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公开(公告)号：US5773444A
公开(公告)日：1998-06-30
申请号：US837176
申请日：1997-04-14
申请人： Kyunghye Ahn , Xue-Min Cheng , Annette Marian Doherty , Edward Faith Elslager , Brian Kornberg , Chitase Lee , Daniele Leonard , Sham Nikam , Leslie Morton Werbel
发明人： Kyunghye Ahn , Xue-Min Cheng , Annette Marian Doherty , Edward Faith Elslager , Brian Kornberg , Chitase Lee , Daniele Leonard , Sham Nikam , Leslie Morton Werbel
IPC分类号： C07D239/74 , A61K31/505 , A61K31/517 , A61P43/00 , C07D239/90 , C07D239/91 , C07D239/94 , C07D401/12 , C07D403/12 , C07D453/02 , A61K31/495 , A61K31/535
CPC分类号： C07D401/12 , C07D239/94 , C07D403/12 , C07D453/02
摘要： Novel quinazoline inhibitors of endothelin converting enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin and in controlling hypertension, myocardial infarction and ischemia, metabolic, endocrinological, and neurological disorders, congestive heart failure, endotoxic and hemorrhagic shock, septic shock, subarachnoid hemorrhage, arrhythmias, asthma, acute and chronic renal failure, cyclosporin-A induced nephrotoxicity, angina, gastric mucosal damage, ischemic bowel disease, cancer, pulmonary hypertension, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, cerebral ischemia and vasospasm, and diabetes.
摘要翻译： 描述了内皮素转化酶的新型喹唑啉抑制剂，以及其制备方法及其药物组合物，其可用于治疗高水平的内皮素和控制高血压，心肌梗死和缺血，代谢，内分泌和神经障碍 ，充血性心力衰竭，内毒素性和出血性休克，败血性休克，蛛网膜下腔出血，心律失常，哮喘，急性和慢性肾功能衰竭，环孢菌素A诱导的肾毒性，心绞痛，胃粘膜损伤，缺血性肠病，癌症，肺动脉高压，先兆子痫，动脉粥样硬化 疾病包括雷诺氏病和再狭窄，脑缺血和血管痉挛以及糖尿病。
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公开(公告)号：US5658902A
公开(公告)日：1997-08-19
申请号：US363104
申请日：1994-12-22
申请人： Kyunghye Ahn , Xue-Min Cheng , Annette Marian Doherty , Edward Faith Elslager , Brian Kornberg , Chitase Lee , Daniele Leonard , Sham Nikam , Leslie Morton Werbel
发明人： Kyunghye Ahn , Xue-Min Cheng , Annette Marian Doherty , Edward Faith Elslager , Brian Kornberg , Chitase Lee , Daniele Leonard , Sham Nikam , Leslie Morton Werbel
IPC分类号： C07D239/74 , A61K31/505 , A61K31/517 , A61P43/00 , C07D239/90 , C07D239/91 , C07D239/94 , C07D401/12 , C07D403/12 , C07D453/02 , C07D405/12
CPC分类号： C07D401/12 , C07D239/94 , C07D403/12 , C07D453/02
摘要： Novel quinazoline inhibitors of endothelin converting enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin and in controlling hypertension, myocardial infarction and ischemia, metabolic, endocrinological, and neurological disorders, congestive heart failure, endotoxic and hemorrhagic shock, septic shock, subarachnoid hemorrhage, arrhythmias, asthma, acute and chronic renal failure, cyclosporin-A induced nephrotoxicity, angina, gastric mucosal damage, ischemic bowel disease, cancer, pulmonary hypertension, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, cerebral ischemia and vasospasm, and diabetes.
