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1. 发明授权

EP0138708B1 Isoefrotomycin 失效
公开(公告)号：EP0138708B1
公开(公告)日：1988-08-03
申请号：EP84402045.3
申请日：1984-10-11
申请人： Merck & Co., Inc.
发明人： Bochis, Richard J. , Dewey, Ray S.
IPC分类号： C07H15/04 , A61K31/70 , A23K1/17
CPC分类号： C07H15/04

2. 发明公开

EP0151529A3 5-(Amino or substituted amino)-1,2,3-triazoles 失效
标题翻译： 5-（氨基或取代的氨基）-1,2,3-三唑
公开(公告)号：EP0151529A3
公开(公告)日：1988-04-27
申请号：EP85300521
申请日：1985-01-25
申请人： MERCK & CO. INC.
发明人： Bochis, Richard J. , Chabala, John C. , Fisher, Michael H.
IPC分类号： C07D249/04 , A61K31/41
CPC分类号： C07C247/00 , C07C45/42 , C07C45/45 , C07C45/46 , C07C45/63 , C07C45/673 , C07C49/813 , C07C255/00 , C07C317/00 , C07C323/00 , C07D249/04 , C07D249/06 , C07F7/1852
摘要： Novel 5-amino or substituted amino 1,2,3-triazoles have the formula
In which
where p is 0,1 or 2; m is 0, 1, 2, 3 or 4; n is 0, 1, 2, 3, 4 or 5; X Is 0, S, SO, SO 2 , CO, CHCN, CH 2 or C=NRe where R 6 is hydrogen, C 1-3 alkyl, hydroxy, C 1-3 alkoxy, amino, C 1-3 alkylamino, di(C 1-3 alkyl)amino or cyano; and each of R 4 and R 5 , independently of the other, is halogen, cyano, trifluoromethyl, C 1-3 alkanoyl, nitro, C 1-3 alkyl, C 1-3 alkoxy, carboxy, alkoxycarbonyl, trifluoromethoxy, acetamido, C 1-3 alkylthio, C 1-3 alkylsulfinyl, C 1-3 alkylsulfonyl, trichlorovinyl, trifluoromethylthio, trifluoromethylsulfinyl or trifluoromethylsulfonyl;
R 2 is amino, C 1-3 alkylamino, di(C 1-3 alkyl)amino, acetamido, acetimido, ureido, formamido, formimido or guanidino; and R 3 is carbamoyl, cyano, carbazoyl, amidino or N-hydroxycarbamoyl. Such compounds are anticoccidial and are useful for controlling coccidiosis when administered in minor quantities to animals, in particular to poultry, usually in admixture with their feed.

3. 发明公开

EP0151529A2 5-(Amino or substituted amino)-1,2,3-triazoles 失效
标题翻译： 5-（氨基或SUBST。氨基）-1,2,3-三唑。
公开(公告)号：EP0151529A2
公开(公告)日：1985-08-14
申请号：EP85300521.3
申请日：1985-01-25
申请人： Merck & Co., Inc.
发明人： Bochis, Richard J. , Chabala, John C. , Fisher, Michael H.
IPC分类号： C07D249/04 , A61K31/41
CPC分类号： C07C247/00 , C07C45/42 , C07C45/45 , C07C45/46 , C07C45/63 , C07C45/673 , C07C49/813 , C07C255/00 , C07C317/00 , C07C323/00 , C07D249/04 , C07D249/06 , C07F7/1852
摘要： Novel 5-amino or substituted amino 1,2,3-triazoles have the formula
In which
where p is 0,1 or 2; m is 0, 1, 2, 3 or 4; n is 0, 1, 2, 3, 4 or 5; X Is 0, S, SO, SO 2 , CO, CHCN, CH 2 or C=NRe where R 6 is hydrogen, C 1-3 alkyl, hydroxy, C 1-3 alkoxy, amino, C 1-3 alkylamino, di(C 1-3 alkyl)amino or cyano; and each of R 4 and R 5 , independently of the other, is halogen, cyano, trifluoromethyl, C 1-3 alkanoyl, nitro, C 1-3 alkyl, C 1-3 alkoxy, carboxy, alkoxycarbonyl, trifluoromethoxy, acetamido, C 1-3 alkylthio, C 1-3 alkylsulfinyl, C 1-3 alkylsulfonyl, trichlorovinyl, trifluoromethylthio, trifluoromethylsulfinyl or trifluoromethylsulfonyl;

R 2 is amino, C 1-3 alkylamino, di(C 1-3 alkyl)amino, acetamido, acetimido, ureido, formamido, formimido or guanidino; and
R 3 is carbamoyl, cyano, carbazoyl, amidino or N-hydroxycarbamoyl. Such compounds are anticoccidial and are useful for controlling coccidiosis when administered in minor quantities to animals, in particular to poultry, usually in admixture with their feed.

