专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US08399476B2 Imidazo[1,2-a]pyridines and their use as pharmaceuticals 有权
标题翻译：咪唑并[1,2-a]吡啶及其作为药物的用途
公开(公告)号：US08399476B2
公开(公告)日：2013-03-19
申请号：US12548636
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： A01N43/42 , A61K31/44 , C07D491/02 , C07D498/02
CPC分类号： C07D471/04
摘要： The present invention relates to derivatives of imidazo[1,2-a]pyridines of formula I, in which R, R1 to R4 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]吡啶衍生物，其中R，R 1至R 4和n具有权利要求中所示的含义，其调节内皮一氧化氮（NO）合酶的转录和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。

2. 发明授权

US08080569B2 Imidazo[2,1-b]thiazoles and their use as pharmaceuticals 有权
标题翻译：咪唑并[2,1-b]噻唑及其作为药物的用途
公开(公告)号：US08080569B2
公开(公告)日：2011-12-20
申请号：US12466576
申请日：2009-05-15
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： A61K31/429 , C07D513/04
CPC分类号： C07D513/04
摘要： The present invention relates to derivatives of imidazo[2,1-b]thiazoles of formula I, in which R, R1 to R3 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 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的咪唑并[2,1-b]噻唑衍生物，其中R，R 1至R 3和n具有权利要求中所示的含义，其调节内皮一氧化氮（NO）合酶的转录和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，包含它们的药物组合物，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的药物中的用途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. 发明申请

US20100004299A1 Imidazo[2,1-b]thiazoles and their use as pharmaceuticals 有权
标题翻译：咪唑并[2,1-b]噻唑及其作为药物的用途
公开(公告)号：US20100004299A1
公开(公告)日：2010-01-07
申请号：US12466576
申请日：2009-05-15
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： A61K31/429 , C07D513/04 , A61P9/10
CPC分类号： C07D513/04
摘要： The present invention relates to derivatives of imidazo[2,1-b]thiazoles of formula I, in which R, R1 to R3 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 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的咪唑并[2,1-b]噻唑衍生物，其中R，R 1至R 3和n具有权利要求中所示的含义，其调节内皮一氧化氮（NO）合酶的转录和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化合物在制备用于刺激内皮NO合成酶表达或用于治疗的药物中的用途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. 发明申请

US20090069565A1 NEW INDOLE DERIVATIVES AS FACTOR XA INHIBITORS 审中-公开
标题翻译：作为因子XA抑制剂的新型吲哚衍生物
公开(公告)号：US20090069565A1
公开(公告)日：2009-03-12
申请号：US12119013
申请日：2008-05-12
申请人： Mark NAZARE , Melanie Essrich , David William WILL , Hans MATTER , Kurt RITTER , Volkmar WEHNER
发明人： Mark NAZARE , Melanie Essrich , David William WILL , Hans MATTER , Kurt RITTER , Volkmar WEHNER
IPC分类号： C07D401/06 , C07D209/34
CPC分类号： C07D413/14 , C04B35/632 , C07D209/22 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D417/14
摘要： The present invention relates to compounds of formula I, in which R0; R1; R2; R3; R4; R5; R6; R7; Q; V, G and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors 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 indicated. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as pharmaceuticals for treating the foregoing conditions, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式I化合物，其中R 0; R1; R2; R3; R4; R5; R6; R7; Q; V，G和M具有权利要求中所示的含义。式I的化合物是有价值的药理活性化合物。它们具有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。它们是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIIa的不期望活性或用于治愈或预防因素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，其用途，特别是作为用于治疗上述病症的药物，以及包含它们的药物制剂。

