PE20060481A1 - N-arilsulfonilaminas heterociclicas sustituidas como inhibidores de gamma-secretasas - Google Patents
N-arilsulfonilaminas heterociclicas sustituidas como inhibidores de gamma-secretasasInfo
- Publication number
- PE20060481A1 PE20060481A1 PE2005000751A PE2005000751A PE20060481A1 PE 20060481 A1 PE20060481 A1 PE 20060481A1 PE 2005000751 A PE2005000751 A PE 2005000751A PE 2005000751 A PE2005000751 A PE 2005000751A PE 20060481 A1 PE20060481 A1 PE 20060481A1
- Authority
- PE
- Peru
- Prior art keywords
- alkylen
- inhibitors
- substitute
- aryl
- gamma
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 102000038383 gamma-secretases Human genes 0.000 title 1
- 108091007739 gamma-secretases Proteins 0.000 title 1
- -1 3,5-DIFLUORO-PHENYL Chemical class 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 abstract 1
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- GEAXLHPORCRESC-UHFFFAOYSA-N chlorocyclohexatriene Chemical class ClC1=CC=C=C[CH]1 GEAXLHPORCRESC-UHFFFAOYSA-N 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical class [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
-
- 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
- C07D487/08—Bridged systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
SE REFIERE A COMPUESTOS DE N-ARILSUFONILAMINAS HETEROCICLICAS DE FORMULA (I), EN DONDE L ES -O-, -N(R6)-, -S-, ENTRE OTROS; R1 ES ARILO O HETEROARILO SUSTITUIDO CON R7; R2 ES -(C0-C6)ALQUILEN-(C3-C6)CICLOALQUILEN-(C0-C6)ALQUILEN-X-C(O)-Y, -(C0-C6)ALQUILEN-(C3-C6)CICLOALQUILEN-(C0-C6)ALQUILEN-C(O)-Y, -(C3-C6)CICLOALQUILEN-(C1-C6)ALQUILEN-C(O)-Y, ENTRE OTROS, SUSTITUIDO EL ALQUILENO CON UNO O MAS HIDROXI; R3 ES ARILO, ALQUILO, CICLOALQUILO,HETEROARILO, ENTRE OTROS, OPCIONALMENTE SUSTITUIDOS CON R7; X ES -O-, -N(R6)-, ENTRE OTROS; Y ES -NR8R9, -N(R6)-(CH2)b-NR8R9-, ARILO, ENTRE OTROS; m Yn SON INDEPENDIENTEMENTE DE 0 A 2, SIEMPRE QUE m + n SEA 1 0 2. SON PREFERIDOS: ESTER 4-(4-CLORO-BENCENSULFONIL)-5-(3,5-DIFLUORO-FENIL)-MORFOLIN-3-IL-METILICO DEL ACIDO 4-(2-HIDROXI-ETIL)-PIPERAZIN-1-CARBOXILICO, ALFA-[1-[4-[(4-CLOROFENIL)SULFONIL]-5(r)-CICLOPROPIL-3(S)-MORFOLINIL]CICLOPROPIL]-BETA-OXO-3,8-DIAZABICICLO[3.2.1]OCTAN-3-ETANOL, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS SON INHIBIDORES DE LA GAMMA SECRETASA POR LO QUE SON UTILES EN EL TRATAMIENTO DEL ALZHEIMER
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US58401004P | 2004-06-30 | 2004-06-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20060481A1 true PE20060481A1 (es) | 2006-06-19 |
Family
ID=35783342
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2005000751A PE20060481A1 (es) | 2004-06-30 | 2005-06-28 | N-arilsulfonilaminas heterociclicas sustituidas como inhibidores de gamma-secretasas |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US7763613B2 (es) |
| EP (1) | EP1789404B1 (es) |
| JP (1) | JP2008505100A (es) |
| CN (2) | CN101048393A (es) |
| AR (1) | AR050994A1 (es) |
| AT (1) | ATE461926T1 (es) |
| CA (1) | CA2570183A1 (es) |
| DE (1) | DE602005020156D1 (es) |
| ES (1) | ES2341560T3 (es) |
| MX (1) | MX2007000040A (es) |
| PE (1) | PE20060481A1 (es) |
| TW (1) | TWI297270B (es) |
| WO (1) | WO2006004880A2 (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2007207481B2 (en) * | 2006-01-20 | 2012-08-23 | Merck Sharp & Dohme Corp. | Carbocyclic and heterocyclic arylsulfones as gamma secretase inhibitors |
