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AR063559A1 - Compuesto de tetrahidrociclopenta [b] indol, su uso para la manufactura de un medicamento y composicion farmaceutica que lo comprende - Google Patents

Compuesto de tetrahidrociclopenta [b] indol, su uso para la manufactura de un medicamento y composicion farmaceutica que lo comprende

Info

Publication number
AR063559A1
AR063559A1 ARP070104913A ARP070104913A AR063559A1 AR 063559 A1 AR063559 A1 AR 063559A1 AR P070104913 A ARP070104913 A AR P070104913A AR P070104913 A ARP070104913 A AR P070104913A AR 063559 A1 AR063559 A1 AR 063559A1
Authority
AR
Argentina
Prior art keywords
alkyl
manufacture
nrarb
cyclopropyl
reduction
Prior art date
Application number
ARP070104913A
Other languages
English (en)
Original Assignee
Lilly Co Eli
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
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of AR063559A1 publication Critical patent/AR063559A1/es

Links

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
    • C07D209/58[b]- or [c]-condensed
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D209/58[b]- or [c]-condensed
    • C07D209/70[b]- or [c]-condensed containing carbocyclic rings other than six-membered

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Anesthesiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

Compuesto de tetrahidrociclopenta[b]indol de fórmula (1) donde el centro de carbono "C*" puede estar en la configuración R, S o R/S, R1 representa ciano, CH=NOCH3, -OCHF2, o -OCF3; R2 representa -COR2a o -SO2R2b; R2a representa alquilo C1-4, alcoxi C1-4, ciclopropilo, o -NRaRb; R2b representa alquilo C1-4, ciclopropilo, o -NRaRb; Ra y Rb cada uno representa independientemente cada que se presenta H o alquilo C1-4; y R3 representa un grupo heteroarilo seleccionado del grupo que consiste en piridinilo, pirimidinilo, pirazinilo, piridazinilo, tiazolilo, isotiazolilo, tiadiazolilo, cada uno de los cuales se substituye opcionalmente con 1 o 2 substituyentes independientemente seleccionado del grupo que consiste de metilo, etilo, bromo, cloro, fluoro, -CHF2, -CF3, hidroxi, amino, y -NHCH2CO2H; o una sal farmacéuticamente aceptable del mismo. Su uso para la manufactura de un medicamento útil para el tratamiento de hipogonadismo, reducción de masa o densidad ósea, osteoporosis, osteopenia, reducción de masa o fuerza muscular, sarcopenia, disminución funcional relacionada con la edad, retraso en la pubertad en los varones, anemia, disfunción sexual masculina o femenina, disfunción eréctil, reducción del libido, depresión, o apatía. Composición farmacéutica que lo comprende.
ARP070104913A 2006-11-20 2007-11-05 Compuesto de tetrahidrociclopenta [b] indol, su uso para la manufactura de un medicamento y composicion farmaceutica que lo comprende AR063559A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US86648406P 2006-11-20 2006-11-20

Publications (1)

Publication Number Publication Date
AR063559A1 true AR063559A1 (es) 2009-02-04

Family

ID=39415431

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070104913A AR063559A1 (es) 2006-11-20 2007-11-05 Compuesto de tetrahidrociclopenta [b] indol, su uso para la manufactura de un medicamento y composicion farmaceutica que lo comprende

Country Status (36)

Country Link
US (1) US7968587B2 (es)
EP (1) EP2094658B1 (es)
JP (1) JP5399259B2 (es)
KR (1) KR101121471B1 (es)
CN (1) CN101541749B (es)
AR (1) AR063559A1 (es)
AT (1) ATE538091T1 (es)
AU (1) AU2007324046B2 (es)
BR (1) BRPI0719092B8 (es)
CA (1) CA2670340C (es)
CL (1) CL2007003182A1 (es)
CO (1) CO6190513A2 (es)
CR (1) CR10802A (es)
CY (1) CY1112284T1 (es)
DK (1) DK2094658T3 (es)
EA (1) EA015627B1 (es)
EC (1) ECSP099350A (es)
ES (1) ES2376048T3 (es)
HR (1) HRP20120032T1 (es)
IL (1) IL198410A (es)
JO (1) JO2800B1 (es)
MA (1) MA31072B1 (es)
MX (1) MX2009005251A (es)
MY (1) MY154547A (es)
NO (1) NO342531B1 (es)
NZ (1) NZ576296A (es)
PE (1) PE20081161A1 (es)
PL (1) PL2094658T3 (es)
PT (1) PT2094658E (es)
RS (1) RS52191B (es)
SI (1) SI2094658T1 (es)
TN (1) TN2009000189A1 (es)
TW (1) TWI398438B (es)
UA (1) UA98777C2 (es)
WO (1) WO2008063867A2 (es)
ZA (1) ZA200903096B (es)

Families Citing this family (21)

