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1. 发明公开

EP0505095A3 New substituted azetidinones as anti-inflammatory and antidegenerative agents 失效
标题翻译：新的取代氮杂环丁酮作为抗炎剂和抗变性剂
公开(公告)号：EP0505095A3
公开(公告)日：1993-01-20
申请号：EP92302147.1
申请日：1992-03-12
申请人： MERCK & CO. INC.
发明人： Maccoss, Malcolm , Durette, Philippe L.
IPC分类号： C07F9/568 , A61K31/675 , C07F9/6558
CPC分类号： C07F9/65586 , C07F9/568 , C07F9/65583 , Y10S514/851
摘要： New substituted azetidinones of the general formula (A), which have been found to be potent elastase inhibitors and thereby useful as anti-inflammatory and antidegenerative agents, are described.
摘要翻译：描述了已被发现是有效的弹性蛋白酶抑制剂并因此可用作抗炎剂和抗退化剂的通式（A）的新的取代的氮杂环丁酮。

2. 发明公开

EP0505095A2 New substituted azetidinones as anti-inflammatory and antidegenerative agents 失效
标题翻译： Neueidylieret氮杂环丁酮抗炎剂和抗变性Mittel。
公开(公告)号：EP0505095A2
公开(公告)日：1992-09-23
申请号：EP92302147.1
申请日：1992-03-12
申请人： MERCK & CO. INC.
发明人： Maccoss, Malcolm , Durette, Philippe L.
IPC分类号： C07F9/568 , A61K31/675 , C07F9/6558
CPC分类号： C07F9/65586 , C07F9/568 , C07F9/65583 , Y10S514/851
摘要： New substituted azetidinones of the general formula (A), which have been found to be potent elastase inhibitors and thereby useful as anti-inflammatory and antidegenerative agents, are described.
摘要翻译：描述了已经被发现是有效的弹性蛋白酶抑制剂并因此可用作抗炎和抗再生剂的通式（A）的新的取代的氮杂环丁酮。

3. 发明公开

EP0224173A1 Steroidal glycolipids as host resistance stimulators 失效
标题翻译：类固醇糖脂人类免疫刺激素。
公开(公告)号：EP0224173A1
公开(公告)日：1987-06-03
申请号：EP86115943.2
申请日：1986-11-17
申请人： Merck & Co., Inc.
发明人： Hagmann, William K. , Durette, Philippe L. , Ponpipom, Mitree M.
IPC分类号： A61K31/705 , C07J31/00 , C07J41/00
CPC分类号： A61K31/704 , C07J31/006 , C07J41/0088
摘要： Described is a pharmaceutical composition for enhancing host resistance in an immunocompromised individual consisting essentially of a compound of the formula:

R' is α or β-D-I-thiomannopyranose, a or β-L-I-thiofucopyranose;
A is (CH 2 ) n where n is 5-7, or (CH 2 ) k X(CH 2 ) m where X is O, S, NH and k, m are independently 2-4 and k + m is 4-6;
R 2 is C 1 -C 8 alkyl or C 2 -C 10 alkene; 0

C B where B is C 1 -C 8 alkyl, C 1 -C 8 alkoxy, NR 3 R 4 where R 3 and R 4 are independently H, C 1 -C 4 alkyl; CH(CH 3 )D where D is OH, NH 2 , NHR 5 where R 5 is C 1 -C 10 alkyl or acetyl. or of a pharmaceutically acceptable salt thereof.
摘要翻译：描述了用于增强免疫受损个体的宿主抗性的药物组合物，其基本上由下式化合物组成：其中：R 1是α或β-D-硫代吗喃吡喃糖，α或β-L-硫代吡喃葡萄糖; A是（CH 2）n，其中n是5-7，或（CH 2）k X（CH 2）m，其中X是O，S，NH和k，m独立地是2-4，k + m是4-6; R 2是C 1 -C 8烷基或C 2 -C 10烯烃; 其中B是C 1 -C 8烷基，C 1 -C 8烷氧基，NR 3 R 4，其中R 3和R 4独立地是H，C 1 -C 4烷基; CH（CH 3）D，其中D是OH，NH 2，NHR 5，其中R 5是C 1 -C 10烷基或乙酰基。或其药学上可接受的盐。

