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21. 发明授权

US07482337B2 Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions 有权
标题翻译：黄嘌呤衍生物，其制备及其作为药物组合物的用途
公开(公告)号：US07482337B2
公开(公告)日：2009-01-27
申请号：US10695597
申请日：2003-10-28
申请人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Roland Maier , Michael Mark , Mohammad Tadayyon , Ralf R. H. Lotz
发明人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Roland Maier , Michael Mark , Mohammad Tadayyon , Ralf R. H. Lotz
IPC分类号： C07D473/06 , C07D519/00 , A61K31/522 , A61K31/538 , A61K31/536 , A61K31/5415 , A61K31/5513 , A61P3/10 , A61P3/04
CPC分类号： C07D473/06
摘要： Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译：公开了以下通式的取代黄嘌呤：其中R1至R4定义如下，其互变异构体，立体异构体，其混合物，其前体药物及其盐具有有价值的药理学性质，特别是对酶二肽基肽酶的活性的抑制作用 -IV（DPP-IV）。

22. 发明申请

US20080255159A1 8-[3-AMINO-PIPERIDIN-1-YL]-XANTHINES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS 有权
标题翻译： 8- [3-氨基 - 哌啶-1-基] - 辛糖，其制备方法及其作为药物组合物的用途
公开(公告)号：US20080255159A1
公开(公告)日：2008-10-16
申请号：US12143219
申请日：2008-06-20
申请人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf R.H. Lotz , Mohammad Tadayyon
发明人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf R.H. Lotz , Mohammad Tadayyon
IPC分类号： A61K31/522 , C07D473/04 , A61P3/10 , A61P3/04
CPC分类号： C07D473/04 , C07D473/06 , C07D473/08 , C07D519/00
摘要： The present invention relates to substituted xanthines of general formula wherein R1 to R3 are defined as in claims 1 to 16, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译：本发明涉及以下通式的取代黄嘌呤：其中R 1至R 3定义如权利要求1至16中所定义，互变异构体，立体异构体，混合物，前体药物其具有有价值的药理学特性的盐，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。

23. 发明授权

US5455273A N,N-disubstituted arylcycloalkylamines, the salts thereof, pharmaceutical compositions containing these compounds and the use thereof and processes for preparing them 失效
标题翻译： N，N-二取代的芳基环烷基胺，其盐，含有这些化合物的药物组合物及其用途及其制备方法
公开(公告)号：US5455273A
公开(公告)日：1995-10-03
申请号：US154644
申请日：1993-11-19
申请人： Roland Maier , Peter Muller , Eberhard Woitun , Rudolf Hurnaus , Michael Mark , Bernhard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
发明人： Roland Maier , Peter Muller , Eberhard Woitun , Rudolf Hurnaus , Michael Mark , Bernhard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
IPC分类号： A61K31/18 , A61K31/27 , A61P1/16 , A61P3/06 , C07C211/27 , C07C211/35 , C07C233/41 , C07C233/62 , C07C233/79 , C07C237/06 , C07C255/24 , C07C311/07 , C07C311/20 , C07D333/38 , A61K31/165
CPC分类号： C07C311/20 , C07C233/62 , C07C233/79 , C07C237/06 , C07C255/24 , C07C311/07 , C07D333/38 , C07C2101/02 , C07C2101/14 , C07C2102/04 , C07C2102/10
摘要： The invention relates to N,N-disubstituted arylcycloalkylamines of general formula ##STR1## wherein n, m, A, X and R.sup.1 to R.sup.7 are defined as in claim 1, the isomers, isomer mixtures and salts thereof, which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis.
摘要翻译：本发明涉及通式为（I）的N，N-二取代的芳基环烷基胺，其中n，m，A，X和R 1至R 7如权利要求1所定义，其异构体，异构体混合物和盐具有有价值的特性，特别是对胆固醇生物合成的抑制作用。

24. 发明授权

US4955300A Adaptive cartridge for a subcaliber barrel system 失效
标题翻译：适用于子套筒系统的墨盒
公开(公告)号：US4955300A
公开(公告)日：1990-09-11
申请号：US428196
申请日：1989-10-27
申请人： Roland Bertiller , Roland Maier
发明人： Roland Bertiller , Roland Maier
IPC分类号： F42B8/10
CPC分类号： F42B8/10
摘要： The invention provides an electrical igniter for an adaptive cartridge of a subcaliber barrel system by which the firing pin extension (12) is arranged axially movable by means of a guide (13) made of an electrically non-conductive material. A slide valve (22) grips a safety rod (17) in the guide (13). The safety rod (17) is situated adjacent the breech mechanism (6) only such that the firing pin (12) borders on the percussion cap (29) of the cartridge (11). By an open breech mechanism (6) the safety rod (17), under spring tension, is moved in the direction of the cartridge (11) together with the firing pin (12).
摘要翻译：本发明提供一种用于子套筒系统的自适应套筒的电点火器，通过该电子点火器，撞击销延伸部12可通过由不导电材料制成的导向件13轴向移动。滑阀（22）夹紧导向件（13）中的安全杆（17）。安全杆（17）仅位于后膛机构（6）附近，使得撞针（12）与盒（11）的冲击盖（29）相接。通过打开的后膛机构（6），弹簧张力下的安全杆（17）与撞击销（12）一起沿着盒（11）的方向移动。

25. 再颁专利

USRE31926E Penicillins and salts thereof 失效
标题翻译：青霉素及其盐
公开(公告)号：USRE31926E
公开(公告)日：1985-06-25
申请号：US420804
申请日：1982-09-21
申请人： Bernd Wetzel , Wolfgang Reuter , Eberhard Woitun , Roland Maier , Uwe Lechner , Hanns Goeth , Rolf Werner
发明人： Bernd Wetzel , Wolfgang Reuter , Eberhard Woitun , Roland Maier , Uwe Lechner , Hanns Goeth , Rolf Werner
IPC分类号： C07D499/66 , A61K31/43 , A61P31/04 , C07D239/42 , C07D239/48 , C07D239/52 , C07D239/56 , C07D499/00 , C07D499/12 , C07D499/64 , C07D499/68 , C07D499/70
CPC分类号： C07D239/42 , C07D239/48 , C07D239/52 , C07D239/56 , C07D499/00
摘要： Compounds of the formula ##STR1## wherein A is phenyl; 4-hydroxy-phenyl; 2- or 3-thienyl; cyclohexyl; cyclohexen-1-yl; cyclohexa-1, 4-dien-1-yl; or 3,4-disubstituted phenyl, where the substituents may be identical to or different from each other and are selected from the group consisting of chlorine, hydroxyl or methoxy; andR is an aliphatic, cycloaliphatic; aromatic or heterocyclic group of diverse types;and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as antibiotics.

26. 发明授权

US4519204A Yarn false twisting apparatus 失效
标题翻译：纱线假捻装置
公开(公告)号：US4519204A
公开(公告)日：1985-05-28
申请号：US429795
申请日：1982-09-30
申请人： Peter Dammann , Hellmut Lorenz , Roland Maier
发明人： Peter Dammann , Hellmut Lorenz , Roland Maier
IPC分类号： D02G1/08
CPC分类号： D02G1/087
摘要： A yarn false twisting apparatus is disclosed which comprises a flexible disc mounted for rotation with a cooperating rigid disc to define a twisting zone therebetween. A pressure applying member is positioned adjacent the back face of the flexible disc for biasing the disc toward the rigid disc locally at the twisting zone so as to firmly engage the yarn passing through the twisting zone. The flexible disc comprises a hub portion disposed adjacent the center of the disc, an annular ring disposed concentrically about the hub portion and including a yarn engaging friction surface on one face thereof, and a distinct and highly flexible junction portion joining the hub portion and annular ring. The highly flexible junction portion permits the annular ring to readily flex in the lateral direction, to thereby permit the deflecting force to be minimized, while still permitting the rotating torque to be transmitted to the annular ring without significant circumferential deformation. The annular ring may also be divided into segments by radial or circumferential slots, to further reduce its resistance to the lateral deforming force of the pressure applying member, and to provide a substantially linear contact with the running yarn.
摘要翻译：公开了一种纱线假捻设备，其包括安装成与协作的刚性盘一起旋转的柔性盘，以在它们之间限定扭转区域。压力施加构件邻近柔性盘的后表面定位，用于在扭转区域局部地朝着刚性盘偏压盘，以便牢固地接合通过扭转区域的纱线。所述柔性盘包括邻近所述盘的中心设置的轮毂部分，围绕所述轮毂部分同心地设置并且在其一个面上包括纱线接合摩擦表面的环形圈和连接所述轮毂部分和环形部分的不同且高度柔性的接合部分环。高度柔性的接合部分允许环形环在横向方向上容易地弯曲，从而允许偏转力最小化，同时仍然允许旋转扭矩传递到环形圈而没有显着的周向变形。环形环也可以通过径向或周向槽分成段，以进一步减小其对压力施加构件的横向变形力的阻力，并提供与运行纱线的基本线性接触。

