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1. 发明授权

US06949516B2 Dipeptide apoptosis inhibitors and the use thereof 失效
公开(公告)号：US06949516B2
公开(公告)日：2005-09-27
申请号：US10429095
申请日：2003-05-05
申请人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe , Eckard Weber
发明人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe , Eckard Weber
IPC分类号： A61K38/00 , C07C237/22 , C07C271/22 , C07C323/60 , C07D233/54 , C07D277/16 , C07K5/06 , A61K38/04 , C07C233/45 , C07K5/04
CPC分类号： C07D233/64 , A61K38/00 , C07C237/22 , C07C271/22 , C07C323/60 , C07D277/16 , C07K5/06191 , C12N2810/40 , Y10S514/885
摘要： The present invention is directed to novel dipeptides thereof, represented by the general Formula I: where R1-R3 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.

2. 发明授权

US06596693B1 Dipeptide apoptosis inhibitors and the thereof 失效
标题翻译：二肽凋亡抑制剂及其
公开(公告)号：US06596693B1
公开(公告)日：2003-07-22
申请号：US09653279
申请日：2000-08-31
申请人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe , Eckard Weber
发明人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe , Eckard Weber
IPC分类号： A61K3805
CPC分类号： C07D233/64 , A61K38/00 , C07C237/22 , C07C271/22 , C07C323/60 , C07D277/16 , C07K5/06191 , C12N2810/40 , Y10S514/885
摘要： The present invention is directed to novel dipeptides thereof, represented by the general Formula I: where R1-R3 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
摘要翻译：本发明涉及其由通式I表示的新型二肽：其中R1-R3和AA在本文中定义。本发明涉及发现具有式I的化合物是凋亡性细胞死亡的有效抑制剂。因此，本发明的抑制剂可以在发生细胞，组织或整个器官的损失的各种临床病症中阻滞或阻断细胞死亡。

3. 发明授权

US06184210B2 Dipeptide apoptosis inhibitors and the use thereof 有权
标题翻译：二肽凋亡抑制剂及其用途
公开(公告)号：US06184210B2
公开(公告)日：2001-02-06
申请号：US09270736
申请日：1999-03-16
申请人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe
发明人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe
IPC分类号： A61K3805
CPC分类号： C07D233/64 , A61K38/00 , C07C237/22 , C07C271/22 , C07C323/60 , C07D277/16 , C07K5/06191 , C12N2810/40 , Y10S514/885
摘要： The present invention is directed to novel dipeptides thereof, represented by the general Formula I: where R1-R3 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
摘要翻译：本发明涉及其由通式I表示的新型二肽：其中R1-R3和AA在本文中定义。本发明涉及发现具有式I的化合物是凋亡性细胞死亡的有效抑制剂。因此，本发明的抑制剂可以在发生细胞，组织或整个器官的损失的各种临床病症中阻滞或阻断细胞死亡。

4. 发明授权

US07270801B2 Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for caspases and other enzymes and the use thereof 失效
标题翻译：荧光或荧光报告分子及其在半胱氨酸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：US07270801B2
公开(公告)日：2007-09-18
申请号：US10829381
申请日：2004-04-22
申请人： Eckard Weber , Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
发明人： Eckard Weber , Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
IPC分类号： A61N49/00
CPC分类号： G01N15/1456 , C12Q1/68 , G01N33/533 , G01N2015/1006 , G01N2015/1488 , Y10S436/80
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, dipeptidyl peptidase IV, calpain, 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，二肽基肽酶IV，钙蛋白酶，氨基肽酶，HIV蛋白酶，腺病毒蛋白酶，HSV-1蛋白酶的活性的新型荧光和荧光报告分子和新的酶测定方法， HCMV蛋白酶和HCV蛋白酶。

