公开(公告)号：HK1203507A1

公开(公告)日：2015-10-30

申请号：HK15104233

申请日：2015-05-04

Applicant: SERVIER LAB

Inventor： LE DIGUARHER THIERRY ,  CASARA PATRICK ,  STARCK JRME-BENOT ,  HENLIN JEAN-MICHEL ,  DAVIDSON JAMES EDWARD PAUL ,  MURRAY JAMES BROOKE ,  GRAHAM CHRISTOPHER JOHN ,  CHEN I-JEN ,  GENESTE OLIVIER ,  HICKMAN JOHN ,  DEPIL STPHANE ,  LE TIRAN ARNAUD ,  NYERGES MIKLOS ,  DE NANTEUIL GUILLAUME

IPC: C07D20060101 ,  A61K20060101 ,  A61P20060101

Abstract: wherein Ra, Rb, Rc, Rd, R1, R2, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.

公开(公告)号：UY35653A

公开(公告)日：2015-02-27

申请号：UY35653

申请日：2014-07-08

Applicant: SERVIER LAB ,  VERNALIS R & D LTD

Inventor： BEDFORD SIMON ,  MADDOX DANIEL ,  RAY STUART ,  WALMSLEY CLAIRE ,  CASARA PATRICK ,  I-JEN CHEN ,  PAUL DAVIDSON JAMES EDWARD ,  GUILLAUME DE NANTEUIL ,  GENESTE OLIVIER ,  JOHN GRAHAM CHRISTOPHER ,  JEAN-MICHEL HENLIN ,  THIERRY LE DIGUARHER ,  ARNAUD LE TIRAN ,  BROOKE MURRAY JAMES ,  JÉRÔME-BENOÎT STARCK

IPC: A61P35/00 ,  A61K31/34 ,  A61K31/357 ,  A61K31/4025 ,  A61K31/403 ,  A61K31/4155 ,  A61K31/4709 ,  C07D217/12 ,  C07D401/10 ,  C07D401/14 ,  C07D405/00

Abstract: Compuestos de fórmula (I):en la que Ra, Rb, Rc, Rd, R3, R4, R5, A1, A2, T y W son tales como se han definido en la descripción.

公开(公告)号：CU23993B1

公开(公告)日：2014-04-24

申请号：CU20100236

申请日：2010-12-02

Applicant: SERVIER LAB

Inventor： CASARA PATRICK ,  CHOLLET ANNE-MARIE ,  DHAINAUT ALAIN ,  LESTAGE PIERRE ,  PANAYI FANY

IPC: C07D209/52

Abstract: Compuestos de azabiciclo [3.2.0] hept-3-ilo de fórmula (I): en la que: ALK representa una cadena alquileno, W representa un grupo ó en el que R y R' son tales como se han definido en la descripción. Medicamento.

公开(公告)号：ME01504B

公开(公告)日：2014-04-20

申请号：MEP4213

申请日：2010-12-08

Applicant: SERVIER LAB

Inventor： CASARA PATRICK ,  CHOLLET ANNE-MARIE ,  DHAINAUT ALAIN ,  PANAYI FANY ,  LESTAGE PIERRE

IPC: A61K31/403 ,  A61P25/00 ,  C07D209/52

Abstract: Spoj formule (1):naznačen time, da:predstavlja lanac alkilena, + W predstavlja skupinu ili u kojem R i R ', svaki neovisno jedan od drugoga, predstavljaju atom vodika ili ravnu ili razgrananu (C1-C6)alkilnu skupinu po izboru supstituiranu s jednim ili više skupina odabranih od halogena, hidroksi i alkoksi, pri čemu treba razumjeti da: - određenje " alkilen" označava ravni ili razgranani dvovalentni radikal koji se sastoji od 2 do 6 atoma ugljika, - određenje " alkoksi" označava alkil-oksi skupinu u kojoj lanac alkila, koji je ravni ili razgranani, sadrži od 1 do 6 atoma ugljika, njihovi enantiomeri i dijastereoizomeri te također njihove adicijske soli s farmaceutski prihvatljivom kiselinom ili lužinom.

公开(公告)号：CY1108529T1

公开(公告)日：2014-04-09

申请号：CY081100520

申请日：2008-05-20

Applicant: SERVIER LAB

Inventor： CASARA PATRICK ,  CHOLLET ANNE-MARIE ,  DHAINAUT ALAIN ,  BERT LIONEL ,  LESTAGE PIERRE ,  LOCKHART BRIAN

IPC: A61K31/403 ,  A61P25/00 ,  C07D209/52 ,  C07D403/12

Abstract: Ηεφεύρεσησχετίζεταιμεενώσειςπουέχουντονγενικότύπο (Ι): ταεναντιομερήκαιδιαστερεοϊσομερήτουςκαθώςκαιταάλατατουςπροσθήκηςμεέναή περισσότεραφαρμακευτικώςαποδεκτάοξέαή βάσεις. Οιενώσειςτηςπαρούσηςεφεύρεσηςείναιιδιαιτέρουενδιαφέροντοςγιατηναλληλεπρίδρασητουςμετακεντρικάισταμινεργικάσυστήματα.

