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554 条记录 (耗时 0.046 秒)

    Substituted sulphonyl cyanamides, method for producing same and their use as medicament
    72.
    发明授权
    Substituted sulphonyl cyanamides, method for producing same and their use as medicament 有权
    取代的磺酰基氰胺，其制备方法及其作为药物的用途

    公开(公告)号：US06573288B1

    公开(公告)日：2003-06-03

    申请号：US09674606

    申请日：2000-11-03

    申请人： Andreas Weichert ,  Hans Jochen Lang ,  Stefan Petry ,  Jan-Robert Schwark ,  Heinz-Werner Kleemann ,  Sabine Faber ,  Hans-Willi Jansen

    发明人： Andreas Weichert ,  Hans Jochen Lang ,  Stefan Petry ,  Jan-Robert Schwark ,  Heinz-Werner Kleemann ,  Sabine Faber ,  Hans-Willi Jansen

    IPC分类号： C07D23390

    CPC分类号： C07D233/90 ,  C07C311/16 ,  C07D233/68

    摘要： The invention relates to compounds of formula (I) in which the symbols have the meanings given in the claims. Said compounds are inhibitors of the sodium-dependent bicarbonate/chloride ion exchanger which can be used as medicines for the prophylaxis or treatment of a wide range of diseases, for example the treatment and/or prophylaxis of myocardial infarction, angina pectoris, diseases caused by ischaemia, impaired respiration, cardiac ischaemia, ischaemia of the peripheral and central nervous system and stroke, ischaemia of the peripheral organs and limbs and diseases in which cell proliferation is a primary or secondary cause, in the treatment of shock, during surgical interventions and organ transplants or for preserving and storing transplants to be used in surgical interventions.

    摘要翻译： 本发明涉及式（I）化合物，其中符号具有权利要求中给出的含义。 所述化合物是钠依赖性碳酸氢盐/氯离子交换剂的抑制剂，其可用作预防或治疗广泛疾病的药物，例如治疗和/或预防心肌梗塞，心绞痛，由 局部缺血，呼吸受阻，心脏局部缺血，外周和中枢神经系统和中风的局部缺血，外周器官和四肢的局部缺血以及细胞增殖是主要或次要原因的疾病，在手术干预和器官期间的休克治疗 移植或用于保存和储存用于外科手术的移植物。

    Quenching reagents for solution phase synthesis
    75.
    发明授权
    Quenching reagents for solution phase synthesis 失效

    公开(公告)号：US06395930B1

    公开(公告)日：2002-05-28

    申请号：US09577393

    申请日：2000-05-25

    申请人： Sham Nikam

    发明人： Sham Nikam

    IPC分类号： C07C32102

    CPC分类号： C07C303/38 ,  B01J2219/00599 ,  C07C231/02 ,  C07C231/24 ,  C07C273/1827 ,  C07C273/189 ,  C40B50/08 ,  C07C311/29 ,  C07C311/16

    摘要： A method for enhancing the purity of a desired compound comprising: Step (a) treating a crude reaction product which contains at least one desired compound, unreacted starting materials and/or byproducts with at least one bifunctional quenching agent that is capable of selective covalent reaction with unwanted byproducts, or excess reagents; Step (b) allowing the quenching agent to covalently react with unreacted starting materials and/or byproducts to afford a derivatized compound of the quenching agent: and Step (c) isolating the desired compound is described as well as novel quenching agents and methods for their use in the rapid purification of synthetic intermediates and products in synthesis, combinatorial chemistry, and automated organic synthesis.

    Aminoguanidines and alkoxyguanidines as protease inhibitors
    78.
    发明授权
    Aminoguanidines and alkoxyguanidines as protease inhibitors 失效
    氨基胍和烷氧基胍作为蛋白酶抑制剂

    公开(公告)号：US06235778B1

    公开(公告)日：2001-05-22

    申请号：US08979234

    申请日：1997-11-26

    申请人： Bruce E. Tomczuk ,  Richard M. Soll ,  Tianbao Lu ,  Cynthia L. Fedde ,  Carl R. Illig ,  Thomas P. Markotan ,  Thomas P. Stagnaro

    发明人： Bruce E. Tomczuk ,  Richard M. Soll ,  Tianbao Lu ,  Cynthia L. Fedde ,  Carl R. Illig ,  Thomas P. Markotan ,  Thomas P. Stagnaro

    IPC分类号： A61K31255

    CPC分类号： C07C309/73 ,  C07C309/75 ,  C07C309/76 ,  C07C309/77 ,  C07C311/16 ,  C07C311/17 ,  C07C311/18 ,  C07C311/19 ,  C07C311/21 ,  C07C317/14 ,  C07C323/66 ,  C07C2601/02 ,  C07C2601/14 ,  C07D211/96 ,  C07D213/42 ,  C07D213/74 ,  C07D215/36 ,  C07D217/02 ,  C07D217/22 ,  C07D239/42 ,  C07D295/13 ,  C07D295/26 ,  C07D307/66

    摘要： Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R114 R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and mare set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents.