5. 发明授权

US07470689B2 4-benzimidazol-2-ylpyridazin-3-one derivatives 失效
标题翻译： 4-苯并咪唑-2-基哒嗪-3-酮衍生物
公开(公告)号：US07470689B2
公开(公告)日：2008-12-30
申请号：US11513574
申请日：2006-08-31
申请人： Swen Hoelder , Karl Schoenafinger , David William Will , Hans Matter , Günter Müller , Cécile Combeau , Christine Delaisi , Anke Steinmetz , Ingrid Sassoon
发明人： Swen Hoelder , Karl Schoenafinger , David William Will , Hans Matter , Günter Müller , Cécile Combeau , Christine Delaisi , Anke Steinmetz , Ingrid Sassoon
IPC分类号： A61K31/501 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D471/04 , C07D401/14 , A61K31/53 , C07D487/04 , A61P35/00
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D471/04
摘要： Disclosed are compounds of the general formula (I), where the definition of the substituents A, B, D, E, R1 and R2 are detailed in the description, and the physiologically tolerated salts thereof, a process for the preparation of these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).
摘要翻译：公开了通式（I）的化合物，其中取代基A，B，D，E，R 1和R 2的定义在说明书中详细描述，以及其生理上可耐受的盐，这些化合物的制备方法和它们用作药物。这些化合物是激酶抑制剂，特别是激酶CDK2（细胞周期蛋白依赖性激酶2）的抑制剂。

6. 发明申请

US20080171739A1 Heteroaryl-Substituted Amides Comprising A Saturated Linker Group, And Their Use As Pharmaceuticals 有权
标题翻译：包含饱和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：US20080171739A1
公开(公告)日：2008-07-17
申请号：US11958483
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： A61K31/541 , C07D401/06 , A61K31/444 , A61P9/00 , A61K31/4545
CPC分类号： C07D213/40 , C07D213/65 , C07D277/42 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/06 , C07D417/06 , C07D417/12
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。

7. 发明授权

US06723706B2 Modified antisense nucleotides complementary to a section of the human Ha-ras gene 失效
标题翻译：与人Ha-ras基因的一部分互补的修饰的反义核苷酸
公开(公告)号：US06723706B2
公开(公告)日：2004-04-20
申请号：US09423198
申请日：2000-02-17
申请人： Eugen Uhlmann , Anuschirwan Peyman , David William Will , Esther Chang , Kathleen Pirollo , Antonina Rait
发明人： Eugen Uhlmann , Anuschirwan Peyman , David William Will , Esther Chang , Kathleen Pirollo , Antonina Rait
IPC分类号： A61K4800
CPC分类号： C07H21/02 , A61K38/00 , C12N15/1135 , C12N2310/11 , C12N2310/315 , C12N2310/322 , C12N2310/345 , C12N2310/351 , C12N2310/3531
摘要： The invention relates to a specific modified oligonucleotide complementary to a section of the human Ha-ras gene and mRNA, and its use to specifically regulate, modulate or inhibit expression of the HA-ras gene, and its use as a pharmaceutical for the treatment of conditions arising from the abnormal expression of the Ha-Ras gene, in particular in combination with chemotherapy and radiotherapy. The modified oligodeoxynucleotide according to the invention has the sequence 5′-TxAxTxTxCxCxGxTxCxAxT-3′-O—PO2—O—R (SEQ ID NO:1), wherein X is an internucleotide linkage of type o or s, with the proviso that x is an s linkage at least 4 times and at most 9 times, and o means a phosphodiester internucleoside linkage, s means a phosphorothioate internucleoside linkage, R means a C8-C21 alkyl group, —(CH2—CH2O)n-(CH2)m—CH3, or —CH2—CH(OH)CH2O—(CH2)q—CH3 wherein n is an integer from 1 to 6, m is an integer from 0 to 20 and q is an integer from 7 to 20 and A is 2′-deoxyadenosine, G is 2′-deoxyguanosine, C is 2′-deoxycytidine and T is thymidine.
摘要翻译：本发明涉及与人Ha-ras基因和mRNA的部分互补的特异性修饰寡核苷酸及其用于特异性调节，调节或抑制HA-ras基因表达的用途及其作为治疗用途的药物的用途 Ha-Ras基因异常表达引起的病情，特别是与化疗和放疗相结合。根据本发明的修饰的寡脱氧核苷酸具有序列5'-TxAxTxTxCxCxGxTxCxAxT-3'-O-PO2-OR（SEQ ID NO：1），其中X是o或s型的核苷酸间键，条件是x是 s是至少4次，最多9次，o表示磷酸二酯核苷间键，s表示硫代磷酸酯核苷间键，R表示C8-C21烷基， - （CH2-CH2O）n-（CH2）m-CH3 ，或-CH 2 -CH（OH）CH 2 O-（CH 2）q -CH 3，其中n为1至6的整数，m为0至20的整数，q为7至20的整数，A为2'- 脱氧腺苷，G为2'-脱氧鸟苷，C为2'-脱氧胞苷，T为胸苷。

