFFFAOYSA-N CCC(C)(CC)C(F)(F)F Chemical compound CCC(C)(CC)C(F)(F)F MGMHILKONGEISP-UHFFFAOYSA-N 0.000 description 1
- NNHJAGVJGIPACA-UHFFFAOYSA-N CCC(C1)C1(F)F Chemical compound CCC(C1)C1(F)F NNHJAGVJGIPACA-UHFFFAOYSA-N 0.000 description 1
- DJDHHXDFKSLEQY-UHFFFAOYSA-N Cc1cc(C(O)=O)cnc1 Chemical compound Cc1cc(C(O)=O)cnc1 DJDHHXDFKSLEQY-UHFFFAOYSA-N 0.000 description 1
- XKVUYEYANWFIJX-UHFFFAOYSA-N Cc1n[nH]cc1 Chemical compound Cc1n[nH]cc1 XKVUYEYANWFIJX-UHFFFAOYSA-N 0.000 description 1
- HNJOAIYFUCQZAA-UHFFFAOYSA-N Cc1n[o]c(C)n1 Chemical compound Cc1n[o]c(C)n1 HNJOAIYFUCQZAA-UHFFFAOYSA-N 0.000 description 1
- XYYXDARQOHWBPO-UHFFFAOYSA-N Cc1nnc(C)[nH]1 Chemical compound Cc1nnc(C)[nH]1 XYYXDARQOHWBPO-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
-
- 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
- A61P17/06—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
- A61P17/08—Antiseborrheics
-
- 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
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
-
- 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
-
- 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
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Child & Adolescent Psychology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16555309P | 2009-04-01 | 2009-04-01 | |
| US61/165,553 | 2009-04-01 | ||
| PCT/EP2010/054234 WO2010112520A1 (en) | 2009-04-01 | 2010-03-30 | Spiro derivatives for the modulation of stearoyl-coa desaturase |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102388052A true CN102388052A (zh) | 2012-03-21 |
Family
ID=42224469
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2010800149196A Pending CN102388052A (zh) | 2009-04-01 | 2010-03-30 | 调节硬脂酰基-CoA去饱和酶的螺环衍生物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20120010135A1 (enExample) |
| EP (1) | EP2414366A1 (enExample) |
| JP (1) | JP2012522748A (enExample) |
| CN (1) | CN102388052A (enExample) |
| WO (1) | WO2010112520A1 (enExample) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105503725A (zh) * | 2015-12-30 | 2016-04-20 | 天津药明康德新药开发有限公司 | 一种叔丁基1-羟基-8-氮杂螺烷[4,5]葵烷-8-羧酸酯的制备方法 |
| CN112174935A (zh) * | 2018-05-09 | 2021-01-05 | 北京加科思新药研发有限公司 | 可用作shp2抑制剂的新型杂环衍生物 |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2766000A2 (en) | 2011-10-15 | 2014-08-20 | F.Hoffmann-La Roche Ag | Scd1 antagonists for treating cancer |
| PT3319959T (pt) | 2015-07-06 | 2021-12-06 | Alkermes Inc | Inibidores hetero-halo de histona desacetilase |
| EP3319968A1 (en) | 2015-07-06 | 2018-05-16 | Rodin Therapeutics, Inc. | Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase |
| US11970486B2 (en) | 2016-10-24 | 2024-04-30 | Janssen Pharmaceutica Nv | Compounds and uses thereof |
| JP2020514293A (ja) | 2017-01-06 | 2020-05-21 | ユマニティ セラピューティクス,インコーポレーテッド | 神経障害を治療する方法 |
| CA3049443A1 (en) | 2017-01-11 | 2018-07-19 | Rodin Therapeutics, Inc. | Bicyclic inhibitors of histone deacetylase |
| JP7152471B2 (ja) | 2017-08-07 | 2022-10-12 | ロダン・セラピューティクス,インコーポレーテッド | ヒストン脱アセチル化酵素の二環阻害剤 |
| CA3083000A1 (en) | 2017-10-24 | 2019-05-02 | Yumanity Therapeutics, Inc. | Compounds and uses thereof |
| EP3768269B1 (en) | 2018-03-23 | 2025-08-20 | Janssen Pharmaceutica NV | Compounds and uses thereof |
| MX2021008903A (es) | 2019-01-24 | 2021-11-04 | Yumanity Therapeutics Inc | Compuestos y usos de los mismos. |
| EA202192047A1 (ru) | 2019-11-13 | 2021-12-08 | Юманити Терапьютикс, Инк. | Соединения и их применение |
| EP4547244A1 (en) * | 2022-06-28 | 2025-05-07 | Modulation Therapeutics, Inc. | Scd1 inhibitors for treating liver disease |
| WO2025018978A1 (en) * | 2023-07-14 | 2025-01-23 | Modulation Therapeutics, Inc. | Scd1 inhibitors for treating hematolymphoid neoplasms |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060199802A1 (en) * | 2003-07-30 | 2006-09-07 | Melwyn Abreo | Pyridyl derivatives and their use as therapeutic agents |
| WO2007027532A2 (en) * | 2005-08-29 | 2007-03-08 | Merck & Co., Inc. | Niacin receptor agonists, compositions containing such compounds and methods of treatment |