| WO2007092435A2 (en) | 2006-02-07 | 2007-08-16 | Wyeth | 11-beta hsd1 inhibitors |
| AU2007245435A1 (en) * | 2006-04-26 | 2007-11-08 | Merck & Co., Inc. | Piperidines and related compounds for treatment of Alzheimer's disease |
| WO2007141029A1 (en) * | 2006-06-08 | 2007-12-13 | Helmholtz Zentrum München Deutsches Forschungszentrum Für Gesundheit Und Umwelt (Gmbh) | Specific protease inhibitors and their use in cancer therapy |
| US8278345B2 (en) | 2006-11-09 | 2012-10-02 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| SI2091948T1 (sl) | 2006-11-30 | 2012-07-31 | Probiodrug Ag | Novi inhibitorji glutaminil ciklaze |
| EA200901140A1 (ru) | 2007-03-01 | 2010-04-30 | Пробиодруг Аг | Новое применение ингибиторов глутаминилциклазы |
| EP2142514B1 (en) | 2007-04-18 | 2014-12-24 | Probiodrug AG | Thiourea derivatives as glutaminyl cyclase inhibitors |
| EA017119B1 (ru) * | 2007-10-19 | 2012-09-28 | Янссен Фармацевтика, Н.В. | МОДУЛЯТОРЫ АКТИВНОСТИ γ-СЕКРЕТАЗЫ ИЗ ГРУППЫ ПИПЕРИДИНИЛА И ПИПЕРАЗИНИЛА |
| 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 |
| US20110190269A1 (en) * | 2010-02-01 | 2011-08-04 | Karlheinz Baumann | Gamma secretase modulators |
| WO2011107530A2 (en) | 2010-03-03 | 2011-09-09 | Probiodrug Ag | Novel inhibitors |
| SG183229A1 (en) | 2010-03-10 | 2012-09-27 | Probiodrug Ag | Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5) |
| EP2560953B1 (en) | 2010-04-21 | 2016-01-06 | Probiodrug AG | Inhibitors of glutaminyl cyclase |
| WO2012123563A1 (en) | 2011-03-16 | 2012-09-20 | Probiodrug Ag | Benz imidazole derivatives as inhibitors of glutaminyl cyclase |
| AR091279A1 (es) | 2012-06-08 | 2015-01-21 | Gilead Sciences Inc | Inhibidores macrociclicos de virus flaviviridae |
| DK3461819T3 (da) | 2017-09-29 | 2020-08-10 | Probiodrug Ag | Inhibitorer af glutaminylcyklase |
| CN109705052B (zh) * | 2019-01-25 | 2020-12-08 | 苏州大学 | 一种制备1,4-二氢噁嗪的方法 |
| CN119060034A (zh) * | 2024-09-02 | 2024-12-03 | 上海信诺维生物医药有限公司 | 一种含吡喃取代的吗啉类化合物的制备方法 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH04247081A (ja) | 1991-02-01 | 1992-09-03 | Takeda Chem Ind Ltd | 5員複素環酸アミド類 |
| US5646167A (en) * | 1993-01-06 | 1997-07-08 | Ciba-Geigy Corporation | Arylsulfonamido-substituted hydroxamix acids |
| JP3834663B2 (ja) * | 1996-02-02 | 2006-10-18 | 株式会社デ・ウエスタン・セラピテクス研究所 | イソキノリン誘導体及び医薬 |
| IL140041A0 (en) * | 1998-06-03 | 2002-02-10 | Guilford Pharm Inc | Multiple heteroatom containing heterocyclic ring compounds substituted with carboxylic acids and isosteres thereof |
| CN1348442A (zh) | 1999-02-26 | 2002-05-08 | 默克公司 | 新的磺胺化合物及其应用 |
| FR2802206B1 (fr) * | 1999-12-14 | 2005-04-22 | Sod Conseils Rech Applic | Derives de 4-aminopiperidine et leur utilisation en tant que medicament |
| SE9904738D0 (sv) * | 1999-12-22 | 1999-12-22 | Astra Pharma Prod | Novel compounds |
| JP2001261657A (ja) * | 2000-03-17 | 2001-09-26 | Yamanouchi Pharmaceut Co Ltd | シアノフェニル誘導体 |
| CA2406652A1 (en) | 2000-04-20 | 2001-11-01 | Nps Allelix Corp. | Aminopiperidines for use as glyt-1 inhibitors |
| US6589978B2 (en) | 2000-06-30 | 2003-07-08 | Hoffman-La Roche Inc. | 1-sulfonyl pyrrolidine derivatives |
| KR20030029978A (ko) | 2000-09-25 | 2003-04-16 | 액테리온 파마슈티칼 리미티드 | 말라리아에 유용한 치환된 아미노-아자-사이클로알칸 |
