EA026371B1 - Индолкарбонитрилы в качестве модуляторов рецептора андрогенов - Google Patents

Индолкарбонитрилы в качестве модуляторов рецептора андрогенов Download PDF

Info

Publication number
EA026371B1
EA026371B1 EA201492237A EA201492237A EA026371B1 EA 026371 B1 EA026371 B1 EA 026371B1 EA 201492237 A EA201492237 A EA 201492237A EA 201492237 A EA201492237 A EA 201492237A EA 026371 B1 EA026371 B1 EA 026371B1
Authority
EA
Eurasian Patent Office
Prior art keywords
muscle atrophy
compound according
atrophy associated
compound
accelerating
Prior art date
Application number
EA201492237A
Other languages
English (en)
Other versions
EA201492237A1 (ru
EA026371B8 (ru
Inventor
Филип Стюарт ТЕРНБУЛЛ
Родольфо Кадилла
Original Assignee
Глаксосмитклайн Интеллекчуал Проперти (№ 2) Дивелопмент Лимитед
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=49117887&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA026371(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Глаксосмитклайн Интеллекчуал Проперти (№ 2) Дивелопмент Лимитед filed Critical Глаксосмитклайн Интеллекчуал Проперти (№ 2) Дивелопмент Лимитед
Publication of EA201492237A1 publication Critical patent/EA201492237A1/ru
Publication of EA026371B1 publication Critical patent/EA026371B1/ru
Publication of EA026371B8 publication Critical patent/EA026371B8/ru

Links

Classifications

    • 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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an alkyl or cycloalkyl radical attached to the ring nitrogen atom
    • 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
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic 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
    • A61K31/403—Heterocyclic 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
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26—Androgens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • 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
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • 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
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • 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
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (AREA)

Abstract

Изобретение относится к нестероидным соединениям, которые являются модуляторами рецептора андрогенов, а также к способам получения и применения таких соединений.

Description

(54) ИНДОЛКАРБОНИТРИЛЫ В КАЧЕСТВЕ МОДУЛЯТОРОВ РЕЦЕПТОРА АНДРОГЕНОВ (31) 61/672,455; 61/748,874 (32) 2012.07.17; 2013.01.04 (33) ϋδ (43) 2015.06.30 (86) РСТДВ2013/001530 (87) \ΥΟ 2014/013309 2014.01.23 (71) (73) Заявитель и патентовладелец:
ГЛАКСОСМИТКЛАЙН ИНТЕЛЛЕКЧУАЛ ПРОПЕРТИ (№ 2) ДИВЕЛОПМЕНТ ЛИМИТЕД (СВ) (72) Изобретатель:
Тернбулл Филип Стюарт, Кадилла Родольфо (ϋδ) (74) Представитель:
Поликарпов А.В. (Κϋ) (56) \¥О-А1-2012097744 АУО-А2-2008042571 \¥0-А1-2010118287 ΥΥΟ-Α2-2007108936 АУО-А1-2005118539 υδ-Α1-2005222148
026371 В1 (57) Изобретение относится к нестероидным соединениям, которые являются модуляторами рецептора андрогенов, а также к способам получения и применения таких соединений.
026371 Β1

Claims (10)