27. 发明授权

US4362725A Cephalosporins 失效
标题翻译：头孢菌素
公开(公告)号：US4362725A
公开(公告)日：1982-12-07
申请号：US305953
申请日：1981-09-28
申请人： Bernd Wetzel , Eberhard Woitun , Wolfgang Reuter , Roland Maier , Uwe Lechner , Hanns Goeth
发明人： Bernd Wetzel , Eberhard Woitun , Wolfgang Reuter , Roland Maier , Uwe Lechner , Hanns Goeth
IPC分类号： A01N43/86 , A61K20060101 , A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D501/00 , C07D501/36 , C07D501/46 , C07D501/56 , C07D501/57
CPC分类号： C07D501/36 , Y02P20/55
摘要： Compounds of the formula ##STR1## wherein A is phenyl, 4-hydroxy-phenyl, 2-thienyl, 2-furyl or 3,4-dihydroxy-phenyl;Y is hydrogen or methoxy;Het is 4H-5,6-dioxo-1,2,4-triazin-3-yl,4-methyl-5,6-dioxo-1,2,4-triazin-3-yl,2-methyl-5,6-dioxo-1,2,4-triazin-3-yl,1-vinyl-tetrazol-5-yl, 1-allyl-tetrazol-5-yl or ##STR2## where n is an integer from 1 to 3, inclusiveR.sub.1 is hydroxyl, amino, dimethylamino, acetylamino, aminocarbonyl, aminocarbonylamino, aminosulfonyl, aminosulfonylamino, methylcarbonyl, methylsulfonylamino, cyano, hydroxysulfonylamino, methylsulfonyl, methylsulfinyl, a carboxylic acid group or a sulfonic acid group, and--(CH.sub.2).sub.n --R.sub.1 may also be alkyl of 2 to 4 carbon atoms or 2,3-dihydroxy-propyl;R is cyclopropyl, 4'-hydroxycyclohexyl-amino ##STR3## where R.sub.2 is straight or branched, saturated or unsaturated hydrocarbyl of 1 to 4 carbon atoms or cycloalkyl of 3 to 6 carbon atoms;G is hydroxyl, aminocarbonyl, aminosulfonyl, aminocarbonylamino, acetylamino, methylsulfonylamino, methylsulfinyl or methylsulfonyl;m is 0 or 1; andR.sub.3 and R.sub.4, which may be identical to or different from each other, are each hydrogen, chlorine, fluorine, hydroxyl, methoxy, acetylamino, aminocarbonylamino, nitro, acetyl, methylcarbonyloxy, methoxycarbonyl, aminocarbonyl, cyano, methylsulfinyl, methylsulfonyl, aminosulfonyl, methylaminosulfonyl or methyl; andE is hydrogen or a protective group which is easily removable in vitro or in vivo;and, when E is hydrogen, non-toxic, pharmacologically acceptable salts thereof; the compounds as well as their salts are useful as antibiotics.
摘要翻译：其中A是苯基，4-羟基 - 苯基，2-噻吩基，2-呋喃基或3,4-二羟基 - 苯基的式IMA化合物; Y是氢或甲氧基; Het是4H-5,6-二氧代-1,2,4-三嗪-3-基，4-甲基-5,6-二氧代-1,2,4-三嗪-3-基，2-甲基-5- 6-二氧代-1,2,4-三嗪-3-基，1-乙烯基 - 四唑-5-基，1-烯丙基 - 四唑-5-基或其中n是1至3的整数，包括1和3 R 1是羟基，氨基，二甲基氨基，乙酰氨基，氨基羰基，氨基羰基氨基，氨基磺酰基，氨基磺酰基氨基，甲基羰基，甲基磺酰基氨基，氰基，羟基磺酰基氨基，甲磺酰基，甲基亚磺酰基，羧酸基或磺酸基，和 - （CH 2）n -R 具有2至4个碳原子的烷基或2,3-二羟基丙基; 其中R 2是具有1至4个碳原子的直链或支链，饱和或不饱和的烃基或3至6个碳原子的环烷基; R 2是环丙基，4'-羟基环己基氨基， G是羟基，氨基羰基，氨基磺酰基，氨基羰基氨基，乙酰氨基，甲基磺酰基氨基，甲基亚磺酰基或甲基磺酰基; m为0或1; 可以相同或不同的R 3和R 4各自为氢，氯，氟，羟基，甲氧基，乙酰氨基，氨基羰基氨基，硝基，乙酰基，甲基羰基氧基，甲氧基羰基，氨基羰基，氰基，甲基亚磺酰基，甲基磺酰基，氨基磺酰基，甲基氨基磺酰基或甲基; E是氢或在体外或体内容易除去的保护基; 并且当E是氢时，其无毒的药学上可接受的盐; 化合物及其盐可用作抗生素。

