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51. 发明专利

CU23488B7 DIHIDROQUINAZOLINAS SUSTITUIDAS CON PROPIEDADES ANTIVIRALES 未知
公开(公告)号：CU23488B7
公开(公告)日：2010-02-23
申请号：CU20050201
申请日：2005-10-18
申请人： BAYER HEALTHCARE AG
发明人： KELDENICH JOERG , NELL PETER , LANG DIETER , HEWLETT GUY , GROSSER ROLF , SUESSMEIER FRANK , REEFSCHLAEGER JUERGEN , JESKE MARIO , BETZ ULRICH , BAUMEISTER JUDITH , ZIMMERMANN HOLGUER , HENNINGER KERSTIN , WUNBERG TOBIAS , NIKOLIC SUSANNE , LAMPE THOMAS , SCHOHE-LOOP RUDOLF
IPC分类号： C07D239/84
摘要： La invención se refiere a dihidroquinazolinas sustituidas de fórmula (I) y a procedimiento para su preparación así como a su uso para la preparación de medicamentos para el tratamiento y/o la profilaxis de enfermedades, especialmente para el uso como agente antiviral, especialmente contra citomegalovirus

52. 发明专利

SV2009002953A NUEVOS DERIVADOS DE FUROPIRIMIDINA ACICLICOS SUSTITUIDOS Y SU USO 未知
公开(公告)号：SV2009002953A
公开(公告)日：2009-04-28
申请号：SV2008002953
申请日：2008-06-19
申请人： BAYER HEALTHCARE AG
发明人： LAMPE THOMAS , BECKER EVA-MARIA , KAST RAIMUND , BECK HARTRNUT , JESKE MARIO , SCHUHMACHER JOACHIM , STOLL FRIEDERIKE , KLEIN MARTINA , AKBABA METIN , KNORR ANDREAS , STASCH JOHANNES-PETER , BAERFACKER LARS , HILLISCH ALEXANDER , KARIG GUNTER , MEININGHAUS MARK , SCHLEMMER KARL-HEINZ , SCHOHE-LOOP RUDOLF
IPC分类号： A61K31/519 , A61P9/00 , C07D491/04
摘要： LA PRESENTE SOLICITUD SE REFIERE A NUEVOS DERIVADOS DE FUROPIRIMIDINA ACÍCLICOS SUSTITUIDOS, A PROCEDIMIENTOS PARA SU PRODUCCIÓN, A SU USO PARA EL TRATAMIENTO Y/O LA PROFILAXIS DE ENFERMEDADES, ASÍ COMO A SU USO PARA LA PREPARACIÓN DE PRODUCTO MEDICINAL PARA EL TRATAMIENTO Y/O LA PROFILAXIS DE ENFERMEDADES, EN PARTICULAR PARA EL TRATAMIENTO Y/O PROFILAXIS DE ENFERMEDADES CARDIOVASCULARES

53. 发明专利

ECSP088569A NUEVOS DERIVADOS DE FUROPIRIMIDINA ACÍCLICOS SUSTITUIDOS Y USO DE LOS MISMOS PARA EL TRATAMIENTO DE ENFERMEDADES CARDIOVASCULARES 未知
公开(公告)号：ECSP088569A
公开(公告)日：2008-08-29
申请号：ECSP088569
申请日：2008-06-20
申请人： BAYER HEALTHCARE AG
发明人： STASCH JOHANNES PETER , HILLISCH ALEXANDER , SCHLEMMER KARL HEINZ , JESKE MARIO , LAMPE THOMAS , SCHOHE-LOOP RUDOLF , KARIG GUNTER , KNORR ANDREAS , BAERFACKER LARS , SCHUHMACHER JOACHIM , KLEIN MARTINA , BECKER EVA-MARIA , KAST RAIMUND , BECK HARTMUT , STOLL FRIEDERIKE , MEININGHAUS MARK
IPC分类号： C07D491/04
摘要： La presente solicitud se refiere a nuevos derivados de furopirimidina acíclicos sustituidos, a procedimientos para su producción, a su uso para el tratamiento y/o la profilaxis de enfermedades, así como a su uso para la preparación de producto medicinal para el tratamiento y/o la profilaxis de enfermedades, en particular para el tratamiento y/o profilaxis de enfermedades cardiovasculares.

