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1. 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。

2. 发明授权

US4880805A 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：US4880805A
公开(公告)日：1989-11-14
申请号：US222215
申请日：1988-07-21
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
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。

3. 发明授权

US4612313A Pharmaceutical phenylacetonitrile derivatives 失效
标题翻译：药用苯乙腈衍生物
公开(公告)号：US4612313A
公开(公告)日：1986-09-16
申请号：US774354
申请日：1985-09-10
申请人： Herbert Leinert , Wolfgang Kampe , Klaus Strein , Bernd Muller-Beckmann , Wolfgang Bartsch
发明人： Herbert Leinert , Wolfgang Kampe , Klaus Strein , Bernd Muller-Beckmann , Wolfgang Bartsch
IPC分类号： A61K31/21 , A61K31/275 , A61K31/445 , A61P9/08 , A61P9/10 , A61P9/12 , C07C67/00 , C07C253/00 , C07C255/24 , C07C255/32 , C07C255/42 , C07C255/43 , C07C255/53 , C07C255/58 , C07C255/59 , C07D207/08 , C07D211/22 , C07D241/04 , C07D295/16 , C07D295/18 , A61K31/495 , C07C121/80
CPC分类号： C07C255/00 , C07D211/22
摘要： The present invention provides phenylacetonitrile derivatives of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, are hydrogen or haolgen atoms or alkyl, alkoxy, nitro, amino or acylamino radicals and two adjacent substituents can together also form a methylenedioxy or ethylenedioxy radical, A is a radical of the general formula: ##STR2## in which R.sub.6 is a straight-chained, cyclic or branched, saturated or unsaturated alkyl radical containing 2 to 12 carbon atoms, R.sub.7 is a hydrogen atom or a straight-chained or branched, saturated alkyl radical containing up to 6 carbon atoms, m and n, which can be the same or different, are 2 or 3, p is 1 or 2 and X is a straight-chained, cyclic or branched alkyl radical containing 2 to 10 carbon atoms which is optionally substituted by an amino group or is a grouping of the general formula: ##STR3## wherein Y and Z, which can be the same or different, are straight-chained or branched alkyl radicals containing up to 8 carbon atoms or cycloalkyl, alkylcycloalkyl or cycloalkylalkyl radicals, in which these radicals are optionally interrupted by an oxygen or sulphur atom, and one of the groups Z in general formula II can also be a hydrogen atom or both Z groups are joined to form a ring containing 4 to 6 carbon atoms which is optionally interrupted by a further nitrogen atom which can be substituted by alkyl or alkanoyl, the --O--NO.sub.2 groups being substituents of Y as well as of Z; as well as the salts thereof with physiologically acceptable acids.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.
摘要翻译：本发明提供以下通式的苯乙腈衍生物：其中R 1，R 2，R 3，R 4和R 5可以相同或不同，为氢或卤素原子或烷基，烷氧基，硝基，氨基或酰基氨基和两个相邻的取代基可以一起形成亚甲二氧基或亚乙二氧基，A是下列通式的基团：其中R 6是含有2至12个直链的直链，环状或支链的饱和或不饱和烷基碳原子，R7是氢原子或含有至多6个碳原子的直链或支链饱和烷基，m和n可相同或不同，为2或3，p为1或2，X为是含有2至10个碳原子的直链，环状或支链烷基，其任选被氨基取代，或者是通式如下的基团：其中Y和Z可以相同或不同，是直链或支链烷基基团引入多达8个碳原子或环烷基，烷基环烷基或环烷基烷基，其中这些基团任选地被氧或硫原子中断，通式II中的基团Z之一也可以是氢原子或两个Z基团连接形成含有4至6个碳原子的环，其任选被可被烷基或烷酰基取代的另外的氮原子中断，-O-NO 2基团是Y和Z的取代基; 以及其与生理上可接受的酸的盐。本发明还提供了制备这些化合物的方法和含有它们的药物组合物。

4. 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。

5. 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.

6. 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：

7. 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。

8. 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。

9. 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。

10. 发明授权

US4824963A Process for the preparation of optically-active carbazole derivatives 失效
标题翻译：光学活性咔唑衍生物的制备方法
公开(公告)号：US4824963A
公开(公告)日：1989-04-25
申请号：US49673
申请日：1987-05-13
申请人： Herbert Leinert
发明人： Herbert Leinert
IPC分类号： A61K31/40 , A61K31/403 , A61K31/44 , A61K31/4427 , A61K31/443 , A61P9/08 , A61P9/12 , A61P25/02 , C07C29/09 , C07D209/56 , C07D209/88 , C07D303/08 , C07D303/12 , C07D303/14 , C07D303/16 , C07D317/20 , C07D401/12 , C07D405/12 , C07D491/056 , C07D209/82
CPC分类号： C07D405/12 , C07C309/00 , C07D209/88 , C07D303/14 , C07D303/16 , C07D317/20 , Y10S514/913 , Y10S514/929
摘要： A process for the preparation of S- or R-carbazole derivatives of the general formula: ##STR1## in which R is an unsubstituted or substituted amino radical and pharmacologically acceptable salts, by either reacting R-(-)-epichlorohydrin (for the S-carbazole derivative); or reacting an S-epoxide derivative of the general formula: ##STR2## in which R.sub.1 is the residue of a substituted sulphonic acid derivative (for the R-carbazole derivative); with 4-hydroxycarbazole and then with ammonia or a substituted amine of the general formula RH, and recovering the compound or converting it to a pharmacologically acceptable salt.The new R-(+)- and S-(-)-carbozole derivatives provided by the inventive process have unexpected beta blocking and vasodilatory properties and are useful in pharmaceutical compositions. R-(+)-carbazole derivatives are also useful for the treatment of glaucoma.
摘要翻译：制备以下通式的S-或R-咔唑衍生物的方法：其中R是未取代或取代的氨基和其药理学上可接受的盐，通过使R - （ - ） - 表氯醇反应（对于S 咔唑衍生物）; 或使下列通式的S-环氧化物衍生物：其中R 1是取代的磺酸衍生物的残基（对于R-咔唑衍生物）; 与4-羟基咔唑然后与氨或通式为RH的取代胺反应，并回收该化合物或将其转化为药理学上可接受的盐。由本发明方法提供的新的R - （+） - 和 - （ - ） - 碳唑衍生物具有意想不到的β阻断和血管扩张性质，并且可用于药物组合物。 R - （+） - 咔唑衍生物也可用于治疗青光眼。

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