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61. 发明申请

US20050075374A1 Sulfonyl aryl or heteroaryl hydroxamic acid compounds 审中-公开
标题翻译：磺酰基芳基或杂芳基异羟肟酸化合物
公开(公告)号：US20050075374A1
公开(公告)日：2005-04-07
申请号：US10867391
申请日：2004-06-14
申请人： Louis Bedell , Joseph McDonald , Thomas Barta , Daniel Becker , Shashidhar Rao , John Freskos , Brent Mischke , Daniel Getman , Gary DeCrescenzo , Clara Villamil
发明人： Louis Bedell , Joseph McDonald , Thomas Barta , Daniel Becker , Shashidhar Rao , John Freskos , Brent Mischke , Daniel Getman , Gary DeCrescenzo , Clara Villamil
IPC分类号： C07C311/16 , C07C311/21 , C07C317/22 , C07C317/44 , C07C323/65 , C07D207/14 , C07D207/16 , C07D211/16 , C07D211/18 , C07D211/46 , C07D211/54 , C07D211/62 , C07D213/30 , C07D213/82 , C07D295/15 , C07D295/26 , C07D309/12 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D211/84 , A61K31/4015 , A61K31/44
CPC分类号： C07D295/26 , C07C311/16 , C07C311/21 , C07C317/22 , C07C317/44 , C07C323/65 , C07D207/14 , C07D207/16 , C07D211/16 , C07D211/18 , C07D211/46 , C07D211/54 , C07D211/62 , C07D213/30 , C07D213/82 , C07D295/15 , C07D309/12 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12
摘要： A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
摘要翻译：公开了包括抑制基质金属蛋白酶活性的磺酰芳族或杂芳族环异羟肟酸化合物，其处理方法包括将具有MMP酶抑制有效量的考虑的磺酰芳族或杂芳族环异羟肟酸化合物施用于具有条件与病理基质金属蛋白酶活性相关。

62. 发明授权

US06846813B2 Compounds to treat alzheimer's disease 失效
标题翻译：治疗阿尔茨海默病的化合物
公开(公告)号：US06846813B2
公开(公告)日：2005-01-25
申请号：US09895843
申请日：2001-06-29
申请人： James P. Beck , Andrea Gailunas , Roy Hom , Barbara Jagodzinska , Varghese John , Michel Maillard
发明人： James P. Beck , Andrea Gailunas , Roy Hom , Barbara Jagodzinska , Varghese John , Michel Maillard
IPC分类号： A61P25/28 , C07C215/28 , C07C233/78 , C07C235/84 , C07C239/20 , C07C243/22 , C07C243/28 , C07C271/16 , C07C271/18 , C07C275/24 , C07C311/03 , C07C311/08 , C07C311/13 , C07C311/16 , C07C311/37 , C07C317/44 , C07C323/60 , C07D211/60 , C07D215/12 , C07D223/10 , C07D277/04 , C07D295/13 , C07D303/36 , C07D307/52 , C07D307/54 , C07D333/24 , A61K31/33 , A61K31/495 , C07D241/00 , C07D241/04
CPC分类号： C07D295/13 , C07C215/28 , C07C233/78 , C07C235/84 , C07C239/20 , C07C243/22 , C07C243/28 , C07C271/16 , C07C271/18 , C07C275/24 , C07C311/03 , C07C311/08 , C07C311/13 , C07C311/16 , C07C311/37 , C07C317/44 , C07C323/60 , C07D211/60 , C07D215/12 , C07D223/10 , C07D277/04 , C07D303/36 , C07D307/52 , C07D307/54 , C07D333/24
摘要： The present invention is disubstituted amines of formula (I) and disubstituted amines of formula (II) useful in treating Alzheimer's disease and other similar diseases.
摘要翻译：本发明是式（I）的二取代胺和式（II）的二取代的胺，其可用于治疗阿尔茨海默病和其它类似疾病。

63. 发明授权

US06844367B1 Benzamides and related inhibitors of factor Xa 有权
标题翻译：苯甲酰胺和相关因子Xa抑制剂
公开(公告)号：US06844367B1
公开(公告)日：2005-01-18
申请号：US09663420
申请日：2000-09-15
申请人： Bing-Yan Zhu , Penglie Zhang , Lingyan Wang , Wenrong Huang , Erick A. Goldman , Wenhao Li , Jingmei Zuckett , Yonghong Song , Robert M. Scarborough
发明人： Bing-Yan Zhu , Penglie Zhang , Lingyan Wang , Wenrong Huang , Erick A. Goldman , Wenhao Li , Jingmei Zuckett , Yonghong Song , Robert M. Scarborough
IPC分类号： C07C311/16 , C07C311/46 , C07C317/40 , C07C317/44 , C07D213/75 , C07D213/81 , C07D213/82 , C07D217/22 , C07D333/38 , C07D401/12 , C07D409/12 , C07D409/14 , C07D521/00 , A61K31/166 , G07C233/64
CPC分类号： C07D213/75 , C07C311/16 , C07C311/46 , C07C317/40 , C07C317/44 , C07D213/81 , C07D213/82 , C07D217/22 , C07D231/12 , C07D233/56 , C07D249/08 , C07D333/38 , C07D401/12 , C07D409/12 , C07D409/14
摘要： Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
摘要翻译：公开了与哺乳动物因子Xa有活性的新型苯甲酰胺化合物，其盐和与其有关的组合物。该化合物在体外或体内可用于预防或治疗凝血障碍。

