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1. 发明申请

WO2005051917B1 PYRAZOLYL DERIVATIVES IN THE FORM OF DRUGS FOR TREATING ACUTE OR CHRONIC NEURONAL REGRESSIONS 审中-公开
标题翻译：用于治疗急性或慢性神经元回顾的药物形式的吡唑衍生物
公开(公告)号：WO2005051917B1
公开(公告)日：2005-08-04
申请号：PCT/FR2004002968
申请日：2004-11-22
申请人： AVENTIS PHARMA SA , GENEVOIS-BORELLA ARIELLE , MALLERON JEAN-LUC , BOUQUEREL JEAN , DOERFLINGER GILLES , BOHME ANDREES , TOUYER GAETAN , SABUCO JEAN-FRANCOIS , TERRIER CORINNE , MIGNANI SERGE , EVERS MICHEL , EL-AHMAD YOUSSEF
发明人： GENEVOIS-BORELLA ARIELLE , MALLERON JEAN-LUC , BOUQUEREL JEAN , DOERFLINGER GILLES , BOHME ANDREES , TOUYER GAETAN , SABUCO JEAN-FRANCOIS , TERRIER CORINNE , MIGNANI SERGE , EVERS MICHEL , EL-AHMAD YOUSSEF
IPC分类号： A61K31/41 , A61K31/416 , A61K31/435 , A61K31/454 , A61K31/55 , C07D231/12 , C07D231/14 , C07D231/20 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D409/04 , C07D453/02 , C07D453/06 , C07D487/08
CPC分类号： C07D231/12 , C07D231/14 , C07D231/20 , C07D401/04 , C07D401/06 , C07D403/06 , C07D409/04 , C07D453/02 , C07D453/06 , C07D487/08
摘要： The invention relates to novel derivatives of general formula (I), wherein A, if present, is an alkyl radical (C1-C6), an alkenyl radical (C3-C6), an alkynyl radical (C3-C6), a cycloalkyl radical (C3-C7), a cycloalkenyl radical (C5-C7), R1 is a NR6R7, azacycloalkyl (C4-C7), azacycloalkenyl (C5-C7) azabicycloalkyl (C5-C9) and azabicycloalkenyl (C5-C9) group; A-R1 is such that nitrogen of R1 et nitrogen 1 of pyrazole are indispensably separated by at lest two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra and NHSO2Ra radical; R4 is an aryl or heteroaryl radical; R5 is a H, halogen, CF3, CHF2, CH2F, linear or branched alkyl (C1-C6) and cycloalkyl (C3-C7) radical, the racemics, enantiomers and diastereoisomers thereof and the mixtures thereof, tautomers thereof and the pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及通式（I）的新衍生物，其中如果存在，A为烷基（C 1 -C 6），烯基（C 3 -C 6），炔基（C 3 -C 6），环烷基（C5-C7），环烯基（C5-C7），R1是NR6R7，氮杂环烷基（C4-C7），氮杂环烯基（C5-C7）氮杂二环烷基（C5-C9）和氮杂双环烯基 A-R 1使得R 1的氮和吡唑的氮1不可或缺地被至少两个碳原子隔开，R 3为H，卤素，OH，SH，NH 2，OR c，SR c，SOR a，SO 2 R a，NHCHO，NR a R b，NHC （O）Ra，NHC（S）Ra和NHSO2Ra基团; R4是芳基或杂芳基; R5是H，卤素，CF3，CHF2，CH2F，直链或支链烷基（C1-C6）和环烷基（C3-C7）基团，其外消旋体，对映体和非对映异构体及其混合物，其互变异构体和药学上可接受的盐它们。

