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31. 发明专利

AR066605A1 DERIVADOS DE HETEROARILAMIDA PIRIMIDONA 未知
公开(公告)号：AR066605A1
公开(公告)日：2009-09-02
申请号：ARP080102086
申请日：2008-05-16
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP
发明人： GALLET THIERRY , LOCHEAD ALISTAIR , SAADY MOURAD , YAICHE PHILIPPE , VERONIQUE CORINNE , CHEREZE NATHALIE
IPC分类号： C07D239/38 , C07D405/12 , C07D403/12 , C07D471/04 , C07D401/12 , C07D417/12 , C07D409/12 , A61K31/506 , A61K31/505 , A61P35/00
摘要： Un derivado de pirimidona representado por la formula (1) o una sal del mismo, o un solvato del mismo o un hidrato del mismo, en la que: X representa dos átomos de hidrogeno, un átomo de azufre, un átomo de oxígeno o un grupo alquilo C1-2, y un átomo de hidrogeno; Z representa un enlace, un átomo de oxigeno, un átomo de nitrogeno sustituido con un átomo de hidrogeno o un grupo alquilo C1-3, un átomo de azufre, un grupo metileno opcionalmente sustituido con uno o dos grupos elegidos entre un grupo alquilo C1-6, un grupo hidroxilo, un grupo alcoxi C1-6, un grupo alquilo C1-2 perhalogenado o un grupo amino; R1 representa un anillo de 2, 4 o 5-pirimidina o un anillo de 4-piridina, estando el anillo opcionalmente sustituido con un grupo alquilo C1-6, un grupo alcoxi C1-6, o un átomo de halogeno; R2 representa un grupo heterocíclico de 4 a 15 miembros, estando este grupo opcionalmente sustituido con 1 a 4 sustituyentes seleccionados entre un grupo alquilo C1-6, un átomo de halogeno, un grupo alquilo C1-2 perhalogenado, un grupo alquilo C1-6 halogenado, un grupo hidroxilo, un grupo alcoxi C1-6, un grupo alcoxi C1-2 perhalogenado, un grupo alcoxi C1-6 halogenado, un grupo nitro, ciano, amino, monoalquilamino C1-6, un grupo dialquilamino C2-12, un grupo S-alquilo C1-6, un grupo heterocíclico, un grupo arilo, un grupo heteroarilo, un grupo O-arilo o un grupo S-arilo, estando los grupos anteriormente mencionados opcionalmente sustituidos con 1 a 4 sustituyentes seleccionados de un grupo alquilo C1-6, un átomo de halogeno, un grupo alcoxi C1-6, un grupo C(O)O-alquilo C1-6, o C(O)O-arilo-, estando el arilo opcionalmente sustituido con 1 a 4 sustituyentes seleccionados de un grupo alquilo C1-6, un átomo de halogeno, un grupo alcoxi C1-6; R3 representa un átomo de hidrogeno, un grupo alquilo C1-6, o un átomo de halogeno; R4 representa un átomo de hidrogeno o un grupo alquilo C1-6; R5 representa un átomo de hidrogeno, un grupo alquilo C1-6; R6 representa un átomo de hidrogeno, un grupo alquilo C1-6; R7 representa un átomo de hidrogeno o un grupo alquilo C1-6; y n representa de 0 a 3 y m representa 0 en forma de una base libre o una sal de adicion con un ácido. Procesos de obtencion y composiciones farmacéuticas que los comprenden y usos. Reivindicacion 18: Un derivado de pirimidona representado por la formula (3) en la que R1, R3, R4, R5, R6 y m son como se han definido para el compuesto de la formula (1) segun la reivindicacion 1.

32. 发明专利

DE602004006169T2 未知
公开(公告)号：DE602004006169T2
公开(公告)日：2008-01-10
申请号：DE602004006169
申请日：2004-12-17
申请人： SANOFI AVENTIS , MITSUBISHI PHARMA CORP
发明人： CHEREZE NATHALIE , LOCHEAD ALISTAIR , SAADY MOURAD , SLOWINSKI FRANCK , YAICHE PHILIPPE
IPC分类号： C07D487/04 , A61K31/505 , A61P25/28
摘要： The invention relates to a dihydrospiro-ÄcycloalkylamineÜ-pyrimidone derivative represented by formula (I) or a salt thereof: wherein: X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, a carbonyl group, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted; R2 represents a benzene ring or a naphthalene ring; the rings being optionally substituted; R3 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom, a C1-4 alkoxy carbonyl group, a C1-6 alkyl group optionally substituted; o and m represent 1 to 2; n represents 0 to 3; p represents 0 to 2; and q represents 0 to 2. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3 beta , such as Alzheimer disease.

