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
-
- 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
-
- 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
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (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) |
Families Citing this family (77)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6984522B2 (en) | 2000-08-03 | 2006-01-10 | Regents Of The University Of Michigan | Isolation and use of solid tumor stem cells |
| 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 |
| JP4329905B2 (ja) | 2001-12-27 | 2009-09-09 | 第一三共株式会社 | βアミロイド蛋白産生・分泌阻害剤 |
| US7521481B2 (en) | 2003-02-27 | 2009-04-21 | Mclaurin Joanne | Methods of preventing, treating and diagnosing disorders of protein aggregation |
| CA2526487A1 (en) | 2003-06-30 | 2005-01-06 | Daiichi Pharmaceutical Co., Ltd. | Heterocyclic methyl sulfone derivative |
| DE602004019793D1 (de) * | 2003-08-08 | 2009-04-16 | Schering Corp | Cyclische amine mit benzamidsubstituent als bace-1-inhibitoren |
| WO2005014540A1 (en) * | 2003-08-08 | 2005-02-17 | Schering Corporation | Cyclic amine base-1 inhibitors having a heterocyclic substituent |
| US20050232927A1 (en) * | 2004-02-03 | 2005-10-20 | The Regents Of The University Of Michigan | Compositions and methods for characterizing, regulating, diagnosing, and treating cancer |
| ATE552851T1 (de) | 2004-02-03 | 2012-04-15 | Univ Michigan | Zusammensetzungen zur behandlung von brust- und bauchspeicheldrüsenkrebs |
| JP2007531742A (ja) * | 2004-04-05 | 2007-11-08 | シェーリング コーポレイション | 新規のγセクレターゼインヒビター |
| CA2567343A1 (en) * | 2004-05-20 | 2005-12-01 | Elan Pharmaceuticals, Inc. | N-cyclic sulfonamido inhibitors of gamma secretase |
| EP1789404B1 (en) * | 2004-06-30 | 2010-03-24 | Schering Corporation | Substituted n-arylsulfonylheterocyclic amines as gamma-secretase inhibitors |
| ATE491693T1 (de) * | 2004-07-22 | 2011-01-15 | Schering Corp | Substituierte amide als inhibitoren der beta- sekretase |
| BRPI0610532A2 (pt) * | 2005-04-08 | 2010-06-29 | Daiichi Sankyo Co Ltd | derivado de piridilmetilsulfona |
| US20060252073A1 (en) * | 2005-04-18 | 2006-11-09 | Regents Of The University Of Michigan | Compositions and methods for the treatment of cancer |
| ES2436795T3 (es) | 2005-06-14 | 2014-01-07 | Merck Sharp & Dohme Corp. | Inhibidores heterocíclicos de aspartil proteasa, preparación y uso de los mismos |
| US7790745B2 (en) | 2005-10-21 | 2010-09-07 | Bristol-Myers Squibb Company | Tetrahydroisoquinoline LXR Modulators |
| US7741317B2 (en) | 2005-10-21 | 2010-06-22 | Bristol-Myers Squibb Company | LXR modulators |
| WO2007053648A2 (en) | 2005-10-31 | 2007-05-10 | The Regents Of The University Of Michigan | Compositions and methods for treating and diagnosing cancer |
| US7723477B2 (en) * | 2005-10-31 | 2010-05-25 | Oncomed Pharmaceuticals, Inc. | Compositions and methods for inhibiting Wnt-dependent solid tumor cell growth |
| EP2511298B1 (en) | 2005-10-31 | 2019-01-16 | Oncomed Pharmaceuticals, Inc. | Compositions and Methods for Treating Cancer based on human FZD receptors |
| CN102702044A (zh) | 2006-01-20 | 2012-10-03 | 先灵公司 | 作为γ分泌酶抑制剂的碳环和杂环芳基砜化合物 |
| EP1998785A4 (en) * | 2006-02-21 | 2009-06-17 | Univ Michigan | TREATMENT OF CANCER BY AN ANTAGONIST OF THE HEDGEHOG SIGNALING PATH |
