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31. 发明公开

EP0228045A3 Aromatic thioethers 失效
标题翻译：芳香硫酯
公开(公告)号：EP0228045A3
公开(公告)日：1988-09-07
申请号：EP86117740
申请日：1986-12-19
申请人： CIBA-GEIGY AG
发明人： VON SPRECHER, ANDREAS, DR. , BREITENSTEIN, WERNER, DR. , BECK, ANDREAS, DR. , LANG, ROBERT W., DR. , OERTLE, KONRAD, DR.
IPC分类号： C07D215/54 , C07D311/24 , C07C149/41 , A61K31/215 , A61K31/35 , A61K31/47 , C07D311/18
CPC分类号： C07D311/24 , C07D215/54

32. 发明公开

EP0262618A2 N-(omega)-cyanoalkyl)aminophenols, and their preparation 失效
标题翻译： N-¬（ω） - 氰基烷基氨基苯酚和Herstellung
公开(公告)号：EP0262618A2
公开(公告)日：1988-04-06
申请号：EP87114058.8
申请日：1987-09-25
申请人： STERLING DRUG INC.
发明人： Schlegel, Donald Charles , Johnson, Robert Ed
IPC分类号： C07C121/43 , C07C149/41 , A61K31/275
CPC分类号： C07C255/00
摘要： useful as lipoxygenase inhibitors and anti-asthmatic agents, are prepared by acylation of an aminophenol with an ω-haloalkanoyl chloride followed by reduction of the resulting amide then displacement of the halide by cyanide.
摘要翻译：用作脂氧合酶抑制剂和抗哮喘剂的通过用ω-卤代烷酰氯酰化氨基苯酚然后还原所得酰胺然后用氰化物置换卤化物来制备。

33. 发明授权

EP0100172B1 Amide derivatives 失效
标题翻译：酰胺衍生物
公开(公告)号：EP0100172B1
公开(公告)日：1987-08-12
申请号：EP83303998.5
申请日：1983-07-08
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC
发明人： Tucker, Howard
IPC分类号： C07C149/23 , C07C149/41 , C07C103/375 , C07C103/50 , C07C121/78 , C07C147/107 , C07C147/14 , C07D213/70 , C07D247/02 , C07D283/02 , C07D285/12
CPC分类号： C07D285/125 , C07C59/68 , C07C255/00 , C07C321/00 , C07C323/00 , C07D213/70 , C07D233/84 , C07D239/38 , C07D277/36 , C07D303/48 , C07D333/62

