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1. 发明授权

US06716845B2 Barbituric acid derivatives 失效
标题翻译：巴比妥酸衍生物
公开(公告)号：US06716845B2
公开(公告)日：2004-04-06
申请号：US10082907
申请日：2002-02-25
申请人： Dagmar Geppert , Frank Grams , Hans-Willi Krell , Herbert Leinert , Ernesto Menta , Gerd Zimmermann
发明人： Dagmar Geppert , Frank Grams , Hans-Willi Krell , Herbert Leinert , Ernesto Menta , Gerd Zimmermann
IPC分类号： A61K31515
CPC分类号： C07D405/12 , C07D239/62
摘要： The present invention pertains to derivatives of 5,5-disubstituted pyrimidine-2,4,6,-trianones having the formula: wherein R1, R2, R3, and R4 are described herein. These compounds have antitumor and antimetastatic activity.
摘要翻译：本发明涉及具有下式的5,5-二取代嘧啶-2,4,6 - 十二烷酮的衍生物：其中R 1，R 2，R 3和R 4在本文中描述。这些化合物具有抗肿瘤和抗转移活性。

2. 发明授权

US06576628B1 3-aryl-succinamido-hydroxamic acids, methods for producing said acids and medicaments containing the same 失效
标题翻译： 3-芳基 - 琥珀酰氨基 - 异羟肟酸，制备所述酸的方法和含有该酸的药物
公开(公告)号：US06576628B1
公开(公告)日：2003-06-10
申请号：US09486038
申请日：2000-07-06
申请人： Frank Grams , Gerd Zimmermann , Hans-Willi Krell , Ernesto Menta , Herbert Leinert
发明人： Frank Grams , Gerd Zimmermann , Hans-Willi Krell , Ernesto Menta , Herbert Leinert
IPC分类号： C07C25906
CPC分类号： C07C259/06
摘要： The invention relates to inhibitors of matrix metalloproteases, more specifically a 3-aryl-succinamido-hydroxamic acid of formula (I) and its salt, ester and derivative thereof, along with methods of producing a compound of formula (I) and pharmaceutical compositions thereof.
摘要翻译：本发明涉及基质金属蛋白酶抑制剂，更具体地说是式（I）的3-芳基 - 琥珀酰氨基 - 异羟肟酸及其盐，酯和衍生物，以及制备式（I）化合物及其药物组合物的方法。

3. 发明授权

US06498252B1 Pyrimidine-2,4,6-trione derivatives, processes for their production and pharmaceutical agents containing these compounds 失效
标题翻译：嘧啶-2,4,6-三酮衍生物，其制备方法和含有这些化合物的药剂
公开(公告)号：US06498252B1
公开(公告)日：2002-12-24
申请号：US09675935
申请日：2000-09-29
申请人： Frank Grams , Hans-Willi Krell , Herbert Leinert , Ernesto Menta , Gerd Zimmermann
发明人： Frank Grams , Hans-Willi Krell , Herbert Leinert , Ernesto Menta , Gerd Zimmermann
IPC分类号： C07D40304
CPC分类号： C07D239/545 , A61K31/515 , C07D405/12
摘要： Compounds of formula I in which R1 represents a substituted or unsubstituted phenoxy, phenylthio, phenylsulfinyl, phenylsulfonyl, phenylamino or phenylmethyl residue, and R2 represents an optionally substituted aryl or heteroaryl residue, with metallo-proteinase inhibitor activity.
摘要翻译： R 1表示取代或未取代的苯氧基，苯硫基，苯基亚磺酰基，苯基磺酰基，苯基氨基或苯基甲基残基的式Iin化合物，R 2表示具有金属蛋白酶抑制剂活性的任选取代的芳基或杂芳基残基。

4. 发明授权

US6121322A Azulene derivatives 失效
标题翻译：薁衍生物
公开(公告)号：US6121322A
公开(公告)日：2000-09-19
申请号：US198722
申请日：1998-11-24
申请人： Joachim Dickhaut , Walter-Gunar Friebe , Frank Grams , Rainer Haag , Herbert Leinert
发明人： Joachim Dickhaut , Walter-Gunar Friebe , Frank Grams , Rainer Haag , Herbert Leinert
IPC分类号： C07D295/08 , A61K31/015 , A61K31/16 , A61K31/357 , A61K31/40 , A61K31/41 , A61K31/4164 , A61K31/445 , A61K31/4453 , A61K31/495 , A61K31/5375 , A61K31/662 , A61P29/00 , C07C239/20 , C07C259/06 , C07C271/60 , C07D233/02 , C07D257/06 , C07D295/088 , C07D295/12 , C07D295/185 , C07D295/20 , C07D317/22 , C07D317/30 , C07F9/38 , C07F9/40 , A61K31/185 , C07C229/28
CPC分类号： C07D295/185 , C07C259/06 , C07C271/60 , C07D295/088 , C07D317/22 , C07F9/3808 , C07F9/4006 , C07C2102/30
摘要： The invention provides novel azulene derivatives of general formula I ##STR1## wherein R.sub.1 to R.sub.6 have the significance given in the description, as well as their tautomers, enantiomers, diastereomers, racemates and physiologically compatible salts or esters and substances which are hydrolyzed or metabolized in vivo to compounds of formula I.The invention is also concerned with a process and intermediates for the manufacture of the above compounds, pharmaceutical compositions which contain such compounds as well as the use of these compounds in the treatment of inflammatory conditions.
摘要翻译：本发明提供了通式I的新颖的薁衍生物，其中R 1至R 6具有本说明书给出的含义，以及它们的互变异构体，对映异构体，非对映异构体，外消旋物和生理上相容的盐或酯和物质，其在体内水解或代谢为化合物本发明还涉及制备上述化合物的方法和中间体，含有这些化合物的药物组合物以及这些化合物在治疗炎性病症中的用途。

5. 发明授权

US5756711A Phospholipid derivatives of nucleosides and their use as anti-viral medicaments 失效
标题翻译：核苷的磷脂衍生物及其作为抗病毒药物的用途
公开(公告)号：US5756711A
公开(公告)日：1998-05-26
申请号：US661038
申请日：1996-06-10
申请人： Harald Zilch , Herbert Leinert , Alfred Mertens , Dieter Herrmann
发明人： Harald Zilch , Herbert Leinert , Alfred Mertens , Dieter Herrmann
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/12 , C07H19/10 , C07H19/20 , C12P19/28 , C12P19/30
CPC分类号： C07H19/10 , C07H19/20 , C12P19/28
摘要： Compounds of the formula I ##STR1## in which R.sub.1 and R.sub.2 represent a possibly substituted C.sub.8 -C.sub.15 -alkyl chain, n the number 0, 1 or 2 and A the residue of a nucleoside, processes for their preparation, as well as antiviral medicaments which contain these compounds.
摘要翻译：其中R1和R2代表可能被取代的C 8 -C 15烷基链，数字0,1或2，A是核苷的残基，其制备方法以及抗病毒药物的式I的化合物其中含有这些化合物。