2. 发明申请

WO2005051917A9 PYRAZOLYL DERIVATIVES IN THE FORM OF DRUGS FOR TREATING ACUTE OR CHRONIC NEURONAL REGRESSIONS 审中-公开
标题翻译：用于治疗急性或慢性神经再生的药物形式中的吡唑啉衍生物
公开(公告)号：WO2005051917A9
公开(公告)日：2005-09-29
申请号：PCT/FR2004002968
申请日：2004-11-22
申请人： AVENTIS PHARMA SA , GENEVOIS-BORELLA ARIELLE , MALLERON JEAN-LUC , BOUQUEREL JEAN , DOERFLINGER GILLES , BOHME ANDREES , TOUYER GAETAN , SABUCO JEAN-FRANCOIS , TERRIER CORINNE , MIGNANI SERGE , EVERS MICHEL , EL-AHMAD YOUSSEF
发明人： GENEVOIS-BORELLA ARIELLE , MALLERON JEAN-LUC , BOUQUEREL JEAN , DOERFLINGER GILLES , BOHME ANDREES , TOUYER GAETAN , SABUCO JEAN-FRANCOIS , TERRIER CORINNE , MIGNANI SERGE , EVERS MICHEL , EL-AHMAD YOUSSEF
IPC分类号： A61K31/41 , A61K31/416 , A61K31/435 , A61K31/454 , A61K31/55 , C07D231/12 , C07D231/14 , C07D231/20 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D409/04 , C07D453/02 , C07D453/06 , C07D487/08
CPC分类号： C07D231/12 , C07D231/14 , C07D231/20 , C07D401/04 , C07D401/06 , C07D403/06 , C07D409/04 , C07D453/02 , C07D453/06 , C07D487/08
摘要： The invention relates to novel derivatives of general formula (I), wherein A, if present, is an alkyl radical (C1-C6), an alkenyl radical (C3-C6), an alkynyl radical (C3-C6), a cycloalkyl radical (C3-C7), a cycloalkenyl radical (C5-C7), R1 is a NR6R7, azacycloalkyl (C4-C7), azacycloalkenyl (C5-C7) azabicycloalkyl (C5-C9) and azabicycloalkenyl (C5-C9) group; A-R1 is such that nitrogen of R1 et nitrogen 1 of pyrazole are indispensably separated by at lest two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra and NHSO2Ra radical; R4 is an aryl or heteroaryl radical; R5 is a H, halogen, CF3, CHF2, CH2F, linear or branched alkyl (C1-C6) and cycloalkyl (C3-C7) radical, the racemics, enantiomers and diastereoisomers thereof and the mixtures thereof, tautomers thereof and the pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及通式（I）的新衍生物，其中A（如果存在）是烷基（C 1 -C 6），烯基（C 3 -C 6），炔基（C 3 -C 6），环烷基（C 3 -C 7），环烯基（C 5 -C 7），R 1是NR 6 R 7，氮杂环烷基（C 4 -C 7），氮杂环烯基（C 5 -C 7）氮杂双环烷基（C 5 -C 9）和氮杂双环链烯基（C 5 -C 9） A-R1使得吡唑的R1和氮1的氮不可避免地被至少两个碳原子分开，R3是H，卤素，OH，SH，NH2，ORc，SRc，SORa，SO2Ra，NHCHO，NRaRb，NHC （O）Ra，NHC（S）Ra和NHSO 2 R a基团; R4是芳基或杂芳基; R5是H，卤素，CF3，CHF2，CH2F，直链或支链烷基（C1-C6）和环烷基（C3-C7）基团，其外消旋物，对映异构体和非对映异构体及其混合物，其互变异构体和药学上可接受的盐它们。

3. 发明申请

WO2009118473A3 AZETIDINE-DERIVED COMPOUNDS, PREPARATION METHOD THEREFOR AND THERAPEUTIC USE OF SAME 审中-公开
标题翻译： AZETIDINE衍生化合物，其制备方法及其治疗用途
公开(公告)号：WO2009118473A3
公开(公告)日：2009-11-19
申请号：PCT/FR2009000214
申请日：2009-02-27
申请人： SANOFI AVENTIS , AUGER FLORIAN , BERNARDELLI PATRICK , EVEN LUC , SABUCO JEAN-FRANCOIS , TERRIER CORINNE
发明人： AUGER FLORIAN , BERNARDELLI PATRICK , EVEN LUC , SABUCO JEAN-FRANCOIS , TERRIER CORINNE
IPC分类号： C07D205/04 , A61K31/40 , A61P3/10 , A61P25/28 , A61P35/00 , C07D405/12
CPC分类号： C07D205/04 , C07D405/12
摘要： The invention relates to compounds having formula (I) in which: R represents a (C1-C6)alkyl group, a halo(C1-C6)alkyl group; R1 represents a hydrogen atom, a (C1-C6)alkyl group; R2 represents (i) a (C1-C6)alkyl group substituted by one or more groups selected from the hydroxy group, the (C1-C6)alkoxy group and optionally substituted by a halo(C1-C6)alkyl group, (ii) a heterocycle group optionally substituted by one or more hydroxy groups, a (C1-C6)alkoxy group, a hydroxy(C1-C6)alkyl group, (iii) a heterocycle(C1-C6)alkyl group optionally substituted by one or more hydroxy groups; R3 and R4 each represent a phenyl group optionally substituted by one or more atoms or groups selected from a hydrogen atom, a halogen, a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, a (C1-C6)alkoxy group, a halo(C1-C6)alkoxy or cyano; Y represents a hydrogen atom, a halogen, a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, a (C1-C6)alkoxy group, a halo(C1-C6)alkoxy group, a (C1-C6)alkylS(O)p or cyano; and p is between 0 and 2; said compounds taking the form of a base or an acid addition salt. The invention also relates to the preparation method thereof and to the therapeutic use of same.
摘要翻译：本发明涉及具有式（I）的化合物，其中：R表示（C 1 -C 6）烷基，卤代（C 1 -C 6）烷基; R1表示氢原子，（C1-C6）烷基; R 2表示（i）被一个或多个选自羟基，（C 1 -C 6）烷氧基和任选被卤代（C 1 -C 6）烷基取代的基团取代的（C 1 -C 6）烷基，（ii）任选被一个或多个羟基取代的杂环基团，（C 1 -C 6）烷氧基，羟基（C 1 -C 6）烷基，（iii）任选被一个或多个羟基取代的杂环（C 1 -C 6）烷基组; R 3和R 4各自表示任选被一个或多个选自氢原子，卤素，（C 1 -C 6）烷基，卤代（C 1 -C 6）烷基，（C 1 -C 6）烷基，）烷氧基，卤代（C 1 -C 6）烷氧基或氰基; Y表示氢原子，卤素，（C1-C6）烷基，卤代（C1-C6）烷基，（C1-C6）烷氧基，卤代（C1-C6）烷氧基，（C1 -C 6）烷基S（O）p或氰基; p在0和2之间; 所述化合物为碱或酸加成盐的形式。本发明还涉及其制备方法及其治疗用途。

