AR056690A1 - Derivados de indol como inhibidores de indol como inhibidores del receptor 3 de histamina para el tartamiento de trastornos del sueno y cognitivos obesidad y otros trastornos de snc - Google Patents
Derivados de indol como inhibidores de indol como inhibidores del receptor 3 de histamina para el tartamiento de trastornos del sueno y cognitivos obesidad y otros trastornos de sncInfo
- Publication number
- AR056690A1 AR056690A1 ARP060104464A ARP060104464A AR056690A1 AR 056690 A1 AR056690 A1 AR 056690A1 AR P060104464 A ARP060104464 A AR P060104464A AR P060104464 A ARP060104464 A AR P060104464A AR 056690 A1 AR056690 A1 AR 056690A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- fluoroalkyl
- alkoxy
- aryl
- Prior art date
Links
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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
-
- 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
-
- 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
- A61P9/10—Drugs 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
-
- 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
- A61P9/12—Antihypertensives
-
- 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
- C07D209/12—Radicals substituted by oxygen 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
- C07D209/30—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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic 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
- C07D403/12—Heterocyclic 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 chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Child & Adolescent Psychology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Anesthesiology (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
Abstract
Se refiere a compuestos que tienen actividad farmacologica, a composiciones que contienen estos compuestos, y a un método de tratamiento que emplea los compuesto y composiciones. Más particularmente, se refiere a ciertos derivados de indol y sus sales y solvatos. Estos compuestos tienen actividad antagonista del receptor H3 de histamina, también se refiere a composiciones farmacéuticas que contienen estos compuestos y a un método para tratar trastornos en los que el bloqueo del receptor H3 de histamina es provechoso. Reivindicacion 1: Un compuesto de formula (1) donde separador es cualquiera de los restos de formulas (A) a (C), Y es CH o N, con la condicion de que si Y es CH entonces n es 0 a 2; si Y es N entonces n es 2 a 4; si Y es CH entonces R1 y R2 tomados en forma conjunta son -(CH2)a-NR11-(CH2)2- donde a es 1-2 que, cuando se lo toma junto con Y forma un anillo piperidina o pirrolidina que está opcionalmente sustituido con 1 a 3 grupos seleccionados entre F, fluoroalquilo, alquilo C1-4, alcoxi, arilo, cicloalquilo C3-7, heterocicloalquilo que contienen 1-2 heteroátomos seleccionados entre (O, S) y alquil C1-5-O-alquilo C1-5, y si Y es N entonces R1 y R2 son independientemente alquilo C1-5 o cicloalquilo C3-6, o R1 y R2 tomados junto con el N al cual están ligados forman un sistema anular heterocíclico de 5 a 7 miembros con 0-1 heteroátomos adicionales seleccionados entre O y S que está opcionalmente sustituido con 1 a 3 grupos alquilo 1-5, fluoroalquilo o cicloalquilo C3-6, R1 y R2 tomados en forma conjunta son -(CH2)a-NR11-(CH2)2-, donde a es 2-3, que, cuando se lo toma junto con Y forman un