| WO2011053822A2 (en) | 2009-11-01 | 2011-05-05 | The Brigham And Women's Hospital, Inc. | Notch inhibition in the treatment and prevention of obesity and metabolic syndrome |
| US9567396B2 (en) | 2006-03-07 | 2017-02-14 | Evonik Degussa Gmbh | Notch inhibition in the prevention of vein graft failure |
| US8133857B2 (en) * | 2006-03-07 | 2012-03-13 | The Brigham and Women's FHospital, Inc. | NOTCH inhibition in the treatment of atherosclerosis |
| TW200813054A (en) * | 2006-06-02 | 2008-03-16 | Elan Pharm Inc | Fused, tricyclic sulfonamide inhibitors of gamma secretase |
| WO2008055945A1 (en) | 2006-11-09 | 2008-05-15 | Probiodrug Ag | 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases |
| ATE554085T1 (de) | 2006-11-30 | 2012-05-15 | Probiodrug Ag | Neue inhibitoren von glutaminylcyclase |
| EP2106439B1 (en) | 2007-01-24 | 2014-11-12 | The Regents of the University of Michigan | Compositions and methods for treating and diagnosing pancreatic cancer |
| EA200901140A1 (ru) | 2007-03-01 | 2010-04-30 | Пробиодруг Аг | Новое применение ингибиторов глутаминилциклазы |
| JP5667440B2 (ja) | 2007-04-18 | 2015-02-12 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのチオ尿素誘導体 |
| BRPI0814256A8 (pt) | 2007-07-05 | 2016-02-10 | Schering Corp | Inibidores de tetrahidropiranocromeno gama secretase |
| CL2008002084A1 (es) * | 2007-07-17 | 2009-01-23 | Schering Corp | Compuestos derivados de bencensulfonil cromano, tiocromano, tetrahidronaftaleno, inhibidores de la gamma secretasa; composicion farmaceutica que lo comprende; y su uso en la preparacion de medicamentos utiles para tratar enfermedades neurodegenerativas |
| BRPI0919473A2 (pt) | 2008-09-26 | 2017-08-29 | Oncomed Pharm Inc | Agentes de ligação frizzled e usos dos mesmos |
| AU2009313527A1 (en) * | 2008-11-06 | 2010-05-14 | Merck Sharp & Dohme Corp. | Gamma secretase modulators |
| WO2010138901A1 (en) * | 2009-05-29 | 2010-12-02 | Biogen Idec Ma Inc | Carboxylic acid-containing compounds, derivatives thereof, and related methods of use |
| WO2011009064A1 (en) * | 2009-07-17 | 2011-01-20 | The J. David Gladstone Institutes | Methods of controlling cell proliferation |
| CN102695546B (zh) | 2009-09-11 | 2014-09-10 | 前体生物药物股份公司 | 作为谷氨酰胺酰环化酶抑制剂的杂环衍生物 |
| EP2485590B1 (en) | 2009-10-08 | 2015-01-07 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| EP2485591B1 (en) | 2009-10-08 | 2016-03-23 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| US8569310B2 (en) | 2009-10-08 | 2013-10-29 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use |
| TWI535445B (zh) | 2010-01-12 | 2016-06-01 | 安可美德藥物股份有限公司 | Wnt拮抗劑及治療和篩選方法 |
| US9181233B2 (en) | 2010-03-03 | 2015-11-10 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| US8269019B2 (en) | 2010-03-10 | 2012-09-18 | Probiodrug Ag | Inhibitors |
| NZ602700A (en) | 2010-04-01 | 2014-10-31 | Oncomed Pharm Inc | Frizzled-binding agents and uses thereof |
| JP5945532B2 (ja) | 2010-04-21 | 2016-07-05 | プロビオドルグ エージー | グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体 |
| JP5275315B2 (ja) * | 2010-10-01 | 2013-08-28 | 学校法人近畿大学 | 新規化合物及びβ−セクレターゼ阻害剤 |
| EP2638014B1 (en) | 2010-11-08 | 2017-01-04 | Lycera Corporation | N-sulfonylated tetrahydroquinolines and related bicyclic compounds for inhibition of ror-gamma activity and the treatment of diseases |