54. 发明专利

DE102006013957A1 Use of new or known N-benzyl N-phenyl benzenesulfonamide derivatives to prepare medicaments for treating or preventing viral diseases 未知
公开(公告)号：DE102006013957A1
公开(公告)日：2007-10-04
申请号：DE102006013957
申请日：2006-03-27
申请人： BAYER HEALTHCARE AG
发明人： URBAN ANDREAS , BROHM DIRK , BIRKMANN ALEXANDER , SCHOHE-LOOP RUDOLF , KOLETZKI DIANA , HARRENGA AXEL , STOLL FRIEDERIKE , MUNDT STEFAN , PAULSEN DANIELA
IPC分类号： C07C311/21 , A61K31/18 , A61P31/14
摘要： N-benzyl N-phenyl benzenesulfonamide derivatives (I) are used to prepare medicaments for treating or preventing viral diseases. N-benzyl N-phenyl benzenesulfonamide derivatives of formula (I) or their salts or solvates are used to prepare medicaments for treating or preventing viral diseases. R 1>OH or NR 9>R 10>; R 9>, R 10>H, 1-6C alkyl, or benzyl or 2-phenylethyl optionally substituted with 1-3 of halo, CN, OH, NH 2, CF 3, OCF 3, 1-4C alkyl, 1-4C alkoxy and 1-4C alkylamino; R 2>, R 3>H, halo, CN, OH, NH 2, CF 3 or OCF 3; 1-4C alkyl, 1-4C alkoxy or 1-4C alkylamino optionally substituted with 1-3 of halo, CN, OH, NH 2, CF 3 or OCF 3; or N-bonded 5- to 7-membered heterocyclyl optionally substituted with 1-3 of halo, CN, OH, NH 2, CF 3, OCF 3, 1-4C alkyl, 1-4C alkoxy and 1-4C alkylamino; R 1>+R 2>OCH 2 with O bonded to the CO group; R 4>halo, CN, Me, Et or cyclopropyl; R 5>H; 1-4C alkyl, 2-4C alkenyl, 1-4C alkoxy, 1-4C alkylthio or 1-4C alkylamino, all optionally substituted with a phenyl or 5- to 10-membered heteroaryl group optionally substituted with 1-3 of halo, CN, OH, NH 2, CF 3, OCF 3, CONH 2, SO 2NH 2, 1-4C alkyl, 1-4C alkoxy and 1-4C alkylamino; or CH 2YR 12>; Y : O, S or NR 12>; R 12>H, 1-4C alkyl or 3-6C cycloalkyl; R 11>5- to 10-membered heteroaryl optionally substituted with 1-3 of halo, CN, OH, NH 2, CF 3, OCF 3, CONH 2, SO 2NH 2, 1-4C alkyl, 1-4C alkoxy and 1-4C alkylamino; R 6>halo, CN, NO 2, Me, Et, CF 3, OCF 3 or 2-cyanovinyl; R 7>H; or 1-4C alkyl, 2-4C alkenyl, 1-4C alkoxy, 1-4C alkylthio or 1-4C alkylamino, all optionally substituted with a phenyl or 5- to 10-membered heteroaryl group optionally substituted with 1-3 of halo, CN, OH, NH 2, CF 3, OCF 3, CONH 2, SO 2NH 2, 1-4C alkyl, 1-4C alkoxy and 1-4C alkylamino; R 8>halo, CN, NO 2, Me, Et, CF 3 or OCF 3. Independent claims are also included for: (1) new compounds (I) with the definitions given below; (2) a process for preparing (I). R 1>OH or NR 9>R 10>; R 9>, R 10>H, or 1-6C alkyl; R 2>, R 3>H, halo, CN, OH, NH 2, CF 3, OCF 3, 1-4C alkyl, 1-4C alkoxy, 1-4C alkylamino or N-bonded 5- to 7-membered heterocyclyl; R 1>+R 2>OCH 2 with O bonded to the CO group; R 3>H; R 4>halo, CN, Me, Et or cyclopropyl; R 5>H; R 6>halo, CN, NO 2, Me, Et, CF 3, OCF 3 or 2-cyanovinyl; R 7>H; R 8>halo, CN, NO 2, Me, Et, CF 3 or OCF 3. [Image] ACTIVITY : Virucide; Hepatotropic; Antiinflammatory. MECHANISM OF ACTION : Hepatitis C virus RNA replication inhibitor. Test details are described but no results given.

