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1. 发明授权

US06288249B1 Vitamin D analogs and methods of preparing these compounds 失效
标题翻译：维生素D类似物和制备这些化合物的方法
公开(公告)号：US06288249B1
公开(公告)日：2001-09-11
申请号：US09180136
申请日：1999-06-16
申请人： Sebastianus J. Halkes , Jan Paul Van De Velde , Silvia Kanzler , Wolfgang Reischl
发明人： Sebastianus J. Halkes , Jan Paul Van De Velde , Silvia Kanzler , Wolfgang Reischl
IPC分类号： C07C40100
CPC分类号： C07C33/38 , C07C2602/08
摘要： The invention relates to vitamin D analogs of general formula (I) wherein: R1 is a hydrogen atom or a substituent selected from the group consisting of hydroxy, CH2OH, CH2CH2OH, CH2CH2CH2OH, OCH3, OCH2OH, OCH2CH2OH and OCH2CH2CH2OH; R2 is a hydrogen atom or a substituent selected from the group consisting of OCH3, OCH2OH, CHm(CH2OH)n(CH2CH2OH)p, (CH2)qOH and O(CH2)rOH; wherein: m is 0 or 1, p, q and n are 0-3, r is 1-3 and m+n+p=3; with the proviso that R1 and/or R2 contain at least one OH group; R3 is a straight or branched, saturated or unsaturated aliphatic hydrocarbon of 6-13 C atoms which may be substituted with one or more substituents from the group hydroxy or fluoro. The invention further relates to methods of preparing these compounds, a pharmaceutical composition containing these compounds and to their use in pharmacotherapy and cosmetics.
摘要翻译：本发明涉及通式（I）的维生素D类似物，其中：R 1是氢原子或选自羟基，CH 2 OH，CH 2 CH 2 OH，CH 2 CH 2 CH 2 OH，OCH 3，OCH 2 OH，OCH 2 CH 2 OH和OCH 2 CH 2 CH 2 OH的取代基; R2是氢原子或选自OCH3，OCH2OH，CHm（CH2OH）n（CH2CH2OH）p，（CH2）qOH和O（CH2）rOH的取代基; 其中：m为0或1，p，q和n为0-3，r为1-3，m + n + p = 3; 条件是R1和/或R2含有至少一个OH基团; R3是6-13个碳原子的直链或支链饱和或不饱和脂族烃基，其可被一个或多个羟基或氟取代基取代。本发明还涉及制备这些化合物的方法，含有这些化合物的药物组合物及其在药物治疗和化妆品中的用途。

