CN105555768B - RORγ调节剂 - Google Patents

RORγ调节剂 Download PDF

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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
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sulfonyl
bases
hexafluoro
methyl
fluorophenyls
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Expired - Fee Related
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Chinese (zh)
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CN105555768A (zh
Inventor
T·G·M·达尔
段敬武
龚华
江斌
陆忠辉
D·S·温斯坦
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Bristol Myers Squibb Co
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (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)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (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)

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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 (enExample)
EP (1) EP3046906B1 (enExample)
JP (1) JP6397488B2 (enExample)
CN (1) CN105555768B (enExample)
WO (1) WO2015042212A1 (enExample)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105705501B (zh) 2013-09-09 2019-04-19 百时美施贵宝公司 RORγ调节剂
CN105555768B (zh) 2013-09-20 2018-10-16 百时美施贵宝公司 RORγ调节剂
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
EP3092221B1 (en) 2014-01-06 2018-10-17 Bristol-Myers Squibb Company Heterocyclic sulfones as ror-gamma modulators
CN106132931B (zh) 2014-01-06 2019-08-02 百时美施贵宝公司 碳环砜RORγ调节剂
DK3212642T3 (da) 2014-10-30 2019-11-25 Janssen Pharmaceutica Nv Amid-substituerede thiazoler som modulatorer af rorgammat
PL3212641T3 (pl) 2014-10-30 2019-05-31 Janssen Pharmaceutica Nv Tiazole jako modulatory RORYT
JOP20200117A1 (ar) 2014-10-30 2017-06-16 Janssen Pharmaceutica Nv كحولات ثلاثي فلوروميثيل كمُعدلات للمستقبل النووي جاما تي المرتبط بحمض الريتيونَويك ROR?t
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
US10934286B2 (en) 2016-10-13 2021-03-02 Bristol-Myers Squibb Company Heterocyclic sulfones as ROR gamma modulators
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
US11345666B2 (en) 2018-06-18 2022-05-31 Janssen Pharmaceutica Nv Phenyl and pyridinyl substituted imidazoles as modulators of RORγT
EP3807261B1 (en) 2018-06-18 2022-07-13 Janssen Pharmaceutica NV Pyridinyl pyrazoles as modulators of roryt
EP3806958B1 (en) 2018-06-18 2022-09-07 Janssen Pharmaceutica NV 6-aminopyridin-3-yl pyrazoles as modulators of roryt
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
CN105705501B (zh) 2013-09-09 2019-04-19 百时美施贵宝公司 RORγ调节剂
CN105555768B (zh) 2013-09-20 2018-10-16 百时美施贵宝公司 RORγ调节剂
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
MX369347B (es) 2014-01-06 2019-11-06 Bristol Myers Squibb Co Derivados de pirrolidinilsulfona y su uso como moduladores del receptor huerfano relacionado con retinoide gamma (ror gamma).
CN106132931B (zh) 2014-01-06 2019-08-02 百时美施贵宝公司 碳环砜RORγ调节剂
EP3092221B1 (en) 2014-01-06 2018-10-17 Bristol-Myers Squibb Company Heterocyclic sulfones 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
WO2015042212A1 (en) 2015-03-26
US9725443B2 (en) 2017-08-08
JP2016530213A (ja) 2016-09-29
EP3046906A1 (en) 2016-07-27
US20160229844A1 (en) 2016-08-11
JP6397488B2 (ja) 2018-09-26
CN105555768A (zh) 2016-05-04

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