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1. 发明授权

US06515179B2 Process for the removal of nitrobenzenesulfonyl 失效
标题翻译：硝基苯磺酰基去除方法
公开(公告)号：US06515179B2
公开(公告)日：2003-02-04
申请号：US10148877
申请日：2002-06-11
申请人： Nobuo Nagashima
发明人： Nobuo Nagashima
IPC分类号： C07D20716
CPC分类号： C07D207/416 , C07C209/62 , C07C213/02 , C07C227/18 , C07C269/04 , C07D205/04 , C07C211/27 , C07C229/36 , C07C271/20
摘要： A 2- or 4-nitrobenzenesulfonamide is allowed to react with an alkali metal alkoxide to remove a nitrobenzenesulfonyl group to thereby obtain an amine corresponding to the amide. Furthermore, a method for producing an amine derivative by allowing the resulting amine without isolation to react with an activated, substituted oxycarbonyl compound or an activated acyl compound is provided. According to this method, a corresponding free amine and its substituted derivative can be produced easily and industrially advantageously from the 2- or 4-nitrobenzenesulfonamide without using a thiol compound.
摘要翻译：使2-或4-硝基苯磺酰胺与碱金属醇盐反应以除去硝基苯磺酰基，从而得到对应于酰胺的胺。此外，提供了通过使得到的胺不经分离而与活化的取代的氧羰基化合物或活化的酰基化合物反应来制备胺衍生物的方法。根据该方法，可以在不使用硫醇化合物的情况下，容易且工业上有利地从2-或4-硝基苯磺酰胺制备相应的游离胺及其取代的衍生物。

2. 发明授权

US06576657B2 Amidino derivatives and their use as thrombin inhibitors 失效
标题翻译：脒衍生物及其作为凝血酶抑制剂的用途
公开(公告)号：US06576657B2
公开(公告)日：2003-06-10
申请号：US09844428
申请日：2001-04-30
申请人： Olle Karlsson , Marcel Linschoten , Jan-Erik Nyström
发明人： Olle Karlsson , Marcel Linschoten , Jan-Erik Nyström
IPC分类号： C07D20716
CPC分类号： C07D405/06 , C07D205/04
摘要： There is provided compounds of formula I, wherein R1, Rx, Y, Ry, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
摘要翻译：提供式I化合物，其中R1，Rx，Y，Ry，n和B具有在描述中给出的含义，其可用作胰蛋白酶样蛋白酶如凝血酶的竞争性抑制剂，特别是在治疗条件需要抑制凝血酶（如血栓形成）或作为抗凝剂。

3. 发明授权

US06531612B2 Nitrile derivatives that inhibit cathepsin K 失效
标题翻译：抑制组织蛋白酶K的腈衍生物
公开(公告)号：US06531612B2
公开(公告)日：2003-03-11
申请号：US09745675
申请日：2000-12-21
申请人： Tobias Gabriel , Michael Pech , Sabine Wallbaum
发明人： Tobias Gabriel , Michael Pech , Sabine Wallbaum
IPC分类号： C07D20716
CPC分类号： C07D403/06 , C07D207/16 , C07D207/48 , C07D209/52 , C07D277/06 , C07D405/12 , C07D405/14
摘要： Compounds of the formula: wherein R1 to R7 and Y are as defined in the specification, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof, are useful for treating diseases associated with cystein proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.
摘要翻译：下式的化合物：其中R 1至R 7和Y如说明书中所定义，及其药学上可接受的盐和/或其药学上可接受的酯可用于治疗与半胱氨酸蛋白酶相关的疾病，例如骨质疏松症，骨关节炎，类风湿性关节炎，肿瘤转移，肾小球性肾炎，动脉粥样硬化，心肌梗塞，心绞痛，不稳定性心绞痛，中风，斑块破裂，短暂性脑缺血发作，黑素瘤假体，外周动脉闭塞性疾病，血管成形术后再狭窄和支架置入，腹主动脉瘤形成，炎症，自身免疫性疾病，疟疾，眼底组织细胞病变和呼吸系统疾病。