64. 发明申请

US20040229946A1 New 3-aryl-2-hydroxypropionic acid derivative I 审中-公开
标题翻译：新的3-芳基-2-羟基丙酸衍生物I
公开(公告)号：US20040229946A1
公开(公告)日：2004-11-18
申请号：US10669131
申请日：2003-09-22
发明人： Kjell Andersson
IPC分类号： A61K031/255 , C07C39/70
CPC分类号： C07C303/30 , C07C217/76 , C07C233/25 , C07C233/29 , C07C233/75 , C07C235/42 , C07C255/54 , C07C271/28 , C07C271/38 , C07C271/44 , C07C271/58 , C07C275/34 , C07C309/65 , C07C309/66 , C07C309/73 , C07C311/08 , C07C311/13 , C07C311/16 , C07C317/22 , C07C317/28 , C07C323/19 , C07C323/44 , C07C323/56 , C07C335/18 , C07C2601/14
摘要： A novel 3-aryl-2-hydroxypropionic acid derivative, a process and intermediate for its manufacture, pharmaceutical preparations containing it and the use of the compound in clinical conditions associated with insulin resistance.
摘要翻译：新型3-芳基-2-羟基丙酸衍生物，其制备方法和中间体，含有它的药物制剂以及该化合物在与胰岛素抵抗相关的临床病症中的用途。

65. 发明申请

US20040181094A1 Transition metal oxo complexes as catalysts of synthetic processes involving alkyne reactants 审中-公开
标题翻译：过渡金属氧代络合物作为涉及炔反应物的合成方法的催化剂
公开(公告)号：US20040181094A1
公开(公告)日：2004-09-16
申请号：US10387328
申请日：2003-03-11
发明人： F. Dean Toste
IPC分类号： B01J023/42 , C07C043/14
CPC分类号： B01J31/18 , B01J31/181 , B01J31/2208 , B01J31/2234 , B01J31/2243 , B01J31/24 , B01J31/2404 , B01J31/2409 , B01J31/2433 , B01J31/2452 , B01J2231/4283 , B01J2231/4288 , B01J2231/52 , B01J2531/0266 , B01J2531/74 , C07B2200/07 , C07C41/09 , C07C41/30 , C07C269/06 , C07C303/40 , C07C271/12 , C07C311/16 , C07C43/176 , C07C43/1787 , C07C43/215 , C07C43/166
摘要： A method is provided for synthesizing substituted alkynes from an alkyne reactant and a nucleophile using rhenium (V) oxo complex as a catalyst. The alkyne reactant is substituted at the propargylic position with a leaving group susceptible to displacement by the nucleophile in a nucleophilic substitution reaction. The method involves contacting the alkyne reactant with a nucleophilic reactant in the presence of a catalytically effective amount of the rhenium (V) oxo complex. The method does not require activation of the leaving group or ionization of the nucleophilic reactant, and may be carried out in the presence of air and moisture. The invention is useful in synthesizing propargyl ethers, propargyl amines, and the like.
摘要翻译：提供了使用铼（V）羰基络合物作为催化剂从炔反应物和亲核试剂合成取代炔的方法。炔炔反应物在炔丙基位置被取代，离去基团在亲核取代反应中易于被亲核试剂置换。该方法包括在催化有效量的铼（V）氧代络合物的存在下使炔反应物与亲核反应物接触。该方法不需要激活离去基团或亲核反应物的离子化，并且可以在空气和水分的存在下进行。本发明可用于合成炔丙基醚，炔丙基胺等。

66. 发明申请

US20040002539A1 Process for preparing aminoguanidines and alkoxyguanidines as protease inhibitors 有权
标题翻译：制备氨基胍和烷氧基胍作为蛋白酶抑制剂的方法
公开(公告)号：US20040002539A1
公开(公告)日：2004-01-01
申请号：US10419972
申请日：2003-04-22
申请人： 3-Dimensional Pharmaceuticals, Inc.
发明人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L. Fedde , Carl R. Illig , Thomas P. Markotan
IPC分类号： C07D317/08 , C07C069/76 , C07C279/10 , A61K031/365
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: 1 wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are 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 L 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NR 9和R 1 -R 4，R 6 -R 9，R 11，R 12，说明书中列出的R a，R b，R c，Y，Z，n和m以及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是描述。还描述了制备式L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，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上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂，血线和支架。