8. 发明授权

US06340679B1 Guanidine derivatives as inhibitors of cell adhesion 有权
标题翻译：胍衍生物作为细胞粘附抑制剂
公开(公告)号：US06340679B1
公开(公告)日：2002-01-22
申请号：US09502577
申请日：2000-02-11
申请人： Anuschirwan Peyman , Jochen Knolle , Karl-Heinz Scheunemann , David William Will , Denis Carniato , Jean-Francois Gourvest , Thomas R. Gadek , Sarah Catherine Bodary
发明人： Anuschirwan Peyman , Jochen Knolle , Karl-Heinz Scheunemann , David William Will , Denis Carniato , Jean-Francois Gourvest , Thomas R. Gadek , Sarah Catherine Bodary
IPC分类号： C07D23916
CPC分类号： C07D409/12 , C07D239/16
摘要： The present invention relates to acylguanidine derivatives of the formula I in which R1, R2, R4, Ar, X and n have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of the formula I are valuable pharmacologically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion. They inhibit, for example, bone resorption by osteoclasts and are suitable for the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example osteoporosis. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceutical preparations, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式Iin的酰基胍衍生物，其中R 1，R 2，R 4，Ar，X和n具有权利要求中所示的含义，其生理上可耐受的盐及其前药。式I的化合物是有价值的药理活性化合物。它们是玻连蛋白受体拮抗剂和细胞粘附抑制剂。它们抑制例如破骨细胞的骨吸收，并且适用于治疗和预防至少部分由不期望的骨吸收程度引起的疾病，例如骨质疏松症。本发明还涉及制备式I化合物的方法，其用途，特别是作为药物制剂中的活性成分，以及包含它们的药物制剂。

9. 发明授权

US06313119B1 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：US06313119B1
公开(公告)日：2001-11-06
申请号：US09564988
申请日：2000-05-05
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： A61K31192
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。

10. 发明授权

US5817811A Process for preparing substituted N-ethyglycine derivatives 失效
标题翻译：制备取代的N-乙基甘氨酸衍生物的方法
公开(公告)号：US5817811A
公开(公告)日：1998-10-06
申请号：US707149
申请日：1996-09-03
申请人： Gerhard Breipohl , Eugen Uhlmann , David William Will
发明人： Gerhard Breipohl , Eugen Uhlmann , David William Will
IPC分类号： C07D473/00 , C07C231/02 , C07C237/22 , C07K5/078 , C07K14/00 , C07D239/02 , C07D487/00
CPC分类号： C07K5/06139 , C07K14/003 , Y02P20/55
摘要： Processes are described for preparing substituted N-ethylglycine derivatives of the formula ##STR1## in which PG is an amino protecting group which is labile towards weak acids and is of the urethane type or the trityl type, X is NH or O, and B' represents bases which are customary in nucleotide chemistry and whose exocyclic amino and/or hydroxyl groups are protected by suitable known protecting groups, and the salts thereof.
摘要翻译：描述了制备式（I）的取代的N-乙基甘氨酸衍生物的方法，其中PG是对弱酸不稳定的氨基保护基，并且是氨基甲酸酯型或三苯甲基型，X是NH或O，并且B'表示在核苷酸化学中常规的碱基，其外环氨基和/或羟基被合适的已知保护基保护，及其盐。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式