28. 发明授权

US4016263A N-Substituted erythromcylamines and salts thereof 失效
公开(公告)号：US4016263A
公开(公告)日：1977-04-05
申请号：US671422
申请日：1976-03-29
申请人： Bernd Wetzel , Eberhard Woitun , Roland Maier , Wolfgang Reuter , Hanns Goeth , Uwe Lechner
发明人： Bernd Wetzel , Eberhard Woitun , Roland Maier , Wolfgang Reuter , Hanns Goeth , Uwe Lechner
IPC分类号： C07H17/08 , A61K31/70
CPC分类号： C07H17/08
摘要： Compounds of the formula ##STR1## wherein E is ##STR2## R.sub.1 is hydrogen; straight or branched alkyl of 1 to 3 carbon atoms; (alkoxy of 1 to 5 carbon atoms)-(alkyl of 1 to 3 carbon atoms); phenyl; or benzyl;R.sub.2 is hydrogen; hydroxyl; straight or branched alkyl of 1 to 3 carbon atoms; or phenyl;R.sub.3 is hydroxyl; alkanoyloxy of 1 to 5 carbon atoms; benzoyloxy; straight or branched alkoxy of 1 to 5 carbon atoms; amino; mono(alkyl of 1 to 5 carbon atoms)-amino; dialkyl-amino, where the sum of carbon atoms in the alkyls is from 2 to 8, inclusive; mono(hydroxy-alkyl of 1 to 4 carbon atoms) -amino; di(hydroxy-alkyl)-amino, where the sum of carbon atoms in the alkyls is from 2 to 8, inclusive; phenyl(alkyl of 1 to 2 carbon atoms)-amino; phenyl-amino, where the phenyl moiety may optionally have one or more halogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms or hydroxyl substituents attached thereto; (alkanoyl of 1 to 5 carbon atoms)-amino; phenyl(alkanoyl of 1 to 5 carbon atoms)-amino; benzoyl-amino; methoxybenzoyl-amino; halobenzoyl-amino; carboxybenzoyl-amino; p-tolylsulfonamino; -HN-NR.sub.4 R.sub.5, where R.sub.4 and R.sub.5 are alkyl of 1 to 3 carbon atoms or, together with each other and the nitrogen atom to which they are attached, form a 5- to 6-membered heterocycle optionally comprising an additional oxygen, sulfur or nitrogen heteroatom in the ring, and said additional nitrogen heteroatom optionally having an alkyl of 1 to 5 carbon atoms substituent attached thereto; ##STR3## where R.sub.6 is amino; mono(straight or branched alkyl of 1 to 8 carbon atoms)-amino; dialkylamino, where the sum of carbon atoms in the alkyls is from 2 to 6, inclusive; cyclohexyl-amino; N-(alkyl of 1 to 3 carbon atoms)-N-cyclohexyl-amino; dicyclohexyl-amino; methoxy(alkyl of 1 to 3 carbon atoms)-amino; di-methoxy(alkyl of 1 to 3 carbon atoms)-amino; benzyl-amino, where the phenyl moiety may optionally have from one to three (alkoxy of 1 to 3 carbon atoms)-substituents attached thereto; phenethyl-amino, where the phenyl moiety may optionally have from one to three(alkoxy of 1 to 3 carbon atoms)-substituents attached thereto; dibenzyl-amino; di(phenethyl)-amino; benzhydrylamino; N-methyl-N-benzyl-amino; N-phenyl-N-benzyl-amino; N-methyl-N-phenyl-amino; N-ethyl-N-phenyl-amino; piperidino; methyl-piperidino; benzyl-piperidino; pyrrolidino; methyl-pyrrolidino; benzyl-pyrrolidino; morpholino; methyl-morpholino; benzyl-morpholino; piperazino; methyl-piperazino; benzyl-piperazino; hexamethyleneimino; methyl-hexamethyleneimino; benzyl-hexamethyleneimino; thiomorpholino; methyl-thiomorpholino; benzyl-thiomorpholino; heptamethyleneimino; methyl-heptamethyleneimino; or benzyl-heptamethylimino; andR.sub.7 is amino; cyclohexylamino; di(alkyl of 1 to 3 carbon atoms)-amino; benzyl-amino; phenethyl-amino; dibenzyl-amino; phenoxy-methyl-amino; phenoxyethyl-amino; N-phenyl-N-benzyl-amino; N-methyl-N-phenyl-amino; piperidino, benzyl-piperidino; pyrrolidino; benzyl-pyrrolidino; morpholino; benzyl-morpholino; piperazino; benzyl-piperazino; thiomorpholino; benzyl-thiomorpholino; hexamethyleneimino; benzyl-hexamethyleneimino; hydrogen; alkyl of 1 to 3 carbon atoms; cyclohexyl, benzyl, methoxy-benzyl; phenethyl; methoxyphenethyl; thienyl; furyl; pyridyl; (alkyl of 1 to 3 carbon atoms)-thio; methoxy(alkyl of 1 to 3 carbon atoms)-thio; cyano(alkyl of 1 to 3 carbon atoms)-thio; benzyl-thio; methylbenzyl-thio; phenyl-thio; or tolyl-thio;R.sub.3 = is also NH-A-B, where A is alkylene of 1 to 4 carbon atoms; and B is alkoxy of 1 to 3 carbon atoms, di(alkyl of 1 to 3 carbon atoms)-amino or carbalkoxy of 2 to 4 carbon atoms;thiazolyl-amino; orpyridyl-amino; andn is 0 or 1;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antibacterials.

