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26 条记录 (耗时 0.026 秒)

    Cytidine nucleoside compound
    1.
    发明授权
    Cytidine nucleoside compound 失效
    胞苷核苷化合物

    公开(公告)号：US4096324A

    公开(公告)日：1978-06-20

    申请号：US654019

    申请日：1976-01-30

    申请人： Robert C. Kelly ,  William J. Wechter

    发明人： Robert C. Kelly ,  William J. Wechter

    IPC分类号： C07H19/06 ,  C07H19/08

    CPC分类号： C07H19/06 ,  Y02P20/55 ,  Y10S514/908

    摘要： 5'-Esters of ara-cytidine (1-.beta.-D-arabinofuranosylcytosine) are prepared by reacting ara-cytidine with .beta.,.beta.,.beta.-trihaloethoxycarbonyl halide or other protective agency to form a protective amido group on the primary amino nitrogen of ara-cytidine and then reacting the thus-protected compound with a reagent reactive with the 5'-O-hydroxyl group, e.g., an acylating agent, to form the 5'-O-derivative. The .beta.,.beta.,.beta.-trihaloethoxycarbonyl or other protective group is then removed. Alternately, the primary amino group of ara-cytidine can be protected from acylation by protonation. The 5'-O-derivatives in their free base of salt form are characterized in that they display the property of sustained release of the compound, ara-cytidine, when administered intramuscularly or subcutaneously. Ara-cytidine is known for its anti-viral action and for its usefulness as an agent for controlling leukemias, including acute leukemia, and the sustained release property extends the usefulness of ara-cytidine for these purposes and as an inmunosuppressive agent. The 5'-O-derivartives of this invention can also be administered orally.

    摘要翻译： 5'-阿糖胞苷（1-β-D-阿拉伯呋喃糖基胞嘧啶）的酯通过ara-cytidine与β，β，β-三卤代乙氧基羰基卤化物或其它保护性物质反应，在ara的伯氨基氮上形成保护性酰氨基 - 胞苷，然后使由此保护的化合物与可与5'-O-羟基反应的试剂，例如酰化剂反应，形成5'-O-衍生物。 然后除去β，β，β-三卤乙氧羰基或其它保护基。 或者，可以通过质子化保护ara-cytidine的伯氨基酰化。 其盐形式的游离碱中的5'-O-衍生物的特征在于，当肌内或皮下给药时，它们显示化合物ara-cytidine的持续释放的性质。 阿拉胞苷由于其抗病毒作用以及作为用于控制白血病（包括急性白血病）的药剂的有效性而已知，并且持续释放特性延长了阿糖胞苷用于这些目的和作为无菌抑制剂的用途。 本发明的5'-O-衍生物也可以口服给药。

    Organic compounds and compositions of ara-cytidine
    2.
    发明授权
    Organic compounds and compositions of ara-cytidine 失效
    有机化合物和ARA-CYTIDINE的组合物

    公开(公告)号：US4145414A

    公开(公告)日：1979-03-20

    申请号：US832965

    申请日：1977-09-13

    申请人： Robert C. Kelly ,  William J. Wechter

    发明人： Robert C. Kelly ,  William J. Wechter

    IPC分类号： C07H19/06 ,  C07H17/00 ,  A61K31/70

    CPC分类号： C07H19/06 ,  Y02P20/55 ,  Y10S514/908

    摘要： 5'-Esters of ara-cytidine (1-.beta.-D-arabinofuranosylcytosine) are prepared by reacting ara-cytidine with .beta.,.beta.,.beta.-trihaloethoxycarbonyl halide or other protective agency to form a protective amido group on the primary amino nitrogen of ara-cytidine and then reacting the thus-protected compound with a reagent reactive with the 5'-O-hydroxyl group, e.g., an acylating agent, to form the 5'-O-derivative. The .beta.,.beta.,.beta.-trihaloethoxycarbonyl or other protective group is then removed. Alternately, the primary amino group of ara-cytidine can be protected from acylation by protonation. The 5'-O-derivatives in their free base or salt form are characterized in that they display the property of sustained release of the compound, ara-cytidine, when administered intramuscularly or subcutaneously. Ara-cytidine is known for its anti-viral action and for its usefulness as an agent for controlling leukemias, including acute leukemia, and the sustained release property extends the usefulness of ara-cytidine for these purposes and as an immunosuppressive agent. The 5'-O-derivatives of this invention can also be administered orally.

    R-NSAID esters and their use
    3.
    发明授权
    R-NSAID esters and their use 失效
    R-NSAID酯及其用途

    公开(公告)号：US07074826B2

    公开(公告)日：2006-07-11

    申请号：US10678430

    申请日：2003-10-03

    申请人： William J. Wechter ,  Elaine Benaksas Schwartz

    发明人： William J. Wechter ,  Elaine Benaksas Schwartz

    IPC分类号： A61K31/341 ,  A61K31/216 ,  C07D307/62 ,  C07C69/612

    CPC分类号： C07D405/04 ,  C07D307/62 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D487/04 ,  C07D491/04

    摘要： The present invention concerns esters of R-enantiomers of a non-steroidal anti-inflammatory drug, which is substantially free from the S-enantiomer. The compounds of the invention may be used in treating a disease or illness in a mammal. To this end, a composition comprising a compound mentioned above, or a pharmaceutically acceptable salt thereof where salt formation occurs, is administered to the mammal in an amount sufficient to elicit a chemopreventative effect or a chemoprotective effect or a therapeutic effect or a prophylactic effect.