4. 发明授权

EP0041896B1 Immunologically active dipeptidyl 2-amino-1,2-dideoxy-D-glucose derivatives and methods of preparation 有权
标题翻译：免疫活性的二磷酸2-氨基-1,2-二脱氧-D-葡萄糖衍生物及其制备方法
公开(公告)号：EP0041896B1
公开(公告)日：1983-12-28
申请号：EP81400901.5
申请日：1981-06-05
申请人： Merck & Co., Inc.
发明人： Durette, Philippe L.
IPC分类号： C07C103/52 , A61K31/02
CPC分类号： C07K9/005 , C07D309/14

5. 发明公开

EP0014159A1 Immunologically active dipeptidyl saccharides and methods of preparation 有权
标题翻译：免疫活性的二肽的糖类及其制备方法。
公开(公告)号：EP0014159A1
公开(公告)日：1980-08-06
申请号：EP80400130.3
申请日：1980-01-28
申请人： Merck & Co., Inc.
发明人： Durette, Philippe L. , Shen, Tsung-Ying
IPC分类号： C07H15/04 , C07H15/12 , C07H15/18 , C07H15/20 , A61K31/70
CPC分类号： C07K9/005
摘要： 2-Amino-2-deoxy-glycoses of the general structural formula:

wherein

R 1 is hydrogen, alkyl (1-7C), substituted alkyl (1-7C), phenyl, substituted phenyl, benzyl, or substituted benzyl;
R 2 is alkyl, substituted alkyl, phenyl, or substituted phenyl;
R 3 is H or lower alkyl (1-10C) with the proviso that when the aminoglycose has the 2-amino-2-deoxy-D-glucose configuration, R 3 cannot be H;
R 4 and R 5 are same or different and are H, aliphatic or aromatic acyl (2-21 C) or substituted acyl (2-21 C);
R 6 is H, or R 6 -R 7 together is -CH 2 -CH 2 -CH 2 -,
R 7 is H, alkyl (1-7C), hydroxymethyl, mercaptomethyl, benzyl, or substituted benzyl;
R 8 and Rg each is carboxyl, esterified carboxyl (1-7C), amidated carboxyl, or mono- or di-alkyl-(1-3C)-amidated carboxyl;
provided that when R 3 is lower alkyl, the stereochemistry at asymmetric center I can be either D or L, but that when the caminoglycose has the 2-amino-2-deoxy-D-glucose configuration, the stereochemistry at I cannot be D;
when R 7 is not H, the stereochemistry at asymmetric center II is either L or D; and
the stereochemistry at asymmetric center III is D.

These compounds possess immunostimulatory properties.

6. 发明公开

EP0393256A1 Aminoalkyl naphthalenediols as host resistance enhancers against viral infection 失效
标题翻译：氨基烷基萘二异氰酸酯Gastwiderstandsvergrösserergegen病毒。
公开(公告)号：EP0393256A1
公开(公告)日：1990-10-24
申请号：EP89201038.0
申请日：1989-04-21
申请人： Merck & Co., Inc.
发明人： Durette, Philippe L. , Gallagher, Timothy F.
IPC分类号： C07C215/50 , C07C217/58 , C07C217/52 , C07D309/14 , A61K31/13
CPC分类号： A61K31/135 , A61K31/35 , C07C215/50 , C07C217/52 , C07C217/58 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D309/14
摘要： Disclosed are specific aminoalkyl naphthalenediol derivatives that enhance natural human host resistance to viral infectious organisms and particularly AIDS-related viruses. Such agents are also administered prophylactically to individuals whose resistance to infection has been specifically immunocompromised by an AIDS-related (HIV) virus.
摘要翻译：公开了特定的氨基烷基萘二醇衍生物，其增强天然人宿主对病毒感染性生物，特别是与艾滋病有关的病毒的抗性。这些药物也预防性施用于其感染的抗性已被艾滋病相关（HIV）病毒特异性地免疫受损的个体。

7. 发明授权

EP0038750B1 Immunologically active dipeptidyl 4-0-, 6-0-acyl-2-amino-2-deoxy-D-glucose derivatives and methods for their preparation 有权
标题翻译：免疫活性的DIPEPTIDYL 4-0-，6-0-ACY-2-AMINO-2-DEOXY-D-葡萄糖衍生物及其制备方法
公开(公告)号：EP0038750B1
公开(公告)日：1986-11-12
申请号：EP81400608.6
申请日：1981-04-15
申请人： Merck & Co., Inc.
发明人： Shen, Tsung-Ying , Durette, Philippe L. , Dorn, Conrad P, Jr. , Doherty, James B. , Dean, Richard T.
IPC分类号： C07H15/04 , A61K31/70
CPC分类号： C07K9/005

