EA019713B1 - ТЕТРАГИДРОЦИКЛОПЕНТА[b]ИНДОЛЬНЫЕ МОДУЛЯТОРЫ РЕЦЕПТОРОВ АНДРОГЕНОВ - Google Patents

ТЕТРАГИДРОЦИКЛОПЕНТА[b]ИНДОЛЬНЫЕ МОДУЛЯТОРЫ РЕЦЕПТОРОВ АНДРОГЕНОВ Download PDF

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Publication number
EA019713B1
EA019713B1 EA201071317A EA201071317A EA019713B1 EA 019713 B1 EA019713 B1 EA 019713B1 EA 201071317 A EA201071317 A EA 201071317A EA 201071317 A EA201071317 A EA 201071317A EA 019713 B1 EA019713 B1 EA 019713B1
Authority
EA
Eurasian Patent Office
Prior art keywords
compound
formula
mmol
tetrahydrocyclopenta
indol
Prior art date
Application number
EA201071317A
Other languages
English (en)
Russian (ru)
Other versions
EA201071317A1 (ru
Inventor
Прабхакар Кондаджи Джадхав
Венкатеш Кришнан
Еуибонг Джемс Ким
Original Assignee
Эли Лилли Энд Компани
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.)
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Publication date
Application filed by Эли Лилли Энд Компани filed Critical Эли Лилли Энд Компани
Publication of EA201071317A1 publication Critical patent/EA201071317A1/ru
Publication of EA019713B1 publication Critical patent/EA019713B1/ru

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56Ring 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/06Anabolic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26Androgens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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

Landscapes

  • 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)
  • Neurology (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
EA201071317A 2008-05-16 2009-05-14 ТЕТРАГИДРОЦИКЛОПЕНТА[b]ИНДОЛЬНЫЕ МОДУЛЯТОРЫ РЕЦЕПТОРОВ АНДРОГЕНОВ EA019713B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US5372208P 2008-05-16 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
EA201071317A1 EA201071317A1 (ru) 2011-06-30
EA019713B1 true EA019713B1 (ru) 2014-05-30

Family

ID=40847864

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201071317A EA019713B1 (ru) 2008-05-16 2009-05-14 ТЕТРАГИДРОЦИКЛОПЕНТА[b]ИНДОЛЬНЫЕ МОДУЛЯТОРЫ РЕЦЕПТОРОВ АНДРОГЕНОВ

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
MX2010009162A (es) 2008-02-22 2010-12-21 Radius Health Inc Moduladores selectivos del receptor de androgeno.
EP2531029B1 (en) 2010-02-04 2016-10-19 Radius Health, Inc. Selective androgen receptor modulators
WO2011143469A1 (en) 2010-05-12 2011-11-17 Radius Health,Inc Therapeutic regimens
US8642632B2 (en) 2010-07-02 2014-02-04 Radius Health, Inc. Selective androgen receptor modulators
BR112013007685B1 (pt) 2010-09-28 2021-11-09 Radius Pharmaceuticals, Inc Compostos moduladores de receptor andrógeno seletivos, composição farmacêutica compreendendo os referidos compostos, método de identificação de um composto capaz de modular um receptor andrógeno, usos de um composto ou da composição e processo para a preparação de um composto
US9421264B2 (en) 2014-03-28 2016-08-23 Duke University Method of treating cancer using selective estrogen receptor modulators
FI3834824T3 (fi) 2014-03-28 2025-12-05 Univ Duke Estrogeenireseptoripositiivisen rintasyövän hoito selektiivisellä estrogeenireseptorin modulaattorilla
JOP20180072A1 (ar) * 2014-09-11 2019-01-30 Lilly Co Eli علاج الأعراض المرتبطة بالعلاج بالحرمان من الأندروجين
JP7221699B2 (ja) 2016-06-22 2023-02-14 エリプセス ファーマ エルティーディー Ar+乳癌の治療方法
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
KR102881465B1 (ko) 2017-01-05 2025-11-04 래디어스 파마슈티컬스, 인코포레이티드 Rad1901-2hcl의 다형 형태
SG11202013177WA (en) 2018-07-04 2021-01-28 Radius Pharmaceuticals Inc Polymorphic forms of rad 1901-2hcl
KR20210127961A (ko) 2019-02-12 2021-10-25 래디어스 파마슈티컬스, 인코포레이티드 방법 및 화합물
US20230096602A1 (en) * 2020-01-27 2023-03-30 Eirgen Pharma Ltd. Tetrahydrocyclopenta[b]indole compounds for treatment of renal disease
CN116761598A (zh) * 2020-07-06 2023-09-15 新月生物科学 Fabp4调节化合物的抗病毒用途

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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

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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)
US7534897B2 (en) 2002-05-16 2009-05-19 Shionogi & Co., Ltd. Indole arylsulfonaimide 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
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US8946444B2 (en) 2004-11-23 2015-02-03 Ptc Therapeutics, Inc. Tetrahydrocarbazoles as active agents for inhibiting VEGF production by translational control
AR052674A1 (es) 2005-02-17 2007-03-28 Wyeth Corp Derivados de indol, benzotiofeno, benzofurano e indeno cicloalquilcondensados
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Publication number Priority date Publication date Assignee Title
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

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CADILLA R. ET AL.: "Selective androgen receptor modulators in drug discovery: medicinal chemistry and therapeutic potential". CURRENT TOPICS IN MEDICINAL CHEMISTRY, BENTHAM SCIENCE PUBLISHERS, HILVERSUM, NL, vol. 6, no. 3, 1 January 2006 (2006-01-01), pages 245-270, XP002482017, ISSN: 1568-0266, the whole document *

Also Published As

Publication number Publication date
KR20100132551A (ko) 2010-12-17
US8486943B2 (en) 2013-07-16
EA201071317A1 (ru) 2011-06-30
CN102026974B (zh) 2013-08-28
AU2009246348B2 (en) 2012-04-12
DK2297100T3 (da) 2012-12-17
JP5603327B2 (ja) 2014-10-08
ES2396612T3 (es) 2013-02-22
CN102026974A (zh) 2011-04-20
WO2009140448A1 (en) 2009-11-19
CA2724629C (en) 2014-08-19
MX2010012436A (es) 2010-12-06
KR101278788B1 (ko) 2013-06-25
AU2009246348A8 (en) 2010-12-16
PL2297100T3 (pl) 2013-03-29
WO2009140448A8 (en) 2010-01-07
CA2724629A1 (en) 2009-11-19
SI2297100T1 (sl) 2013-02-28
CY1113341T1 (el) 2016-06-22
EP2297100B1 (en) 2012-10-31
HRP20120917T1 (hr) 2012-12-31
JP2011520903A (ja) 2011-07-21
AU2009246348A1 (en) 2009-11-19
BRPI0912394A2 (pt) 2016-07-26
US20110039855A1 (en) 2011-02-17
EP2297100A1 (en) 2011-03-23
PT2297100E (pt) 2013-01-24

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Legal Events

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU