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公开(公告)号：US5008250A
公开(公告)日：1991-04-16
申请号：US198271
申请日：1988-05-25
IPC分类号： C07H17/08 , A01N43/90 , A61K31/365 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , A61P33/00 , A61P33/10 , C07D493/20 , C07D493/22 , C07H19/01
摘要： There are disclosed novel avermectin compounds having a cleaved furan ring and a hydroxy group in the 8a position. Processes for preparing these novel compounds are also disclosed. These compounds have utility as anti-parasitic agents and as insecticides against agricultural pests.
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公开(公告)号：US5606054A
公开(公告)日：1997-02-25
申请号：US166440
申请日：1993-12-14
IPC分类号： C07D471/04 , C07D487/04 , C07D495/04 , A61K31/55
CPC分类号： C07D471/04 , C07D487/04 , C07D495/04
摘要： There are disclosed certain novel compounds identified as heterocyclic-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such heterocyclic-fused lactams as the active ingredient thereof are also disclosed.
摘要翻译： 公开了鉴定为杂环稠合内酰胺的某些新化合物，其促进人和动物中生长激素的释放。 该物质可用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人体中，增加受缺乏正常分泌天然生长激素影响的人的身高。 还公开了含有这样的杂环稠合内酰胺作为其活性成分的生长促进组合物。
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公开(公告)号：US5284841A
公开(公告)日：1994-02-08
申请号：US13448
申请日：1993-02-04
申请人： Lin Chu , Michael H. Fisher , Helmut Mrozik , William R. Schoen
发明人： Lin Chu , Michael H. Fisher , Helmut Mrozik , William R. Schoen
IPC分类号： A61K31/55 , A61P3/00 , A61P3/02 , A61P3/04 , A61P5/00 , A61P43/00 , C07D223/16 , C07D403/10 , C07D403/14 , C07D409/06 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/14 , C07K5/06 , C07D209/34 , C07D215/227
CPC分类号： C07D223/16 , C07D403/10 , C07D403/14 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/14 , C07K5/06
摘要： There are disclosed certain novel compounds identified as benzo-fused lactams ##STR1## which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.
摘要翻译： 公开了一些确定为促进人和动物中生长激素释放的苯并稠合内酰胺的新化合物。 该物质可用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人体中，增加受缺乏正常分泌天然生长激素影响的人的身材。 通过用取代的酰胺官能团取代氨基 - 内酰胺来制备化合物。 还公开了含有这样的苯并稠合内酰胺作为其活性成分的生长促进组合物。
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公开(公告)号：US5789587A
公开(公告)日：1998-08-04
申请号：US744296
申请日：1996-11-06
IPC分类号： C07D471/04 , C07D487/04 , C07D495/04 , A61K31/55
CPC分类号： C07D471/04 , C07D487/04 , C07D495/04
摘要： There are disclosed certain novel compounds identified as heterocyclic-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such heterocyclic-fused lactams as the active ingredient thereof are also disclosed.
摘要翻译： 公开了鉴定为杂环稠合内酰胺的某些新化合物，其促进人和动物中生长激素的释放。 该物质可用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人体中，增加受缺乏正常分泌天然生长激素影响的人的身高。 还公开了含有这样的杂环稠合内酰胺作为其活性成分的生长促进组合物。
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公开(公告)号：US5015630A
公开(公告)日：1991-05-14
申请号：US298710
申请日：1989-01-19
申请人： Michael H. Fisher , Helmut Mrozik
发明人： Michael H. Fisher , Helmut Mrozik
IPC分类号： A01N43/90 , A01N47/34 , A01N55/00 , A61K31/365 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P33/00 , A61P33/10 , C07D493/22 , C07F7/18 , C07H17/08 , C07H19/01
摘要： Novel avermectin derivatives are disclosed, wherein the 5-hydroxy group is replaced by an oxime group. The avermectin-5-oximes can further be derivatized at the 4"- or 4'-positions as amino, substituted amino, acylhydrazone, semicarbazone, or substituted semicarbazone analogues. The avermectin-5-oximes are prepared by the oxidation of the 5-hydroxy compounds with manganese dioxide or with pyridinium dichromate to the known 5-oxo analogues, and these are then reacted with a hydroxylamine salt. The new compounds are potent anti-parasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.
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公开(公告)号：US4806527A
公开(公告)日：1989-02-21
申请号：US26409
申请日：1987-03-16
IPC分类号： C07D493/22 , A01N43/90 , A61K31/365 , A61P33/00 , C07H17/08 , C07H19/01 , A61K31/70 , C07D313/06 , C07H17/04
摘要： There are disclosed derivatives of avermectin compounds with a .DELTA.26,27-alkyl chain of 4, 5 or 6 members at the 25-position. The compounds are prepared from the known .DELTA.26,27-compounds by the appropriate synthetic procedures at the 5-, 8-, 9-, 13- , 22- and 23-positions. The compounds are potent antiparasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.
