CN102026974B - 四氢环戊二烯并[b]吲哚雄激素受体调节剂 - Google Patents

四氢环戊二烯并[b]吲哚雄激素受体调节剂 Download PDF

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Publication number
CN102026974B
CN102026974B CN200980117076XA CN200980117076A CN102026974B CN 102026974 B CN102026974 B CN 102026974B CN 200980117076X A CN200980117076X A CN 200980117076XA CN 200980117076 A CN200980117076 A CN 200980117076A CN 102026974 B CN102026974 B CN 102026974B
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compound
formula
indol
cyano
cyclopenta
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CN102026974A (zh
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P·K·贾达夫
V·克里什南
E·J·金
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Eli Lilly and Co
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/94—[b, c]- or [b, d]-condensed containing carbocyclic rings other than six-membered
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Neurology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN200980117076XA 2008-05-16 2009-05-14 四氢环戊二烯并[b]吲哚雄激素受体调节剂 Active CN102026974B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US5372208P 2008-05-16 2008-05-16
US61/053,722 2008-05-16
US61/053722 2008-05-16
PCT/US2009/043875 WO2009140448A1 (en) 2008-05-16 2009-05-14 Tetrahydrocyclopenta[b]indole androgen receptor modulators

Publications (2)

Publication Number Publication Date
CN102026974A CN102026974A (zh) 2011-04-20
CN102026974B true CN102026974B (zh) 2013-08-28

Family

ID=40847864

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Application Number Title Priority Date Filing Date
CN200980117076XA Active CN102026974B (zh) 2008-05-16 2009-05-14 四氢环戊二烯并[b]吲哚雄激素受体调节剂

Country Status (18)

Country Link
US (1) US8486943B2 (enExample)
EP (1) EP2297100B1 (enExample)
JP (1) JP5603327B2 (enExample)
KR (1) KR101278788B1 (enExample)
CN (1) CN102026974B (enExample)
AU (1) AU2009246348B2 (enExample)
BR (1) BRPI0912394A2 (enExample)
CA (1) CA2724629C (enExample)
CY (1) CY1113341T1 (enExample)
DK (1) DK2297100T3 (enExample)
EA (1) EA019713B1 (enExample)
ES (1) ES2396612T3 (enExample)
HR (1) HRP20120917T1 (enExample)
MX (1) MX2010012436A (enExample)
PL (1) PL2297100T3 (enExample)
PT (1) PT2297100E (enExample)
SI (1) SI2297100T1 (enExample)
WO (1) WO2009140448A1 (enExample)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA98777C2 (en) 2006-11-20 2012-06-25 Эли Лилли Энд Компани Tetrahydrocyclopenta[b]indole compounds as androgen receptor modulators
US8268872B2 (en) 2008-02-22 2012-09-18 Radius Health, Inc. Selective androgen receptor modulators
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
JP5964756B2 (ja) 2010-02-04 2016-08-03 ラジウス ヘルス，インコーポレイテッド 選択的アンドロゲン受容体モジュレーター
PL2568806T3 (pl) 2010-05-12 2017-03-31 Radius Health, Inc. Schematy lecznicze
US8642632B2 (en) 2010-07-02 2014-02-04 Radius Health, Inc. Selective androgen receptor modulators
AU2011312490B2 (en) 2010-09-28 2015-06-25 Radius Pharmaceuticals, Inc. Selective androgen receptor modulators
ES2939940T3 (es) 2014-03-28 2023-04-28 Univ Duke Tratamiento del cáncer de mama utilizando moduladores selectivos de los receptores de estrógenos
US9421264B2 (en) 2014-03-28 2016-08-23 Duke University Method of treating cancer using selective estrogen receptor modulators
JOP20180072A1 (ar) * 2014-09-11 2019-01-30 Lilly Co Eli علاج الأعراض المرتبطة بالعلاج بالحرمان من الأندروجين
WO2017223115A1 (en) 2016-06-22 2017-12-28 Radius Health, Inc. Ar+ breast cancer treatment methods
US20180185347A1 (en) * 2016-11-16 2018-07-05 Transition Therapeutics (Ireland 2) Limited Tetrahydrocyclopenta[b]indole compounds and phosphodiesterase inhibitors for the treatment of the signs and symptoms of bhp
EP3565542B1 (en) 2017-01-05 2024-04-10 Radius Pharmaceuticals, Inc. Polymorphic forms of rad1901-2hcl
SG11202013177WA (en) 2018-07-04 2021-01-28 Radius Pharmaceuticals Inc Polymorphic forms of rad 1901-2hcl
US12441745B2 (en) 2019-02-12 2025-10-14 Radius Pharmaceuticals, Inc. Processes and compounds
AU2021213297A1 (en) * 2020-01-27 2022-08-18 Eirgen Pharma Ltd. Tetrahydrocyclopenta[b]indole compounds for the treatment of renal disease
JP2023532996A (ja) * 2020-07-06 2023-08-01 クレセンタ バイオサイエンシズ Ｆａｂｐ４調節化合物の抗ウイルス的使用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006089053A2 (en) * 2005-02-17 2006-08-24 Wyeth Cycloalkylfused indole, benzothiophene, benzofuran and indene derivatives
WO2007002181A2 (en) * 2005-06-24 2007-01-04 Eli Lilly And Company Tetrahydrocarbazole derivatives useful as androgen receptor modulators (sarm)
WO2008063867A2 (en) * 2006-11-20 2008-05-29 Eli Lilly And Company Tetrahydrocyclopenta[b] indole compounds as androgen receptor modulators