摘要翻译： 描述了内皮素转化酶的新型喹唑啉抑制剂，以及其制备方法及其药物组合物，其可用于治疗高水平的内皮素和控制高血压，心肌梗死和缺血，代谢，内分泌和神经障碍 ，充血性心力衰竭，内毒素性和出血性休克，败血性休克，蛛网膜下腔出血，心律失常，哮喘，急性和慢性肾功能衰竭，环孢菌素A诱导的肾毒性，心绞痛，胃粘膜损伤，缺血性肠病，癌症，肺动脉高压，先兆子痫，动脉粥样硬化 疾病包括雷诺氏病和再狭窄，脑缺血和血管痉挛以及糖尿病。
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公开(公告)号：US6133270A
公开(公告)日：2000-10-17
申请号：US882846
申请日：1997-06-26
申请人： Gary Louis Bolton , John Michael Domagala , Edward Faith Elslager , Rocco Dean Gogliotti , Terri Stoeber Purchase , Joseph Peter Sanchez , Bharat Kalidas Trivedi
发明人： Gary Louis Bolton , John Michael Domagala , Edward Faith Elslager , Rocco Dean Gogliotti , Terri Stoeber Purchase , Joseph Peter Sanchez , Bharat Kalidas Trivedi
IPC分类号： A61K31/428 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/519 , A61K31/5377 , A61P9/10 , A61P29/00 , A61P31/12 , A61P31/14 , C07D275/04 , C07D417/04 , C07D513/04 , C07D513/14 , A61K31/505
CPC分类号： C07D275/04 , C07D513/04 , C07D513/14
摘要： Isothiazolones having the general structure ##STR1## where A is a monocyclic or bicyclic ring which may contain up to 3 heteroatoms selected from O, S, and N; R.sup.1 and R.sup.2 are substituent groups such as alkyl, alkoxy, hydroxy, nitro, cyano, amino, and carboxy; and R.sup.5 is alkyl, cycloalkyl, phenyl, and Het. The isothiazolones are useful as anti-retroviral agents, anti-inflammatory agents, and anti-atherosclerotic agents.
摘要翻译： 具有一般结构的异噻唑酮，其中A是可以含有至多3个选自O，S和N的杂原子的单环或双环; R1和R2是取代基，例如烷基，烷氧基，羟基，硝基，氰基，氨基和羧基; R5是烷基，环烷基，苯基和Het。 异噻唑酮可用作抗逆转录病毒剂，抗炎剂和抗动脉粥样硬化剂。
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公开(公告)号：US5889034A
公开(公告)日：1999-03-30
申请号：US40777
申请日：1998-03-18
申请人： Gary Louis Bolton , John Michael Domagala , Edward Faith Elslager , Rocco Dean Gogliotti , Terri Stoeber Purchase , Joseph Peter Sanchez , Bharat Kalidas Trivedi
发明人： Gary Louis Bolton , John Michael Domagala , Edward Faith Elslager , Rocco Dean Gogliotti , Terri Stoeber Purchase , Joseph Peter Sanchez , Bharat Kalidas Trivedi
IPC分类号： C07D275/04 , C07D513/04 , A61K31/41
CPC分类号： C07D275/04 , C07D513/04
摘要： Isothiazolones having the general structure ##STR1## where A is a monocyclic or bicyclic ring which may contain up to 3 heteroatoms selected from O, S, and N; R.sup.1 and R.sup.2 are substituent groups such as alkyl, alkoxy, hydroxy, nitro, cyano, amino, and carboxy; and R.sup.5 is alkyl, cycloalkyl, phenyl, and Het. The isothiazolones are useful as anti-retroviral agents, anti-inflammatory agents, and anti-atherosclerotic agents.
摘要翻译： 具有一般结构
的异噻唑酮，其中A是可以含有至多3个选自O，S和N的杂原子的单环或双环; R1和R2是取代基，例如烷基，烷氧基，羟基，硝基，氰基，氨基和羧基; R5是烷基，环烷基，苯基和Het。 异噻唑酮可用作抗逆转录病毒剂，抗炎剂和抗动脉粥样硬化剂。 -
公开(公告)号：US5733921A
公开(公告)日：1998-03-31
申请号：US757716
申请日：1996-11-26
申请人： Gary Louis Bolton , John Michael Domagala , Edward Faith Elslager , Rocco Dean Gogliotti , Terri Stoeber Purchase , Joseph Peter Sanchez , Bharat Kalidas Trivedi
发明人： Gary Louis Bolton , John Michael Domagala , Edward Faith Elslager , Rocco Dean Gogliotti , Terri Stoeber Purchase , Joseph Peter Sanchez , Bharat Kalidas Trivedi
IPC分类号： A61K31/428 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/519 , A61K31/5377 , A61P9/10 , A61P29/00 , A61P31/12 , A61P31/14 , C07D275/04 , C07D417/04 , C07D513/04 , C07D513/14 , A61K31/41
CPC分类号： C07D275/04 , C07D513/04 , C07D513/14
摘要： Isothiazolones having the general structure ##STR1## where A is a monocyclic or bicyclic ring which may contain up to 3 heteroatoms selected from O, S, and N; R.sup.1 and R.sup.2 are substituent groups such as alkyl, alkoxy, hydroxy, nitro, cyano, amino, and carboxy; and R.sup.5 is alkyl, cycloalkyl, phenyl, and Het. The isothiazolones are useful as anti-retroviral agents, anti-inflammatory agents, and anti-atherosclerotic agents.