4. 发明公开

EP0138708A2 Isoefrotomycin 失效
公开(公告)号：EP0138708A2
公开(公告)日：1985-04-24
申请号：EP84402045.3
申请日：1984-10-11
申请人： Merck & Co., Inc.
发明人： Bochis, Richard J. , Dewey, Ray S.
IPC分类号： C07H15/04 , A61K31/70 , A23K1/17
CPC分类号： C07H15/04
摘要： © There is disclosed the novel compound isoefrotomycin which is synthesized from efrotomycin as a Michael adduct by treatment with a mixture of polar and nonpolar solvents. Isoefrotomycin is an effective antimicrobial agent and growth promotant in animals.
摘要翻译： ©公开了通过用极性和非极性溶剂的混合物处理由埃托霉素作为迈克尔加合物合成的新型化合物异氟诺沙星。 Isoefrotomycin是动物中有效的抗菌剂和生长促进剂。

5. 发明授权

EP0151529B1 5-(Amino or substituted amino)-1,2,3-triazoles 失效
标题翻译： 5-（氨基或取代的氨基）-1,2,3-三唑
公开(公告)号：EP0151529B1
公开(公告)日：1991-09-18
申请号：EP85300521.3
申请日：1985-01-25
申请人： Merck & Co., Inc.
发明人： Bochis, Richard J. , Chabala, John C. , Fisher, Michael H.
IPC分类号： C07D249/04 , A61K31/41
CPC分类号： C07C247/00 , C07C45/42 , C07C45/45 , C07C45/46 , C07C45/63 , C07C45/673 , C07C49/813 , C07C255/00 , C07C317/00 , C07C323/00 , C07D249/04 , C07D249/06 , C07F7/1852

6. 发明公开

EP0018837A1 3-Substituted imidazo (1,2-a) pyridines, their production, compositions containing them, and their use as anthelmintics 失效
标题翻译： 3-取代的咪唑并吡啶（1,2-a）中，它们的制备，含有它们和它们作为驱肠虫剂的组合物。
公开(公告)号：EP0018837A1
公开(公告)日：1980-11-12
申请号：EP80301440.6
申请日：1980-05-01
申请人： Merck & Co., Inc.
发明人： Bochis, Richard J. , Kulsa, Peter , Tolman, Richard A.
IPC分类号： C07D471/04 , A61K31/44
CPC分类号： C07D471/04
摘要： Imidazo pyridines of the formula
in which X is sulfur or sulfinyl; R, is halogen, acetyl, haloge nated acetyl, hydroxy methyl, formyl or
where R 4 is hydrogen or loweralkyl and R 5 is hydrogen, lower alkyl, lower hydroxy alkyl, carboxy-(lower alkyl), amino-(lower alkyl), (lower alkyl) amino-(lower alkyl), di(lower alkyl)amino-(lower alkyl) or sulfo-(lower alkyl), or
represents a morpholino or N-methyl piperazino ring; R 2 is hydrogen or lower alkyl; and R 3 is lower alkoxy; provided that when R 1 is chlorine, X is sulfinyl, are novel active anthelmintic agents. Compositions and methods for the use of such compounds against helmintic infections, and methods for preparing such compounds, are also disclosed.

7. 发明公开

EP0010440A1 Pyromellitic diimides, processes for their preparation, these compounds in orally administrable form for use in increasing the feed efficiency of a ruminant animal and compositions for this purpose containing them 失效
标题翻译： Pyromellitsäurediimide新，它们的制备方法，在口服给药的形式为在反刍动物的饲料利用率的提高使用的化合物和含有它们的合适的制剂。
公开(公告)号：EP0010440A1
公开(公告)日：1980-04-30
申请号：EP79302278.1
申请日：1979-10-19
申请人： Merck & Co., Inc.
发明人： Bochis, Richard J. , Fisher, Michael H. , Linn, Bruce O.
IPC分类号： C07D487/04 , A23K1/16 , A23K1/18
CPC分类号： C07D209/48 , A23K20/137 , C07D307/89 , C07D487/04 , C07D491/04
摘要： Asymmetrically substituted pyromellitic diimides of formula:
in which R, and R 2 are not the same and each represents hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, lower alkanoyl, benzoyl, di(lower alkyl)amino, lower alkanoylamino, benzoylamino, lower alkoxycarbonylamino or certain substituted phenyl or substituted lower alkyl radicals and each ofX and Y is hydrogen, halogen or lower alkyl, are novel compounds that are obtainable by treating pyromellitic dianhydride with two appropriately substituted amines or with ammonia and one amine.
The compounds can be administered to ruminant animals to increase their feed efficiency and suitable compositions for this purpose include the compounds with an inert carrier.
摘要翻译：式的不对称substituiertem均苯四羧酸二酰亚胺：其中R 1和R 2不是相同的，并且每个darstellt氢，烷基，烯基，炔基，环烷基，低级烷酰基，苯甲酰基，二（低级烷基）氨基，低级烷酰基氨基，苯甲酰基氨基低，烷氧基羰基或某些substituiertem苯基或低级烷基substituiertem自由基并且每个X和Y是氢，卤素或低级烷基，是新的化合物是可获得的那样通过处理均苯四甲酸酐具有两个适当地substituiertem cardamines或者与氨和胺之一。所述化合物可施用于反刍动物，以增加饲料效率和它们的组成适合于该目的包括与惰性载体的化合物。