    摘要翻译： 氨基胍和烷氧基胍化合物，包括下式的化合物：其中X是O或NR9，R114R4，R6-R9，R11，R12，Ra，Rb，Rc，Y，Z，n和母本也在说明书中列出 描述了抑制蛋白水解酶如凝血酶的水合物，溶剂合物或其药学上可接受的盐。 还描述了制备式I化合物的方法。本发明的新化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，例如胰凝乳蛋白酶，胰蛋白酶，凝血酶，纤溶酶和因子Xa。 某些化合物通过直接，选择性抑制凝血酶表现出抗血栓形成活性，或者是用于形成具有抗血栓形成活性的化合物的中间体。 本发明包括用于抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制哺乳动物栓塞形成的组合物，其包含本发明化合物在药学上可接受的载体中。 本发明化合物的其它用途是作为凝血剂或者物理连接于制造用于血液收集，血液循环和血液储存中的装置的材料的抗凝剂，例如导管，血液透析机，采血注射器和管， 血线和支架。

    Carbamoylphenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators
    80.
    发明授权
    Carbamoylphenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators 失效
    氨基甲酰基苯基磺酰脲，其制备方法及其作为除草剂和植物生长调节剂的用途

    公开(公告)号：US06228808B1

    公开(公告)日：2001-05-08

    申请号：US09182763

    申请日：1998-10-30

    申请人： Heinz Kehne ,  Lothar Willms ,  Christian Waldraff ,  Hansjörg Dietrich ,  Hermann Bieringer ,  Christopher Rosinger ,  Thomas Auler

    发明人： Heinz Kehne ,  Lothar Willms ,  Christian Waldraff ,  Hansjörg Dietrich ,  Hermann Bieringer ,  Christopher Rosinger ,  Thomas Auler

    IPC分类号： A01N4354

    CPC分类号： C07D275/06 ,  C07C311/16 ,  C07D521/00

    摘要： Compounds of the formula (I) or salts thereof in which R1, R3=H, (subst.) hydrocarbon radical (HC) or (subst.) heterocyclyl which, including substituents, have 1-30 carbon atoms, R2=R0—Q0—, in which R0=H, (subst.) HC or (subst.) heterocyclyl radical, in each case having 1-30 carbon atoms including substituents, and Q0=a direct bond or —O—, —SO2-, —NH—, —N[(C1-C6)alkyl]-, —CO—, —CO—NH— or —O—CO—NH—; R4=H, halogen, NO2, CN, (C1-C4)alkyl, (C1-C4)alkoxy, [(C1-C4)alkyl]carbonyl or [(C1-C4)alkoxy]carbonyl, where each of the last four radicals may be halogenated; R5=H or (C1-C4)alkyl; Q=O or NR*; R*=H. (C1-C4)alkyl, (C3-C4)alkenyl or (C3-C4)alkynyl, where each of the last three radicals may be substituted by halogen, (C1-C4)alkoxy and/or (C1-C4)alkylthio, W=O or S; X,Y=H, halogen, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)alkylthio, where each of the last three radicals may be substituted by halogen, (C1-C4)alkoxy and/or (C1-C4)alkylthio, or mono- or di[(C1-C4)alkyl]amino, (C3-C4)cycloalkyl, (C2-C5)alkenyl, (C2-C5)alkynyl, (C2-C5)alkenyloxy or (C2-C5)alkynyloxy, Z=CH or N, are suitable as herbicides or plant growth regulators, for example for controlling harmful plants in crop plants, including transgenic crop plants. They can be prepared by processes according to claim 6, via intermediates, some of which are novel.

    摘要翻译： 式（I）化合物或其盐，其中R 1，R 3 = H，（取代）烃基（HC）或（取代）杂环基，其包括取代基，具有1-30个碳原子，R 2 = R 0 -Q 0-， 其中R 0 = H，（低级）HC或（取代）杂环基，在每种情况下具有包含取代基的1-30个碳原子，Q 0 =直接键或-O-，-SO 2 - ， - NH-， -N [（C 1 -C 6）烷基] - ， - CO - ， - CO-NH-或-O-CO-NH-; R4 = H，卤素，NO2，CN，（C1-C4）烷基，（C1-C4）烷氧基，[（C1-C4）烷基]羰基或[（C1-C4）烷氧基]羰基， 自由基可以被卤化; R5 = H或（C1-C4）烷基; Q = O或NR *; R * = H。 （C 1 -C 4）烷基，（C 3 -C 4）烯基或（C 3 -C 4）炔基，其中最后三个基团中的每一个可以被卤素，（C 1 -C 4）烷氧基和/或（C 1 -C 4）烷硫基取代， W = O或S; X，Y = H，卤素，（C1-C4）烷基，（C1-C4）烷氧基，（C1-C4）烷硫基，其中最后三个基团中的每一个可以被卤素，（C 1 -C 4）烷氧基和/ 或（C 1 -C 4）烷硫基或单或二[（C 1 -C 4）烷基]氨基，（C 3 -C 4）环烷基，（C 2 -C 5）烯基，（C 2 -C 5）炔基，（C 2 -C 5） 或（C 2 -C 5）炔氧基Z = CH或N适合作为除草剂或植物生长调节剂，例如用于控制作物植物（包括转基因作物植物）中的有害植物。 它们可以通过根据权利要求6的方法通过中间体制备，其中一些是新颖的。