| WO2009037542A2 (en) * | 2007-09-20 | 2009-03-26 | Glenmark Pharmaceuticals, S.A. | Spirocyclic compounds as stearoyl coa desaturase inhibitors |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60012721D1 (de) | 1999-03-29 | 2004-09-09 | Uutech Ltd | Analoge des magensaft inhibierenden peptides und ihre verwendung für die behandlung von diabetes |
| RU2269354C2 (ru) | 1999-09-28 | 2006-02-10 | Байер Корпорейшн | Агонисты рецептора-3(r3) пептида-активатора гипофизарной аденилатциклазы(расар) и способы их фармакологического применения |
| CA2398940C (en) | 2000-02-24 | 2012-02-21 | Xenon Genetics, Inc. | Methods and compositions using stearoyl-coa desaturase to identify triglyceride reducing therapeutic agents |
| CA2423885A1 (en) | 2000-09-29 | 2003-03-27 | Shionogi & Co., Ltd. | Thiazole and oxazole derivatives |
| WO2010103381A1 (en) * | 2009-03-13 | 2010-09-16 | Glenmark Pharmaceuticals S.A. | Spirocyclic piperidine derivatives as trpm 8 modulators |
-
2010
- 2010-03-30 US US13/258,121 patent/US20120010135A1/en not_active Abandoned
- 2010-03-30 EP EP10712932A patent/EP2414366A1/en not_active Withdrawn
- 2010-03-30 WO PCT/EP2010/054234 patent/WO2010112520A1/en not_active Ceased
- 2010-03-30 JP JP2012502648A patent/JP2012522748A/ja not_active Withdrawn
- 2010-03-30 CN CN2010800149196A patent/CN102388052A/zh active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060199802A1 (en) * | 2003-07-30 | 2006-09-07 | Melwyn Abreo | Pyridyl derivatives and their use as therapeutic agents |
| WO2007027532A2 (en) * | 2005-08-29 | 2007-03-08 | Merck & Co., Inc. | Niacin receptor agonists, compositions containing such compounds and methods of treatment |
| WO2009037542A2 (en) * | 2007-09-20 | 2009-03-26 | Glenmark Pharmaceuticals, S.A. | Spirocyclic compounds as stearoyl coa desaturase inhibitors |
Non-Patent Citations (1)
| Title |
|---|
| HONGYU ZHAO,等: "Discovery of 1-(4-phenoxypiperidin-1-yl)-2-arylaminoethanone stearoyl-CoA desaturase 1 inhibitors", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》 * |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105503725A (zh) * | 2015-12-30 | 2016-04-20 | 天津药明康德新药开发有限公司 | 一种叔丁基1-羟基-8-氮杂螺烷[4,5]葵烷-8-羧酸酯的制备方法 |
| CN105503725B (zh) * | 2015-12-30 | 2018-03-27 | 天津药明康德新药开发有限公司 | 一种叔丁基1‑羟基‑8‑氮杂螺烷[4,5]葵烷‑8‑羧酸酯的制备方法 |
| CN112174935A (zh) * | 2018-05-09 | 2021-01-05 | 北京加科思新药研发有限公司 | 可用作shp2抑制剂的新型杂环衍生物 |
| CN112174935B (zh) * | 2018-05-09 | 2022-12-06 | 北京加科思新药研发有限公司 | 可用作shp2抑制剂的杂环衍生物 |
| CN115969853A (zh) * | 2018-05-09 | 2023-04-18 | 北京加科思新药研发有限公司 | 可用作shp2抑制剂的新型杂环衍生物 |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2010112520A1 (en) | 2010-10-07 |
| US20120010135A1 (en) | 2012-01-12 |
| EP2414366A1 (en) | 2012-02-08 |
| JP2012522748A (ja) | 2012-09-27 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN102388052A (zh) | 调节硬脂酰基-CoA去饱和酶的螺环衍生物 | |
| CN101516877B (zh) | 杂环有机化合物 | |
| JP5043668B2 (ja) | 複素環誘導体および治療薬としてのそれらの使用 | |
| EP2086970B1 (en) | 2-(pyrazin-2-yl)-thiazole and 2-(1h pyrazol-3-yl)-thiazole derivatives as well as related compounds as stearoyl-coa desaturase (scd) inhibitors for the treatment of metabolic, cardiovascular and other disorders | |
| JP4958787B2 (ja) | ヒトステアロイル−CoAデサチュラーゼを阻害するためのピリジン誘導体 | |
| CN101595105B (zh) | 作为scd抑制剂的2-取代的5元杂环化合物 | |
| EP2245029B1 (en) | Heterocyclic inhibitors of stearoyl-coa desaturase | |
| JP2008513506A (ja) | ヒトステアロイル−CoAデサチュラーゼを阻害するためのピリダジン誘導体 | |
| JP2008513499A (ja) | ステアロイル−CoAデサチュラーゼ酵素によって媒介される疾患の処置のための複素環誘導体 | |
| CN101460476A (zh) | 有机化合物 | |
| US20130011361A1 (en) | Pyrazole derivatives which modulate stearoyl-coa desaturase |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 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. |
|
| COR | Change of bibliographic data |
Free format text: CORRECT: APPLICANT; FROM: NOVARTIS AG TO: NOVARTIS CO., LTD. |
|
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20120321 |