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公开(公告)号：US4977276A
公开(公告)日：1990-12-11
申请号：US458132
申请日：1989-12-28
申请人： Kenneth D. Berlin , Warren T. Ford , Shirish N. Rajadhyaksha , Jonathan B. Gale , Lyle W. Spruce
发明人： Kenneth D. Berlin , Warren T. Ford , Shirish N. Rajadhyaksha , Jonathan B. Gale , Lyle W. Spruce
IPC分类号： C07D307/79 , C07D311/58 , C07D333/54 , C07D335/06 , C07D407/06 , C07D409/12
CPC分类号： C07D307/79 , C07D311/58 , C07D333/54 , C07D335/06 , C07D407/06 , C07D409/12
摘要： Novel heteroarotinoid compositions characterized by the formulae: ##STR1## where: X is S or O; OAc is the acetate group ##STR2## and R is --H, --OH, --OCH.sub.3, or --OC.sub.2 H.sub.5 and includes ##STR3## for formulae (1) and (2). Such compositions exhibit activity as anticancer agents.
摘要翻译： 特征在于以下结构式的新型杂亚油酸酯组合物：其中：X是S或O;其中：X是S或O; OAc是乙酸酯基团，R是-H，-OH，-OCH 3或-OC 2 H 5，并且包括式（1）和（2）的
。 这样的组合物表现出作为抗癌剂的活性。 -
公开(公告)号：US4833254A
公开(公告)日：1989-05-23
申请号：US48586
申请日：1987-05-11
申请人： Kenneth D. Berlin , Warren T. Ford , Shirish N. Rajadhyaksha , Jonathan B. Gale , Lyle W. Spruce
发明人： Kenneth D. Berlin , Warren T. Ford , Shirish N. Rajadhyaksha , Jonathan B. Gale , Lyle W. Spruce
IPC分类号： C07D307/79 , C07D311/58 , C07D333/54 , C07D335/06 , C07D407/06 , C07D409/12
CPC分类号： C07D307/79 , C07D311/58 , C07D333/54 , C07D335/06 , C07D407/06 , C07D409/12
摘要： Novel heteroarotinoid compositions characterized by the formulae: ##STR1## where: X is S or O; OAc is the acetate group ##STR2## and R is --H, --OH, --OCH.sub.3, or --OC.sub.2 H.sub.5 and includes ##STR3## for formulae (1) and (2). Such compositions exhibit activity as anticancer agents.
摘要翻译： （E）异构体（Z）异构体（E）异构体（Z）异构体（Z）异构体（Z）异构体 其中：X为S或O; OAc是乙酸酯基团，R是-H，-OH，-OCH 3或-OC 2 H 5，并且包括式（1）和（2）的
。 这样的组合物表现出作为抗癌剂的活性。 -
公开(公告)号：US07071218B2
公开(公告)日：2006-07-04
申请号：US10298024
申请日：2002-11-15
申请人： Magnus Pfahl , Catherine Tachdjian , Lyle W. Spruce , Hussien A. Al-Shamma , Mohamed Boudjelal , Andrea N. Fanjul , Torsten R. Wiemann , David P. M. Pleynet
发明人： Magnus Pfahl , Catherine Tachdjian , Lyle W. Spruce , Hussien A. Al-Shamma , Mohamed Boudjelal , Andrea N. Fanjul , Torsten R. Wiemann , David P. M. Pleynet
IPC分类号： A61K31/426 , C07D277/36 , C07D401/02
CPC分类号： C07D277/20 , C07D417/06 , C07D417/10 , C07D417/14
摘要： The present invention relates to certain compounds of Formula (I) which can be useful in the treatment of diseases, such as, cancer, metabolic disorders, Type 2 Diabetes, dyslipidemia and/or hyperchloesterolemia:
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4.发明授权Thiazolidinedione derivatives for the treatment of diabetes and other diseases 失效噻唑烷二酮衍生物用于治疗糖尿病等疾病公开(公告)号：US06765013B2
公开(公告)日：2004-07-20
申请号：US10334932
申请日：2002-12-31
申请人： Magnus Pfahl , Catherine Tachdjian , Hussien A. Al-Shamma , Andrea Fanjul , David P. M. Pleynet , Lyle W. Spruce
发明人： Magnus Pfahl , Catherine Tachdjian , Hussien A. Al-Shamma , Andrea Fanjul , David P. M. Pleynet , Lyle W. Spruce
IPC分类号： A61K31425
CPC分类号： C07D277/20 , C07D233/40 , C07D233/42 , C07D233/72 , C07D233/84 , C07D233/86 , C07D233/96 , C07D261/12 , C07D277/34 , C07D277/36 , C07D401/06 , C07D401/10 , C07D403/10 , C07D405/10 , C07D417/06 , C07D417/10
摘要： The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease.