8. 发明授权

EP0018901B1 Immunologically active peptidyl disaccharides, methods of preparation and vaccine 失效
标题翻译：免疫活性肽分泌物，制备方法和疫苗
公开(公告)号：EP0018901B1
公开(公告)日：1982-12-15
申请号：EP80400566.8
申请日：1980-04-25
申请人： Merck & Co., Inc.
发明人： Durette, Philippe L. , Shen, Tsung-Ying
IPC分类号： C07H15/00 , C07H13/00 , A61K31/70
CPC分类号： C07K9/005 , Y10S514/885

9. 发明公开

EP0038750A1 Immunologically active dipeptidyl 4-0-, 6-0-acyl-2-amino-2-deoxy-D-glucose derivatives and methods for their preparation 有权
标题翻译： 4-0，6-0酰基-2-胺-2-脱氧-D-葡萄糖的二肽衍生物具有用于它们的制备的免疫活性和过程。
公开(公告)号：EP0038750A1
公开(公告)日：1981-10-28
申请号：EP81400608.6
申请日：1981-04-15
申请人： Merck & Co., Inc.
发明人： Shen, Tsung-Ying , Durette, Philippe L. , Dorn, Conrad P, Jr. , Doherty, James B. , Dean, Richard T.
IPC分类号： C07H15/04 , A61K31/70
CPC分类号： C07K9/005
摘要： Immunologically active compounds of the formula:
wherein:

R 1 is C 1-7 alkyl; substituted C 1-7 alkyl; phenyl; or substituted phenyl;
R 2 is hydrogen; C 1-7 alkyl; substituted C 1-7 alkyl; phenyl; substituted phenyl; phenyl C 1-4 alkyl; or substituted phenyl C 1-4 alkyl;
R 3 and R 4 may be the same or different and are each independently hydrogen, provided that R 3 and R 4 may not both be hydrogen; or
where
X is -O-; -S-; or

R 10 is hydrogen; C 1-30 alkyl; C 2 - 30 alkenyl; C 1-30 alkoxy; phenyl; C 1-20 alkylsulfonyl; or cholesteryl;
R 11 , R 12 , R 13 , R 14 and R 15 may be the same or different and are each independently hydrogen; C 1-20 alkyl; C 1-20 alkylcarbonyloxy; amino; benzyl; C 1-20 alkoxymethyl; C 1-20 alkylamido; or
r is 0 or 1; s is 0 or 1; and t is 0 to 20; provided that s may only be 0 when both rand tare greater than 0 or when r is 0 and R 10 is amino; phenyl; substituted phenyl; 1-adamantyl; or heterocycle selected from the group consisting of 2- or 3-furyl, 2- or 3- thienyl, 2- or 3- pyrrolidinyl, 2-, 3- or 4- pyridyl, and 1-tetrazolyl, said heterocycle optionally substituted with C 1-20 alkylcarbonyl; and where R 3 or R 4 is other than hydrogen, the other of R 3 or R 4 may additionally be Ci-4 alkylcarbonyl;
R 5 is hydrogen or C 1-10 alkyl;
R 6 is hydrogen or R 6 and R 7 taken together are -(CH 2 ) 3 -;
R 7 is hydrogen; C 1-7 alkyl; hydroxymethyl; mercaptomethyl; benzyl; or substituted benzyl;
Rs and R 9 may be the same or different and are each independently COOR, or CONR'R", where R is hydrogen or Ci-7 alkyl, and R' and R" are hydrogen or C 1-3 alkyl;
when R 5 is C 1-10 alkyl, the stereochemistry at asymmetric . center I is D or L;
when R 7 is other than hydrogen, the stereochemistry at asymmetric centre II is L; and

the stereochemistry at asymmetric center III is D; and acid addition and quaternary salts thereof.

10. 发明授权

EP0595557B1 New substituted azetidinones as anti-inflammatory and antidegenerative agents 失效
标题翻译：取代氮杂环丁酮作为entzüngdungshemmende和抗变性剂
公开(公告)号：EP0595557B1
公开(公告)日：2004-06-30
申请号：EP93308421.2
申请日：1993-10-22
申请人： Merck & Co., Inc.
发明人： Doherty, James B. , Finke, Paul E. , Dorn, Conrad P. , Maccoss, Malcolm , Durette, Philippe L. , Mills, Sander G. , Shah, Shrenik K. , Lanza, Thomas J. , Sahoo, Soumya P. , Hagmann, William K. , Hale, Jeffrey J.
IPC分类号： C07D205/08 , C07D405/12 , C07D403/12 , C07D401/12 , A61K31/395
CPC分类号： C07D231/12 , C07D205/08 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12

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