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公开(公告)号：US5350742A
公开(公告)日：1994-09-27
申请号：US74763
申请日：1993-06-10
IPC分类号： C07H17/08 , A01N43/90 , A61K31/365 , A61K31/366 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P33/00 , A61P33/10 , C07D493/22 , C07H19/01
摘要： Avermectin derivatives are disclosed which incorporate two fluorine atoms at the 4' monosaccharide position, the 4" disaccharide position or the 23 position. Avermectin aglycone derivatives are also disclosed which incorporate two fluorine atoms at position 13 or 23. These difluoro avermectin analogs are derived from corresponding ketones and enones which in turn are prepared by chemical modification of naturally occurring avermectins. These compounds are used as antiparisitic, insecticidal and antihelmintic agents in humans and animals and compositions containing such compounds as the active ingredient thereof are also disclosed.
摘要翻译： 公开了阿维菌素衍生物，其在4'单糖位置，4“二糖位置或23位置引入两个氟原子。 还公开了阿维菌素糖苷配基衍生物，其在13或23位上引入两个氟原子。这些二氟阿维菌素类似物衍生自相应的酮和烯酮，其又通过天然存在的阿凡曼菌素的化学修饰来制备。 这些化合物在人和动物中用作止痛药，杀虫剂和抗脑炎药，还公开了含有其活性成分的化合物的组合物。
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公开(公告)号：US5229416A
公开(公告)日：1993-07-20
申请号：US875486
申请日：1992-04-29
IPC分类号： C07H17/08 , A01N43/90 , A61K31/365 , A61K31/366 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P33/00 , A61P33/10 , C07D493/22 , C07H19/01
摘要： Avermectin derivatives are disclosed which incorporate two fluorine atoms at the 4' monosaccharide position, the 4" disaccharide position or the 23 position. Avermectin aglycone derivatives are also disclosed which incorporate two fluorine atoms at position 13 or 23. These difluoro avermectin analogs are derived from corresponding ketones and enones which in turn are prepared by chemical modification of naturally occurring avermectins. These compounds are used as antiparisitic, insecticidal and antihelmintic agents in humans and animals and compositions containing such compounds as the active ingredient thereof are also disclosed.
摘要翻译： 公开了阿维菌素衍生物，其在4'单糖位置，4“二糖位置或23位置引入两个氟原子。 还公开了阿维菌素糖苷配基衍生物，其在13或23位上引入两个氟原子。这些二氟阿维菌素类似物衍生自相应的酮和烯酮，其又通过天然存在的阿凡曼菌素的化学修饰来制备。 这些化合物在人和动物中用作止痛药，杀虫剂和抗脑炎药，还公开了含有其活性成分的化合物的组合物。
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公开(公告)号：US5830875A
公开(公告)日：1998-11-03
申请号：US429919
申请日：1989-10-30
申请人： Helmut Mrozik , Thomas L. Shih
发明人： Helmut Mrozik , Thomas L. Shih
IPC分类号： C12P17/18 , A01N43/90 , A61K31/365 , A61K31/70 , A61P33/10 , C07D493/22 , C07F7/18 , C07H19/01 , C12R1/465 , A61K31/335 , C07H17/08 , C07D300/00
CPC分类号： C07H19/01
摘要： Novel avermectin and milbemycin derivatives are disclosed, where the C-24 and C-25 carbon atoms are substituted by hydrogen, alkyl, alkenyl, substituted alkyl or substituted alkenyl groups. These compounds can be further substituted at the 4"-, 5-, 13-, and 23-positions. The new C-24 and C-25 substituted avermect prepared by cleavage of known and suitably protected avermectin and milbemycin compounds. The new compounds are potent anti-parasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.
摘要翻译： 公开了新的除虫菌素和米尔倍霉素衍生物，其中C-24和C-25碳原子被氢，烷基，烯基，取代的烷基或取代的烯基取代。 这些化合物可以在4“，5”，“13”和“23”位进一步取代。 通过裂解已知和适当保护的阿维菌素和米尔倍霉素化合物制备的新C-24和C-25取代的除虫剂。 新化合物是有效的抗寄生虫剂，特别是化合物是驱肠虫，杀虫剂和杀螨剂。
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公开(公告)号：US4895837A
公开(公告)日：1990-01-23
申请号：US296172
申请日：1989-01-13
申请人： Helmut Mrozik , Frank S. Waksmunski
发明人： Helmut Mrozik , Frank S. Waksmunski
IPC分类号： C07H17/08 , A01N43/90 , A61K31/365 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P33/00 , A61P33/10 , C07D493/22 , C07H19/01
摘要： There are disclosed novel avermectin .DELTA. 23,24-derivatives (also referred to as 23,24-dehydro compounds). The compounds are prepared by selective dehydration of avermectin A2 or B2 compounds. The avermectin compounds have utility as anti-parasitic agents and compositions for that use are also disclosed. The compounds are also highly potent insecticides against agricultural pests. The .DELTA. 23,24-avermectin compounds have increased activity relative to the A2 or B2 compounds.
摘要翻译： 公开了新的除虫菌素DELTA 23,24衍生物（也称为23,24-脱氢化合物）。 通过阿维菌素A2或B2化合物的选择性脱水制备化合物。 除虫菌素化合物可用作抗寄生虫剂，并且还公开了用于该用途的组合物。 这些化合物对农业有害生物也是非常有效的杀虫剂。 DELTA 23,24-阿维菌素化合物相对于A2或B2化合物具有增加的活性。
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