67. 发明申请

US20030191317A1 Sulfonyl aryl or heteroaryl hydroxamic acid compounds 失效
标题翻译：磺酰基芳基或杂芳基异羟肟酸化合物
公开(公告)号：US20030191317A1
公开(公告)日：2003-10-09
申请号：US09728408
申请日：2000-12-01
申请人： G. D. Searle & Co.,
发明人： Louis J. Bedell , Joseph J. McDonald , Thomas E. Barta , Daniel P. Becker , Shashidhar N. Rao , John N. Freskos , Brent V. Mischke , Daniel P. Getman , Gary A. DeCrescenzo , Clara I. Villamil
IPC分类号： C07D213/62
CPC分类号： C07D295/26 , C07C311/16 , C07C311/21 , C07C317/22 , C07C317/44 , C07C323/65 , C07D207/14 , C07D207/16 , C07D211/16 , C07D211/18 , C07D211/46 , C07D211/54 , C07D211/62 , C07D213/30 , C07D213/82 , C07D295/15 , C07D309/12 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12
摘要： A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
摘要翻译：公开了包括抑制基质金属蛋白酶活性的磺酰芳族或杂芳族环异羟肟酸化合物，其处理方法包括将具有MMP酶抑制有效量的考虑的磺酰芳族或杂芳族环异羟肟酸化合物施用于具有条件与病理基质金属蛋白酶活性相关。

68. 发明申请

US20030171341A1 Modulators of Rho C activity 失效
标题翻译： Rho C活动的调制器
公开(公告)号：US20030171341A1
公开(公告)日：2003-09-11
申请号：US10300650
申请日：2002-11-19
发明人： Dongxu Sun , Edward L. Perkins , Stuart Tugendreich
IPC分类号： A61K031/44 , A61K031/63 , C07D213/26 , A61K031/40 , A61K031/18 , C07D207/46
CPC分类号： C07D213/75 , C07C311/16 , C07C311/17 , C07C311/29 , C07D209/08 , C07D307/52
摘要： Compounds of formula 1 modulate the activity of Rho C: 1 wherein R is a direct bond, lower alkylene, nullC(O)NHnull, or nullNHC(O)null; Ar is aryl or heteroaryl, substituted with R7, R8, R9, and R10, wherein R7, R8, and R9 are each independently H, halo, lower alkyl, OH, lower alkoxy, and R10 is H, halo, lower alkyl, OH, lower alkoxy, or forms a ring with R1; R1 is H, lower alkyl, or forms a ring with R10; R2, R3, R4, R5, and R6 are each independently H, lower alkyl, halo, nitro, OH, lower alkoxy, NH2, lower alkylamino, di(lower alkyl)amino, or two adjacent groups together form a saturated or unsaturated ring; or a pharmaceutically acceptable salt thereof.
摘要翻译：式1的化合物调节Rho C的活性：其中R是直接键，低级亚烷基，-C（O）NH-或-NHC（O） - ; Ar是被R7，R8，R9和R10取代的芳基或杂芳基，其中R7，R8和R9各自独立地是H，卤素，低级烷基，OH，低级烷氧基，R10是H，卤素，低级烷基，OH ，低级烷氧基，或与R1形成环; R1是H，低级烷基，或与R10形成环; R2，R3，R4，R5和R6各自独立地为H，低级烷基，卤素，硝基，OH，低级烷氧基，NH2，低级烷基氨基，二（低级烷基）氨基或两个相邻的基团一起形成饱和或不饱和环 ; 或其药学上可接受的盐。

69. 发明申请

US20030162690A1 Benzamides and related inhibitors of factor Xa 审中-公开
标题翻译：苯甲酰胺和相关因子Xa抑制剂
公开(公告)号：US20030162690A1
公开(公告)日：2003-08-28
申请号：US10126976
申请日：2002-04-22
申请人： COR Therapeutics, Inc.
发明人： Bing-Yan Zhu , Penglie Zhang , Lingyan Wang , Wenrong Huang , Erick A. Goldman , Wenhao Li , Jingmei Zuckett , Yonghong Song , Robert M. Scarborough
IPC分类号： A61K031/00
CPC分类号： A61K31/44 , A61K9/20 , A61K9/2013 , A61K9/2054 , A61K9/48 , A61K9/4858 , A61K9/4866 , A61K31/616 , A61K45/06 , A61K2201/094 , C07C237/42 , C07C255/60 , C07C257/18 , C07C259/18 , C07C311/16 , C07C311/46 , C07C317/40 , C07C317/44 , C07D213/75 , C07D213/81 , C07D213/82 , C07D217/22 , C07D231/12 , C07D233/56 , C07D233/64 , C07D249/08 , C07D295/125 , C07D333/38 , C07D401/12 , C07D409/12 , C07D409/14
摘要： Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described Compositions containing such compounds are also described The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders
摘要翻译：描述了包含其对哺乳动物因子Xa具有活性的其药学上可接受的异构体，盐，水合物，溶剂合物和前药衍生物的新型苯甲酰胺化合物。还描述了含有这些化合物的组合物。化合物和组合物可用于体外或体内用于预防或治疗凝血障碍

70. 发明授权

US06573288B1 Substituted sulphonyl cyanamides, method for producing same and their use as medicament 有权
标题翻译：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。

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