  1. ФОРМУЛА ИЗОБРЕТЕНИЯ
    1. Соединение
  2. 2. Фармацевтическая композиция для лечения расстройств, опосредованных андрогенной активностью, содержащая соединение по п.1 и один или более фармацевтически приемлемых эксципиентов.
    - 42 026371
  3. 3. Способ лечения расстройства, выбранного из мышечной атрофии, ассоциированной с хроническим обструктивным заболеванием легких (СОРЭ), мышечной атрофии, ассоциированной с хроническим заболеванием почек (СКЭ), мышечной атрофии, ассоциированной с хронической сердечной недостаточностью (СИР), и недержания мочи, включающий введение соединения по п. 1 субъекту-человеку.
  4. 4. Применение соединения по п.1 в изготовлении лекарственного средства для лечения расстройства, выбранного из мышечной атрофии, ассоциированной с хроническим обструктивным заболеванием легких (СОРЭ), мышечной атрофии, ассоциированной с хроническим заболеванием почек (СКЭ), мышечной атрофии, ассоциированной с хронической сердечной недостаточностью (СЫР), и недержания мочи.
  5. 5. Способ ускорения репарации и заживления перелома костей тазобедренного сустава, включающий введение соединения по п. 1 субъекту-человеку.
  6. 6. Применение соединения по п.1 в изготовлении лекарственного средства для ускорения репарации и заживления перелома костей тазобедренного сустава.
  7. 7. Способ ускорения заживления ожога, включающий введение соединения по п.1 субъектучеловеку.
  8. 8. Применение соединения по п.1 в изготовлении лекарственного средства для ускорения заживления ожога.
  9. 9. Фармацевтическая композиция по п.2, содержащая 0,1-50 мг соединения.
  10. 10. Способ по любому из пп.3, 5 или 7, при котором вводят 0,1-50 мг соединения.
EA201492237A 2012-07-17 2013-07-15 Индолкарбонитрилы в качестве модуляторов рецептора андрогенов EA026371B8 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261672455P 2012-07-17 2012-07-17
US201361748874P 2013-01-04 2013-01-04
PCT/IB2013/001530 WO2014013309A1 (en) 2012-07-17 2013-07-15 Indolecarbonitriles as selective androgen receptor modulators

Publications (3)

Publication Number Publication Date
EA201492237A1 EA201492237A1 (ru) 2015-06-30
EA026371B1 true EA026371B1 (ru) 2017-03-31
EA026371B8 EA026371B8 (ru) 2017-06-30

Family

ID=49117887

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201492237A EA026371B8 (ru) 2012-07-17 2013-07-15 Индолкарбонитрилы в качестве модуляторов рецептора андрогенов

Country Status (39)

Country Link
US (5) US8957104B2 (ru)
EP (1) EP2875013B1 (ru)
JP (1) JP6106746B2 (ru)
KR (1) KR102127939B1 (ru)
CN (1) CN104619693B (ru)
AR (1) AR091770A1 (ru)
AU (1) AU2013291721B2 (ru)
BR (1) BR112015000940B1 (ru)
CA (1) CA2879104C (ru)
CL (1) CL2015000119A1 (ru)
CO (1) CO7240378A2 (ru)
CR (1) CR20150008A (ru)
CY (1) CY1120064T1 (ru)
DK (1) DK2875013T3 (ru)
DO (1) DOP2015000004A (ru)
EA (1) EA026371B8 (ru)
ES (1) ES2657912T3 (ru)
HK (1) HK1208867A1 (ru)
HR (1) HRP20180061T1 (ru)
HU (1) HUE036238T2 (ru)
IL (1) IL236448A (ru)
IN (1) IN2014KN02993A (ru)
JO (1) JO3384B1 (ru)
LT (1) LT2875013T (ru)
ME (1) ME02996B (ru)
MX (1) MX349943B (ru)
MY (2) MY173845A (ru)
NZ (1) NZ703129A (ru)
PE (1) PE20150371A1 (ru)
PH (1) PH12015500104B1 (ru)
PL (1) PL2875013T3 (ru)
PT (1) PT2875013T (ru)
RS (1) RS56810B1 (ru)
SG (1) SG11201408493WA (ru)
SI (1) SI2875013T1 (ru)
TW (1) TWI574946B (ru)
UY (1) UY34911A (ru)
WO (1) WO2014013309A1 (ru)
ZA (1) ZA201500096B (ru)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10155099B2 (en) 2009-09-21 2018-12-18 Cook Regentec Llc Method for infusing stem cells
JP6106746B2 (ja) 2012-07-17 2017-04-05 グラクソスミスクライン、インテレクチュアル、プロパティー、（ナンバー２）、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ （Ｎｏ．２） Ｌｉｍｉｔｅｄ 選択的アンドロゲン受容体調節剤としてのインドールカルボニトリル類
WO2015110958A1 (en) 2014-01-21 2015-07-30 Glaxosmithkline Intellectual Property (No.2) Limited Crystalline forms of (r)-1 -(1-(methylsulfonyl)propan-2-yl)-4-(trifluoromethyl)indoline-5-carbonitrile
EP3206675A4 (en) * 2014-10-16 2018-07-11 GTx, Inc. METHODS OF TREATING UROLOGICAL DISORDERS USING SARMs
CN105130872B (zh) * 2015-08-25 2018-01-30 江西师范大学 一种3位三氟甲基取代吲哚的制备方法
CN110437125B (zh) * 2019-09-06 2021-03-12 苏州旺山旺水生物医药有限公司 一种Tezacaftor中间体II的制备方法
WO2022204235A1 (en) * 2021-03-23 2022-09-29 Nido Biosciences, Inc. Bicyclic compounds as androgen receptor modulators
CN115010574B (zh) * 2022-06-06 2024-01-05 爱斯特（成都）生物制药股份有限公司 1-溴-2-氯-4-氟-2碘苯的合成方法

