BR0210721A - Composto, sal ou éster farmaceuticamente aceitável, método para fabricar um composto, e, método para tratar um paciente que tem, ou para evitar que o paciente adquira uma doença ou condição - Google Patents
Composto, sal ou éster farmaceuticamente aceitável, método para fabricar um composto, e, método para tratar um paciente que tem, ou para evitar que o paciente adquira uma doença ou condiçãoInfo
- Publication number
- BR0210721A BR0210721A BR0210721-0A BR0210721A BR0210721A BR 0210721 A BR0210721 A BR 0210721A BR 0210721 A BR0210721 A BR 0210721A BR 0210721 A BR0210721 A BR 0210721A
- Authority
- BR
- Brazil
- Prior art keywords
- patient
- compound
- disease
- treating
- salt
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 6
- 238000000034 method Methods 0.000 title abstract 4
- 201000010099 disease Diseases 0.000 title abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 2
- 150000002148 esters Chemical class 0.000 title abstract 2
- 150000003839 salts Chemical class 0.000 title abstract 2
- DZHSAHHDTRWUTF-SIQRNXPUSA-N amyloid-beta polypeptide 42 Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(C)C)C1=CC=CC=C1 DZHSAHHDTRWUTF-SIQRNXPUSA-N 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 abstract 1
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 abstract 1
- 101710137189 Amyloid-beta A4 protein Proteins 0.000 abstract 1
- 101710151993 Amyloid-beta precursor protein Proteins 0.000 abstract 1
- 102100022704 Amyloid-beta precursor protein Human genes 0.000 abstract 1
- 101800001718 Amyloid-beta protein Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 150000001298 alcohols Chemical class 0.000 abstract 1
- 210000004556 brain Anatomy 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
Classifications
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- 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
- C07D409/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- A61P25/14—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
- A61P25/28—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
-
- 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
- C07D233/66—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 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
- C07D233/84—Sulfur atoms
-
- 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
- C07D233/66—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 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
- C07D233/90—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
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
- C07D235/28—Sulfur 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
- C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
- C07D249/12—Oxygen or sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/36—Sulfur atom
- C07D473/38—Sulfur atom attached in position 6
Abstract
"COMPOSTO, SAL OU éSTER FARMACEUTICAMENTE ACEITáVEL, MéTODO PARA FABRICAR UM COMPOSTO, E, MéTODO PARA TRATAR UM PACIENTE QUE TEM, OU PARA EVITAR QUE O PACIENTE ADQUIRA UMA DOENçA OU CONDIçãO". A invenção refere-se a compostos de álcool substituídos da fórmula (I), em que X, R~ 1~, R~ 2~, R~ 3~, R~ N~, R~ 20~ e R~ C~ são definidos neste. Os compostos são úteis no tratamento ou prevenção do mal de Alzheimer e mais especificamente a compostos que são capazes de inibir beta-secretase, uma enzima que cliva proteína precursora de amilóide para produzir peptídeo amilóide beta (A-beta), um componente principal das placas de amilóide encontrados nos cérebros dos sofredores de Alzheimer.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US30121001P | 2001-06-27 | 2001-06-27 | |
US32339601P | 2001-09-18 | 2001-09-18 | |
US33273601P | 2001-11-19 | 2001-11-19 | |
PCT/US2002/020754 WO2003002122A1 (en) | 2001-06-27 | 2002-06-27 | Beta-hydroxyamine derivatives useful in treatment of alzheimer's disease |
Publications (1)
Publication Number | Publication Date |
---|---|
BR0210721A true BR0210721A (pt) | 2004-07-20 |
Family
ID=27404798
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR0210721-0A BR0210721A (pt) | 2001-06-27 | 2002-06-27 | Composto, sal ou éster farmaceuticamente aceitável, método para fabricar um composto, e, método para tratar um paciente que tem, ou para evitar que o paciente adquira uma doença ou condição |
Country Status (7)
Country | Link |
---|---|
US (2) | US6982264B2 (pt) |
EP (1) | EP1401452A1 (pt) |
JP (1) | JP2005500319A (pt) |
BR (1) | BR0210721A (pt) |
CA (1) | CA2452039A1 (pt) |
