AR034390A1 - Derivados de 1-sulfonil-tetrahidro quinolinas sustituidas, composiciones farmaceuticas y el uso de las mismas para la elaboracion de medicamentos como inhibidores de la gama secretasa - Google Patents
Derivados de 1-sulfonil-tetrahidro quinolinas sustituidas, composiciones farmaceuticas y el uso de las mismas para la elaboracion de medicamentos como inhibidores de la gama secretasaInfo
- Publication number
- AR034390A1 AR034390A1 ARP020102926A ARP020102926A AR034390A1 AR 034390 A1 AR034390 A1 AR 034390A1 AR P020102926 A ARP020102926 A AR P020102926A AR P020102926 A ARP020102926 A AR P020102926A AR 034390 A1 AR034390 A1 AR 034390A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- independently selected
- substituted
- derivatives
- groups
- Prior art date
Links
- 239000003814 drug Substances 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 150000003248 quinolines Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- 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
- A61P25/28—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/58—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- 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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Quinoline Compounds (AREA)
Abstract
Derivados 1-sulfonil-tetrahidro quinolinas sustituidos, caracterizados porque comprenden un compuesto de la fórmula (1) o una sal o solvato farmacéuticamente aceptable del mismo, en la cual: R1 se selecciona entre arilo no sustituido, arilo sustituido con uno o más (por ejemplo, 1-3) grupos R5, heteroarilo, o heteroarilo sustituido con uno o más (por ejemplo, 1-3) grupos R5; R2 es seleccionado entre alquilo, -X(CO)Y, -(CR32)1-4X(CO)y, o cualquira de los grupos mencionados para R1; cada R3 es independientemente seleccionado entre H ó alquilo; cada R3A es independientemente seleccionado entre H ó alquilo; R4 es independientemente seleccionado entre halógeno, -CF3, -OH, -Oalquilo, -OCF3, -CN, -NH2, -CO2alquilo, -CONR6R7, -alquilen-NR6R7, -NR6COalquilo, -NR6COarilo, -NR6COheteroarilo, o -NR6CONR6R7; R5 es independientemente seleccionado entre halógeno, -CF3, -OH, -Oalquilo, -OCF3, -CN, -NH2, -CO2alquilo, -CONR6R7, -alquilen-NR6R7, -NR6COalquilo, -NR6COarilo, -NR6COheteroarilo, o -NR6CONR6R7; X es seleccionado entre -O-, -NH, o -N-alquilo; Y es seleccionado entre -NR6R7 ó -N(R3)(CH2)2-6NR6R7; R6 y R7 son independientemente seleccionados entre H, alquilo, cicloalquilo, -arilalquilo, -heteroarilalquilo, un compuesto de fórmula (a), ó de fórmula (b); o R6 y R7 tomados junto con el átomo de nitrógeno al cual están unidos forman un grupo heterocicloalquilo seleccionado entre los restos de fórmulas (c) a (h); cada R8 es independientemente seleccionado entre alquilo o alquilo sustituido con 1 a 4 grupos hidroxi; cada R9 es independientemente seleccionados entre H, alquilo, alquilo sustituido con 1 a 4 grupos hidroxi, cicloalquilo, cicloalquilo sustituido con 1 a 4 grupos hidroxi, -arilalquilo, -heteroarilalquilo, -COOalquilo, o cualquiera de los grupos mencionados para R1; cada R10 es independientemente seleccionado entre H o alquilo; m representa de 0 a 3 y n es de 0 a 3, de tal manera que m + n sea 1, 2, 3, ó 4; p es de 0 a 4; r es de 0 a 4; s es de 0 a 3; y con la salvedad de que los compuestos de la fórmula (1) no incluyen a los compuestos de fórmulas (2) a (8). Composiciones farmacéuticas y el uso de dichos derivados para la elaboración de medicamentos útiles para el tratamiento de la Enfermedad de Alzheimer.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31001301P | 2001-08-03 | 2001-08-03 | |
