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1. 发明申请

WO2007006922A8 NOVEL 1H-INDOLE-PYRIDINECARBOXAMIDE DERIVATIVES AND 1H-INDOLE-PIPERIDINECARBOXAMIDE AND THEIR USE AS HYDROXYLASE TYROSINE INDUCERS 审中-公开
标题翻译：新型1H-吲哚基吡啶甲酰胺衍生物和1H-吲哚 - 哌啶甲酰胺及其作为羟基酶诱导剂的用途
公开(公告)号：WO2007006922A8
公开(公告)日：2008-01-10
申请号：PCT/FR2006001610
申请日：2006-07-06
申请人： SERVIER LAB , CENTRE NAT RECH SCIENT , UNIV PARIS SUD , BRION JEAN-DANIEL , BINTEIN FABRICE , RAZET RODOLPHE , RAZON PATRICK , RENKO ZAFIARISOA DOLOR , LEVOIRIER ERIC , PUJOL JEAN-FRANCOIS , WEISSMANN DINAH , LE RIDANT ALAIN , HARPEY CATHERINE
发明人： BRION JEAN-DANIEL , BINTEIN FABRICE , RAZET RODOLPHE , RAZON PATRICK , RENKO ZAFIARISOA DOLOR , LEVOIRIER ERIC , PUJOL JEAN-FRANCOIS , WEISSMANN DINAH , LE RIDANT ALAIN , HARPEY CATHERINE
IPC分类号： A61K31/4439 , A61K31/454 , A61P25/00 , C07D401/12
CPC分类号： C07D401/12
摘要： The invention relates to compounds of formula (I), to their enantiomers, diastereoisomers, N-oxides, as well as to their pharmaceutically acceptable acid or base addition salts. The inventive compounds are hydroxylase tyrosine inducers.
摘要翻译：本发明涉及式（I）化合物，其对映异构体，非对映异构体，N-氧化物，及其药学上可接受的酸或碱加成盐。本发明化合物是羟化酶酪氨酸诱导剂。

2. 发明申请

WO2007006922A3 NOVEL 1H-INDOLE-PYRIDINECARBOXAMIDE DERIVATIVES AND 1H-INDOLE-PIPERIDINECARBOXAMIDE AND THEIR USE AS HYDROXYLASE TYROSINE INDUCERS 审中-公开
标题翻译：新型1H-吲哚基吡啶甲酰胺衍生物和1H-吲哚 - 哌啶甲酰胺及其作为羟基酶诱导剂的用途
公开(公告)号：WO2007006922A3
公开(公告)日：2007-04-05
申请号：PCT/FR2006001610
申请日：2006-07-06
申请人： SERVIER LAB , CENTRE NAT RECH SCIENT , UNIV PARIS SUD , BRION JEAN-DANIEL , BINTEIN FABRICE , RAZET RODOLPHE , RAZON PATRICK , RENKO ZAFIARISOA DOLOR , LEVOIRIER ERIC , PUJOL JEAN-FRANCOIS , WEISSMAN DINAH , LE RIDANT ALAIN , HARPEY CATHERINE
发明人： BRION JEAN-DANIEL , BINTEIN FABRICE , RAZET RODOLPHE , RAZON PATRICK , RENKO ZAFIARISOA DOLOR , LEVOIRIER ERIC , PUJOL JEAN-FRANCOIS , WEISSMAN DINAH , LE RIDANT ALAIN , HARPEY CATHERINE
IPC分类号： A61K31/4439 , A61K31/454 , A61P25/00 , C07D401/12
CPC分类号： C07D401/12
摘要： The invention relates to compounds of formula (I), to their enantiomers, diastereoisomers, N-oxides, as well as to their pharmaceutically acceptable acid or base addition salts. The inventive compounds are hydroxylase tyrosine inducers.
摘要翻译：本发明涉及式（I）化合物，其对映异构体，非对映异构体，N-氧化物及其药学上可接受的酸或碱加成盐。本发明化合物是羟化酶酪氨酸诱导剂。

