BRPI0412286A - composto macrocìclos tendo atividade inibidora da protease aspástica e usos farmacêuticos dos mesmos - Google Patents
composto macrocìclos tendo atividade inibidora da protease aspástica e usos farmacêuticos dos mesmosInfo
- Publication number
- BRPI0412286A BRPI0412286A BRPI0412286-0A BRPI0412286A BRPI0412286A BR PI0412286 A BRPI0412286 A BR PI0412286A BR PI0412286 A BRPI0412286 A BR PI0412286A BR PI0412286 A BRPI0412286 A BR PI0412286A
- Authority
- BR
- Brazil
- Prior art keywords
- sub
- alkyl
- cycloalkyl
- alkylen
- hydrogen
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 102000035101 Aspartic proteases Human genes 0.000 title 1
- 108091005502 Aspartic proteases Proteins 0.000 title 1
- 230000002401 inhibitory effect Effects 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 11
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 3
- 150000001370 alpha-amino acid derivatives Chemical class 0.000 abstract 2
- 235000008206 alpha-amino acids Nutrition 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- -1 piperidino, pyrrolidinyl Chemical group 0.000 abstract 2
- 102000013455 Amyloid beta-Peptides Human genes 0.000 abstract 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 238000004220 aggregation Methods 0.000 abstract 1
- 230000002776 aggregation Effects 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000005529 alkyleneoxy group Chemical group 0.000 abstract 1
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 abstract 1
- 229910002091 carbon monoxide Inorganic materials 0.000 abstract 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 150000002678 macrocyclic compounds Chemical class 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 abstract 1
- 230000000926 neurological effect Effects 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 208000019553 vascular disease Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
-
- 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
-
- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
- C07D273/02—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having two nitrogen atoms and only one oxygen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D291/00—Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms
- C07D291/08—Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
"COMPOSTOS MACROCìCLICOS TENDO ATIVIDADE INIBIDORA DA PROTEASE ASPáSTICA E USOS FARMACêUTICOS DOS MESMOS". A presente invenção refere-se aos compostos macrocíclicos de fórmula (I), na qual R~ 1~ é (C~ 1-8~) alquila, (C~ 1-4~)alcóxi(C~ 1-4~) alquila, hidróxi(C~ 1-6~) alquila, (C~ 1- 4~) alquiltio (C~ 1-4~) alquila, (C~ 1-6~) alquenila, (C~ 3-7~) Cicloalquila, (C~ 3-7~) Cicloalquil (C~ 14~ ) alquila, piperidinila ou pirrolidinila; R~ 2 e R~ 4~ são independentemente hidrogênio ou (C~ 1-8~) alquila, (C~ 3-7~) cicloalquila, (C~ 3-7~) Cicloalquil (C~ 1-4~) alquila, arila, aril (C~ 1-4~) alquila, heteroarila ou heteroaril (C~ 1-4~) alquila opcionalmente substituída, ou R~ 2~ e R~ 4~ juntamente com o nitrogênio ao qual estão ligados, formam um grupo piperidino, pirrolidinila, morfolino ou piperazinila opcionalmente substituído; R~ 3~ é hidrogênio ou (C~ 1-4~) alquila; X~ 1~ é CH~ 2~: X~ 2~ é CH~ 2~, O, S, CO, COO, OCO, NHCO, CONH ou NR, sendo R hidrogênio ou (C~ 1-4~) alquila; Y é (C~ 1-8~) alquileno ou (C~ 1-8~) alquilenóxi (C~ 1-6~) alquileno, (C~ 1-8~) alquenileno ou (C~ 1-8~) alquenilenóxi (C~ 1-6~) alquileno; Ar é um anel fenila opcionalmente mono di ou trissubstituído por, independentemente, hidróxi ou halogênio, no qual X~ 1~ e X~ 2~ estão na posição meta ou para relativo um ao outro e Z é CO; AA é um alfa-aminoácido natural ou não-natural e n é O ou 1 ou Z é SO~ 2~; AA é um grupo etilenocarbonila opcionalmente substituído (derivado de um alfa-aminoácido natural ou não-natural por substituição do nitrogênio por um grupo metileno) e n é 1; processos para a preparação desses compostos; composições e combinações farmacêuticas contendo os mesmos e seus usos no tratamento de distúrbios neurológicos e vasculares relacionados com a geração e/ou a agregação da beta-amilóide.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0315654.4A GB0315654D0 (en) | 2003-07-03 | 2003-07-03 | Organic compounds |