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050222148A1 (en) * 2004-03-30 2005-10-06 Wyeth Phenylaminopropanol derivatives and methods of their use
WO2005118539A1 (en) * 2004-06-01 2005-12-15 F.Hoffmann-La Roche Ag 3-amino-1-arylpropyl indoles as monoamine reuptake inhibitor
WO2007108936A2 (en) * 2006-03-15 2007-09-27 Wyeth N-substituted-azacyclylamines as histamine-3 antagonists
WO2008042571A2 (en) * 2006-09-29 2008-04-10 Smithkline Beecham Corporation Substituted indole compounds
WO2010118287A1 (en) * 2009-04-10 2010-10-14 Radius Health, Inc. Selective androgen receptor modulators
WO2012097744A1 (en) * 2011-01-20 2012-07-26 Merck Sharp & Dohme Corp. Mineralocorticoid receptor antagonists

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1056719A2 (en) 1998-02-25 2000-12-06 Genetics Institute, Inc. Inhibitors of phospholipase enzymes
ID26698A (id) * 1998-06-19 2001-02-01 Pfizer Prod Inc SENYAWA-SENYAWA PIROLO [2,3-d] PIRIMIDINA
US6576265B1 (en) 1999-12-22 2003-06-10 Acell, Inc. Tissue regenerative composition, method of making, and method of use thereof
US7235668B2 (en) 2002-05-24 2007-06-26 Bayer Cropscience Ag Process for the preparation of thioalkylamine derivatives
CN1960973A (zh) * 2004-03-30 2007-05-09 惠氏公司 作为去甲肾上腺素(ne)与血清素(5－h t)活性和单胺重摄取的调控剂以治疗血管舒缩症状(vms)的1－(1h－吲哚－1－基)－3－(4－甲基哌嗪－1－基)－1－苯基丙烷－2－醇衍生物和相关化合物
ATE525354T1 (de) 2004-05-03 2011-10-15 Janssen Pharmaceutica Nv Benzofuranderivate als selektive androgenrezeptormodulatoren (sarms)
US7427682B2 (en) 2004-05-03 2008-09-23 Janssen Pharmaceutica N.V. Indole derivatives as selective androgen receptor modulators (SARMS)
EP1753749B1 (en) 2004-05-03 2014-07-30 Janssen Pharmaceutica NV Novel indole derivatives as selective androgen receptor modulators (sarms)
EP1913000B1 (en) * 2005-07-29 2012-01-11 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidine derivatives; their intermediates and synthesis
GB0526246D0 (en) * 2005-12-22 2006-02-01 Novartis Ag Organic compounds
CN101426778A (zh) * 2006-03-15 2009-05-06 惠氏公司 作为组胺-3拮抗剂的n-经取代-氮杂环基胺
JP4884570B2 (ja) * 2008-08-20 2012-02-29 ファイザー・インク ピロロ［２，３−ｄ］ピリミジン化合物
IN2012DN02577A (ru) * 2009-10-15 2015-08-28 Pfizer
JP5739446B2 (ja) * 2009-12-18 2015-06-24 ファイザー・インク ピロロ［２，３−ｄ］ピリミジン化合物
DK2590647T3 (en) 2010-07-07 2018-02-12 Univ Texas Pro-neurogenic compounds
PL2796460T3 (pl) * 2011-12-21 2018-12-31 Jiangsu Hengrui Medicine Co. Ltd. Sześcioczłonowa pirolowa heteroarylowa pochodna pierścieniowa, sposób jej otrzymywania i zastosowania medyczne
JP6106746B2 (ja) * 2012-07-17 2017-04-05 グラクソスミスクライン、インテレクチュアル、プロパティー、（ナンバー２）、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ （Ｎｏ．２） Ｌｉｍｉｔｅｄ 選択的アンドロゲン受容体調節剤としてのインドールカルボニトリル類
WO2015110958A1 (en) * 2014-01-21 2015-07-30 Glaxosmithkline Intellectual Property (No.2) Limited Crystalline forms of (r)-1 -(1-(methylsulfonyl)propan-2-yl)-4-(trifluoromethyl)indoline-5-carbonitrile

