CN115335367B - 用于炎性疾病和雄性避孕的RAR-α化合物 - Google Patents

用于炎性疾病和雄性避孕的RAR-α化合物 Download PDF

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Publication number
CN115335367B
CN115335367B CN202080097179.0A CN202080097179A CN115335367B CN 115335367 B CN115335367 B CN 115335367B CN 202080097179 A CN202080097179 A CN 202080097179A CN 115335367 B CN115335367 B CN 115335367B
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unsubstituted
pharmaceutically acceptable
acceptable salt
alkyl
compound
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Chinese (zh)
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CN115335367A (zh
Inventor
拉杰·库马尔·拉赫加
保罗·达米安·克罗
陶海燕
斯科特·麦克尼尔·撒切尔
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Overn Pharmaceuticals
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Overn Pharmaceuticals
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D311/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16Masculine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/04Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN202080097179.0A 2019-12-19 2020-12-17 用于炎性疾病和雄性避孕的RAR-α化合物 Active CN115335367B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962950473P 2019-12-19 2019-12-19
US62/950,473 2019-12-19
PCT/US2020/065719 WO2021127250A1 (en) 2019-12-19 2020-12-17 Rar-alpha compounds for inflammatory disease and male contraception

Publications (2)

Publication Number Publication Date
CN115335367A CN115335367A (zh) 2022-11-11
CN115335367B true CN115335367B (zh) 2024-08-13

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CN202080097179.0A Active CN115335367B (zh) 2019-12-19 2020-12-17 用于炎性疾病和雄性避孕的RAR-α化合物

Country Status (7)

Country Link
US (1) US12492177B2 (https=)
EP (1) EP4077300A1 (https=)
JP (1) JP7657223B2 (https=)
CN (1) CN115335367B (https=)
AU (1) AU2020408043A1 (https=)
CA (1) CA3165166A1 (https=)
WO (1) WO2021127250A1 (https=)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12492177B2 (en) 2019-12-19 2025-12-09 Orphagen Pharmaceuticals, Inc. RAR-α compounds for inflammatory disease and male contraception

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5877207A (en) * 1996-03-11 1999-03-02 Allergan Sales, Inc. Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
WO2000019990A2 (en) * 1998-10-08 2000-04-13 Allergan Sales, Inc. Rar antagonists as male anti-fertility agents

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4783443A (en) 1986-03-03 1988-11-08 The University Of Chicago Amino acyl cephalosporin derivatives
US6521641B1 (en) * 1998-10-08 2003-02-18 Allergan, Inc. Male anti-fertility agents
US20020193403A1 (en) 2001-05-03 2002-12-19 Allergan Sales, Inc. Methods of treating hyperlipidemia
US7105566B2 (en) * 2002-10-22 2006-09-12 Allergan, Inc. Methods of treatment during vascular procedures
DK3204357T3 (da) 2014-10-10 2022-04-04 High Force Res Limited Fluorescerende, syntetiske retinoider
WO2017201200A1 (en) 2016-05-19 2017-11-23 Orphagen Pharmaceuticals, Inc. Therapeutic compositions containing rar-alpha antagonists
DE102016123286B4 (de) 2016-12-01 2019-03-07 Deutsches Zentrum für Luft- und Raumfahrt e.V. Verfahren und Vorrichtung zur Georeferenzierung von Luftbilddaten
EP3709990A4 (en) * 2017-11-17 2021-12-01 The Regents of the University of California MANIPULATION OF THE RETIC ACID SIGNAL PATH
CN114041070B (zh) 2018-11-19 2024-03-08 棱镜传感器公司 边缘式光子计数检测器
US12492177B2 (en) 2019-12-19 2025-12-09 Orphagen Pharmaceuticals, Inc. RAR-α compounds for inflammatory disease and male contraception

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5877207A (en) * 1996-03-11 1999-03-02 Allergan Sales, Inc. Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
WO2000019990A2 (en) * 1998-10-08 2000-04-13 Allergan Sales, Inc. Rar antagonists as male anti-fertility agents

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Identification of Highly Potent Retinoic Acid Receptorr-Selective Antagonists;Min Teng et al.;J. Med. Chem.;第40卷(第16期);第2445页Chart 3,第2447页Table 1 *

Also Published As

Publication number Publication date
CN115335367A (zh) 2022-11-11
AU2020408043A1 (en) 2022-07-28
US20230357175A1 (en) 2023-11-09
WO2021127250A1 (en) 2021-06-24
JP2023509372A (ja) 2023-03-08
US12492177B2 (en) 2025-12-09
EP4077300A1 (en) 2022-10-26
JP7657223B2 (ja) 2025-04-04
CA3165166A1 (en) 2021-06-24

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