anillo piperazina u homopiperazina que está opcionalmente sustituido con 1 a 3 grupos seleccionados entre F, fluoroalquilo, alquilo C1-4, alcoxi, arilo, cicloalquilo C3-7, heterocicloalquilo que contienen 1-2 heteroátomos seleccionados entre (O, S) y alquil C1-5-O-alquilo C1-5; R3 es 0 a 2 grupos seleccionados entre halogeno, alquilo C1-6, alcoxi C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-6, heterocicloalquilo que contienen 1 a 3 heteroátomos seleccionados entre (O, S) y alquil C1-3-O-alquilo C1-5; R4 y R5 se seleccionan independientemente entre H, alquilo C1-5, alcoxi C1-8, alquil C1-5-O-alquilo C1-5, cicloalquilo C3-6, arilo, CF3 y halogeno; R6 es CONR7R8, -(CH2)x-O-R9, alquilo, fluoroalquilo o SO2NR7R8; x es 1 a 4; R7 y R8 son independientemente H, alquilo c1-5 o cicloalquilo C3-6, o R7 y R8 junto con el N al cual están ligados forman un sistema anular heterocíclico de 5 a 7 miembros con 0-1 heteroátomos adicionales seleccionados entre O, S y N(R10), donde el anillo resultante está opcionalmente sustituido con 1 a 3 grupos alquilo C1-5 o cicloalquilo C3- 6; R9 es , alquilo C1-5, cicloalquilo C3-7 o arilo; R10 es alquilo C1-5, alcoxi C1-8, alquil C1-5-O-alquilo C1-5, cicloalquilo C3-6 o arilo; y R11 es alquilo C1-5, fluoroalquilo o cicloalquilo C3-6 y las sales y estereoisomeros individuales farmacéuticamente aceptables de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US72679305P | 2005-10-14 | 2005-10-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR056690A1 true AR056690A1 (es) | 2007-10-17 |
Family
ID=37962842
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060104464A AR056690A1 (es) | 2005-10-14 | 2006-10-11 | Derivados de indol como inhibidores de indol como inhibidores del receptor 3 de histamina para el tartamiento de trastornos del sueno y cognitivos obesidad y otros trastornos de snc |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US7528262B2 (es) |
| EP (1) | EP1945206B1 (es) |
| JP (1) | JP5250420B2 (es) |
| AR (1) | AR056690A1 (es) |
| AU (1) | AU2006304584B2 (es) |
| CA (1) | CA2626028C (es) |
| DK (1) | DK1945206T3 (es) |
| ES (1) | ES2429940T3 (es) |
| HK (1) | HK1122497A1 (es) |
| IL (1) | IL190783A (es) |
| RU (1) | RU2423360C2 (es) |
| TW (1) | TWI378097B (es) |
| WO (1) | WO2007047775A1 (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20080076987A (ko) * | 2005-11-30 | 2008-08-20 | 에프. 호프만-라 로슈 아게 | 5-치환된 인돌-2-카복스아미드 유도체 |
| RS54165B1 (en) | 2008-04-16 | 2015-12-31 | Karo Bio Ab | NEW LIGANDS FOR THE ESTROGENIC RECEPTOR |
| GB201113538D0 (en) | 2011-08-04 | 2011-09-21 | Karobio Ab | Novel estrogen receptor ligands |
| US10174008B2 (en) | 2014-12-03 | 2019-01-08 | Wisconsin Alumni Research Foundation | Synthesis of cyclopropyl indoles and cyclohepta[B]indoles, pharmaceutical compositions containing them and method of using them |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3799943A (en) * | 1971-06-23 | 1974-03-26 | Sterling Drug Inc | 1,2-diphenylindoles |
| TW229140B (es) | 1992-06-05 | 1994-09-01 | Shell Internat Res Schappej B V | |
| US5399599A (en) * | 1993-04-06 | 1995-03-21 | Thiokol Corporation | Thermoplastic elastomeric internal insulation for rocket motors for low temperature applications |
| ATE189676T1 (de) | 1995-04-21 | 2000-02-15 | Rhone Poulenc Agrochimie | Herstellungsverfahren für 1- (chloroaryl)heterozyklische pestizide |