5. 发明授权

US06342611B1 Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for capsases and other enzymes and the use thereof 失效
标题翻译：荧光或荧光报道分子及其在全酶抑制剂中的应用及其用途
公开(公告)号：US06342611B1
公开(公告)日：2002-01-29
申请号：US09168888
申请日：1998-10-09
申请人： Eckard Weber , Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
发明人： Eckard Weber , Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
IPC分类号： C07D31188
CPC分类号： G01N15/1456 , C12Q1/68 , G01N33/533 , G01N2015/1006 , G01N2015/1488 , Y10S436/80
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, dipeptidyl peptidase IV, calpain, 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，二肽基肽酶IV，钙蛋白酶，氨基肽酶，HIV蛋白酶，腺病毒蛋白酶，HSV-1蛋白酶的活性的新型荧光和荧光报告分子和新的酶测定方法， HCMV蛋白酶和HCV蛋白酶。

6. 发明授权

US06759207B2 Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for caspases and other enzymes and the use thereof 失效
标题翻译：荧光或荧光报告分子及其在半胱氨酸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：US06759207B2
公开(公告)日：2004-07-06
申请号：US09947387
申请日：2001-09-07
申请人： Eckard Weber , Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
发明人： Eckard Weber , Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
IPC分类号： G01N33573
CPC分类号： G01N15/1456 , C12Q1/68 , G01N33/533 , G01N2015/1006 , G01N2015/1488 , Y10S436/80
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, dipeptidyl peptidase IV, calpain, 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，二肽基肽酶IV，钙蛋白酶，氨基肽酶，HIV蛋白酶，腺病毒蛋白酶，HSV-1蛋白酶的活性的新型荧光和荧光报告分子和新的酶测定方法， HCMV蛋白酶和HCV蛋白酶。

7. 发明授权

US06335429B1 Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for caspases and other enzymes and the use thereof 有权
标题翻译：荧光或荧光报告分子及其在半胱氨酸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：US06335429B1
公开(公告)日：2002-01-01
申请号：US09521650
申请日：2000-03-08
申请人： Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
发明人： Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
IPC分类号： C07K1702
CPC分类号： G01N15/1456 , C12Q1/68 , G01N33/533 , G01N2015/1006 , G01N2015/1488 , Y10S436/80
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, dipeptidyl peptidase IV, calpain, 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，二肽基肽酶IV，钙蛋白酶，氨基肽酶，HIV蛋白酶，腺病毒蛋白酶，HSV-1蛋白酶的活性的新型荧光和荧光报告分子和新的酶测定方法， HCMV蛋白酶和HCV蛋白酶。

8. 发明授权

US06534525B1 2-substituted piperidine analogs and their use as subtype-selective NMDA receptor antagonists 失效
标题翻译： 2-取代的哌啶类似物及其作为亚型选择性NMDA受体拮抗剂的用途
公开(公告)号：US06534525B1
公开(公告)日：2003-03-18
申请号：US09598162
申请日：2000-06-21
申请人： Christopher F. Bigge , John F. W. Keana , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Anthony P. Guzikowski
发明人： Christopher F. Bigge , John F. W. Keana , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Anthony P. Guzikowski
IPC分类号： A61K31445
CPC分类号： C07D401/12 , A61K31/445 , A61K31/454 , C07D211/14
摘要： Novel 2-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 2-substituted piperidine analogs as selectively active antagonist of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headaches, chronics pain, glaucoma, CMV retinitis, psychosis, urinary incontinence, opioid tolerance or withdrawal, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.
摘要翻译：新的2-取代的哌啶类似物，含有它们的药物组合物和使用2-取代的哌啶类似物作为N-甲基-D-天冬氨酸（NMDA）受体亚型的选择性活性拮抗剂的方法，用于治疗诸如中风，脑缺血，中枢神经系统创伤，低血糖症，焦虑症，抽搐，氨基糖苷类抗生素诱发的听力损失，偏头痛，脊髓痛，青光眼，CMV视网膜炎，精神病，尿失禁，阿片样物质耐受或戒断，或神经退行性疾病，如幻影，阿尔茨海默病，帕金森综合征并描述亨廷顿氏病。