4. 发明授权

US06218551B1 Combinatorial hydroxy-amino acid amide libraries 失效
标题翻译：组合羟基 - 氨基酸酰胺文库
公开(公告)号：US06218551B1
公开(公告)日：2001-04-17
申请号：US09337618
申请日：1999-06-21
申请人： Roland Ellwood Dolle, III , Tao Guo , Theodore Otto Johnson, Jr. , Hitesh K. Patel , Shiwei Tao , Zhen Min He
发明人： Roland Ellwood Dolle, III , Tao Guo , Theodore Otto Johnson, Jr. , Hitesh K. Patel , Shiwei Tao , Zhen Min He
IPC分类号： C07D20716
CPC分类号： C07D207/14 , C07D207/16 , C07D241/04
摘要： Combination chemical libraries of Formula I and methods for preparation are disclosed. The libraries allow one to screen large numbers of compounds for a desired biological activity with relative ease. The libraries may be tagged or untagged. In preferred libraries, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or substituted piperazinealkanoic acid. The use of the libraries to discover biologically active compounds is also disclosed.
摘要翻译：公开了式I的组合化学文库和制备方法。这些文库允许相对容易地筛选大量化合物以获得所需的生物活性。库可能被标记或未标记。在优选的文库中，Y是N-酰化氨基酸，取代的4-氨基脯氨酸或取代的哌嗪烷酸的残基。还公开了使用这些文库发现生物活性化合物。

5. 发明授权

US06509477B1 Small molecule inhibitors of rotamase enzyme activity 失效
标题翻译：旋转异构酶活性的小分子抑制剂
公开(公告)号：US06509477B1
公开(公告)日：2003-01-21
申请号：US09359351
申请日：1999-07-21
申请人： Gregory S. Hamilton , Joseph P. Steiner
发明人： Gregory S. Hamilton , Joseph P. Steiner
IPC分类号： C07D20716
CPC分类号： C07D405/12 , C07D207/16
摘要： This invention relates to neurotrophic compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.
摘要翻译：本发明涉及对FKBP型免疫亲和素具有亲和力的神经营养化合物，它们的制备和用作与免疫亲和素蛋白相关的酶活性的抑制剂，特别是肽基 - 脯氨酰异构酶或旋转异构酶活性抑制剂。

6. 发明授权

US06500959B1 Pyrrolidine derivatives and processes for preparing same 失效
标题翻译：吡咯烷衍生物及其制备方法
公开(公告)号：US06500959B1
公开(公告)日：2002-12-31
申请号：US09605475
申请日：2000-06-28
申请人： Gregory S. Hamilton , Joseph P. Steiner
发明人： Gregory S. Hamilton , Joseph P. Steiner
IPC分类号： C07D20716
CPC分类号： C07D401/06 , A61K31/444 , C07D207/16 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12
摘要： This invention relates to neurotrophic N-glyoxyl-prolyl ester compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.
摘要翻译：本发明涉及对FKBP型免疫亲和素具有亲和性的神经营养的N-乙醛酰脯氨酰酯化合物，它们的制备和用作与免疫亲和素蛋白相关的酶活性的抑制剂，特别是肽基 - 脯氨酰异构酶或旋转异构酶活性的抑制剂。

7. 发明授权

US06239150B1 Penicillaminamide derivatives 失效
标题翻译：青霉胺衍生物
公开(公告)号：US06239150B1
公开(公告)日：2001-05-29
申请号：US08983321
申请日：1998-03-12
申请人： Masahiro Oshima , Norimichi Iwase , Naoto Inakoshi , Koichi Sugawara , Misao Okitsu
发明人： Masahiro Oshima , Norimichi Iwase , Naoto Inakoshi , Koichi Sugawara , Misao Okitsu
IPC分类号： C07D20716
CPC分类号： C07K5/0606 , A61K38/00
摘要： Compounds represented by the general formula (I) wherein n represents 1 or 2; R1 represents, for example, a C1-C10 alkyl group which may be substituted with a C3-C10 cycloalkyl group or carboxyl group; R2 represents hydrogen atom, a C1-C10 alkyl group or other; and R3 represents amino group or amidino group, whose example include trans-4-amino-[(S)-N-[(S)-2-propoxycarbonylamino-3-isopropylthio-3-methyl-butanoyl]prolyl]aminomethylcyclohexane. The compounds have potent inhibitory activity against thrombin, and are useful as anticoagulants.
摘要翻译：由通式（I）表示的化合物，其中n表示1或2; R1表示例如可被C 3 -C 10环烷基或羧基取代的C 1 -C 10烷基; R2表示氢原子，C1-C10烷基或其他; 并且R 3表示氨基或脒基，其实例包括反式-4-氨基 - [（S）-N - [（S）-2-丙氧基羰基氨基-3-异丙硫基-3-甲基 - 丁酰基]脯氨酰基]氨基甲基环己烷。这些化合物对凝血酶具有有效的抑制活性，可用作抗凝剂。

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