| US8530670B2 (en) | 2011-03-16 | 2013-09-10 | Probiodrug Ag | Inhibitors |
| US9221839B2 (en) | 2011-04-07 | 2015-12-29 | Merck Sharp & Dohme Corp. | C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
| US9145426B2 (en) | 2011-04-07 | 2015-09-29 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
| CN103874496A (zh) | 2011-08-22 | 2014-06-18 | 默沙东公司 | 作为bace抑制剂的2-螺-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其用途 |
| WO2013059302A1 (en) | 2011-10-17 | 2013-04-25 | Nationwide Children's Hospital, Inc. | Products and methods for aortic abdominal aneurysm |
| RU2014149136A (ru) | 2012-05-08 | 2016-07-10 | Мерк Шарп И Доум Корп. | ТЕТРАГИДРОНАФТИРИДИНОВЫЕ И РОДСТВЕННЫЕ БИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ ДЛЯ ИНГИБИРОВАНИЯ RORγ АКТИВНОСТИ И ЛЕЧЕНИЯ ЗАБОЛЕВАНИЯ |
| JP6242868B2 (ja) | 2012-05-08 | 2017-12-06 | リセラ・コーポレイションLycera Corporation | RORγのアゴニストとしての使用のためおよび疾患の処置のためのテトラヒドロ[1,8]ナフチリジンスルホンアミドおよび関連化合物 |
| JP2015536933A (ja) | 2012-10-23 | 2015-12-24 | オンコメッド ファーマシューティカルズ インコーポレイテッド | Wnt経路結合剤を用いて神経内分泌腫瘍を処置する方法 |
| AU2014212081A1 (en) | 2013-02-04 | 2015-08-13 | Oncomed Pharmaceuticals, Inc. | Methods and monitoring of treatment with a Wnt pathway inhibitor |
| US9168300B2 (en) | 2013-03-14 | 2015-10-27 | Oncomed Pharmaceuticals, Inc. | MET-binding agents and uses thereof |
| WO2015095788A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | 2-ACYLAMIDOMETHYL AND SULFONYLAMIDOMETHYL BENZOXAZINE CARBAMATES FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE |
| WO2015095792A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Carbamate benzoxaxine propionic acids and acid derivatives for modulation of rorgamma activity and the treatment of disease |
| WO2015095795A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | TETRAHYDRONAPHTHYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE, AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE |
| US10532088B2 (en) | 2014-02-27 | 2020-01-14 | Lycera Corporation | Adoptive cellular therapy using an agonist of retinoic acid receptor-related orphan receptor gamma and related therapeutic methods |
| US9896441B2 (en) | 2014-05-05 | 2018-02-20 | Lycera Corporation | Tetrahydroquinoline sulfonamide and related compounds for use as agonists of RORγ and the treatment of disease |
| US10189777B2 (en) | 2014-05-05 | 2019-01-29 | Lycera Corporation | Benzenesulfonamido and related compounds for use as agonists of RORγ and the treatment of disease |
| CN104027810B (zh) * | 2014-06-30 | 2016-02-10 | 王涛 | 一种构建先天性肝内胆管发育不良综合征动物模型的方法 |
| CA2975997A1 (en) | 2015-02-11 | 2016-08-18 | Merck Sharp & Dohme Corp. | Substituted pyrazole compounds as rorgammat inhibitors and uses thereof |
| US10421751B2 (en) | 2015-05-05 | 2019-09-24 | Lycera Corporation | Dihydro-2H-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of RORγ and the treatment of disease |
| WO2016201225A1 (en) | 2015-06-11 | 2016-12-15 | Lycera Corporation | Aryl dihydro-2h-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of rory and the treatment of disease |
| EP3368535B1 (en) | 2015-10-27 | 2020-12-02 | Merck Sharp & Dohme Corp. | Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof |
| WO2017075178A1 (en) | 2015-10-27 | 2017-05-04 | Merck Sharp & Dohme Corp. | SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF |
| US10287272B2 (en) | 2015-10-27 | 2019-05-14 | Merck Sharp & Dohme Corp. | Substituted indazole compounds as RORgammaT inhibitors and uses thereof |
| PL3461819T3 (pl) | 2017-09-29 | 2020-11-30 | Probiodrug Ag | Inhibitory cyklazy glutaminylowej |
| WO2020016377A1 (en) | 2018-07-19 | 2020-01-23 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Combination for treating cancer |
| EP4244391A1 (en) | 2020-11-16 | 2023-09-20 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and compositions for predicting and treating uveal melanoma |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| AP2001002037A0 (en) * | 1998-07-30 | 2001-03-31 | Warner Lambert Co | Tricyclic sulfonamides and their derivatives as inhibitors of matrix metalloproteinases. |
| CZ20013000A3 (cs) | 1999-02-26 | 2002-02-13 | Merck & Co., Inc. | Nové sulfonamidové sloučeniny a jejich pouľití |
| 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 |
| WO2001027108A1 (en) * | 1999-10-08 | 2001-04-19 | Bristol-Myers Squibb Pharma Company | AMINO LACTAM SULFONAMIDES AS INHIBITORS OF Aβ PROTEIN PRODUCTION |
-
2002
- 2002-08-01 PL PL02372212A patent/PL372212A1/xx unknown
- 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 MX MXPA04001014A patent/MXPA04001014A/es active IP Right Grant
- 2002-08-01 JP JP2003519025A patent/JP4418671B2/ja not_active Expired - Fee Related
- 2002-08-01 US US10/210,829 patent/US6683091B2/en not_active Expired - Fee Related
- 2002-08-01 IL IL15984802A patent/IL159848A0/xx unknown
- 2002-08-01 CN CNB028152603A patent/CN1304390C/zh not_active Expired - Fee Related
- 2002-08-01 CA CA2455863A patent/CA2455863C/en not_active Expired - Fee Related
- 2002-08-01 BR BR0211698-7A patent/BR0211698A/pt not_active IP Right Cessation
- 2002-08-01 RU RU2004106540/04A patent/RU2004106540A/ru not_active Application Discontinuation
- 2002-08-01 AT AT02759233T patent/ATE515495T1/de not_active IP Right Cessation
- 2002-08-01 EP EP02759233A patent/EP1492765B1/en not_active Expired - Lifetime
- 2002-08-01 WO PCT/US2002/024323 patent/WO2003014075A2/en not_active Ceased
- 2002-08-01 TW TW091117313A patent/TWI242555B/zh active
- 2002-08-01 HU HU0600673A patent/HUP0600673A3/hu unknown
- 2002-08-01 AU AU2002324582A patent/AU2002324582B9/en not_active Ceased
-
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 |
|---|---|
| EP1492765A2 (en) | 2005-01-05 |
| CA2455863C (en) | 2010-10-12 |
| IL159848A0 (en) | 2004-06-20 |
| HUP0600673A3 (en) | 2011-08-29 |
| ATE515495T1 (de) | 2011-07-15 |
| EP1492765B1 (en) | 2011-07-06 |
| AU2002324582B9 (en) | 2006-02-16 |
| PL372212A1 (en) | 2005-07-11 |
| NO20040933L (no) | 2004-03-03 |
| TWI242555B (en) | 2005-11-01 |
| WO2003014075A3 (en) | 2004-09-30 |
| US20030135044A1 (en) | 2003-07-17 |
| RU2004106540A (ru) | 2005-07-27 |
| JP4418671B2 (ja) | 2010-02-17 |
| JP2005504760A (ja) | 2005-02-17 |
| HUP0600673A2 (en) | 2006-12-28 |
| KR20040019094A (ko) | 2004-03-04 |
| CA2455863A1 (en) | 2003-02-20 |
| CN1304390C (zh) | 2007-03-14 |
| US6683091B2 (en) | 2004-01-27 |
| CO5550419A2 (es) | 2005-08-31 |
| CN1630651A (zh) | 2005-06-22 |
| WO2003014075A2 (en) | 2003-02-20 |
| AU2002324582B2 (en) | 2006-01-05 |
| BR0211698A (pt) | 2004-11-09 |