34. 发明授权

EP0115997B1 Nouveaux dérivés de omega-mercaptopropanamide et de ses homologues, leur procédé de préparation, leur application comme médicaments, les compositions les renfermant et les nouveaux intermédiaires obtenus 失效
公开(公告)号：EP0115997B1
公开(公告)日：1987-07-22
申请号：EP84400216.2
申请日：1984-02-01
申请人： ROUSSEL-UCLAF
发明人： Vevert, Jean-Paul F. , Delevallée, Françoise F. , Deraedt, Roger F.
IPC分类号： C07C149/23 , C07C149/41 , C07C153/09 , C07D213/75 , C07D235/30 , C07D277/00 , A61K31/16 , A61K31/265 , A61K31/41 , A61K31/44
CPC分类号： C07D213/75 , C07D235/30 , C07D277/18 , C07D277/46 , C07D277/82
摘要： For the Contracting States : BE CH DE FR GB IT LI LU NL SE 1. Compounds with the formula (I) : see diagramm : EP0115997,P26,F1 in which R1 represents a hydrogen atom or a see diagramm : EP0115997,P26,F2 radical, R'1 being an alkyl radical containing from 1 to 5 carbon atoms or an aryl radical possibly substituted by a hydroxy radical, an alkyl radical containing from 1 to 5 carbon atoms, an alkoxy radical containing from 1 to 5 carbon atoms, a nitro radical or a halogen atom, n represents a whole number able to vary from 1 to 5, R2 represents a hydrogen atom, an alkyl radical containing from 1 to 5 carbon atoms, an aryl or arylalkyl radical containing from 6 to 15 carbon atoms, possibly substituted by an alkyl radical containing from 1 to 5 carbon atoms, an alkoxy radical containing from 1 to 5 carbon atoms, a hydroxyl radical, a halogen atom or a trifluoromethyl radical, R3 represents a heterocyclic radical chosen from the following radicals :- thiazolyl, 4,5-dihydrothiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl, tetrazolyl, benzimidazolyl, benzothiazolyl or benzoxazolyl, possibly substituted by an alkyl radical containing from 1 to 5 carbon atoms or R3 represents a hydrogen atom, a phenyl radical possibly substituted by one or more radicals chosen from the group constituted by alkyl radicals containing from 1 to 5 carbon atoms, alkoxy radicals containing from 1 to 5 carbon atoms, a hydroxyl radical, a nitro radical, halogen atoms, a trifluoromethyl radical, a carboxymethyl radical, alkoxy carbonylmethyl radicals in which the alkoxy radical contains from 1 to 5 carbon atoms, aralkyloxy radicals containing from 7 to 15 carbon atoms and the radicals : see diagramm : EP0115997,P27,F3 in which X and X', identical or different, represent a hydrogen atom or an alkyl radical containing from 1 to 5 carbon atoms, R3 however not being able to represent a phenyl radical, not substituted or substituted by one or more radicals chosen from the group constituted by alkyl radicals containing from 1 to 5 carbon atoms, alkoxy radicals containing from 1 to 5 carbon atoms, and halogen atoms, when R2 represents a hydrogen atom and when n is equal to 1 or 2, and R3 not being able to represent a phenyl radical substituted by a carboxymethyl radical when R2 represents a methyl radical and when n is equal to 1, as well as their addition salts with acids and bases. For the Contracting State : AT 1. Process for preparing compounds with the formula (I) : see diagramm : EP0115997,P28,F1 in which R1 represents a hydrogen atom or a see diagramm : EP0115997,P28,F2 radical, R'1 being an alkyl radical containing from 1 to 5 carbon atoms or an aryl radical possibly substituted by a hydroxy radical, an alkyl radical containing from 1 to 5 carbon atoms, an alkoxy radical containing from 1 to 5 carbon atoms, a nitro radical or a halogen atom, n represents a whole number able to vary from 1 to 5, R2 represents a hydrogen atom, an alkyl radical containing from 1 to 5 carbon atoms, an aryl or arylalkyl radical containing from 6 to 15 carbon atoms, possibly substituted by an alkyl radical containing from 1 to 5 carbon atoms, an alkoxy radical containing from 1 to 5 carbon atoms, a hydroxyl radical, a halogen atom or a trifluoromethyl radical, R3 represents a heterocyclic radical chosen from the following radicals :- thiazolyl, 4,5-dihydrothiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl, tetrazolyl, benzimidazolyl, benzothiazolyl or benzoxazolyl, possibly substituted by an alkyl radical containing from 1 to 5 carbon atoms or R3 represents a hydrogen atom, a phenyl radical possibly substituted by one or more radicals chosen from the group constituted by alkyl radicals containing from 1 to 5 carbon atoms, alkoxy radicals containing from 1 to 5 carbon atoms, a hydroxyl radical, a nitro radical, halogen atoms, a trifluoromethyl radical, a carboxymethyl radical, alkoxy carbonylmethyl radicals in which the alkoxy radical contains from 1 to 5 carbon atoms, aralkyloxy radicals containing from 7 to 15 carbon atoms and the radicals : see diagramm : EP0115997,P29,F3 in which X and X', identical or different, represent a hydrogen atom or an alkyl radical containing from 1 to 5 carbon atoms, R3 however not being able to represent a phenyl radical, not substituted or substituted by one or more radicals chosen from the group constituted by alkyl radicals containing from 1 to 5 carbon atoms, alkoxy radicals containing from 1 to 5 carbon atoms, and halogen atoms, when R2 represents a hydrogen atom and when n is equal to 1 or 2, and R3 not being able to represent a phenyl radical substituted by a carboxymethyl radical when R2 represents a methyl radical and when n is equal to 1, as well as their addition salts with acids and bases, characterized in that : - to prepare compounds with the formula (I) in which R1 , R2 and R3 have the previously given significance and in which n=1, as well as their addition salts with acids and bases, and acid with the formula (II) : see diagramm : EP0115997,P29,F4 in which R'1 and R2 have the significances already indicated, or a functional derivative of this acid, is submitted to the action of a product with the formula (III) : H2 N-R3 in which R3 has the significance already indicated, so as to obtain a product with the formula (I) in which : see diagramm : EP0115997,P29,F5 R'1 as well as R2 and R3 have the significances already indicated and in which n=1, which product with the formula (I), if necessary or desired, is saponified, so as to obtain a product with the formula (I) in which R1 represents a hydrogen atom, which products with the formula (I) are submitted, if desired, to the action of a base or an acid so as to form the corresponding salts ; - to prepare compounds with the formula (I) in which R1 , R2 and R3 have the previously given significance and in which n is a whole number varying from 1 to 5, as well as their addition salts with acids and bases, an acid with the formula (IV) : see diagramm : EP0115997,P29,F6 in which X1 is a halogen atom and in which n and R2 have the significances given above, or a functional derivative of this acid, is submitted to the action of a product with the previous formula (III) (NH2 -R3 ), so as to obtain a product with the formula (V) : see diagramm : EP0115997,P29,F7 in which X1 , n, R2 and R3 have the previosu significances, which is submitted to the action of the anion of a thioacid with the formula (VI) : see diagramm : EP0115997,P30,F8 in which R'1 keeps its significance, so as to obtain a product with the formula (I) in which r1 = R'1 see diagramm : EP0115997,P30,F9 n represents a whole number able to vary from 1 to 5 and in which R'1 , R2 and R3 have the significances given above, which product with the formula (I), if necessary or desired, is saponified, so as to obtain a product with the formula (I) in which R1 represents a hydrogen atom, which products with the formula (I) are submitted, if desired, to the action of an acid or of a base so as to form the corresponding salts.

