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1. 发明授权

EP1233962B1 COMPOSES HETEROCYCLIQUES ET LEUR APPLICATION A TITRE DE MEDICAMENTS 有权
标题翻译：杂环化合物和它们作为药物
公开(公告)号：EP1233962B1
公开(公告)日：2006-03-01
申请号：EP00974646.2
申请日：2000-11-03
申请人： SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)
发明人： AUVIN, Serge , CHABRIER de LASSAUNIERE, Pierre-Etienne
IPC分类号： C07D407/12 , A61K31/35 , A61K31/40 , A61K31/42 , A61K31/34 , C07D307/24 , C07D405/12 , C07D413/12 , C07D263/24 , A61P39/06
CPC分类号： C07D407/12 , C07D263/24 , C07D307/24 , C07D405/12 , C07D413/12
摘要： The invention concerns novel heterocyclic derivatives having a calpain inhibiting activity and/or an activity trapping reactive oxygen species, of formula (I) wherein A, X, Y, R1, R2 and Het represent variable groups. The invention also concerns methods for preparing said compounds, pharmaceutical preparations containing them and their therapeutic use, in particular as calpain inhibitors and/or as trapping agents for reactive oxygen species, whether selectively or not.

2. 发明公开

EP1701974A2 NOUVEAUX DERIVES DU 2-HYDROXYTETRAHYDROFURANNE ET LEUR APPLICATION A TITRE DE MEDICAMENTS 有权
标题翻译： NOUVEAUX衍生物2-羟基四氢呋喃及其衍生物在药物中的应用
公开(公告)号：EP1701974A2
公开(公告)日：2006-09-20
申请号：EP04816363.8
申请日：2004-12-08
申请人： SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)
发明人： AUVIN, Serge , CHABRIER DE LASSAUNIERE, Pierre, Etienne
IPC分类号： C07K5/06 , A61K38/05
CPC分类号： C07K5/1024 , A61K38/00 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06139 , C07K5/06165 , C07K5/0821
摘要： The invention relates to 2-hydroxytetrahydrofurane derivatives having general formula (I) wherein A represents the radical (II) wherein R1, R2, R4, R5 and R6 individually represent H, a halogen atom, OH, alkyl or alkoxy, R3 represents H, alkyl or -COR1(), R10 represents H, alkyl or alkoxy, and W represents a CH2-CH2-, -CH=CH-, -0-, -S- or -NR11 bond wherein R11 represents H or alkyl; X represents CO-, -Y-CO-, -O-Y-CO- or -NR12-Y-CO-, Y represents an alkylene radical or a haloalkylene radical, R12 represents H, alkyl or -COR13, R13 represents H, alkyl, haloalkyl or alkoxy, AA represents, each time when it occurs, a natural amino acid or not; n represents 2 or 3; and R represents H, alkyle or -CO-R19, R19 represents alkyl. Said compounds inhibit calpains and / or trap reactive forms of oxygen and can be used to prepare a medicament used to treat inflammatory diseases and immunological diseases, cardiovascular diseases and cerebro-vascular diseases, disorders of the central or peripheral nervous system, osteoporosis, muscular distrophy, proliferative diseases, cataracts, rejection reactions following organ transplants and viral and auto-immune diseases.
摘要翻译：本发明涉及具有通式（I）的2-羟基四氢呋喃衍生物，其中A代表其中R1，R2，R4，R5和R6分别代表H，卤素原子，OH，烷基或烷氧基，R3代表H，烷基或-COR 1（），R 10代表H，烷基或烷氧基，且W代表CH 2 -CH 2 - ， - CH = CH-，-O - ， - S-或-NR 11键，其中R 11代表H或烷基; X代表CO-，-Y-CO-，-OY-CO-或-NR12-Y-CO-，Y代表亚烷基或卤代亚烷基，R12代表H，烷基或-COR13，R13代表H，烷基，卤代烷基或烷氧基，AA每次出现时代表天然氨基酸; n代表2或3; 和R代表H，烷基或-CO-R19，R19代表烷基。所述化合物抑制钙蛋白酶和/或捕获氧的反应性形式，并且可用于制备用于治疗炎性疾病和免疫性疾病，心血管疾病和脑血管疾病，中枢或外周神经系统疾病，骨质疏松症，肌肉萎缩症的药物，增殖性疾病，白内障，器官移植后的排斥反应以及病毒和自身免疫疾病。

3. 发明授权

EP0991654B1 NOUVEAUX DERIVES DU 2-(IMINOMETHYL)AMINO-PHENYLE, LEUR PREPARATION, LEUR APPLICATION A TITRE DE MEDICAMENTS ET LES COMPOSITIONS PHARMACEUTIQUES LES CONTENANT 失效
标题翻译： 2-（亚氨基甲基）氨基衍生物，生产，用作药物和药物制剂含有它们
公开(公告)号：EP0991654B1
公开(公告)日：2005-06-15
申请号：EP98932205.2
申请日：1998-06-15
申请人： SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)
发明人： AUVIN, Serge , HARNETT, Jeremiah , BIGG, Dennis , CHABRIER DE LASSAUNIERE, Pierre-Etienne
IPC分类号： C07D521/00 , A61K31/38 , A61K31/425 , A61K31/445 , A61K31/415 , C07D417/12 , C07D277/04 , C07D409/12 , C07D211/70 , C07D333/70 , C07D277/06 , C07D307/68 , C07D233/78 , C07D277/14 , C07D207/16
CPC分类号： C07D417/12 , C07D333/38 , C07D409/12 , C07D409/14 , C07D413/12
摘要： The invention concerns novel 2-(iminomethyl)amino-phenyl derivatives, their preparation, their application as medicines and compositions containing them.