2. 发明授权

US6075015A Vitamin D compounds and method of preparing these compounds 失效
标题翻译：维生素D化合物及其制备方法
公开(公告)号：US6075015A
公开(公告)日：2000-06-13
申请号：US863947
申请日：1997-05-27
申请人： Jose P. Sestelo , Antonio Mourino , Jose L. Mascarenas , Sebastianus J. Halkes , Jan Zorgdrager , Gerhardus D. H. Dijkstra , Jan-Paul van de Velde
发明人： Jose P. Sestelo , Antonio Mourino , Jose L. Mascarenas , Sebastianus J. Halkes , Jan Zorgdrager , Gerhardus D. H. Dijkstra , Jan-Paul van de Velde
IPC分类号： C07C35/32 , C07C45/29 , C07C49/477 , C07C49/513 , C07C401/00 , A61K31/59
CPC分类号： C07C401/00 , C07C35/32 , C07C45/292 , C07C49/477 , C07C49/513 , Y10S514/861 , Y10S514/863
摘要： Vitamin D.sub.3 analogues of the formula (I): ##STR1## wherein R.sub.1 is hydrogen or hydroxy, R.sub.2 is (C.sub.1 -C.sub.3)alkyl, hydroxy(C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.2)alkoxymethyl, (C.sub.2 -C.sub.3)alkenyl, or (C.sub.2 -C.sub.3)alkynyl, R.sub.3 is a branched or unbranched, saturated or unsaturated aliphatic 3- to 5- membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy, R.sub.4 is sec. or tert. (C.sub.3 -C.sub.6)alkyl or (C.sub.3 -C.sub.6)cycloalkyl, A and B are each individually hydrogen or methyl, or A and B together from methylene. The compounds of the present invention exhibit pharmacotherapeutic activities, including in particular, the treatment of osteoporosis, renal osteodystrophy, osteomalacia, skin disorders such as psoriasis and other hyperproliferative skin diseases, eczema and dermatitis, nmyopathy, leukemia, breast and colon cancer, osteosarcomas, squamous cell carcinomas, melanoma, certain immunological disorders, and transplant rejections. Several methods of synthesis, including reaction of an ester compound of general formula (IX) with an inorganometallic compound of formula (III) followed by deprotection or, alternatively, first finalization of the C.sub.17 -side chain are also disclosed.
摘要翻译：式（I）的维生素D3类似物：其中R1是氢或羟基，R2是（C1-C3）烷基，羟基（C1-C3）烷基，（C1-C2）烷氧基甲基，（C2-C3）烯基或（ C 2 -C 3）炔基，R 3是支链或非支链的饱和或不饱和的脂族3-至5-元烃基或氧杂烃双基，在主链中具有至少3个原子，并且任选地被一个或多个选自环氧基，氟和羟基，R4是秒。或叔。（C 3 -C 6）烷基或（C 3 -C 6）环烷基，A和B各自独立地为氢或甲基，或A和B一起为亚甲基。本发明的化合物具有药物治疗活性，特别包括治疗骨质疏松症，肾性骨营养不良，骨软化症，皮肤疾病如牛皮癣和其它过度增生性皮肤病，湿疹和皮炎，纳米病，白血病，乳腺和结肠癌，骨肉瘤，鳞状细胞癌，黑素瘤，某些免疫性疾病和移植排斥。还公开了几种合成方法，包括通式（IX）的酯化合物与式（III）的无机金属化合物反应，然后进行脱保护，或者也可以首先终止C17-侧链。

3. 发明授权

US5449668A Vitamin D compounds and method of preparing these compounds 失效
标题翻译：维生素D化合物及其制备方法
公开(公告)号：US5449668A
公开(公告)日：1995-09-12
申请号：US70998
申请日：1993-06-04
申请人： Jose P. Sestelo , Antonio Mourino , Jose L. Mascarenas , Sebastianus J. Halkes , Jan Zorgdrager , Gerhardus D. H. Dijkstra , Jan-Paul van de Velde
发明人： Jose P. Sestelo , Antonio Mourino , Jose L. Mascarenas , Sebastianus J. Halkes , Jan Zorgdrager , Gerhardus D. H. Dijkstra , Jan-Paul van de Velde
IPC分类号： C07C35/32 , C07C45/29 , C07C49/477 , C07C49/513 , C07C401/00 , A61K31/24 , A61K31/205
CPC分类号： C07C401/00 , C07C35/32 , C07C45/292 , C07C49/477 , C07C49/513 , Y10S514/861 , Y10S514/863
摘要： The invention relates to a new vitamin D compound of the general formula ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group;R.sub.2 is a (C.sub.1 -C.sub.3)alkyl group, a hydroxy(C.sub.1 -C.sub.3)alkyl group, a (C.sub.1 -C.sub.2)alkoxymethyl group or a (C.sub.2 -C.sub.3)alkenyl or alkynyl group;R.sub.3 is a branched or non-branched, saturated or unsaturated aliphatic 3- to 5 -membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy;R.sub.4 is a sec. or tert. (C.sub.3 -C.sub.6)alkyl group or a (C.sub.3 -C.sub.6)cycloalkyl group; andA and B are each individually hydrogen atoms or methyl groups, orA and B form together a methylene group.The invention further relates to a method of preparing these compounds and to their use in pharmacotherapy and cosmetics.
摘要翻译：本发明涉及通式（I）的新的维生素D化合物，其中：R1是氢原子或羟基; R2是（C1-C3）烷基，羟基（C1-C3）烷基，（C1-C2）烷氧基甲基或（C2-C3）烯基或炔基; R3是在主链中具有至少3个原子且任选地被一个或多个选自环氧基，氟和羟基的取代基取代的支化或非支化的饱和或不饱和脂族3-至5-元烃或二烃基双基。 R4是秒或叔。（C 3 -C 6）烷基或（C 3 -C 6）环烷基; A和B各自为氢原子或甲基，或A和B一起形成亚甲基。本发明还涉及这些化合物的制备方法及其在药物治疗和化妆品中的应用。

