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1. 发明申请

WO2007012761A8 NOVEL POLYSUBSTITUTED 1,1-PYRIDINYL AMINOCYCLOPROPANAMINE DERIVATIVES, METHOD FOR PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：新的多取代的1,1-吡啶基亚氨基环丙胺衍生物，其制备方法及含有该化合物的药物组合物
公开(公告)号：WO2007012761A8
公开(公告)日：2007-12-21
申请号：PCT/FR2006001831
申请日：2006-07-27
申请人： SERVIER LAB , GOLDSTEIN SOLO , GUILLONNEAU CLAUDE , CHARTON YVES , LOCKHART BRIAN , LESTAGE PIERRE
发明人： GOLDSTEIN SOLO , GUILLONNEAU CLAUDE , CHARTON YVES , LOCKHART BRIAN , LESTAGE PIERRE
IPC分类号： C07D213/74 , A61K31/44 , A61P25/00
CPC分类号： C07D213/74
摘要： The invention concerns compounds of formula (I), wherein: n represents an integer between 1 and 6 inclusively; R 1 and R 2 represent a hydrogen atom a (C 1 -C 6 ) alkyl or (C 1 -C 6 ) arylalkyl group; R 3 and R 4 represent a hydrogen atom, a (C 1 -C 6 ) alkyl group; R 5 and R 6 represent a hydrogen atom, a (C 1 -C 6 ) alkyl group, halogen, hydroxy, (C 1 -C 6 ) alkoxy, cyano, nitro, (C 2 -C 6 ) acyl, (C 1 -C 6 ) alkoxycarbonyl, (C 1 -C 6 ) trihalogenoalkyl, (C 1 -C 6 ) trihalogenoalkoxy or amino optionally substituted; R 7 represents a hydrogen atom, a (C 1 -C 6 ) alkyl group or arylalkyl. The invention is useful for preparing medicines.
摘要翻译：本发明涉及式（I）的化合物，其中：n表示1至6的整数; R 1和R 2代表氢原子a（C 1 -C 6）烷基或（C 1 -C 6烷基） 1〜6）芳基烷基; R 3和R 4代表氢原子，（C 1 -C 6）烷基;并且R 4代表氢原子，（C 1 -C 6） R 5和R 6代表氢原子，（C 1 -C 6）6烷基，卤素，羟基，（C 1 -C 6）烷氧基，氰基，硝基，（C≡C2 -C 6））酰基，（C 1 -C 6）烷氧基羰基，（C 1 -C 6）亚烷基，（（C 1 -C 6） C1-C6）任选取代的三卤代烷氧基或氨基; R 7代表氢原子，（C 1 -C 6）烷基或芳基烷基。本发明对于制备药物是有用的。

2. 发明专利

JP2002069046A NEW 1,1- AND 1,2-DISUBSTITUTED CYCLOPROPANE COMPOUND, METHOD FOR PRODUCING THE SAME AND MEDICINAL COMPOSITION CONTAINING THE SAME 审中-公开
公开(公告)号：JP2002069046A
公开(公告)日：2002-03-08
申请号：JP2001191541
申请日：2001-06-25
申请人： SERVIER LAB
发明人： GOLDSTEIN SOLO , GUILLONNEAU CLAUDE , CHARTON YVES , LOCKHART BRIAN , LESTAGE PIERRE
IPC分类号： C07D295/08 , A61K31/10 , A61K31/13 , A61K31/133 , A61K31/15 , A61K31/16 , A61K31/215 , A61K31/22 , A61K31/221 , A61K31/223 , A61K31/27 , A61K31/40 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/445 , A61K31/455 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/28 , A61P25/34 , A61P29/00 , A61P29/02 , A61P43/00 , C07C62/02 , C07C209/00 , C07C211/37 , C07C213/00 , C07C213/02 , C07C213/06 , C07C215/20 , C07C215/42 , C07C217/44 , C07C217/52 , C07C219/18 , C07C219/20 , C07C219/24 , C07C269/00 , C07C269/02 , C07C271/12 , C07C271/22 , C07C271/24 , C07C271/34 , C07C319/14 , C07C321/28 , C07C323/26 , C07C323/33 , C07D213/30 , C07D213/38 , C07D213/53 , C07D213/65 , C07D213/70 , C07D213/80 , C07D213/803 , C07D295/096 , C07D417/12
摘要： PROBLEM TO BE SOLVED: To provide a new 1,1- and 1,2-disubstituted cyclopropane compound having specific interaction with central nicotinic receptors of type α4β2. SOLUTION: This compound is represented by formula (1), and concretely exemplified by 2-[1-(dimethylamino)cyclopropyl] ethylmethylcarbamate. The compound is useful for treatment of deficiencies of memory associated with cerebral ageing and neurodegenerative diseases.

