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61. 发明授权

US06281211B1 Substituted semicarbazides and the use thereof 有权
标题翻译：取代氨基脲及其用途
公开(公告)号：US06281211B1
公开(公告)日：2001-08-28
申请号：US09601698
申请日：2000-09-21
申请人： Sui Xiong Cai , Nancy C. Lan , Soo Hong-Bae
发明人： Sui Xiong Cai , Nancy C. Lan , Soo Hong-Bae
IPC分类号： A61K31535
CPC分类号： C07D317/64 , C07C281/06 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07D209/08
摘要： This invention is related to substituted semicarbazides represented by Formula (I) or a pharmaceutically acceptable salt or prodrug thereof, wherein: R1 and R2 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; R3, R4, R5 and R6 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl, or R3 and R4 is defined as above, and R5 and R6 together with the nitrogen atom to which they are attached form a heterocycle, including piperidine, piperazine, morpholine; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one of O, S, NR7, CH2, C(O), NR7C(O), C(O)NR7, SO, SO2 or a covalent bond; where R7 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; n is 0, 1, 2 or 3. m is 0, 1, 2 or 3. The invention also is directed to the use of substituted semi-carbazides for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as anticonvulsants, and as antimanic depressants, as anti-nigraine agents, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
摘要翻译：本发明涉及由式（I）表示的取代氨基脲或其药学上可接受的盐或前药，其中：R 1和R 2独立地为氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基 ; R3，R4，R5和R6独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基，或R3和R4定义如上，R5和R6连同氮原子它们连接形成杂环，包括哌啶，哌嗪，吗啉; A1和A2独立地是芳基，杂芳基，饱和或部分不饱和的碳环或饱和或部分不饱和的杂环，其中任何一个任选被取代; X是O，S，NR7，CH2，C（O），NR7C（O），C（O）NR7，SO，SO2或共价键之一; 其中R 7是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基; n为0,1,2或3.m为0,1,2或3.本发明还涉及用于治疗全身和局灶性缺血后的神经元损伤的治疗或预防的替代半卡巴肼的用途的神经退行性疾病如肌萎缩性侧索硬化（ALS），以及用作治疗，预防或改善急性或慢性疼痛的抗惊厥药，作为抗躁狂抑制剂，作为局部麻醉剂作为抗心律失常药物，治疗或预防糖尿病性神经病变。

62. 发明授权

US06248904B1 Fluorescence dyes and their applications for whole-cell fluorescence screening assays for caspases, peptidases, proteases and other enzymes and the use thereof 有权
标题翻译：荧光染料及其在半胱氨酸蛋白酶，肽酶，蛋白酶和其他酶的全细胞荧光筛选测定中的应用及其用途
公开(公告)号：US06248904B1
公开(公告)日：2001-06-19
申请号：US09357952
申请日：1999-07-21
申请人： Han-Zhong Zhang , Sui Xiong Cai
发明人： Han-Zhong Zhang , Sui Xiong Cai
IPC分类号： C07D31188
CPC分类号： C07D493/10 , C07D311/82 , C07K5/06191 , C07K5/0827 , C07K5/1027 , C07K7/06 , Y10T436/142222
摘要： The present invention relates to novel fluorescent dyes, novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of caspases and other enzymes involved in apoptosis in whole cells, cell lines and tissue samples derived from any living organism or organ. The reporter molecules and assay processes can be used in drug screening procedures to identify compounds which act as inhibitors or inducers of the caspase cascade in whole cells or tissues. The reagents and assays described herein are also useful for determining the chemosensitivity of human cancer cells to treatment with chemotherapeutic drugs. The present invention also relates to novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of type 2 methionine aminopeptidase, HIV protease, adenovirus protease, HSV-1 protease, HCMV protease and HCV protease.
摘要翻译：本发明涉及新的荧光染料，新的荧光和荧光报道分子和新的酶测定方法，其可用于检测来自任何活生物体的全细胞，细胞系和组织样品中参与细胞凋亡的半胱天冬酶和其它酶的活性或器官。报告分子和测定方法可以用于药物筛选程序中，以鉴定在整个细胞或组织中作为半胱天冬酶级联的抑制剂或诱导剂的化合物。本文所述的试剂和测定法也可用于确定人类癌细胞对用化学治疗药物治疗的化学敏感性。本发明还涉及可用于检测2型甲硫氨酸氨基肽酶，HIV蛋白酶，腺病毒蛋白酶，HSV-1蛋白酶，HCMV蛋白酶和HCV蛋白酶的活性的新的荧光和荧光报告分子和新的酶测定方法。