4. 发明授权

US5395953A Method of preparing hydrindane compounds and hydrindane-related compounds 失效
标题翻译：制备氢化茚烃化合物和氢化茚相关化合物的方法
公开(公告)号：US5395953A
公开(公告)日：1995-03-07
申请号：US109708
申请日：1993-08-20
申请人： Miguel A. Maestro , Antonio Mourino , Benjamin Borsje , Sebastianus J. Halkes
发明人： Miguel A. Maestro , Antonio Mourino , Benjamin Borsje , Sebastianus J. Halkes
IPC分类号： C07C45/29 , C07C45/64 , C07C49/513 , C07J9/00 , C07J75/00 , A01M43/04
CPC分类号： C07J9/00 , C07C45/29 , C07C45/64 , C07C49/513
摘要： The invention relates to a method of preparing a compound having an alkyl or alkoxyalkyl side-chain with a terminal 2-hydroxyprop-2-yl group, by oxidizing a compound having a terminal isopropyl group in its side-chain with a dioxirane as the oxidant.
摘要翻译：本发明涉及一种通过用二环氧乙烷作为氧化剂氧化其侧链具有末端异丙基的化合物来制备具有末端2-羟基丙-2-基的具有烷基或烷氧基烷基侧链的化合物的方法。

5. 发明授权

US5175217A Method for the photochemical conversion of tachysterol compounds into previtamin D compounds and of trans-vitamin D compounds into cis-vitamin D compounds using a polymeric photoinitiator 失效
标题翻译：使用聚合物光引发剂将快速组合物化合物转化为前维生素D化合物和反式维生素D化合物转化为顺式维生素D化合物的方法
公开(公告)号：US5175217A
公开(公告)日：1992-12-29
申请号：US571415
申请日：1990-08-23
申请人： Eric Goethals , Sebastianus J. Halkes , Robert B. Koolstra
发明人： Eric Goethals , Sebastianus J. Halkes , Robert B. Koolstra
IPC分类号： C07C401/00 , C08F8/00 , C08G65/333 , C08G65/337 , C08G73/04
CPC分类号： C08G65/333 , C07C401/00 , C08F8/00 , C08G65/337
摘要： The invention relates to a method for the photochemical conversion of tachysterol compounds into previtamin D compounds and of trans-vitamin D compounds into cis-vitamin D compounds under the influence of radiation, by exposing the tachysterol compound and trans-vitamin D compound, respectively, dissolved in a suitable solvent system, in the presence of a polymeric photosensitizer consisting of a polymer chain ("backbone") comprising covalently bound sensitizers suitable for the photochemical conversion, to light with a wavelength of preferably between approx. 300 and approx. 1,000 nm, and by then isolating the resulting previtamin D compound and cis-vitamin D compound, respectively, in which a polymeric photosensitizer is used, the polymer chain of which has been selected from the group consisting of a polyether chain, an amino groups-containing polymer chain and a block copolymer chain comprising polyether segments and/or amino groups-containing polymer segments, in such a manner that the polymeric photosensitizer dissolves in the solvent system during the exposure to radiation but either upon cooling precipitates from the solution and can be separated, or, in case said polymer chain comprises amino groups, can be protonated with a suitable acid substance and be removed in an after-treatment. The invention also relates to a polymeric photosensitizer to be used for the said method.
摘要翻译：本发明涉及一种通过分别暴露高速半胱氨酸化合物和反式维生素D化合物将快速组合物化合物转化为前驱物D化合物和反式维生素D化合物转化为辐射影响的顺式维生素D化合物的方法，溶解在合适的溶剂体系中，在由包含共价结合的适用于光化学转化的敏化剂的聚合物链（“主链”）组成的聚合物光敏剂存在下，其波长优选在约 300和约然后分别分离其中使用聚合物光敏剂的得到的维生素D化合物和顺式维生素D化合物，其聚合物链选自聚醚链，氨基 - 含有聚合物链和包含聚醚链段和/或含氨基聚合物链段的嵌段共聚物链，使得聚合物光敏剂在暴露于辐射期间溶解在溶剂体系中，但是在从溶液中冷却沉淀物时可以或者在所述聚合物链包含氨基的情况下，可用合适的酸性物质进行质子化，并在后处理中除去。本发明还涉及用于所述方法的聚合物光敏剂。

