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41. 发明授权

US5446035A 20-methyl-substituted vitamin D derivatives 失效
标题翻译： 20-甲基取代的维生素D衍生物
公开(公告)号：US5446035A
公开(公告)日：1995-08-29
申请号：US307081
申请日：1994-09-16
申请人： Gunter Neef , Andreas Steinmeyer , Gerald Kirsch , Katica Schwarz , Ruth Thieroff-Ekerdt , Herbert Wiesinger , Martin Haberey
发明人： Gunter Neef , Andreas Steinmeyer , Gerald Kirsch , Katica Schwarz , Ruth Thieroff-Ekerdt , Herbert Wiesinger , Martin Haberey
IPC分类号： A61K31/59 , A61P3/02 , A61P3/14 , A61P17/00 , A61P35/02 , A61P37/00 , A61P43/00 , C07C401/00
CPC分类号： C07C401/00
摘要： New 20-methyl-substituted vitamin D derivatives of general formula I ##STR1## are described in whichR.sup.1 means a hydrogen atom, a hydroxy group or an alkanoyloxy group with 1 to 12 carbon atoms or a benzoyloxy group,R.sup.2 means a hydrogen atom or an alkanoyl group with 1 to 12 carbon atoms or a benzoyl group andR.sup.3 means a saturated or unsaturated, straight-chain or branched hydrocarbon radical with up to 18 C atoms, which optionally contains carbocyclic structures, optionally substituted with one or more hydroxy, oxo, amino group(s) and/or one or more halogen atom(s) as well as optionally exhibits one or more oxygen, sulfur and/or nitrogen atom(s) as a bridging link or links in the hydrocarbon radical, and a process for their production.Relative to calcitriol, the new compounds exhibit a greatly improved induction of cell differentiation (HL-60) and are suitable for the production of pharmaceutical agents.
摘要翻译：描述了通式I的新的20-甲基取代的维生素D衍生物（I），其中R 1表示氢原子，羟基或具有1至12个碳原子的烷酰氧基或苯甲酰氧基，R2表示氢原子或具有1至12个碳原子的烷酰基或苯甲酰基，R 3表示具有至多18个C原子的饱和或不饱和的直链或支链烃基，其任选地含有碳环结构，任选地被一个或多个羟基，氧代，氨基和/或一个或多个卤素原子，以及任选地表现出一个或多个氧，硫和/或氮原子作为烃基中的桥连或连接，及其生产过程。相对于骨化三醇，新化合物表现出极大改善的细胞分化诱导（HL-60），适用于制药。

42. 发明授权

US4868166A 2,2:6,6-diethylen-3-oxo-17alpha-pregn-4-ene-21,17alpha-carbolactones, process for their production & pharmaceutical preparations containing them 失效
标题翻译： 2,2,6,6-二乙基-3-氧代-17α-孕-4-烯-21,17α-卡宾内酯，其制备方法和含有它们的药物制剂
公开(公告)号：US4868166A
公开(公告)日：1989-09-19
申请号：US150413
申请日：1988-02-05
申请人： Dieter Bittler , Klaus Nickisch , Henry Laurent , Rudolf Wiechert , Martin Haberey
发明人： Dieter Bittler , Klaus Nickisch , Henry Laurent , Rudolf Wiechert , Martin Haberey
IPC分类号： A61K31/57 , C07J1/00 , C07J53/00
CPC分类号： C07J53/001 , C07J53/008
摘要： 2,2;6,6-diethylene-3-oxo-17alpha-pregn-4-ene-21,17-carbolactones of general formula I, ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group,R.sub.2 represents a methyl or ethyl group and ##STR2## process for their production and their pharmaceutical use.
摘要翻译： PCT No.PCT / DE87 / 00208 Sec。 371日期1988年2月5日 102（e）日期1988年2月5日PCT提交1987年5月5日PCT公布。出版物WO87 / 06937 1987年11月19日2.2.1通式I的6,6-二亚乙基-3-氧代-17α-孕-4-烯-21,17-碳内酯，其中R1表示氢原子或甲基，R2代表甲基或乙基和它们的制备方法及其药物用途。

43. 发明授权

US06642218B2 Vitamin D derivatives with carbo- or heterocyclic substituents at C-25, a process for their production, intermediate products and their use for producing medicaments 失效
标题翻译：在C-25具有碳或杂环取代基的维生素D衍生物，其生产方法，中间产物及其用于生产药物的用途
公开(公告)号：US06642218B2
公开(公告)日：2003-11-04
申请号：US09180018
申请日：1998-12-11
申请人： Andreas Steinmeyer , Gerald Kirsch , Günter Neef , Katica Schwarz , Ruth Thieroff-Ekerdt , Herbert Wiesinger , Martin Haberey , Marianne Fahnrich
发明人： Andreas Steinmeyer , Gerald Kirsch , Günter Neef , Katica Schwarz , Ruth Thieroff-Ekerdt , Herbert Wiesinger , Martin Haberey , Marianne Fahnrich
IPC分类号： A61K3159
CPC分类号： C07D207/333 , C07C35/32 , C07C401/00 , C07D233/64 , C07D263/32 , C07D271/06 , C07D271/10 , C07D277/24 , C07D307/42 , C07D333/16
摘要： The invention relates to vitamin D derivatives of formula (I), processes for the production thereof and uses thereof: wherein Y1, Y2, R1-R6, Q and Z are as defined herein.
摘要翻译：本发明涉及式（I）的维生素D衍生物，其制备方法及其用途：其中Y1，Y2，R1-R6，Q和Z如本文所定义。

44. 发明授权

US06531459B1 Vitamin D derivatives with phosphorus atoms in the side chains 失效
标题翻译：维生素D衍生物与侧链中的磷原子
公开(公告)号：US06531459B1
公开(公告)日：2003-03-11
申请号：US09581907
申请日：2000-08-04
申请人： Andreas Steinmeyer , Günter Neef , Gerald Kirsch , Katica Schwarz , Herbert Wiesinger , Martin Haberey , Marianne Fähnrich , Gernot Langer
发明人： Andreas Steinmeyer , Günter Neef , Gerald Kirsch , Katica Schwarz , Herbert Wiesinger , Martin Haberey , Marianne Fähnrich , Gernot Langer
IPC分类号： A61K3159
CPC分类号： C07C401/00 , C07F9/383 , C07F9/386 , C07F9/4018 , C07F9/404 , C07F9/405 , C07F9/532
摘要： Described are new vitamin D derivatives such as of the formula (I) detailed in this disclosure. Also described are methods for preparing these derivatives, inter mediates used to prepare the derivatives and use of the derivatives as pharmaceutical agents.
摘要翻译：描述了新的维生素D衍生物，例如本公开中详述的式（I）。还描述了制备这些衍生物的方法，用于制备衍生物的中间体和作为药剂的衍生物的用途。

45. 发明授权

US5583125A 25-Carboxylic acid derivatives in the vitamin D series, process for their production, intermediate products for these processes, pharmaceutical preparations containing these derivatives as well as their use for the production of pharmaceutical agents 失效
标题翻译：维生素D系列中的25-羧酸衍生物，其制备方法，用于这些方法的中间产物，含有这些衍生物的药物制剂及其制备药剂的用途
公开(公告)号：US5583125A
公开(公告)日：1996-12-10
申请号：US132176
申请日：1993-10-06
申请人： Andreas Steinmeyer , G unter Neef , Gerald Kirsch , Katica Schwarz , Ruth Thieroff-Ekerdt , Herbert Wiesinger , Martin Haberey
发明人： Andreas Steinmeyer , G unter Neef , Gerald Kirsch , Katica Schwarz , Ruth Thieroff-Ekerdt , Herbert Wiesinger , Martin Haberey
IPC分类号： A61K31/59 , A61P3/02 , A61P3/08 , A61P11/00 , A61P17/00 , A61P31/12 , A61P35/00 , A61P37/00 , A61P37/04 , A61P43/00 , C07C401/00
CPC分类号： C07C401/00
摘要： New 25-carboxylic acid derivatives of general formula I, ##STR1## R.sup.19 and R.sup.19a each mean a hydrogen atom or together form an exocyclic methylene group,R.sup.21 and R.sup.21a independently of one another mean a hydrogen atom, a chlorine or fluorine atom, an alkyl group with 1 to 4 carbon atoms, together a methylene group, together with quaternary carbon atom 20 mean a 3-7 membered, saturated or unsaturated carboxylic ring,Y preferably means a derivatized carboxyl radical, and the other substituents have the meanings indicated in the description as well as process for their production, are described.The new compounds have vitamin D activity as well as proliferation-inhibiting and cell-differentiating effects and are suitable for the production of pharmaceutical agents.
摘要翻译：通式I，（I）R 19和R 19a的新的25-羧酸衍生物各自表示氢原子或一起形成环外亚甲基，R 21和R 21a彼此独立地表示氢原子，氯或氟原子，具有1至4个碳原子的烷基，一起亚甲基与季碳原子20一起表示3-7元饱和或不饱和羧基，Y优选是衍生化的羧基，其它取代基具有以下含义：在描述中指出了它们的生产过程。新化合物具有维生素D活性以及增殖抑制和细胞分化作用，适用于制药。