63. 发明授权

US5891871A Substituted 2,3-benzodiazepin-4-ones and the use thereof 失效
标题翻译：取代的2,3-苯并二氮杂-4-酮及其用途
公开(公告)号：US5891871A
公开(公告)日：1999-04-06
申请号：US821638
申请日：1997-03-20
申请人： Haiji Xia , Sui Xiong Cai , George Field , Nancy C. Lan , Yan Wang
发明人： Haiji Xia , Sui Xiong Cai , George Field , Nancy C. Lan , Yan Wang
IPC分类号： A61K31/00 , A61K31/55 , A61K31/551 , A61P25/08 , A61P25/16 , A61P25/28 , C07D243/02 , C07D243/04 , C07D243/10 , C07D491/04 , C07D491/056
CPC分类号： C07D491/04 , C07D243/02 , C07D243/10
摘要： The invention relates to substituted 2,3-benzodiazepin-4-ones which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, CMV retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition enhancers. The invention also is directed to the process for the preparation of the substituted 2,3-benzodiazepin-4-ones.
摘要翻译：本发明涉及作为AMPA受体的拮抗剂或阳性调节剂的取代2,3-苯并二氮杂-4-酮及其用于治疗，预防或改善与中风，全身和局灶性缺血，CNS创伤，低血糖和手术，以及治疗或改善神经变性疾病，包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病，帕金森病和唐氏综合症，治疗，预防或改善兴奋性氨基酸过度刺激的不良后果，治疗或改善焦虑，精神病，抽搐，慢性疼痛，青光眼，CMV视网膜炎，尿失禁，肌肉痉挛和诱导麻醉，以及治疗或改善兴奋性氨基酸缺乏症如精神分裂症，阿尔茨海默病和营养不良以及神经发育不良的不良后果以及认知增强剂。本发明还涉及制备取代的2,3-苯并二氮杂-4-酮的方法。

64. 发明授权

US09290460B2 1-(Arylmethyl)quinazoline-2,4(1H,3H)-diones as PARP inhibitors and the use thereof 有权
标题翻译： 1-（芳基甲基）喹唑啉-2,4（1H，3H） - 二酮作为PARP抑制剂及其用途
公开(公告)号：US09290460B2
公开(公告)日：2016-03-22
申请号：US14006722
申请日：2012-03-31
申请人： Sui Xiong Cai , Ye Edward Tian , Xiuhua Hu
发明人： Sui Xiong Cai , Ye Edward Tian , Xiuhua Hu
IPC分类号： C07D403/12 , A61K31/517 , C07D239/96 , C07D401/06 , A61K45/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
CPC分类号： C07D409/12 , A61K31/517 , A61K45/06 , C07D239/96 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： Disclosed are 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones thereof, represented by the Formula (I) wherein Ar, R1-R6 are defined herein. Compounds having Formula (I) are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity.
摘要翻译：公开了由式（I）表示的1-（芳基甲基）喹唑啉-2,4（1H，3H） - 二酮，其中Ar，R 1 -R 6在本文中定义。具有式（I）的化合物是PARP抑制剂。因此，本发明的化合物可用于治疗对抑制PARP活性有反应的临床病症。