3. 发明申请

WO2008099081A3 NOVEL TRIAZABENZO[?]NAPHTHO[2,L,8-CDE]AZULENE DERIVATIVES, METHOD FOR PREPARING THE SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME 审中-公开
标题翻译：新型三唑并[α]萘基[2，L，8-CDE]亚苄基衍生物，其制备方法和含有该衍生物的药物组合物
公开(公告)号：WO2008099081A3
公开(公告)日：2008-10-23
申请号：PCT/FR2008000012
申请日：2008-01-04
申请人： SERVIER LAB , CENTRE NAT RECH SCIENT , UNIV PARIS SUD , BRION JEAN-DANIEL , HERVE MAUD , MOREAU ANNE , RENKO ZAFIARISOA DOLOR , LE RIDANT ALAIN , HARPEY CATHERINE
发明人： BRION JEAN-DANIEL , HERVE MAUD , MOREAU ANNE , RENKO ZAFIARISOA DOLOR , LE RIDANT ALAIN , HARPEY CATHERINE
IPC分类号： C07D471/22 , A61K31/551 , A61P25/00
CPC分类号： C07D471/22
摘要： The invention relates to compounds of formula (I), to their enantiomers, diastereoisomers, and N-oxides, as well as to their addition salts to a pharmaceutically acceptable acid or base. The compounds according to the invention are powerful tyrosine hydroxylase inducers.
摘要翻译：本发明涉及式（I）化合物，其对映异构体，非对映异构体和N-氧化物，以及它们与药学上可接受的酸或碱的加成盐。根据本发明的化合物是强大的酪氨酸羟化酶诱导剂。

4. 发明申请

WO2008099083A3 USE OF NEUROPROTECTIVE COMPOUNDS FOR OBTAINING DRUGS FOR TREATING NEURODEGENERATIVE DISEASES 审中-公开
标题翻译：神经保护性化合物用于获得治疗神经退行性疾病的药物的用途
公开(公告)号：WO2008099083A3
公开(公告)日：2008-12-11
申请号：PCT/FR2008000014
申请日：2008-01-04
申请人： SERVIER LAB , LE RIDANT ALAIN , HARPEY CATHERINE
发明人： LE RIDANT ALAIN , HARPEY CATHERINE
IPC分类号： A61K31/437 , A61K31/4439 , A61K31/553 , A61P25/00 , C07D401/12 , C07D487/06
CPC分类号： C07D487/06 , C07D401/12
摘要： The invention relates to the use of neuroprotective compounds for obtaining drugs for the curative treatment of neurodegenerative diseases and/or for preventing the occurrence of problems resulting from said diseases.
摘要翻译：本发明涉及神经保护性化合物用于获得用于治疗性治疗神经变性疾病和/或用于预防由所述疾病引起的问题的发生的药物的用途。

5. 发明专利

AR070070A1 DERIVADOS DE 1H-INDOL-1-IL-UREA, PROCEDIMIENTO DE PREPARACION, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y USOS DE LOS MISMOS EN EL TRATAMIENTO DE TRASTORNOS ASOCIADOS AL SNC. 未知
公开(公告)号：AR070070A1
公开(公告)日：2010-03-10
申请号：ARP080105775
申请日：2008-12-30
申请人： CENTRE NAT RECH SCIENT , SERVIER LAB , UNIV PARIS SUD
发明人： DEYINE ABDALLAH , LE RIDANT ALAIN , HARPEY CATHERINE , BRION JEAN-DANIEL
IPC分类号： C07D209/08 , C07D209/30 , C07D211/56 , C07D213/75 , C07D215/06 , C07D401/12 , C07D403/12 , A61K31/404 , A61K31/4406 , A61K31/4462 , A61K31/4709 , A61P25/24 , A61P25/22 , A61P25/16 , A61P25/28
摘要： Reivindicacion 1: Compuestos de formula (1): en la que R1 y R2, idénticos o diferentes, representan un átomo de hidrogeno o un grupo alquilo C1-6 lineal o ramificado, R3 representa un átomo de hidrogeno o de halogeno, un grupo alquilo C1-6 lineal o ramificado, o un grupo alcoxi C1-6 lineal o ramificado, Het representa un grupo piridilo, pirimidilo, piperidilo, 2-metilpiridilo, 3-metilpiridilo, 4-metilpiridilo, fenilo, bencilo, quinolinilo, piridacinilo o indolilo, sustituidos opcionalmente con uno o varios grupos elegidos entre halogeno, alquilo C1-6 lineal o ramificado, alcoxi C1-6 lineal o ramificado, ------------ representa un enlace sencillo o un enlace doble, entendiéndose que R3 puede estar incorporado en cualquiera de los carbonos del nucleo indol/indolina que lo permita, sus enantiomeros y diastereoisomeros así como sus sales de adicion a un ácido o a una base aceptable farmacéuticamente.

6. 发明专利

AU2006268527B2 Novel 1H-indole-pyridinecarboxamide and 1H-indole-piperidinecarboxamide derivatives and their use as hydroxylase tyrosine inducers 未知
公开(公告)号：AU2006268527B2
公开(公告)日：2009-12-24
申请号：AU2006268527
申请日：2006-07-06
申请人： CENTRE NAT RECH SCIENT , SERVIER LAB , UNIV PARIS SUD
发明人： PUJOL JEAN-FRANCOIS , WEISSMAN DINAH , BRION JEAN-DANIEL , RENKO ZAFIARISOA DOLOR , RAZET RODOLPHE , HARPEY CATHERINE , LEVOIRIER ERIC , RAZON PATRICK , BINTEIN FABRICE , RIDANT ALAIN LE
IPC分类号： A61K31/4439 , A61K31/454 , A61P25/00 , C07D401/12
摘要： Compounds of formula (I): wherein: A represents a divalent radical: wherein: Z represents an oxygen atom or a sulphur atom, R6 represents a hydrogen atom, an alkyl, alkenyl, arylalkyl or polyhaloalkyl group or a substituted, linear or branched alkyl chain, represents a single bond or a double bond, R1, R2, R3 and R4 represent a hydrogen or halogen atom, an alkyl, alkoxy, hydroxy, cyano, nitro, polyhaloalkyl or optionally substituted amino group, or a linear or branched alkyl chain substituted by one or more groups, R5 represents a hydrogen atom or an alkyl, aminoalkyl or hydroxyalkyl group, X and Y represent a hydrogen atom or an alkyl group, Ra, Rb, Rc and Rd represent a hydrogen or halogen atom, an alkyl, hydroxy, alkoxy, cyano, nitro, polyhaloalkyl, optionally substituted amino group, or a substituted, linear or branched alkyl chain, Re represents a hydrogen atom or an alkyl, arylalkyl or alkenyl group or a substituted, linear or branched alkyl chain, their enantiomers, diastereoisomers, and N-oxides, and also addition salts thereof with a pharmaceutically acceptable acid or base.

7. 发明专利

AR064747A1 DERIVADOS DE TRIAZABENZO[(ALFA)]NAFTO[2,1,8-CDE]AZULENO SU PORCEDIMIENTO DE PREPARACION Y LAS COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN 未知
公开(公告)号：AR064747A1
公开(公告)日：2009-04-22
申请号：ARP080100029
申请日：2008-01-04
申请人： SERVIER LAB , UNIV PARIS SUD , CENTRE NAT RECH SCIENT
发明人： HERVET MAUD , MOREAU ANNE , RENKO ZAFIARISOA DOLOR , LE RIDANT ALAIN , HARPEY CATHERINE , BRION JEAN-DANIEL
IPC分类号： C07D471/22 , C07D487/12 , A61K31/551 , A61P25/00
摘要： Reivindicacion 1: Compuesto de formula (1), en la que R1 representa un átomo de hidrogeno o un grupo alquilo C1-6 lineal o ramificado, aminoalquilo C1-6 lineal o ramificado, o hidroxialquilo C1-6 lineal o ramificado, R2 representa un átomo de hidrogeno, o R1 y R2 junto con los átomos de carbono a los que están unidos forman un enlace carbono-carbono, R3 representa un átomo de hidrogeno, R4 representa un átomo de hidrogeno o un grupo metilo o alquilo C3-6 lineal o ramificado, aminoalquilo C1-6 lineal o ramificado, hidroxialquilo C1-6 lineal o ramificado, arilalquilo C1-6 lineal o ramificado, heterocicloalquilalquilo C1-6 lineal o ramificado, o R3 y R4 junto con los átomos de carbono a los que están unidos forman un enlace carbono- carbono, R5, R6, R7, R8, idénticos o diferentes, independientemente el uno del otro, representan un átomo de hidrogeno, o dos sustituyentes geminados (R5 y R6 y/o R7 y R8) forman un grupo oxo, tioxo o imino, R9 representa un átomo de hidrogeno o de halogeno o un grupo alquilo C1-6 lineal o ramificado sustituido opcionalmente, alcoxi C1-6 lineal o ramificado, hidroxi, ciano, nitro, polihalogenoalquilo C1-6 lineal o ramificado, amino (sustituido opcionalmente con uno o dos alquilo C1-6 lineal o ramificado, alquenilo C2-6 lineal o ramificado, pudiendo ser alquilo y alquenilo idénticos o diferentes), R10, R11, idénticos o diferentes, independientemente el uno del otro, representan un átomo de hidrogeno o de halogeno o un grupo alquilo C1-6 lineal o ramificado, alcoxi C1-6 lineal o ramificado, hidroxi, ciano, nitro, polihalogenoalquilo C1-6 lineal o ramificado, amino (sustituido opcionalmente con uno o dos alquilo C1-6 lineal o ramificado, alquenilo C2-6 lineal o ramificado, pudiendo ser alquilo y alquenilo idénticos o diferentes), n representa un numero entero comprendido entre 0 y 4 (0, 1, 2, 3, 4), m representa un numero entero comprendido entre 0 y 2 (0, 1, 2), p representa un numero entero comprendido entre 0 y 3 (0, 1, 2, 3), X representa un grupo NR12, R12 representa un átomo de hidrogeno o un grupo alquilo C1-6 lineal o ramificado sustituido opcionalmente, alquenilo C2-6 lineal o ramificado sustituido opcionalmente, arilalquilo C1-6 lineal o ramificado, polihalogenoalquilo C1-6 lineal o ramificado, sus enantiomeros, diastereoisomeros, N-oxidos, así como sus sales de adicion a un ácido o a una base aceptable farmacéuticamente, entendiéndose que: por arilalquilo, se entiende el grupo arilo-alquilo en el que el grupo alquilo designa una cadena de 1 a 6 átomos de carbono, lineal o ramificado y el grupo arilo designa un grupo fenilo o naftilo sustituido opcionalmente, la expresion ôsustituido opcionalmenteö cuando se refiere a los grupos alquilo C1- 6 lineal, ramificado o alquenilo C2-6 lineal o ramificado o arilalquilo significa que estos grupos pueden estar sustituidos con uno o varios átomos de halogeno, uno o varios grupos hidroxi, alcoxi C1-6 lineal o ramificado o amino sustituido opcionalmente con uno o dos grupos, idénticos o diferentes, alquilo C1-6 lineal o ramificado, por a, b, c y d se entiende los centros quirales presentes opcionalmente en los compuestos de formula (1).

8. 发明专利

CA2674097A1 NOUVEAUX DERIVES AMINOPYRROLO[1,2-A]INDOLE ET AMINOPYRIDAZINO[1,6-A]INDOLE, LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT 未知
公开(公告)号：CA2674097A1
公开(公告)日：2008-08-21
申请号：CA2674097
申请日：2008-01-04
申请人： CENTRE NAT RECH SCIENT , UNIV PARIS SUD , SERVIER LAB
发明人： GALTIER CHRISTOPHE , LE RIDANT ALAIN , HARPEY CATHERINE , RENKO ZAFIARISOA DOLOR , HERVET MAUD , LE STRAT FREDERIC , MOREAU ANNE , BRION JEAN-DANIEL
IPC分类号： C07D471/04 , A61K31/4375 , A61K31/5025 , A61P25/22 , A61P25/24 , C07D471/14 , C07D471/16
摘要： L'invention concerne les composés de formule (I); Formule (I) leurs énant iomères, diastcréoisomcres, N-oxydes, ainsi que leurs sels d'addition à un a cide ou à une base pharmaceutiquement acceptable. Les composés de formule (I ) sont des inducteurs de tyrosine hydroxylase.