35. 发明公开

EP0147778A3 Anti-inflammatory derivatives of 1,4-naphthoquinone 失效
标题翻译： 1,4-萘醌的防炎剂衍生物
公开(公告)号：EP0147778A3
公开(公告)日：1986-06-25
申请号：EP84115774
申请日：1984-12-19
申请人： Troponwerke GmbH & Co. KG
发明人： Opitz, Wolfgang, Dr. , Pelster, Bernhard, Dr. , Fruchtmann Romania , Krupka, Udo, Dr. , Gauss, Walter, Dr. , Kiehne, Hartmut, Dr. , Oediger, Hermann, Dr.
IPC分类号： A61K31/12 , A61K31/16 , A61K31/18 , A61K31/19 , C07C50/32 , C07C143/80 , C07C103/42 , C07C149/40 , C07C149/41
CPC分类号： C07C50/24 , A61K31/12 , A61K31/135 , A61K31/16 , C07C50/32 , C07C50/38
摘要： Die 1,4-Naphthochinonderivate entsprechen der allge meinen Formel worin
R¹ für ein Halogenatom oder eine freie oder substituierte Hydroxyl-, Sulfhydryl- oder Amino-Gruppe stehen kann,
R² die gleiche Bedeutung wie R¹ hat und gleich oder von diesem verschieden sein kann oder für einen Alkylrest oder ein Wasserstoffatom stehen kann und
R³ und R⁴ gleich oder verschieden sind und Wasserstoff, Alkyl, Hydroxyl, Alkoxy, Sulfonamid oder Halogen bedeuten können, wobei für den Fall, daß R¹ Hydroxyl bedeutet, die Reste R², R³ und R⁴ Wasserstoff bedeuten, und können als Wirkstoffe in Arzneimitteln verwendet werden.

