BR9713351A - N-(aril/heteroaril/alquilacetil) aminoácido amidas, composições farmacêuticas compreendendo as mesmas, e métodos para a inibição da liberação de peptìdeo beta-amilóide e/ou de sua sìntese pelo uso de tais compostos - Google Patents
N-(aril/heteroaril/alquilacetil) aminoácido amidas, composições farmacêuticas compreendendo as mesmas, e métodos para a inibição da liberação de peptìdeo beta-amilóide e/ou de sua sìntese pelo uso de tais compostosInfo
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- BR9713351A BR9713351A BR9713351-5A BR9713351A BR9713351A BR 9713351 A BR9713351 A BR 9713351A BR 9713351 A BR9713351 A BR 9713351A BR 9713351 A BR9713351 A BR 9713351A
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- heteroaryl
- aryl
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- compounds
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- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
- C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
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- C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
- C07C233/35—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
- C07C233/37—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a saturated carbon skeleton containing rings
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- C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
- C07C233/35—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
- C07C233/39—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of an unsaturated carbon skeleton containing rings other than six-membered aromatic rings
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- C07C233/45—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
- C07C233/46—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
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- C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
- C07C235/34—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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- C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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- C07C255/32—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
- C07C255/42—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms
- C07C255/44—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms at least one of the singly-bound nitrogen atoms being acylated
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- C07C255/65—Carboxylic acid nitriles containing cyano groups and nitrogen atoms further bound to other hetero atoms, other than oxygen atoms of nitro or nitroso groups, bound to the same carbon skeleton with the nitrogen atoms further bound to nitrogen atoms
- C07C255/66—Carboxylic acid nitriles containing cyano groups and nitrogen atoms further bound to other hetero atoms, other than oxygen atoms of nitro or nitroso groups, bound to the same carbon skeleton with the nitrogen atoms further bound to nitrogen atoms having cyano groups and nitrogen atoms being part of hydrazine or hydrazone groups bound to the same carbon skeleton
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- C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
- C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
- C07C323/57—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups
- C07C323/58—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups with amino groups bound to the carbon skeleton
- C07C323/59—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups with amino groups bound to the carbon skeleton with acylated amino groups bound to the carbon skeleton
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- C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
- C07C323/62—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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- C07D213/72—Nitrogen atoms
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- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
- C07D333/60—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
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- C07C2601/14—The ring being saturated
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- C07C2601/16—Systems containing only non-condensed rings with a six-membered ring the ring being unsaturated
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Abstract