10. 发明专利

AT466863T 未知
公开(公告)号：AT466863T
公开(公告)日：2010-05-15
申请号：AT08761737
申请日：2008-01-04
申请人： SERVIER LAB , CENTRE NAT RECH SCIENT , UNIV PARIS SUD
发明人： BRION JEAN-DANIEL , GALTIER CHRISTOPHE , HERVET MAUD , LE STRAT FREDERIC , MOREAU ANNE , RENKO ZAFIARISOA , LE RIDANT ALAIN , HARPEY CATHERINE
IPC分类号： C07D471/04 , A61K31/4375 , A61K31/5025 , A61P25/22 , A61P25/24 , C07D471/14 , C07D471/16
摘要： Amino-pyrrolo(1,2-a)indole and amino-pyridazino(1,6-a)indole derivatives (I) are new. Fused indole derivatives of formula (I) (including enantiomers and diastereomers) and their N-oxides and acid or base addition salts are new. X : CO or -N(R 10)-CO- (bonded to N at the left-hand terminal); R 1H, alkyl, aminoalkyl, hydroxyalkyl or arylalkyl; R 2 - R 4H, alkyl, aminoalkyl or hydroxyalkyl; or R 1 + R 2 or R 3 + R 4additional C-C bond; R 5, R 6H or alkyl; R 7, R 8H; or alkyl, alkenyl or alkynyl (all optionally substituted (os) by one or more of OH, CN, alkoxy and NR 13R 14); or R 5 + R 8 or R 7 + R 8group completing a 5-7 membered heterocycle (os by R 11), provided that at least one heterocycle-completing group as R 5 + R 8 or R 7 + R 8 must be present; R 9H, halo, alkyl (os by one or more of halo, OH, alkoxy or NR 15R 16), alkoxy, OH, CN, NO 2, polyhaloalkyl or NR 15R 16; n : 0-4; R 10H, alkyl (os by one or more of halo, OH, alkoxy or NR 15R 16), alkenyl, arylalkyl or polyhaloalkyl; R 11COOT or CH 2OU'; T, U' : H or alkyl; R 13, R 14H or alkyl; or NR 13R 14os 4-8 membered heterocycle, optionally containing a double bond or a second O or N heteroatom; R 15, R 16H, alkyl or alkenyl; aryl moieties : phenyl or naphthyl (both os by one or more of halo, NO 2, NH 2, alkyl or alkoxy); 5-7 membered heterocycle : e.g. pyrrolidine, piperidine or azepane; 4-8 membered heterocycle : e.g. pyrrolidine, piperidine, azepane, piperazine or morpholine (all os by one or more of alkyl, hydroxyalkyl, alkoxyalkyl, aminoalkyl or mono- or dialkylaminoalkyl; alkyl moieties have 1-6C and alkenyl or alkynyl moieties 2-6C; the compound (3aSR,RSR)-3-benzyl-4-ethyl-2,3,3a,4-tetrahydro-benzo(b)pyrido(2,3,4-gh)pyrrolizin-5(1H)-one is excluded. Independent claims are included for the preparation of (I). [Image] ACTIVITY : Tranquilizer; Antidepressant; Nootropic; Neuroprotective; Antiparkinsonian. MECHANISM OF ACTION : Tyrosine hydroxylase (TH) inducer. (4aSR,11aSR,11bRS)-1-Methyl-1,2,3,4,4a,11,11a,11b-octahydro-pyrido(2',3':3,4)pyrrolo(1,2-a)indol-5-one (Ia) induced an increase in the TH levels in the locus coeruleus of the brain in mice after intravenous injection at a dose of 20 mg/kg.

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