3. 发明专利

CY1108529T1 ΝΕΑ ΑΖΑΔΙΚΥΚΛΙΚΑ ΠΑΡΑΓΩΓΑ, ΜΕΘΟΔΟΣ ΠΑΡΑΣΚΕΥΗΣ ΤΟΥΣ ΚΑΙ ΦΑΡΜΑΚΕΥΤΙΚΕΣ ΣΥΝΘΕΣΕΙΣ ΠΟΥ ΤΑ ΠΕΡΙΕΧΟΥΝ 未知
公开(公告)号：CY1108529T1
公开(公告)日：2014-04-09
申请号：CY081100520
申请日：2008-05-20
申请人： SERVIER LAB
发明人： CASARA PATRICK , CHOLLET ANNE-MARIE , DHAINAUT ALAIN , BERT LIONEL , LESTAGE PIERRE , LOCKHART BRIAN
IPC分类号： A61K31/403 , A61P25/00 , C07D209/52 , C07D403/12
摘要： Ηεφεύρεσησχετίζεταιμεενώσειςπουέχουντονγενικότύπο (Ι): ταεναντιομερήκαιδιαστερεοϊσομερήτουςκαθώςκαιταάλατατουςπροσθήκηςμεέναή περισσότεραφαρμακευτικώςαποδεκτάοξέαή βάσεις. Οιενώσειςτηςπαρούσηςεφεύρεσηςείναιιδιαιτέρουενδιαφέροντοςγιατηναλληλεπρίδρασητουςμετακεντρικάισταμινεργικάσυστήματα.

4. 发明专利

EA015227B1 ЗАМЕЩЕННЫЕ СОЕДИНЕНИЯ ПИРИДИНИЛАМИНОАЛКИЛЕН- И ПИРИДИНИЛОКСИАЛКИЛЕНЦИКЛОПРОПАНАМИНА, СПОСОБ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ ИХ 未知
公开(公告)号：EA015227B1
公开(公告)日：2011-06-30
申请号：EA200801681
申请日：2007-01-30
申请人： SERVIER LAB
发明人： GOLDSTEIN SOLO , GUILLONNEAU CLAUDE , CHARTON YVES , LOCKHART BRIAN , LESTAGE PIERRE
IPC分类号： C07D213/65 , A61K31/4418 , A61P25/00 , C07D401/10
摘要： Изобретениеотноситсяк соединениямформулы (I)вкоторой n представляетсобойцелоечислоот 1 до 6 включительно, X представляетсобойатомкислородаилигруппу NR, Y представляетсобойатомуглеродаилиатомазота, Z представляетсобойатомуглеродаилиатомазота, Rи Rпредставляютсобойатомводородаилиалкильнуюилиарилалкильнуюгруппу, Rи Rпредставляютсобойатомводородаилиалкильнуюгруппу, Rпредставляетсобойатомводородаилиалкил, галоген, гидрокси, алкокси, циано, нитро, ацил, алкоксикарбонил, тригалоалкил, тригалоалкоксиилинеобязательнозамещеннуюаминогруппу, Rпредставляетсобойатомводородаилиалкильнуюилиарилалкильнуюгруппу, Ra, Rb, Rc, Rd и Re имеютзначения, указанныев описании, атакжек способуихполученияи фармацевтическимкомпозициям, содержащимих.

5. 发明专利

RS51065B NOVA JEDINJENJA PIRIDINILAMINOALKILEN- I PIRIDINILOKSIALKILEN-CIKLOPROPANAMINA, POSTUPAK NJIHOVE PROIZVODNJE I FARMACEUTSKE SMEŠE KOJE IH SADRŽE 未知
公开(公告)号：RS51065B
公开(公告)日：2010-10-31
申请号：RSP20090450
申请日：2007-01-30
申请人： SERVIER LAB
发明人： LESTAGE PIERRE , GOLDSTEIN SOLO , GUILLONNEAU CLAUDE , CHARTON YVES , LOCKHART BRIAN
IPC分类号： C07D213/65 , A61K31/4418 , A61P25/00 , C07D401/10

6. 发明专利

GEP20105090B NOVEL PYRIDINYLAMINO ALKYLENE- AND PYRIDINYLOXYALKYLENE-CYCLOPROPANAMINES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知
公开(公告)号：GEP20105090B
公开(公告)日：2010-10-11
申请号：GEAP2007010875
申请日：2007-01-30
申请人： SERVIER LAB
发明人： GOLDSTEIN SOLO , GUILLONNEAU CLAUDE , CHARTON YVES , LOCKHART BRIAN , LESTAGE PIERRE
IPC分类号： C07D213/65 , A61K31/4418 , A61P25/00 , C07D401/10
摘要： Compounds of formula in which R1, R2, R3, R4, R5, Ra, Rb, Rc, Rd, Re, X, Y and Z are provided in the description, method for its production, pharmaceutical compositions on its base and use thereof as receptors of α4ß2 specific nicotinic ligands, for treatment of abnormalities of memory and neurodegenerative diseases related to cerebral senility. Tables: 1