6. 发明授权

US4927834A 1,2-diamino compounds, processes for their preparation and pharmaceutical compositions containing them 失效
公开(公告)号：US4927834A
公开(公告)日：1990-05-22
申请号：US230946
申请日：1988-08-11
申请人： Herbert Leinert , Christos Tsaklakidis , Gisbert Sponer
发明人： Herbert Leinert , Christos Tsaklakidis , Gisbert Sponer
IPC分类号： A61K31/215 , A61K31/135 , A61K31/19 , A61K31/33 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/40 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61P9/00 , A61P9/08 , C07D213/38 , C07D213/74 , C07D295/12 , C07D295/13 , C07D307/52 , C07D317/58 , C07D317/66 , C07D333/20 , C07D521/00
CPC分类号： C07D213/74 , C07D213/38 , C07D295/13 , C07D307/52 , C07D317/58 , C07D317/66 , C07D333/20
摘要： The present invention provides compounds of the general formula: ##STR1## wherein R.sub.1 is a straight-chained or branched C.sub.1 -C.sub.12 -alkyl radical which can be substituted by phenyl, naphthyl or a C.sub.3 -C.sub.7 -cycloalkyl radical; a straight-chained or branched C.sub.2 -C.sub.6 -alkenyl radical which can be substituted by a C.sub.3 -C.sub.7 -cycloalkyl radical or a phenyl or naphthyl radical; a C.sub.3 -C.sub.7 -cycloalkyl radical or a mono- or bicyclic aromatic radical which is unsubstituted or substituted one or more times, the substituents being C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, carboxyl or carbethoxy, R.sub.2 and R.sub.3, which can be the same or different, are straight-chained or branched, saturated or unsaturated C.sub.1 -C.sub.6 -alkyl radicals which are optionally substituted by hydroxyl, C.sub.1 -C.sub.3 -alkoxy or C.sub.1 -C.sub.3 -alkoxy-C.sub.1 -C.sub.3 -alkoxy or, together with the nitrogen atom to which they are attached, form a saturated or unsaturated ring which can contain further heteroatoms and is optionally substituted by a lower alkyl or lower alkoxy radical or by an oxygen atom, A is a valency bond or a straight-chained or branched alkylene radical containing up to 6 and preferably up to 3 carbon atoms, R.sub.4 is a mono- or bicyclic aromatic or heteroaromatic radical which is unsubstituted or substituted one or more times, whereby the substituents are alkyl, C.sub.2 -C.sub.6 -alkenyl, alkoxy, C.sub.2 -C.sub.6 -alkenyloxy, hydroxyalkyl, C.sub.2 -C.sub.6 -alkylenedioxy, hydroxyalkoxy, alkoxyethoxy, alkylamino, dialkylamino, alkoxycarbonylethyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylsulphonyloxy, carboxyl, alkoxycarbonyl, aminocarbonyl, mono- or dialkylaminocarbonyl, haloalkyl or cyano, as well as halogen atoms, such as chlorine, bromine or fluorine, X is a valency bond or a straight-chained or branched, saturated or unsaturated hydrocarbon radical containing up to 6 carbon atoms, Y is a valency bond or an oxygen atom and R.sub.5 is a C.sub.3 -C.sub.7 -cycloalkyl radical or a mono- or bicyclic aromatic or heteroaromatic radical which is unsubstituted or substituted one or more times, the substituents being alkyl, alkoxy, C.sub.2 -C.sub.6 -alkenyloxy, aralkoxy, hydroxyl, hydroxyalkoxy, alkoxyalkoxy, alkoxycarbonylalkoxy, C.sub.1 -C.sub.2 -alkenylenedioxy, dialkylamino, alkylthio, alkylsulphinyl, alkyl-sulphonyl, alkylsulphonyloxy, hydroxyalkyl, carboxyl, alkoxycarbonyl, aminocarbonyl, mono- or dialkylaminocarbonyl or cyano, as well as halogen atoms, such as chlorine, bromine or fluorine, with the proviso that Y cannot be an oxygen atom when X is a valency bond and that when R.sub.1 is a saturated hydrocarbon radical, X must be a radical with at least 2 carbon atoms; as well as the pharmacologically acceptable salts thereof and the optical isomers thereof.The present invention also provides processes for the preparation of these 1,2-diamino compounds and pharmaceutical compositions containing them.

7. 发明授权

US4780474A Use of alkylenediamine derivatives for the treatment of blood flow disturbances and pharmaceutical compositions containing them 失效
标题翻译：使用亚烷基二胺衍生物治疗血流紊乱和含有它们的药物组合物
公开(公告)号：US4780474A
公开(公告)日：1988-10-25
申请号：US6275
申请日：1987-01-20
申请人： Erwin Bohm , Jens-Peter Holck , Wolfgang Kampe , Herbert Leinert , Bernd Muller-Beckmann , Klaus Strein
发明人： Erwin Bohm , Jens-Peter Holck , Wolfgang Kampe , Herbert Leinert , Bernd Muller-Beckmann , Klaus Strein
IPC分类号： C07D295/20 , A61K31/135 , A61K31/165 , A61K31/22 , A61K31/33 , A61K31/415 , A61K31/505 , A61K31/535 , A61K31/5375 , A61P7/00 , A61P9/00 , C07C67/00 , C07C213/00 , C07C217/84 , C07C231/00 , C07C233/25 , C07C233/78 , C07C235/44 , C07C235/46 , C07C235/50 , C07C237/22 , C07C237/34 , C07C239/00 , C07C241/00 , C07C253/00 , C07C255/54 , C07C275/00 , C07C313/00 , C07C323/36 , C07C323/60 , C07D231/38 , C07D231/56 , C07D239/54 , C07D521/00 , A61K31/40 , A61K31/405 , A61K31/41
CPC分类号： A61K31/505 , A61K31/135 , A61K31/165 , A61K31/415
摘要： The present invention is concerned with the use of compounds of the general formula: ##STR1## wherein A is an optionally substituted phenyl or heteroaromatic radical, R.sub.6 and R.sub.7 are hydrogen or lower alkyl, X is an alkylene chain containing up to 6 carbon atoms, Y is a valency bond or a >C.dbd.O group and B is an optionally substituted phenyl or heteroaromatic radical, as well as of their pharmacologically acceptable salts for the treatment of blood flow disturbances. The present invention also provides pharmaceutical compositions which contain these compounds.
摘要翻译：本发明涉及以下通式的化合物的用途：其中A是任选取代的苯基或杂芳族基团，R 6和R 7是氢或低级烷基，X是含有至多6个亚烷基的亚烷基链碳原子，Y是价键或> C = O基团，B是任选取代的苯基或杂芳族基团，以及它们的药理学上可接受的盐用于治疗血流紊乱。本发明还提供含有这些化合物的药物组合物。