摘要翻译： 本发明涉及某些可用于治疗与脂质和碳水化合物代谢有关的疾病的取代的式（I）的杂环，例如2型糖尿病，脂肪细胞分化，不受控制的增殖，例如淋巴瘤，霍奇金病，白血病，乳腺癌 一般癌症，前列腺癌或癌症; 和炎症，例如骨关节炎，类风湿性关节炎，克罗恩病或炎症性肠病。
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5.发明授权公开(公告)号：US06515003B1
公开(公告)日：2003-02-04
申请号：US09652810
申请日：2000-08-31
申请人： Magnus Pfahl , Catherine Tachdjian , Hussien A. Al-Shamma , Andrea Fanjul , David P. M. Pleynet , Lyle W. Spruce
发明人： Magnus Pfahl , Catherine Tachdjian , Hussien A. Al-Shamma , Andrea Fanjul , David P. M. Pleynet , Lyle W. Spruce
IPC分类号： C07D27734
CPC分类号： C07D277/20 , C07D233/40 , C07D233/42 , C07D233/72 , C07D233/84 , C07D233/86 , C07D233/96 , C07D261/12 , C07D277/34 , C07D277/36 , C07D401/06 , C07D401/10 , C07D403/10 , C07D405/10 , C07D417/06 , C07D417/10
摘要： The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease.
摘要翻译： 本发明涉及某些可用于治疗与脂质和碳水化合物代谢有关的疾病的取代的式（I）的杂环，例如2型糖尿病，脂肪细胞分化，不受控制的增殖，例如淋巴瘤，霍奇金病，白血病，乳腺癌 一般癌症，前列腺癌或癌症; 和炎症，例如骨关节炎，类风湿性关节炎，克罗恩病或炎症性肠病。
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6.发明授权Indole and tetrahydroisoquinoline containing Alpha-keto oxadiazoles as serine protease inhibitors 失效含有α-酮基恶二唑的吲哚和四氢异喹啉作为丝氨酸蛋白酶抑制剂
公开(公告)号：US6100238A
公开(公告)日：2000-08-08
申请号：US89587
申请日：1998-06-03
申请人： Albert C. Gyorkos , Lyle W. Spruce
发明人： Albert C. Gyorkos , Lyle W. Spruce
IPC分类号： A61K38/00 , C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07K5/083 , C07K5/12 , A61K38/05 , A61K38/06
CPC分类号： C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/06052 , C07K5/06139 , C07K5/06165 , A61K38/00
摘要： The present invention relates to certain substituted oxadiazole nonpeptides, which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.
摘要翻译： 本发明涉及某些取代的恶二唑非肽，其可用作人嗜中性粒细胞弹性蛋白酶（HNE）的抑制剂，用于治疗涉及诸如成人呼吸窘迫综合征，败血性休克和多器官功能衰竭等病症的HNE介导的过程。 一系列研究也表明HNE参与心肌缺血再灌注损伤，肺气肿。 HNE介导的过程涉及诸如关节炎，牙周病，肾小球性肾炎，皮炎，牛皮癣，囊性纤维化，慢性支气管炎，动脉粥样硬化，阿尔茨海默氏病，器官移植，角膜溃疡和恶性肿瘤的侵袭行为等其他病症。
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公开(公告)号：US6015791A
公开(公告)日：2000-01-18
申请号：US984881
申请日：1997-12-04
申请人： Albert Gyorkos , Lyle W. Spruce
发明人： Albert Gyorkos , Lyle W. Spruce
IPC分类号： A61K38/00 , C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07K5/083 , C07K5/12 , A61K31/55 , A61K38/05 , A61K38/06
CPC分类号： C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/0202 , C07K5/06017 , C07K5/06026 , C07K5/06052 , C07K5/06139 , C07K5/06191 , C07K5/0806 , C07K5/0808 , C07K5/0821 , C07K5/0827 , C07K5/12 , A61K38/00
摘要： The present invention relates to certain substituted oxadiazole, thiadiazole, and triazoles, in particular those including a cycloheptane structure, that are useful as serine protease inhibitors, including inhibitors for human neutrophil elastase. Compounds of the invention are useful in treating conditions such as adult respiratory distress syndrome, septic shock, and multiple organ failure.
