BRPI0408962A - inibidores sulfonamidas heterocìclicos contendo flúor- e trifluoroalquila da produção de beta amilóide e seus derivados - Google Patents
inibidores sulfonamidas heterocìclicos contendo flúor- e trifluoroalquila da produção de beta amilóide e seus derivadosInfo
- Publication number
- BRPI0408962A BRPI0408962A BRPI0408962-6A BRPI0408962A BRPI0408962A BR PI0408962 A BRPI0408962 A BR PI0408962A BR PI0408962 A BRPI0408962 A BR PI0408962A BR PI0408962 A BRPI0408962 A BR PI0408962A
- Authority
- BR
- Brazil
- Prior art keywords
- optionally substituted
- hydrogen
- lower alkyl
- production
- alkyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D333/38—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
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, 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
- 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
-
- 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
- C07D231/14—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/18—One oxygen or sulfur atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D333/30—Hetero atoms other than halogen
- C07D333/34—Sulfur atoms
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)
- Neurology (AREA)
- Neurosurgery (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
"INIBIDORES SULFONAMIDAS HETEROCìCLICOS CONTENDO FLúOR- E TRIFLUOROALQUILA DA PRODUçãO DE BETA AMILóIDE E SEUS DERIVADOS". Compostos de fórmula (I) São fornecidos onde T é CHO, COR~ 8~ ou C(OH)R~ 1~R~ 2~, R~ 1~ e R~ 2~ são hidrogênio, alquila inferior opcionalmente substituída, CF~ 3~, alquenila opcionalmente substituída ou alquinila opcionalmente substituída; R~ 3~ é hidrogênio ou alquila inferior opcionalmente substituída; R~ 4~ é (CF~ 3~)~ n~alquila, (CF~ 3~)~ n~(alquila substituída), (CF~ 3~)~ n~alquiifenila,(CF~ 3~)~ n~alquila-(fenila substituída), ou (F)~ n~cicloalquila; n = 1 a 3; R~ 5~ é hidrogênio, halogeno, CF~ 3~, dieno fundido a Y quando Y = C, ou dieno substituído fundido a Y quando Y = C; W, Y e Z são C, CR~ 6~ ou N onde pelo menos um de W, Y ou Z é C; R~ 6~ é hidrogênio, halogeno ou alquila inferior opcionalmente substituída; X é O, S, SO~ 2~ ou NR~ 7~; R~ 7~ é hidrogênio, alquila inferior opcionalmente substituída, benzila opcionalmente substituída ou fenila opcionalmente substituída; e R~ 8~ é alquila inferior, CF~ 3~ ou fenila opcionalmente substítuida. Métodos de preparação e uso destes compostos para a inibição da produção de beta amilóide e para o tratamento de Doença de Alzheimer e síndrome de Down são também descritos; ou um sal, hidrato ou pró-medicamento farmaceuticamente aceitáveis destes.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US45922803P | 2003-03-31 | 2003-03-31 | |
PCT/US2004/009268 WO2004092155A1 (en) | 2003-03-31 | 2004-03-26 | Fluoro-and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof |
Publications (1)
Publication Number | Publication Date |
---|---|
BRPI0408962A true BRPI0408962A (pt) | 2006-04-04 |
Family
ID=33299665
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BRPI0408962-6A BRPI0408962A (pt) | 2003-03-31 | 2004-03-26 | inibidores sulfonamidas heterocìclicos contendo flúor- e trifluoroalquila da produção de beta amilóide e seus derivados |
Country Status (22)
Country | Link |
---|---|
US (3) | US7300951B2 (pt) |
EP (1) | EP1608638A1 (pt) |
JP (1) | JP2006522126A (pt) |
KR (1) | KR20060002908A (pt) |
CN (2) | CN1780829B (pt) |
