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1. 发明授权

US06699997B2 Carvedilol 失效
公开(公告)号：US06699997B2
公开(公告)日：2004-03-02
申请号：US09894798
申请日：2001-06-28
申请人： Jean Hildesheim , Sergey Finogueev , Ben-Zion Dolitzky , Shoshana Ben-Valid
发明人： Jean Hildesheim , Sergey Finogueev , Ben-Zion Dolitzky , Shoshana Ben-Valid
IPC分类号： C07D20982
CPC分类号： C07D209/88
摘要： This invention relates to an improved process of preparing carvedilol, as well as a new crystalline hydrate and solvate and forms of carvedilol, processes for the manufacture thereof, and pharmaceutical compositions thereof.

2. 发明授权

US06649772B2 3,6,9-Trisubstituted carbazoles for light emitting diodes 失效
标题翻译：用于发光二极管的3,6,9-三取代咔唑
公开(公告)号：US06649772B2
公开(公告)日：2003-11-18
申请号：US09990576
申请日：2001-11-21
申请人： Jiann T'Suen Lin , K. R. Justin Thomas , Yu-Tai Tao , Chung-Wen Ko
发明人： Jiann T'Suen Lin , K. R. Justin Thomas , Yu-Tai Tao , Chung-Wen Ko
IPC分类号： C07D20982
CPC分类号： C07D209/88 , C07D409/14
摘要： The present invention features substituted carbazole compounds of formula (I): Each of Z1 and Z2, independently, is each of A1 and A2, independently, is S, O, NR, or CH═CH; each of Y1 and Y2, independently, is aryl or heteroaryl; each of R1-R5, independently, is aryl or heteroaryl; and each of R6-R11, independently, is H, CN, alkyl, OR, NRR′, COR, or C(O)OR; and each of R and R′, independently, is H or alkyl. The compounds are useful as hole-transporting, light-emitting molecules with high glass transition temperatures.
摘要翻译：本发明具有式（I）的取代的咔唑化合物：Z 1和Z 2各自独立地为A 1和A 2，独立地是S，O，NR或CH = CH; Y 1和Y 2各自独立地是芳基或杂芳基; R 1 -R 5各自独立地是芳基或杂芳基; R 6 -R 11各自独立地是H，CN，烷基，OR，NRR'，COR或C（O）OR; R和R'各自独立地为H或烷基。这些化合物可用作具有高玻璃化转变温度的空穴传输的发光分子。

3. 发明授权

US06495701B1 Method for manufacturing tricyclic amino alcohol derivatives 失效
标题翻译：制备三环氨基醇衍生物的方法
公开(公告)号：US06495701B1
公开(公告)日：2002-12-17
申请号：US09937488
申请日：2001-09-26
申请人： Koki Matsubara , Hitoshi Kida
发明人： Koki Matsubara , Hitoshi Kida
IPC分类号： C07D20982
CPC分类号： C07D209/88 , C07C311/08 , C07C311/13
摘要： The present invention is directed to processes for the preparation of a compound useful for treating diabetes, obesity, hyperlipidemia and the like, which compound is represented by the formula (1): wherein R1 represents a lower alkyl group or a benzyl group; *1 represents an asymmetric carbon atom; R2 hydrogen atom, a halogen atom or a hydroxyl group; and A represents one of the following groups: wherein X represents NH, O or S; R6 represents a hydrogen atom, a hydroxyl group, an amino group or an acetylamino group; and *2 represents an asymmetric carbon atom when R6 is not a hydrogen atom, and to intermediates useful for the said processes. The processes of the present invention are convenient, practical preparing processes with low cost which comprise a small number of steps with good industrial work efficiency.
摘要翻译：本发明涉及制备用于治疗糖尿病，肥胖症，高脂血症等的化合物的方法，该化合物由式（1）表示：其中R1表示低级烷基或苄基; * 1表示不对称碳原子; R2氢原子，卤素原子或羟基; A表示下列基团之一：其中X表示NH，O或S; R6表示氢原子，羟基，氨基或乙酰氨基; 和* 2表示当R6不是氢原子时的不对称碳原子，并且可用于所述方法的中间体。本发明的方法是方便，实用的低成本的制备方法，其包括具有良好工业工作效率的少量步骤。

4. 发明授权

US06727274B2 Arylsulphonyl substituted-tetrahydro- and hexahydro-carbazoles 失效
标题翻译：芳基磺酰基取代的四氢 - 咔唑
公开(公告)号：US06727274B2
公开(公告)日：2004-04-27
申请号：US10268627
申请日：2002-10-08
申请人： Jian-Min Fu
发明人： Jian-Min Fu
IPC分类号： C07D20982
CPC分类号： C07D209/88
摘要： The invention provides compounds of formula I for use in treating conditions in which 5-HT6 receptors are involved such as in anxiety, depression, schizophrenia, Alzheimer's disease, stress-related disease, panic, a phobia, obsessive compulsive disorder, obesity, post-traumatic stress syndrome, epilepsy, and other CNS disorders.
摘要翻译：本发明提供式I化合物，其用于治疗其中涉及5-HT 6受体的病症，例如焦虑，抑郁，精神分裂症，阿尔茨海默病，紧张相关疾病，恐慌症，恐惧症，强迫症，肥胖症，创伤性应激综合征，癫痫和其他CNS疾病。