8. 发明授权

US3976779A 1,2,3,4-Tetrahydro-carbazole compounds and .beta.-adrenergic compositions 失效
标题翻译： 1,2,3,4-四氢咔唑化合物和{62-肾上腺素能组合物
公开(公告)号：US3976779A
公开(公告)日：1976-08-24
申请号：US568743
申请日：1975-04-16
申请人： Herbert Leinert , Alfred Popelak , Kurt Stach , Wolfgang Bartsch , Karl Dietmann
发明人： Herbert Leinert , Alfred Popelak , Kurt Stach , Wolfgang Bartsch , Karl Dietmann
IPC分类号： C07D209/88 , A61K31/40
CPC分类号： C07D209/88
摘要： New 1,2,3,4-tetra-hydrocarbazole derivatives of the formula: ##SPC1##Wherein R.sup.1 is straight-chained or branched alkyl, and the pharmacologically compatible salts thereof, are markedly effective as inhibitors of adrogenic .beta.-receptors and thus useful for the treatment and prophylaxis of cardiac and circulatory diseases.
摘要翻译：新的具有下式的1,2,3,4-四烃基衍生物：

9. 发明授权

US5563257A Phospholipid derivatives of nucleosides 失效
标题翻译：核苷的磷脂衍生物
公开(公告)号：US5563257A
公开(公告)日：1996-10-08
申请号：US438240
申请日：1995-05-09
申请人： Harald Zilch , Herbert Leinert , Alfred Mertens , Dieter Herrmann
发明人： Harald Zilch , Herbert Leinert , Alfred Mertens , Dieter Herrmann
IPC分类号： C07H19/10 , C07H19/20 , C12P19/28
CPC分类号： C07H19/10 , C07H19/20 , C12P19/28
摘要： Liponucleotides containing an ether linkage in the 2-position and a thioether, sulfoxide, or sulfone linkage in the 3-position. The nucleoside component of said liponucleotide is AZT or 3'-deoxy-3'-fluorothymidine. These compounds exhibit antiviral activity.
摘要翻译：在2位上含有醚键的脂核苷酸和3位的硫醚，亚砜或砜键。所述脂核苷酸的核苷组分是AZT或3'-脱氧-3'-氟胸苷。这些化合物表现出抗病毒活性。

10. 发明授权

US5397794A Use of thiazoloisoindolinone derivatives as antiviral medicaments 失效
标题翻译：噻唑并二吲哚啉酮衍生物作为抗病毒药物的使用
公开(公告)号：US5397794A
公开(公告)日：1995-03-14
申请号：US50067
申请日：1993-07-20
申请人： Harald Zilch , Alfred Mertens , Herbert Leinert , Ulrike Leser , Bernhard Konig , Hans Seidel
发明人： Harald Zilch , Alfred Mertens , Herbert Leinert , Ulrike Leser , Bernhard Konig , Hans Seidel
IPC分类号： A61K31/425 , A61P31/12 , C07D513/04
CPC分类号： A61K31/425 , Y10S514/934
摘要： The present invention concerns the use of compounds of the general formula I ##STR1## for the preparation of medicaments for the treatment of viral or retroviral infections, whereby R signifies a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl radical with 1-7 carbon atoms, which can possibly be substituted by phenyl, or a phenyl ring which can possibly be substituted one or more times by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, hydroxyl, trifluoromethyl, methylsulphonyl or halogen, such as fluorine, chlorine or bromine, n stands for the numbers 0, 1 or 2, as well as of their pharmacologically compatible salts or tautomers.
摘要翻译： PCT No.PCT / EP91 / 02101 Sec。 371日期：1993年7月20日 102（e）日期1993年7月20日PCT 1991年11月6日PCT PCT。公开号WO92 / 08457 日期：1992年5月29日。本发明涉及通式I的化合物（I）用于制备用于治疗病毒或逆转录病毒感染的药物，其中R表示氢原子或直链或具有1-7个碳原子的支链，饱和或不饱和的烷基，其可以被苯基取代，或可以被C1-C4-烷基，C1-C4-烷氧基，羟基取代一次或多次的苯环，三氟甲基，甲基磺酰基或卤素如氟，氯或溴，n代表数字0,1或2，以及它们的药理学上相容的盐或互变异构体。

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