55. 发明专利

DE50206175D1 未知
公开(公告)号：DE50206175D1
公开(公告)日：2006-05-11
申请号：DE50206175
申请日：2002-05-21
申请人： BAYER HEALTHCARE AG
发明人： MEIER HEINRICH , ALLERHEILIGEN SWEN , GERISCH MICHAEL , SCHOHE-LOOP RUDOLF , VOERSTE ARND , MAULER FRANK , DE VRY MARIE , MUELLER THOMAS , METHFESSEL CHRISTOPH
IPC分类号： C07D335/06 , A61K31/382 , A61K31/395 , A61K31/40 , A61K31/4025 , A61K31/4035 , A61K31/41 , A61K31/4155 , A61K31/4178 , A61K31/4245 , A61K31/428 , A61K31/4436 , A61K31/453 , A61K31/4535 , A61K31/496 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/55 , A61P1/08 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P19/08 , A61P21/04 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P29/00 , A61P31/04 , A61P31/12 , A61P43/00 , C07D335/04 , C07D335/16 , C07D409/04 , C07D409/10 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/12 , C07D491/10 , C07D491/113
摘要： The invention relates to novel thiochromenones and processes for their preparation, to their use for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of states of pain and neurodegenerative disorders.

56. 发明专利

NO20055649L 未知
公开(公告)号：NO20055649L
公开(公告)日：2006-01-31
申请号：NO20055649
申请日：2005-11-30
申请人： BAYER HEALTHCARE AG
发明人： SCHOHE-LOOP RUDOLF , GROSSER ROLF , HENNINGER KERSTIN , KELDENICH JORG , LAMPE THOMAS , ZIMMERMANN HOLGER , WUNBERG TOBIAS , BAUMEISTER JUDITH , BETZ ULRICH , JESKE MARIO , NIKOLIC SUSANNE , REEFSCHLAGER JUERGEN , SUESSMEIER FRANK , HEWLETT GUY , LANG DIETER , NELL PETER
IPC分类号： C07D239/84 , A61P31/22
摘要： The invention relates to substituted dihydroquinazolines and to processes for their preparation and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for use as antiviral agents, in particular against cytomegalo viruses.