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Publication number Priority date Publication date Assignee Title
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.
HRP20120917T1 (hr) * 2008-05-16 2012-12-31 Eli Lilly & Company TETRAHIDROCIKLOPENTA[b]INDOLSKI MODULATORI ANDROGENOG RECEPTORA
AR078862A1 (es) 2009-11-13 2011-12-07 Lilly Co Eli Ester isopropilico del acido ((s)-7-ciano-4-((2r,3s)-3-hidroxitetrahidrofuran-2-ilmetil)-1,2,3,4-tetrahidro-ciclopenta(b)indol-2-il)carbamico, composiciones farmaceuticas que lo comprenden y su uso en terapia
MX338831B (es) 2010-02-04 2016-05-03 Radius Health Inc Moduladores selectivos de receptores de androgenos.
ME02474B (me) 2010-05-12 2017-02-20 Radius Health Inc Terapijski režimi
US8642632B2 (en) 2010-07-02 2014-02-04 Radius Health, Inc. Selective androgen receptor modulators
EP2621901B1 (en) 2010-09-28 2015-07-29 Radius Health, Inc Selective androgen receptor modulators
US20140113824A1 (en) 2011-05-10 2014-04-24 Bayer Intellectual Property Gmbh Bicyclic (thio)carbonylamidines
CN103265479B (zh) * 2013-06-14 2017-12-08 南开大学 一种6‑氯甲基烟酸叔丁酯的合成方法
SMT202300072T1 (it) 2014-03-28 2023-05-12 Univ Duke Cancro della mammella mediante l'utilizzo di modulatori selettivi del recetiore degli estrogeni
US9421264B2 (en) 2014-03-28 2016-08-23 Duke University Method of treating cancer using selective estrogen receptor modulators
TWI744723B (zh) 2014-06-20 2021-11-01 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
JOP20180072A1 (ar) * 2014-09-11 2019-01-30 Lilly Co Eli علاج الأعراض المرتبطة بالعلاج بالحرمان من الأندروجين
RU2022108295A (ru) 2016-06-22 2022-04-06 Эллипсес Фарма Лтд Способы лечения ar+ рака молочной железы
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
CN117417263A (zh) 2017-01-05 2024-01-19 雷迪厄斯制药公司 Rad1901-2hcl的多晶型形式
CN112423844B (zh) 2018-07-04 2024-08-13 雷迪厄斯制药公司 Rad1901-2hcl的多晶型形式
MA54946A (fr) 2019-02-12 2021-12-22 Radius Pharmaceuticals Inc Procédés et composés
CN115023225A (zh) * 2020-01-27 2022-09-06 伊尔根制药有限公司 用于治疗肾病的四氢环戊[b]吲哚化合物
US11986461B1 (en) * 2023-08-24 2024-05-21 King Faisal University 3-(1-(3-(dimethylamino)propyl)-4,5-diphenyl-1H-imidazol-2-yl)pyridin-2-ol as an antitumor and antimicrobial compound

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JP5204650B2 (ja) 2005-06-24 2013-06-05 イーライ リリー アンド カンパニー アンドロゲン受容体調節物質として有用なテトラヒドロカルバゾール誘導体
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WO2008019825A1 (en) 2006-08-14 2008-02-21 Santhera Pharmaceuticals (Schweiz) Ag Use of tricyclic indole derivatives for the treatment of muscular diseases
HRP20120917T1 (hr) 2008-05-16 2012-12-31 Eli Lilly & Company TETRAHIDROCIKLOPENTA[b]INDOLSKI MODULATORI ANDROGENOG RECEPTORA

Also Published As

Publication number Publication date
RS52191B (sr) 2012-10-31
CN101541749A (zh) 2009-09-23
CL2007003182A1 (es) 2008-06-27
CY1112284T1 (el) 2015-12-09
ZA200903096B (en) 2010-07-28
NO342531B1 (no) 2018-06-11
MY154547A (en) 2015-06-30
ES2376048T3 (es) 2012-03-08
PE20081161A1 (es) 2008-08-15
US7968587B2 (en) 2011-06-28
NZ576296A (en) 2011-11-25
KR101121471B1 (ko) 2012-02-28
CN101541749B (zh) 2013-03-27
EP2094658B1 (en) 2011-12-21
KR20090082229A (ko) 2009-07-29
TW200827347A (en) 2008-07-01
PT2094658E (pt) 2012-02-22
ECSP099350A (es) 2009-06-30
CR10802A (es) 2009-07-13
TN2009000189A1 (en) 2010-10-18
EA015627B1 (ru) 2011-10-31
US20100069404A1 (en) 2010-03-18
IL198410A0 (en) 2010-02-17
JP5399259B2 (ja) 2014-01-29
CA2670340C (en) 2014-05-20
MX2009005251A (es) 2009-08-19
PL2094658T3 (pl) 2012-05-31
CO6190513A2 (es) 2010-08-19
DK2094658T3 (da) 2012-02-13
EP2094658A2 (en) 2009-09-02
AU2007324046A1 (en) 2008-05-29
ATE538091T1 (de) 2012-01-15
BRPI0719092A2 (pt) 2013-12-03
SI2094658T1 (sl) 2012-04-30
CA2670340A1 (en) 2008-05-29
HRP20120032T1 (hr) 2012-02-29
JP2010510231A (ja) 2010-04-02
WO2008063867A2 (en) 2008-05-29
BRPI0719092B1 (pt) 2020-08-18
WO2008063867A3 (en) 2008-07-31
HK1134089A1 (en) 2010-04-16
JO2800B1 (en) 2014-03-15
TWI398438B (zh) 2013-06-11
IL198410A (en) 2013-09-30
UA98777C2 (en) 2012-06-25
AU2007324046B2 (en) 2012-04-05
NO20092103L (no) 2009-05-28
EA200970500A1 (ru) 2009-10-30
BRPI0719092B8 (pt) 2021-05-25
MA31072B1 (fr) 2010-01-04

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