Family Cites Families (14)

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US4988820A (en) 1986-02-21 1991-01-29 Bayer Aktiengesellschaft Cycloalkano(1,2-B) indole-sulponamides
GB8924392D0 (en) 1989-10-30 1989-12-20 Bayer Ag Substituted cycloalkano/b/dihydroindole-and-indolesulphonamides
GB9008108D0 (en) 1990-04-10 1990-06-06 Bayer Ag Cycloalkano(b)dihydroindoles and-indolesulphonamides substituted by heterocycles
DE4027278A1 (de) 1990-08-29 1992-03-05 Bayer Ag Heterocyclisch substituierte indolsulfonamide
DE4131346A1 (de) 1991-09-20 1993-03-25 Bayer Ag Indolsulfonamid substituierte dihydropyridine, verfahren zu ihrer herstellung und ihre verwendung in arzneimitteln
JP2005527464A (ja) 2001-08-09 2005-09-15 イーライ・リリー・アンド・カンパニー ｓＰＬＡ２インヒビターとしてのシクロヘプタＢインドール誘導体
DE10164564B4 (de) 2001-12-14 2007-05-16 Zentaris Gmbh Tetrahydrocarbazolderivate als Liganden für G-Protein gekoppelte Rezeptoren (GPCR)
EP2423190A1 (en) 2002-05-16 2012-02-29 Shionogi&Co., Ltd. Compounds Exhibiting PGD 2 Receptor Antagonism
US20060074124A1 (en) 2003-09-12 2006-04-06 Andrew Napper Methods of treating a disorder
US7019022B2 (en) 2003-12-15 2006-03-28 Merck Frosst Canada & Co. Substituted tetrahydrocarbazole and cyclopentanoindole derivatives
WO2005092854A1 (en) 2004-03-03 2005-10-06 Eli Lilly And Company Bicyclic substituted indole-derivative steroid hormone nuclear receptor modulators
EP1817025A2 (en) 2004-11-23 2007-08-15 PTC Therapeutics, Inc. Tetrahydrocarbazoles as active agents for inhibiting vegf production by translational control
US20090022694A1 (en) 2005-10-18 2009-01-22 Distefano Peter Sirt1 inhibition
WO2008019825A1 (en) 2006-08-14 2008-02-21 Santhera Pharmaceuticals (Schweiz) Ag Use of tricyclic indole derivatives for the treatment of muscular diseases

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006089053A2 (en) * 2005-02-17 2006-08-24 Wyeth Cycloalkylfused indole, benzothiophene, benzofuran and indene derivatives
WO2007002181A2 (en) * 2005-06-24 2007-01-04 Eli Lilly And Company Tetrahydrocarbazole derivatives useful as androgen receptor modulators (sarm)
WO2008063867A2 (en) * 2006-11-20 2008-05-29 Eli Lilly And Company Tetrahydrocyclopenta[b] indole compounds as androgen receptor modulators

Also Published As

Publication number Publication date
CN102026974A (zh) 2011-04-20
AU2009246348A8 (en) 2010-12-16
EP2297100A1 (en) 2011-03-23
ES2396612T3 (es) 2013-02-22
EP2297100B1 (en) 2012-10-31
EA201071317A1 (ru) 2011-06-30
AU2009246348B2 (en) 2012-04-12
DK2297100T3 (da) 2012-12-17
US20110039855A1 (en) 2011-02-17
CY1113341T1 (el) 2016-06-22
BRPI0912394A2 (pt) 2016-07-26
AU2009246348A1 (en) 2009-11-19
MX2010012436A (es) 2010-12-06
CA2724629A1 (en) 2009-11-19
EA019713B1 (ru) 2014-05-30
KR20100132551A (ko) 2010-12-17
KR101278788B1 (ko) 2013-06-25
CA2724629C (en) 2014-08-19
PL2297100T3 (pl) 2013-03-29
JP2011520903A (ja) 2011-07-21
SI2297100T1 (sl) 2013-02-28
WO2009140448A1 (en) 2009-11-19
PT2297100E (pt) 2013-01-24
WO2009140448A8 (en) 2010-01-07
HRP20120917T1 (hr) 2012-12-31
JP5603327B2 (ja) 2014-10-08
US8486943B2 (en) 2013-07-16

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