公开(公告)号：US20070265301A1

公开(公告)日：2007-11-15

申请号：US11569209

申请日：2005-05-20

申请人： Paul Edwards ,  Victor Matassa ,  Achim Feurer ,  Sonja Nordhoff ,  Silvia Cerezo-Galvez ,  Christian Rummey

发明人： Paul Edwards ,  Victor Matassa ,  Achim Feurer ,  Sonja Nordhoff ,  Silvia Cerezo-Galvez ,  Christian Rummey

IPC分类号： A61K31/404 ,  A61K31/47 ,  A61P3/10 ,  C07D209/04 ,  C07D215/00

CPC分类号： C07D217/16 ,  C07D217/14

摘要： The invention relates to compounds of formula (I), wherein Z, R1-8, n, A1, X1 and X2 have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.

摘要翻译： 本发明涉及式（I）化合物，其中Z，R 1-8，N，A 1，X 1和X 2， SUP> 2 具有在说明书和权利要求书中引用的含义。 所述化合物可用作DPP-IV抑制剂。 本发明还涉及这种化合物的制备以及其作为药物的生产和使用。

公开(公告)号：US20070265261A1

公开(公告)日：2007-11-15

申请号：US11569552

申请日：2005-06-08

申请人： Paul Edwards ,  Claudia Rosenbaum ,  Christian Rummey ,  Silvia Cerezo-Galvez ,  Achim Feurer ,  Oliver Hill ,  Meinolf Thiemann ,  Victor Matassa ,  Sonja Nordhoff ,  Barbara Hoffmann

发明人： Paul Edwards ,  Claudia Rosenbaum ,  Christian Rummey ,  Silvia Cerezo-Galvez ,  Achim Feurer ,  Oliver Hill ,  Meinolf Thiemann ,  Victor Matassa ,  Sonja Nordhoff ,  Barbara Hoffmann

IPC分类号： A61K31/4545 ,  A61K31/4525 ,  A61K31/5377 ,  A61P3/04 ,  C07D211/06 ,  C07D211/96 ,  C07D401/06 ,  C07D405/06 ,  C07D413/06

CPC分类号： C07D211/26

摘要： The invention relates to compounds of formula (1) wherein Z, R1-3 and A have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.

摘要翻译： 本发明涉及式（1）的化合物，其中Z，R 1-3和A具有在说明书和权利要求书中引用的含义。 所述化合物可用作DPP-IV抑制剂。 本发明还涉及这种化合物的制备以及其作为药物的生产和使用。

公开(公告)号：US07410982B2

公开(公告)日：2008-08-12

申请号：US10532765

申请日：2003-10-24

申请人： Serge Louis Boulet ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Kevin John Hudziak ,  Anette Margareta Johansson ,  Rushad E. Karanjawala ,  John Joseph Masters ,  Brian Michael Mathes ,  Richard Edmund Rathmell ,  Maria Ann (nee Fagan) Whatton ,  Victor Matassa ,  Chad Nolan Wolfe

发明人： Serge Louis Boulet ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Kevin John Hudziak ,  Anette Margareta Johansson ,  Rushad E. Karanjawala ,  John Joseph Masters ,  Brian Michael Mathes ,  Richard Edmund Rathmell ,  Maria Ann (nee Fagan) Whatton ,  Victor Matassa ,  Chad Nolan Wolfe

IPC分类号： A61K31/4365 ,  C07D409/02

CPC分类号： C07D275/04 ,  C07D215/20 ,  C07D217/02 ,  C07D217/04 ,  C07D217/24 ,  C07D277/62 ,  C07D333/54 ,  C07D471/04 ,  C07D495/04

摘要： There is provided a heretoaryloxy/thio 3-substituted propanamine compound of formula (I) wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl —S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, and thienopyridyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro acetyl, —CF3, —SCF3 and cyano; Z is selected from H, OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof.

公开(公告)号：US20070299103A1

公开(公告)日：2007-12-27

申请号：US11791799

申请日：2005-12-01

申请人： Ulrich Abel ,  Holger Deppe ,  Achim Feurer ,  Ulrich Gradler ,  Inge Ott ,  Victor Matassa

发明人： Ulrich Abel ,  Holger Deppe ,  Achim Feurer ,  Ulrich Gradler ,  Inge Ott ,  Victor Matassa

IPC分类号： A61K31/44 ,  A61P35/00 ,  C07D471/02

CPC分类号： C07D471/04

摘要： The invention provides novel, substituted 7-arylamino[1,2,4]triazolo[4,3-a]pyridine compounds Formula (I): pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10 R11, R12, R13, R14 and L are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.

摘要翻译： 本发明提供新颖的取代的7-芳基氨基[1,2,4]三唑并[4,3-a]吡啶化合物式（I）：其药学上可接受的盐，溶剂合物和前药化合物，其中W，R 1， R 1，R 2，R 9，R 10，R 11，R 12， R 13，R 13，R 14和L如说明书中所定义。 这些化合物是MEK抑制剂，可用于治疗过度增殖性疾病，如癌症，再狭窄和炎症。 还公开了这样的化合物在哺乳动物，特别是人类中过度增殖性疾病的治疗和含有这些化合物的药物组合物中的应用。

公开(公告)号：US20070099927A1

公开(公告)日：2007-05-03

申请号：US10576698

申请日：2004-10-12

申请人： Achim Feurer ,  Sara Bosio ,  Stephan Bulat ,  Silvia Cerezo-Galvez ,  Victor Matassa ,  Inge Ott ,  Michael Papadopoulos ,  Claudia Rosenbaum ,  Jens Schamberger ,  Gunther Metz

发明人： Achim Feurer ,  Sara Bosio ,  Stephan Bulat ,  Silvia Cerezo-Galvez ,  Victor Matassa ,  Inge Ott ,  Michael Papadopoulos ,  Claudia Rosenbaum ,  Jens Schamberger ,  Gunther Metz

IPC分类号： A61K31/497 ,  A61K31/4965 ,  A61K31/506 ,  A61K31/4745 ,  C07D403/02 ,  C07D401/02 ,  A61K31/4709

CPC分类号： C07D401/12 ,  C07D241/20 ,  C07D401/14 ,  C07D409/12 ,  C07D409/14

摘要： The invention relates to compounds of formula (I) wherein A, B, X, R1, R2, G, R3, D and E have the meaning as cited in the description and the claims. Said compounds are useful as coagulants. The invention also relates to the production and use thereof as medicament.

摘要翻译： 本发明涉及式（I）化合物，其中A，B，X，R 1，R 2，G，R 3，D 和E具有在说明书和权利要求书中引用的含义。 所述化合物可用作凝结剂。 本发明还涉及其作为药物的生产和使用。

公开(公告)号：US20060058360A1

公开(公告)日：2006-03-16

申请号：US10532765

申请日：2003-10-24

申请人： Serge Boulet ,  Sandra Filla ,  Peter Gallagher ,  Kevin Hudziak ,  Anette Johansson ,  Rushad Karanjawala ,  John Masters ,  Brian Mathes ,  Richard Rathmell ,  Maria Whatton ,  Victor Matassa ,  Chad Wolfe

发明人： Serge Boulet ,  Sandra Filla ,  Peter Gallagher ,  Kevin Hudziak ,  Anette Johansson ,  Rushad Karanjawala ,  John Masters ,  Brian Mathes ,  Richard Rathmell ,  Maria Whatton ,  Victor Matassa ,  Chad Wolfe

IPC分类号： A61K31/428 ,  A61K31/425 ,  C07D277/62 ,  C07D275/06

CPC分类号： C07D275/04 ,  C07D215/20 ,  C07D217/02 ,  C07D217/04 ,  C07D217/24 ,  C07D277/62 ,  C07D333/54 ,  C07D471/04 ,  C07D495/04

摘要： There is provided a heretoaryloxy/thio 3-substituted propanamine compound of formula (I) wherein A is selected from —)— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl —S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, and thienopyridyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro acetyl, —CF3, —SCF3 and cyano; Z is selected from H, OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof.

公开(公告)号：US20050075356A1

公开(公告)日：2005-04-07

申请号：US10493279

申请日：2002-10-21

申请人： Maria Di Francesco ,  Cristina Gardelli ,  Steven Harper ,  Victor Matassa ,  Ester Murgalia ,  Emanuela Nizi ,  Paola Pace ,  Barbara Pacini ,  Alessia Petrocchi ,  Marco Poma ,  Vincenzo Summa

发明人： Maria Di Francesco ,  Cristina Gardelli ,  Steven Harper ,  Victor Matassa ,  Ester Murgalia ,  Emanuela Nizi ,  Paola Pace ,  Barbara Pacini ,  Alessia Petrocchi ,  Marco Poma ,  Vincenzo Summa

IPC分类号： C07D239/54 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61K45/00 ,  A61K45/06 ,  A61P31/18 ,  A61P43/00 ,  C07D239/557 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/08 ,  C07D491/10

CPC分类号： C07D239/557 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/08 ,  C07D491/10

摘要： 4,5-Dihydroxypyrimidine-6-carboxamides of formula (I); are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

摘要翻译： 式（I）的4,5-二羟基嘧啶-6-甲酰胺; 被描述为HIV整合酶和HIV复制抑制剂的抑制剂，其中R 1，R 2，R 3和R 4在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及艾滋病的预防，延迟发作和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。 还描述了预防，治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。