| US6630496B1 (en) | 1996-08-26 | 2003-10-07 | Genetics Institute Llc | Inhibitors of phospholipase enzymes |
| TR200002445T2 (tr) | 1998-02-25 | 2000-12-21 | Genetics Institute, Inc. | Fosfolipaz inhibitörleri. |
| WO2001074815A2 (en) * | 2000-03-31 | 2001-10-11 | Ortho Mcneil Pharmaceutical, Inc. | Phenyl-substituted imidazopyridines |
| DE60138605D1 (de) * | 2000-03-31 | 2009-06-18 | Ortho Mcneil Pharm Inc | Phenyl-substituierte indole als h3 histaminrezeptorantagonisten |
| US6353007B1 (en) * | 2000-07-13 | 2002-03-05 | Boehringer Ingelheim Pharmaceuticals, Inc. | Substituted 1-(4-aminophenyl)indoles and their use as anti-inflammatory agents |
| EP1311482B1 (en) * | 2000-08-08 | 2007-02-21 | Ortho-McNeil Pharmaceutical, Inc. | Non-imidazole aryloxypiperidines as h3 receptor ligands |
| ES2201907B1 (es) * | 2002-05-29 | 2005-06-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de indolilpiperidina como potentes agentes antihistaminicos y antialergicos. |
| GB0224557D0 (en) * | 2002-10-22 | 2002-11-27 | Glaxo Group Ltd | Novel compounds |
| JP2006525366A (ja) | 2003-04-30 | 2006-11-09 | ジ インスチチュート フォー ファーマシューティカル ディスカバリー、エルエルシー | 複素環式カルボン酸置換基 |
| ES2315877T3 (es) * | 2004-06-18 | 2009-04-01 | Biolipox Ab | Indoles utiles en el tratamiento de inflamaciones. |
-
2006
- 2006-10-11 AR ARP060104464A patent/AR056690A1/es unknown
- 2006-10-12 TW TW095137574A patent/TWI378097B/zh not_active IP Right Cessation
- 2006-10-16 DK DK06826203.9T patent/DK1945206T3/da active
- 2006-10-16 EP EP06826203.9A patent/EP1945206B1/en not_active Not-in-force
- 2006-10-16 RU RU2008118904/04A patent/RU2423360C2/ru not_active IP Right Cessation
- 2006-10-16 AU AU2006304584A patent/AU2006304584B2/en not_active Ceased
- 2006-10-16 ES ES06826203T patent/ES2429940T3/es active Active
- 2006-10-16 US US11/581,631 patent/US7528262B2/en not_active Expired - Fee Related
- 2006-10-16 JP JP2008535801A patent/JP5250420B2/ja not_active Expired - Fee Related
- 2006-10-16 WO PCT/US2006/040744 patent/WO2007047775A1/en active Application Filing
- 2006-10-16 CA CA2626028A patent/CA2626028C/en not_active Expired - Fee Related
-
2008
- 2008-04-10 IL IL190783A patent/IL190783A/en not_active IP Right Cessation
- 2008-09-23 US US12/284,574 patent/US7855224B2/en not_active Expired - Fee Related
-
2009
- 2009-01-14 HK HK09100386.3A patent/HK1122497A1/xx not_active IP Right Cessation
-
2010
- 2010-11-10 US US12/943,659 patent/US8129424B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| DK1945206T3 (da) | 2013-07-29 |
| EP1945206A1 (en) | 2008-07-23 |
| US8129424B2 (en) | 2012-03-06 |
| AU2006304584B2 (en) | 2011-11-24 |
| US20090036446A1 (en) | 2009-02-05 |
| IL190783A (en) | 2014-07-31 |
| AU2006304584A1 (en) | 2007-04-26 |
| HK1122497A1 (en) | 2009-05-22 |
| US7528262B2 (en) | 2009-05-05 |
| US7855224B2 (en) | 2010-12-21 |
| TW200745091A (en) | 2007-12-16 |
| JP2009511605A (ja) | 2009-03-19 |
| RU2423360C2 (ru) | 2011-07-10 |
| IL190783A0 (en) | 2008-11-03 |
| WO2007047775A1 (en) | 2007-04-26 |
| ES2429940T3 (es) | 2013-11-18 |
| TWI378097B (en) | 2012-12-01 |
| RU2008118904A (ru) | 2009-11-20 |
| CA2626028A1 (en) | 2007-04-26 |
| US20110059966A1 (en) | 2011-03-10 |
| JP5250420B2 (ja) | 2013-07-31 |
| EP1945206A4 (en) | 2011-05-04 |
| US20070161676A1 (en) | 2007-07-12 |
| EP1945206B1 (en) | 2013-04-24 |
| CA2626028C (en) | 2014-06-17 |
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