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1. 发明授权

US4444688A Imidazobenzothiadiazepines 失效
标题翻译：咪唑并噻二氮杂
公开(公告)号：US4444688A
公开(公告)日：1984-04-24
申请号：US406822
申请日：1982-08-09
申请人： Isidoros Vlattas
发明人： Isidoros Vlattas
IPC分类号： C07D233/84 , C07D513/04
CPC分类号： C07D513/04 , C07D233/84
摘要： 5-Diazacycloalkyl-imidazo[2,1-b][1,3,5]benzothiadiazepines, e.g. those of the formula ##STR1## the N-oxides and salts thereof are neuroleptic agents, lacking extrapyramidal side-effects.
摘要翻译： 5-二氮杂环烷基 - 咪唑并[2,1-b] [1,3,5]苯并噻二嗪等。式中R1，R2 = H或烷基R4 = H，烷基或HO烷基; R5 = H，烷基，烷氧基，卤素或CF3; p = 0〜2，N-氧化物及其盐是神经安定药，缺乏锥体束外副作用。

2. 发明授权

US07291635B2 5-substituted 1,1-dioxo-1,2,5,-thiadiazolidin-3-one derivatives 有权
标题翻译： 5-取代的1,1-二氧代-1,2,5-噻二唑烷-3-酮衍生物
公开(公告)号：US07291635B2
公开(公告)日：2007-11-06
申请号：US10510026
申请日：2003-04-02
申请人： Gary Mark Coppola , John William Davies , Charles Francis Jewell, Jr. , Yu-Chin Li , James Richard Wareing , Donald Mark Sperbeck , Travis Mathew Stams , Sidney Wolf Topiol , Isidoros Vlattas
发明人： Gary Mark Coppola , John William Davies , Charles Francis Jewell, Jr. , Yu-Chin Li , James Richard Wareing , Donald Mark Sperbeck , Travis Mathew Stams , Sidney Wolf Topiol , Isidoros Vlattas
IPC分类号： A61K31/433 , C07D285/10
CPC分类号： C07D285/10 , C07D417/06 , C07D417/10 , C07K5/06078
摘要： Compounds of the formula provide pharmacological agents which are inhibitors of PTPases, in particular, the compounds of formula I inhibit PTP-1B and TC PTP, and thus may be employed for the treatment of conditions associated with PTPase activity. The compounds of the present invention may also be employed for inhibition of other enzymes with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula I may be employed for prevention or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels. The compounds of the present invention may also be employed in the treatment, prevention or control of a number of conditions that accompany Type 2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
摘要翻译：式的化合物提供作为PTPase抑制剂的药理学试剂，特别是式I化合物抑制PTP-1B和TC PTP，因此可用于治疗与PTPase活性相关的病症。本发明的化合物也可用于抑制具有磷酸酪氨酸结合区的其它酶，例如SH2结构域。因此，式I化合物可用于预防或治疗与肥胖，葡萄糖不耐受，糖尿病，高血压和大血管和小血管缺血性疾病相关的胰岛素抵抗。本发明的化合物还可用于治疗，预防或控制伴随2型糖尿病的多种病症，包括高脂血症，高甘油三酯血症，动脉粥样硬化，血管再狭窄，肠易激综合征，胰腺炎，脂肪细胞瘤和癌。作为脂肪肉瘤，血脂异常和其他指示胰岛素抵抗的疾病。此外，本发明的化合物可用于治疗或预防癌症，骨质疏松症，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。