MX (1) | MXPA04000140A (pt) |
WO (1) | WO2003002122A1 (pt) |
Families Citing this family (33)
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US7872009B2 (en) | 2005-11-21 | 2011-01-18 | Amgen Inc. | Beta-Secretase modulators and methods of use |
JP5274258B2 (ja) | 2005-11-21 | 2013-08-28 | アムジエン・インコーポレーテツド | β−セクレターゼ調節物質及び使用方法 |
US7745484B2 (en) * | 2005-11-21 | 2010-06-29 | Amgen Inc. | Beta-secretase modulators and methods of use |
US7838676B2 (en) * | 2005-11-21 | 2010-11-23 | Amgen Inc. | Beta-secretase modulators and methods of use |
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 |
WO2008065141A1 (en) | 2006-11-30 | 2008-06-05 | Probiodrug Ag | Novel inhibitors of glutaminyl cyclase |
ZA200905537B (en) | 2007-03-01 | 2010-10-27 | Probiodrug Ag | New use of glutaminyl cyclase inhibitors |
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 |
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US8173810B2 (en) * | 2007-05-25 | 2012-05-08 | Amgen Inc. | Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use |
US8163909B2 (en) | 2007-05-25 | 2012-04-24 | Amgen Inc. | Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use |
US7803809B2 (en) | 2008-11-12 | 2010-09-28 | Amgen Inc. | Substituted pyrano [2,3-b] pyridinamine compounds as beta-secretase modulators and methods of use |
WO2009076352A1 (en) * | 2007-12-11 | 2009-06-18 | Schering Corporation | Gamma secretase modulators |
EP3403650A3 (en) | 2008-07-28 | 2019-02-13 | Blanchette Rockefeller Neurosciences, Institute | Pkc-activating compounds for the treatment of neurodegenerative diseases |
CA2736130C (en) * | 2008-09-11 | 2014-01-14 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta-secretase modulators and methods of use |
MX2012002993A (es) | 2009-09-11 | 2012-04-19 | Probiodrug Ag | Derivados heterociclicos como inhibidores de ciclasa glutaminilo. |
WO2011063233A1 (en) | 2009-11-23 | 2011-05-26 | Amgen Inc. | Amino heteroaryl compounds as beta-secretase modulators and methods of use |
WO2011063272A1 (en) | 2009-11-23 | 2011-05-26 | Amgen Inc. | Amino heteroaryl compounds as beta-secretase modulators and methods of use |
EP2526092B1 (en) | 2010-01-19 | 2014-08-06 | Amgen Inc. | Amino heteroaryl compounds as beta-secretase modulators and methods of use |
JP6026284B2 (ja) | 2010-03-03 | 2016-11-16 | 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 |
MX2012010470A (es) | 2010-03-10 | 2012-10-09 | Probiodrug Ag | Inhibidores heterociclicos d ciclasa de glutaminilo (qc, ec .3 2. 5). |
US8497264B2 (en) | 2010-03-15 | 2013-07-30 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
US8883782B2 (en) | 2010-03-15 | 2014-11-11 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta-secretase modulators and methods of use |
US8541596B2 (en) | 2010-04-21 | 2013-09-24 | Probiodrug Ag | Inhibitors |
US9346827B2 (en) | 2011-02-07 | 2016-05-24 | Amgen Inc. | 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use |
WO2012123563A1 (en) | 2011-03-16 | 2012-09-20 | Probiodrug Ag | Benz imidazole derivatives as inhibitors of glutaminyl cyclase |
WO2013044092A1 (en) | 2011-09-21 | 2013-03-28 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
US9725469B2 (en) | 2012-11-15 | 2017-08-08 | Amgen, Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
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EP3461819B1 (en) | 2017-09-29 | 2020-05-27 | Probiodrug AG | Inhibitors of glutaminyl cyclase |
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-
2002
- 2002-06-27 WO PCT/US2002/020754 patent/WO2003002122A1/en active Application Filing
- 2002-06-27 CA CA002452039A patent/CA2452039A1/en not_active Abandoned
- 2002-06-27 JP JP2003508361A patent/JP2005500319A/ja active Pending
- 2002-06-27 US US10/183,126 patent/US6982264B2/en not_active Expired - Fee Related
- 2002-06-27 MX MXPA04000140A patent/MXPA04000140A/es not_active Application Discontinuation
- 2002-06-27 EP EP02744767A patent/EP1401452A1/en not_active Withdrawn
- 2002-06-27 BR BR0210721-0A patent/BR0210721A/pt not_active IP Right Cessation
-
2006
- 2006-01-03 US US11/324,678 patent/US20060178345A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
MXPA04000140A (es) | 2004-06-03 |
US20060178345A1 (en) | 2006-08-10 |
US6982264B2 (en) | 2006-01-03 |
EP1401452A1 (en) | 2004-03-31 |
WO2003002122A1 (en) | 2003-01-09 |
JP2005500319A (ja) | 2005-01-06 |
US20030083518A1 (en) | 2003-05-01 |
CA2452039A1 (en) | 2003-01-09 |
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