6. 发明授权

US5035783A Method for the photochemical conversion of tachysterol compounds into previtamin D compounds and of trans-vitamin D compounds into cis-vitamin D compounds 失效
标题翻译：快速组合物化合物转化为维生素D化合物和反维生素D化合物转化为顺式维生素D化合物的方法
公开(公告)号：US5035783A
公开(公告)日：1991-07-30
申请号：US447509
申请日：1989-12-07
申请人： Eric Goethals , Sebastianus J. Halkes , Robert B. Koolstra
发明人： Eric Goethals , Sebastianus J. Halkes , Robert B. Koolstra
IPC分类号： C07C401/00 , C08F8/00 , C08F8/30 , C08F8/32 , C08G65/20 , C08G65/32 , C08G65/333 , C08G65/337
CPC分类号： C08G65/333 , C07C401/00 , C08F8/00 , C08G65/337
摘要： The invention relates to a method for the photochemical conversion of tachysterol compounds into previtamin D compounds and of trans-vitamin D compounds into cis-vitamin D compounds under the influence of radiation, by exposing the tachysterol compound and trans-vitamin D compound, respectively, dissolved in a suitable solvent system, in the presence of a polymeric photosensitizer consisting of a polymer chain ("backbone") comprising covalently bound sensitizers suitable for the photochemical conversion, to light with a wavelength of preferably between approx. 300 and approx. 1,000 nm, and by then isolating the resulting previtamin D compound and cis-vitamin D compound, respectively, in which a polymeric photosensitizer is used, the polymer chain of which has been selected from the group consisting of a polyether chain, an amino groups-containing polymer chain and a block copolymer chain comprising polyether segments and/or amino groups-containing polymer segments, in such a manner that the polymeric photosensitizer dissolves in the solvent system during the exposure to radiation but either upon cooling precipitates from the solution and can be separated, or, in case said polymer chain comprises amino groups, can be protonated with a suitable acid substance and be removed in an after-treatment. The invention also relates to a polymeric photosensitizer to be used for the said method.

7. 再颁专利

USRE36854E Vitamin D compounds and method of preparing these compounds 失效
标题翻译：维生素D化合物及其制备方法
公开(公告)号：USRE36854E
公开(公告)日：2000-09-05
申请号：US931073
申请日：1997-09-15
申请人： Jose P. Sestelo , Antonio Mourino , Jose L. Mascarenas , Sebastianus J. Halkes , Jan Zorgdrager , Gerhardus D. H. Dijkstra , Jan-Paul van de Velde
发明人： Jose P. Sestelo , Antonio Mourino , Jose L. Mascarenas , Sebastianus J. Halkes , Jan Zorgdrager , Gerhardus D. H. Dijkstra , Jan-Paul van de Velde
IPC分类号： C07C35/32 , C07C45/29 , C07C49/477 , C07C49/513 , C07C401/00 , A61K31/205 , A61K31/59
CPC分类号： C07C401/00 , C07C35/32 , C07C45/292 , C07C49/477 , C07C49/513 , Y10S514/861 , Y10S514/863
摘要： The invention relates to a new vitamin D compound of the general formula ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group;R.sub.2 is a (C.sub.1 -C.sub.3)alkyl group, a hydroxy(C.sub.1 -C.sub.3)alkyl group, a (C.sub.1 -C.sub.2)alkoxymethyl group or a (C.sub.2 -C.sub.3)alkenyl or alkynyl group;R.sub.3 is a branched or non-branched, saturated or unsaturated aliphatic 3- to 5 -membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy;R.sub.4 is a sec. or tert. (C.sub.3 -C.sub.6)alkyl group or a (C.sub.3 -C.sub.6)cycloalkyl group; andA and B are each individually hydrogen atoms or methyl groups, orA and B form together a methylene group.The invention further relates to a method of preparing these compounds and to their use in pharmacotherapy and cosmetics.
摘要翻译：本发明涉及以下通式的新的维生素D化合物：其中：R1是氢原子或羟基; R2是（C1-C3）烷基，羟基（C1-C3）烷基，（C1-C2）烷氧基甲基或（C2-C3）烯基或炔基; R3是在主链中具有至少3个原子且任选地被一个或多个选自环氧基，氟和羟基的取代基取代的支化或非支化的饱和或不饱和脂族3-至5-元烃或二烃基双基。 R4是秒或叔。（C 3 -C 6）烷基或（C 3 -C 6）环烷基; A和B各自为氢原子或甲基，或A和B一起形成亚甲基。本发明还涉及这些化合物的制备方法及其在药物治疗和化妆品中的应用。