8. 发明公开

EP0480623A1 New halomacrolides and derivatives having immunosuppressive activity 失效
标题翻译： Halomakrolide和Deriv mit mit免疫抑制剂Wirkung。
公开(公告)号：EP0480623A1
公开(公告)日：1992-04-15
申请号：EP91309025.4
申请日：1991-10-02
申请人： MERCK & CO. INC.
发明人： Bochis, Richard J. , Wyvratt Jr., Matthew J.
IPC分类号： C07H19/01 , A61K31/70
CPC分类号： C07H19/01
摘要： Novel C-3˝ and C-4˝ halogen-substituted immunosuppressant macrolides of FK-506 type structural Formula I:

are described.
摘要翻译：描述了FK-506型结构式I的新型C-3秒和C-4秒卤素取代的免疫抑制剂大环内酯：。 C

9. 发明公开

EP0445975A1 New hydroxymacrolide derivatives having immunosuppressive activity 失效
标题翻译：羟基马来酰胺 - 诱导mit免疫抑制剂Wirkung。
公开(公告)号：EP0445975A1
公开(公告)日：1991-09-11
申请号：EP91301686.1
申请日：1991-02-28
申请人： MERCK & CO. INC.
发明人： Bochis, Richard J. , Ok, Hyun O. , Wyvratt, Matthew J.
IPC分类号： C07H19/01 , C07D498/18 , A61K31/70
CPC分类号： C07H19/01
摘要： Novel hydroxymacrolide derivatives of the general structual Formula I:

have been prepared from (a) suitable precursor(s) by selective reduction of the ketone at C-2. These macrolide immunosuppressants are useful in a human host for the treatment of autoimmune diseases (such as juvenile-onset diabetes melitus, multiple sclerosis and rheumatoid arthritis), infectous diseases and/or the prevention of rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses such as: psoriasis, atopical dermatitiis, contact dermatitis and further eczematous dermatitises, seborrhoeic dermatitis, Lichen planus, Pemphigus, bullous Pemphigoid, Epidermolysis bullosa, urticaria, angioedemas, vasculitides, erythemas, cutaneous eosinophilias, Lupus erythematosus or Alopecia areata.
摘要翻译：已经通过在C-2上选择性还原酮从（a）合适的前体制备了一般结构式I的新羟基麦角酰胺衍生物：。这些大环内酯类免疫抑制剂可用于人宿主中用于治疗自身免疫性疾病（如幼年型糖尿病，多发性硬化和类风湿性关节炎），感染性疾病和/或预防外来器官移植排斥反应。骨髓和心脏移植。此外，这些大环内酯类免疫抑制剂可用于局部治疗炎性和过度增生性皮肤病以及免疫介导疾病的皮肤表现，如牛皮癣，特应性皮肤病，接触性皮炎和进一步湿疹性皮肤病，脂溢性皮炎，扁平苔藓，天疱疮，大疱类天疱疮，大疱表皮松解症，荨麻疹，血管瘤，血管炎，红斑，皮肤嗜酸粒细胞，红斑狼疮或斑秃。

10. 发明公开

EP0138708A3 Isoefrotomycin 失效
标题翻译： ISOEFROTOMYCIN
公开(公告)号：EP0138708A3
公开(公告)日：1985-05-29
申请号：EP84402045
申请日：1984-10-11
申请人： MERCK & CO. INC.
发明人： Bochis, Richard J. , Dewey, Ray S.
IPC分类号： C07H15/04 , A61K31/70 , A23K01/17
CPC分类号： C07H15/04
摘要： © There is disclosed the novel compound isoefrotomycin which is synthesized from efrotomycin as a Michael adduct by treatment with a mixture of polar and nonpolar solvents. Isoefrotomycin is an effective antimicrobial agent and growth promotant in animals.

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