3. 发明授权

US4460587A 5-Diazacycloalkyl imidazo[1,2-c][1,3]benzodiazepines 失效
标题翻译： 5-二氮杂环烷基咪唑并[1,2-c] [1,3]苯并二氮杂卓
公开(公告)号：US4460587A
公开(公告)日：1984-07-17
申请号：US444957
申请日：1982-11-29
申请人： Isidoros Vlattas
发明人： Isidoros Vlattas
IPC分类号： C07D233/54 , C07D295/205 , C07D403/12 , C07D487/04 , C07F7/10 , A61K31/415
CPC分类号： C07D233/56 , C07C255/00 , C07D295/205 , C07D403/12 , C07D487/04 , C07F7/10
摘要： 5-Diazacycloalkylimidazo[1,2-c][1,3]benzodiazepines, for example compounds of the formula ##STR1## in which e.g., R.sub.1, R.sub.2 and R.sub.4 are hydrogen, R.sub.3 is methyl and C.sub.n H.sub.2n is CH.sub.2 CH.sub.2, have neuroleptic and/or antihistaminic activity. The synthesis, pharmaceutical compositions and methods of treatment utilizing such compounds are described.
摘要翻译： 5-二氮杂环烷基咪唑并[1,2-c] [1,3]苯并二氮杂，例如其中例如R 1，R 2和R 4为氢，R 3为甲基，C n H 2n为CH 2 CH 2的式IMA化合物，具有精神抑制作用和/ 或抗组胺活性。描述了使用这些化合物的合成，药物组合物和处理方法。

4. 发明申请

US20050090502A1 5-Substituted 1,1-dioxo-'1,2,5!thiazolidine-3-one derivatives as ptpase 1b inhibitors 有权
标题翻译： 5-取代的1,1-二氧代-1,2,5'噻唑烷-3-酮衍生物作为ptpase 1b抑制剂
公开(公告)号：US20050090502A1
公开(公告)日：2005-04-28
申请号：US10510026
申请日：2003-04-02
申请人： Gary Coppola , John Davies , Charles Jewell Jr , Yu-Chin Li , James Wareing , Donald Sperbeck , Travis Stams , Sidney Topiol , Isidoros Vlattas
发明人： Gary Coppola , John Davies , Charles Jewell Jr , Yu-Chin Li , James Wareing , Donald Sperbeck , Travis Stams , Sidney Topiol , Isidoros Vlattas
IPC分类号： A61K31/433 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/5513 , A61K38/55 , A61K45/00 , A61P1/00 , A61P1/18 , A61P3/06 , A61P3/08 , A61P3/10 , A61P5/50 , A61P9/00 , A61P9/10 , A61P9/12 , A61P19/10 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07D285/10 , C07D285/14 , C07D417/02 , C07D417/06 , C07D417/10
CPC分类号： C07D285/10 , C07D417/06 , C07D417/10 , C07K5/06078
摘要： Compounds of the formula provide pharmacological agents which are inhibitors of PTPases, in particular, the compounds of formula I inhibit PTP-1B and TC PTP, and thus may be employed for the treatment of conditions associated with PTPase activity. The compounds of the present invention may also be employed for inhibition of other enzymes with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula I may be employed for prevention or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels. The compounds of the present invention may also be employed in the treatment, prevention or control of a number of conditions that accompany Type 2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
摘要翻译：式的化合物提供作为PTPase抑制剂的药理学试剂，特别是式I化合物抑制PTP-1B和TC PTP，因此可用于治疗与PTPase活性相关的病症。本发明的化合物也可用于抑制具有磷酸酪氨酸结合区的其它酶，例如SH2结构域。因此，式I化合物可用于预防或治疗与肥胖，葡萄糖不耐受，糖尿病，高血压和大血管和小血管缺血性疾病相关的胰岛素抵抗。本发明的化合物还可用于治疗，预防或控制伴随2型糖尿病的多种病症，包括高脂血症，高甘油三酯血症，动脉粥样硬化，血管再狭窄，肠易激综合征，胰腺炎，脂肪细胞瘤和癌。作为脂肪肉瘤，血脂异常和其他指示胰岛素抵抗的疾病。此外，本发明的化合物可用于治疗或预防癌症，骨质疏松症，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。

