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1. 发明公开

EP0056319A3 Substituted pyrimidin-2-ones and the salts thereof 有权
标题翻译：取代的吡咯烷二酮及其盐
公开(公告)号：EP0056319A3
公开(公告)日：1982-10-27
申请号：EP82300106
申请日：1982-01-08
申请人： NYEGAARD & CO. A/S
发明人： Benneche, Tore , Undheim, Kjell
IPC分类号： C07D239/36 , C07D403/12 , C07D409/12 , A61K31/505 , C07D239/38
CPC分类号： C07D239/36 , C07D239/38
摘要： Compounds of the general formula:
(wherein
X represents a halogen atom or a trifluoromethyl group; R 1 and R 2 independently represent a hydrogen atom or a lower alkyl group; Z is -0-, -S-, -SO-, -SO 2 - or the group -NR 4 -wherein R 4 is as defined for R hereinafter or represents the group COR 5 in which R 5 represents a hydrogen atom or an optionally substituted aryl, heterocyclic, aralkyl, lower alkyl or lower alkoxy group; R represents a C 6-10 carbocyclic aromatic group or a heterocyclic group containing a 5-9 membered unsaturated or aromatic heterocyclic ring which ring contains one or more heteroatoms selected from 0, N and S and optionally carries a fused ring which carbocyclic or heterocyclic group may carry one or more C 1-4 alkyl or phenyl groups, said groups being optionally substituted; or, where Z represents the group >R 4 , the group -ZR may represent a heterocyclic ring optionally carrying a fused ring and/or optionally substituted as defined for R; and R 3 represents a hydrogen atom or a lower alkyl, lower alkenyl, lower alkynyl, lower alkanoyl, lower alkenoyl, C 7-16 aralkyl or C 6-10 aryl group or a 5-9 membered unsaturated or aromatic heterocyclic ring); and, where acid or basic groups are present, the salts thereof; are useful in combating abnormal cell proliferation. The compounds of the invention are prepared by inter alia alkylation, ring closure and oxidation.

2. 发明授权

EP0074820B1 Substituted pyrimid-2-ones, the salts thereof, processes for their preparation and pharmaceutical compositions containing them 失效
标题翻译：取代PYRIMID-2-ONES及其制备方法及其制备方法及含有它们的药物组合物
公开(公告)号：EP0074820B1
公开(公告)日：1986-08-27
申请号：EP82304780.8
申请日：1982-09-10
申请人： NYEGAARD & CO. A/S
发明人： Benneche, Tore , Gacek, Mikkel Josef , Undheim, Kjell
IPC分类号： C07D239/36 , A61K31/505
CPC分类号： C07D239/36 , A61K31/70 , C07D401/12 , C07D409/12 , A61K31/505 , A61K2300/00

3. 发明授权

EP0032131B1 5-Halo-pyrimidin-2-ones, the salts thereof, processes for their preparation and pharmaceutical compositions containing them 有权转让
标题翻译： 5-HALO-PYRIMIDIN-2-ONES，其销售，其制备方法和含有它们的药物组合物
公开(公告)号：EP0032131B1
公开(公告)日：1983-09-21
申请号：EP81300031.2
申请日：1981-01-06
申请人： NYEGAARD & CO. A/S
发明人： Gacek, Mikkel Josef , Undheim, Kjell
IPC分类号： C07D409/06 , C07D401/06 , C07D403/06 , C07D405/06 , C07D413/06 , C07D417/06 , A61K31/505
CPC分类号： C07D239/30 , C07D243/08 , C07D277/42 , C07D277/56 , C07D333/16 , C07D333/28

4. 发明公开

EP0032131A1 5-Halo-pyrimidin-2-ones, the salts thereof, processes for their preparation and pharmaceutical compositions containing them 有权转让
标题翻译： 5-卤代 - 嘧啶-2-酮，它们的盐，它们的制备方法和含有它们的药物组合物。
公开(公告)号：EP0032131A1
公开(公告)日：1981-07-15
申请号：EP81300031.2
申请日：1981-01-06
申请人： NYEGAARD & CO. A/S
发明人： Gacek, Mikkel Josef , Undheim, Kjell
IPC分类号： C07D409/06 , C07D401/06 , C07D403/06 , C07D405/06 , C07D413/06 , C07D417/06 , A61K31/505
CPC分类号： C07D239/30 , C07D243/08 , C07D277/42 , C07D277/56 , C07D333/16 , C07D333/28
摘要： Compounds of the formula :-
(wherein