5. 发明授权

US06689784B2 Carbamate caspase inhibitors and uses thereof 失效
标题翻译：氨基甲酸酯半胱天冬酶抑制剂及其用途
公开(公告)号：US06689784B2
公开(公告)日：2004-02-10
申请号：US09821161
申请日：2001-03-29
申请人： David Bebbington , Ronald Knegtel , Michael Mortimore , David Kay , Julian M. C. Golec
发明人： David Bebbington , Ronald Knegtel , Michael Mortimore , David Kay , Julian M. C. Golec
IPC分类号： C07D20982
CPC分类号： C07D403/12 , C07D209/08 , C07D209/86 , C07D221/12 , C07D223/26 , C07D223/28 , C07D279/30
摘要： This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1&bgr; secretion.
摘要翻译：本发明提供了式I的半胱天冬酶抑制剂：其中Z是氧或硫; R 1是氢，-CHN 2，R 1，CH 2 OR，CH 2 SR或-CH 2 Y; Y是电负离子团; R 2是CO 2 H，CH 2 CO 2 H或其酯，酰胺或等体积体; R 3是能够适应半胱天冬酶的S2亚位点的基团; R 4和R 5与中间的氮一起形成杂环，R如说明书中所述。这些化合物是凋亡和IL-1β分泌的有效抑制剂。

6. 发明授权

US06337404B1 Diamine hole transport agent and organic electroluminescent device containing same 失效
标题翻译：二胺空穴传输剂和含有它的有机电致发光器件
公开(公告)号：US06337404B1
公开(公告)日：2002-01-08
申请号：US09461238
申请日：1999-12-16
申请人： Ki-jong Han , Youngkyoo Kim , Jae-Gyoung Lee , Dong-Kwon Choi
发明人： Ki-jong Han , Youngkyoo Kim , Jae-Gyoung Lee , Dong-Kwon Choi
IPC分类号： C07D20982
CPC分类号： C07D209/86 , H01L51/0059 , H01L51/0072 , H01L51/0081 , H01L51/5012 , H01L2251/308 , Y10S428/917
摘要： A novel diamine compound of formula (I) of the present invention having a high glass transition temperature is useful as an improved hole transport agent, and an organic electroluminescent device containing the diamine compound of formula (I) has good thermal and mechanical stabilities, and prolonged lifetime.
摘要翻译：具有高玻璃化转变温度的本发明的式（I）的新型二胺化合物可用作改进的空穴传输剂，并且含有式（I）的二胺化合物的有机电致发光器件具有良好的热和机械稳定性，长寿命

7. 发明授权

US06624177B1 Matrix metalloproteinase inhibitors and their therapeutic uses 失效
标题翻译：基质金属蛋白酶抑制剂及其治疗用途
公开(公告)号：US06624177B1
公开(公告)日：2003-09-23
申请号：US09254384
申请日：1999-03-02
申请人： Patrick Michael O'Brien , Joseph Armand Picard , Drago Robert Sliskovic , Andrew David White
发明人： Patrick Michael O'Brien , Joseph Armand Picard , Drago Robert Sliskovic , Andrew David White
IPC分类号： C07D20982
CPC分类号： C07D307/91 , A61K31/343 , A61K31/381 , C07C311/19 , C07C2603/18 , C07D333/76
摘要： The present invention relates to a method of inhibiting matrix metalloproteinases using compounds that are dibenzofuran sulfonamide derivatives having the Formula I More particularly, the present invention relates to a method of treating diseases in which matrix melatoproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.
摘要翻译：本发明涉及使用具有式IIIO的二苯并呋喃磺酰胺衍生物的化合物抑制基质金属蛋白酶的方法，本发明涉及一种治疗涉及多发性硬化症，动脉粥样硬化斑块破裂，再狭窄的基质蛋白酶的疾病的方法，主动脉瘤，心力衰竭，牙周病，角膜溃疡，烧伤，褥疮性溃疡，慢性溃疡或创伤，癌症转移，肿瘤血管生成，关节炎或依赖于白细胞组织侵袭的其他自身免疫性或炎性疾病。

