公开(公告)号：JP2002069046A

公开(公告)日：2002-03-08

申请号：JP2001191541

申请日：2001-06-25

Applicant: SERVIER LAB

Inventor： GOLDSTEIN SOLO ,  GUILLONNEAU CLAUDE ,  CHARTON YVES ,  LOCKHART BRIAN ,  LESTAGE PIERRE

IPC: 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

Abstract: 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.

公开(公告)号：JP2002265469A

公开(公告)日：2002-09-18

申请号：JP2002065233

申请日：2002-03-11

Applicant: SERVIER LAB

Inventor： WIERZBICKI MICHEL ,  BOUSSARD MARIE FRANCOISE ,  ROUSSEAU ANNE ,  BOUTIN JEAN-ALBERT ,  DELAGRANGE PHILIPPE

IPC: C07D487/06 ,  A61K31/407 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P15/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04

Abstract: PROBLEM TO BE SOLVED: To provide a medicine which contains a compound having high affinity with a melatonin receptor and is useful for treating diseases related to the melatonin operation system. SOLUTION: The compound represented by the formula (R1 , R2 , R3 , R4 , R5 , R6 , and R8 are each H or the like, R7 is H or the like, or one of R1 to R8 forms a 1 to 2C alkylenedioxy together with another adjacent one of R1 to R8 ), its optically isomer (when the optical isomer exists), and its pharmacologically acceptable acid or base adduct; a process for preparing the same; and a pharmaceutical composition containing the same.

公开(公告)号：JP2003113156A

公开(公告)日：2003-04-18

申请号：JP2002203408

申请日：2002-07-12

Applicant: SERVIER LAB

Inventor： LAVIELLE GILBERT ,  DUBUFFET THIERRY ,  CIMETIERE BERNARD ,  VERBEUREN TONY ,  SIMONET SERGE ,  VAYSSETTES-COURCHAY CHRISTINE

IPC: C07D295/08 ,  A61K31/18 ,  A61K31/195 ,  A61K31/40 ,  A61K31/445 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  A61K31/535 ,  A61K31/5375 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P25/06 ,  C07B53/00 ,  C07C303/40 ,  C07C311/16 ,  C07C311/17 ,  C07C311/19 ,  C07C311/21 ,  C07D207/08 ,  C07D211/00 ,  C07D261/20 ,  C07D265/30 ,  C07D275/04 ,  C07D275/06 ,  C07D295/088 ,  C07D295/092 ,  C07D413/04 ,  C07D417/04

Abstract: PROBLEM TO BE SOLVED: To provide a medicine useful for treatment of atherothrombotic cardiovascular diseases such as cardiac infarction, stenocardia, cerebrovascular diseases, etc. SOLUTION: This compound is represented by the formula (I) [wherein G is a group represented by the formula (II) (R and R each independently represent hydrogen atom, an alkyl group or the like or R and R form a heterocycloalkyl group together with nitrogen atom) or the like; R represents hydrogen atom, an alkyl group or the like; Ra is hydroxy group, a 1-6C alkoxy group or amino group; Rb and Rc are same or different and each represents hydrogen atom, a halogen atom, an alkyl group or the like; m is an integer of 0-1; n and q are same or different integer of 0-6; p and r are same or different integer of 1-6]. This pharmaceutical composition comprises the compound.

公开(公告)号：JP2003096057A

公开(公告)日：2003-04-03

申请号：JP2002205661

申请日：2002-07-15

Applicant: SERVIER LAB

Inventor： LABIDALLE SERGE ,  TILLEMENT JEAN PAUL ,  TESTA BERNARD ,  CECCHELLI ROMEO ,  LE RIDANT ALAIN ,  HARPEY CATHERINE ,  SPEDDING MICHAEL ,  SCHENKER ESTHER

IPC: C07D295/08 ,  A61K31/495 ,  A61K31/496 ,  A61K31/506 ,  A61P9/00 ,  A61P9/10 ,  A61P25/00 ,  A61P25/28 ,  A61P41/00 ,  C07D239/42 ,  C07D239/50 ,  C07D295/03 ,  C07D295/092 ,  C07D295/096 ,  C07D295/14 ,  C07D295/15

Abstract: PROBLEM TO BE SOLVED: To provide a pharmaceutical composition which is useful for prevention or treatment of cellular ischemia, ischemic brain, ischemic heart or peripheral ischemia; treatment of chronic neurodegenerative symptoms, and for storage of organs for the purpose of transplantation, as well as for improving recovery of functioning transplant piece of after being reperfused. SOLUTION: An N-benzylpiperazine compound is represented by formula (I), [wherein, R1 is a straight chain or branched chain (C1 -C6 ) alkyl group; R2 is a hydroxyl group or the like; R3 is a hydrogen atom or the like; n is an integer of 1 to 12], and an optical isomer thereof, an addition salt thereof with a pharmaceutically acceptable acid or base, and a method for preparing thereof, as well as a pharmaceutical composition containing said compound are provided.