X represents a halogen atom;
R' and R 2 , which may be the same or different, each represents a hydrogen atom, or a C 1-4 alkyl group;
Het represents a C-attached 3-9 membered, saturated, unsaturated or aromatic heterocyclic ring containing one or more hetero atoms selected from 0,N and S and optionally carrying a fused ring and/or optionally substituted by one or more substituents; and
alk represents a C 1-4 saturated or unsaturated, straight or branched chain, divalent aliphatic hydrocarbyl group optionally substituted and, where an acidic or basic group is present, the salts thereof have been found to possess metaphase arresting ability which by virtue of its reversibility is of use in combating abnormal cell proliferation. Thus a knowledge of the cell division cycles of the normal and abnormal cells enables a cytotoxic drug to be administered whilst the abnormal cells are in a phase susceptible to attack and whilst the normal cells are in a non-susceptible phase.

The compounds of the invention are prepared by alkylation, ring closure of the pyrimidine ring, halogenation, ring closure of the heterocyclic ring Het or dehydrazination.

5. 发明授权

EP0056319B1 Substituted pyrimidin-2-ones and the salts thereof 有权
标题翻译：取代的吡哩啶-2-酮及其盐
公开(公告)号：EP0056319B1
公开(公告)日：1986-04-16
申请号：EP82300106.0
申请日：1982-01-08
申请人： NYEGAARD & CO. A/S
发明人： Benneche, Tore , Undheim, Kjell
IPC分类号： C07D239/36 , C07D403/12 , C07D409/12 , A61K31/505
CPC分类号： C07D239/36 , C07D239/38

6. 发明公开

EP0056319A2 Substituted pyrimidin-2-ones and the salts thereof 有权
标题翻译：取代的嘧啶-2-酮及其盐。
公开(公告)号：EP0056319A2
公开(公告)日：1982-07-21
申请号：EP82300106.0
申请日：1982-01-08
申请人： NYEGAARD & CO. A/S
发明人： Benneche, Tore , Undheim, Kjell
IPC分类号： C07D239/36 , C07D403/12 , C07D409/12 , A61K31/505
CPC分类号： C07D239/36 , C07D239/38
摘要： Compounds of the general formula:
(wherein

X represents a halogen atom or a trifluoromethyl group;
R 1 and R 2 independently represent a hydrogen atom or a lower alkyl group;
Z is -0-, -S-, -SO-, -SO 2 - or the group -NR 4 -wherein R 4 is as defined for R hereinafter or represents the group COR 5 in which R 5 represents a hydrogen atom or an optionally substituted aryl, heterocyclic, aralkyl, lower alkyl or lower alkoxy group;
R represents a C 6-10 carbocyclic aromatic group or a heterocyclic group containing a 5-9 membered unsaturated or aromatic heterocyclic ring which ring contains one or more heteroatoms selected from 0, N and S and optionally carries a fused ring which carbocyclic or heterocyclic group may carry one or more C 1-4 alkyl or phenyl groups, said groups being optionally substituted; or, where Z represents the group >R 4 , the group -ZR may represent a heterocyclic ring optionally carrying a fused ring and/or optionally substituted as defined for R; and
R 3 represents a hydrogen atom or a lower alkyl, lower alkenyl, lower alkynyl, lower alkanoyl, lower alkenoyl, C 7-16 aralkyl or C 6-10 aryl group or a 5-9 membered unsaturated or aromatic heterocyclic ring); and, where acid or basic groups are present, the salts thereof; are useful in combating abnormal cell proliferation.

The compounds of the invention are prepared by inter alia alkylation, ring closure and oxidation.

7. 发明公开

EP0033195A1 Pyrimidine-2-sulphides and their S-oxides for use in medicine, pharmaceutical compositions containing them, processes for their preparation and such compounds when novel per se 有权转让
标题翻译：嘧啶-2-硫化物和它们的S-氧化物用于医药用途，含有它们的药物组合物，它们的制备方法和所述化合物本身，只要它们是新的。
公开(公告)号：EP0033195A1
公开(公告)日：1981-08-05
申请号：EP81300098.1
申请日：1981-01-09
申请人： NYEGAARD & CO. A/S
发明人： Benneche, Tore , Gacek, Mikkel Josef , Undheim, Kjell
IPC分类号： C07D239/38 , C07D403/12 , C07D405/12 , C07D409/12 , C07F9/65 , C07H17/02 , A61K31/505
CPC分类号： C07D239/40 , C07C233/07 , C07D239/38 , C07F9/65122 , C07H17/02 , Y10S514/863 , Y10S514/885 , Y10S514/908
摘要： Compounds of the formula
(wherein X represents a halogen atom; nis 0,1 or 2; R 1 and R 2 , which may be the same or different, each represents a hydrogen atom or a carboxyl, esterified carboxyl, amido or mono-or di-C1-4 alkylamido group or a C1-4 alkyl group which may if desired carry a carboxyl or esterified carboxyl group; and R 3 represents a Ci-32 saturated or unsaturated, straight or branched, cyclic or acyclic aliphatic group or an araliphatic or heterocyclic substituted aliphatic group, a heterocyclic group or an aryl group which groups may if desired carry one or more substituents selected from halogen atoms and oxo, nitro, hydroxy, etherified hydroxy, esterified hydroxy, primary, secondary or tertiary amino, acylamino etherified mercapto or S = 0 or -SO 2 derivatives thereof and esterified phosphoric acid groups) and, where an acidic or basic group is present, physiologically compatible salts thereof have been found to be of use in combating abnormal cell proliferation. The compounds are prepared inter alia by oxidation of the corresponding sulfide, displacement of a leaving atom or group from the 2-position of the pyrimidine by reaction with a sulfinic acid or by ring closure of the pyrimidine ring.

8. 发明授权

EP0033195B1 Pyrimidine-2-sulphides and their S-oxides for use in medicine, pharmaceutical compositions containing them, processes for their preparation and such compounds when novel per se 有权转让
标题翻译：吡咯烷-2-磺酸及其在医药中使用的S-氧化物，含有它们的药物组合物，其制备方法和这些化合物
公开(公告)号：EP0033195B1
公开(公告)日：1985-12-04
申请号：EP81300098.1
申请日：1981-01-09
申请人： NYEGAARD & CO. A/S
发明人： Benneche, Tore , Gacek, Mikkel Josef , Undheim, Kjell
IPC分类号： C07D239/38 , C07D403/12 , C07D405/12 , C07D409/12 , C07F9/65 , C07H17/02 , A61K31/505
CPC分类号： C07D239/40 , C07C233/07 , C07D239/38 , C07F9/65122 , C07H17/02 , Y10S514/863 , Y10S514/885 , Y10S514/908

9. 发明公开

EP0074820A1 Substituted pyrimid-2-ones, the salts thereof, processes for their preparation and pharmaceutical compositions containing them 失效
标题翻译：取代的嘧啶-2-酮，它们的盐，它们的制备方法和含有它们的药物组合物。
公开(公告)号：EP0074820A1
公开(公告)日：1983-03-23
申请号：EP82304780.8
申请日：1982-09-10
申请人： NYEGAARD & CO. A/S
发明人： Benneche, Tore , Gacek, Mikkel Josef , Undheim, Kjell
IPC分类号： C07D239/36 , A61K31/505
CPC分类号： C07D239/36 , A61K31/70 , C07D401/12 , C07D409/12 , A61K31/505 , A61K2300/00
摘要： Compounds of general formula:
(wherein X represents a halogen atom or a trifluoromethyl group; R 1 and R 2 , which may be the same or different, each represents a hydrogen atom, or a C 1-4 alkyl group, and R 3 represents a hydrogen atom or a C 1-5 saturated or unsaturated, straight or branched acyclic aliphatic group; a C34 saturated or unsaturated cyclic aliphatic group; a heterocyclic substituted aliphatic group; an araliphatic group; or a heterocyclic or carbocyclic aryl group; any of said groups optionally carrying one or more substituents selected from halogen, oxo, hydroxy, mercapto, C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyloxy and amino) and, where an acidic or basic group is present, physiologically compatible salts thereof have been found to be of use in combating abnormal cell proliferation.
The compounds of formula I may be prepared by reaction of a 5-halo- or 5-trifluoromethyl-pyrimidin-2-one with an appropriate isocyanate.

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