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1. 发明授权

US06265578B1 Pyrimidine-2,4,6-triones 失效
标题翻译：嘧啶-2,4,6-三硝基吡啶
公开(公告)号：US06265578B1
公开(公告)日：2001-07-24
申请号：US09483858
申请日：2000-01-17
申请人： Louise Helen Foley , Robert Edward Palermo , Ping Wang
发明人： Louise Helen Foley , Robert Edward Palermo , Ping Wang
IPC分类号： C07D23962
CPC分类号： C07D239/62 , A61K31/513
摘要： A compound of formula I wherein R1 is hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, aryloxy or alkylalkoxy, and R2 is aryloxy, or a pharmaceutically acceptable salt of an acidic compound of formula I, or a prodrug thereof. The compounds of formula I and their aforementioned salts and prodrugs can be used in the treatment or control of cancer associated with overexpresison of gelatinase-A and/or gelatinase-B, particularly skin cancer, breast cancer, prostate cancer, colon cancer, lung cancer, and gastric cancer. The compounds of the invention are also useful for other diseases associated with unregulated degradation of extracellular matrix, including rheumatoid arthritis, osteoarthritis, multiple sclerosis, corneal ulceration, periodontal disease and the like.
摘要翻译：式I的化合物，其中R 1是氢，烷基，取代的烷基，烯基，取代的烯基，炔基，取代的炔基，烷氧基，取代的烷氧基，芳氧基或烷基烷氧基，R 2是芳氧基或式I的酸性化合物的药学上可接受的盐，其前药。式I化合物及其上述盐和前药可用于治疗或控制与明胶酶-A和/或明胶酶-B（特别是皮肤癌，乳腺癌，前列腺癌，结肠癌，肺癌）过度表达相关的癌症和胃癌。本发明的化合物还可用于与细胞外基质的不受限制降解有关的其它疾病，包括类风湿性关节炎，骨关节炎，多发性硬化，角膜溃疡，牙周病等。

2. 发明授权

US06706723B2 Pyrimidine-2,4,6-trione metalloproteinase inhibitors 失效
标题翻译：嘧啶-2,4,6-三酮金属蛋白酶抑制剂
公开(公告)号：US06706723B2
公开(公告)日：2004-03-16
申请号：US10032837
申请日：2001-10-25
申请人： Mark C. Noe , Lawrence A. Reiter , Martin J. Wythes
发明人： Mark C. Noe , Lawrence A. Reiter , Martin J. Wythes
IPC分类号： C07D23962
CPC分类号： C07D239/62 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, A, B and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
摘要翻译：本发明涉及X，Y，A，B和R 1的嘧啶-2,4,6-三酮金属蛋白酶抑制剂，如本说明书中所定义，以及治疗炎症，癌症和其他疾病。

3. 发明授权

US06242455B1 Pyrimidin-2,4,6-trion derivatives, method for producing the same and medicinal products containing these compounds 失效
标题翻译：嘧啶-2,4,6-三取代衍生物，其制备方法和含有这些化合物的药用产品
公开(公告)号：US06242455B1
公开(公告)日：2001-06-05
申请号：US09445460
申请日：2000-03-22
申请人： Frank Grams , Gerd Zimmermann
发明人： Frank Grams , Gerd Zimmermann
IPC分类号： C07D23962
CPC分类号： C07D239/60
摘要： Compounds of formula I wherein R1, R2, R3 and R4 have the meanings indicated in the specification. The compounds are useful as inhibitors of metalloproteases of the M2, M3 family and the astacin subfamily of M12 and M13.
摘要翻译： R1，R2，R3和R4中的式Ⅰ化合物具有说明书中所述的含义。该化合物可用作M12和M13的M2，M3家族和astacin亚家族的金属蛋白酶抑制剂。

4. 发明授权

US06683086B2 Ultrashort acting hypnotic barbiturates 失效
标题翻译：超短效催眠巴比妥类
公开(公告)号：US06683086B2
公开(公告)日：2004-01-27
申请号：US10145601
申请日：2002-05-13
申请人： Pascal Druzgala , Peter G. Milner
发明人： Pascal Druzgala , Peter G. Milner
IPC分类号： C07D23962
CPC分类号： C07D239/62 , C07D239/66
摘要： The subject invention concerns novel compounds that are useful as ultrashort acting hypnotic barbiturates. Specifically exemplified are derivatives of barbituric and thiobarbituric acids. They are rapidly metabolized by blood and tissue enzymes to form polar metabolites with no hypnotic activity and which are rapidly eliminated.
摘要翻译：本发明涉及可用作超短效催眠巴比妥酸盐的新型化合物。具体举例说明的是巴比妥酸和硫代巴比妥酸的衍生物。它们被血液和组织酶快速代谢，以形成无催眠活性的极性代谢物，并迅速消除。