7. 发明专利

AT437857T 未知
公开(公告)号：AT437857T
公开(公告)日：2009-08-15
申请号：AT07730888
申请日：2007-01-30
申请人： SERVIER LAB
发明人： GOLDSTEIN SOLO , GUILLONNEAU CLAUDE , CHARTON YVES , LOCKHART BRIAN , LESTAGE PIERRE
IPC分类号： C07D213/65 , A61K31/4418 , A61P25/00 , C07D401/10
摘要： Compounds of formula (I): wherein: n represents an integer of from 1 to 6 inclusive, X represents an oxygen atom or an NR6 group, Y represents a carbon atom or a nitrogen atom, Z represents a carbon atom or a nitrogen atom, R1 and R2 represent a hydrogen atom or an alkyl or arylalkyl group, R3 and R4 represent a hydrogen atom or an alkyl group, R5 represents a hydrogen atom or an alkyl, halogen, hydroxy, alkoxy, cyano, nitro, acyl, alkoxycarbonyl, trihaloalkyl, trihaloalkoxy or optionally substituted amino group, R6 represents a hydrogen atom or an alkyl or arylalkyl group, Ra, Rb, Rc, Rd and Re are as defined in the description. Medicinal products containing the same which are useful as specific nicotinic ligands of α4&bgr;2 receptors.

8. 发明专利

ES2313589T3 DERIVADOS 1,1-PIRIDINILOXICICLOPROPANOAMINAS POLISUSTITUIDOS, SU PROCEDIMIENTO DE PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN. 未知
公开(公告)号：ES2313589T3
公开(公告)日：2009-03-01
申请号：ES06291219
申请日：2006-07-27
申请人： SERVIER LAB
发明人： GOLDSTEIN SOLO , GUILLONNEAU CLAUDE , CHARTON YVES , LOCKHART BRIAN , LESTAGE PIERRE
IPC分类号： A61K31/44 , C07D213/65 , A61P25/16 , A61P25/26 , A61P25/28 , A61P25/30
摘要： Compuestos de fórmula (I): (Ver fórmula) donde: n representa un número entero comprendido entre 1 y 6, ambos inclusive, R1 y R2, idénticos o diferentes, independientemente uno del otro, representan un átomo de hidrógeno o un grupo alquilo(C1-C6) lineal o ramificado o arilalquilo (C1-C6) lineal o ramificado, R3 y R4, idénticos o diferentes, independientemente uno del otro, representan un átomo de hidrógeno o un grupo alquilo(C1-C6) lineal o ramificado, entendiéndose que al menos uno de los dos grupos R3 ó R4 representa un grupo alquilo(C1-C6) lineal o ramificado, R5 y R6, idénticos o diferentes, independientemente uno del otro, representan un átomo de hidrógeno o un grupo alquilo(C1-C6) lineal o ramificado, un halógeno, hidroxilo, alcoxi(C1-C6) lineal o ramificado, ciano, nitro, acilo(C2-C6) lineal o ramificado, alcoxicarbonilo(C1-C6) lineal o ramificado, trihaloalquilo(C1-C6) lineal o ramificado, trihaloalcoxi( C1-C6) lineal o ramificado o amino, eventualmente sustituido con uno o dos grupos alquilo(C1-C6) lineales o ramificados, por grupo arilo se entiende un grupo fenilo, bifenilo, naftilo, dihidronaftilo, tetrahidronaftilo, indanilo e indenilo, estando cada uno de estos grupos eventualmente sustituido con uno o varios grupos, idénticos o diferentes, seleccionados de entre halógeno, alquilo(C1-C6) lineal o ramificado, hidroxilo, ciano, nitro, alcoxi(C1-C6) lineal o ramificado, acilo(C2-C7) lineal o ramificado, alcoxicarbonilo(C1-C6) lineal o ramificado, trihaloalquilo(C1-C6) lineal o ramificado, trihaloalcoxi(C1-C6) lineal o ramificado y amino, eventualmente sustituido con uno o dos grupos alquilo(C1-C6) lineales o ramificados, sus enantiómeros, diastereoisómeros, así como sus sales de adición de un ácido o de una base farmacéuticamente aceptables.