36. 发明授权

EP0054936B1 Aroyl amino acids 失效
标题翻译： AROYL氨基酸
公开(公告)号：EP0054936B1
公开(公告)日：1986-06-04
申请号：EP81110594.9
申请日：1981-12-18
申请人： USV PHARMACEUTICAL CORPORATION
发明人： Suh, John Taiyoung , Menard, Paul Russell , Jones, Howard
IPC分类号： C07C153/09 , C07C149/41 , C07C103/84
CPC分类号： C07C327/00 , C07C323/00

37. 发明公开

EP0173120A1 Alterungsschutzmittel und diese enthaltende Polymere 失效
标题翻译：抗老化剂和含有这些聚合物。
公开(公告)号：EP0173120A1
公开(公告)日：1986-03-05
申请号：EP85109815.2
申请日：1985-08-05
申请人： BAYER AG
发明人： Buysch, Hans-Josef, Dr. , Witte, Josef, Dr. , Szentivanyi, Zsolt, Dr.
IPC分类号： C07C149/23 , C07C149/41 , C07C149/437 , C08K5/37
CPC分类号： C08K5/3725 , C07C323/44
摘要： Verbindungen der allgemeinen Formel
worin

R 3 H, CH,
R 4 H, C 1-12 Alkyl, C 1-4 Alkoxy. C 1-12 Alkylamino, C 7-18 Aral- kylamino, Arylamino, C 7 - 2o Aralkyl
A einen zweibindigen Rest der Struktur
X eine einfache Bindung oder -CO-, wenn es an ein C-Atom und nur CO, wenn es an ein Heteroatom gebunden ist,
R' und R 2 H oder C 1-4 Alkyl,
m 1 oder 2 und
n eine ganze Zahl von 1-12 bedeuten, eignen sich als einbaubare Alterungsschutzmittel für Polymere, insbesondere Nitrilkautschuk.
摘要翻译：下式的化合物其中R是H，CH 3 R 4是H，C 1-12烷基，C 1-4烷氧基，C1-12Alkylamino，C7-18Aralkylamino，芳基氨基，C7-20Aralkyl A是二价基团结构的 X是单键或 -CO-时，它比与碳原子和仅CO，当结合于一个杂原子，R 1和R 2是H或C 1-4烷基，m是1或2，n是1-12的整数。合适的平均可掺入的抗老化剂的聚合物，尤其是丁腈橡胶。

38. 发明公开

EP0150118A3 Antagonists of slow reacting substances of anaphylaxis 失效
标题翻译：慢性反应物质的拮抗作用
公开(公告)号：EP0150118A3
公开(公告)日：1985-08-28
申请号：EP85300367
申请日：1985-01-18
申请人： MERCK FROSST CANADA INC.
发明人： Rokach, Joshua , Young, Robert N.
IPC分类号： C07C149/41 , C07C147/14 , C07C147/107 , A61K31/195 , C07D207/16
CPC分类号： A61K31/18
摘要： Compounds having the formula:
and their pharmaceutically acceptable salts and acid- addition salts, are antagonists of leukotrienes of C 4 , D 4 and E 4 , the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-Inflammatory agents and cytoprotective agents. In the formula, each R, independently of the others, is hydrogen, hydroxy, C 1-6 alkyl, C 2-6 alkenyl, trifluoromethyl, C 1-6 alkoxy, mercapto, C 1-6 thioalkyl, phenyl, phenyl substituted by C 1-3 alkyl or by halogen, benzyl, phenethyl, halogen, amino, N(R 3 ) 2 , COOR 3 , CH 2 0R 3 , formyl, cyano, trifluoromethylthio or nitro;
each R', independently of the others, R 3 or R 4 , or R' and R' together are an oxo or methylene group; each R 1 , independently of the others, is hydrogen or C 1-4 alkyl; R 2 is C 1-6 alkyl or C 3-6 alkenyl; each R 3 , independently of any others, is hydrogen or C 1-6 alkyl; R 4 is hydrogen, C 1-6 alkyl or C 1-6 alkoxy; R 6 is hydrogen, C 1-6 alkyl, R 3 CO- or R 3 0CH 2 -; each R 6 , independently of any others, is R 3 or is such that HNR 6 -(CR 6 R 6 )-COOR 3 is an amino acid or amino acid ester; each of X 1 and X 2 , independently of the other, is oxygen, sulfur, sulfoxide, sulfone;
Z is 0, S or NR 3 ; each n, independently of any others, is 0 or an integer from 1 to 6.