    摘要翻译： 本发明涉及基本上不含S-对映异构体的非甾族抗炎药的R-对映体的酯。 本发明的化合物可用于治疗哺乳动物的疾病或疾病。 为此，将含有上述化合物或其药学上可接受的盐形成的组合物以足以引发化学预防作用或化学保护作用或治疗效果或预防效果的量施用给哺乳动物。

    3-Cyano thiophen-2-yl oxamic acid and derivatives
    5.
    发明授权
    3-Cyano thiophen-2-yl oxamic acid and derivatives 失效
    3-氰基噻吩-2-基氨基甲酸及其衍生物

    公开(公告)号：US3953468A

    公开(公告)日：1976-04-27

    申请号：US451509

    申请日：1974-03-15

    申请人： William J. Wechter ,  John B. Wright

    发明人： William J. Wechter ,  John B. Wright

    IPC分类号： C07D333/38 ,  C07D333/24

    CPC分类号： C07D333/38

    摘要： Compounds represented below ##SPC1##And pharmaceutical compositions thereof are useful in the prophylactic treatment of mammals for allergy and all anaphylactic reactions of a reagin or non-reagin mediated nature.

    摘要翻译： 其代表的化合物及其药物组合物可用于哺乳动物用于过敏反应和非依赖性介导的自然反应的所有神经酰胺反应的主动物的预处理。

    Method for treatment of inflammation with R-NSAIDS
    6.
    发明授权
    Method for treatment of inflammation with R-NSAIDS 失效
    药物组合物和治疗炎症的方法

    公开(公告)号：US06472433B2

    公开(公告)日：2002-10-29

    申请号：US09797022

    申请日：2001-03-01

    申请人： William J. Wechter

    发明人： William J. Wechter

    IPC分类号： A61K3119

    CPC分类号： A61K31/192 ,  A61K31/381 ,  A61K31/402 ,  A61K31/403 ,  A61K31/407 ,  A61K31/423

    摘要： This invention relates to the use of enantiomerically pure R-NSAIDs for the treatment of inflammation. Preferably, the R-NSAID used is R-flurbiprofen and is administered in a dose of at least 5 milligrams per kilogram of body weight per day. The anti-inflammatory action of R-NSAIDs is due to their ability to interfere with the biosynthesis of COX-2 by inhibiting COX-2 mRNA synthesis, rather than by just blocking the action of the enzyme itself. In order to effect the inhibition of COX-2 mRNA synthesis, the R-NSAID must be present at relatively high doses. Because the R-NSAID is selective in its action, that is, it does not inhibit either COX-1 mRNA synthesis or the COX-1 enzyme itself, it can be administered in the required high doses because the tissue protective effects of prostaglandins made through the COX-1 pathway are not interfered with.

    摘要翻译： 本发明涉及对映异构体纯的R-NSAIDs用于治疗炎症的用途。 优选地，所用的R-NSAID是R-氟比洛芬，并且以每千克体重每天至少5毫克的剂量施用。 R-NSAIDs的抗炎作用是由于其通过抑制COX-2 mRNA合成而干扰COX-2的生物合成的能力，而不是仅仅阻断酶本身的作用。 为了实现COX-2 mRNA合成的抑制，R-NSAID必须以相当高的剂量存在。 因为R-NSAID在其作用中是选择性的，即它不抑制COX-1 mRNA合成或COX-1酶本身，因此可以以所需的高剂量施用，因为前列腺素的组织保护作用通过 COX-1途径不受干扰。

    Use of &ggr;-tocopherol and its oxidative metabolite LLU-&agr; in the treatment of disease
    7.
    发明授权
    Use of &ggr;-tocopherol and its oxidative metabolite LLU-&agr; in the treatment of disease 有权

    公开(公告)号：US06410589B1

    公开(公告)日：2002-06-25

    申请号：US09814330

    申请日：2001-03-21

    申请人： William J. Wechter

    发明人： William J. Wechter

    IPC分类号： A61K3135

    摘要： The present invention is generally related to the discovery of the therapeutic benefit of administering &ggr;-tocopherol and &ggr;-tocopherol derivatives. More specifically, the use of &ggr;-tocopherol and racemic LLU-&agr;, (S)-LLU-&agr;, or &ggr;-tocopherol derivatives as antioxidants and nitrogen oxide scavengers which treat and prevent high blood pressure, thromboembolic disease, cardiovascular disease, cancer, natriuretic disease, the formation of neuropathological lesions, and a reduced immune system response are disclosed.

    Method of treating rheumatoid arthritis
    10.
    发明授权
    Method of treating rheumatoid arthritis 失效

    公开(公告)号：US4172889A

    公开(公告)日：1979-10-30

    申请号：US895674

    申请日：1978-04-12

    申请人： William J. Wechter ,  Carter D. Brooks

    发明人： William J. Wechter ,  Carter D. Brooks

    IPC分类号： C07H19/06 ,  A61K31/70 ,  C07H19/08

    CPC分类号： C07H19/06 ,  Y10S514/825

    摘要： A process of treatment for the management of the condition known as rheumatoid arthritis. The process manages rheumatoid arthritis by controlling the inflammatory process in a rheumatoid joint by the intra-articular administration to said joint of an effective amount for controlling the inflammatory process of certain N.sup.4 -acyl-ara-cytidines, 5'-O-acyl-ara-cytidines and pharmaceutically acceptable acid addition salts thereof, and pharmaceutically acceptable acid addition salts of 5'-O-acyl-2,2'-anhydro-ara-cytidines.