摘要翻译： 本发明涉及可用作丝氨酸蛋白酶抑制剂的某些取代的恶二唑，噻二唑和三唑，特别是包括环庚烷结构的那些，包括人中性粒细胞弹性蛋白酶抑制剂。 本发明的化合物可用于治疗诸如成人呼吸窘迫综合征，败血性休克和多器官衰竭的病症。
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公开(公告)号：US07196108B2
公开(公告)日：2007-03-27
申请号：US10384391
申请日：2003-03-06
申请人： Magnus Pfahl , Catherine Tachdjian , Hussien A. Al-Shamma , Andrea Fanjul Giachino , Karine Jakubowicz-Jaillardon , Jianhua Guo , Richard M. Fine , Lyle W. Spruce , James W. Zapf
发明人： Magnus Pfahl , Catherine Tachdjian , Hussien A. Al-Shamma , Andrea Fanjul Giachino , Karine Jakubowicz-Jaillardon , Jianhua Guo , Richard M. Fine , Lyle W. Spruce , James W. Zapf
IPC分类号： A61K31/343 , A61K31/381 , A61K31/382 , A61K31/403 , A61K31/4166 , A61K31/427 , A61K31/4353 , A61K31/538 , A61K31/5415 , C07D277/34 , C07D265/36 , C07D243/10 , C07D241/36 , C07D233/72 , C07D223/14 , C07D221/02 , C07D209/04 , C07D335/04 , C07D333/50 , C07D319/14 , C07D311/04 , C07D307/77
CPC分类号： C07D277/20 , C07D417/06 , C07D417/10 , C07D417/14
摘要： The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis.
摘要翻译： 本发明涉及某些具有下列结构的双环杂环，其可用于治疗与脂质和碳水化合物代谢相关的疾病，例如2型糖尿病和动脉粥样硬化。
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9.发明授权Val-pro containing .alpha.-keto oxadiazoles as serine protease inhibitors 失效含有α-酮恶二唑作为丝氨酸蛋白酶抑制剂的Val-pro
公开(公告)号：US6001813A
公开(公告)日：1999-12-14
申请号：US090046
申请日：1998-06-03
申请人： Albert C. Gyorkos , Lyle W. Spruce
发明人： Albert C. Gyorkos , Lyle W. Spruce
IPC分类号： A61K38/00 , C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07K5/083 , C07K5/12 , A61K38/06
CPC分类号： C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/0202 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/06078 , C07K5/06086 , C07K5/06104 , C07K5/06139 , C07K5/06156 , C07K5/06191 , C07K5/0806 , C07K5/12 , A61K38/00
摘要： The present invention relates to certain substituted oxadiazole tripeptides, which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.
摘要翻译： 本发明涉及某些取代的恶二唑三肽，其可用作人嗜中性粒细胞弹性蛋白酶（HNE）的抑制剂，用于治疗涉及诸如成人呼吸窘迫综合征，败血性休克和多器官功能衰竭等病症的HNE介导的过程。 一系列研究也表明HNE参与心肌缺血再灌注损伤，肺气肿。 HNE介导的过程涉及诸如关节炎，牙周病，肾小球性肾炎，皮炎，牛皮癣，囊性纤维化，慢性支气管炎，动脉粥样硬化，阿尔茨海默氏病，器官移植，角膜溃疡和恶性肿瘤的侵袭行为等其他病症。
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公开(公告)号：US6001811A
公开(公告)日：1999-12-14
申请号：US984884
申请日：1997-12-04
申请人： Albert Gyorkos , Lyle W. Spruce
发明人： Albert Gyorkos , Lyle W. Spruce
IPC分类号： A61K38/00 , C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07K5/083 , C07K5/12 , A61K38/05 , A61K38/06 , C07K5/08
CPC分类号： C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/0202 , C07K5/06026 , C07K5/06052 , C07K5/06139 , C07K5/06191 , C07K5/0806 , C07K5/0808 , C07K5/0821 , C07K5/0827 , C07K5/12 , A61K38/00
摘要： The present invention relates to oxadiazole, thiadiazole, and triazole peptoids that are inhibitors of serine protease, specifically human neutrophil elastase; which proteases are useful in treatment of adult respiratory distress syndrome, septic shock, and multiple organ failure.
摘要翻译： 本发明涉及作为丝氨酸蛋白酶，特别是人嗜中性粒细胞弹性蛋白酶抑制剂的恶二唑，噻二唑和三唑拟肽; 哪些蛋白酶可用于治疗成人呼吸窘迫综合征，败血性休克和多器官衰竭。
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