33. 发明专利

SI1699795T1 Substituirani 8-piri(mi)dinil-dihidrospiro-(cikloalkilamin)pirimido(1,2a) pirimidin-6-onski derivati 未知
公开(公告)号：SI1699795T1
公开(公告)日：2007-10-31
申请号：SI200430369
申请日：2004-12-17
申请人： SANOFI AVENTIS , MITSUBISHI PHARMA CORP
发明人： CHEREZE NATHALIE , LOCHEAD ALISTAIR , SAADY MOURAD , SLOWINSKI FRANCK , YAICHE PHILIPPE
IPC分类号： C07D487/00 , A61K31/00 , A61K31/505 , A61P25/00 , C07D487/04

34. 发明专利

CA2630360A1 SUBSTITUTED BICYCLIC PYRIMIDONE DERIVATIVES 未知
公开(公告)号：CA2630360A1
公开(公告)日：2007-05-24
申请号：CA2630360
申请日：2006-11-21
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP
发明人： YAICHE PHILIPPE , LOCHEAD ALISTAIR , SAADY MOURAD , SLOWINSKI FRANCK , CHEREZE NATHALIE
IPC分类号： C07D471/04 , A61K31/519
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C 1-2 alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom substituted by a hydrogen atom or a C 1-3 alkyl group, a sulphur atom, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted; R2 represents a benzene ring or a naphthalene ring; the rings being optionally substituted; R3 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom or a C 1-6 alkyl group; R5 represents a hydrogen atom, a C 1-6 alkoxy carbonyl group or a C 1-6 alkyl group optionally substituted; R6 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R7 represents a hydrogen atom or a C 1-6 alkyl group; n represents 0 to 3; m represents 0 to 1; o represents 0 to 2. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3², such as Alzheimer disease.

35. 发明专利

NZ592740A CARBAMATE DERIVATIVES OF ALKYL-HETEROCYCLES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF 未知
公开(公告)号：NZ592740A
公开(公告)日：2013-03-28
申请号：NZ59274009
申请日：2009-11-13
申请人： SANOFI AVENTIS
发明人： ABOUABDELLAH AHMED , CHEREZE NATHALIE , FAYOL AUDE , SAADY MOURAD , VACHE JULIEN , VERONIQUE CORINNE , YAICHE PHILIPPE
IPC分类号： C07D417/14 , A61K31/445 , A61K31/4709 , A61K31/497 , A61K31/498 , A61K31/501 , A61K31/502 , A61K31/506 , A61P25/00 , A61P29/00 , C07D401/14 , C07D403/14 , C07D407/14 , C07D413/12 , C07D413/14
摘要： 592740 Disclosed herein is a compound of the general formula (I), wherein the variables are defined in the specification, and the use thereof in the treatment of a pathology in which the endogenous cannabinoids and/or any other substrate metabolised by the enzyme FAAH are involved, such as acute or chronic pain, vertigo, vomiting, nausea, eating disorders, neurological and psychiatric pathologies, acute or chronic neurodegenerative diseases, epilepsy, sleeping disorders, cardiovascular diseases, renal ischaemia, cancers, immune system disorders, allergic diseases, parasitic, viral or bacterial infectious diseases, inflammatory diseases, osteoporosis, ocular complaints, pulmonary complaints, gastrointestina1 diseases or urinary incontinence. Specific embodiments of the compound of the general formula (I) include: 3-Methylcarbamoylisoxazol-5-ylmethyl (+)-[1-(4-chloropyrimidin-2-yl)pyrrolidin-3-ylmethyl] carbamate 3-Carbamoylisoxazol-5-ylmethyl { 2-[1-(4-trifluoromethyltrifluoromethylpyrimidin-2-yl) azetidin-3-yl] ethyl} carbamate, and Ethyl 5-[1-(6-chloroquinolin-2-yl)-4-fluoropiperidin-4-ylmethylcarbamoyloxymethyl] isoxazole-3-carboxylate

