公开(公告)号：CY1107472T1

公开(公告)日：2012-12-19

申请号：CY071101471

申请日：2007-11-14

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： TEGTMEIER FRANK ,  JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  VAN ROSSEM KOENRAAD ARTHUR ,  ALCAZAR-VACA MANUEL JESUS ,  MARTINEZ-JIMENEZ PEDRO ,  BARTOLOME-NEBREDA JOSE MANUEL ,  GOMEZ-SANCHEZ ANTONIO ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  VAN REEMPTS JOZEF LEO HENRI

IPC: C07D487/04 ,  C07D519/00 ,  A61K31/415 ,  A61K31/425 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/55 ,  A61P1/04 ,  A61P9/10 ,  A61P29/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  C07D471/00 ,  C07D471/04 ,  C07D487/00

Abstract: Ηεφεύρεσηαφοράένανέοανταγωνιστήυποδοχέαισταμίνηςκαιτηχρήσηενόςανταγωνιστήυποδοχέαισταμίνηςγιατημείωσητηςενδοκρανιακήςπίεσης (ΕΚΠ), συγκεκριμέναγιατηπρόληψηκαιτηθεραπείατηςαυξημένηςενδοκρανιακήςπίεσηςκαι/ήδευτερεύουσαςισχαιμίας, πουπροκαλείταισυγκεκριμένααπόεγκεφαλικότραυματισμό, πιοσυγκεκριμέναπροκαλείταιαπότραυματικό (ΤΕΤ) καιμητραυματικόεγκεφαλικότραυματισμό. ΟινέεςενώσειςπεριλαμβάνουνενώσειςσύμφωναμετογενικόΤύπο (I) ταφαρμακευτικάαποδεκτάάλαταπρόσθεσηςοξέοςή βάσεωςαυτού, τιςστερεοχημικάισομερείςμορφέςαυτούκαιτημορφήΝ-οξειδίουαυτού. Συγκεκριμένα, ηπροτιμώμενηένωσηείναι 3-[2-[4-(11,12-διυδρο-6H-βενζιμιδαζο[2,1-b][3]βενζαζεπιν-6-υλ)-2-(φαινυλ-μεθυλ)-1-πιπεριδινυλ]αιθυλ]-2,10-διμεθυλπυριμιδο[1,2-α]βενζιμιδαζολ-4(10H)-όνη, ταφαρμακευτικάαποδεκτάάλαταπρόσθεσηςοξέοςή βάσεωςαυτής, οιστερεοχημικάισομερείςμορφέςαυτήςκαιη μορφήΝ-οξειδίουαυτής. Επίσηςαξιώνεταιη νέαχρήσηεμπορικάδιαθέσιμωνανταγωνιστώνυποδοχέαισταμίνης H1-καιΗ2 γιατημείωσητηςενδοκρανιακήςπίεσης (ΕΚΠ).

公开(公告)号：AU2011202995B2

公开(公告)日：2012-02-02

申请号：AU2011202995

申请日：2011-06-21

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： CID-NUNEZ JOSE MARIA ,  MEGENS ANTONIUS ADRIANUS HENDRIKUS PETRUS ,  TRABANCO-SUAREZ ANDRES AVELINO ,  KOUKNI MOHAMED ,  HOORNAERT GEORGES JOSEPH CORNELIUS ,  COMPERNOLLE FRANS JOSEF CORNELIUS ,  KOZLECKI TOMASZ ,  MAO HUA ,  JHA SUSHIL CHANDRA ,  FERNANDEZ-GADEA FRANCISCO JAVIER

IPC: C07D209/70 ,  A61K31/343 ,  A61K31/352 ,  A61K31/381 ,  A61K31/403 ,  A61K31/407 ,  A61K31/4188 ,  A61K31/496 ,  A61K31/4985 ,  C07D221/18 ,  C07D307/93 ,  C07D311/94 ,  C07D333/80 ,  C07D487/04 ,  C07D491/044

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT 2c receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition 10 properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (1) (R9i A B (R9j 20 and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

公开(公告)号：CA2462953C

公开(公告)日：2011-01-04

申请号：CA2462953

申请日：2002-10-10

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  GOMEZ-SANCHEZ ANTONIO ,  MEERT THEO FRANS

IPC: C07D401/04 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61P1/00 ,  A61P1/04 ,  A61P1/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/10 ,  A61P17/06 ,  A61P19/02 ,  A61P25/02 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to novel 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives according to Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. In particular are claimed compounds according to Formula (I) in which A=B is C=O or SO2, X is a covalent bond, R1 is alkyloxy, alkyloxyalkyl, Ar or NR9R10, wherein R9 and R10 each independently are hydrogen or Ar; or A=B and R1 together form a benzoxazolyl radical ; p is zero, R3 is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R4 and R5 each are hydrogen. The invention also relates to processes for the preparation of the compounds according to the invention and their use in medicine, in particular as selective non-peptide d-opioid agonists for use in the treatment of various pain conditions.