| MXPA04001014A (es) | 2004-05-27 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR034390A1 (es) | 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 | |
| RU2403258C2 (ru) | Тиазолилдигидроиндазолы | |
| AR035260A1 (es) | Derivados de piperidina amino sustituidas, composiciones farmaceuticas y el uso de dichos derivados para la preparacion de medicamentos como inhibidores de la gama secretasa, y para el tratamiento de la enfermedad de alzheimer | |
| PE20212302A1 (es) | Inhibidores de apol1 y sus metodos de uso | |
| AR055878A1 (es) | Derivados de ciclopropanocarboxamida | |
| CO5721006A2 (es) | Derivados de pirazolo-quinazolina, proceso para su preparacion y su uso como inhibidores de quinasa | |
| HUP0302526A2 (hu) | Makrolid vegyületek, eljárás az előállításukra, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények | |
| AR037534A1 (es) | Derivado de adamantano, su uso en la fabricacion de un medicamento para usar en terapia, composicion farmaceutica, proceso para la preparacion de dicho compuesto y dicha composicion y compuestos intermediarios | |
| RU92004336A (ru) | Водорастворимые производные камптотецина, способ их получения, фармацевтическая композиция, способ ингибирования энзима топоизомеразы, промежуточные продукты | |
| ES2093367T3 (es) | Derivados de quinazolina. | |
| AR037907A1 (es) | Derivados de azaindolilalquilamina como ligandos de 5-hidroxitriptamina-6 | |
| AR053195A1 (es) | Compuestos inhibidores de dipeptidil peptidasa-iv metodos para preparar los mismos y composiciones farmaceuticas que los contienen como un agente activo | |
| AR034261A1 (es) | Compuestos derivados de pirazol[1,5-a]piridina; composiciones farmaceuticas, su uso en la fabricacion de medicamentos, y metodos de tratamiento de enfermedades mediadas por quinasas | |
| AR011174A1 (es) | Compuestos de pirazina, composiciones farmaceuticas que los contienen, su uso en la peparacion de medicamentos y proceso para prepararlos | |
| AR110153A1 (es) | ÁCIDOS PROPIÓNICOS 3-SUSTITUIDOS COMO INHIBIDORES DE LA INTEGRINA aV | |
| UY28578A1 (es) | Derivados de amida | |
| AR044909A1 (es) | Derivados de tiazolilpiperidina, procesos para su preparacion, composiciones farmaceuticas que los comprenden y aplicaciones de dichos derivados en el tratamiento de hipertrigliceridemia , hipercolesterolemia y dislipidemia | |
| AR058287A1 (es) | Derivados de isoquinolina y composicion farmaceutica | |
| AR052903A1 (es) | Compuestos de bis arilo y heteroarilo sustituidos como antagonistas selectivos de 5ht2a, composiciones farmaceuticas que los contienen y su empleo en el tratamiento de trastornos del sueno. | |
| AR063804A1 (es) | Compuestos de azoniabiciclo[2.2.2]octano | |
| AR051753A1 (es) | Metodos para preparar compuestos de indazol | |
| AR009938A1 (es) | Nuevos derivados de arilglicinamida, procedimientos para su preparacion y composiciones farmaceuticas que contienen estos compuestos | |
| AR037906A1 (es) | Derivados de indolilalquilamina como ligandos de 5-hidroxitriptamina-6 | |
| AR045155A1 (es) | Derivados de 6-indolilsulfonamidas, su preparacion y su aplicacion como medicamentos | |
| AR045156A1 (es) | Derivados de 5-indolilsulfonamidas, su preparacion y su aplicacion como medicamentos |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |