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1.发明授权Medicaments, vicinal dihydroxyalkylxanthines contained therein, processes for the preparation of these xanthine compounds and intermediate products suitable for these 失效药物，其中所含的邻位二羟基烷基黄嘌呤，制备这些黄嘌呤化合物的方法和适用于这些的黄嘌呤化合物的中间产物
公开(公告)号：US4616020A
公开(公告)日：1986-10-07
申请号：US420932
申请日：1982-09-17
IPC分类号： A61K31/52 , A61K31/522 , A61P11/08 , C07C21/04 , C07C29/10 , C07C31/42 , C07D303/08 , C07D317/16 , C07D317/20 , C07D473/06 , C07D473/08 , C07D473/10 , A61K31/505
CPC分类号： C07D473/08 , C07C29/10 , C07C31/42 , C07D303/08 , C07D317/16 , C07D317/20 , C07D473/06
摘要： Compounds of the formula ##STR1## wherein one of the radicals R.sup.1, R.sup.2 or R.sup.3 denotes a straight-chain alkyl group having 4 to 8 C atoms and two vicinal hydroxyl groups in the .omega.,.omega.-1 or .omega.-1,.omega.-2 positions and the two other radicals represent straight-chain or branched alkyl groups having up to 12 C atoms in the position of R.sup.1 and R.sup.3 and up to 4 C atoms in the position of R.sup.2, the total of C atoms in these two alkyl substituents being a maximum of 14, are prepared by oxidation of the corresponding alkenylxanthines and by alkylation with compounds which introduce the dihydroxyalkyl radical or a precursor thereof. The dihydroxyalkyldialkylxanthines are suitable for the treatment of obstructive respiratory tract diseases.
摘要翻译： 式（I）的化合物其中基团R 1，R 2或R 3中的一个表示具有4至8个C原子的直链烷基和ω，ω-1或ω-1中的两个邻位羟基， ω-2位，另外两个基团表示在R 2和R 3的位置具有至多12个C原子的直链或支链烷基，R2的位置中具有至多4个C原子的直链或支链烷基，这两个基团中的C原子总数 通过氧化相应的链烯基黄嘌呤并通过引入二羟基烷基或其前体的化合物进行烷基化来制备最多14个的烷基取代基。 二羟基烷基二烷基黄嘌呤适用于治疗阻塞性呼吸道疾病。
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公开(公告)号：US4713455A
公开(公告)日：1987-12-15
申请号：US848139
申请日：1986-04-04
IPC分类号： A61K31/52 , A61K31/522 , A61P11/08 , C07C21/04 , C07C29/10 , C07C31/42 , C07D303/08 , C07D317/16 , C07D317/20 , C07D473/06 , C07D473/08 , C07D473/10 , C07D405/06
CPC分类号： C07D473/08 , C07C29/10 , C07C31/42 , C07D303/08 , C07D317/16 , C07D317/20 , C07D473/06
摘要： Compounds of the formula ##STR1## wherein one of the radicals R.sup.1, R.sup.2 or R.sup.3 denotes a straight-chain alkyl group having 4 to 8 C atoms and two vicinal hydroxyl groups in the .omega.,.omega.-1 or .omega.-1,.omega.-2 positions and the two other radicals represent straight-chain or branched alkyl groups having up to 12 C atoms in the position of R.sup.1 and R.sup.3 and up to 4 C atoms in the position of R.sup.2, the total of C atoms in these two alkyl substituents being a maximum of 14, are prepared by oxidation of the corresponding alkenylxanthines and by alkylation with compounds which introduce the dihydroxyalkyl radical or a precursor thereof. The dihydroxyalkyldialkylxanthines are suitable for the treatment of obstructive respiratory tract diseases.
摘要翻译： 式（I）的化合物其中基团R 1，R 2或R 3中的一个表示具有4至8个C原子的直链烷基和ω，ω-1或ω-1中的两个邻位羟基， ω-2位，另外两个基团表示在R 2和R 3的位置具有至多12个C原子的直链或支链烷基，R2的位置中具有至多4个C原子的直链或支链烷基，这两个基团中的C原子总数 通过氧化相应的链烯基黄嘌呤并通过引入二羟基烷基或其前体的化合物进行烷基化来制备最多14个的烷基取代基。 二羟基烷基二烷基黄嘌呤适用于治疗阻塞性呼吸道疾病。
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公开(公告)号：US5710272A
公开(公告)日：1998-01-20
申请号：US480801
申请日：1995-06-07
IPC分类号： A61K31/52 , A61K31/522 , A61P9/00 , C07B37/10 , C07D473/04 , C07D473/06 , C07D473/08 , C07D473/10 , C12N1/16 , C12P17/18 , C12P41/00 , C12R1/645
CPC分类号： C12P41/002 , C07D473/06 , C07D473/08 , C07D473/10 , C12P17/18 , Y10S435/822 , Y10S435/911
摘要： A Rhodotorula rubra strain has been found which reduces pentoxifylline to 100% to give the S-alcohol. Moreover, other oxoalkylxanthine derivatives can also be convened into the corresponding S-alcohol. The microbiologically obtained S-(+)-enantiomers can then be converted stereoselectively into the respective R-(-)-enantiomers. The corresponding S-alcohols and the R-alcohols obtained by enantioselective inversion of configuration cause an increase in cerebral blood flow.
摘要翻译： 已经发现红酵母菌株将己酮可可碱降至100％以得到S-醇。 此外，其它氧代烷基黄嘌呤衍生物也可以被引入到相应的S-醇中。 然后将微生物获得的S - （+） - 对映异构体立体选择性地转化成相应的R - （ - ） - 对映异构体。 通过配置对映选择性反转获得的相应的S-醇和R-醇导致脑血流量的增加。
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4.发明授权Process for the enantioselective preparation of (.beta.-1)-hydroxyalkylxanthines by reduction using Rhodotorula rubra 失效通过使用红酵母（Rhodotorula rubra）进行还原的对映选择性制备（β-1） - 羟基烷基黄嘌呤的方法
公开(公告)号：US5310666A
公开(公告)日：1994-05-10
申请号：US975996
申请日：1992-11-13
IPC分类号： A61K31/52 , A61K31/522 , A61P9/00 , C07B37/10 , C07D473/04 , C07D473/06 , C07D473/08 , C07D473/10 , C12N1/16 , C12P17/18 , C12P41/00 , C12R1/645
CPC分类号： C12P41/002 , C07D473/06 , C07D473/08 , C07D473/10 , C12P17/18 , Y10S435/822 , Y10S435/911
摘要： A Rhodotorula rubra strain has been found which reduces pentoxifylline to 100% to give the S-alcohol. Moreover, other oxoalkylxanthine derivatives can also be converted into the corresponding S-alcohol. The microbiologically obtained S-(+)-enantiomers can then be converted stereoselectively into the respective R-(-)-enantiomers. The corresponding S-alcohols and the R-alcohols obtained by enantioselective inversion of configuration cause an increase in cerebral blood flow.
摘要翻译： 已经发现红酵母菌株将己酮可可碱降至100％以得到S-醇。 此外，其它氧代烷基黄嘌呤衍生物也可以转化为相应的S-醇。 然后将微生物获得的S - （+） - 对映异构体立体选择性地转化成相应的R - （ - ） - 对映异构体。 通过配置对映选择性反转获得的相应的S-醇和R-醇导致脑血流量的增加。
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5.发明授权Rhodotorula rubra useful in a process for the preparation of (.omega.-1)-hydroxyalkylxanthines 失效Rhodotorula rubra可用于制备（ω-1） - 羟基烷基黄嘌呤的方法
公开(公告)号：US5472873A
公开(公告)日：1995-12-05
申请号：US194563
申请日：1994-02-10
IPC分类号： A61K31/52 , A61K31/522 , A61P9/00 , C07B37/10 , C07D473/04 , C07D473/06 , C07D473/08 , C07D473/10 , C12N1/16 , C12P17/18 , C12P41/00 , C12R1/645
CPC分类号： C12P41/002 , C07D473/06 , C07D473/08 , C07D473/10 , C12P17/18 , Y10S435/822 , Y10S435/911
摘要： A Rhodotorula rubra strain has been found which reduces pentoxifylline to 100% to give the S-alcohol. Moreover, other oxoalkylxanthine derivatives can also be converted into the corresponding S-alcohol. The microbiologically obtained S-(+)-enantiomers can then be converted stereo-selectively into the respective R-(-)-enantiomers. The corresponding S-alcohols and the R-alcohols obtained by enantioselective inversion of configuration cause an increase in cerebral blood flow.