36. 发明专利

MA32884B1 Derives de carbamates d'alkyl-heterocycles, leur preparation et leur application en therapeutique 未知
公开(公告)号：MA32884B1
公开(公告)日：2011-12-01
申请号：MA33921
申请日：2011-06-08
申请人： SANOFI AVENTIS
发明人： ABOUABDELLAH AHMED , CHEREZE NATHALIE , FAYOL AUDE , SAADY MOURAD , VACHE JULIEN , VERONIQUE CORINNE , YAICHE PHILIPPE
IPC分类号： C07D401/14 , A61K31/445 , A61K31/4709 , A61K31/497 , A61K31/498 , A61K31/501 , A61K31/502 , A61K31/506 , A61P25/00 , A61P29/00 , C07D403/14 , C07D407/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Composé répondant à la formule (i) dans laquelle r2 représente un atome d'hydrogène, de fluor ou un groupe hydroxyle, cyano, trifluorométhyle, c1-6-alkyle, c1-6- alcoxy, nr8r9; n représente un nombre entier égal à 1, 2 ou 3 et m représente un nombre entier égal à 1 ou 2; a représente une liaison covalente ou un groupe c1-8-alkylène; r1 représente un groupe phényle, pyridinyle, pyridazinyle, pyrimidinyle, pyrazinyle, triazinyle, naphtalènyle, quinolinyle, isoquinolinyle, phtalazinyle, quinazolinyle, quinoxalinyle, cinnolinyle, naphthyridinyle, ce groupe étant éventuellement substitué; r3 représente un atome d'hydrogène, de fluor, un groupe c1-6-alkyle ou un groupe trif luorométhyle; r4 représente un groupe choisi parmi un furanyle, pyrrolyle, thiènyle, isothiazolyle, oxazolyle, isoxazolyle, pyrazolyle, oxadiazolyle, thiadiazolyle, imidazole, triazolyle, tétrazolyle, oxazolone, oxazolidinone, isoxazolone, isoxazolidinone, isothiazolone, isothiazolidinone, imidazolone, imidazolidinone, pyrazolone, pyrazolidinone, oxadiazolone, thiadiazolone, triazolone, ce groupe étant éventuellement substitué; à l'état de base ou de sel d'addition à un acide. Application en thérapeutique.

37. 发明专利

RS51654B SUBSTITUTED BICYCLIC PYRIMIDONE DERIVATIVES 未知
公开(公告)号：RS51654B
公开(公告)日：2011-10-31
申请号：RSP20110055
申请日：2006-11-21
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP
发明人： LOCHEAD ALISTAIR , CHEREZE NATHALIE , SAADY MOURAD , SLOWINSKI FRANCK , YAICHE PHILIPPE
IPC分类号： C07D471/04 , A61K31/519
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C 1-2 alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom substituted by a hydrogen atom or a C 1-3 alkyl group, a sulphur atom, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted; R2 represents a benzene ring or a naphthalene ring; the rings being optionally substituted; R3 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom or a C 1-6 alkyl group; R5 represents a hydrogen atom, a C 1-6 alkoxy carbonyl group or a C 1-6 alkyl group optionally substituted; R6 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R7 represents a hydrogen atom or a C 1-6 alkyl group; n represents 0 to 3; m represents 0 to 1; o represents 0 to 2. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3², such as Alzheimer disease.

38. 发明专利

NZ581162A HETEROARYLAMIDE-SUBSTITUTED PYRIMIDONE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES 未知
公开(公告)号：NZ581162A
公开(公告)日：2011-10-28
申请号：NZ58116208
申请日：2008-05-14
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP
发明人： CHEREZE NATHALIE , GALLET THIERRY , LOCHEAD ALISTAIR , SAADY MOURAD , VERONIQUE CORINNE , YAICHE PHILIPPE
IPC分类号： A61K31/495 , A61P3/00 , A61P25/00 , A61P35/00 , C07D239/38 , C07D401/14 , C07D403/14 , C07D409/14 , C07D417/14 , C07D471/04
摘要： A pyrimidine derivative of formula (I) wherein X, Z, R1-R7, m and n are defined in claim 1. Also claimed is a process for the synthesis of the compound of formula (I) by reacting a compound of formula (II) with a compound of formula (III). The compound of formula (I) is a glycogen synthase kinase 3-beta (GSK3-beta) inhibitor and can be used to treat a neurodegenerative disease, cancer, malaria, bone diseases, Pemphigus vulgaris and neutropenia induced by cancer chemotherapy.

39. 发明专利

BRPI0618752A2 未知
公开(公告)号：BRPI0618752A2
公开(公告)日：2011-09-27
申请号：BRPI0618752
申请日：2006-11-21
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP
发明人： LOCHEAD ALISTAIR , SAADY MOURAD , SLOWINSKI FRANCK , YAICHE PHILIPPE , CHEREZE NATHALIE
IPC分类号： C07D471/04 , A61K31/519
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C 1-2 alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom substituted by a hydrogen atom or a C 1-3 alkyl group, a sulphur atom, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted; R2 represents a benzene ring or a naphthalene ring; the rings being optionally substituted; R3 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom or a C 1-6 alkyl group; R5 represents a hydrogen atom, a C 1-6 alkoxy carbonyl group or a C 1-6 alkyl group optionally substituted; R6 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R7 represents a hydrogen atom or a C 1-6 alkyl group; n represents 0 to 3; m represents 0 to 1; o represents 0 to 2. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3², such as Alzheimer disease.

40. 发明专利

SI1957492T1 Substituirani biciklični pirimidonski derivati 未知
公开(公告)号：SI1957492T1
公开(公告)日：2011-02-28
申请号：SI200630901
申请日：2006-11-21
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP
发明人： CHEREZE NATHALIE , LOCHEAD ALISTAIR , SAADY MOURAD , SLOWINSKI FRANCK , YAICHE PHILIPPE
IPC分类号： C07D471/00 , A61K31/519

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