CL2015000119A1 - El compuesto (r)-1-(1-(metil-sulfonil)-propan-2-il)-4-(trifluoro-metil)-1h-indol-5-carbonitrilo, modulador del receptor de androgeno; composicion farmaceutica; y su uso para tratar consuncion muscular asociada con epoc, con enfermedad cronica del riñon, con insuficiencia cardiaca cronica, e incontinencia urinaria, y para acelerar la reparacion y sanado de fractura de cadera. - Google Patents
El compuesto (r)-1-(1-(metil-sulfonil)-propan-2-il)-4-(trifluoro-metil)-1h-indol-5-carbonitrilo, modulador del receptor de androgeno; composicion farmaceutica; y su uso para tratar consuncion muscular asociada con epoc, con enfermedad cronica del riñon, con insuficiencia cardiaca cronica, e incontinencia urinaria, y para acelerar la reparacion y sanado de fractura de cadera.Info
- Publication number
- CL2015000119A1 CL2015000119A1 CL2015000119A CL2015000119A CL2015000119A1 CL 2015000119 A1 CL2015000119 A1 CL 2015000119A1 CL 2015000119 A CL2015000119 A CL 2015000119A CL 2015000119 A CL2015000119 A CL 2015000119A CL 2015000119 A1 CL2015000119 A1 CL 2015000119A1
- Authority
- CL
- Chile
- Prior art keywords
- methyl
- epoc
- carbonitrile
- propan
- trifluoro
- Prior art date
Links
- SKDVMPZQJMZEAC-SECBINFHSA-N 1-[(2r)-1-methylsulfonylpropan-2-yl]-4-(trifluoromethyl)indole-5-carbonitrile Chemical compound N#CC1=CC=C2N([C@@H](CS(C)(=O)=O)C)C=CC2=C1C(F)(F)F SKDVMPZQJMZEAC-SECBINFHSA-N 0.000 title 1
- 206010007558 Cardiac failure chronic Diseases 0.000 title 1
- 206010020100 Hip fracture Diseases 0.000 title 1
- 206010028289 Muscle atrophy Diseases 0.000 title 1
- 206010046543 Urinary incontinence Diseases 0.000 title 1
- 208000020832 chronic kidney disease Diseases 0.000 title 1
- 150000001875 compounds Chemical class 0.000 title 1
- VZCCETWTMQHEPK-QNEBEIHSSA-N gamma-linolenic acid Chemical compound CCCCC\C=C/C\C=C/C\C=C/CCCCC(O)=O VZCCETWTMQHEPK-QNEBEIHSSA-N 0.000 title 1
- 230000035876 healing Effects 0.000 title 1
- 201000000585 muscular atrophy Diseases 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 239000000849 selective androgen receptor modulator Substances 0.000 title 1
Classifications
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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
- C07D209/02—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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Endocrinology (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261672455P | 2012-07-17 | 2012-07-17 | |
| US201361748874P | 2013-01-04 | 2013-01-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CL2015000119A1 true CL2015000119A1 (es) | 2015-04-24 |
Family
ID=49117887
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2015000119A CL2015000119A1 (es) | 2012-07-17 | 2015-01-16 | El compuesto (r)-1-(1-(metil-sulfonil)-propan-2-il)-4-(trifluoro-metil)-1h-indol-5-carbonitrilo, modulador del receptor de androgeno; composicion farmaceutica; y su uso para tratar consuncion muscular asociada con epoc, con enfermedad cronica del riñon, con insuficiencia cardiaca cronica, e incontinencia urinaria, y para acelerar la reparacion y sanado de fractura de cadera. |
Country Status (39)
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10155099B2 (en) | 2009-09-21 | 2018-12-18 | Cook Regentec Llc | Method for infusing stem cells |
| CN104619693B (zh) | 2012-07-17 | 2019-08-13 | 葛兰素史克知识产权第二有限公司 | 作为选择性雄激素受体调节剂的吲哚腈类 |
| 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 |
| KR20190077607A (ko) * | 2014-10-16 | 2019-07-03 | 지티엑스, 인코포레이티드 | Sarm을 이용하는 비뇨기 장애의 치료 방법 |
| 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 |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ID27280A (id) | 1998-02-25 | 2001-03-22 | Genetics Inst | Inhibitor-inhibitor dari enzim-enzim fosfolipase |
| AU3951899A (en) * | 1998-06-19 | 2000-01-05 | Pfizer Products Inc. | Pyrrolo(2,3-d)pyrimidine compounds |