65. 发明授权

US08426431B2 Substituted 2-aminoacetamides and the use thereof 有权
标题翻译：取代的2-氨基乙酰胺及其用途
公开(公告)号：US08426431B2
公开(公告)日：2013-04-23
申请号：US12986587
申请日：2011-01-07
申请人： Nancy C. Lan , Yan Wang , Sui Xiong Cai
发明人： Nancy C. Lan , Yan Wang , Sui Xiong Cai
IPC分类号： A61K31/505 , A61K31/47 , A61K31/165
CPC分类号： C07C233/05 , A61K31/165 , C07C237/06 , C07C237/08 , C07C2601/14 , C07D211/46 , C07D213/65 , C07D213/68 , C07D215/20 , C07D239/34 , C07D241/08 , C07D309/12 , C07D317/64
摘要： The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, anxiety, or manic depression, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
摘要翻译：本发明涉及由式（II）表示的取代的2-氨基乙酰胺及其药学上可接受的盐和前药，其中取代基在本文中定义。本发明还涉及取代的2-氨基乙酰胺在治疗全球和局灶性缺血后的神经元损伤的方法中的用途，以及用作治疗，预防或改善作为抗惊厥药物的抗痉挛剂的疼痛，焦虑或躁狂抑郁症，作为局部麻醉剂，作为抗心律失常药物和治疗或预防糖尿病性神经病变。

66. 发明授权

US08258145B2 Method of treating brain cancer 有权
标题翻译：治疗脑癌的方法
公开(公告)号：US08258145B2
公开(公告)日：2012-09-04
申请号：US11773285
申请日：2007-07-03
申请人： Sui Xiong Cai , Mark B. Anderson , Adam Willardsen , Nilantha Sudath Sirisoma
发明人： Sui Xiong Cai , Mark B. Anderson , Adam Willardsen , Nilantha Sudath Sirisoma
IPC分类号： A61K31/517 , A61K31/535 , A61K31/47
CPC分类号： A61K31/4709 , A61K31/517 , A61K31/5377
摘要： Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and in particular to the use of these compounds in treating brain cancer.
摘要翻译：公开了作为胱天蛋白酶的活化剂和凋亡诱导剂的4-芳基氨基 - 喹唑啉及其类似物。本发明的化合物可用于治疗发生异常细胞的不受控制的生长和扩散的各种临床病症，特别是这些化合物在治疗脑癌中的用途。

67. 发明授权

US07989462B2 4-arylamin-or-4-heteroarylamino-quinazolines and analogs as activators of caspases and inducers of apoptosis and the use thereof 失效
标题翻译： 4-芳基氨基 - 或 - 4-杂芳基氨基 - 喹唑啉及其类似物作为胱天蛋白酶的活化剂和凋亡诱导剂及其用途
公开(公告)号：US07989462B2
公开(公告)日：2011-08-02
申请号：US11773303
申请日：2007-07-03
申请人： Sui Xiong Cai , Mark B. Anderson , Adam Willardsen , Nilantha Sudath Sirisoma , Hong Zhang , Kazuyuki Suzuki
发明人： Sui Xiong Cai , Mark B. Anderson , Adam Willardsen , Nilantha Sudath Sirisoma , Hong Zhang , Kazuyuki Suzuki
IPC分类号： A01N43/90 , A61K31/519 , C07D401/00 , C07D403/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D239/02
CPC分类号： C07D239/94 , C07D239/72 , C07D403/12
摘要： Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
摘要翻译：公开了作为胱天蛋白酶的活化剂和凋亡诱导剂的4-芳基氨基 - 喹唑啉及其类似物。本发明的化合物可用于治疗异常细胞发生不受控制的生长和扩散的各种临床病症。

68. 发明授权

US07842805B2 Pharmaceutical compounds as activators of caspases and inducers of apoptosis and the use thereof 失效
标题翻译：药物化合物作为胱天蛋白酶的活化剂和凋亡诱导剂及其用途
公开(公告)号：US07842805B2
公开(公告)日：2010-11-30
申请号：US11773293
申请日：2007-07-03
申请人： Sui Xiong Cai , Mark B. Anderson , Adam Willardsen , Songchun Jiang , Robert J. Halter , Rachel Slade , Yevgeniya Klimova
发明人： Sui Xiong Cai , Mark B. Anderson , Adam Willardsen , Songchun Jiang , Robert J. Halter , Rachel Slade , Yevgeniya Klimova
IPC分类号： C07D403/12 , C07D253/08 , A61K31/53 , A61P35/00
CPC分类号： C07D237/34 , C07D253/08
摘要： Disclosed are 1-arylamino-phthalazines, 4-arylamino-benzo[d][1,2,3]triazines, and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
摘要翻译：公开了1-芳基氨基 - 酞嗪，4-芳基氨基 - 苯并[d] [1,2,3]三嗪及其类似物作为胱天蛋白酶的活化剂和凋亡诱导剂。本发明的化合物可用于治疗异常细胞发生不受控制的生长和扩散的各种临床病症。