公开(公告)号：JP2002212184A

公开(公告)日：2002-07-31

申请号：JP2001378235

申请日：2001-12-12

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  GLOANEC PHILIPPE ,  VERBEUREN TONY ,  RUPIN ALAIN ,  VALLEZ MARIE ODILE

IPC: C07D487/04 ,  A61K31/4985 ,  A61K31/536 ,  A61K38/00 ,  A61P7/02 ,  A61P9/10 ,  A61P43/00 ,  C07D471/04 ,  C07K5/078

Abstract: PROBLEM TO BE SOLVED: To obtain a new inhibitor of serine proteases such as thrombin having improved effects and selectivity. SOLUTION: This compound is represented by formula (I) [wherein, R1 represents hydrogen atom or a linear or a branched 1-6C alkyl group which is optionally substituted; a group represented by formula (II) represents a saturated ring having 4 to 7 ring members that may contain, in addition to nitrogen atom, one or two heteroatoms selected from O, S and N; n represents an integer of 1

公开(公告)号：JP2002193932A

公开(公告)日：2002-07-10

申请号：JP2001311565

申请日：2001-10-09

Applicant: SERVIER LAB

Inventor： PEGLION JEAN-LOUIS ,  VILAINE JEAN-PAUL ,  VILLENEUVE NICOLE ,  THOLLON CATHERINE ,  BOURGUIGNON MARIE-PIERRE ,  POITEVIN CHRISTOPHE

IPC: C07D491/056 ,  A61K31/438 ,  A61K31/445 ,  A61K31/4525 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/497 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D211/22 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/04 ,  C07D491/107 ,  C07D519/00

Abstract: PROBLEM TO BE SOLVED: To provide a compound which can restrain endothelium malfunction and the drop in possible use of NO by blood vessels, and is useful for the treatment of the crisis and expansion of the legion of atherosclerosis, the prevention of diseases complicated with it, the prevention of a blood vessel complication after blood vessel bypass, vasodilation, blood vessel re-circulation and heart transplantation, the treatment of cardiac muscle or peripheral ischemia, cardiac incompetence and pulmonary hypertension. SOLUTION: The compound represented by formula (1) [X is a 5 to 12-membered heterocyclic group or the like; n is 0 or 1; R1 is hydrogen atom or the like; Ra is single bond or the like; A is nitrogen atom or the like; E is nitrogen atom or the like; Rb is single bond or the like; W is an aryl or the like] and its optical isomer, its hydrate, its solvate and its addition salt with a pharmaceutically acceptable acid are included.

公开(公告)号：JP2002179652A

公开(公告)日：2002-06-26

申请号：JP2001319183

申请日：2001-10-17

Applicant: SERVIER LAB

Inventor： METH-COHN OTTO ,  YU CHU-YI ,  LESTAGE PIERRE ,  LEBRUN MARIE-CECILE ,  CAIGNARD DANIEL-HENRI ,  RENARD PIERRE

IPC: C07D211/00 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4418 ,  A61K31/4425 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/4458 ,  A61K31/451 ,  A61K31/452 ,  A61K31/5377 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/16 ,  A61P25/28 ,  B01J23/42 ,  C07B61/00 ,  C07D211/22 ,  C07D211/32 ,  C07D213/30 ,  C07D213/36 ,  C07D213/38 ,  C07D213/50 ,  C07D401/06

Abstract: PROBLEM TO BE SOLVED: To obtain a compound capable of resisting dysgnosia with aging and ameliorating a recognition process, having analgesic characteristics. SOLUTION: This compound is represented by formula (I) [A is pyridine, or the like; R2 is hydrogen atom, or the like; R3 is hydroxy group, or the like; R4 is phenyl group, or the like; R1 is hydrogen atom, or the like; R5 is a five- or six-membered ring which may contain a nitrogen atom combined with the ring A and another hetero atom selected from sulfur, oxygen and nitrogen; R6 is hydrogen atom, or the like], its enantiomer, a diastereoisomer, pharmacologically acceptable acid, base or their addition salts. The method for producing the compound is provided. The medicine composition comprises the compound.

