CN103842348B - 选择性雄激素受体调节剂 - Google Patents

选择性雄激素受体调节剂 Download PDF

Info

Publication number
CN103842348B
CN103842348B CN201280049445.8A CN201280049445A CN103842348B CN 103842348 B CN103842348 B CN 103842348B CN 201280049445 A CN201280049445 A CN 201280049445A CN 103842348 B CN103842348 B CN 103842348B
Authority
CN
China
Prior art keywords
methyl
compound
mmol
chloro
benzonitrile
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.)
Active
Application number
CN201280049445.8A
Other languages
English (en)
Chinese (zh)
Other versions
CN103842348A (zh
Inventor
P.K.贾哈夫
A.塞伊德
J.E.格林
V.克里什南
D.P.马修斯
G.A.斯蒂芬森
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.)
Eli Lilly and Co
Original Assignee
Eli Lilly and 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47046879&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN103842348(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of CN103842348A publication Critical patent/CN103842348A/zh
Application granted granted Critical
Publication of CN103842348B publication Critical patent/CN103842348B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • 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
    • C07D309/14—Nitrogen atoms not forming part of a nitro radical
    • 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
    • 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
    • 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
    • A61P21/06—Anabolic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26—Androgens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-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
    • C07D307/18—Heterocyclic compounds containing five-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
    • C07D307/22—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN201280049445.8A 2011-10-13 2012-10-05 选择性雄激素受体调节剂 Active CN103842348B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161546711P 2011-10-13 2011-10-13
US61/546711 2011-10-13
PCT/US2012/058824 WO2013055577A1 (en) 2011-10-13 2012-10-05 Selective androgen receptor modulators

Publications (2)

Publication Number Publication Date
CN103842348A CN103842348A (zh) 2014-06-04
CN103842348B true CN103842348B (zh) 2015-08-19

Family

ID=47046879

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201280049445.8A Active CN103842348B (zh) 2011-10-13 2012-10-05 选择性雄激素受体调节剂

Country Status (28)

Country Link
US (1) US8658693B2 (enExample)
EP (1) EP2766350B1 (enExample)
JP (1) JP6002228B2 (enExample)
KR (1) KR20140067102A (enExample)
CN (1) CN103842348B (enExample)
AP (1) AP2014007548A0 (enExample)
AR (1) AR088082A1 (enExample)
AU (1) AU2012321113B2 (enExample)
BR (1) BR112014008668A2 (enExample)
CA (1) CA2847889A1 (enExample)
CL (1) CL2014000895A1 (enExample)
CO (1) CO6910195A2 (enExample)
CR (1) CR20140156A (enExample)
DO (1) DOP2014000075A (enExample)
EA (1) EA201490519A1 (enExample)
EC (1) ECSP14013305A (enExample)
ES (1) ES2626820T3 (enExample)
GT (1) GT201400067A (enExample)
IL (1) IL231440A0 (enExample)
MX (1) MX2014004558A (enExample)
PE (1) PE20141669A1 (enExample)
PH (1) PH12014500808A1 (enExample)
PL (1) PL2766350T3 (enExample)
PT (1) PT2766350T (enExample)
SG (1) SG11201401794YA (enExample)
TN (1) TN2014000136A1 (enExample)
TW (1) TWI449686B (enExample)
WO (1) WO2013055577A1 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140045856A1 (en) 2012-07-31 2014-02-13 Boehringer Ingelheim International Gmbh 4-Methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalenes
TW201534586A (zh) * 2013-06-11 2015-09-16 Orion Corp 新穎cyp17抑制劑/抗雄激素劑
US10093660B2 (en) 2013-12-04 2018-10-09 Evotec Internatonal Gmbh Sulfoximine substituted quinazolines for pharmaceutical compositions
US9682960B2 (en) 2013-12-19 2017-06-20 Endorecherche, Inc. Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety
JP6479854B2 (ja) 2014-05-07 2019-03-06 エヴォテック・インターナショナル・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングEvotec International GmbH 医薬組成物のためのスルホキシイミン置換キナゾリン
CN109803968A (zh) 2016-08-15 2019-05-24 辉瑞公司 吡啶并嘧啶酮cdk2/4/6抑制剂
PL3507289T3 (pl) 2016-09-02 2021-01-25 Suven Life Sciences Limited Dodatnie allosteryczne modulatory receptora muskarynowego m1
EP3684761A1 (en) 2017-09-18 2020-07-29 Basf Se Substituted trifluoromethyloxadiazoles for combating phytopathogenic fungi
TWI702219B (zh) * 2018-07-12 2020-08-21 美商美國禮來大藥廠 選擇性雌激素受體降解劑
IL297963A (en) 2020-05-07 2023-01-01 Adorx Therapeutics Ltd Antagonists of the adenosine a2a receptor
JP7778095B2 (ja) * 2020-06-24 2025-12-01 セルジーン コーポレーション セレブロン結合化合物、その組成物及びそれによる治療方法
WO2025104624A1 (en) * 2023-11-14 2025-05-22 Pfizer Inc. Synthesis of 1,5-anhydro-3-({5-chloro-4-[4-fluoro-2-(2-hydroxypropan-2-yl)-1-(propan-2-yl)-1h-benzimidazol-6-yl]pyrimidin-2-yl}amino)-2,3-dideoxy-d-threo-pentitol

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101175747A (zh) * 2005-05-13 2008-05-07 伊莱利利公司 作为选择性雄激素受体调节剂的取代的n-芳基吡咯烷化合物
WO2008130879A2 (en) * 2007-04-16 2008-10-30 Serenex, Inc. Tetrahydroindole and tetrahydroindazole derivatives

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3594405A (en) * 1968-05-17 1971-07-20 Du Pont Substituted pyranyl anilines as plant growth modifiers
DE60208630T2 (de) * 2001-05-11 2006-08-17 Pfizer Products Inc., Groton Thiazolderivate und ihre Verwendung als cdk-Inhibitoren
US8519158B2 (en) * 2004-03-12 2013-08-27 Ligand Pharmaceuticals Incorporated Androgen receptor modulator compounds and methods
BRPI0619208A2 (pt) * 2005-11-30 2011-09-20 Astellas Pharma Inc derivado de 2-aminobenzamida c07d 307/14 c07d 307/22 c07d 309/14 c07d 319/12 c07d 401/12 c07d 405/12 c07d 413/12 c07d 417/12
US8190467B2 (en) * 2007-10-19 2012-05-29 Michelle Letendre-Hedlund Methods of identifying environmentally friendly businesses or individuals
BRPI0907844B8 (pt) * 2008-02-22 2021-05-25 Radius Health Inc compostos e método para modular um receptor de andrógeno, processos de preparação e composição farmacêutica dos mesmos e seus usos

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101175747A (zh) * 2005-05-13 2008-05-07 伊莱利利公司 作为选择性雄激素受体调节剂的取代的n-芳基吡咯烷化合物
WO2008130879A2 (en) * 2007-04-16 2008-10-30 Serenex, Inc. Tetrahydroindole and tetrahydroindazole derivatives

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
雄激素受体抑制剂的研究进展;刘波等;《中国药物化学杂志》;20101031;第20卷(第5期);389-466 *

Also Published As

Publication number Publication date
SG11201401794YA (en) 2014-09-26
PE20141669A1 (es) 2014-11-08
GT201400067A (es) 2015-02-27
AR088082A1 (es) 2014-05-07
US20130217762A1 (en) 2013-08-22
PT2766350T (pt) 2017-05-22
AU2012321113A1 (en) 2014-03-27
EP2766350B1 (en) 2017-04-05
CA2847889A1 (en) 2013-04-18
ECSP14013305A (es) 2014-05-31
US8658693B2 (en) 2014-02-25
JP6002228B2 (ja) 2016-10-05
DOP2014000075A (es) 2014-06-01
TN2014000136A1 (en) 2015-07-01
CO6910195A2 (es) 2014-03-31
EA201490519A1 (ru) 2014-09-30
PL2766350T3 (pl) 2017-08-31
EP2766350A1 (en) 2014-08-20
ES2626820T3 (es) 2017-07-26
JP2014530818A (ja) 2014-11-20
KR20140067102A (ko) 2014-06-03
CN103842348A (zh) 2014-06-04
AP2014007548A0 (en) 2014-03-31
CR20140156A (es) 2014-05-16
BR112014008668A2 (pt) 2017-04-25
PH12014500808A1 (en) 2019-07-03
AU2012321113B2 (en) 2015-07-09
MX2014004558A (es) 2014-08-01
WO2013055577A1 (en) 2013-04-18
TW201329026A (zh) 2013-07-16
CL2014000895A1 (es) 2014-08-22
TWI449686B (zh) 2014-08-21
IL231440A0 (en) 2014-04-30

Similar Documents

Publication Publication Date Title
JP6002228B2 (ja) 選択的アンドロゲン受容体調節剤
CN108366996B (zh) 四氢-1H-吡啶[3,4-b]吲哚类抗雌激素药物
AU2020215380A2 (en) Heterocyclic compound and use thereof
CN110382503A (zh) 制备acc抑制剂及其固体形式的方法
JP6762507B2 (ja) エチホキシンの重水素化類似体、それらの誘導体、およびそれらの使用
CN106470985A (zh) 作为可溶性鸟苷酸环化酶激活剂的茚满和二氢吲哚衍生物及其用途
EP3303308B1 (en) Separation of enantiomers of 3-ethylbicyclo[3.2.0]hept-3-en-6-one
CA2905570A1 (en) Salts, co-crystals, and polymorphs of an anxiolytic compound
TW202517609A (zh) 氘化有機化合物及其用途(二)
HK1254800A1 (zh) 2,3,4,5-四氢吡啶-6-胺衍生物
EP2066677B1 (en) Pyridooxazepine progesteron receptor modulators
CN104203922A (zh) 螺乙内酰脲化合物及其作为选择性雄激素受体调节剂的用途
TWI738162B (zh) 稠合三環氘代衍生物及其組合物和用途
KR20190040340A (ko) 장애의 치료를 위한 하이드록시노르케타민 유도체
JP2023531399A (ja) CAV1.2活性化物質としてのメチル2-メチル-5-オキソ-1,4,5,7-テトラヒドロフロ[3,4-b]ピリジン-3-カルボキシレート化合物
CA2842566A1 (en) Pyrazoline derivatives and their use as selective androgen receptor modulators
HK40056233A (en) Tetrahydro-1h-pyrido[3,4-b]indole anti-estrogenic drugs
HK1192877A1 (zh) 新的皮质多巴胺能-和nmda-受体介导的谷氨酸能神经传递调节剂
HK1192877B (en) Novel modulators of cortical dopaminergic- and nmda-receptor-mediated glutamatergic neurotransmission
TW201309691A (zh) 促代謝性麩胺酸受體調節劑

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant