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1. 发明授权

US07488818B2 Method for producing 1,4-diphenyl azetidinone derivatives 有权
标题翻译： 1,4-二苯基氮杂环丁酮衍生物的制备方法
公开(公告)号：US07488818B2
公开(公告)日：2009-02-10
申请号：US11561626
申请日：2006-11-20
申请人： Andreas Lindenschmidt , David William Will , Gerhard Jaehne , Theodor Andreas Wollmann , Wendelin Frick , Bernd Junker , David Rigal , Guenter Billen , Heiner Jendralla
发明人： Andreas Lindenschmidt , David William Will , Gerhard Jaehne , Theodor Andreas Wollmann , Wendelin Frick , Bernd Junker , David Rigal , Guenter Billen , Heiner Jendralla
IPC分类号： C07D205/08 , C07F9/6503 , C07F9/6506 , C07F9/6541 , C07F9/653 , C07F9/572 , C07F9/54
CPC分类号： C07D205/08 , A61K31/33
摘要： The present invention is directed to the preparation of novel compounds useful in the treatment of hyperlipidemia, arteriosclerosis, hypercholesterolemia, and other related metabolic disorders. More specifically, the present invention is a novel process for the preparation of 1,4-diphenylazetidinone derivatives from β-substituted amino amides which are protected in the presence of silylating agents and at least one cyclization catalyst whose structural formula is represented by one of the general formula: wherein the various R-groups are defined herein.
摘要翻译：本发明涉及可用于治疗高脂血症，动脉硬化，高胆固醇血症和其它相关代谢紊乱的新化合物的制备。更具体地说，本发明是一种从β-取代氨基酰胺制备1,4-二苯基氮杂环丁酮衍生物的新方法，其在甲硅烷基化试剂和至少一种环化催化剂存在下被保护，其结构式由通式：其中各种R基团在本文中定义。

2. 发明授权

US08642620B2 Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals 有权
标题翻译：包含不饱和或环状连接基团的杂芳基取代的酰胺及其作为药物的用途
公开(公告)号：US08642620B2
公开(公告)日：2014-02-04
申请号：US11958503
申请日：2007-12-18
申请人： Harmut Strobel , Paulus Wohlfart , Gerhard Zoller , David William Will
发明人： Harmut Strobel , Paulus Wohlfart , Gerhard Zoller , David William Will
IPC分类号： A61K31/4545 , C07D401/06
CPC分类号： C07D401/14 , C07D401/06 , C07D401/08 , C07D409/14 , C07D417/06
摘要： The present invention relates to N-alkylamides of the formula I, in which A, Het, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
摘要翻译：本发明涉及式I的N-烷基酰胺，其中A，Het，X，R 1，R 2和R 3具有权利要求中所述的含义，其调节内皮一氧化氮（NO）合酶的转录并且是有价值的药理学活性化合物。具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下应用。本发明还涉及制备式I化合物的方法，包括它们的药物组合物，以及式I化合物在制备用于刺激内皮NO合成酶表达或用于治疗包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全等各种疾病。

3. 发明授权

US08304438B2 Heteroarylacrylamides and their use as pharmaceuticals 有权
标题翻译：杂芳基丙烯酰胺及其作为药物的用途
公开(公告)号：US08304438B2
公开(公告)日：2012-11-06
申请号：US12486117
申请日：2009-06-17
申请人： Hartmut Strobel , Paulus Wohlfart , Heinz-Werner Kleemann , Gerhard Zoller , David William Will
发明人： Hartmut Strobel , Paulus Wohlfart , Heinz-Werner Kleemann , Gerhard Zoller , David William Will
IPC分类号： C07D401/06 , A61K31/44
CPC分类号： C07D213/56 , C07D213/64 , C07D213/73 , C07D213/75 , C07D215/12 , C07D233/64 , C07D233/68 , C07D239/26 , C07D277/30 , C07D277/46 , C07D333/24 , C07D333/60 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/06 , C07D417/12
摘要： The present invention relates to heteroarylacrylamides of the formula I, in which Het, X, Ra, Rb, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
摘要翻译：本发明涉及式I的杂芳基丙烯酰胺，其中Het，X，Ra，Rb，R 1，R 2和R 3具有权利要求中所示的含义，其调节内皮一氧化氮（NO）合酶的转录并且是有价值的药理学活性化合物。具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下应用。本发明还涉及制备式I化合物的方法，包括它们的药物组合物，以及式I化合物在制备用于刺激内皮NO合成酶表达或用于治疗包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全等各种疾病。

4. 发明授权

US07968546B2 Pyridazinone kinase inhibitors 失效
标题翻译：哒嗪酮激酶抑制剂
公开(公告)号：US07968546B2
公开(公告)日：2011-06-28
申请号：US12359754
申请日：2009-01-26
申请人： Swen Hoelder , Gunter Muller , Karl Schoenafinger , David William Will , Hans Matter , Martin Bossart , Cecile Combeau , Christine Delaisi , Ingrid Sassoon , Anke Steinmetz , Didier Benard
发明人： Swen Hoelder , Gunter Muller , Karl Schoenafinger , David William Will , Hans Matter , Martin Bossart , Cecile Combeau , Christine Delaisi , Ingrid Sassoon , Anke Steinmetz , Didier Benard
IPC分类号： C07D401/04 , A61K31/501 , A61P29/00 , A61P7/12 , A61P3/10 , A61P25/28 , A61P35/00
CPC分类号： C07D403/04 , C07D401/14
摘要： Disclosed are compounds of Formula I wherein X is and R2, R1, A, B, D, E, R9 are as defined herein useful for treating cancers.
摘要翻译：公开了式I的化合物，其中X和R 2，R 1，A，B，D，E，R 9如本文所定义，可用于治疗癌症。

5. 发明授权

US07462613B2 Pyridazinone derivatives as pharmaceuticals and pharmaceutical compositions containing them 失效
标题翻译：哒嗪酮衍生物作为药物和含有它们的药物组合物
公开(公告)号：US07462613B2
公开(公告)日：2008-12-09
申请号：US10715556
申请日：2003-11-19
申请人： Swen Hölder , Thorsten Naumann , Karl Schönafinger , David William Will , Hans Matter , Günther Müller , Dominique Le Suisse , Bernard Baudoin , Thomas Rooney , Franck Halley , Gilles Tiraboschi , Cécile Combeau , Ingrid Sassoon , Anke Steinmetz
发明人： Swen Hölder , Thorsten Naumann , Karl Schönafinger , David William Will , Hans Matter , Günther Müller , Dominique Le Suisse , Bernard Baudoin , Thomas Rooney , Franck Halley , Gilles Tiraboschi , Cécile Combeau , Ingrid Sassoon , Anke Steinmetz
IPC分类号： C07D403/02 , A61K31/501
CPC分类号： C07D401/04 , C07D237/14
摘要： The present invention relates to novel pyridazinone derivatives of the general formula (I) wherein A is A1 or A2; R is unsubstituted or at least monosubstituted C1-C10-alkyl, aryl, aryl-(C1-C10-alkyl)-, heteroaryl, heteroaryl-(C1-C10-alkyl)-, heterocyclyl, heterocyclyl-(C1-C10-alkyl)-, C3-C10-cycloalkyl, polycycloalkyl, C2-C10-alkenyl or C2-C10-alkinyl and Ar is unsubstituted or at least monosubstituted aryl or heteroaryl.
摘要翻译：本发明涉及通式（I）的新的哒嗪酮衍生物，其中A为A 1或A 2; R是未取代的或至少单取代的C 1 -C 10 - 烷基，芳基，芳基 - （C 1 -C 10 - 烷基） - ，杂芳基，杂芳基 - （C 1 -C 10 - 烷基） - ，杂环基，杂环基 - （C 1 -C 10 - 烷基） C 3 -C 10 - 环烷基，多环烷基，C 2 -C 10 - 烯基或C 2 -C 10 - 炔基，Ar是未取代的或至少单取代的芳基或杂芳基。

6. 发明授权

US06747148B2 Sulfonamide derivatives as inhibitors of bone resorption and as inhibitors of cell adhesion 失效
标题翻译：磺酰胺衍生物作为骨吸收抑制剂和细胞粘附抑制剂
公开(公告)号：US06747148B2
公开(公告)日：2004-06-08
申请号：US09972190
申请日：2001-10-09
申请人： Anuschirwan Peyman , David William Will , Jochen Knolle , Karlheinz Scheunemann , Denis Carniato , Jean-Francois Gourvest , Thomas R. Gadek , Robert McDowell , Sarah Catherine Bodary , Robert Andrew Cuthbertson
发明人： Anuschirwan Peyman , David William Will , Jochen Knolle , Karlheinz Scheunemann , Denis Carniato , Jean-Francois Gourvest , Thomas R. Gadek , Robert McDowell , Sarah Catherine Bodary , Robert Andrew Cuthbertson
IPC分类号： C07C211119
CPC分类号： C07D409/12 , C07D239/16
摘要： Sulfonamide derivatives, their physiologically tolerable salts and their prodrugs according to the present invention are vitronectin receptor antagonists and inhibitors of cell adhesion, as well as inhibit bone resorption by osteoclasts. These derivatives, salts and prodrugs are pharmaceutically active compounds useful in the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. Processes for the preparation of the sulfonamide derivatives according to the present invention, the use of these derivatives as pharmaceutically active ingredients, and pharmaceutical preparations comprising these derivatives also are disclosed.
摘要翻译：根据本发明的磺酰胺衍生物，其生理上可耐受的盐及其前药是玻连蛋白受体拮抗剂和细胞粘附抑制剂，以及抑制破骨细胞的骨吸收。这些衍生物，盐和前药是用于治疗和预防由至少部分由不期望的骨吸收程度引起的疾病的药物活性化合物，例如骨质疏松症。本发明的磺酰胺衍生物的制备方法，这些衍生物作为药物活性成分的用途，以及包含这些衍生物的药物制剂也被公开。

7. 发明授权

US06566366B1 Thienyl substituted acylguanidines as inhibitors of bone resorption and vitronectin receptor antagonists 有权
标题翻译：噻吩基取代的酰基胍被用作骨吸收抑制剂和玻连蛋白受体拮抗剂
公开(公告)号：US06566366B1
公开(公告)日：2003-05-20
申请号：US09700655
申请日：2001-03-06
申请人： Karl-Heinz Scheunemann , Jochen Knolle , Amuschirwan Peyman , David William Will , Denis Carniato , Jean-Francois Gourvest , Thomas Gadek , Robert McDowell , Sarah Catherine Bodary , Robert Andrew Cuthbertson
发明人： Karl-Heinz Scheunemann , Jochen Knolle , Amuschirwan Peyman , David William Will , Denis Carniato , Jean-Francois Gourvest , Thomas Gadek , Robert McDowell , Sarah Catherine Bodary , Robert Andrew Cuthbertson
IPC分类号： A61K31505
CPC分类号： C07D409/12 , C07D333/24 , C07D409/14
摘要： Compounds of the formula and salts thereof wherein the substituents are defined as in accordance with the specification useful for the treatment of tumor growth, osteoporosis, inflammation and cardiovascular disorders.
摘要翻译：式及其盐的化合物，其中取代基根据可用于治疗肿瘤生长，骨质疏松症，炎症和心血管疾病的说明书定义。

8. 发明授权

US08188291B2 Heteroaryl-substituted carboxamides and their use as pharmaceuticals 有权
标题翻译：杂芳基取代的甲酰胺及其作为药物的用途
公开(公告)号：US08188291B2
公开(公告)日：2012-05-29
申请号：US12486144
申请日：2009-06-17
申请人： Hartmut Strobel , Paulus Wohlfart , Heinz-Werner Kleemann , Gerhard Zoller , David William Will
发明人： Hartmut Strobel , Paulus Wohlfart , Heinz-Werner Kleemann , Gerhard Zoller , David William Will
IPC分类号： C07D213/62 , C07D417/00 , C07D285/08 , A61K31/44 , A61K31/415
CPC分类号： C07D409/06 , C07D213/56 , C07D213/65 , C07D213/74 , C07D213/89 , C07D239/26 , C07D271/113 , C07D277/36 , C07D277/46 , C07D285/135 , C07D333/24 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12
摘要： The present invention relates to heteroaryl-substituted carboxamides of the formula I, in which Het, A, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
摘要翻译：本发明涉及式I的杂芳基取代的甲酰胺，其中Het，A，X，R 1，R 2和R 3具有权利要求所述的含义，其调节内皮一氧化氮（NO）合酶的转录并且是有价值的药理活性化合物。具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下应用。本发明还涉及制备式I化合物的方法，包括它们的药物组合物，以及式I化合物在制备用于刺激内皮NO合成酶表达或用于治疗包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全等各种疾病。

9. 发明授权

US08044050B2 Imidazo[1,2-a]azines and their use as pharmaceuticals 有权
标题翻译：咪唑并[1,2-a]吖嗪及其作为药物的用途
公开(公告)号：US08044050B2
公开(公告)日：2011-10-25
申请号：US12548641
申请日：2009-08-27
申请人： Gerhard Zoller , Hartmut Strobel , David William Will , Paulus Wohlfart
发明人： Gerhard Zoller , Hartmut Strobel , David William Will , Paulus Wohlfart
IPC分类号： A61K31/5025 , A61K31/519 , C07D487/04
CPC分类号： C07D487/04 , A61K31/4188 , A61K31/4985 , A61K31/5025 , A61K31/519
摘要： The present invention relates to derivatives of imidazo[1,2-a]azines of formula I, in which R, R1 to R3, X, Y and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of formula I, to pharmaceutical compositions comprising them, and to the use of compounds of formula I for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
摘要翻译：本发明涉及式I的咪唑并[1,2-a]吖嗪衍生物，其中R，R 1至R 3，X，Y和n具有权利要求中所示的含义，其调节内皮一氧化氮的转录（ NO）合酶，是有价值的药理活性化合物。具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下使用。本发明还涉及制备式I化合物的方法，包含它们的药物组合物，以及式I化合物用于刺激内皮NO合成酶表达或用于治疗各种疾病，包括心血管疾病例如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全。

10. 发明授权

US07910606B2 Pyrazole-derivatives as factor Xa inhibitors 有权
标题翻译：吡唑衍生物作为因子Xa抑制剂
公开(公告)号：US07910606B2
公开(公告)日：2011-03-22
申请号：US12562276
申请日：2009-09-18
申请人： Marc Nazare , Volkmar Wehner , David William Will , Hans Matter
发明人： Marc Nazare , Volkmar Wehner , David William Will , Hans Matter
IPC分类号： A61K31/454 , A61K31/415 , A61K31/4245 , C07D413/02 , C07D419/02 , C07D401/04
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D409/14 , C07D417/14
摘要： The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is a pharmacologically active compound. It exhibits a strong anti-thrombotic effect and is suitable, for example, for the therapy and prophylaxis of a cardio-vascular disorder like a thromboembolic disease or restenosis. It is a reversible inhibitor of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore is directed to a process for the preparation of the compound of formula I, and pharmaceutical preparation comprising it.
摘要翻译：本发明涉及式I化合物，其中R 0; R1; R2; R3; R4; Q; V，G和M具有以下含义。式I化合物是药理活性化合物。它表现出强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。它是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可以在其中存在因子Xa和/或因子VIIa的不希望的活性或对于治疗或预防因素Xa和/或因子VIIa的抑制。本发明还涉及制备式I化合物的方法和包含其的药物制剂。

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