CN106061956B - 作为RORγ调节剂的杂环砜 - Google Patents

作为RORγ调节剂的杂环砜 Download PDF

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Publication number
CN106061956B
CN106061956B CN201580011973.8A CN201580011973A CN106061956B CN 106061956 B CN106061956 B CN 106061956B CN 201580011973 A CN201580011973 A CN 201580011973A CN 106061956 B CN106061956 B CN 106061956B
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substituted
alkyl
hydrogen
independently
pharmaceutically acceptable
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Chinese (zh)
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CN106061956A (zh
Inventor
段敬武
T.G.M.达
江斌
A.卡马卡
A.K.古普塔
Z.卢
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/54—Sulfur atoms
    • 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
    • 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
    • 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
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/96—Sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring 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
    • C07D401/06—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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrane Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201580011973.8A 2014-01-06 2015-01-05 作为RORγ调节剂的杂环砜 Expired - Fee Related CN106061956B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461923904P 2014-01-06 2014-01-06
US61/923904 2014-01-06
PCT/US2015/010090 WO2015103510A1 (en) 2014-01-06 2015-01-05 Heterocyclic sulfone as ror-gamma modulators

Publications (2)

Publication Number Publication Date
CN106061956A CN106061956A (zh) 2016-10-26
CN106061956B true CN106061956B (zh) 2021-03-12

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ID=52392247

Family Applications (1)

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CN201580011973.8A Expired - Fee Related CN106061956B (zh) 2014-01-06 2015-01-05 作为RORγ调节剂的杂环砜

Country Status (6)

Country Link
US (1) US9637455B2 (enExample)
EP (1) EP3092221B1 (enExample)
JP (1) JP6476205B2 (enExample)
CN (1) CN106061956B (enExample)
ES (1) ES2705400T3 (enExample)
WO (1) WO2015103510A1 (enExample)

Families Citing this family (16)

* 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
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
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).
DK3212642T3 (da) 2014-10-30 2019-11-25 Janssen Pharmaceutica Nv Amid-substituerede thiazoler som modulatorer af rorgammat
JOP20200117A1 (ar) 2014-10-30 2017-06-16 Janssen Pharmaceutica Nv كحولات ثلاثي فلوروميثيل كمُعدلات للمستقبل النووي جاما تي المرتبط بحمض الريتيونَويك ROR?t
PL3212641T3 (pl) 2014-10-30 2019-05-31 Janssen Pharmaceutica Nv Tiazole jako modulatory RORYT
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
CA3042877A1 (en) * 2016-11-09 2018-05-17 Bristol-Myers Squibb Company Tricyclic 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

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE735866C (de) * 1941-01-17 1943-06-11 Ig Farbenindustrie Ag Verfahren zur Darstellung von Aminoalkylsulfonverbindungen
US2802013A (en) * 1954-02-12 1957-08-06 Searle & Co 2-(oxo and imino)-3-(phenyl and halophenyl)-tetrahydrofuransulfones and processes for the manufacture thereof
US2812330A (en) * 1956-05-02 1957-11-05 Searle & Co Sulfone derivatives of 2, 6-piperidinedione
US3016403A (en) * 1955-07-29 1962-01-09 Searle & Co 1-aryl-3-hydroxypropyl sulfones and processes
WO2002081435A1 (en) * 2001-04-05 2002-10-17 Merck Sharp & Dohme Limited Sulphones which modulate the action of gamma secretase
CN100562516C (zh) * 2001-12-27 2009-11-25 第一制药株式会社 β-淀粉样蛋白产生和分泌的抑制剂
WO2013092939A1 (en) * 2011-12-22 2013-06-27 F. Hoffmann-La Roche Ag BENZYL SULFONAMIDE DERIVATIVES AS RORc MODULATORS
WO2013169588A1 (en) * 2012-05-08 2013-11-14 Merck Sharp & Dohme Corp. BICYCLIC SULFONE COMPOUNDS FOR INHIBITION OF RORy ACTIVITY AND THE TREATMENT OF DISEASE

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2312945A4 (en) * 2008-08-13 2012-05-09 Merck Sharp & Dohme PURE DERIVATIVES FOR THE TREATMENT OF MORBUS ALZHEIMER
WO2014028669A1 (en) * 2012-08-15 2014-02-20 Biogen Idec Ma Inc. Novel compounds for modulation of ror-gamma activity
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
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
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

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE735866C (de) * 1941-01-17 1943-06-11 Ig Farbenindustrie Ag Verfahren zur Darstellung von Aminoalkylsulfonverbindungen
US2802013A (en) * 1954-02-12 1957-08-06 Searle & Co 2-(oxo and imino)-3-(phenyl and halophenyl)-tetrahydrofuransulfones and processes for the manufacture thereof
US3016403A (en) * 1955-07-29 1962-01-09 Searle & Co 1-aryl-3-hydroxypropyl sulfones and processes
US2812330A (en) * 1956-05-02 1957-11-05 Searle & Co Sulfone derivatives of 2, 6-piperidinedione
WO2002081435A1 (en) * 2001-04-05 2002-10-17 Merck Sharp & Dohme Limited Sulphones which modulate the action of gamma secretase
CN100562516C (zh) * 2001-12-27 2009-11-25 第一制药株式会社 β-淀粉样蛋白产生和分泌的抑制剂
WO2013092939A1 (en) * 2011-12-22 2013-06-27 F. Hoffmann-La Roche Ag BENZYL SULFONAMIDE DERIVATIVES AS RORc MODULATORS
WO2013169588A1 (en) * 2012-05-08 2013-11-14 Merck Sharp & Dohme Corp. BICYCLIC SULFONE COMPOUNDS FOR INHIBITION OF RORy ACTIVITY AND THE TREATMENT OF DISEASE

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Epoxy-Ramberg-Backlund Reaction(ERBR): A Sulfone-Based Method for the Synthesis of Allylic Alcohols;Paul Evans，等;《European Journal of Organic Chemistry》;20060401;第2006卷(第7期);第1743页 *
Jerzy Golinski，等.Reactions of Organic Anions *
Lead optimization of 4,4-biaryl piperidine amides as γ-secretease inhibitors;Joshua Close，等;《Bioorganic & Medicinal Chemistry Letters》;20120308;第22卷(第9期);第3204页 *
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Part LXXXIV 1. A Convenient Method for Synthesis of 1-Chloro-，1,1-Dichloro-，and 1,2-Epoxyalkanesulfonamides.《Synthesis》.1978,第1978卷(第11期),第824页. *
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Also Published As

Publication number Publication date
ES2705400T3 (es) 2019-03-25
CN106061956A (zh) 2016-10-26
EP3092221B1 (en) 2018-10-17
WO2015103510A1 (en) 2015-07-09
US20160326115A1 (en) 2016-11-10
EP3092221A1 (en) 2016-11-16
US9637455B2 (en) 2017-05-02
JP2017501237A (ja) 2017-01-12
JP6476205B2 (ja) 2019-02-27

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