公开(公告)号：US20080015146A1

公开(公告)日：2008-01-17

申请号：US11569938

申请日：2005-06-08

申请人： Paul Edwards ,  Silvia Cerezo-Galvez ,  Achim Feurer ,  Victor Matassa ,  Sonja Nordhoff ,  Stephan Bulat ,  Meritxell Lopez-Canet ,  Christian Rummey ,  Claudia Rosenbaum

发明人： Paul Edwards ,  Silvia Cerezo-Galvez ,  Achim Feurer ,  Victor Matassa ,  Sonja Nordhoff ,  Stephan Bulat ,  Meritxell Lopez-Canet ,  Christian Rummey ,  Claudia Rosenbaum

IPC分类号： A61K31/40 ,  A61K31/4245 ,  A61K31/4406 ,  A61K31/443 ,  A61K38/02 ,  A61K38/28 ,  A61P1/00 ,  A61P25/00 ,  A61P31/18 ,  A61P35/00 ,  A61P7/00 ,  C07D207/09 ,  C07D271/06 ,  C07D413/14

CPC分类号： C07D403/04 ,  C07D413/04 ,  C07D413/14

摘要： The invention relates to compounds of formula (I) wherein Z, R1-9, n, A, X and Rb have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.

摘要翻译： 本发明涉及式（I）化合物，其中Z，R 1〜9，n，A，X和R b具有说明书中引用的含义， 声称。 所述化合物可用作DPP-IV抑制剂。 本发明还涉及这种化合物的制备以及其作为药物的生产和使用。

公开(公告)号：US20070197522A1

公开(公告)日：2007-08-23

申请号：US10591108

申请日：2005-02-25

申请人： Paul Edwards ,  Achim Feurer ,  Silvia Cerezo-Galves ,  Victor Matassa ,  Sonja Nordhoff ,  Claudia Rosenbaum ,  Stephan Bulat

发明人： Paul Edwards ,  Achim Feurer ,  Silvia Cerezo-Galves ,  Victor Matassa ,  Sonja Nordhoff ,  Claudia Rosenbaum ,  Stephan Bulat

IPC分类号： A61K31/135 ,  A61K31/535 ,  C07C211/08 ,  C07D207/09 ,  C07D295/03

CPC分类号： C07D213/40 ,  C07C237/20 ,  C07C237/42 ,  C07C311/35 ,  C07C311/46 ,  C07C323/41 ,  C07C2602/08 ,  C07C2602/10 ,  C07D205/04 ,  C07D207/10 ,  C07D207/14 ,  C07D213/42 ,  C07D213/75 ,  C07D217/14 ,  C07D231/12 ,  C07D233/54 ,  C07D235/14 ,  C07D241/12 ,  C07D241/18 ,  C07D249/08 ,  C07D261/08 ,  C07D271/06 ,  C07D295/125 ,  C07D295/13 ,  C07D295/135 ,  C07D307/79 ,  C07D311/76 ,  C07D319/18 ,  C07D471/04

摘要： The invention relates to compounds of formula (I) Z-C(R1R2)—C(R3NH2)—C(R4R5)—X—N(R6R7)  (I), wherein Z, R1-7 and X have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.

摘要翻译： 本发明涉及式（I）化合物<？in-line-formula description =“In-line Formulas”end =“lead”→> ZC（R 1> 2 ）（C（R 3）NH 2）-C（R 4，R 5） - XN（R 4） （I），<？在线公式描述=“在线公式”end =“tail”？>其中Z，R < SUP> 1-7和X具有在说明书和权利要求书中引用的含义。 所述化合物可用作DPP-IV抑制剂。 本发明还涉及这种化合物的制备以及其作为药物的生产和使用。

公开(公告)号：US20070083045A1

公开(公告)日：2007-04-12

申请号：US11516831

申请日：2006-09-07

申请人： Maria Di Francesco ,  Cristina Gardelli ,  Steven Harper ,  Victor Matassa ,  Ester Murgalia ,  Emanuela Nizi ,  Paola Pace ,  Barbara Pacini ,  Alessia Petrocchi ,  Marco Poma ,  Vincenzo Summa

发明人： Maria Di Francesco ,  Cristina Gardelli ,  Steven Harper ,  Victor Matassa ,  Ester Murgalia ,  Emanuela Nizi ,  Paola Pace ,  Barbara Pacini ,  Alessia Petrocchi ,  Marco Poma ,  Vincenzo Summa

IPC分类号： C07D417/02 ,  C07D403/14 ,  C07D413/02

CPC分类号： C07D239/557 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/08 ,  C07D491/10

摘要： 4,5-Dihydroxypyrimidine-6-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

摘要翻译： 具有下式的4,5-二羟基嘧啶-6-甲酰胺被描述为HIV整合酶的抑制剂和HIV复制抑制剂，其中R 1，R 2，R 2， 3和R 4在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及艾滋病的预防，延迟发作和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。 还描述了预防，治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。