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1. 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

2. 发明授权

US5637742A Vitamin D compound, method of preparing this compound and intermediate therefor 失效
标题翻译：维生素D化合物，制备该化合物的方法及其中间体
公开(公告)号：US5637742A
公开(公告)日：1997-06-10
申请号：US333305
申请日：1994-11-01
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化合物具有通式

3. 发明授权

US5403940A Vitamin D compound, method of preparing this compound and intermediate thereof 失效
标题翻译：维生素D化合物，该化合物的制备方法及其中间体
公开(公告)号：US5403940A
公开(公告)日：1995-04-04
申请号：US180463
申请日：1994-01-12
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化合物具有通式

4. 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。

5. 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。

6. 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。

7. 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。

8. 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。

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

US09018194B2 Vitamin D receptor modulators with partial agonist activity 有权
标题翻译：具有部分激动剂活性的维生素D受体调节剂
公开(公告)号：US09018194B2
公开(公告)日：2015-04-28
申请号：US14002502
申请日：2012-03-01
申请人： Makoto Makishima , Sachiko Yamada , Antonio Mourino , Hiroaki Tokiwa , Takeru Kudo , Yusuke Watarai , Kazuki Maekawa
发明人： Makoto Makishima , Sachiko Yamada , Antonio Mourino , Hiroaki Tokiwa , Takeru Kudo , Yusuke Watarai , Kazuki Maekawa
IPC分类号： A61K31/593 , C07C401/00
CPC分类号： C07C401/00 , C07C2601/14 , C07C2602/24 , C07C2603/74
摘要： The present invention provides a compound which functions as a selective vitamin D receptor modulator and has action-selectivity or tissue-selectivity such that it does not induce hypercalcemia but causes other effects. There is provided a compound represented by formula (I), a solvate thereof or a prodrug thereof. wherein m and n each independently represent 1 or 0; R represents a hydrogen atom or an alkyl group; Y represents an ethane-1,1-diyl group or an ethyne-1,2-diyl group; and Z1 represents a hydrogen atom and Z2 represents a hydroxyalkoxy group, or Z1 and Z2 jointly form a methylene group.
摘要翻译：本发明提供了作为选择性维生素D受体调节剂起作用且具有动作选择性或组织选择性的化合物，使得其不诱导高钙血症而引起其他作用。提供由式（I）表示的化合物，其溶剂合物或其前药。其中m和n各自独立地表示1或0; R表示氢原子或烷基; Y表示乙-1,1-二基或乙炔-1,2-二基; Z1表示氢原子，Z2表示羟基烷氧基，Z1或Z2共同形成亚甲基。

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