CN105555768B - RORγ调节剂 - Google Patents

RORγ调节剂 Download PDF

Info

Publication number
CN105555768B
CN105555768B CN201480051836.2A CN201480051836A CN105555768B CN 105555768 B CN105555768 B CN 105555768B CN 201480051836 A CN201480051836 A CN 201480051836A CN 105555768 B CN105555768 B CN 105555768B
Authority
CN
China
Prior art keywords
sulfonyl
bases
hexafluoro
methyl
fluorophenyls
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.)
Expired - Fee Related
Application number
CN201480051836.2A
Other languages
English (en)
Chinese (zh)
Other versions
CN105555768A (zh
Inventor
T·G·M·达尔
段敬武
龚华
江斌
陆忠辉
D·S·温斯坦
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.)
Bristol Myers Squibb Co
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of CN105555768A publication Critical patent/CN105555768A/zh
Application granted granted Critical
Publication of CN105555768B publication Critical patent/CN105555768B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • 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
    • A61P37/08—Antiallergic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/58—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
CN201480051836.2A 2013-09-20 2014-09-18 RORγ调节剂 Expired - Fee Related CN105555768B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361880391P 2013-09-20 2013-09-20
US61/880,391 2013-09-20
PCT/US2014/056197 WO2015042212A1 (en) 2013-09-20 2014-09-18 RORγ MODULATORS

Publications (2)

Publication Number Publication Date
CN105555768A CN105555768A (zh) 2016-05-04
CN105555768B true CN105555768B (zh) 2018-10-16

Family

ID=51726859

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201480051836.2A Expired - Fee Related CN105555768B (zh) 2013-09-20 2014-09-18 RORγ调节剂

Country Status (5)

Country Link
US (1) US9725443B2 (https=)
EP (1) EP3046906B1 (https=)
JP (1) JP6397488B2 (https=)
CN (1) CN105555768B (https=)
WO (1) WO2015042212A1 (https=)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6407285B2 (ja) 2013-09-09 2018-10-17 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ＲＯＲγ調節因子
JP6397488B2 (ja) 2013-09-20 2018-09-26 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ＲＯＲγ調節因子
JP6463362B2 (ja) * 2013-12-19 2019-01-30 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ ＲＯＲ−ガンマ阻害剤としてのテトラヒドロ−テトラゾロ［１，５−ａ］ピラジン
CN106061947B (zh) 2014-01-06 2019-12-03 百时美施贵宝公司 环己基砜RORγ调节剂
WO2015103508A1 (en) 2014-01-06 2015-07-09 Bristol-Myers Squibb Company CARBOCYCLIC SULFONE RORγ MODULATORS
WO2015103510A1 (en) 2014-01-06 2015-07-09 Bristol-Myers Squibb Company Heterocyclic sulfone as ror-gamma modulators
WO2016069978A1 (en) 2014-10-30 2016-05-06 Janssen Pharmaceutica Nv AMIDE SUBSTITUTED THIAZOLES AS MODULATORS OF RORγT
EP3212641B1 (en) 2014-10-30 2018-12-05 Janssen Pharmaceutica NV Thiazoles as modulators of roryt
TWI667230B (zh) 2014-10-30 2019-08-01 比利時商健生藥品公司 用作ＲＯＲγｔ調節劑之三氟甲基醇
KR102114536B1 (ko) 2015-05-07 2020-05-22 브리스톨-마이어스 스큅 컴퍼니 RORγ 조정제로서의 트리시클릭 술폰
TW201803869A (zh) 2016-04-27 2018-02-01 健生藥品公司 作為ＲＯＲγＴ調節劑之６－胺基吡啶－３－基噻唑
WO2017213210A1 (ja) * 2016-06-10 2017-12-14 武田薬品工業株式会社 複素環化合物
ES2872005T3 (es) * 2016-10-13 2021-11-02 Bristol Myers Squibb Co Sulfonas heterocíclicas como moduladores de ROR gamma
CA3103770A1 (en) 2018-06-18 2019-12-26 Janssen Pharmaceutica Nv Phenyl and pyridinyl substituted imidazoles as modulators of roryt
ES2925473T3 (es) 2018-06-18 2022-10-18 Janssen Pharmaceutica Nv Pirazoles de piridinilo como moduladores de RORyt
EP3806958B1 (en) 2018-06-18 2022-09-07 Janssen Pharmaceutica NV 6-aminopyridin-3-yl pyrazoles as modulators of roryt
JP2021528405A (ja) 2018-06-18 2021-10-21 ヤンセン ファーマシューティカ エヌ．ベー． ＲＯＲγｔのモジュレータとしてのアミド置換チアゾール
CN111635373B (zh) * 2019-03-01 2022-07-12 山东轩竹医药科技有限公司 多环磺酰胺类RORγ调节剂

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1564820A (zh) * 2001-10-05 2005-01-12 瑞蔻达蒂股份有限公司 用于治疗泌尿道疾病的杂环化合物
WO2007050425A2 (en) * 2005-10-21 2007-05-03 Bristol-Myers Squibb Company Lxr modulators
EP2368886A1 (en) * 2010-03-01 2011-09-28 Phenex Pharmaceuticals AG Novel compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (ROR gamma, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune desease
WO2012064744A2 (en) * 2010-11-08 2012-05-18 Lycera Corporation Tetrahydroquinoline and related bicyclic compounds for inhibition of rorϒ activity and the treatment of disease
WO2013064231A1 (en) * 2011-10-31 2013-05-10 Phenex Pharmaceuticals Ag SEVEN-MEMBERED SULFONAMIDES AS MODULATORS OF RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORγ, NR1F3)