5. 发明授权

US4665087A 1-(carbamyl, thiocarbamyl, and iminocarbamyl)-indoline derivatives 失效
标题翻译： 1-（氨甲酰基，硫代氨基甲酰基和亚氨基戊酰基） - 二氢吲哚衍生物
公开(公告)号：US4665087A
公开(公告)日：1987-05-12
申请号：US772793
申请日：1985-09-05
申请人： Isidoros Vlattas
发明人： Isidoros Vlattas
IPC分类号： C07D209/42 , A61K31/405 , C07D209/26
CPC分类号： C07D209/42
摘要： 1-(Carbamyl, thiocarbamyl, and iminocarbamyl)-indoline derivatives of the formula ##STR1## where each R.sub.1 is independently alkyl, alkoxy, acyloxy, hydroxy, halo or trifluoromethyl, n is 0, 1, 2 or 3, R.sub.2 and R.sub.3 are independently hydroxy, alkoxy, amino or substituted amino, R.sub.4 and R.sub.5 are independently hydrogen, alkyl or substituted alkyl, R.sub.6 is hydrogen, alkyl or substituted alkyl, and Y is O, S or N--R.sub.7 where R.sub.7 is hydrogen, alkyl, cyano or substituted alkyl, and salts thereof, which are useful as antihypertensive and cardioactive agents, methods of preparing the same, and pharmaceutical compositions thereof, are provided.
摘要翻译：其中每个R 1独立地是烷基，烷氧基，酰氧基，羟基，卤素或三氟甲基，n是0,1,2或3，R 2和R 3是（C 1 -C 6）烷基，独立地是羟基，烷氧基，氨基或取代的氨基，R4和R5独立地是氢，烷基或取代的烷基，R6是氢，烷基或取代的烷基，Y是O，S或N-R7，其中R7是氢，烷基，氰基或取代的烷基及其盐，其可用作抗高血压和心脏活性剂，其制备方法及其药物组合物。

6. 发明授权

US4500472A Process for preparing imidazobenzothiadiazepines 失效
标题翻译：咪唑并噻二氮杂的制备方法
公开(公告)号：US4500472A
公开(公告)日：1985-02-19
申请号：US406760
申请日：1982-08-09
申请人： Isidoros Vlattas
发明人： Isidoros Vlattas
IPC分类号： C07D233/84 , C07D513/04
CPC分类号： C07D513/04 , C07D233/84
摘要： 5-Diazacycloalkyl-imidazo[2,1-b][1,3,5] benzothiadiazepines, e.g. those of the formula ##STR1## R.sub.1, R.sub.2 =H or alkyl R.sub.4 =H, alkyl or HO--alkyl;R.sub.5 =H, alkyl, alkoxy, halo or CF.sub.3 ;p=0 to 2the N-oxides and salts thereof are neuroleptic agents, lacking extrapyramidal side-effects.
摘要翻译： 5-二氮杂环烷基 - 咪唑并[2,1-b] [1,3,5]苯并噻二嗪等。式中R1，R2 = H或烷基R4 = H，烷基或HO-烷基; R5 = H，烷基，烷氧基，卤素或CF3; p = 0〜2，N-氧化物及其盐是神经安定药，缺乏锥体束外副作用。

7. 发明授权

US4077980A 9-Thiaprostaglandins 失效
标题翻译： 9-硫代前列腺素
公开(公告)号：US4077980A
公开(公告)日：1978-03-07
申请号：US741277
申请日：1976-11-12
申请人： Isidoros Vlattas
发明人： Isidoros Vlattas
IPC分类号： A61K31/38 , C07C405/00 , C07D307/20 , C07D307/33 , C07D317/26 , C07D317/30 , C07D333/02 , C07D333/24 , C07D333/32 , C07D333/38 , C07D333/48
CPC分类号： C07D307/33 , C07D307/20 , C07D317/26 , C07D317/30 , C07D333/32 , C07D333/38 , C07D333/48 , Y10S514/826
摘要： 7-[3.alpha.-(3-hydroxy-3-hydrocarbylpropyl, or -1-propenyl, or 1-propynyl)-4-hydroxy-tetrahydro-2.beta.-thienyl]-heptanoic or 5-heptenoic acids, sulfoxides, sulfones, esters or salts thereof are stable, prostaglandin-like acting and antiasthmatic agents.
摘要翻译： 7- [3α-（3-羟基-3-烃基丙基或-1-丙烯基或1-丙炔基）-4-羟基 - 四氢-2β-噻吩基] - 庚酸或5-庚烯酸，亚砜，砜，酯或其盐是稳定的，前列腺素样作用和止喘剂。

8. 发明授权

US4477379A Imidazobenzothiadiazepines 失效
标题翻译：咪唑并噻二氮杂
公开(公告)号：US4477379A
公开(公告)日：1984-10-16
申请号：US406759
申请日：1982-08-09
申请人： Isidoros Vlattas
发明人： Isidoros Vlattas
IPC分类号： C07D233/84 , C07D513/04
CPC分类号： C07D513/04 , C07D233/84
摘要： 5-Diazacycloalkyl-imidazo[imidazo]2,1-b][1,3,5]benzothiadiazepines of the formula ##STR1## e.g. a compound of formula I wherein Ph=phenylene, m=2, n=3, R.sub.1 and R.sub.2 =H, and R.sub.3 =methyl, oxides and salts thereof, are neuroleptic agents.
摘要翻译：式（I）的5-二氮杂环烷基 - 咪唑并[咪唑并[2,1-b] [1,3,5]苯并噻二嗪类式I的化合物，其中Ph =亚苯基，m = 2，n = 3，R 1和R 2 = H，R 3 =甲基，其氧化物和盐是神经安定药剂。

9. 发明授权

US4088779A 9-Oxaprostaglandins 失效
公开(公告)号：US4088779A
公开(公告)日：1978-05-09
申请号：US729572
申请日：1976-10-04
申请人： Isidoros Vlattas
发明人： Isidoros Vlattas
IPC分类号： C07D307/20 , C07D307/24 , C07D307/32 , C07D307/33 , C07D307/42 , C07D307/16 , A61K31/34
CPC分类号： C07D307/33 , C07D307/20 , C07D307/24 , C07D307/32 , C07D307/42
摘要： 7-[3.alpha.-(3-hydroxy-3-hydrocarbylpropyl, or -1-propenyl, or 1-propynyl)-4-hydroxy-tetrahydro-2.beta.-furyl]-heptanoic or 4-heptenoic acids, esters or salts thereof are stable, prostaglandin-like acting agents.
摘要翻译： 7- [3α-（3-羟基-3-烃基丙基或-1-丙烯基或1-丙炔基）-4-羟基 - 四氢-2β-呋喃基] - 庚酸或4-庚烯酸，其酯或其盐是稳定的前列腺素样作用剂。

10. 发明授权

US3970670A 9-Thiaprostaglandins 失效
标题翻译： 9-硫代前列腺素
公开(公告)号：US3970670A
公开(公告)日：1976-07-20
申请号：US516293
申请日：1974-10-21
申请人： Isidoros Vlattas
发明人： Isidoros Vlattas
IPC分类号： A61K31/38 , C07C405/00 , C07D307/20 , C07D307/33 , C07D317/26 , C07D317/30 , C07D333/02 , C07D333/24 , C07D333/32 , C07D333/38 , C07D333/48
CPC分类号： C07D307/33 , C07D307/20 , C07D317/26 , C07D317/30 , C07D333/32 , C07D333/38 , C07D333/48 , Y10S514/826
摘要： 7-[3.alpha.-(3-hydroxy-3-hydrocarbylpropyl,-1-propenyl or -propynyl)-4-hydroxy-tetrahydro-2.beta.-thienyl -heptanoic or 5-heptenoic acids, sulfoxides, sulfones, esters or salts thereof are stable, prostaglandin-like acting and antiasthmatic agents.
摘要翻译： 7- [3α-（3-羟基-3-烃基丙基，-1-丙烯基或 - 丙炔基）-4-羟基 - 四氢-2β-噻吩基 - 庚酸或5-庚烯酸，其亚砜，砜，酯或其盐是稳定的，前列腺素样的作用和抗哮喘药。

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