9. 发明授权

US06124323A 4-substituted piperidine analogs and their use as subtype selective NMDA receptor antagonists 失效
标题翻译： 4-取代的哌啶类似物及其作为亚型选择性NMDA受体拮抗剂的用途
公开(公告)号：US06124323A
公开(公告)日：2000-09-26
申请号：US091598
申请日：1998-09-16
申请人： Christopher F. Bigge , Po-Wai Yuen , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Zhang-Lin Zhou , John F. W. Keana , Anthony P. Guzikowski
发明人： Christopher F. Bigge , Po-Wai Yuen , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Zhang-Lin Zhou , John F. W. Keana , Anthony P. Guzikowski
IPC分类号： C07D211/14 , C07D211/18 , C07D211/22 , C07D211/28 , C07D211/30 , C07D211/38 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D417/12 , C07D487/04 , A01N43/40 , C07D211/20 , C07D211/26 , C07D211/60
CPC分类号： C07D401/04 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/28 , C07D211/30 , C07D211/38 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/64 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D417/12 , C07D487/04
摘要： Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs are selective active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, psychosis, anxiety, migraine headaches, glaucoma, CMV retinitis, aminoglycoside antibiotics-induced hearing loss, convulsions, chronic pain, opioid tolerance or withdrawal, urinary incontinence or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.
摘要翻译： PCT No.PCT / US96 / 20872 Sec。 371日期：1998年9月16日 102（e）1998年9月16日PCT PCT 1996年12月20日PCT公布。第WO97 / 23216号公报日期1997年7月3日新颖的4-取代的哌啶类似物，含有它们的药物组合物和使用4-取代的哌啶类似物的方法是N-甲基-D-天冬氨酸（NMDA）受体亚型的选择性活性拮抗剂，用于治疗诸如中风，脑缺血，中枢神经系统创伤，低血糖症，精神病，焦虑症，偏头痛，青光眼，CMV视网膜炎，氨基糖苷类抗生素诱发的听力损失，惊厥，慢性疼痛，阿片样物质耐受或戒断，尿失禁或神经退行性疾病，如幻影，描述了阿尔茨海默病，帕金森综合征和亨廷顿氏病。

10. 发明授权

US06458843B1 Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof 有权
标题翻译：碳环和杂环取代的缩氨基脲和缩氨基硫脲和其用途
公开(公告)号：US06458843B1
公开(公告)日：2002-10-01
申请号：US09421403
申请日：1999-10-21
申请人： Yan Wang , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana , Victor I. Ilyin , Eckard Weber
发明人： Yan Wang , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana , Victor I. Ilyin , Eckard Weber
IPC分类号： A61K3117
CPC分类号： C07D213/643 , A61K31/17 , A61K31/175 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/505 , C07C281/12 , C07C281/14 , C07C2601/14 , C07D209/14 , C07D211/46 , C07D213/68 , C07D215/12 , C07D307/91 , C07D309/12 , C07D317/50 , C07D317/58 , C07D317/62 , C07D317/64 , C07D319/18
摘要： This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; 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 or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention also is directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones 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), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.
摘要翻译：本发明涉及由式I表示的碳环和杂环取代的缩氨基脲和缩氨基硫脲或其药学上可接受的盐或前药，其中：Y是氧或硫; R1，R21，R22和R23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R 22和R 23与N一起形成杂环; 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1或O，S，NR 24，CR 25 R 26，C（O），NR 24 C（O），C（O）NR 24，SO，SO 2或共价键; 其中R 24，R 25和R 26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。本发明还涉及使用碳环和杂环取代的缩氨基脲和缩氨基硫脲来治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS），用于治疗和预防涉及谷氨酸毒性和治疗，预防或改善疼痛，作为抗惊厥药，以及作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病和尿失禁的抗疟药抑制剂。

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