| US35551002P | 2002-02-06 | 2002-02-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR034390A1 true AR034390A1 (es) | 2004-02-25 |
Family
ID=26977148
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020102926A AR034390A1 (es) | 2001-08-03 | 2002-08-01 | Derivados de 1-sulfonil-tetrahidro quinolinas sustituidas, composiciones farmaceuticas y el uso de las mismas para la elaboracion de medicamentos como inhibidores de la gama secretasa |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US6683091B2 (es) |
| EP (1) | EP1492765B1 (es) |
| JP (1) | JP4418671B2 (es) |
| KR (1) | KR20040019094A (es) |
| CN (1) | CN1304390C (es) |
| AR (1) | AR034390A1 (es) |
| AT (1) | ATE515495T1 (es) |
| AU (1) | AU2002324582B9 (es) |
| BR (1) | BR0211698A (es) |
| CA (1) | CA2455863C (es) |
| CO (1) | CO5550419A2 (es) |
| HU (1) | HUP0600673A3 (es) |
| IL (1) | IL159848A0 (es) |
| MX (1) | MXPA04001014A (es) |
| NO (1) | NO20040933L (es) |
| PL (1) | PL372212A1 (es) |
| RU (1) | RU2004106540A (es) |
| TW (1) | TWI242555B (es) |
| WO (1) | WO2003014075A2 (es) |
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| US8044259B2 (en) | 2000-08-03 | 2011-10-25 | The Regents Of The University Of Michigan | Determining the capability of a test compound to affect solid tumor stem cells |
| EP1453516A2 (de) * | 2001-10-17 | 2004-09-08 | Boehringer Ingelheim Pharma GmbH & Co.KG | 5-substituierte 4-amino-2-phenylamino-pyrimdinderivate und ihre verwendung als beta-amyloid modulatoren |
| RU2304140C2 (ru) | 2001-12-27 | 2007-08-10 | Дайити Фармасьютикал Ко., Лтд. | ИНГИБИТОРЫ ПРОДУЦИРОВАНИЯ / СЕКРЕЦИИ β-АМИЛОИДНОГО БЕЛКА |
| US7521481B2 (en) | 2003-02-27 | 2009-04-21 | Mclaurin Joanne | Methods of preventing, treating and diagnosing disorders of protein aggregation |
| RU2336270C2 (ru) | 2003-06-30 | 2008-10-20 | Дайити Фармасьютикал Ко., Лтд. | Гетероциклические метилсульфоновые производные |
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| US7598250B2 (en) * | 2003-08-08 | 2009-10-06 | Schering Corporation | Cyclic amine BACE-1 inhibitors having a heterocyclic substituent |
| WO2005074633A2 (en) * | 2004-02-03 | 2005-08-18 | The Regents Of The University Of Michigan | Compositions and methods for characterizing, regulating, diagnosing, and treating cancer |
| ES2383306T3 (es) | 2004-02-03 | 2012-06-20 | The Regents Of The University Of Michigan | Composiciones para el tratamiento del cáncer de mama y de páncreas |
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| HK1253734A1 (zh) | 2015-06-11 | 2019-06-28 | The Regents Of The University Of Michigan | 用作RORγ激动剂和用於治疗疾病的芳基二氢-2H-苯并[B][1,4]恶嗪磺酰胺和相关化合物 |
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| JP2018531958A (ja) | 2015-10-27 | 2018-11-01 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | RORγT阻害薬としてのヘテロアリール置換安息香酸及びその使用 |
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| FR1328176A (fr) * | 1962-07-06 | 1963-05-24 | Monsanto Chemicals | Procédé de préparation de dérivés des hydroquinoléines |