57. 发明专利

PE01452005A1 DIHIDROQUINAZOLINAS SUSTITUIDAS COMO AGENTES ANTIVIRALES 未知
公开(公告)号：PE01452005A1
公开(公告)日：2005-05-22
申请号：PE0004322004
申请日：2004-04-30
申请人： BAYER HEALTHCARE AG
发明人： WUNBERG TOBIAS , BAUMEISTER JUDITH , JESKE MARIO , NIKOLIC SUSANNE , SCHOHE-LOOP RUDOLF , ZIMMERMANN HOLGER , HENNINGER KERSTIN , KELDENICH JORG , HEWLETT GUY , GROSSER ROLF , SUSMEIER FRANK , REEFSCHLAGER JURGEN , LAMPE THOMAS , BETZ ULRICH , LANG DIETER , NELL PETER
IPC分类号： A61K31/517 , A61P31/22 , C07D239/84
CPC分类号： C07D239/84
摘要： SE REFIERE A DIHIDROQUINAZOLINAS SUSTITUIDAS DE FORMULA I DONDE Ar ES ARILO CON 1 A 3 SUSTITUYENTES SELECCIONADOS DE ALQUILO, ALCOXI, FORMILO, CARBOXILO, ENTRE OTROS; R1 ES H, AMINO, ALQUILO, ALCOXI, ALQUILAMINO, ALQUILTIO, ENTRE OTROS; R2 ES H, ALQUILO, ALCOXI, CIANO, ENTRE OTROS; R3 ES AMINO, ALQUILO, ALCOXI, ALQUILAMINO, ALQUILTIO, ENTRE OTROS; O BIEN UNO DE LOS RESTOS R1, R2 Y R3 ES H, ALQUILO, ALCOXI, CIANO, ENTRE OTROS Y LOS OTROS DOS JUNTO CON EL CARBONO AL QUE ESTAN UNIDOS FORMAN UN 1,3-DIOXOLANO, UN ANILLO CICLOPENTANO O UN ANILLO CICLOHEXANO; R4 Y R5 SON H o ALQUILO; O BIEN R4 Y R5 EN EL ANILLO DE PIPERAZINA ESTAN UNIDOS A ATOMOS DE CARBONO EXACTAMENTE OPUESTOS Y FORMAN UN PUENTE METILENO SUSTITUIDO O NO CON 1 A 2 GRUPOS METILO; R6 ES ALQUILO, ALCOXI, ALQUILTIO, FORMILO, CARBOXILO, AMINOCARBONILO, ENTRE OTROS; R7 ES H, ALQUILO, ALCOXI, ALQUILTIO, FORMILO, CARBOXILO, ALQUILCARBONILO, ENTRE OTROS; R8 ES H, ALQUILO, ALCOXI, ALQUILTIO, FORMILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ACIDO {8-FLUORO-2-[4-(4-FLUOROFENIL)-1-PIPERAZINIL]-3-[3-(TRIFLUORMETIL)FENIL]-3,4-DIHIDRO-4-QUINAZOLINIL}ACETICO; ACIDO {8-FLUORO-2-[4-(3-METILFENIL)-1-PIPERAZINIL]-3-[3-(TRIFLUORMETIL)FENIL]-3,4-DIHIDRO-4-QUINAZOLINIL}ACETICO; ACIDO {8-FLUORO-2-[4-(3-METOXIFENIL)-1-PIPERAZINIL]-3-[3-(TRIFLUORMETIL)FENIL]-3,4-DIHIDRO-4-QUINAZOLINIL}ACETICO; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION. ESTOS COMPUESTOS SON UTILES COMO AGENTE ANTIVIRAL CONTRA CITOMEGALOVIRUS

58. 发明专利

DE10337993A1 未知
公开(公告)号：DE10337993A1
公开(公告)日：2005-03-17
申请号：DE10337993
申请日：2003-08-19
申请人： BAYER HEALTHCARE AG
发明人： SCHOHE-LOOP RUDOLF , PAESENS ARNOLD , BAUSER MARCUS , KOEBBERLING JOHANNES , DITTMER FRANK , HENNINGER KERSTIN , LANG DIETER , PAULSEN DANIELA
IPC分类号： A61P31/18 , C07D235/30 , A61K31/4184 , C07C233/00

59. 发明专利

DE10305785A1 New 2-(2-phenylpiperanyl-3-phenyl-dihydroquinazolinyl)-acetic acid derivatives, useful as antiviral agents, especially effective against human cytomegalovirus infections 未知
公开(公告)号：DE10305785A1
公开(公告)日：2004-08-26
申请号：DE10305785
申请日：2003-02-12
申请人： BAYER HEALTHCARE AG
发明人： WUNBERG TOBIAS , BAUMEISTER JUDITH , BETZ ULRICH , JESKE MARIO , KLEYMANN GERALD , LAMPE THOMAS , NIKOLIC SUSANNE , REEFSCHLAEGER JUERGEN , SCHOHE-LOOP RUDOLF , SUESMEIER FRANK , ZIMMERMANN HOLGER , GROSSER ROLF , HENNINGER KERSTIN , HEWLETT GUY , KELDENICH JOERG , KRAEMER THOMAS , NELL PETER , LIN TSE-I
IPC分类号： A61P31/22 , C07D239/84 , A61K31/517 , A61P31/12
摘要： 2-(2-(4-Phenyl-1-piperazinyl)-3-phenyl-3,4-dihydro-4-quinazolinyl)-acetic acid derivatives (I) are new. 2-(2-(4-Phenyl-1-piperazinyl)-3-phenyl-3,4-dihydro-4-quinazolinyl)-acetic acid derivatives of formula (I) and their salts, solvates and hydrated salts are new. [Image] Ar : aryl (optionally substituted (os) by 1-3 Q); Q : alkyl, alkoxy, CHO, COOH, alkylcarbonyl, alkoxycarbonyl, CF 3, halo, CN, OH, NH 2, alkylamino, CONH 2 or NO 2 (where alkyl is os by 1-3 halo, NH 2, alkylamino, OH or aryl), or Q + Q : a group completing a fused 1,3-dioxolan, cyclopentane or cyclohexane ring; R 1>-R 3>H, alkyl, alkoxy, CN, halo, NO 2 or CF 3, or two of R 1>-R 3>a group completing a fused 1,3-dioxolan, cyclopentane or cyclohexane ring, and R 4>, R 5>H or alkyl, or R 4> and R 5> on opposite C atoms : CH 2, CHMe or CMe 2 bridge. provided that R 1>-R 3> are not all H. An independent claim is included for the preparation of (I). ACTIVITY : Virucide. In tests for effectiveness against human cytomegalovirus (HCMV) infections in human foreskin fibroblast cultures, 2-(2-(4-(4-fluoro-3-methylphenyl)-1-piperazinyl)-3-(3-trifluoromethyl)-phenyl)-3,4-dihydro-4-quinazolinyl)-acetic acid (Ia) had an antiviral EC 50 value of 0.027 mu M and a cytotoxic CC 5 0 value of 17 mu M (corresponding to a selectivity index of 630). MECHANISM OF ACTION : None given.