8. 发明授权

US06072062A Synthesis of C.sub.18 -modified vitamin D compounds and compounds resulting therefrom 失效
标题翻译： C18改性维生素D化合物的合成及由此产生的化合物
公开(公告)号：US06072062A
公开(公告)日：2000-06-06
申请号：US799346
申请日：1997-02-13
申请人： Maria J. Valles , Jose L. Mascarenas , Antonio Mourino , Sebastianus J. Halkes , Jan Zorgdrager
发明人： Maria J. Valles , Jose L. Mascarenas , Antonio Mourino , Sebastianus J. Halkes , Jan Zorgdrager
IPC分类号： A61K31/59 , A61P3/02 , C07C29/143 , C07C35/32 , C07C43/305 , C07C43/315 , C07C401/00 , C07D305/14 , C07D307/93 , C07D307/94 , C07D311/94 , C07D317/20 , C07D407/04 , C07F7/18 , C07F9/53
CPC分类号： C07D407/04 , C07C401/00 , C07C43/315 , C07D307/93 , C07D307/94 , C07D311/94 , C07D317/20 , C07F7/1856 , C07F9/532 , C07C2101/14 , C07C2102/24
摘要： The invention relates to a new vitamin D compound, substituted in the 18-position with an alkyl group, a hydroxy group, an alkoxy group, an alkenyl group, an alkynyl group, a fluorinated alkyl group or a fluorinated alkenyl group. The invention also relates to a method of preparing said vitamin D compound and to a lactone and a hydrindane intermediate. The vitamin D compound is of the general formula ##STR1##
摘要翻译：本发明涉及在18位被烷基，羟基，烷氧基，烯基，炔基，氟化烷基或氟化烯基取代的新的维生素D化合物。本发明还涉及一种制备所述维生素D化合物以及内酯和氢化茚中间体的方法。维生素D化合物为通式