AR (1) | AR043940A1 (pt) |
AU (1) | AU2004230844B2 (pt) |
BR (1) | BRPI0408962A (pt) |
CA (1) | CA2517155A1 (pt) |
CL (1) | CL2004000647A1 (pt) |
CO (1) | CO5640049A2 (pt) |
CR (1) | CR7951A (pt) |
EC (1) | ECSP056128A (pt) |
MX (1) | MXPA05010368A (pt) |
NO (1) | NO20054263L (pt) |
NZ (1) | NZ542468A (pt) |
RU (1) | RU2342374C2 (pt) |
SG (1) | SG167669A1 (pt) |
TW (1) | TWI336698B (pt) |
UA (1) | UA82093C2 (pt) |
WO (1) | WO2004092155A1 (pt) |
ZA (1) | ZA200507896B (pt) |
Families Citing this family (35)
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KR100869061B1 (ko) * | 2000-12-13 | 2008-11-17 | 와이어쓰 | 베타 아밀로이드 생성의 헤테로고리 술폰아미드 저해제 |
DE60232276D1 (de) * | 2001-12-20 | 2009-06-18 | Bristol Myers Squibb Co | Alpha-(n-sulfonamid)acetamidderivate als beta-amyloidinhibitoren |
IL165265A0 (en) * | 2002-06-11 | 2005-12-18 | Wyeth Corp | Substituted phenylsulfonamide inhibitors of beta amyloid production |
CL2004000647A1 (es) * | 2003-03-31 | 2005-02-04 | Wyeth Corp | Compuestos derivados de heterociclicos de sulfonamida que contienen fluoro y trifluoro alquilo; composicion farmaceutica; kit farmaceutico; procedimiento de preparacion; y su uso como inhibidores de beta amiloides para tratar alzheimer, angiopatia am |
ATE443701T1 (de) * | 2004-01-16 | 2009-10-15 | Wyeth Corp | Heterocyclische, ein azol enthaltende sulfonamidinhibitoren der beta-amyloid-produktion |
US7687666B2 (en) * | 2006-02-17 | 2010-03-30 | Wyeth | Methods for preparing sulfonamide substituted alcohols and intermediates thereof |
PE20080109A1 (es) * | 2006-02-17 | 2008-04-01 | Wyeth Corp | N-sulfonilacion selectiva de alcoholes sustituidos con 2-aminotrifluoralquilo |
US7476762B2 (en) * | 2006-04-21 | 2009-01-13 | Wyeth | Methods for preparing sulfonamide compounds |
BRPI0710470A2 (pt) | 2006-04-21 | 2011-08-16 | Wyeth Corp | métodos para preparar seletivamente um aminoálcool quiral e uma sulfonamida quiral |
US7550629B2 (en) | 2006-04-21 | 2009-06-23 | Wyeth | Trifluoromethyl-containing phenylsulfonamide beta amyloid inhibitors |
CA2667802A1 (en) * | 2006-11-03 | 2008-05-29 | Northwestern University | Multiple sclerosis therapy |
EP2193117A1 (en) * | 2007-07-16 | 2010-06-09 | Wyeth a Corporation of the State of Delaware | Inhibitors of beta amyloid production |
TW200911778A (en) * | 2007-07-16 | 2009-03-16 | Wyeth Corp | Process for the preparation of trifluoroalkyl-phenyl and heterocyclic sulfonamides |
AR067533A1 (es) * | 2007-07-16 | 2009-10-14 | Wyeth Corp | Procesos e inetermediarios para la preparacion de compuestos de sulfonamida heterociclica |
US8093276B2 (en) * | 2007-10-31 | 2012-01-10 | Bristol-Myers Squibb Company | Alpha-(N-sulfonamido)acetamide compound as an inhibitor of beta amyloid peptide production |
US8084477B2 (en) | 2007-10-31 | 2011-12-27 | Bristol-Myers Squibb Company | Alpha-(N-sulfonamido)acetamide compound as an inhibitor of beta amyloid peptide production |
TW200934482A (en) * | 2008-01-11 | 2009-08-16 | Wyeth Corp | Compositions containing o-sulfate and o-phosphate containing aryl sulfonamide derivatives useful as β -amyloid inhibitors |
CN102088855A (zh) * | 2008-05-08 | 2011-06-08 | 百时美施贵宝公司 | 2-芳基甘氨酰胺衍生物 |
WO2010025968A2 (en) * | 2008-09-05 | 2010-03-11 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e. V. | Process for enantioseparation of chiral systems with compound formation using two subsequent crystallization steps |
