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DK2875013T3 - Indolecarbonitriler som selektive androgenreceptormodulatorer - Google Patents

Indolecarbonitriler som selektive androgenreceptormodulatorer Download PDF

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Publication number
DK2875013T3
DK2875013T3 DK13758975.0T DK13758975T DK2875013T3 DK 2875013 T3 DK2875013 T3 DK 2875013T3 DK 13758975 T DK13758975 T DK 13758975T DK 2875013 T3 DK2875013 T3 DK 2875013T3
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DK
Denmark
Prior art keywords
compound
muscle
trifluoromethyl
compounds
disease
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DK13758975.0T
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English (en)
Inventor
Philip Stewart Turnbull
Rodolfo Cadilla
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Glaxosmithkline Intellectual Property (No 2) Ltd
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Application filed by Glaxosmithkline Intellectual Property (No 2) Ltd filed Critical Glaxosmithkline Intellectual Property (No 2) Ltd
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Publication of DK2875013T3 publication Critical patent/DK2875013T3/da

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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

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  • 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)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)

Claims (14)

1. Forbindelsen
(R)-1 -(1 -(Methylsulfonyl)propan-2-yl)-4-(trifluormethyl)-1 H-indol-5-carbonitril
2. Enantomerisk beriget blanding omfattende forbindelsen ifølge krav 1.
3. Forbindelse til anvendelse ifølge krav 1 i krystallinsk form.
4. Forbindelse ifølge krav 1 til krav 3 til anvendelse som et aktivt terapeutisk stof.
5. Forbindelse ifølge krav 1 til krav 3 til anvendelse ved behandling af en lidelse udvalgt blandt muskelsvind associeret med kronisk obstruktiv lungesygdom (COPD), muskelsvind associeret med kronisk nyresygdom (CKD), muskelsvind associeret med kronisk hjertesvigt (CHF) og urininkontinens.
6. Forbindelse ifølge krav 1 til krav 3 til anvendelse ved accelerering af reparation og heling af hoftefraktur.
7. Forbindelse ifølge krav 1 til krav 3 til anvendelse ved accelerering af heling af brandsår.
8. Farmaceutisk sammensætning omfattende forbindelsen ifølge krav 1 til krav 3 og et eller flere farmaceutisk acceptable hjælpestoffer.
9. Farmaceutisk sammensætning ifølge krav 8, hvor sammensætningen omfatter 0,1-50 mg af forbindelsen.
10. Forbindelse til anvendelse ifølge et af kravene 5 til 7, hvor der indgives 0,1-50 mg af forbindelsen.
11. Forbindelse ifølge et af kravene 1 til 3 i kombination med et andet terapeutisk middel.
12. Kombination ifølge krav 11 til anvendelse ved behandling af en lidelse udvalgt blandt muskelsvind associeret med kronisk obstruktiv lungesygdom (COPD), muskelsvind associeret med kronisk nyresygdom (CKD), muskelsvind associeret med kronisk hjertesvigt (CHF) og urininkontinens.
13. Kombination ifølge krav 12 til anvendelse ved accelerering af reparation og heling af hoftefraktur.
14. Kombination ifølge krav 12 til anvendelse ved accelerering af heling af brandsår.
DK13758975.0T 2012-07-17 2013-07-15 Indolecarbonitriler som selektive androgenreceptormodulatorer DK2875013T3 (da)

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 (1)

Publication Number Publication Date
DK2875013T3 true DK2875013T3 (da) 2018-01-22

Family

ID=49117887

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Application Number Title Priority Date Filing Date
DK13758975.0T DK2875013T3 (da) 2012-07-17 2013-07-15 Indolecarbonitriler som selektive androgenreceptormodulatorer

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US (5) US8957104B2 (da)
EP (1) EP2875013B1 (da)
JP (1) JP6106746B2 (da)
KR (1) KR102127939B1 (da)
CN (1) CN104619693B (da)
AR (1) AR091770A1 (da)
AU (1) AU2013291721B2 (da)
BR (1) BR112015000940B1 (da)
CA (1) CA2879104C (da)
CL (1) CL2015000119A1 (da)
CO (1) CO7240378A2 (da)
CR (1) CR20150008A (da)
CY (1) CY1120064T1 (da)
DK (1) DK2875013T3 (da)
DO (1) DOP2015000004A (da)
EA (1) EA026371B8 (da)
ES (1) ES2657912T3 (da)
HR (1) HRP20180061T1 (da)
HU (1) HUE036238T2 (da)
IL (1) IL236448A (da)
IN (1) IN2014KN02993A (da)
JO (1) JO3384B1 (da)
LT (1) LT2875013T (da)
ME (1) ME02996B (da)
MX (1) MX349943B (da)
MY (2) MY173845A (da)
NZ (1) NZ703129A (da)
PE (1) PE20150371A1 (da)
PH (1) PH12015500104B1 (da)
PL (1) PL2875013T3 (da)
PT (1) PT2875013T (da)
RS (1) RS56810B1 (da)
SG (1) SG11201408493WA (da)
SI (1) SI2875013T1 (da)
SM (1) SMT201800115T1 (da)
TW (1) TWI574946B (da)
UY (1) UY34911A (da)
WO (1) WO2014013309A1 (da)
ZA (1) ZA201500096B (da)

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JP6556738B2 (ja) * 2014-01-21 2019-08-07 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 （ｒ）−１−（１−（メチルスルホニル）プロパン−２−イル）−４−（トリフルオロメチル）インドリン−５−カルボニトリルの結晶形
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KR102127939B1 (ko) 2020-06-29
SG11201408493WA (en) 2015-02-27
WO2014013309A1 (en) 2014-01-23
RS56810B1 (sr) 2018-04-30
MX349943B (es) 2017-08-21
IL236448A0 (en) 2015-02-26
PH12015500104A1 (en) 2015-03-02
US10710963B2 (en) 2020-07-14
UY34911A (es) 2014-02-28
SMT201800115T1 (it) 2018-03-08
MX2015000825A (es) 2015-07-17
SI2875013T1 (en) 2018-03-30
CN104619693B (zh) 2019-08-13
US10196353B2 (en) 2019-02-05
BR112015000940A2 (pt) 2017-06-27
AU2013291721B2 (en) 2016-02-25
US20170073309A1 (en) 2017-03-16
EA201492237A1 (ru) 2015-06-30
ME02996B (me) 2018-10-20
CA2879104A1 (en) 2014-01-23
CN104619693A (zh) 2015-05-13
BR112015000940B1 (pt) 2022-05-17
KR20150032333A (ko) 2015-03-25
IN2014KN02993A (da) 2015-05-08
HK1208867A1 (en) 2016-03-18
TWI574946B (zh) 2017-03-21
EA026371B1 (ru) 2017-03-31
EP2875013A1 (en) 2015-05-27
JP6106746B2 (ja) 2017-04-05
LT2875013T (lt) 2018-02-26
US20200270210A1 (en) 2020-08-27
JO3384B1 (ar) 2019-03-13
ES2657912T3 (es) 2018-03-07
US8957104B2 (en) 2015-02-17
US20150080449A1 (en) 2015-03-19
AU2013291721A1 (en) 2015-02-26
CL2015000119A1 (es) 2015-04-24
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