公开(公告)号：BRPI0611408A2

公开(公告)日：2010-09-08

申请号：BRPI0611408

申请日：2006-05-24

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MEGENS ANTONIUS ADRIANUS HENDRIKUS PETRUS ,  TRABANCO-SUAREZ ANDRES AVELINO ,  KOUKNI MOHAMED ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  KOZLECKI TOMASZ ,  CID-NUNEZ JOSE MARIA ,  MAO HUA ,  JHA SUSHIL CHANDRA ,  HOORNAERT GEORGES JOSEPH CORNELIUS ,  COMPERNOLLE FRANS JOSEF CORNELIUS

IPC: C07D487/04 ,  A61K31/403 ,  A61K31/407 ,  A61P25/00 ,  C07D209/94 ,  C07D221/18 ,  C07D307/93 ,  C07D311/94 ,  C07D333/80 ,  C07D491/04

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

公开(公告)号：IS2618B

公开(公告)日：2010-04-15

申请号：IS6591

申请日：2002-10-25

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： EMELEN KRISTOF VAN ,  BRUYN MARCEL FRANS LEOPOLD DE ,  ALCAZAR-VACA MANUEL JESUS ,  ANDRES-GIL JOSE IGNACIO ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  MATESANZ-BALLESES-TEROS MARIA ENCARNACIO ,  BARTOLOME-NEBREDA JOSE MANUEL

IPC: C07D491/056 ,  C07D491/06 ,  A61K31/435 ,  A61K31/436 ,  A61K31/4545 ,  A61K31/513 ,  A61K31/5383 ,  A61P1/00 ,  A61P1/14 ,  C07D411/04 ,  C07D491/04 ,  C07D491/052 ,  C07D497/04 ,  C07D498/04

公开(公告)号：EA012628B1

公开(公告)日：2009-10-30

申请号：EA200702530

申请日：2006-05-17

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： FERNANDEZ-GADEA FRANCISCO JAVIER ,  ANDRES-GIL JOSE IGNACIO ,  TRABANCO-SUAREZ ANDRES AVELINO ,  CID-NUNEZ JOSE MARIA ,  MEGENS ANTONIUS ADRIANUS HENDRIKUS PETRUS

IPC: C07D405/06 ,  C07D493/04 ,  C07D495/04

Abstract: Изобретениеотноситсяк новымтетрациклическимпроизводнымтетрагидрофурана, содержащимв боковойцепигруппуциклическогоаминаи обладающимсродствомсвязыванияв отношениисеротониновыхрецепторов, вчастности 5-HTи 5-HTрецепторов, ив отношениидопаминовыхрецепторов, вчастностидопаминовых Dрецепторов, фармацевтическимкомпозициям, включающимсоединениясогласноизобретению, ихприменениюв качествелекарственногосредства, вчастностидляпрофилактикии/илилечениярядапсихическихи неврологическихрасстройств, вособенностинекоторыхпсихических, сердечно-сосудистыхи желудочно-кишечныхрасстройств, ик способамихполучения. Соединениясогласнонастоящемуизобретениюмогутбытьпредставленыобщейформулой (I) ивключаюттакжеихфармацевтическиприемлемыеаддитивныесолис кислотойилиоснованием, стереохимическиизомерныеформы, N-оксидныеформыи четвертичныеаммониевыесоли, гдезначениязаместителейопределеныв п.1.

公开(公告)号：JO2352B

公开(公告)日：2006-12-12

申请号：JO200184

申请日：2001-05-29

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： VAN EMELEN KRISTOF ,  DE BRUYN MARCEL FRANS LEOPOLD ,  ALCAZAR-VACA MANUEL JESUS ,  ANDRES-GIL JOSE IGNACIO ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  MATESANZ-BALLESTEROS ENCARNACION ,  BARTOLOME-NEBREDA JOSE MANUEL

IPC: C07D491/056 ,  A61K31/435 ,  A61K31/436 ,  A61K31/4545 ,  A61K31/513 ,  A61K31/5383 ,  A61P1/00 ,  A61P1/14 ,  C07D411/04 ,  C07D491/04 ,  C07D491/052 ,  C07D491/06 ,  C07D497/04 ,  C07D498/04

CPC classification number: C07D411/04 ,  C07D491/04

Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -a =a -a =a - is a bivalent radical wherein one or two of a to a are nitrogen and the remaining a to a are -CH-; -Z -Z - is a bivalent radical; -A- is a bivalent radical of formula -N(R )-Alk - or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R , R and R are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk and Alk are optionally substituted C1-6alkanediyl; R is a radical of formula wherein n is 1 or 2; p is 0, and p is 1 or 2; or p is 1 or 2, and p is 0; X is oxygen, sulfur or -NR ; Y is oxygen or sulfur; R is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R is cyano, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to disturbed fundic accomodation.

公开(公告)号：RO116729B1

公开(公告)日：2001-05-30

申请号：RO9600283

申请日：1994-08-12

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： VAN LOMMEN GUY ROSALIA EUGENE ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  ANDRES-GIL JOSE IGNACIO ,  MATESANZ-BALLESTEROS MARIA ENCARNACION

IPC: A61K31/35 ,  A61K31/436 ,  A61K31/44 ,  A61K31/453 ,  A61K31/505 ,  A61P9/02 ,  A61P9/08 ,  A61P25/04 ,  A61P25/06 ,  C07D405/12 ,  C07D491/04 ,  C07D491/052

Abstract: Invenţia se referă la derivaţi de dihidropiranopiridine cu formula (I):în care = a=a=a=aeste un radical bivalent cu formula: =N-CH=CH-CH= (a) =CH-N=CH-CH= (b) =CH-CH=N-CH= (c) =CH-CH=CH-N= (d) în care unul sau doi atomi de hidrogen, din radicalii bivalenţi, pot fi substituiţi cu halogen, hidroxi, Calchil sau Calchiloxi; Reste hidrogen sau Calchil; Reste hidrogen sau C; Reste hidrogen sau Calchil; Alkeste Calcandiil; Alkeste Calcandiil, la procedeele de preparare a acestor compuşi şi la un intermediar utilizat la obţinerea derivaţilor cu formula (i). Derivaţii de dihidropiranopiridine cu formula (I) sunt utilizaţi la tratarea bolilor caracterizate printr-o vasodilataţie excesivă, în special migrena, în tratamentul insuficienţei venoase şi a hipotensiunii.

公开(公告)号：NO20001792L

公开(公告)日：2000-04-06

申请号：NO20001792

申请日：2000-04-06

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  GIL-LOPETEGUI PILAR ,  DIAZ-MARTINEZ ADOLFO

IPC: A61K31/34 ,  A61K31/343 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/445 ,  A61K31/4525 ,  A61K31/495 ,  A61K31/496 ,  A61K31/535 ,  A61K31/5377 ,  A61K31/55 ,  A61P25/00 ,  A61P25/06 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/30 ,  C07D307/93 ,  C07D401/06 ,  C07D405/06 ,  C07D493/04

Abstract: This invention concerns the compounds of formula (I),the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero, 1, 2, 3, 4, 5 or 6; X is CH2 or O; R and R each independently are hydrogen, C1-6alkyl, C1-6alkylcarbonyl, halomethylcarbonyl or C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R and R taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R and R are both halogen; or R is halogen and R is hydrogen; or R is hydrogen and R is halogen; and aryl is phenyl or phenyl substituted with 1, 2 or 3 substituents selected from halo, hydroxy, C1-6alkyl and halomethyl. The compounds of formula (I) may be used as therapeutic agents.

公开(公告)号：NO20001792A

公开(公告)日：2000-04-06

申请号：NO20001792

申请日：2000-04-06

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  GIL-LOPETEGUI PILAR ,  DIAZ-MARTINEZ ADOLFO

IPC: A61K31/34 ,  A61K31/343 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/445 ,  A61K31/4525 ,  A61K31/495 ,  A61K31/496 ,  A61K31/535 ,  A61K31/5377 ,  A61K31/55 ,  A61P25/00 ,  A61P25/06 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/30 ,  C07D307/93 ,  C07D401/06 ,  C07D405/06 ,  C07D493/04

CPC classification number: C07D405/06 ,  C07D307/93 ,  C07D493/04