摘要翻译： 具有一般结构
的异噻唑酮，其中A是可以含有至多3个选自O，S和N的杂原子的单环或双环; R1和R2是取代基，例如烷基，烷氧基，羟基，硝基，氰基，氨基和羧基; R5是烷基，环烷基，苯基和Het。 异噻唑酮可用作抗逆转录病毒剂，抗炎剂和抗动脉粥样硬化剂。 -
公开(公告)号：US6001863A
公开(公告)日：1999-12-14
申请号：US882845
申请日：1997-06-26
申请人： Gary Louis Bolton , John Michael Domagala , Edward Faith Elslager , Rocco Dean Gogliotti , Terri Stoeber Purchase , Joseph Peter Sanchez , Bharat Kalidas Trivedi
发明人： Gary Louis Bolton , John Michael Domagala , Edward Faith Elslager , Rocco Dean Gogliotti , Terri Stoeber Purchase , Joseph Peter Sanchez , Bharat Kalidas Trivedi
IPC分类号： C07D275/04 , C07D513/04 , A61K31/41
CPC分类号： C07D275/04 , C07D513/04
摘要： Isothiazolones having the general structure ##STR1## where A is a monocyclic or bicyclic ring which may contain up to 3 heteroatoms selected from O, S, and N; R.sup.1 and R.sup.2 are substituent groups such as alkyl, alkoxy, hydroxy, nitro, cyano, amino, and carboxy; and R.sup.5 is alkyl, cycloalkyl, phenyl, and Het. The isothiazolones are useful as anti-retroviral agents, anti-inflammatory agents, and anti-atherosclerotic agents.
摘要翻译： 具有一般结构的异噻唑酮，其中A是可以含有至多3个选自O，S和N的杂原子的单环或双环; R1和R2是取代基，例如烷基，烷氧基，羟基，硝基，氰基，氨基和羧基; R5是烷基，环烷基，苯基和Het。 异噻唑酮可用作抗逆转录病毒剂，抗炎剂和抗动脉粥样硬化剂。
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公开(公告)号：US4026899A
公开(公告)日：1977-05-31
申请号：US670762
申请日：1976-03-26
IPC分类号： C07D491/06 , C07D495/06
CPC分类号： C07D495/06 , C07D491/06
摘要： 2H(1)Benzothiopyrano[4,3,2-cd]indazole N-oxides, 2H(1)benzopyrano[4,3,2-cd]indazole N-oxides and acid addition salts thereof are disclosed. These compounds can be produced by oxidation of the corresponding amines with oxidizing agents capable of forming an N-oxide derivative. The compounds are parasiticidal agents useful in the treatment of schistosome infections.
摘要翻译： 2H（1）苯并噻喃并[4,3,2-cd]吲唑N-氧化物，2H（1）苯并吡喃并[4,3,2-cd]吲唑N-氧化物及其酸加成盐。 这些化合物可以通过用能够形成N-氧化物衍生物的氧化剂氧化相应的胺来制备。 这些化合物是可用于治疗血吸虫感染的杀寄生虫剂。
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公开(公告)号：US5929114A
公开(公告)日：1999-07-27
申请号：US857116
申请日：1997-05-15
IPC分类号： C07D295/16 , A61K31/105 , A61K31/165 , A61K31/166 , A61K31/167 , A61K31/18 , A61K31/195 , A61K31/198 , A61K31/215 , A61K31/216 , A61K31/225 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/495 , A61K31/54 , A61K31/63 , A61K38/00 , A61P31/04 , A61P31/12 , C07C323/22 , C07C323/47 , C07C323/62 , C07C323/63 , C07C323/65 , C07C323/67 , C07D207/08 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/60 , C07D211/62 , C07D213/82 , C07D239/42 , C07D239/69 , C07D295/13 , C07D295/18 , C07D295/192 , C07D295/205 , C07D333/20 , C07D333/36 , C07D333/38 , C07D521/00 , C07F9/40 , C07K5/06 , A01N37/20
CPC分类号： C07D207/08 , A61K31/166 , A61K31/167 , A61K31/198 , A61K31/216 , A61K31/225 , A61K31/63 , C07C323/22 , C07C323/47 , C07C323/62 , C07C323/63 , C07C323/65 , C07C323/67 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/62 , C07D213/82 , C07D239/42 , C07D239/69 , C07D295/13 , C07D295/192 , C07D295/205 , C07D333/20 , C07F9/4056 , C07K5/06043 , A61K38/00 , C07C2101/02 , C07C2101/14
摘要： Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O, S, and N,R.sup.1 and R.sup.2 are substituent groups, X is ##STR2## or SO.sub.2 NR.sup.4 Z, Y is H or SZ when n is 1, a single bond when n is 2; R.sup.4 and Z can be hydrogen or alkyl.