46. 发明授权

US5411949A 23-oxa-derivatives in the vitamin D series, process for their production, pharmaceutical preparations containing these derivatives as well as their use pharmaceutical agents 失效
标题翻译：维生素D系列中的23-氧杂衍生物，其制备方法，含有这些衍生物的药物制剂及其用途药剂
公开(公告)号：US5411949A
公开(公告)日：1995-05-02
申请号：US90201
申请日：1993-07-19
申请人： Gunter Neef , Andreas Steinmeyer , Gerald Kirsch , Katica Schwarz , Martin Haberey , Ruth Thieroff-Ekerdt , Petra Rach
发明人： Gunter Neef , Andreas Steinmeyer , Gerald Kirsch , Katica Schwarz , Martin Haberey , Ruth Thieroff-Ekerdt , Petra Rach
IPC分类号： A61K31/59 , A61P17/00 , A61P35/00 , C07C401/00
CPC分类号： C07C401/00
摘要： 23-Oxa-derivatives in the vitamin D series of formula I ##STR1## are described in which R.sup.1, R.sup.2 and R.sup.4 independently of one another mean a hydrogen atom or an acyl group with 1 to 9 carbon atoms,R.sup.3 each means a hydrogen atom or each a linear or branched alkyl group with 1 to 4 carbon atoms and X means an alkylene radical--(CH.sub.2).sub.n -- with n=1, 2, 3, and if n=1, R.sup.3 each cannot be a methyl or propyl group, as well as a process for their production.The compounds have proliferation-inhibiting and cell-differentiation effects and are suitable for the production of pharmaceutical agents.
摘要翻译： PCT No.PCT / EP92 / 00123 Sec。 371日期：1993年7月19日 102（e）日期1993年7月19日PCT提交1992年1月20日PCT公布。公开号WO92 / 12963 日期1992年8月6日23.描述了式I的维生素D系列中的氧化衍生物，其中R1，R2和R4彼此独立地表示氢原子或具有1至9个碳原子的酰基原子，R3各自表示氢原子或每个具有1至4个碳原子的直链或支链烷基，X表示具有n = 1,2,3的亚烷基 - （CH 2）n - ，如果n = 1，R 3 每个不能是甲基或丙基，以及它们的生产过程。这些化合物具有增殖抑制和细胞分化作用，并且适用于制药。

47. 发明授权

US5190973A 20-alkyl-7-oxoprostacyclin derivatives useful as pharmaceuticals 失效
标题翻译：可用作药物的20-烷基-7-氧代前列环素衍生物
公开(公告)号：US5190973A
公开(公告)日：1993-03-02
申请号：US599916
申请日：1990-10-19
申请人： Robert Nickolson , Helmut Vorbrueggen , Claus S. Stuerzebecher , Martin Haberey
发明人： Robert Nickolson , Helmut Vorbrueggen , Claus S. Stuerzebecher , Martin Haberey
IPC分类号： C07C405/00 , C07D307/935 , C07D307/937
CPC分类号： C07D307/935 , C07C405/00 , C07D307/937
摘要： The invention concerns 20-alkyl-7-oxoprostacyclin derivatives of general Formula I ##STR1## wherein R.sub.1 is the residue OR.sub.3 where R.sub.3 means hydrogen or alkyl of 1-10 carbon atoms optionally substituted by halogen, phenyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -dialkylamino; cycloalkyl, aryl or a heterocyclic residue, or the residue NHR.sub.4 where R.sub.4 means hydrogen or an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms,n is 1 or 2,A is a CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH-- or trans--CH.dbd.CH--group,W is a ##STR2## or a ##STR3## wherein the OH-group can respectively be esterified with a benzoyl or alkanoic acid residue of 1-4 carbon atoms, or etherified with a tetrahydropyranol, tetrahydrofuranyl, alkoxyalkyl or trialkylsilyl residue, wherein the free or esterified OH-group can be in the .alpha.- or .beta.-position,R.sub.2 is a straight-chain or branched-chain alkyl group of 1-6 carbon atoms,R.sub.5 is a hydroxy group which can be esterified with an alkanoic acid residue of 1-4 carbon atoms or etherified with a tetrahydropyranyl, tetrahydrofuranyl, alkoxyalkyl or trialkylsilyl residue,R.sub.6 and R.sub.7 are hydrogen or a straight-chain or branched-chain alkyl group of 1-4 carbon atoms, or R.sub.6 and R.sub.7 jointly represent a trimethylene group,R.sub.8 and R.sub.9 jointly represent a linkage or hydrogen or a straight-chain or branched-chain alkyl group of 1-4 carbon atoms,and, if R.sub.3 is hydrogen, the salts thereof with physiologically compatible bases; their production; and their use as medicinal agents.
摘要翻译：本发明涉及通式I（I）的20-烷基-7-氧代前列环素衍生物，其中R 1是残基OR 3，其中R 3表示氢或1-10个碳原子的任选被卤素，苯基，C 1 -C 4 - 烷氧基或C 1 -C 4 - 二烷基氨基; 环烷基，芳基或杂环残基，或残基NHR4，其中R4表示氢或分别为1-10个碳原子的烷酰基或烷磺酰基，n为1或2，A为CH2-CH2-，顺式-CH = CH- 或反式-CH = CH-基团，W为“IMAGE”或“IMAGE”，其中OH基团可分别用1-4个碳原子的苯甲酰基或链烷酸残基酯化，或用四氢吡喃醇醚化，四氢呋喃基，烷氧基烷基或三烷基甲硅烷基残基，其中游离或酯化的OH基可以是α或β-位，R2是1-6个碳原子的直链或支链烷基，R5是羟基，可以用1-4个碳原子的链烷酸残基酯化，或与四氢吡喃基，四氢呋喃基，烷氧基烷基或三烷基甲硅烷基残基醚化，R6和R7是氢或1-4个碳原子的直链或支链烷基，或R6和R7共同表示三亚甲基，R8和R9共同表示键或氢或1-4个碳原子的直链或支链烷基，如果R 3是氢，则其与生理上相容的碱的盐; 他们的生产; 并将其用作药剂。

48. 发明授权

US5190964A 5-fluorocarbacyclins, their preparation and pharmaceutical use 失效
标题翻译： 5-氟卡巴环素，其制备和药物用途
公开(公告)号：US5190964A
公开(公告)日：1993-03-02
申请号：US480448
申请日：1990-02-15
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Martin Haberey , Claus-Steffen Sturzebecher , Michael-Harold Town
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Martin Haberey , Claus-Steffen Sturzebecher , Michael-Harold Town
IPC分类号： C07C405/00 , C07D263/14
CPC分类号： C07D263/14 , C07C405/0083
摘要： 5-fluorocarbacyclin derivatives of the Formula I ##STR1## wherein R.sub.1 is CH.sub.2 OH orA is --CH.sub.2 --CH.sub.2 --, trans --CH.dbd.CH-- or --C.tbd.C--,W is a free or functionally modified hydroxymethylene group or free or functionally modified ##STR2## in which the OH group can be in the .alpha.-- or .beta.-position, D is ##STR3## a C.sub.1-10 -aliphatic group (e.g., alkyl or alkenyl) which optionally can be substituted by fluorine atoms,n is 1, 2 or 3,E is a direct bond, --C.tbd.C-- or --CR.sub.6 .tbd.CR.sub.7 -- in which R.sub.6 represents a hydrogen atom or an alkyl group with 1-5 atoms and R.sub.7 represents a hydrogen atom, a halogen atom or an alkyl group with 1-5 C atoms,R.sub.4 is alkyl, cycloalkyl or optionally substituted aryl or a heterocyclic group,R.sub.5 is a free or functionally modified hydroxy groupand, when R.sub.2 is a hydrogen atom, its salts with physiologically compatible bases,have valuable pharmacological properties.
摘要翻译：其中R 1是CH 2 OH或A是-CH 2 -CH 2 - ，反式-CH = CH-或-CB 3 C，其中W是游离的或官能改性的羟基亚甲基，或游离或官能改性的羟基亚甲基，官能改性的“IMAGE”，其中OH基团可以是α或β-位，D是可任选被氟原子取代的C 1-10脂族基团（例如烷基或烯基），n 是1,2或3，E是直接键，-C 3 D或-CR 6 3BOND CR 7 - ，其中R 6表示氢原子或具有1-5个原子的烷基，R 7表示氢原子，卤素原子或具有1-5个C原子的烷基，R4是烷基，环烷基或任选取代的芳基或杂环基，R5是游离或官能改性的羟基，当R2是氢原子时，其与生理上相容的碱的盐，具有宝贵的药理性质。

49. 发明授权

US07115758B2 Vitamin D derivatives with cyclic substructures in the side chains, process and intermediate products for their production, and the use for the production of pharmaceutical agents 失效
标题翻译：侧链中具有循环亚结构的维生素D衍生物，用于其生产的方法和中间产物，以及用于生产药剂的用途
公开(公告)号：US07115758B2
公开(公告)日：2006-10-03
申请号：US10303916
申请日：2002-11-26
申请人： Andreas Steinmeyer , Katica Schwarz , Claudia Giesen , Martin Haberey , Marianne Fähnrich
发明人： Andreas Steinmeyer , Katica Schwarz , Claudia Giesen , Martin Haberey , Marianne Fähnrich
IPC分类号： A61K31/59 , C07C401/00 , C07C403/00
CPC分类号： B21C25/10 , B21C25/02 , C07C401/00 , C07D235/12 , C07D263/32 , C07D277/24 , C07D307/80 , C07D333/16 , C07D333/22 , Y02P20/55
摘要： The invention relates to vitamin D derivatives of general formula I, process for their production, intermediate products of the process as well as the use for the production of pharmaceutical agents.
摘要翻译：本发明涉及通式I的维生素D衍生物，其制备方法，该方法的中间产物以及用于生产药剂的用途。

50. 发明申请

US20050227951A1 Verification of translation 审中-公开
标题翻译：验证翻译
公开(公告)号：US20050227951A1
公开(公告)日：2005-10-13
申请号：US11141060
申请日：2005-06-01
申请人： Andreas Steinmeyer , Gunter Neef , Gerald Kirsch , Katica Schwarz , Herbert Wiesinger , Martin Haberey , Marianne Fahnrich , Gernot Langer
发明人： Andreas Steinmeyer , Gunter Neef , Gerald Kirsch , Katica Schwarz , Herbert Wiesinger , Martin Haberey , Marianne Fahnrich , Gernot Langer
IPC分类号： C07D317/20 , A61K31/59 , A61K31/593 , A61K38/13 , A61K39/395 , A61P3/02 , A61P3/10 , A61P3/14 , A61P9/10 , A61P11/06 , A61P15/16 , A61P15/18 , A61P17/04 , A61P17/14 , A61P19/02 , A61P19/08 , A61P19/10 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/04 , C07C47/293 , C07C401/00 , C07D317/26 , C07D319/06
CPC分类号： C07C401/00 , A61K31/59 , A61K38/13 , A61K39/395 , A61K31/445 , A61K31/435 , A61K2300/00
摘要： The invention relates to new vitamin D derivatives of general formula (I), process for their production, intermediate products of the process as well as the use for production of pharmaceutical agents.
摘要翻译：本发明涉及通式（I）的新维生素D衍生物，其生产方法，该方法的中间产物以及制药用途的用途。

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