29. 发明申请

US20100144703A1 XANTHINE DERIVATIVES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译： XANTHINE衍生物，其制备方法及其作为药物组合物的用途
公开(公告)号：US20100144703A1
公开(公告)日：2010-06-10
申请号：US12706739
申请日：2010-02-17
申请人： Frank HIMMELSBACH , Elke LANGKOPF , Matthias ECKHARDT , Roland MAIER , Michael MARK , Mohammad TADAYYON , Ralf R. H. LOTZ
发明人： Frank HIMMELSBACH , Elke LANGKOPF , Matthias ECKHARDT , Roland MAIER , Michael MARK , Mohammad TADAYYON , Ralf R. H. LOTZ
IPC分类号： A61K31/553 , C07D473/04 , A61K31/522 , A61K31/5513 , A61K31/554
CPC分类号： C07D473/06
摘要： Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译：公开了以下通式的取代黄嘌呤：其中R1至R4定义如下，其互变异构体，立体异构体，其混合物，其前体药物及其盐具有有价值的药理学性质，特别是对酶二肽基肽酶的活性的抑制作用 -IV（DPP-IV）。

30. 发明申请

US20090093457A1 XANTHINE DERIVATIVES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS 有权
标题翻译： XANTHINE衍生物，其制备方法及其作为药物组合物的用途
公开(公告)号：US20090093457A1
公开(公告)日：2009-04-09
申请号：US12331720
申请日：2008-12-10
申请人： Frank HIMMELSBACH , Elke LANGKOPF , Matthias ECKHARDT , Roland MAIER , Michael MARK , Mohammad TADAYYON , Ralf R. H. LOTZ
发明人： Frank HIMMELSBACH , Elke LANGKOPF , Matthias ECKHARDT , Roland MAIER , Michael MARK , Mohammad TADAYYON , Ralf R. H. LOTZ
IPC分类号： A61K31/522 , C07D473/04 , C07D265/14 , C07D279/16 , A61K31/54 , A61K31/554 , A61P3/00 , A61K31/5513 , A61K31/536 , C07D243/12 , C07D285/36
CPC分类号： C07D473/06
摘要： Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译：公开了以下通式的取代黄嘌呤：其中R1至R4定义如下，其互变异构体，立体异构体，其混合物，其前体药物及其盐具有有价值的药理学性质，特别是对酶二肽基肽酶的活性的抑制作用 -IV（DPP-IV）。

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