公开(公告)号：US5057499A

公开(公告)日：1991-10-15

申请号：US360621

申请日：1989-06-02

Applicant: Helmut Mrozik ,  Peter J. Sinclair

Inventor： Helmut Mrozik ,  Peter J. Sinclair

IPC: C07H17/08 ,  A01N43/90 ,  A61K31/365 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P33/10 ,  C07D493/22 ,  C07H19/01

CPC classification number: C07H19/01 ,  A01N43/90

Abstract: There are disclosed novel avermectin derivatives wherein the outer oleandrose ring of avermectin or avermectin monosaccharide is homologated by addition of diazomethane to 4"- or 4'-oxo-avermectin to afford the perhydrooxepine derivatives. The homologated avermectins can then be further derivatized to afford additional novel avermectins. The new compounds are potent antiparasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

公开(公告)号：US4978656A

公开(公告)日：1990-12-18

申请号：US231318

申请日：1988-08-12

Applicant: Timothy A. Blizzard ,  Helmut Mrozik ,  Gaye Marino ,  Peter J. Sinclair

Inventor： Timothy A. Blizzard ,  Helmut Mrozik ,  Gaye Marino ,  Peter J. Sinclair

IPC: H04N5/222 ,  A01N43/90 ,  A61K31/435 ,  A61K31/495 ,  A61P33/10 ,  C07D471/18 ,  C07D471/22 ,  C07D491/22 ,  C07D498/22 ,  C07F7/18 ,  C07F9/6561 ,  G06T7/00 ,  H04N5/232 ,  H04N5/33 ,  H04N5/365 ,  H04N17/00

CPC classification number: C07D491/22 ,  A01N43/90 ,  C07D498/22 ,  C07F7/1856 ,  C07F9/6561

Abstract: There are disclosed synthetic derivatives of the natural product paraherquamide. The synthetic derivatives are prepared by reactions at the parahequamide A, B, E, F and G rings, that is at carbon atoms 14 to 16, the lactam ring and carbon atoms 24 to 26 as well as carbon atoms 5 and 12. The compounds are active antiparasitic agents and compositions for that use are also disclosed.

公开(公告)号：US5030622A

公开(公告)日：1991-07-09

申请号：US360620

申请日：1989-06-02

Applicant: Helmut Mrozik ,  Peter J. Sinclair

Inventor： Helmut Mrozik ,  Peter J. Sinclair

IPC: C07H17/08 ,  A01N43/90 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P33/10 ,  C07H19/01

CPC classification number: C07H19/01

Abstract: There are disclosed novel avermectin derivatives wherein the outer oleandrose ring of avermectin or avermectin monosaccharide is homologated by addition of diazomethane to 4"- or 4'-oxo-avermectin to afford the oleandrose 4"- or 4'-spiro-epoxide. The homologated avermectins can then be further derivatized to afford additional novel avermectins. The new compounds are potent antiparasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

公开(公告)号：US5830875A

公开(公告)日：1998-11-03

申请号：US429919

申请日：1989-10-30

Applicant: Helmut Mrozik ,  Thomas L. Shih

Inventor： Helmut Mrozik ,  Thomas L. Shih

IPC: 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 classification number: C07H19/01

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5008250A

公开(公告)日：1991-04-16

申请号：US198271

申请日：1988-05-25

Applicant: Michael H. Fisher ,  Matthew J. Wyvratt ,  Helmut Mrozik

Inventor： Michael H. Fisher ,  Matthew J. Wyvratt ,  Helmut Mrozik

IPC: C07H17/08 ,  A01N43/90 ,  A61K31/365 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  A61P33/00 ,  A61P33/10 ,  C07D493/20 ,  C07D493/22 ,  C07H19/01

CPC classification number: C07H19/01 ,  A01N43/90

Abstract: 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.

公开(公告)号：US4895837A

公开(公告)日：1990-01-23

申请号：US296172

申请日：1989-01-13

Applicant: Helmut Mrozik ,  Frank S. Waksmunski

Inventor： Helmut Mrozik ,  Frank S. Waksmunski

IPC: C07H17/08 ,  A01N43/90 ,  A61K31/365 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P33/00 ,  A61P33/10 ,  C07D493/22 ,  C07H19/01

CPC classification number: C07H19/01 ,  A01N43/90

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US4831016A

公开(公告)日：1989-05-16

申请号：US925772

申请日：1986-10-31

Applicant: Helmut Mrozik ,  Thomas L. Shih

Inventor： Helmut Mrozik ,  Thomas L. Shih

IPC: C07D493/22 ,  A01N43/90 ,  A01N47/18 ,  A01N47/24 ,  A01N47/34 ,  A01N51/00 ,  A01N55/00 ,  A23K1/16 ,  A23K1/17 ,  A61K31/365 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P33/00 ,  A61P33/10 ,  C07F7/18 ,  C07H17/08 ,  C07H19/01

CPC classification number: C07H19/01 ,  A01N43/90 ,  A23K20/195

Abstract: There are disclosed novel avermectin reduction products. The compounds are prepared by selective catalytic hydrogenation of avermectin-like compounds or by reaction of selected double bonds with electrophylic reagents. The reduced 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 reduced avermectin compounds have increased stability towards light which prolongs their insecticidal activities when applied to field crops subject to irradiation by sunlight.

公开(公告)号：US5606054A

公开(公告)日：1997-02-25

申请号：US166440

申请日：1993-12-14

Applicant: Michael H. Fisher ,  Helmut Mrozik ,  William R. Schoen ,  Thomas L. Shih ,  Matthew J. Wyvratt

Inventor： Michael H. Fisher ,  Helmut Mrozik ,  William R. Schoen ,  Thomas L. Shih ,  Matthew J. Wyvratt

IPC: C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  A61K31/55

CPC classification number: C07D471/04 ,  C07D487/04 ,  C07D495/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5284841A

公开(公告)日：1994-02-08

申请号：US13448

申请日：1993-02-04

Applicant: Lin Chu ,  Michael H. Fisher ,  Helmut Mrozik ,  William R. Schoen

Inventor： Lin Chu ,  Michael H. Fisher ,  Helmut Mrozik ,  William R. Schoen

IPC: 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 classification number: C07D223/16 ,  C07D403/10 ,  C07D403/14 ,  C07D409/10 ,  C07D409/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  C07K5/06

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5244879A

公开(公告)日：1993-09-14

申请号：US853452

申请日：1992-03-18

Applicant: Peter T. Meinke ,  Helmut Mrozik

Inventor： Peter T. Meinke ,  Helmut Mrozik

IPC: C07H19/01

CPC classification number: C07H19/01

Abstract: Avermectin analogs are prepared where the 23-position ring carbon atom is deleted and replaced by an oxygen atom. The compounds are prepared by opening the outer spiroketal ring to gain access to the 23-position atom, substituting the ring-opened compounds with a substituent containing the oxygen atom in the appropriate position and closing the ring to prepare the desired compounds. The compounds are potent anthelmintic agents and methods and compositions including such 23-nor-23-oxa compounds are also disclosed.

Abstract translation: 制备阿维菌素类似物，其中23位环碳原子被缺失并被氧原子代替。 通过打开外螺旋酮环以获得进入23位原子，用含有氧原子的取代基取代开环化合物在适当位置并封闭环以制备所需化合物来制备化合物。 这些化合物是有效的驱肠剂，并且还公开了包括这种23-降-23-氧杂化合物的方法和组合物。