69. 发明授权

US07592143B2 Methods of treating diseases responsive to induction of apoptosis and screening assays 失效
标题翻译：治疗对凋亡诱导作用的疾病的筛选方法和筛选试验
公开(公告)号：US07592143B2
公开(公告)日：2009-09-22
申请号：US10826909
申请日：2004-04-19
申请人： Shailaja Kasibhatla , Sui Xiong Cai , Ben Tseng , Katayoun Alavi Jessen , Nicole Marion English , Serguei Maliartchouk , Songchun Jiang , Nilantha Sudath Sirisoma , Han-Zhong Zhang , Jared Kuemmerle
发明人： Shailaja Kasibhatla , Sui Xiong Cai , Ben Tseng , Katayoun Alavi Jessen , Nicole Marion English , Serguei Maliartchouk , Songchun Jiang , Nilantha Sudath Sirisoma , Han-Zhong Zhang , Jared Kuemmerle
IPC分类号： G01N33/53
CPC分类号： A61K49/0052 , A61K31/352 , A61K49/0043 , A61K51/0412 , A61K51/0419 , A61K51/0421 , A61K51/0453 , A61K51/0495
摘要： The present invention relates to screening methods useful for drug discovery of apoptosis inducing compounds. In particular, the screening methodology relates to using Apoptosis Inducing Proteins (AIPs) as a target for the discovery of apoptosis activators useful as anticancer agents. The screening methods of the present invention can employ homogenous or heterogeneous binding assays using purified or partially purified AIPs; or whole cell assays using cells with altered levels of one or more AIPs. The invention also contemplates use of gambogic acid or GA-related compounds which bind AIPs and can accordingly be used to raise antibodies useful for drug discovery. Alternatively, labeled GA is used for competitive binding assays for drug discovery. Such assays afford high throughput screening of chemical libraries for apoptosis activators.
摘要翻译：本发明涉及可用于药物发现凋亡诱导化合物的筛选方法。特别地，筛选方法涉及使用细胞凋亡诱导蛋白（AIPs）作为发现用作抗癌剂的凋亡激活剂的靶标。本发明的筛选方法可以使用纯化或部分纯化的AIPs进行均一或异质结合测定; 或使用具有改变水平的一种或多种AIP的细胞的全细胞测定。本发明还考虑使用结合AIP的葡萄糖酸或GA相关化合物，因此可以用于产生可用于药物发现的抗体。或者，标记的GA用于药物发现的竞争性结合测定。这样的测定提供用于凋亡激活剂的化学文库的高通量筛选。

70. 发明授权

US07541465B2 Substituted 2-aminoacetamides and the use thereof 失效
标题翻译：取代的2-氨基乙酰胺及其用途
公开(公告)号：US07541465B2
公开(公告)日：2009-06-02
申请号：US11443174
申请日：2006-05-31
申请人： Nancy Lan , Yan Wang , Sui Xiong Cai
发明人： Nancy Lan , Yan Wang , Sui Xiong Cai
IPC分类号： C07D211/94 , C07D211/96 , C07D211/98 , A61K31/513
CPC分类号： C07C233/05 , A61K31/165 , C07C237/06 , C07C237/08 , C07C2601/14 , C07D211/46 , C07D213/65 , C07D213/68 , C07D215/20 , C07D239/34 , C07D241/08 , C07D309/12 , C07D317/64
摘要： The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
摘要翻译：本发明涉及由式（II）表示的取代的2-氨基乙酰胺及其药学上可接受的盐和前药，其中取代基在本文中定义。本发明还涉及取代的2-氨基乙酰胺在治疗全球和局灶性缺血后的神经元损伤的方法中的用途，以及用作治疗，预防或改善疼痛的抗惊厥药作为抗痉挛剂，作为局部麻醉剂，如抗心律失常药物和治疗或预防糖尿病性神经病变。

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