公开(公告)号：JP2006342158A

公开(公告)日：2006-12-21

申请号：JP2006133321

申请日：2006-05-12

Applicant: SERVIER LAB

Inventor： DESOS PATRICE ,  CORDI ALEX ,  LESTAGE PIERRE

IPC: C07D213/74 ,  A61K31/496 ,  A61K31/5377 ,  A61P3/04 ,  A61P25/00 ,  A61P25/02 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07B61/00

Abstract: PROBLEM TO BE SOLVED: To provide an antagonist of a new H 3 type central histamine receptor. SOLUTION: The compound represented by formula (I) is provided [wherein R 1 is an NR 3 SO 2 R 4 (R 3 is H or an alkyl, and R 4 is an alky, an aryl or NR 5 R 6 ); and R 2 is an alkyl, a cycloalkyl or a cycloalkylalkyl]. COPYRIGHT: (C)2007,JPO&INPIT

公开(公告)号：JP2002363167A

公开(公告)日：2002-12-18

申请号：JP2002087792

申请日：2002-03-27

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  PORTEVIN BERNARD ,  BENOIST ALAIN ,  LEVENS NIGEL ,  NOSJEAN OLIVIER ,  HUSSON-ROBERT BERNADETTE

IPC: C07D295/18 ,  A61K31/40 ,  A61K31/4178 ,  A61K31/426 ,  A61K31/5377 ,  A61K38/00 ,  A61P1/00 ,  A61P1/02 ,  A61P3/04 ,  A61P3/10 ,  A61P31/18 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07B57/00 ,  C07D207/16 ,  C07D231/04 ,  C07D233/06 ,  C07D233/48 ,  C07D277/04 ,  C07D277/06 ,  C07D277/10 ,  C07D295/22 ,  C07D403/12 ,  C07K5/062 ,  C07K5/078 ,  C07K5/087 ,  C07K5/097

Abstract: PROBLEM TO BE SOLVED: To provide a medicine used as an inhibitor of dipeptidyl peptidase IV and usable for treatment of hyperglycemia and related disorders, prevention of transplanted piece refuse after transplantation, treatment of cancer and prevention of tumor metastasis, treatment of AIDS and paradentitis and recovery of intestine after resection. SOLUTION: This invention relates to a compound represented by the formula (I) [wherein the ring A represents a five-membered nitrogen-containing heterocycle which may be substituted by cyano group; R1 represents hydrogen atom or the like; Ak represents a straight or branched (1-6C)alkylene chain or the like; X represents a single bond or the like; R2 represents a straight-chain or a branched (1-6C)alkyl group or the like; Y represents a group of NR3 or the like (wherein R3 is hydrogen atom or the like)], its optical isomer and addition salt of its pharmaceutically acceptable acid, a method for producing the compound and a pharmaceutical composition containing the compound.

公开(公告)号：JP2002356486A

公开(公告)日：2002-12-13

申请号：JP2002114443

申请日：2002-04-17

Applicant: SERVIER LAB

Inventor： LAVIELLE GILBERT ,  DUBUFFET THIERRY ,  MULLER OLIVIER ,  MILLAN MARK ,  DEKEYNE ANNE ,  BROCCO MAURICETTE

IPC: A61K31/519 ,  A61P1/14 ,  A61P15/10 ,  A61P15/12 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D471/00 ,  C07D471/04 ,  C07D491/048 ,  C07D491/052 ,  C07D513/00 ,  C07D519/00

Abstract: PROBLEM TO BE SOLVED: To provide a medicine useful for treatment of depression, impulsive behavioral disorder, anxiety, schizophrenia, Parkinson's disease, dysgnosia, libido dysfunction, sexual dysfunction, appetite disorder and somnipathy due to α2 /5-HT2c antagonist characteristics possessed thereby. SOLUTION: This compound is represented by the formula (I) [wherein, R1 , R2 , R3 and R4 denote each hydrogen atom or the like; X denotes oxygen atom or the like; A denotes a linear or a branched (1-6C) alkylene chain; ring-B denotes an unsaturated nitrogen-containing heterocyclic ring; and R5 denotes a linear or a branched (1-6C) alkyl chain], its enantiomer and diastereoisomer and its addition salt with a pharmaceutically acceptable acid or base. The method for preparing the same and the pharmaceutical composition comprising the same are provided.