9. 发明专利

SI1748043T1 POLISUBSTITUIRANE SPOJINE 1,1-PIRIDINILOKSICIKLOPROPANAMINOV, POSTOPEK ZA NJIHOVO PRIPRAVO IN FARMACEVTSKI SESTAVKI, KI JIH VSEBUJEJO 未知
公开(公告)号：SI1748043T1
公开(公告)日：2008-12-31
申请号：SI200630083
申请日：2006-07-27
申请人： SERVIER LAB
发明人： GOLDSTEIN SOLO , GUILLONNEAU CLAUDE , CHARTON YVES , LOCKHART BRIAN , LESTAGE PIERRE
IPC分类号： C07D213/00 , A61K31/00 , A61P25/00

10. 发明专利

HRP20080184T5 NOVEL AZABICYCLIC DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 未知
公开(公告)号：HRP20080184T5
公开(公告)日：2008-10-31
申请号：HRP20080184
申请日：2008-04-22
申请人： SERVIER LAB
发明人： CASARA PATRICK , CHOLLET ANNE-MARIE , DHAINAUT ALAIN , BERT LIONEL , LESTAGE PIERRE , LOCKHART BRIAN
IPC分类号： A61K31/403 , A61P25/00 , C07D209/52 , C07D403/12
摘要： Azabicyclic derivatives (I) are new. Azabicyclic derivatives of formula (I) and their enantiomers, diastereoisomers or acid or base addition salts are new. ALK : alkylene, 2-6C alkenylene (contains 1-3 double bonds) or 2-6C alkynylene (contains 1-3 triple bonds); Y, Y 1> : H, halo, alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, SH, OH, perhaloalkyl, nitro, amino (optionally substituted by one or two alkyl), acyl of formula C(O)R1a, aminocarbonyl (optionally N-substituted by one or two alkyl), acylamino (optionally N-substituted by alkyl), alkoxycarbonyl, COOH, sulfo or CN; R1a : H or alkyl; X : O, S or NR; R : H or alkyl; W 1> : CN (only when X = O or NR), N(R 1>)Z 1>R 2>or Z 1>NR 1>R 2>; Z 1> : C(O), C(S), C(NR 4>), C(O)N(R 3>), C(S)N(R 3>), C(NR 4>)N(R 3>), C(O)O, C(S)O or S(O) r; r : 1 or 2; Z 2> : C(O), C(S), C(NR 4>), S(O) ror bond; R 1>-R 4> : alkyl, 3-6C alkenyl (contains 1-3 double bonds), 3-6C alkynyl (contains 1-3 triple bonds), cycloalkyl, heterocycloalkyl, aryl or heteroaryl (all optionally substituted), alkoxy or H; or R 1>+R 2>or R 2>+R 3> : heterocyclyl or heteroaryl (both optionally substituted); m, n : 0-2, where the sum of m+n is 2 or 3; and p, q : 0-2. alkyl = 1-6C unless specified; perhaloalkyl = 1-3C with 1-7 halogen; aryl = phenyl, naphthyl, indanyl, indenyl, dihydronaphthyl or tetrahydronaphthyl; cycloalkyl = 3-11 membered mono- or bi-cyclic ring system, optionally with 1 or 2 unsaturations; heterocyclyl = 4-11 membered mono- or bicyclic ring system optionally with 1 or 2 unsaturations and/or 1-4 heteroatoms from N, O and/or S; heteroaryl = 5-11 membered mono- or bicyclic ring system with 1-4 heteroatoms from N, O and/or S; for cycloalkyl, aryl, heteroaryl or heterocyclyl, 'optionally substituted' comprises 1-3 substituents from alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, halogen, OH, SH, perhaloalkyl, nitro, amino or aminocarbonyl (optionally substituted by 1 or 2 alkyl), C(O)R1a, NHC(O)R1a (optionally N-substituted by alkyl), alkoxycarbonyl, COOH, sulfo or CN; or aryl, heteroaryl, cycloalkyl, heterocyclyl or benzyl with one or two optional oxo substituents where possible; for alkyl, alkenyl or alkynyl, 'optionally substituted ' comprises one or two of alkylthio, alkylsulfinyl, alkylsulfonyl, alkoxy, halogen, OH, SH, nitro, amino, C(O)R1a, aminocarbonyl, NHC(O)R1a, alkoxycarbonyl, COOH, sulfo, CN or aryl, heteroaryl, cycloalkyl, heterocylyl or aryloxy (all optionally substituted). An independent claim is included for the preparation of (I). [Image] ACTIVITY : Nootropic; Neuroprotective; Anticonvulsant; Tranquilizer; Anorectic; Analgesic. MECHANISM OF ACTION : Histamine (H3) activator. The ability of (I) to activate histamine was tested in mice. The results showed that 4-(3-hexahydrocyclopenta[c]-pyrrol-2(1H)-ylpropoxy)benzonitrile oxalate exhibited the percentage increase of N-methylhistamine in brain of 92%.

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