US8044077B2 (en) * | 2009-03-19 | 2011-10-25 | Bristol-Myers Squibb Company | Alpha-(N-sulfonamido)acetamide compounds incorporating deuterium as inhibitors of beta amyloid peptide production |
US7977362B2 (en) * | 2009-03-20 | 2011-07-12 | Bristol-Myers Squibb Company | Alpha-(N-benzenesulfonamido)cycloalkyl derivatives |
US20110071199A1 (en) * | 2009-03-20 | 2011-03-24 | Bristol-Myers Squibb Company | Thiophenyl Sulfonamides for the Treatment of Alzheimer's Disease |
TW201043269A (en) * | 2009-04-14 | 2010-12-16 | Bristol Myers Squibb Co | Bioavailable compositions of amorphous alpha-(N-sulfonamido)acetamide compound |
US8252821B2 (en) * | 2009-04-14 | 2012-08-28 | Bristol-Myers Squibb Company | Bioavailable capsule compositions of amorphous alpha-(N-sulfonamido)acetamide compound |
WO2010126002A1 (ja) * | 2009-04-28 | 2010-11-04 | 塩野義製薬株式会社 | ヘテロ環スルホンアミド化合物を含有する医薬 |
WO2011084503A1 (en) * | 2009-12-16 | 2011-07-14 | North Carolina Central University | Phenoxy thiophene sulfonamides and their use in the treatment of neurodegenerative diseases |
US9223209B2 (en) * | 2010-02-19 | 2015-12-29 | International Business Machines Corporation | Sulfonamide-containing photoresist compositions and methods of use |
US9223217B2 (en) | 2010-02-19 | 2015-12-29 | International Business Machines Corporation | Sulfonamide-containing topcoat and photoresist additive compositions and methods of use |
US9617239B2 (en) | 2010-03-10 | 2017-04-11 | North Carolina Central University | Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
JP2015527398A (ja) | 2012-09-07 | 2015-09-17 | マサチューセッツ アイ アンド イヤー インファーマリー | 聴覚喪失治療 |
JP6319912B2 (ja) | 2013-04-19 | 2018-05-09 | 国立大学法人 岡山大学 | アミロイドβ蛋白質により誘発される認知障害の治療剤およびアルツハイマー病治療薬、ならびにこれらに関連する治療方法および病態解析方法 |
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KR100869061B1 (ko) * | 2000-12-13 | 2008-11-17 | 와이어쓰 | 베타 아밀로이드 생성의 헤테로고리 술폰아미드 저해제 |
MXPA04005366A (es) | 2001-12-11 | 2004-09-27 | Wyeth Corp | Produccion de alfa-aminoacidos de n-sulfonilo y alfa-aminoacidos quiralmente puros. |
KR100921641B1 (ko) | 2001-12-11 | 2009-10-14 | 와이어쓰 | 순수한 키랄성 β-아미노 알콜의 합성방법 |
IL165265A0 (en) * | 2002-06-11 | 2005-12-18 | Wyeth Corp | Substituted phenylsulfonamide inhibitors of beta amyloid production |
CL2004000647A1 (es) | 2003-03-31 | 2005-02-04 | Wyeth Corp | Compuestos derivados de heterociclicos de sulfonamida que contienen fluoro y trifluoro alquilo; composicion farmaceutica; kit farmaceutico; procedimiento de preparacion; y su uso como inhibidores de beta amiloides para tratar alzheimer, angiopatia am |
ATE443701T1 (de) | 2004-01-16 | 2009-10-15 | Wyeth Corp | Heterocyclische, ein azol enthaltende sulfonamidinhibitoren der beta-amyloid-produktion |
PE20080109A1 (es) | 2006-02-17 | 2008-04-01 | Wyeth Corp | N-sulfonilacion selectiva de alcoholes sustituidos con 2-aminotrifluoralquilo |
US7687666B2 (en) | 2006-02-17 | 2010-03-30 | Wyeth | Methods for preparing sulfonamide substituted alcohols and intermediates thereof |
BRPI0710470A2 (pt) | 2006-04-21 | 2011-08-16 | Wyeth Corp | métodos para preparar seletivamente um aminoálcool quiral e uma sulfonamida quiral |
US7476762B2 (en) | 2006-04-21 | 2009-01-13 | Wyeth | Methods for preparing sulfonamide compounds |
US7550629B2 (en) | 2006-04-21 | 2009-06-23 | Wyeth | Trifluoromethyl-containing phenylsulfonamide beta amyloid inhibitors |
EP2193117A1 (en) | 2007-07-16 | 2010-06-09 | Wyeth a Corporation of the State of Delaware | Inhibitors of beta amyloid production |