8. 发明授权

US06599648B2 Heterarylbenzene compounds 失效
标题翻译：异芳基苯化合物
公开(公告)号：US06599648B2
公开(公告)日：2003-07-29
申请号：US10316507
申请日：2002-12-11
申请人： Jiann T'Suen Lin , Iuan-Yuan Wu , Yu-Tai Tao , E. Balasubramaniam
发明人： Jiann T'Suen Lin , Iuan-Yuan Wu , Yu-Tai Tao , E. Balasubramaniam
IPC分类号： C07D20982
CPC分类号： C07D409/04 , C07D333/36 , C07D409/14
摘要： A method of preparing a compound of formula I is described. In this compound, each of R1-R6 is, independently, in which Y is O, S, NH, or C(R7)═C(R8). Each of R7-R11 is, independently, H, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C26 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted C6-20 aryl, or substituted or unsubstituted C4-20 heteroaryl. Alternatively, each of R7-R11 is OH, C1-6 alkoxy, or N(R12)(R13), in which each of R12 and R13 is, independently, H, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, or substituted or unsubstituted C6-20 aryl. Each of R7-R11 can also be NO2, CN, or CO2R14, in which R14 is H or C1-6 alkyl.
摘要翻译：描述了制备式I化合物的方法。在该化合物中，R 1 -R 6各自独立地为Y，O，S，NH或C（R 7）= C（R 8）。取代或未取代的C 2-6链烯基，取代或未取代的C 2-6炔基，取代或未取代的C 6-20芳基或取代或未取代的C 4-20杂芳基，R 7 -R 11各自独立地为H，取代或未取代的C 1-6烷基。或者，R7-R11各自为OH，C1-6烷氧基或N（R12）（R13），其中R12和R13各自独立地为H，取代或未取代的C1-6烷基，取代或未取代的C2- 6烯基，取代或未取代的C 2-6炔基，或取代或未取代的C 6-20芳基。 R7-R11中的每一个也可以是NO 2，CN或CO 2 R 14，其中R 14是H或C 1-6烷基。

9. 发明授权

US06512123B2 Tricyclic alkylhydroxamate derivatives 失效
标题翻译：三环烷基羟肟酸衍生物
公开(公告)号：US06512123B2
公开(公告)日：2003-01-28
申请号：US10127100
申请日：2002-04-22
申请人： Adelbert Grossmann , Wolfgang von der Saal , Tim Sattelkau , Ulrich Tibes
发明人： Adelbert Grossmann , Wolfgang von der Saal , Tim Sattelkau , Ulrich Tibes
IPC分类号： C07D20982
CPC分类号： C07C259/06 , C07D209/88 , C07D313/12
摘要： Compounds of formula I wherein R1, R2, A, X, Y and Z have the meanings provided in the specification, and their enantiomers, diastereoisomers, racemates, pharmaceutically acceptable salts and mixtures thereof. These compounds have HDAC inhibitory activity for inhibiting cell proliferation. Also provided is a process of manufacturing these compounds.
摘要翻译： R1，R2，A，X，Y和Z中的式I化合物具有说明书中提供的含义及其对映异构体，非对映异构体，外消旋体，药学上可接受的盐及其混合物。这些化合物具有抑制细胞增殖的HDAC抑制活性。还提供了制造这些化合物的方法。

10. 发明授权

US06512122B2 Hetarylbenzene compounds 失效
标题翻译：杂芳基苯化合物
公开(公告)号：US06512122B2
公开(公告)日：2003-01-28
申请号：US09991488
申请日：2001-11-21
申请人： Jiann T'suen Lin , Iuan-Yuan Wu , Yu-Tai Tao , E. Balasubramaniam
发明人： Jiann T'suen Lin , Iuan-Yuan Wu , Yu-Tai Tao , E. Balasubramaniam
IPC分类号： C07D20982
CPC分类号： C07D409/04 , C07D333/36 , C07D409/14
摘要： A method of preparing a compound of formula I is described. In this compound, each of R1-R6 is, independently, in which Y is O, S, NH, or C(R7)═C(R8). Each of R7-R11 is, independently, H, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted C6-20 aryl, or substituted or unsubstituted C4-20 heteroaryl. Alternatively, each of R7-R11 is OH, C1-6 alkoxy, or N(R12)(R13), in which each of R12 and R13 is, independently, H, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, or substituted or unsubstituted C6-20 aryl. Each of R7-R11 can also be NO2, CN, or CO2R14, in which R14 is H or C1-6 alkyl.
摘要翻译：描述了制备式I化合物的方法。在该化合物中，R 1 -R 6各自独立地为Y，O，S，NH或C（R 7）= C（R 8）。 R 7 -R 11各自独立地为H，取代或未取代的C 1-6烷基，取代或未取代的C 2-6烯基，取代或未取代的C 2-6炔基，取代或未取代的C 6-20芳基，或取代或未取代的C 4-20 杂芳基。或者，R7-R11各自为OH，C1-6烷氧基或N（R12）（R13），其中R12和R13各自独立地为H，取代或未取代的C1-6烷基，取代或未取代的C2- 6烯基，取代或未取代的C 2-6炔基，或取代或未取代的C 6-20芳基。 R7-R11中的每一个也可以是NO 2，CN或CO 2 R 14，其中R 14是H或C 1-6烷基。

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