4. 发明授权

EP1115719B1 DERIVES D'AMIDINES, LEUR PREPARATION, LEUR APPLICATION A TITRE DE MEDICAMENTS ET LES COMPOSITIONS PHARMACEUTIQUES LES CONTENANT 有权
标题翻译：脒，生产，它们的使用毒品和装有药剂
公开(公告)号：EP1115719B1
公开(公告)日：2003-03-05
申请号：EP99943024.2
申请日：1999-09-22
申请人： SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)
发明人： AUVIN, Serge , CHABRIER DE LASSAUNIERE, Pierre-Etienne , HARNETT, Jeremiah , PONS, Dominique , ULIBARRI, Gérard
IPC分类号： C07D333/36 , A61K31/38 , A61K31/495 , C07D409/12 , C07D333/38
CPC分类号： C07D409/12 , C07C217/84 , C07D333/20 , C07D333/36 , C07D333/38 , C07D409/14 , C07D417/12 , C07D473/08
摘要： The invention concerns novel amidine derivatives, and in particular the following compounds: 2-hydroxy -5-methoxy -N-{2-[4-[(2 -thienyl(imino) methyl) amino]phenyl]ethyl} -benzamide; 2.5-dihydroxy -N-{2-[4[2 -thienyl(imino)methyl) amino]phenyl]ethyl} -benzamide ; and their use as medicines and pharmaceutical compositions containing them.

5. 发明公开

EP1954288A1 DERIVES D'AMIDINE ET LEURS APPLICATIONS A TITRE DE MEDICAMENT 有权
标题翻译：脒衍生物及其作为医药
公开(公告)号：EP1954288A1
公开(公告)日：2008-08-13
申请号：EP06820232.4
申请日：2006-10-18
申请人： SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)
发明人： AUVIN, Serge , BIGG, Dennis , CHABRIER DE LASSAUNIERE, Pierre-Etienne , PIGNOL, Bernadette
IPC分类号： A61K31/5415 , C07D417/12 , C07D279/20
CPC分类号： C07D417/12 , C07D279/16 , C07D279/20
摘要： The invention concerns amidine derivatives of general formula (I) exhibiting an inhibitory activity of calpains and/or a trapping activity of reactive forms of oxygen.

6. 发明授权

EP1115720B1 DERIVES DE N-(IMINOMETHYL)AMINES, LEUR PREPARATIONLEUR APPLICATION A TITRE DE MEDICAMENTS ET LES COMPOSITI ONS PHARMACEUTIQUES LES CONTENANT 有权
标题翻译： N-（亚氨基甲基）胺衍生物，它们的生产和它们在新药与装有药剂
公开(公告)号：EP1115720B1
公开(公告)日：2008-07-02
申请号：EP99943025.9
申请日：1999-09-22
申请人： SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)
发明人： BIGG, Dennis , CHABRIER DE LASSAUNIERE, Pierre-Etienne , AUVIN, Serge , HARNETT, Jeremiah , ULIBARRI, Gérard
IPC分类号： C07D333/38 , A61K31/38 , C07D409/12 , C07D417/12
CPC分类号： C07D333/38
摘要： The invention concerns novel N-(iminomethyl)amine derivatives comprising in their skeleton the aminophenylamine, oxodiphenylamine, carbazole, phenazine, phenoxazine or oxodiphenyl motif, their use as medicines and pharmaceutical compositions containing them. The invention concerns in particular the following compounds: -4-{[2-thienyl (imino) methyl]amino}-N- [2-(phenylamino) phenyl]- benzenebutanamide; -4-{[2- thienyl (imino) methyl]amino}- N-[4-(phenylamino) phenyl]- benzenebutanamide; -N'-[4- (10H- phenothiazin - 2-yloxy) phenyl]- 2-thiophenecarboximidamide; -4-(4-{[amino (2-thienyl) methylidene] amino}phenyl) -N-(10H- phenothiazin- 3-ylH) butanamide; -3-[(3-{[amino (2-thienyl) methylidene] amino}-benzyl) amino]-N- (4-anilinophenyl) propanamide; -N'-(4-{2- [(10H-phenothiazin- 3-ylmethyl) amino] ethyl}phenyl- 2-thiophene carboximidamide.

7. 发明公开

EP1732567A1 UTILISATION D'UN DERIVE DE LA PHENOTHIAZINE POUR LA PREVENTION ET/OU LE TRAITEMENT DE LA PERTE D'AUDITION 有权
标题翻译： USING A吩噻嗪衍生物用于预防和/或治疗的GERHÖRVERLUST
公开(公告)号：EP1732567A1
公开(公告)日：2006-12-20
申请号：EP05744629.6
申请日：2005-03-25
申请人： Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S) SAS
发明人： PIGNOL, Bernadette , PUEL, Jean-Luc , AUVIN, Serge , CHABRIER de LASSAUNIERE, Pierre-Etienne , WANG, Jing
IPC分类号： A61K31/5415 , A61K45/06 , A61P27/16
CPC分类号： A61K31/5415 , C09B21/00
摘要： The invention concerns the use of a phenothiazine derivative of formula (I), wherein: R represents the hydrogen atom, an alkyl radical, arylalkyl, or -C(O)R', for preparing a medicine for preventing and/or treating hearing loss.

8. 发明公开

EP0891344A1 ANTAGONISTES DU RECEPTEUR ALPHA 1-ADRENERGIQUE 失效
标题翻译：受体α-1肾上腺素能受体拮抗剂
公开(公告)号：EP0891344A1
公开(公告)日：1999-01-20
申请号：EP97919488.0
申请日：1997-04-04
申请人： SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)
发明人： BIGG, Dennis , CHARBIER de LASSAUNIERE, Pierre-Etienne , AUVIN, Serge , AUGUET, Michel
IPC分类号： C07D295 , A61K31 , A61P9 , A61P13 , A61P15 , A61P43 , C07D311
CPC分类号： C07D295/13
摘要： Phenylpiperazine derivatives having a high affinity for the α1-adrenergic receptor and pharmaceutical compositions containing same are disclosed. A method for the use of such derivatives to treat benign prostatic hyperplasia is also described.

9. 发明授权

EP1732567B1 UTILISATION D'UN DERIVE DE LA PHENOTHIAZINE POUR LA PREVENTION ET/OU LE TRAITEMENT DE LA PERTE D'AUDITION 有权
标题翻译： USING A吩噻嗪衍生物用于预防和/或治疗的GERHÖRVERLUST
公开(公告)号：EP1732567B1
公开(公告)日：2008-10-08
申请号：EP05744629.6
申请日：2005-03-25
申请人： Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S) SAS
发明人： PIGNOL, Bernadette , PUEL, Jean-Luc , AUVIN, Serge , CHABRIER de LASSAUNIERE, Pierre-Etienne , WANG, Jing
IPC分类号： A61K31/5415 , A61K45/06 , A61P27/16
CPC分类号： A61K31/5415 , C09B21/00
摘要： The invention concerns the use of a phenothiazine derivative of formula (I), wherein: R represents the hydrogen atom, an alkyl radical, arylalkyl, or -C(O)R', for preparing a medicine for preventing and/or treating hearing loss.

10. 发明授权

EP1701974B1 NOUVEAUX DERIVES DU 2-HYDROXYTETRAHYDROFURANNE ET LEUR APPLICATION A TITRE DE MEDICAMENTS 有权
标题翻译： 2 HYDROXYTETRAHYDROFURANDERIVATE及其作为药物
公开(公告)号：EP1701974B1
公开(公告)日：2008-03-26
申请号：EP04816363.8
申请日：2004-12-08
申请人： SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)
发明人： AUVIN, Serge , CHABRIER DE LASSAUNIERE, Pierre, Etienne
IPC分类号： C07K5/06 , A61K38/05
CPC分类号： C07K5/1024 , A61K38/00 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06139 , C07K5/06165 , C07K5/0821
摘要： The invention relates to 2-hydroxytetrahydrofurane derivatives having general formula (I) wherein A represents the radical (II) wherein R1, R2, R4, R5 and R6 individually represent H, a halogen atom, OH, alkyl or alkoxy, R3 represents H, alkyl or -COR1(), R10 represents H, alkyl or alkoxy, and W represents a CH2-CH2-, -CH=CH-, -0-, -S- or -NR11 bond wherein R11 represents H or alkyl; X represents CO-, -Y-CO-, -O-Y-CO- or -NR12-Y-CO-, Y represents an alkylene radical or a haloalkylene radical, R12 represents H, alkyl or -COR13, R13 represents H, alkyl, haloalkyl or alkoxy, AA represents, each time when it occurs, a natural amino acid or not; n represents 2 or 3; and R represents H, alkyle or -CO-R19, R19 represents alkyl. Said compounds inhibit calpains and / or trap reactive forms of oxygen and can be used to prepare a medicament used to treat inflammatory diseases and immunological diseases, cardiovascular diseases and cerebro-vascular diseases, disorders of the central or peripheral nervous system, osteoporosis, muscular distrophy, proliferative diseases, cataracts, rejection reactions following organ transplants and viral and auto-immune diseases.

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