| PCT/EP2004/007247 WO2005003106A1 (en) | 2003-07-03 | 2004-07-02 | Macrocyclic compounds having aspartic protease inhibiting activity and pharmaceutical uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0412286A true BRPI0412286A (pt) | 2006-09-19 |
Family
ID=27741562
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0412286-0A BRPI0412286A (pt) | 2003-07-03 | 2004-07-02 | composto macrocìclos tendo atividade inibidora da protease aspástica e usos farmacêuticos dos mesmos |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US20060223745A1 (pt) |
| EP (1) | EP1654241B1 (pt) |
| JP (1) | JP2009513510A (pt) |
| CN (1) | CN1809542A (pt) |
| AT (1) | ATE389642T1 (pt) |
| AU (1) | AU2004253667B2 (pt) |
| BR (1) | BRPI0412286A (pt) |
| CA (1) | CA2529571A1 (pt) |
| DE (1) | DE602004012572T2 (pt) |
| ES (1) | ES2300790T3 (pt) |
| GB (1) | GB0315654D0 (pt) |
| MX (1) | MXPA05014011A (pt) |
| PL (1) | PL1654241T3 (pt) |
| PT (1) | PT1654241E (pt) |
| WO (1) | WO2005003106A1 (pt) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0606636A2 (pt) * | 2005-01-13 | 2009-07-07 | Novartis Ag | compostos macrocìclicos úteis como inibidores de bace |
| GB0500683D0 (en) * | 2005-01-13 | 2005-02-23 | Novartis Ag | Organic compounds |
| CA2609562A1 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Macrocyclic heterocyclic aspartyl protease inhibitors |
| GB0526614D0 (en) | 2005-12-30 | 2006-02-08 | Novartis Ag | Organic compounds |
| CN107849026B (zh) | 2015-07-29 | 2021-01-01 | 百时美施贵宝公司 | 携带烷基或环烷基p2′部分的因子xia大环抑制剂 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6184241B1 (en) * | 1998-08-24 | 2001-02-06 | Kansas State University Research Foundation | Aspartic protease inhibitors |
-
2003
- 2003-07-03 GB GBGB0315654.4A patent/GB0315654D0/en not_active Ceased
-
2004
- 2004-07-02 JP JP2006518098A patent/JP2009513510A/ja active Pending
- 2004-07-02 CA CA002529571A patent/CA2529571A1/en not_active Abandoned
- 2004-07-02 PT PT04740596T patent/PT1654241E/pt unknown
- 2004-07-02 ES ES04740596T patent/ES2300790T3/es not_active Expired - Lifetime
- 2004-07-02 EP EP04740596A patent/EP1654241B1/en not_active Expired - Lifetime
- 2004-07-02 CN CNA2004800174050A patent/CN1809542A/zh active Pending
- 2004-07-02 AU AU2004253667A patent/AU2004253667B2/en not_active Ceased
- 2004-07-02 BR BRPI0412286-0A patent/BRPI0412286A/pt not_active IP Right Cessation
- 2004-07-02 US US10/561,949 patent/US20060223745A1/en not_active Abandoned
- 2004-07-02 DE DE602004012572T patent/DE602004012572T2/de not_active Expired - Lifetime
- 2004-07-02 MX MXPA05014011A patent/MXPA05014011A/es active IP Right Grant
- 2004-07-02 AT AT04740596T patent/ATE389642T1/de not_active IP Right Cessation
- 2004-07-02 PL PL04740596T patent/PL1654241T3/pl unknown
- 2004-07-02 WO PCT/EP2004/007247 patent/WO2005003106A1/en not_active Ceased
-
2007
- 2007-11-14 US US11/939,936 patent/US20080070885A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU2004253667B2 (en) | 2008-12-18 |
| WO2005003106A1 (en) | 2005-01-13 |
| AU2004253667A1 (en) | 2005-01-13 |
| US20060223745A1 (en) | 2006-10-05 |
| GB0315654D0 (en) | 2003-08-13 |
| HK1090366A1 (en) | 2006-12-22 |
| CN1809542A (zh) | 2006-07-26 |
| EP1654241B1 (en) | 2008-03-19 |
| EP1654241A1 (en) | 2006-05-10 |
| JP2009513510A (ja) | 2009-04-02 |
| ES2300790T3 (es) | 2008-06-16 |
| MXPA05014011A (es) | 2006-03-02 |
| US20080070885A1 (en) | 2008-03-20 |
| ATE389642T1 (de) | 2008-04-15 |
| DE602004012572T2 (de) | 2009-04-16 |
| PL1654241T3 (pl) | 2008-09-30 |
| CA2529571A1 (en) | 2005-01-13 |
| PT1654241E (pt) | 2008-06-03 |
| DE602004012572D1 (de) | 2008-04-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: CONFORME ARTIGO 10O DA RESOLUCAO 124/06, CABE SER ARQUIVADO REFERENTE AO NAO RECOLHIMENTO DA 7A ANUIDADE. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2138 DE 27/12/2011. |