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050222148A1 (en) * 2004-03-30 2005-10-06 Wyeth Phenylaminopropanol derivatives and methods of their use
WO2005118539A1 (en) * 2004-06-01 2005-12-15 F.Hoffmann-La Roche Ag 3-amino-1-arylpropyl indoles as monoamine reuptake inhibitor
WO2007108936A2 (en) * 2006-03-15 2007-09-27 Wyeth N-substituted-azacyclylamines as histamine-3 antagonists
WO2008042571A2 (en) * 2006-09-29 2008-04-10 Smithkline Beecham Corporation Substituted indole compounds
WO2010118287A1 (en) * 2009-04-10 2010-10-14 Radius Health, Inc. Selective androgen receptor modulators
WO2012097744A1 (en) * 2011-01-20 2012-07-26 Merck Sharp & Dohme Corp. Mineralocorticoid receptor antagonists

Also Published As

Publication number Publication date
JP2015522603A (ja) 2015-08-06
ZA201500096B (en) 2017-07-26
HUE036238T2 (hu) 2018-06-28
MX349943B (es) 2017-08-21
EP2875013A1 (en) 2015-05-27
US11299457B2 (en) 2022-04-12
BR112015000940A2 (pt) 2017-06-27
SI2875013T1 (en) 2018-03-30
CY1120064T1 (el) 2018-12-12
US20200270210A1 (en) 2020-08-27
BR112015000940B1 (pt) 2022-05-17
PE20150371A1 (es) 2015-03-27
IL236448A0 (en) 2015-02-26
US20140024694A1 (en) 2014-01-23
CL2015000119A1 (es) 2015-04-24
CN104619693B (zh) 2019-08-13
DOP2015000004A (es) 2015-03-15
AU2013291721B2 (en) 2016-02-25
CO7240378A2 (es) 2015-04-17
EA201492237A1 (ru) 2015-06-30
US10710963B2 (en) 2020-07-14
KR102127939B1 (ko) 2020-06-29
LT2875013T (lt) 2018-02-26
PH12015500104A1 (en) 2015-03-02
ES2657912T3 (es) 2018-03-07
US8957104B2 (en) 2015-02-17
JP6106746B2 (ja) 2017-04-05
PL2875013T3 (pl) 2018-06-29
JO3384B1 (ar) 2019-03-13
CA2879104A1 (en) 2014-01-23
US20190127326A1 (en) 2019-05-02
US10196353B2 (en) 2019-02-05
UY34911A (es) 2014-02-28
KR20150032333A (ko) 2015-03-25
EA026371B8 (ru) 2017-06-30
US20170073309A1 (en) 2017-03-16
CR20150008A (es) 2015-03-09
IN2014KN02993A (ru) 2015-05-08
WO2014013309A1 (en) 2014-01-23
AU2013291721A1 (en) 2015-02-26
DK2875013T3 (en) 2018-01-22
RS56810B1 (sr) 2018-04-30
AR091770A1 (es) 2015-02-25
MY173845A (en) 2020-02-24
IL236448A (en) 2016-10-31
TWI574946B (zh) 2017-03-21
HK1208867A1 (en) 2016-03-18
US20150080449A1 (en) 2015-03-19
CA2879104C (en) 2020-08-25
ME02996B (me) 2018-10-20
US9533948B2 (en) 2017-01-03
SG11201408493WA (en) 2015-02-27
HRP20180061T1 (hr) 2018-02-23
MY198512A (en) 2023-09-01
PH12015500104B1 (en) 2015-03-02
EP2875013B1 (en) 2017-11-29
CN104619693A (zh) 2015-05-13
NZ703129A (en) 2017-06-30
TW201416349A (zh) 2014-05-01
PT2875013T (pt) 2018-02-28
MX2015000825A (es) 2015-07-17

