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37 条记录 (耗时 0.036 秒)

    Guanidine and amidine derivatives as factor Xa inhibitors
    1.
    发明授权
    Guanidine and amidine derivatives as factor Xa inhibitors 失效
    胍和脒衍生物作为因子Xa抑制剂

    公开(公告)号：US07435747B2

    公开(公告)日：2008-10-14

    申请号：US10886312

    申请日：2004-07-07

    申请人： Anuschirwan Peyman ,  David William Will ,  Uwe Gerlach ,  Marc Nazaré ,  Gerhard Zoller ,  Hans-Peter Nestler ,  Hans Matter ,  Fahad Al-Obeidi

    发明人： Anuschirwan Peyman ,  David William Will ,  Uwe Gerlach ,  Marc Nazaré ,  Gerhard Zoller ,  Hans-Peter Nestler ,  Hans Matter ,  Fahad Al-Obeidi

    IPC分类号： A61K31/445 ,  C07D211/26

    CPC分类号： C07D401/12 ,  C07D211/26 ,  C07D211/34

    摘要： The present invention relates to compounds of the formula I, in which R0; Q; X; Q′, D, R10 and V have the meanings indicated in the claims. The compounds of the 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 intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

    摘要翻译： 本发明涉及式I化合物，其中R 0是 Q; X; Q'，D，R 10和V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 或预防因子Xa和/或因子VIIa的抑制。 本发明还涉及式I化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

    Modified antisense nucleotides complementary to a section of the human Ha-ras gene
    6.
    发明授权
    Modified antisense nucleotides complementary to a section of the human Ha-ras gene 失效
    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。

    Guanidine derivatives as inhibitors of cell adhesion
    7.
    发明授权
    Guanidine derivatives as inhibitors of cell adhesion 有权
    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。

    Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals
    9.
    发明授权
    Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals 有权
    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。

    Heteroarylacrylamides and their use as pharmaceuticals
    10.
    发明授权
    Heteroarylacrylamides and their use as pharmaceuticals 有权
    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。