5. 发明授权

US06472396B1 Barbituric acid derivatives, processes for their production and pharmaceutical agents containing these compounds 失效
标题翻译：巴比妥酸衍生物，其制备方法和含有这些化合物的药剂
公开(公告)号：US06472396B1
公开(公告)日：2002-10-29
申请号：US09594700
申请日：2000-06-16
申请人： Elmar Bosies , Angelika Esswein , Frank Grams , Hans-Willi Krell , Ernesto Menta
发明人： Elmar Bosies , Angelika Esswein , Frank Grams , Hans-Willi Krell , Ernesto Menta
IPC分类号： C07D23962
CPC分类号： C07D401/04 , C07D239/62
摘要： Compounds of formula I, useful as matrix metalloprotease inhibitors, wherein X, Y and Z are each oxygen; R1 is selected from the group consisting of (a) n-octyl, (b) n-decyl, (c) biphenyl and (d) (4-phenoxy)phenyl, wherein the terminal monocycle for moieties (c)-(d) is unsubstituted or substituted by a substituent selected from the group consisting of —NH2, —NO2, —SO2NH2, —SO2CH3, acetyl, hydroxy, methoxy, ethoxy, cyano and halogen; R2 and R3 are each hydrogen; and R4 and R5, together with the nitrogen atom to which they are bound, form a piperazinyl or piperidyl ring, wherein the piperazinyl ring is substituted in the 4-position with a substituent selected from the group consisting of (a) a 6-membered aromatic monocycle having 0, 1 or 2 nitrogen atoms and the remainder of the atoms in the monocycle being carbon and (b) hydroxy-C1-C6 alkyl, wherein the monocycle is unsubstituted or substituted by a substituent selected from the group consisting of halogen, —NH2, —NO2, —SO2NH2, —SO2CH3, acetyl and cyano.
摘要翻译：可用作基质金属蛋白酶抑制剂的式I化合物，其中X，Y和Z各自为氧; R 1选自（a）正辛基，（b）正癸基，（c）联苯和（d）（4-苯氧基）苯基，其中部分（c） - （d）的末端单环是未取代的或被选自-NH 2，-NO 2，-SO 2 NH 2，-SO 2 CH 3，乙酰基，羟基，甲氧基，乙氧基，氰基和卤素; R 2和R 3各自为氢; 和R 4和R 5与它们所连接的氮原子一起形成哌嗪基或哌啶基环，其中哌嗪环在4位被取代基取代，所述取代基选自（a）6元芳族具有0,1或2个氮原子的单环，并且单环中的其余原子为碳和（b）羟基-C 1 -C 6烷基，其中所述单环是未取代的或被选自以下的取代基取代：卤素， NH 2，-NO 2，-SO 2 NH 2，-SO 2 CH 3，乙酰基和氰基。

6. 发明授权

US06387914B2 Ultrashort acting hypnotic barbiturates 失效
标题翻译：超短效催眠巴比妥类
公开(公告)号：US06387914B2
公开(公告)日：2002-05-14
申请号：US09841738
申请日：2001-04-24
申请人： Pascal Druzgala , Peter G. Milner
发明人： Pascal Druzgala , Peter G. Milner
IPC分类号： C07D23962
CPC分类号： C07D239/62 , C07D239/66
摘要： The subject invention concerns novel compounds that are useful as ultrashort acting hypnotic barbiturates. Specifically exemplified are derivatives of barbituric and thiobarbituric acids. They are rapidly metabolized by blood and tissue enzymes to form polar metabolites with no hypnotic activity and which are rapidly eliminated.
摘要翻译：本发明涉及可用作超短效催眠巴比妥酸盐的新型化合物。具体举例说明的是巴比妥酸和硫代巴比妥酸的衍生物。它们被血液和组织酶快速代谢，以形成无催眠活性的极性代谢物，并迅速消除。

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