公开(公告)号：CA2782469C

公开(公告)日：2014-04-08

申请号：CA2782469

申请日：2010-12-08

Applicant: SERVIER LAB

Inventor： CASARA PATRICK ,  CHOLLET ANNE-MARIE ,  DHAINAUT ALAIN ,  HENLIN JEAN-MICHEL ,  LESTAGE PIERRE ,  PANAYI FANY

IPC: C07D209/52 ,  A61K31/403 ,  A61P25/00

Abstract: La présente invention concerne des composés de formule (I) : dans laquelle : ALK représente une chaîne alkylène, W représente un groupement de formule (II) ou de formule (III) où R et R' sont tels que définis dans la description. (voir formule I)(voir formula II)(voir formule III) L'invention s'étend à leur procédé de préparation, leurs utilisations ainsi que les compositions pharmaceutiques qui les contiennent.

公开(公告)号：AU2010329762B2

公开(公告)日：2013-10-03

申请号：AU2010329762

申请日：2010-12-08

Applicant: SERVIER LAB

Inventor： CASARA PATRICK ,  CHOLLET ANNE-MARIE ,  DHAINAUT ALAIN ,  HENLIN JEAN-MICHEL ,  LESTAGE PIERRE ,  PANAYI FANY

IPC: C07D209/52 ,  A61K31/403 ,  A61P25/00

Abstract: The invention relates to the compounds of formula (I), where: ALK is an alkylene chain, and W is a grouping of formula (II) or formula (III), where R and R' are as defined in the description. The invention can be used as a drug.

公开(公告)号：UY34578A

公开(公告)日：2013-09-02

申请号：UY34578

申请日：2013-01-17

Applicant: SERVIER LAB ,  VERNALIS R & D LTD

Inventor： CASARA PATRICK ,  I-JEN CHEN ,  PAUL DAVIDSON JAMES EDWARD ,  GUILLAUME DE NANTEUIL ,  STEPHANE DEPIL ,  GENESTE OLIVIER ,  JOHN GRAHAM CHRISTOPHER ,  JEAN-MICHEL HENLIN ,  HICKMAN JOHN ,  THIERRY LE DIGUARHER ,  ARNAUD LE TIRAN ,  BROOKE MURRAY JAMES ,  MIKLOS NYERGES ,  JEROME-BENOIT STARCK

IPC: A61P35/00 ,  A61K31/437 ,  A61K31/5383 ,  C07D209/04 ,  C07D217/00 ,  C07D231/02 ,  C07D231/56 ,  C07D295/00 ,  C07D317/46 ,  C07D319/16 ,  C07D471/04 ,  C07D498/04

Abstract: Compuestos de fórmula (I): en la que Ra, Rb, Rc, Rd, R1, R2, R3, R4, R5, X, Y y Het son tales como se han definido en la descripción. Medicamentos.

公开(公告)号：BRPI1005270A2

公开(公告)日：2013-04-30

申请号：BRPI1005270

申请日：2010-12-08

Applicant: SERVIER LAB

Inventor： CASARA PATRICK ,  CHOLLET ANNE-MARIE ,  DHAINAUT ALAIN ,  LESTAGE PIERRE ,  PANAYI FANY

IPC: C07D209/52 ,  A61K31/198 ,  A61K31/4035 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28

Abstract: Azabicyclo [3.2.0] hept-3-yl derivatives (I) and their enantiomers, diastereoisomers, or addition salts with an acid or a base are new. Azabicyclo [3.2.0] hept-3-yl derivatives of formula (I) and their enantiomers, diastereoisomers, or addition salts with an acid or a base are new. ALK : an alkylene chain; W1 : amide group of formula (-NR1a-C(=O)-R) or (-C(=O)-NR1a-R); and R1a, R : H or 1-6C alkyl optionally substituted by one or more groups comprising halo, hydroxy or alkoxy, provided that the alkylene denotes 2-6C divalent radical, and the alkoxy is 1-6C alkyloxy. Independent claims are included for: (1) the preparation of (I); and (2) intermediates comprising alkylene benzoic acid substituted aza-bicycloheptane compounds of formula (VI), alkylene benzoyl chloride substituted aza-bicycloheptane compounds of formula (VII), alkylene benzoic acid ester substituted aza-bicyclo-heptane compounds of formula (VIII), and alkylene oxy phenyl substituted aza-bicyclo-heptane compounds of formula (IX), for preparing (I) (where W1 represents -CONRR1a). R2a : 1-6C alkyl or benzyl. [Image] [Image] ACTIVITY : Nootropic; Neuroleptic; Neuroprotective; Cerebroprotective; Vulnerary; Hypnotic; Tranquilizer; Antidepressant; CNS-Gen. MECHANISM OF ACTION : Histamine H3 receptor antagonist. The histamine H3 receptor antagonistic activity of (I) was tested in Naval medical research institute (NMRI) mice. The result showed that 4-{3-[(1R,5S)-3-aza-bicyclo[3.2.0]hept-6-yl]-propoxy}benzamide hydrochloride increased the endogenous cerebral concentration of N-methylhistamine to 100%, at 3 mg/kg.

公开(公告)号：AP2012006352A0

公开(公告)日：2012-08-31

申请号：AP2012006352

申请日：2010-12-08

Applicant: SERVIER LAB

Inventor： CASARA PATRICK ,  CHOLLET ANNE-MARIE ,  PANAYI FANY

IPC: C07D209/52 ,  A61K31/403 ,  A61P25/00

Abstract: Compounds of formula: wherein: ALK represents an alkylene chain, W represents a group wherein R and R′ are as defined in the description. Medicinal products containing the same which are useful in treating cognitive disorders associated with cerebral aging or with neurodegenerative diseases.