| IL159848A0 (en) * | 2001-08-03 | 2004-06-20 | Schering Corp | Novel gamma secretase inhibitors |
| WO2003013527A1 (en) * | 2001-08-03 | 2003-02-20 | Schering Corporation | Sulfonamide derivatives as gamma secretase inhibitors |
| US20040171614A1 (en) | 2002-02-06 | 2004-09-02 | Schering-Plough Corporation | Novel gamma secretase inhibitors |
| US7256186B2 (en) * | 2002-02-06 | 2007-08-14 | Schering Corporation | Gamma secretase inhibitors |
| TW200302717A (en) | 2002-02-06 | 2003-08-16 | Schering Corp | Novel gamma secretase inhibitors |
| ES2308206T3 (es) | 2003-05-13 | 2008-12-01 | Schering Corporation | N-arilsulfonilpiperidinas con fuentes como inhibidores de gamma-secretasa. |
| JP4247081B2 (ja) | 2003-09-24 | 2009-04-02 | 三菱電機株式会社 | レーザアニール装置のレーザビーム強度モニタ方法とレーザアニール装置 |
| AU2005230681B2 (en) * | 2004-04-05 | 2009-07-30 | Schering Corporation | Novel gamma secretase inhibitors |
| US20060035884A1 (en) * | 2004-05-20 | 2006-02-16 | Elan Pharmaceuticals, Inc. | N-cyclic sulfonamido inhibitors of gamma secretase |
| AU2007207481B2 (en) * | 2006-01-20 | 2012-08-23 | Merck Sharp & Dohme Corp. | Carbocyclic and heterocyclic arylsulfones as gamma secretase inhibitors |
-
2005
- 2005-06-28 JP JP2007519415A patent/JP2008505100A/ja active Pending
- 2005-06-28 DE DE602005020156T patent/DE602005020156D1/de not_active Expired - Lifetime
- 2005-06-28 PE PE2005000751A patent/PE20060481A1/es not_active Application Discontinuation
- 2005-06-28 AR ARP050102662A patent/AR050994A1/es not_active Application Discontinuation
- 2005-06-28 ES ES05790194T patent/ES2341560T3/es not_active Expired - Lifetime
- 2005-06-28 CN CNA2005800284229A patent/CN101048393A/zh active Pending
- 2005-06-28 CA CA002570183A patent/CA2570183A1/en not_active Abandoned
- 2005-06-28 CN CNA200910152119XA patent/CN101602741A/zh active Pending
- 2005-06-28 US US11/168,797 patent/US7763613B2/en not_active Expired - Fee Related
- 2005-06-28 AT AT05790194T patent/ATE461926T1/de not_active IP Right Cessation
- 2005-06-28 EP EP05790194A patent/EP1789404B1/en not_active Expired - Lifetime
- 2005-06-28 WO PCT/US2005/023187 patent/WO2006004880A2/en not_active Ceased
- 2005-06-28 MX MX2007000040A patent/MX2007000040A/es active IP Right Grant
- 2005-06-29 TW TW094121770A patent/TWI297270B/zh not_active IP Right Cessation
-
2009
- 2009-12-08 US US12/633,286 patent/US20100087425A1/en not_active Abandoned
- 2009-12-08 US US12/633,311 patent/US7998958B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| CN101048393A (zh) | 2007-10-03 |
| AR050994A1 (es) | 2006-12-13 |
| CN101602741A (zh) | 2009-12-16 |
| MX2007000040A (es) | 2007-03-07 |
| WO2006004880A2 (en) | 2006-01-12 |
| JP2008505100A (ja) | 2008-02-21 |
| US20060040936A1 (en) | 2006-02-23 |
| US7998958B2 (en) | 2011-08-16 |
| EP1789404A2 (en) | 2007-05-30 |
| US20100087425A1 (en) | 2010-04-08 |
| ES2341560T3 (es) | 2010-06-22 |
| TW200612928A (en) | 2006-05-01 |
| US20100093695A1 (en) | 2010-04-15 |
| WO2006004880A3 (en) | 2007-03-08 |
| DE602005020156D1 (de) | 2010-05-06 |
| HK1099300A1 (en) | 2007-08-10 |
| ATE461926T1 (de) | 2010-04-15 |
| TWI297270B (en) | 2008-06-01 |
| CA2570183A1 (en) | 2006-01-12 |
| EP1789404B1 (en) | 2010-03-24 |
| US7763613B2 (en) | 2010-07-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |