CN110945002A - 作为RORγ抑制剂的双环化合物 - Google Patents

作为RORγ抑制剂的双环化合物 Download PDF

Info

Publication number
CN110945002A
CN110945002A CN201880047103.XA CN201880047103A CN110945002A CN 110945002 A CN110945002 A CN 110945002A CN 201880047103 A CN201880047103 A CN 201880047103A CN 110945002 A CN110945002 A CN 110945002A
Authority
CN
China
Prior art keywords
compound
group
hydrogen
formula
alkyl
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.)
Granted
Application number
CN201880047103.XA
Other languages
English (en)
Other versions
CN110945002B (zh
Inventor
陈新海
周凯
于衍新
胡伯羽
吴灵慧
陈小员
林江凤
陈浩民
王祥建
张喜全
田心
徐宏江
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.)
Chia Tai Tianqing Pharmaceutical Group Co Ltd
Medshine Discovery Inc
Original Assignee
Chia Tai Tianqing Pharmaceutical Group Co Ltd
Medshine Discovery 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
Application filed by Chia Tai Tianqing Pharmaceutical Group Co Ltd, Medshine Discovery Inc filed Critical Chia Tai Tianqing Pharmaceutical Group Co Ltd
Publication of CN110945002A publication Critical patent/CN110945002A/zh
Application granted granted Critical
Publication of CN110945002B publication Critical patent/CN110945002B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D515/04—Ortho-condensed systems

Abstract

一种作为RORγ抑制剂的双环化合物，提供式(I)化合物或其药学上可接受的盐，其具有式(I‑A)或式(I‑B)所示的结构，所提供的式(I‑A)化合物、式(I‑B)或其药学上可接受的盐具有良好的RORγ抑制活性，有望用于治疗哺乳动物由RORγ受体介导的疾病。

Description

PCT国内申请，说明书已公开。

Claims (18)

  1. PCT国内申请，权利要求书已公开。
CN201880047103.XA 2017-08-01 2018-07-27 作为RORγ抑制剂的双环化合物 Active CN110945002B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201710650300 2017-08-01
CN2017106503008 2017-08-01
PCT/CN2018/097551 WO2019024809A1 (zh) 2017-08-01 2018-07-27 作为RORγ抑制剂的双环化合物

Publications (2)

Publication Number Publication Date
CN110945002A true CN110945002A (zh) 2020-03-31
CN110945002B CN110945002B (zh) 2021-12-24

Family

ID=65233479

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880047103.XA Active CN110945002B (zh) 2017-08-01 2018-07-27 作为RORγ抑制剂的双环化合物

Country Status (4)

Country Link
US (1) US11466024B2 (zh)
EP (1) EP3663299B1 (zh)
CN (1) CN110945002B (zh)
WO (1) WO2019024809A1 (zh)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111484505B (zh) * 2019-01-28 2022-11-15 正大天晴药业集团股份有限公司 一种双环RORγ抑制剂的盐酸盐结晶型
CN111606844A (zh) * 2020-05-29 2020-09-01 江西富祥药业股份有限公司 一种瑞利巴坦中间体的制备方法

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004007504A1 (en) * 2002-07-17 2004-01-22 Pharmacia Italia S.P.A. Heterobicyclic pyrazole derivatives as kinase inhibitors
US20050026984A1 (en) * 2003-07-29 2005-02-03 Aventis Pharma S.A. Substituted thieno [2,3-c] pyrazoles and their use as medicinal products
WO2007009898A1 (en) * 2005-07-19 2007-01-25 Nerviano Medical Sciences S.R.L. 1h-thieno[2,3-c]pyrazole compounds useful as kinase inhibitors
CN1946395A (zh) * 2004-02-03 2007-04-11 辉瑞意大利有限公司 用作激酶抑制剂的1H－噻吩并[2,3－c]吡唑衍生物
WO2007113198A2 (en) * 2006-03-30 2007-10-11 Nerviano Medical Sciences S.R.L. Use of a kinase inhibitor for the treatment of particular resistant tumors
WO2015008234A1 (en) * 2013-07-17 2015-01-22 Glenmark Pharmaceuticals S.A. Bicyclic heterocyclic compounds as ror gamma modulators
WO2015101928A1 (en) * 2013-12-31 2015-07-09 Aurigene Discovery Technologies Limited Fused thiophene and thiazole derivatives as ror gamma modulators
CN105980364A (zh) * 2013-12-10 2016-09-28 格兰马克药品股份有限公司 可用作RORγ调节剂的双环杂芳基吲哚类似物
US20170008910A1 (en) * 2013-05-01 2017-01-12 Vitae Pharmaceuticals, Inc. Thiazolopyrrolidine inhibitors of ror-gamma
WO2017075178A1 (en) * 2015-10-27 2017-05-04 Merck Sharp & Dohme Corp. SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201116641D0 (en) 2011-09-27 2011-11-09 Glaxo Group Ltd Novel compounds
GB201207406D0 (en) 2012-04-27 2012-06-13 Glaxo Group Ltd Novel compounds
WO2013160418A1 (en) 2012-04-27 2013-10-31 Glaxo Group Limited Novel compounds
EP3527569B1 (en) 2014-02-03 2021-08-25 Vitae Pharmaceuticals, LLC Dihydropyrrolopyridine inhibitors of ror-gamma for use in treating drye eye
PT3207043T (pt) 2014-10-14 2019-03-25 Vitae Pharmaceuticals Llc Inibidores de di-hidropirrolopiridina de ror-gama
CR20200618A (es) * 2018-06-19 2021-01-21 Novartis Ag Derivados de tetrahidrotienopiridina n-sustituidos y sus usos

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004007504A1 (en) * 2002-07-17 2004-01-22 Pharmacia Italia S.P.A. Heterobicyclic pyrazole derivatives as kinase inhibitors
US20050026984A1 (en) * 2003-07-29 2005-02-03 Aventis Pharma S.A. Substituted thieno [2,3-c] pyrazoles and their use as medicinal products
CN1946395A (zh) * 2004-02-03 2007-04-11 辉瑞意大利有限公司 用作激酶抑制剂的1H－噻吩并[2,3－c]吡唑衍生物
WO2007009898A1 (en) * 2005-07-19 2007-01-25 Nerviano Medical Sciences S.R.L. 1h-thieno[2,3-c]pyrazole compounds useful as kinase inhibitors
WO2007113198A2 (en) * 2006-03-30 2007-10-11 Nerviano Medical Sciences S.R.L. Use of a kinase inhibitor for the treatment of particular resistant tumors
US20170008910A1 (en) * 2013-05-01 2017-01-12 Vitae Pharmaceuticals, Inc. Thiazolopyrrolidine inhibitors of ror-gamma
WO2015008234A1 (en) * 2013-07-17 2015-01-22 Glenmark Pharmaceuticals S.A. Bicyclic heterocyclic compounds as ror gamma modulators
CN105980364A (zh) * 2013-12-10 2016-09-28 格兰马克药品股份有限公司 可用作RORγ调节剂的双环杂芳基吲哚类似物
WO2015101928A1 (en) * 2013-12-31 2015-07-09 Aurigene Discovery Technologies Limited Fused thiophene and thiazole derivatives as ror gamma modulators
WO2017075178A1 (en) * 2015-10-27 2017-05-04 Merck Sharp & Dohme Corp. SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
CHRISTIAN GEGE: "Retinoid-related orphan receptor γt modulators:comparison of Glenmark’s me-too patent application (WO2015008234) with the originator application from Merck Sharp and Dohme (WO2012106995)", 《EXPERT OPIN. THER. PATENTS》 *
COLUMBUS, OHIO, US REGISTRY[ONLINE]: "STN检索报告", 《STN REGISTRY》 *
JING CUI，ET AL.: "BCR-ABL tyrosine kinase inhibitor pharmacophore model derived from a series of phenylaminopyrimidine-based (PAP) derivatives", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》 *
王威 等: "核受体RORγt抑制剂的发现及对IL-17A表达影响的研究", 《免疫学杂志》 *

Also Published As

Publication number Publication date
EP3663299A4 (en) 2021-03-31
US20200231597A1 (en) 2020-07-23
CN110945002B (zh) 2021-12-24
EP3663299A1 (en) 2020-06-10
WO2019024809A1 (zh) 2019-02-07
EP3663299B1 (en) 2023-03-08
US11466024B2 (en) 2022-10-11

Similar Documents

Publication Publication Date Title
KR102089234B1 (ko) Ask1 억제제로서의 피리딘 유도체 및 이의 제조방법과 용도
EP3177611B1 (en) Optionally fused heterocyclyl-substituted derivatives of pyrimidine useful for the treatment of inflammatory, metabolic, oncologic and autoimmune diseases
WO2020048547A1 (zh) 三环并呋喃取代哌啶二酮类化合物
BR102018002879A2 (pt) composto, e, método para tratamento de uma doença ou distúrbio relacionado com a inflamação em um paciente em necessidade do mesmo.
US11453644B1 (en) Compounds
US11866433B2 (en) Diarylthiohydantoin compound as androgen receptor antagonist
US20160122358A1 (en) Novel substituted pyrazolo-piperazines as casein kinase 1 d/e inhibitors
EP3762368B1 (en) Aminopyrazine diol compounds as pi3k-y inhibitors
CN114616232A (zh) 氮杂环庚烷并嘧啶类衍生物及其医药用途
EA035168B1 (ru) Полициклические соединения в качестве ингибиторов тирозинкиназы брутона
IL259862A (en) Brutonine Tyrosine Kinase Inhibitors and Methods of Using Them
EP3766882A1 (en) Phthalazine isoxazole alkoxy derivatives, preparation method thereof, pharmaceutical composition and use thereof
JP2021119163A (ja) メマンチン化合物及びその調整並びにその使用
CN111902417A (zh) 一种二芳基巨环化合物、药物组合物以及其用途
EP3929185A1 (en) Nitrogen-containing fused cyclic compound, preparation method therefor and use thereof
CN113166061B (zh) 含有磺酰基结构的RORγ抑制剂
CN110945002B (zh) 作为RORγ抑制剂的双环化合物
CN114206850A (zh) 作为crac抑制剂的2h-苯并吡喃衍生物
EP4223751A1 (en) Benzamide compound and use thereof
WO2020057604A1 (zh) Tlr8激动剂
JPWO2019235553A1 (ja) アゼチジン誘導体及びそのプロドラッグ
TWI652265B (zh) 氮雜吲哚衍生物
CN114685532A (zh) 大环类化合物及其医药用途
EP3686197B1 (en) 2-substituted pyrazole amino-4-substituted amino-5-pyrimidine formamide compound, composition, and application thereof
CN109206423B (zh) 作为RORγ抑制剂的硫代酰胺取代的二氢吡咯并吡啶化合物

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant