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1. 发明授权

US4338312A Method for preventing parturient paresis in dairy cattle 失效
标题翻译：防止奶牛分娩麻痹的方法
公开(公告)号：US4338312A
公开(公告)日：1982-07-06
申请号：US262093
申请日：1981-05-11
申请人： Hector F. DeLuca , Heinrich K. Schnoes , Neal A. Jorgensen
发明人： Hector F. DeLuca , Heinrich K. Schnoes , Neal A. Jorgensen
IPC分类号： A61K31/59 , A61P15/00 , C07J9/00 , A01N45/00
CPC分类号： A61K31/59
摘要： A method for prophylactically treating dairy cattle for parturient paresis by administering to the cattle a 25-hydroxylated vitamin D compound and a 1.alpha.-hydroxylated vitamin D compound in combination in an amount sufficient to induce said prophylaxsis.
摘要翻译：一种通过以足以诱导所述预防的量组合施用25-羟基化维生素D化合物和1α-羟化维生素D化合物来预防性治疗分娩麻疹的奶牛的方法。

2. 发明授权

US4428946A Method of preventing milk fever in dairy cattle 失效
标题翻译：防止奶牛发热的方法
公开(公告)号：US4428946A
公开(公告)日：1984-01-31
申请号：US401996
申请日：1982-07-26
申请人： Hector F. DeLuca , Heinrich K. Schnoes , Neal A. Jorgensen
发明人： Hector F. DeLuca , Heinrich K. Schnoes , Neal A. Jorgensen
IPC分类号： A61K31/59 , A01N45/00
CPC分类号： A61K31/59
摘要： A method for prophylactically treating dairy cattle for parturient paresis by administering to cattle vitamin D derivatives which are characterized by the presence of a hydroxyl group at at least one of the C-1 and C-25 positions and a metabolically stable blocking group at the C-24 position in an amount sufficient to induce said prophylaxsis.
摘要翻译：一种通过给予牛维生素D衍生物预防性治疗分娩麻疹的方法，所述维生素D衍生物的特征在于在C-1和C-25位置中的至少一个存在羟基，在C处具有代谢稳定的阻断基团 -24位置，其量足以诱导所述预防。

3. 发明授权

US5880292A All-trans-retinol metabolite 失效
标题翻译：全反式视黄醇代谢物
公开(公告)号：US5880292A
公开(公告)日：1999-03-09
申请号：US927511
申请日：1997-09-11
申请人： Hector F. DeLuca , Heinrich K. Schnoes , Rafal R. Sicinski , Xiujuan Jia
发明人： Hector F. DeLuca , Heinrich K. Schnoes , Rafal R. Sicinski , Xiujuan Jia
IPC分类号： C07D333/22 , C07D333/10 , A61K31/38
CPC分类号： C07D333/22
摘要： In vitro incubation of all-trans-retinol (atROL) with kidney homogenate from vitamin A deficient and retinoic acid supplemented (VAD-RAS) female rats produced a new retinol metabolite. The metabolite has the structure ##STR1## and is believed useful for the treatment of skin disorders such as acne, psoriasis, and ultraviolet light skin damage, as well as for promoting female fertility and the maintenance of pregnancy.
摘要翻译：全反式视黄醇（atROL）与来自维生素A缺乏和视黄酸补充（VAD-RAS）雌性大鼠的肾匀浆体外孵育产生新的视黄醇代谢物。代谢物具有结构，被认为可用于治疗皮肤疾病如痤疮，牛皮癣和紫外线皮肤损伤，以及促进女性生殖力和维持妊娠。

4. 发明授权

US5618805A 19-nor-vitamin D compounds 失效
标题翻译： 19-维生素D化合物
公开(公告)号：US5618805A
公开(公告)日：1997-04-08
申请号：US442483
申请日：1995-05-16
申请人： Hector F. DeLuca , Heinrich K. Schnoes , Kato L. Perlman , Rafal R. Sicinski , Jean M. Prahl
发明人： Hector F. DeLuca , Heinrich K. Schnoes , Kato L. Perlman , Rafal R. Sicinski , Jean M. Prahl
IPC分类号： A61K31/59 , A61K20060101 , A61P5/12 , A61P17/00 , A61P35/00 , A61P35/02 , C07C20060101 , C07C401/00 , C12N20060101 , G01N33/48 , G01N33/574 , A61K31/695
CPC分类号： C07C401/00 , Y02P20/55
摘要： This invention provides a novel class of vitamin D-related compounds, namely the 1.alpha.-hydroxy-19-nor-vitamin D analogs, as well as a general method for their chemical synthesis. The compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells, including malignant cells, and in inducing their differentiation, and thus represent novel therapeutic agents for the treatment of malignant and other diseases characterized by the proliferative growth of undifferentiated cells. Formulations for therapeutic use and treatment methods are also provided.
摘要翻译：本发明提供了一类新颖的维生素D相关化合物，即1α-羟基-19-去甲维生素D类似物，以及它们化学合成的一般方法。该化合物在阻止未分化细胞（包括恶性细胞）的增殖以及诱导其分化中表现出明显的活性，因此代表治疗以未分化细胞增殖生长为特征的恶性和其它疾病的新型治疗剂。还提供了治疗用途和治疗方法的制剂。

5. 发明授权

US5587497A 19-nor-vitamin D compounds 失效
标题翻译： 19-维生素D化合物
公开(公告)号：US5587497A
公开(公告)日：1996-12-24
申请号：US442492
申请日：1995-05-16
申请人： Hector F. DeLuca , Heinrich K. Schnoes , Kato L. Perlman , Rafal R. Sicinski , Jean M. Prahl
发明人： Hector F. DeLuca , Heinrich K. Schnoes , Kato L. Perlman , Rafal R. Sicinski , Jean M. Prahl
IPC分类号： A61K31/59 , A61K20060101 , A61P5/12 , A61P17/00 , A61P35/00 , A61P35/02 , C07C20060101 , C07C401/00 , C12N20060101 , G01N33/48 , G01N33/574
CPC分类号： C07C401/00 , Y02P20/55
摘要： This invention provides a novel class of vitamin D-related compounds, namely the 1.alpha.-hydroxy-19-nor-vitamin D analogs, as well as a general method for their chemical synthesis. The compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells, including malignant cells, and in inducing their differentiation, and thus represent novel therapeutic agents for the treatment of malignant and other diseases characterized by the proliferative growth of undifferentiated cells. Formulations for therapeutic use and treatment methods are also provided. The 19-nor vitamin D compounds have the formula: ##STR1## where X.sup.1 and X.sup.2 are each hydrogen or a hydroxy protecting group and R is a side chain.
摘要翻译：本发明提供了一类新颖的维生素D相关化合物，即1α-羟基-19-去甲维生素D类似物，以及它们化学合成的一般方法。该化合物在阻止未分化细胞（包括恶性细胞）的增殖以及诱导其分化中表现出明显的活性，因此代表治疗以未分化细胞增殖生长为特征的恶性和其它疾病的新型治疗剂。还提供了治疗用途和治疗方法的制剂。 19-维生素D化合物具有下式：其中X1和X2各自为氢或羟基保护基，R为侧链。

6. 发明授权

US5563286A Synthesis of 19-nor vitamin D compounds 失效
标题翻译：合成19-维生素D化合物
公开(公告)号：US5563286A
公开(公告)日：1996-10-08
申请号：US441878
申请日：1995-05-16
申请人： Hector F. DeLuca , Heinrich K. Schnoes , Kato L. Perlman , Rolf E. Swenson
发明人： Hector F. DeLuca , Heinrich K. Schnoes , Kato L. Perlman , Rolf E. Swenson
IPC分类号： A61K31/59 , A61P35/00 , C07C35/14 , C07C35/17 , C07C43/115 , C07C49/497 , C07C67/343 , C07C69/732 , C07C69/734 , C07C69/74 , C07C317/18 , C07C401/00 , C07D307/20 , C07D309/12 , C07F7/08 , C07F7/18 , C07F9/40 , C07F9/53 , C07F7/04
CPC分类号： C07F7/1856 , C07C401/00 , C07F9/532 , Y02P20/55
摘要： A process is disclosed for the removal of the 4-protected hydroxy group from compounds of the following formula: ##STR1## where A is --COOAlkyl and B is hydroxy, or A and B together represent either oxo or .dbd.CHCOOAlkyl, where X.sup.1 and X.sup.2 are the same or different and represent hydrogen or a hydroxy-protecting group, and where X.sup.3 is ##STR2## with a hydrogen radical source, such as tributyltin hydride or tris(trimethylsilyl)silane, and a radical initiator, such as AIBN or irradiation.
摘要翻译：公开了从下式化合物中除去4-保护的羟基的方法：其中A是-COOA烷基，B是羟基，或A和B一起代表氧代或= CHCOOA烷基，其中X1和X2 相同或不同，代表氢或羟基保护基，并且其中X 3与氢原子源如氢化三丁基锡或三（三甲基甲硅烷基）硅烷和自由基引发剂如AIBN 或照射。

7. 发明授权

US5525745A Intermediates in the preparation of 19-nor vitamin D compounds 失效
标题翻译：中间体制备19-维生素D化合物
公开(公告)号：US5525745A
公开(公告)日：1996-06-11
申请号：US410858
申请日：1995-03-27
申请人： Hector F. DeLuca , Heinrich K. Schnoes , Fariba Aria
发明人： Hector F. DeLuca , Heinrich K. Schnoes , Fariba Aria
IPC分类号： C07C29/17 , C07C35/17 , C07C35/27 , C07C401/00 , C07F7/18
CPC分类号： C07F7/1856 , C07C401/00 , Y02P20/55
摘要： The invention describes intermediates for use in the synthesis of 1.alpha.-hydroxy-19-nor-vitamin D compounds. The intermediates have the following formula: ##STR1## The disclosed process includes (a) the construction of a 5,8-diol-6-yne intermediate by joining ring-A and ring-C/D portions of the desired end product via the condensation of an acetylenic derivative containing the C/D-ring portion of the desired end product with a cyclic dihydroxy ketone representing the A-ring of the desired end product; (b) the partial reduction of the 6,7 acetylenic triple bond linkage between the A and C/D ring portions to obtain a 5,8-diol-6-ene intermediate; and (c) the reductive removal of the 5,8-oxygen functions to generate the required 5,7-diene end product from which the desired 7-trans(7E)-isomer is purified directly, or after optional double bond isomerization of the 7-cis(7Z)-isomer employing a novel thiophenol-promoted isomerization step.
摘要翻译：本发明描述了用于合成1α-羟基-19-去甲维生素D化合物的中间体。中间体具有以下分子式：所公开的方法包括（a）通过将期望的最终产物的环A和环-C / D部分连接到所述中间体上来构建5,8-二醇-6-中间体含有所需最终产物的C / D环部分的炔属衍生物与表示所需最终产物的A环的环状二羟基酮缩合; （b）部分还原A和C / D环部分之间的6,7炔基三键键，得到5,8-二醇-6-烯中间体; 或（c）还原去除5,8-氧官能团以产生所需的5,7-二烯最终产物，从其中直接纯化所需的7-反式（7E） - 异构体，或在任选的双键异构化使用新的苯硫酚促进异构化步骤的7-顺式（7Z） - 异构体。

8. 发明授权

US5488183A Acetylenic cyclohexane triol derivatives 失效
标题翻译：乙酸环己烷三醇衍生物
公开(公告)号：US5488183A
公开(公告)日：1996-01-30
申请号：US448105
申请日：1995-05-23
申请人： Hector F. DeLuca , Heinrich K. Schnoes , Fariba Aria
发明人： Hector F. DeLuca , Heinrich K. Schnoes , Fariba Aria
IPC分类号： C07C29/17 , C07C35/17 , C07C35/27 , C07C401/00 , C07F7/18 , C07C35/08 , C07F7/08
CPC分类号： C07F7/1856 , C07C401/00 , Y02P20/55
摘要： A synthesis of 1.alpha.-hydroxy-19-nor-vitamin D compounds comprises (a) the construction of a 5,8-diol-6-yne intermediate by joining ring-A and ring-C/D portions of the desired end product via the condensation of an acetylenic derivative containing the C/D-ring portion of the desired end product with a cyclic dihydroxy ketone representing the A-ring of the desired end product; (b) the partial reduction of the 6,7 acetylenic triple bond linkage between the A and C/D ring portions to obtain a 5,8-diol-6-ene intermediate; and (c) the reductive removal of the 5,8-oxygen functions to generate the required 5,7-diene end product from which the desired 7-trans(7E)-isomer is purified directly, or after optional double bond isomerization of the 7-cis(7Z)-isomer employing a novel thiophenol-promoted isomerization step.
摘要翻译： 1α-羟基-19-去甲维生素D化合物的合成包括（a）通过将期望的最终产物的环A和环-C / D部分连接而构建5,8-二醇-6-中间体通过含有所需最终产物的C / D环部分的炔属衍生物与代表期望最终产物的A环的环状二羟基酮缩合; （b）部分还原A和C / D环部分之间的6,7炔基三键键，得到5,8-二醇-6-烯中间体; 或（c）还原去除5,8-氧官能团以产生所需的5,7-二烯最终产物，从其中直接纯化所需的7-反式（7E） - 异构体，或在任选的双键异构化使用新的苯硫酚促进异构化步骤的7-顺式（7Z） - 异构体。

9. 发明授权

US5089641A Synthesis of 1.alpha.-hydroxy-secosterol compounds 失效
标题翻译： 1α-羟基 - 甾醇化合物的合成
公开(公告)号：US5089641A
公开(公告)日：1992-02-18
申请号：US667440
申请日：1991-03-11
申请人： Hector F. DeLuca , Heinrich K. Schnoes , Kato L. Perlman
发明人： Hector F. DeLuca , Heinrich K. Schnoes , Kato L. Perlman
IPC分类号： C07C401/00 , C07J9/00 , C07J51/00
CPC分类号： C07J9/005 , C07C401/00 , C07J51/00
摘要： This invention provides a new method of making secosterol compounds, and in particular to the preparation of 1.alpha.-hydroxy-homopregnacalciferol which is a secosterol compound that is effective in inducing the differentiation of malignant cells and is therefore useful for the treatment of malignancies such as leukemia.
摘要翻译：本发明提供了一种制备西蒙托甾醇化合物的新方法，特别是制备1α-羟基 - 高孕蛋白胨，它是有效诱导恶性细胞分化的季戊四醇化合物，因此可用于治疗恶性肿瘤，例如白血病。

10. 发明授权

US5086191A Intermediates for the synthesis of 19-nor vitamin D compounds 失效
标题翻译：用于合成19-维生素D化合物的中间体
公开(公告)号：US5086191A
公开(公告)日：1992-02-04
申请号：US705932
申请日：1991-05-28
申请人： Hector F. DeLuca , Heinrich K. Schnoes , Kato L. Perlman
发明人： Hector F. DeLuca , Heinrich K. Schnoes , Kato L. Perlman
IPC分类号： C07C401/00 , C07C47/267 , C07C47/277 , C07F7/18
CPC分类号： C07F7/1856 , C07C47/267 , C07C47/277
摘要： New intermediate compounds that can be used effectively for the synthesis of a broad range of 1.alpha.-hydroxy-19-nor-vitamin D compounds. These novel intermediates are characterized by a group selected from hydroxy methyl (--CH.sub.2 OH), carboxaldehyde (--CHO), and carboxy ester (--COOAlkyl) at the carbon 22 position of the side chain of a 19-nor-vitamin D nucleus. Intermediates of this type are useful for the introduction of side chain units and thus represent important synthons for the preparation of many different 19-nor-vitamin D compounds.

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