AR067533A1 (es) | 2007-07-16 | 2009-10-14 | Wyeth Corp | Procesos e inetermediarios para la preparacion de compuestos de sulfonamida heterociclica |
TW200911778A (en) | 2007-07-16 | 2009-03-16 | Wyeth Corp | Process for the preparation of trifluoroalkyl-phenyl and heterocyclic sulfonamides |
-
2004
- 2004-03-26 CL CL200400647A patent/CL2004000647A1/es unknown
- 2004-03-26 CA CA002517155A patent/CA2517155A1/en not_active Abandoned
- 2004-03-26 UA UAA200510177A patent/UA82093C2/uk unknown
- 2004-03-26 WO PCT/US2004/009268 patent/WO2004092155A1/en active Application Filing
- 2004-03-26 EP EP04758978A patent/EP1608638A1/en not_active Withdrawn
- 2004-03-26 US US10/810,517 patent/US7300951B2/en not_active Expired - Fee Related
- 2004-03-26 JP JP2006509331A patent/JP2006522126A/ja active Pending
- 2004-03-26 CN CN2004800087813A patent/CN1780829B/zh not_active Expired - Fee Related
- 2004-03-26 AU AU2004230844A patent/AU2004230844B2/en not_active Expired - Fee Related
- 2004-03-26 AR ARP040101022A patent/AR043940A1/es unknown
- 2004-03-26 TW TW093108219A patent/TWI336698B/zh not_active IP Right Cessation
- 2004-03-26 BR BRPI0408962-6A patent/BRPI0408962A/pt not_active IP Right Cessation
- 2004-03-26 MX MXPA05010368A patent/MXPA05010368A/es active IP Right Grant
- 2004-03-26 KR KR1020057018637A patent/KR20060002908A/ko not_active Application Discontinuation
- 2004-03-26 SG SG200708961-8A patent/SG167669A1/en unknown
- 2004-03-26 RU RU2005133434/04A patent/RU2342374C2/ru not_active IP Right Cessation
- 2004-03-26 NZ NZ542468A patent/NZ542468A/en not_active IP Right Cessation
- 2004-03-26 CN CNA2008100013400A patent/CN101274926A/zh active Pending
-
2005
- 2005-08-19 CR CR7951A patent/CR7951A/es unknown
- 2005-09-15 NO NO20054263A patent/NO20054263L/no not_active Application Discontinuation
- 2005-09-29 ZA ZA200507896A patent/ZA200507896B/en unknown
- 2005-10-26 CO CO05109226A patent/CO5640049A2/es not_active Application Discontinuation
- 2005-10-28 EC EC2005006128A patent/ECSP056128A/es unknown
-
2007
- 2007-06-15 US US11/818,630 patent/US7547725B2/en not_active Expired - Fee Related
-
2009
- 2009-05-05 US US12/435,442 patent/US7858658B2/en not_active Expired - Fee Related
Also Published As
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US20090227667A1 (en) | 2009-09-10 |
US7300951B2 (en) | 2007-11-27 |
US7547725B2 (en) | 2009-06-16 |
ECSP056128A (es) | 2006-03-01 |
UA82093C2 (uk) | 2008-03-11 |
KR20060002908A (ko) | 2006-01-09 |
WO2004092155A1 (en) | 2004-10-28 |
TW200504047A (en) | 2005-02-01 |
CN101274926A (zh) | 2008-10-01 |
SG167669A1 (en) | 2011-01-28 |
CN1780829B (zh) | 2010-12-29 |
TWI336698B (en) | 2011-02-01 |
US20040198778A1 (en) | 2004-10-07 |
CR7951A (es) | 2008-10-29 |
US7858658B2 (en) | 2010-12-28 |
RU2342374C2 (ru) | 2008-12-27 |
JP2006522126A (ja) | 2006-09-28 |
MXPA05010368A (es) | 2005-11-17 |
AR043940A1 (es) | 2005-08-17 |
AU2004230844A1 (en) | 2004-10-28 |
ZA200507896B (en) | 2007-03-28 |
US20070254929A1 (en) | 2007-11-01 |
AU2004230844B2 (en) | 2010-12-09 |
NZ542468A (en) | 2009-01-31 |
CL2004000647A1 (es) | 2005-02-04 |
CN1780829A (zh) | 2006-05-31 |
NO20054263L (no) | 2005-12-14 |
RU2005133434A (ru) | 2006-07-10 |
CA2517155A1 (en) | 2004-10-28 |
NO20054263D0 (no) | 2005-09-15 |
CO5640049A2 (es) | 2006-05-31 |
EP1608638A1 (en) | 2005-12-28 |
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