Similar Documents

Publication Publication Date Title
EA026371B1 (ru) Индолкарбонитрилы в качестве модуляторов рецептора андрогенов
EA201491460A1 (ru) ПРИМЕНЕНИЕ ЛАХИНИМОДА В ЛЕЧЕНИИ ПАЦИЕНТОВ С БОЛЕЗНЬЮ КРОНА, У КОТОРЫХ НЕ ЭФФЕКТИВНА ТЕРАПИЯ ПЕРВОЙ ЛИНИИ АНТИ-TNFα
EA201690069A1 (ru) Применение высоких доз придопидина для лечения болезни хантингтона
RU2014111478A (ru) Лечение с использованием ацетата эсликарбазепина или эсликарбазепина
MY167423A (en) Quinoline carboxamide and quinoline carbonitrile derivatives as mglur2-negative allosteric modulators,compositions,and their use
NZ606993A (en) Combination pharmaceutical composition and methods of treating and preventing the infectious diseases
JP2010505850A5 (ru)
JP5767122B2 (ja) 特定の癌の治療のためのｒｄｅａ１１９／ｂａｙ８６９７６６を含む組み合わせ医薬
MX2018008021A (es) Metodos y composiciones para el tratamiento de trastornos relacionados con convulsiones.
RU2012108656A (ru) Применение 4-аминопиридина для улучшения состояния при нейрокогнитивном и/или нейропсихиатрическом нарушении у пациентов с демиелинизирующими и другими заболеваниями нервной системы
JP2015522603A5 (ru)
RU2013127420A (ru) Способы уменьшения психогенного или компульсивного переедания
RU2011146032A (ru) Соединения-агонисты рецептора 5-ht4 для лечения расстройств познавательной способности
JP2015532293A5 (ja) 糖尿病患者における心不全の治療用組成物
RU2020120156A (ru) Лечение приливов и потери костной ткани, вызванных андрогенной депривационной терапией с применением цис-кломифена
WO2009003694A3 (en) Method for treating diseases related to mitochondrial dysfunction
RU2011142152A (ru) Доза ave5026 для лечения тромбоэмболии вен у пациентов с тяжелой почечной недостаточностью
NZ625673A (en) Use of a neuregulin to treat peripheral nerve injury
RU2012107483A (ru) Отамиксабан для лечения инфаркта миокарда без подъема сегмента st у пациентов пожилого возраста и пациентов с нарушенной функцией почек
DK1830857T3 (da) Beclomethasondipropionat og prednison til reducering af dødelighed associeret med Graft-Versus-Host sygdom
MX2010006310A (es) O-desmetil-venlafaxina para el tratamiento de transtorno depresivo mayor.
WO2020234431A8 (en) Treatment of hyperammonemia in patients with renal insufficiency
EA201590825A1 (ru) Способы контролирования кровяного давления и снижения диспноэ при сердечной недостаточности
HRP20120422T1 (hr) Farmaceutski pripravak koji sadrži stefaglabrin sulfat za liječenje demijelinizirajućih bolesti živčanog sustava i za unaprjeđivanje procesa obnavljanja mijelinske ovojnice živčanih vlakana
Bedair et al. Angiotensin receptor blockers improve muscle regeneration and decrease fibrosis in injured skeletal muscle

Legal Events

Date Code Title Description
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 KG TM