摘要翻译： 已经发现红酵母菌株将己酮可可碱降至100％以得到S-醇。 此外，其它氧代烷基黄嘌呤衍生物也可以转化为相应的S-醇。 然后将微生物获得的S - （+） - 对映异构体立体选择性转化成相应的R - （ - ） - 对映体。 通过配置对映选择性反转获得的相应的S-醇和R-醇导致脑血流量的增加。
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6.发明授权公开(公告)号：US06214992B1
公开(公告)日：2001-04-10
申请号：US08868641
申请日：1997-06-04
申请人： Ulrich Gebert , Erhard Wolf , Elisabeth Defossa , Uwe Heinelt , Hiristo Anagnostopulos , Karl Rudolphi , John J. Grome
发明人： Ulrich Gebert , Erhard Wolf , Elisabeth Defossa , Uwe Heinelt , Hiristo Anagnostopulos , Karl Rudolphi , John J. Grome
IPC分类号： A61K3152
CPC分类号： C07D473/06
摘要： Theophylline derivatives having at least one ether function in the structurally modified methyl radical in the 1-position that are useful in the treatment and prophylaxis of states of shock, new xanthine compounds having this substitution pattern, and processes for their preparation.
摘要翻译： 在1位结构改性的甲基基团中具有至少一个醚功能的茶碱衍生物可用于治疗和预防休克状态，具有该取代模式的新的黄嘌呤化合物及其制备方法。
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7.发明授权Use of antibodies to TNF or fragments derived thereof and xanthine derivatives for combination therapy and compositions therefor 失效使用TNF抗体或衍生自其的片段和黄嘌呤衍生物进行组合治疗及其组合物
公开(公告)号：US5958413A
公开(公告)日：1999-09-28
申请号：US966544
申请日：1997-11-10
申请人： Hiristo Anagnostopulos , Ulrich Gebert , Heinz Hanel , Michael Limbert , Mark William Bodmer , Gerald Anthony Higgs
发明人： Hiristo Anagnostopulos , Ulrich Gebert , Heinz Hanel , Michael Limbert , Mark William Bodmer , Gerald Anthony Higgs
CPC分类号： C07K16/241 , A61K39/395 , A61K2039/505 , Y10S514/929
摘要： A combined preparation for simultaneous combined, simultaneous separate, or sequential use in the therapy of prophylaxis of disorders associated with undesirable high levels of TNF, e.g. septic or endotoxic shock and immunoregulatory and inflammatory disorders, which comprises an antibody to TNF or a TNF binding fragment thereof and a xanthine derivative. Particular preferred xanthine derivatives are 3,7-dimethyl-1(5-oxo-hexyl)xanthine (known as Pentoxifylline or TRENTAL) and 1-(5-hydroxy-5-methylhexyl)-3-methylxanthine and similar compounds. The anti-TNF antibody or fragment is preferably monospecific especially a humanized recombinant antibody or fragment.
摘要翻译： 用于同时联合，同时分离或顺序使用的治疗预防与不期望的高水平TNF相关的疾病的组合制剂，例如。 脓毒性或内毒素性休克和免疫调节性和炎症性疾病，其包含TNF抗体或其TNF结合片段和黄嘌呤衍生物。 特别优选的黄嘌呤衍生物是3,7-二甲基-1（5-氧代 - 己基）黄嘌呤（称为己酮可可碱或TRENTAL）和1-（5-羟基-5-甲基己基）-3-甲基黄嘌呤和类似化合物。 抗TNF抗体或片段优选是单特异性的，特别是人源化的重组抗体或片段。
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公开(公告)号：US4216216A
公开(公告)日：1980-08-05
申请号：US915899
申请日：1978-06-15
IPC分类号： A61K31/495 , A61K31/505 , A61P25/04 , A61P43/00 , C07D239/22 , C07D239/54 , C07D239/56 , C07D295/13 , C07D401/06 , C07D403/06
CPC分类号： C07D239/22 , C07D295/13
摘要： Compounds of general formula ##STR1## are disclosed wherein appropriate substituents for R.sup.1, R.sup.2 to R.sup.5, R.sup.6, A, Q, X, and Z are defined for these novel hexahydropyrimidines. Procedures for the preparation of these compounds are also given. Because of the highly effective serotonin antagonistic activity in combination with a strong inhibiting effect on thrombocyte aggregation and good compatibility these compounds are effective in treating migraine. Additionally, the compounds also exhibit an anti-histamine activity, cause an increase in erythrocyte fluidity, a psychotropic activity, a weak bradykinin antagonism and hypotensive effects.
摘要翻译： 公开了通式“IMAGE”的化合物，其中适用于R1，R2至R5，R6，A，Q，X和Z的取代基用于这些新的六氢嘧啶。 还给出了这些化合物的制备方法。 由于高度有效的5-羟色胺拮抗活性与对血栓细胞聚集的强抑制作用以及良好的相容性，这些化合物在治疗偏头痛方面是有效的。 此外，化合物还表现出抗组胺活性，导致红细胞流动性增加，精神活性，弱缓激肽拮抗作用和降血压作用。
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9.发明授权Therapeutic xanthine derivatives for the treatment of peptic ulcer disease 失效用于治疗胃泌素疾病的治疗性Xanthine衍生物
公开(公告)号：US5082845A
公开(公告)日：1992-01-21
申请号：US311910
申请日：1989-02-17
申请人： Erhard Wolf , Ulrich Gebert , Harald Furrer , Toshizo Tanaka , Masao Sakurai , Masayoshi Goto
发明人： Erhard Wolf , Ulrich Gebert , Harald Furrer , Toshizo Tanaka , Masao Sakurai , Masayoshi Goto
IPC分类号： A61K31/52 , A61K31/522 , A61P1/04 , C07D473/04 , C07D473/06
CPC分类号： A61K31/52 , C07D473/04 , C07D473/06
摘要： Therapeutic agents for the treatment of peptic ulcer disease, containing as active ingredient, at least one compound of the general formula ##STR1## wherein R.sup.1 and R.sup.3 are the same or different and are each (C.sub.1 -C.sub.8)alkyl, ##STR2## R.sup.2 is (C.sub.1 -C.sub.4)alkyl; R.sup.4 and R.sup.5 are the same or different and are each hydrogen or (C.sub.1 -C.sub.2)alkyl; R.sup.6 is (C.sub.1 -C.sub.2)alkyl; and m, n and p are the same or different and are each 1, 2, 3, 4, 5 or 6; with the proviso that one of the groups R.sup.1 and R.sup.3 is ##STR3## or that R.sup.3 represents ##STR4## Some of the compounds of formula I are novel.
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10.发明授权R-(-)-1-(5-hydroxyhexyl)-3-methyl-7-propylxanthine, a process for its preparation and pharmaceuticals containing this compound 失效R - （ - ） - 1-（5-羟基己基）-3-甲基-7-丙基黄嘌呤，其制备方法和含该化合物的药物
公开(公告)号：US5407815A
公开(公告)日：1995-04-18
申请号：US631415
申请日：1990-12-21
申请人： Harald Furrer , Ulrich Gebert , Karl Rudolphi
发明人： Harald Furrer , Ulrich Gebert , Karl Rudolphi
IPC分类号： A61K31/52 , A61K31/522 , A61P9/08 , C07D473/04 , C07D473/06 , C12P17/18 , C12P41/00 , C12R1/865
CPC分类号： C07D473/04 , C12P17/182
摘要： R-(-)-1-(5-Hydroxyhexyl)-3-methyl-7-propylxanthine, a process for its preparation, and pharmaceuticals which contain this compound and which are suitable, in particular, for the prophylaxis and treatment of cerebral vascular disorders.
摘要翻译： R - （ - ） - 1-（5-羟基己基）-3-甲基-7-丙基黄嘌呤，其制备方法和含有该化合物的药物，特别适用于预防和治疗脑血管 疾病
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