9. 发明授权

US5929056A Vitamin D compounds and method of preparing these compounds 失效
标题翻译：维生素D化合物及其制备方法
公开(公告)号：US5929056A
公开(公告)日：1999-07-27
申请号：US570560
申请日：1995-12-11
申请人： Antonio Mourino , Jose Antonio Martinez , Maria de los Angeles Rey , Juan Granja , Sebastianus J. Halkes
发明人： Antonio Mourino , Jose Antonio Martinez , Maria de los Angeles Rey , Juan Granja , Sebastianus J. Halkes
IPC分类号： A61K31/59 , A61P3/02 , A61P3/08 , A61P9/12 , A61P11/00 , A61P17/00 , A61P19/10 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00 , C07C49/513 , C07C49/517 , C07C401/00 , C07F7/18
CPC分类号： C07C401/00
摘要： The present invention relates to vitamin D compounds of the general formula ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group;R.sub.2 is a (C.sub.1 -C.sub.3)alkyl group, a hydroxy(C.sub.1 -C.sub.3)alkyl group, a (C.sub.1 -C.sub.2)alkoxymethyl group or a (C.sub.2 -C.sub.3)alkenyl or alkynyl group;n is 1;R.sub.3 is a branched or non-branched, saturated or unsaturated, substituted or unsubstituted aliphatic (C.sub.3 -C.sub.7)hydrocarbon or oxyhydrocarbon biradical;R.sub.4 is a branched or straight (C.sub.1 -C.sub.6) alkyl group or a (C.sub.3 -C.sub.6)cycloalkyl group; andA and B are each individually hydrogen atoms or methyl groups, orA and B form together a methylene group.The present compounds find use in cosmetic application and in human and veterinary pharmacotherapeutic practice in the treatment of skin and bone diseases, diseases related to cell differentiation/cell proliferation, imbalance in the immune system and inflammatory diseases.
摘要翻译：本发明涉及以下通式的维生素D化合物：其中：R1是氢原子或羟基; R2是（C1-C3）烷基，羟基（C1-C3）烷基，（C1-C2）烷氧基甲基或（C2-C3）烯基或炔基; n为1; R 3是支链或非支链的饱和或不饱和的取代或未取代的脂族（C 3 -C 7）烃或氧代烃双基; R4是支链或直链（C1-C6）烷基或（C3-C6）环烷基; A和B各自为氢原子或甲基，或A和B一起形成亚甲基。本发明化合物用于化妆品应用和人和兽药药物治疗实践中用于治疗皮肤和骨骼疾病，与细胞分化/细胞增殖相关的疾病，免疫系统中的不平衡和炎性疾病。

10. 发明授权

US6080878A Method of preparing 16-dehydro vitamin D compounds 失效
标题翻译：制备16-脱氢维生素D化合物的方法
公开(公告)号：US6080878A
公开(公告)日：2000-06-27
申请号：US67903
申请日：1998-04-29
申请人： Maria de los Angeles Rey , Antonio Mourino , Ana Fernandez-Gacio , Yagamare Fall , Sebastianus J. Halkes , Koen M. Halkes , Jan-Paul van de Velde , Jan Zorgdrager
发明人： Maria de los Angeles Rey , Antonio Mourino , Ana Fernandez-Gacio , Yagamare Fall , Sebastianus J. Halkes , Koen M. Halkes , Jan-Paul van de Velde , Jan Zorgdrager
IPC分类号： A61K31/59 , A61P11/00 , A61P17/00 , A61P29/00 , A61P35/00 , A61P37/00 , C07C35/27 , C07C49/665 , C07C401/00
CPC分类号： C07C401/00 , C07C59/90 , C07F7/1892 , C07C2102/24 , Y02P20/55
摘要： The invention relates to a new method of preparing 16-dehydro vitamin D compounds having formula I ##STR1## wherein: R has the epi-configuration or the normal configuration and represents straight or branched C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl, C.sub.3-6 -cycloalkyl, or an aromatic group optionally substituted with halogen, C.sub.1-3 -alkyl or alkoxy,Z is a saturated or unsaturated straight hydrocarbon group or oxahydrocarbon group containing 3-6 C-atoms which may be substituted with OH, F, alkyl (C.sub.1-3) or cycloalkyl (C.sub.3-5),R.sub.1 is hydrogen or an hydroxy protecting group,R.sub.2 is hydrogen or hydroxy, andA and B represent hydrogen or methyl, or together form the methylene group, to the new compounds having this formula and to new intermediates obtainable according to this process.
摘要翻译：本发明涉及一种制备具有式I的16-脱氢维生素D化合物的新方法，其中：R具有外延构型或正构构型，并表示直链或支链C 1-6 - 烷基，C 2-6 - 烯基，C 3-6 环烷基或任选被卤素，C 1-3 - 烷基或烷氧基取代的芳基，Z是含有3-6个C原子的饱和或不饱和直链烃基或氧杂烃基，其可以被OH，F，烷基（ C 1-3）或环烷基（C 3-5），R 1是氢或羟基保护基，R 2是氢或羟基，A和B代表氢或甲基，或一起形成亚甲基，以及根据该方法可获得的新中间体。

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