摘要翻译： 芳硫醇和二硫代二芳基酰胺抗菌和抗病毒剂具有以下通式：其中A是可以含有至多3个选自O，S和N的杂原子的单环或双环芳基，R 1和R 2是取代基，X是或SO 2 NR 4 Z，Y是H或 当n为1时为SZ，n为2时为单键; R4和Z可以是氢或烷基。
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公开(公告)号：US5734081A
公开(公告)日：1998-03-31
申请号：US446917
申请日：1995-06-01
IPC分类号： C07D295/16 , A61K31/105 , A61K31/165 , A61K31/166 , A61K31/167 , A61K31/18 , A61K31/195 , A61K31/198 , A61K31/215 , A61K31/216 , A61K31/225 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/495 , A61K31/54 , A61K31/63 , A61K38/00 , A61P31/04 , A61P31/12 , C07C323/22 , C07C323/47 , C07C323/62 , C07C323/63 , C07C323/65 , C07C323/67 , C07D207/08 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/60 , C07D211/62 , C07D213/82 , C07D239/42 , C07D239/69 , C07D295/13 , C07D295/18 , C07D295/192 , C07D295/205 , C07D333/20 , C07D333/36 , C07D333/38 , C07D521/00 , C07F9/40 , C07K5/06 , C07C303/00
CPC分类号： C07D207/08 , A61K31/166 , A61K31/167 , A61K31/198 , A61K31/216 , A61K31/225 , A61K31/63 , C07C323/22 , C07C323/47 , C07C323/62 , C07C323/63 , C07C323/65 , C07C323/67 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/62 , C07D213/82 , C07D239/42 , C07D239/69 , C07D295/13 , C07D295/192 , C07D295/205 , C07D333/20 , C07F9/4056 , C07K5/06043 , A61K38/00 , C07C2101/02 , C07C2101/14
摘要： Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O, S, and N, R.sup.1 and R.sup.2 are substituent groups, X is ##STR2## or SO.sub.2 NR.sup.4 Z, Y is H or SZ when n is 1, a single bond when n is 2; R.sup.4 and Z can be hydrogen or alkyl.
摘要翻译： 芳硫醇和二硫代双芳酰胺抗菌和抗病毒剂具有通式
，其中A是可以含有至多3个选自O，S和N的杂原子的单环或双环芳基，R 1和R 2是取代基，X是<或> SO2NR4Z，当n为1时，Y为H或SZ，n为2时为单键; R4和Z可以是氢或烷基。 -
公开(公告)号：US3963740A
公开(公告)日：1976-06-15
申请号：US507634
申请日：1974-09-20
IPC分类号： C07D491/06 , C07D495/06 , C07D231/56 , A61K31/415
CPC分类号： C07D495/06 , C07D491/06
摘要： 2H(1)Benzothiopyrano[4,3,2-cd]indazole N-oxides, 2H(1)benzopyrano[4,3,2-cd]indazole N-oxides and acid addition salts thereof are disclosed. These compounds can be produced by oxidation of the corresponding amines with oxidizing agents capable of forming an N-oxide derivative. The compounds are parasiticidal agents useful in the treatment of schistosome infections.
摘要翻译： 2H（1）苯并噻喃并[4,3,2-cd]吲唑N-氧化物，2H（1）苯并吡喃并[4,3,2-cd]吲唑N-氧化物及其酸加成盐。 这些化合物可以通过用能够形成N-氧化物衍生物的氧化剂氧化相应的胺来制备。 这些化合物是可用于治疗血吸虫感染的杀寄生虫剂。
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