60. 发明专利

CA2515545A1 2-(3-PHENYL-2-PIPERAZINYL-3,4-DIHYDROQUINAZOLINE-4-YL) ACETIC ACIDS AS ANTI-VIRAL AGENTS, ESPECIALLY AGAINST CYTOMEGALO VIRUSES 未知
公开(公告)号：CA2515545A1
公开(公告)日：2004-08-26
申请号：CA2515545
申请日：2004-01-29
申请人： BAYER HEALTHCARE AG
发明人： WUNBERG TOBIAS , BAUMEISTER JUDITH , LIN TSE-I , JESKE MARIO , BETZ ULRICH , KRAEMER THOMAS , NELL PETER , KELDENICH JOERG , REEFSCHLAEGER JUERGEN , NIKOLIC SUSANNE , LAMPE THOMAS , KLEYMANN GERALD , HEWLETT GUY , SCHOHE-LOOP RUDOLF , HENNINGER KERSTIN , GROSSER ROLF , SUESSMEIER FRANK , ZIMMERMANN HOLGER
IPC分类号： A61P31/22 , C07D239/84 , A61K31/517
摘要： 2-(2-(4-Phenyl-1-piperazinyl)-3-phenyl-3,4-dihydro-4-quinazolinyl)-acetic acid derivatives (I) are new. 2-(2-(4-Phenyl-1-piperazinyl)-3-phenyl-3,4-dihydro-4-quinazolinyl)-acetic acid derivatives of formula (I) and their salts, solvates and hydrated salts are new. [Image] Ar : aryl (optionally substituted (os) by 1-3 Q); Q : alkyl, alkoxy, CHO, COOH, alkylcarbonyl, alkoxycarbonyl, CF 3, halo, CN, OH, NH 2, alkylamino, CONH 2 or NO 2 (where alkyl is os by 1-3 halo, NH 2, alkylamino, OH or aryl), or Q + Q : a group completing a fused 1,3-dioxolan, cyclopentane or cyclohexane ring; R 1>-R 3>H, alkyl, alkoxy, CN, halo, NO 2 or CF 3, or two of R 1>-R 3>a group completing a fused 1,3-dioxolan, cyclopentane or cyclohexane ring, and R 4>, R 5>H or alkyl, or R 4> and R 5> on opposite C atoms : CH 2, CHMe or CMe 2 bridge. provided that R 1>-R 3> are not all H. An independent claim is included for the preparation of (I). ACTIVITY : Virucide. In tests for effectiveness against human cytomegalovirus (HCMV) infections in human foreskin fibroblast cultures, 2-(2-(4-(4-fluoro-3-methylphenyl)-1-piperazinyl)-3-(3-trifluoromethyl)-phenyl)-3,4-dihydro-4-quinazolinyl)-acetic acid (Ia) had an antiviral EC 50 value of 0.027 mu M and a cytotoxic CC 5 0 value of 17 mu M (corresponding to a selectivity index of 630). MECHANISM OF ACTION : None given.

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