39. 发明公开

EP0150118A2 Antagonists of slow reacting substances of anaphylaxis 失效
标题翻译：反刍动物on am den den den den ie ie ie（（（。。。。。。。。。。。
公开(公告)号：EP0150118A2
公开(公告)日：1985-07-31
申请号：EP85300367.1
申请日：1985-01-18
申请人： MERCK FROSST CANADA INC.
发明人： Rokach, Joshua , Young, Robert N.
IPC分类号： C07C149/41 , C07C147/14 , C07C147/107 , A61K31/195 , C07D207/16
CPC分类号： A61K31/18
摘要： Compounds having the formula:
and their pharmaceutically acceptable salts and acid- addition salts, are antagonists of leukotrienes of C 4 , D 4 and E 4 , the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-Inflammatory agents and cytoprotective agents.
In the formula, each R, independently of the others, is hydrogen, hydroxy, C 1-6 alkyl, C 2-6 alkenyl, trifluoromethyl, C 1-6 alkoxy, mercapto, C 1-6 thioalkyl, phenyl, phenyl substituted by C 1-3 alkyl or by halogen, benzyl, phenethyl, halogen, amino, N(R 3 ) 2 , COOR 3 , CH 2 0R 3 , formyl, cyano, trifluoromethylthio or nitro;

each R', independently of the others, R 3 or R 4 , or R' and R' together are an oxo or methylene group;
each R 1 , independently of the others, is hydrogen or C 1-4 alkyl;
R 2 is C 1-6 alkyl or C 3-6 alkenyl;
each R 3 , independently of any others, is hydrogen or C 1-6 alkyl;
R 4 is hydrogen, C 1-6 alkyl or C 1-6 alkoxy;
R 6 is hydrogen, C 1-6 alkyl, R 3 CO- or R 3 0CH 2 -;
each R 6 , independently of any others, is R 3 or is such that HNR 6 -(CR 6 R 6 )-COOR 3 is an amino acid or amino acid ester;
each of X 1 and X 2 , independently of the other, is oxygen, sulfur, sulfoxide, sulfone;

Z is 0, S or NR 3 ;
each n, independently of any others, is 0 or an integer from 1 to 6.
摘要翻译：具有下式的化合物及其药学上可接受的盐和酸加成盐是C4，D4和E4的白三烯，慢性反应物质的过敏反应的拮抗剂。这些化合物可用作抗哮喘，抗过敏，抗炎剂和细胞保护剂。在该式中，各R独立地为氢，羟基，C 1-6烷基，C 2-6烯基，三氟甲基，C 1-6烷氧基，巯基，C 1-6硫烷基，苯基，被C 1-3烷基取代的苯基或卤素，苄基，苯乙基，卤素，氨基，N（R3）2，COOR3，CH2OR3，甲酰基，氰基，三氟甲硫基或硝基; 每个R min独立地为R3或R4，或Rmin和Rmin一起为氧代或亚甲基; 每个R 1独立地为氢或C 1-4烷基; R2是C1-6烷基或C3-6烯基; 每个R 3，独立于任何其它的是氢或C 1-6烷基; R4是氢，C1-6烷基或C1-6烷氧基; R5是氢，C1-6烷基，R3CO-或R3OCH2-; 每个R 6独立地为R 3，或者使得HNR 6 - （CR 6 R 6）-COOR 3是氨基酸或氨基酸酯; X1和X2各自独立地为氧，硫，亚砜，砜; @ = NR3; N - @ - R4; N-CN; 或NCONHR3; Z是O，S或NR 3; 每个n独立于任何其它，为O或1至6的整数。

40. 发明授权

EP0040932B1 Amide derivatives, process for their manufacture and pharmaceutical or veterinary compositions containing them 失效
标题翻译：酰胺衍生物及其制备方法及含有它们的药物或兽药组合物
公开(公告)号：EP0040932B1
公开(公告)日：1985-07-03
申请号：EP81302147.4
申请日：1981-05-14
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC
发明人： Crossley, Neville Stanton , Glen, Alasdair Thomas , Hughes, Leslie Richard
IPC分类号： C07C103/76 , C07C121/78 , C07C121/52 , C07C147/107 , C07C147/12 , C07C147/14 , C07C149/41 , C07C149/42 , A61K31/165 , A61K31/275
CPC分类号： C07D263/44 , C07C59/56 , C07C205/56 , C07C255/00 , C07C323/00 , C07D303/48 , Y10S514/859 , Y10S514/864

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