| US6576265B1 (en) | 1999-12-22 | 2003-06-10 | Acell, Inc. | Tissue regenerative composition, method of making, and method of use thereof |
| ES2471240T3 (es) | 2002-05-24 | 2014-06-25 | Bayer Cropscience Ag | Procedimiento de preparación de derivados de tioalquilamina |
| US7517899B2 (en) * | 2004-03-30 | 2009-04-14 | Wyeth | Phenylaminopropanol derivatives and methods of their use |
| 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 |
| CA2564953A1 (en) | 2004-05-03 | 2005-11-24 | Janssen Pharmaceutica N.V. | Novel indole derivatives as selective androgen receptor modulators (sarms) |
| WO2005111028A1 (en) | 2004-05-03 | 2005-11-24 | Janssen Pharmaceutica N.V. | Novel indole derivatives as selective androgen receptor modulators (sarms) |
| ATE525354T1 (de) | 2004-05-03 | 2011-10-15 | Janssen Pharmaceutica Nv | Benzofuranderivate als selektive androgenrezeptormodulatoren (sarms) |
| DE602005020280D1 (de) * | 2004-06-01 | 2010-05-12 | Hoffmann La Roche | 3-amino-1-arylpropyl-indole als monoamin-wiederaufnahmehemmer |
| WO2007012953A2 (en) * | 2005-07-29 | 2007-02-01 | 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 |
| WO2007108936A2 (en) | 2006-03-15 | 2007-09-27 | Wyeth | N-substituted-azacyclylamines as histamine-3 antagonists |
| 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 |
| WO2008042571A2 (en) | 2006-09-29 | 2008-04-10 | Smithkline Beecham Corporation | Substituted indole compounds |
| RS53382B (sr) * | 2008-08-20 | 2014-10-31 | Zoetis Llc | Jedinjenja pirol [2,3-d]pirimidina |
| US9095572B2 (en) | 2009-01-09 | 2015-08-04 | Board Of Regents Of The University Of Texas System | Pro-neurogenic compounds |
| WO2010118287A1 (en) * | 2009-04-10 | 2010-10-14 | Radius Health, Inc. | Selective androgen receptor modulators |
| AU2010308028A1 (en) * | 2009-10-15 | 2012-04-19 | Pfizer Inc. | Pyrrolo[2,3-d] pyrimidine compounds |
| CA2782720A1 (en) * | 2009-12-18 | 2011-06-23 | Pfizer Inc. | Pyrrolo[2,3-d]pyrimidine compounds |
| RU2598842C2 (ru) * | 2011-01-20 | 2016-09-27 | Мерк Шарп Энд Домэ Корп. | Антагонисты рецептора минералокортикоидов |
| JP6075736B2 (ja) * | 2011-12-21 | 2017-02-08 | ジエンス ヘンルイ メデイシンカンパニー リミテッドＪｉａｎｇｓｕ Ｈｅｎｇｒｕｉ Ｍｅｄｉｃｉｎｅ Ｃｏ．，Ｌｔｄ． | ピロール−６員ヘテロアリール環誘導体、その合成法およびその医薬用途 |
| CN104619693B (zh) * | 2012-07-17 | 2019-08-13 | 葛兰素史克知识产权第二有限公司 | 作为选择性雄激素受体调节剂的吲哚腈类 |
| 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 |
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2013
- 2013-07-15 CN CN201380048232.8A patent/CN104619693B/zh active Active
- 2013-07-15 PT PT137589750T patent/PT2875013T/pt unknown
- 2013-07-15 ES ES13758975.0T patent/ES2657912T3/es active Active
- 2013-07-15 KR KR1020157003959A patent/KR102127939B1/ko active Active
- 2013-07-15 TW TW102125297A patent/TWI574946B/zh active
- 2013-07-15 PE PE2015000039A patent/PE20150371A1/es active IP Right Grant
- 2013-07-15 BR BR112015000940-9A patent/BR112015000940B1/pt active IP Right Grant
- 2013-07-15 JO JOP/2013/0214A patent/JO3384B1/ar active
- 2013-07-15 WO PCT/IB2013/001530 patent/WO2014013309A1/en not_active Ceased
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- 2013-07-15 AU AU2013291721A patent/AU2013291721B2/en active Active
- 2013-07-15 UY UY0001034911A patent/UY34911A/es not_active Application Discontinuation
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- 2013-07-15 US US13/941,911 patent/US8957104B2/en active Active
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2014
- 2014-11-20 US US14/549,034 patent/US9533948B2/en active Active
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- 2015-01-14 PH PH12015500104A patent/PH12015500104B1/en unknown
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- 2016-11-22 US US15/358,458 patent/US10196353B2/en active Active
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