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10035790B2 (en) 2012-10-19 2018-07-31 Exelixis, Inc. RORγ modulators
JP6407285B2 (ja) 2013-09-09 2018-10-17 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ＲＯＲγ調節因子
JP6397488B2 (ja) 2013-09-20 2018-09-26 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ＲＯＲγ調節因子
KR101544975B1 (ko) * 2013-09-30 2015-08-18 주식회사 플라즈마트 임피던스 매칭 방법 및 임피던스 매칭 시스템
CN106061947B (zh) 2014-01-06 2019-12-03 百时美施贵宝公司 环己基砜RORγ调节剂
WO2015103508A1 (en) 2014-01-06 2015-07-09 Bristol-Myers Squibb Company CARBOCYCLIC SULFONE RORγ MODULATORS
WO2015103509A1 (en) 2014-01-06 2015-07-09 Bristol-Myers Squibb Company Pyrrolidinyl sulfone derivatives and their use as ror gamma modulators
WO2015103510A1 (en) 2014-01-06 2015-07-09 Bristol-Myers Squibb Company Heterocyclic sulfone as ror-gamma modulators

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1564820A (zh) * 2001-10-05 2005-01-12 瑞蔻达蒂股份有限公司 用于治疗泌尿道疾病的杂环化合物
WO2007050425A2 (en) * 2005-10-21 2007-05-03 Bristol-Myers Squibb Company Lxr modulators
EP2368886A1 (en) * 2010-03-01 2011-09-28 Phenex Pharmaceuticals AG Novel compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (ROR gamma, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune desease
WO2012064744A2 (en) * 2010-11-08 2012-05-18 Lycera Corporation Tetrahydroquinoline and related bicyclic compounds for inhibition of rorϒ activity and the treatment of disease
WO2013064231A1 (en) * 2011-10-31 2013-05-10 Phenex Pharmaceuticals Ag SEVEN-MEMBERED SULFONAMIDES AS MODULATORS OF RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORγ, NR1F3)

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Ring Opening/C-N Cyclization of Activated Aziridines with Carbon Nucleophiles: Highly Diastereo- and Enantioselective Synthesis of Tetrahydroquinolines;Manas K. Ghorai et al;《ORGANIC LETTER》;20110718;第13卷(第16期);4256-4259 *
Solid-Phase Synthesis of Heterocycles via Palladium-Catalyzed Annulation;Yao Wang et al;《Tetrahedron Letters》;19981224;第39卷;9605-9608 *
Tetrahydroquinoline sulfonamides as γ-secretase inhibitors;Theodros Asberom et al;《Bioorganic & Medicinal Chemistry Letters》;20061012;第17卷;205-207 *

Also Published As

Publication number Publication date
EP3046906B1 (en) 2017-08-16
US20160229844A1 (en) 2016-08-11
CN105555768A (zh) 2016-05-04
EP3046906A1 (en) 2016-07-27
US9725443B2 (en) 2017-08-08
JP6397488B2 (ja) 2018-09-26
WO2015042212A1 (en) 2015-03-26
JP2016530213A (ja) 2016-09-29

Similar Documents

Publication Publication Date Title
CN105555768B (zh) RORγ调节剂
CN111032655B (zh) Egfr和/或her2抑制剂和使用方法
JP6407285B2 (ja) ＲＯＲγ調節因子
CN105229003B (zh) 作为补体因子b抑制剂用于治疗眼科疾病的2‑(1h‑吲哚‑4‑基甲基)‑3h‑咪唑并[4,5‑b]吡啶‑6‑甲腈衍生物
CN106061947B (zh) 环己基砜RORγ调节剂
CN106132931B (zh) 碳环砜RORγ调节剂
CN111018861B (zh) 吡咯并嘧啶化合物
AU2021389180A9 (en) Heteroaryl carboxamide compound
CN1938307A (zh) 9－取代的8－氧化腺嘌呤
US20250066322A1 (en) Substituted heterocyclic compounds
CN111936139A (zh) 6-氨基异喹啉的单(酸)盐及其用途
US20230035184A1 (en) Diarylthiohydantoin compound as androgen receptor antagonist
EP4175642A1 (en) Compounds, compositions and methods
US20240270723A1 (en) Substituted heterocyclic compounds
EP3274335A1 (en) Aminoindazole derivatives as sodium channel inhibitors
EP3999499A1 (en) Prodrugs in the modulation of interleukin
US10435369B2 (en) Tricyclic sulfones as ROR gamma modulators
EP4289833A1 (en) Tyk2 inhibitor compound containing bicyclic ring
CN114222744B (zh) 可用作IL-12、IL-23和/或IFNα反应调节剂的咪唑并哒嗪化合物
CN117279906A (zh) 经取代的杂环化合物
WO2019222438A1 (en) Tricyclic sulfone compound as a ror gamma modulator
HK40083482A (en) Inhibitors of egfr and/or her2 and methods of use
JP2007509127A (ja) ホスホジエステラーゼ−４阻害剤としてのアザベンゾジアゼピン
HK40128737A (zh) 磷醯胺酯单糖、药物组合物及诊断和治疗应用

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20181016

Termination date: 20210918

CF01 Termination of patent right due to non-payment of annual fee