Patente de Invenção: <B>"N-(ARIL/HETEROARIL/ALQUILACETIL) AMINOáCIDO AMIDAS, COMPOSIçõES FARMACêUTICAS COMPREENDENDO AS MESMAS, E MéTODOS PARA A INIBIçãO DA LIBERAçãO DE PEPTìDEO BETA-AMILóIDE E/OU DE SUA SìNTESE PELO USO DE TAIS COMPOSTOS"<D>. São divulgados compostos que inibem a liberação de peptídeo -amilóide e/ou a sua síntese, e, assim, têm utilidade no tratamento da doença de Alzheimer. Também divulgadas são as composições farmacêuticas compreendendo um composto, o qual inibe a liberação de peptídeo -amilóide e/ou a sua síntese, assim como os métodos para o tratamento da doença de Alzheimer, tanto profilática como terapeuticamente, com tais composições farmacêuticas. Os ditos compostos são representados pela fórmula (I), onde R^ 1^ é selecionado do grupo consistindo em: a) alquila, alquenila, alcarila, alquicicloalquila, arila, cicloalquila, cicloalquenila, heteroarila e heterocíclico; b) um grupo fenila substituído de fórmula II, onde R é alquileno de 1 a 8 átomos de carbono, m é um número inteiro igual a 0 ou 1, e c) 1- ou 2-naftila substituída nas posições nas posições 5, 6, 7 e/ou 8, R^ 2^ é selecionado do grupo consistindo em hidrogênio, alquila de 1 a 4 átomos de carbono, alquilalcóxi de 1 a 4 átomos de carbono, alquiltioalcóxi de 1 a 4 átomos de carbono; e R^ 3^ e R^ 3'^ são independentemente selecionados do grupo consistindo em: (a) hidrogênio, (b) alquila, (c) -(R^ 7^)~ n~(W)~ p~ onde R^ 7^ é um grupo alquileno, W é selecionado do grupo consistindo em (i) fórmula A; (ii) heteroarila; e (iii) N-heterocíclico, e n é um número inteiro igual a 0 ou 1, e p é um número inteiro igual a 1 a 3; (d) -CH(<237>)CH~ 2~C(O)O-Q, onde Q é selecionado do grupo consistindo em alquila, arila, heteroarila e heterocíclico; X' é hidrogênio, hidróxipu flúor; X" é hidrogênio, hidróxi ou flúor, ou X' é X" juntos formam um grupo oxo, Z é selecionado do grupo consistindo em uma ligação covalentemente ligando R^ 1^ a -CHX'X", oxigênio e enxofre.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US75489596A | 1996-11-22 | 1996-11-22 | |
US80753897A | 1997-02-28 | 1997-02-28 | |
PCT/US1997/022231 WO1998022433A1 (en) | 1996-11-22 | 1997-11-21 | N-(ARYL/HETEROARYL/ALKYLACETYL) AMINO ACID AMIDES, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, AND METHODS FOR INHIBITING β-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS BY USE OF SUCH COMPOUNDS |
Publications (1)
Publication Number | Publication Date |
---|---|
BR9713351A true BR9713351A (pt) | 2000-01-25 |
Family
ID=27116009
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR9713351-5A BR9713351A (pt) | 1996-11-22 | 1997-11-21 | N-(aril/heteroaril/alquilacetil) aminoácido amidas, composições farmacêuticas compreendendo as mesmas, e métodos para a inibição da liberação de peptìdeo beta-amilóide e/ou de sua sìntese pelo uso de tais compostos |
Country Status (16)
Country | Link |
---|---|
EP (1) | EP0946499B1 (pt) |
JP (1) | JP2001504498A (pt) |
KR (1) | KR20000069075A (pt) |
CN (1) | CN1238760A (pt) |
AT (1) | ATE296797T1 (pt) |
AU (1) | AU729133B2 (pt) |
BR (1) | BR9713351A (pt) |
CA (1) | CA2272065A1 (pt) |
DE (1) | DE69733432T2 (pt) |
ID (1) | ID22499A (pt) |
IL (1) | IL129504A0 (pt) |
NO (1) | NO992381L (pt) |
NZ (1) | NZ335280A (pt) |
PL (1) | PL334516A1 (pt) |
TR (1) | TR199901603T2 (pt) |
WO (1) | WO1998022433A1 (pt) |
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1997
- 1997-11-21 IL IL12950497A patent/IL129504A0/xx unknown
- 1997-11-21 CN CN97199988A patent/CN1238760A/zh active Pending
- 1997-11-21 BR BR9713351-5A patent/BR9713351A/pt unknown
- 1997-11-21 PL PL97334516A patent/PL334516A1/xx unknown
- 1997-11-21 TR TR1999/01603T patent/TR199901603T2/xx unknown
- 1997-11-21 JP JP52401898A patent/JP2001504498A/ja active Pending
- 1997-11-21 KR KR1019997004508A patent/KR20000069075A/ko not_active Application Discontinuation
- 1997-11-21 WO PCT/US1997/022231 patent/WO1998022433A1/en not_active Application Discontinuation
- 1997-11-21 EP EP97947643A patent/EP0946499B1/en not_active Expired - Lifetime
- 1997-11-21 CA CA002272065A patent/CA2272065A1/en not_active Abandoned
- 1997-11-21 DE DE69733432T patent/DE69733432T2/de not_active Expired - Fee Related
- 1997-11-21 ID IDW990396A patent/ID22499A/id unknown
- 1997-11-21 NZ NZ335280A patent/NZ335280A/en unknown
- 1997-11-21 AU AU52677/98A patent/AU729133B2/en not_active Ceased
- 1997-11-21 AT AT97947643T patent/ATE296797T1/de not_active IP Right Cessation
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1999
- 1999-05-18 NO NO992381A patent/NO992381L/no unknown
Also Published As
Publication number | Publication date |
---|---|
KR20000069075A (ko) | 2000-11-25 |
AU729133B2 (en) | 2001-01-25 |
CA2272065A1 (en) | 1998-05-28 |
TR199901603T2 (xx) | 2000-02-21 |
DE69733432D1 (de) | 2005-07-07 |
JP2001504498A (ja) | 2001-04-03 |
EP0946499B1 (en) | 2005-06-01 |
IL129504A0 (en) | 2000-02-29 |
NO992381D0 (no) | 1999-05-18 |
PL334516A1 (en) | 2000-02-28 |
EP0946499A1 (en) | 1999-10-06 |
ID22499A (id) | 1999-10-21 |
WO1998022433A1 (en) | 1998-05-28 |
NO992381L (no) | 1999-07-21 |
AU5267798A (en) | 1998-06-10 |
CN1238760A (zh) | 1999-12-15 |
ATE296797T1 (de) | 2005-06-15 |
NZ335280A (en) | 2001-05-25 |
DE69733432T2 (de) | 2006-05-04 |
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