| JPS556321A (en) * | 1978-06-27 | 1980-01-17 | Konishiroku Photo Ind Co Ltd | Color photographic material |
| JPS6395447A (ja) * | 1986-10-11 | 1988-04-26 | Konica Corp | 色素画像の光堅牢性が改良されたハロゲン化銀写真感光材料 |
| KR20010072089A (ko) * | 1998-07-30 | 2001-07-31 | 로즈 암스트롱, 크리스틴 에이. 트러트웨인 | 매트릭스 메탈로프로테이나제 억제제로서 트리시클릭술폰아미드 및 그의 유도체 |
| EP1159263A1 (en) * | 1999-02-26 | 2001-12-05 | Merck & Co., Inc. | Novel sulfonamide compounds and uses thereof |
| IL138686A0 (en) * | 1999-10-01 | 2001-10-31 | Pfizer Prod Inc | α- SULFONYLAMINO HYDROXAMIC ACID INHIBITORS OF MATRIX METALLOPROTEINASES FOR THE TREATMENT OF PERIPHERAL OR CENTRAL NERVOUS SYSTEM DISORDERS |
| EP1222176A1 (en) * | 1999-10-08 | 2002-07-17 | Bristol-Myers Squibb Pharma Company | AMINO LACTAM SULFONAMIDES AS INHIBITORS OF A$g(b) PROTEIN PRODUCTION |
-
2002
- 2002-08-01 AT AT02759233T patent/ATE515495T1/de not_active IP Right Cessation
- 2002-08-01 MX MXPA04001014A patent/MXPA04001014A/es active IP Right Grant
- 2002-08-01 RU RU2004106540/04A patent/RU2004106540A/ru not_active Application Discontinuation
- 2002-08-01 AR ARP020102926A patent/AR034390A1/es unknown
- 2002-08-01 KR KR10-2004-7001505A patent/KR20040019094A/ko not_active Withdrawn
- 2002-08-01 HU HU0600673A patent/HUP0600673A3/hu unknown
- 2002-08-01 CN CNB028152603A patent/CN1304390C/zh not_active Expired - Fee Related
- 2002-08-01 WO PCT/US2002/024323 patent/WO2003014075A2/en not_active Ceased
- 2002-08-01 PL PL02372212A patent/PL372212A1/xx unknown
- 2002-08-01 US US10/210,829 patent/US6683091B2/en not_active Expired - Fee Related
- 2002-08-01 AU AU2002324582A patent/AU2002324582B9/en not_active Ceased
- 2002-08-01 BR BR0211698-7A patent/BR0211698A/pt not_active IP Right Cessation
- 2002-08-01 JP JP2003519025A patent/JP4418671B2/ja not_active Expired - Fee Related
- 2002-08-01 IL IL15984802A patent/IL159848A0/xx unknown
- 2002-08-01 EP EP02759233A patent/EP1492765B1/en not_active Expired - Lifetime
- 2002-08-01 TW TW091117313A patent/TWI242555B/zh active
- 2002-08-01 CA CA2455863A patent/CA2455863C/en not_active Expired - Fee Related
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2004
- 2004-01-21 CO CO04003799A patent/CO5550419A2/es not_active Application Discontinuation
- 2004-03-03 NO NO20040933A patent/NO20040933L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| IL159848A0 (en) | 2004-06-20 |
| HUP0600673A3 (en) | 2011-08-29 |
| BR0211698A (pt) | 2004-11-09 |
| CN1304390C (zh) | 2007-03-14 |
| CA2455863A1 (en) | 2003-02-20 |
| US20030135044A1 (en) | 2003-07-17 |
| MXPA04001014A (es) | 2004-05-27 |
| PL372212A1 (en) | 2005-07-11 |
| RU2004106540A (ru) | 2005-07-27 |
| EP1492765B1 (en) | 2011-07-06 |
| EP1492765A2 (en) | 2005-01-05 |
| TWI242555B (en) | 2005-11-01 |
| WO2003014075A3 (en) | 2004-09-30 |
| JP4418671B2 (ja) | 2010-02-17 |
| NO20040933L (no) | 2004-03-03 |
| CA2455863C (en) | 2010-10-12 |
| US6683091B2 (en) | 2004-01-27 |
| HUP0600673A2 (en) | 2006-12-28 |
| JP2005504760A (ja) | 2005-02-17 |
| KR20040019094A (ko) | 2004-03-04 |
| AU2002324582B9 (en) | 2006-02-16 |
| ATE515495T1 (de) | 2011-07-15 |
| AU2002324582B2 (en) | 2006-01-05 |
| CN1630651A (zh) | 2005-06-22 |
| WO2003014075A2 (en) | 2003-02-20 |
| CO5550419A2 (es) | 2005-08-31 |
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