CN105899507B - 作为RORc调节剂的芳基磺内酰胺衍生物 - Google Patents

作为RORc调节剂的芳基磺内酰胺衍生物 Download PDF

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Publication number
CN105899507B
CN105899507B CN201580004086.8A CN201580004086A CN105899507B CN 105899507 B CN105899507 B CN 105899507B CN 201580004086 A CN201580004086 A CN 201580004086A CN 105899507 B CN105899507 B CN 105899507B
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alkyl
formula
certain embodiments
phenyl
methyl
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Expired - Fee Related
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CN201580004086.8A
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Chinese (zh)
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CN105899507A (zh
Inventor
M·博迪范奈尔
B·法贝尔
E·甘西亚
S·盖恩斯
A·戈比
C·赫尔利
T·拉迪瓦海蒂
O·雷内
D·维赛
S·沃德
P·温希普
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/02—1,2-Thiazines; Hydrogenated 1,2-thiazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • 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
    • 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
    • A61P17/02—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
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • C07D417/10—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 aromatic rings
    • 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
    • C07D417/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201580004086.8A 2014-01-10 2015-01-09 作为RORc调节剂的芳基磺内酰胺衍生物 Expired - Fee Related CN105899507B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201461925845P 2014-01-10 2014-01-10
US61/925,845 2014-01-10
US201462091861P 2014-12-15 2014-12-15
US62/091,861 2014-12-15
PCT/EP2015/050292 WO2015104354A1 (en) 2014-01-10 2015-01-09 ARYL SULTAM DERIVATIVES AS RORc MODULATORS

Publications (2)

Publication Number Publication Date
CN105899507A CN105899507A (zh) 2016-08-24
CN105899507B true CN105899507B (zh) 2019-06-07

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CN201580004086.8A Expired - Fee Related CN105899507B (zh) 2014-01-10 2015-01-09 作为RORc调节剂的芳基磺内酰胺衍生物

Country Status (9)

Country Link
US (1) US10131644B2 (cg-RX-API-DMAC7.html)
EP (1) EP3092239B1 (cg-RX-API-DMAC7.html)
JP (1) JP6458041B2 (cg-RX-API-DMAC7.html)
KR (1) KR20160106705A (cg-RX-API-DMAC7.html)
CN (1) CN105899507B (cg-RX-API-DMAC7.html)
CA (1) CA2935012A1 (cg-RX-API-DMAC7.html)
MX (1) MX2016008721A (cg-RX-API-DMAC7.html)
RU (1) RU2016131363A (cg-RX-API-DMAC7.html)
WO (1) WO2015104354A1 (cg-RX-API-DMAC7.html)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2760521T3 (es) 2014-01-10 2020-05-14 Hoffmann La Roche Derivados de aril-sultamo como moduladores de RORc
WO2017005668A1 (en) * 2015-07-08 2017-01-12 F. Hoffmann-La Roche Ag ARYL SULTAM DERIVATIVES AS RORc MODULATORS
CN107690431A (zh) * 2015-07-08 2018-02-13 豪夫迈·罗氏有限公司 作为RORc调节剂的芳基磺内酰胺衍生物
CN114901640A (zh) * 2019-12-24 2022-08-12 兹杜斯生命科学有限公司 适用于治疗血脂异常的新型化合物
AU2021341508A1 (en) 2020-09-10 2023-05-25 Precirix N.V. Antibody fragment against fap
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
IL318992A (en) 2022-05-02 2025-04-01 Precirix N V Cancer treatment through advance directives

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013064231A1 (en) * 2011-10-31 2013-05-10 Phenex Pharmaceuticals Ag SEVEN-MEMBERED SULFONAMIDES AS MODULATORS OF RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORγ, NR1F3)
WO2013092941A1 (en) * 2011-12-22 2013-06-27 F. Hoffmann-La Roche Ag BENZYL SULFONAMIDE DERIVATIVES AS RORc MODULATORS

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US20130190356A1 (en) * 2011-12-22 2013-07-25 Genentech, Inc. Benzyl sulfonamide derivatives as rorc modulators
TW201408652A (zh) * 2012-07-11 2014-03-01 Hoffmann La Roche 作爲ＲＯＲｃ調節劑之芳基磺內醯胺衍生物
HK1214598A1 (zh) * 2012-12-10 2016-07-29 F. Hoffmann-La Roche Ag 作为rorc调节剂的苄基磺酰胺衍生物
EP2928863A1 (en) * 2012-12-10 2015-10-14 F. Hoffmann-La Roche AG BENZYL SULFONAMIDE DERIVATIVES AS RORc MODULATORS
CN105121404A (zh) * 2013-03-15 2015-12-02 豪夫迈·罗氏有限公司 作为RORc调节剂的芳基磺酰胺和氨基磺酸衍生物
EP3010919B1 (en) * 2013-06-21 2017-04-12 F. Hoffmann-La Roche AG Aryl sultam derivatives as ror-c modulators
ES2760521T3 (es) * 2014-01-10 2020-05-14 Hoffmann La Roche Derivados de aril-sultamo como moduladores de RORc
JP2017502070A (ja) * 2014-01-10 2017-01-19 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ＲＯＲｃモジュレーターとしてのヘテロアリールスルタム誘導体

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013064231A1 (en) * 2011-10-31 2013-05-10 Phenex Pharmaceuticals Ag SEVEN-MEMBERED SULFONAMIDES AS MODULATORS OF RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORγ, NR1F3)
WO2013092941A1 (en) * 2011-12-22 2013-06-27 F. Hoffmann-La Roche Ag BENZYL SULFONAMIDE DERIVATIVES AS RORc MODULATORS

Non-Patent Citations (2)

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Synthetic modulators of the retinoic acid receptor-related orphan receptors;Theodore M.，等;《Med. Chem. Commun》;20130403;第4卷(第5期);764-776 *
Targeting the Nuclear Hormone Receptor RORγt for the Treatment of Autoimmune and Inflammatory Disorders;T. G. MuraliDhar，等;《Annual Reports in Medicinal Chemistry》;20131231;第48卷;169-182 *

Also Published As

Publication number Publication date
MX2016008721A (es) 2017-01-26
KR20160106705A (ko) 2016-09-12
RU2016131363A (ru) 2018-02-16
CN105899507A (zh) 2016-08-24
CA2935012A1 (en) 2015-07-16
EP3092239A1 (en) 2016-11-16
WO2015104354A1 (en) 2015-07-16
JP6458041B2 (ja) 2019-01-23
US10131644B2 (en) 2018-11-20
US20170137393A1 (en) 2017-05-18
EP3092239B1 (en) 2019-10-02
JP2017503808A (ja) 2017-02-02

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