4. 发明申请

WO2009106708A3 AZETIDINE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPY 审中-公开
标题翻译：炔诺酮衍生物的制备及其在治疗中的应用
公开(公告)号：WO2009106708A3
公开(公告)日：2009-12-30
申请号：PCT/FR2008001748
申请日：2008-12-16
申请人： SANOFI AVENTIS , SABUCO JEAN-FRANCOIS
发明人： SABUCO JEAN-FRANCOIS
IPC分类号： C07D205/04 , A61K31/397 , A61P1/00 , A61P3/00 , A61P19/00 , A61P29/00 , A61P35/00 , C07D413/12
CPC分类号： C07D205/04 , C07D413/12
摘要： The present invention provides the compounds conforming to the formula (I) in which: R represents a (C1-C6)alkyl or halo(C1-C6)alkyl group; R' represents a group NR4R5 or OR8; A and B, when present, represent independently of one another, one or two carbon atoms, these carbon atoms being substituted by one or more hydrogens or (C1-C6)alkyl groups; the (C1-C6)alkyl group or groups being optionally substituted; A+B represent two carbons at most; R1 represents a hydrogen atom or a (C1-C6)alkyl group; R2 and R3 represent, independently of one another, a hydrogen atom or a (C1-C6)alkyl group; the (C1-C6)alkyl group being optionally substituted; R4 and R5 represent, independently of one another, a hydrogen atom or a (C1-C6)alkyl group, or form, with the nitrogen atom which carries them, a heterocycle of the azetidine, pyrrolidine, piperidine, azepan, piperazine, homopiperazine, morpholine, thiomorpholine, thiomorpholine S-oxide or thiomorpholine S-dioxide type, this heterocycle being optionally substituted by a (C1-C6)alkyl group; R6 and R7 each represent a phenyl group, which is optionally substituted; Y represents a hydrogen atom, a halogen or a (C1-C6)alkyl group, halo(C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkoxy, (C1-C6)alkylS(O)p or cyano group; R8 is a hydrogen atom, a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, an allyl group or a phenyl(C1-C6)alkyl group, the phenyl group being optionally substituted by 1 or 2 O-methyl groups; p represents an integer selected from 0, 1 and 2; in the form of the base or an addition salt with an acid or with a base. Preparation process and application in therapy.
摘要翻译：本发明提供符合式（I）的化合物，其中：R代表（C 1 -C 6）烷基或卤代（C 1 -C 6）烷基; R'表示基团NR 4 R 5或OR 8; A和B当存在时彼此独立地表示一个或两个碳原子，这些碳原子被一个或多个氢或（C 1 -C 6）烷基取代; （C 1 -C 6）烷基基团任选地被取代; A + B最多代表两个碳; R1表示氢原子或（C1-C6）烷基; R2和R3彼此独立地表示氢原子或（C1-C6）烷基; （C 1 -C 6）烷基被任选取代; R 4和R 5彼此独立地表示氢原子或（C 1 -C 6）烷基，或与携带它们的氮原子一起形成氮杂环丁烷，吡咯烷，哌啶，氮杂环庚烷，哌嗪，高哌嗪，吗啉，硫代吗啉，硫代吗啉S-氧化物或硫代吗啉S-二氧化物型，该杂环任选被（C 1 -C 6）烷基取代; R6和R7各自代表任选被取代的苯基; Y表示氢原子，卤素或（C1-C6）烷基，卤代（C1-C6）烷基，（C1-C6）烷氧基，卤代（C1-C6）烷氧基，（C1-C6） p或氰基; R8为氢原子，（C1-C6）烷基，卤代（C1-C6）烷基，烯丙基或苯基（C1-C6）烷基，该苯基任选被1或2个O - 甲基; p表示选自0,1和2的整数; 以碱或与酸或碱的加成盐的形式存在。治疗过程中的准备过程和应用。

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