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61. 发明授权

US4188345A Fluorovitamin D compounds and processes for their preparation 失效
公开(公告)号：US4188345A
公开(公告)日：1980-02-12
申请号：US928279
申请日：1978-07-26
申请人： Hector F. DeLuca , Heinrich K. Schnoes , Joseph L. Napoli, Jr. , Bruce L. Onisko
发明人： Hector F. DeLuca , Heinrich K. Schnoes , Joseph L. Napoli, Jr. , Bruce L. Onisko
IPC分类号： A61K31/59 , A61K31/593 , A61P3/02 , C07C67/00 , C07C401/00 , G06F11/14 , G06F11/18 , G06F11/20 , G06F15/16 , G06F15/177 , C07C41/00
CPC分类号： A61K31/593 , C07C401/00 , C07C2101/14 , C07C2101/16 , C07C2102/18 , C07C2102/24 , Y02P20/582
摘要： Fluorine-substituted vitamin D compounds, methods for preparation of such compounds and fluorinated intermediate compounds used in such methods are disclosed. The fluorine-substituted vitamin D compounds are characterized by vitamin D-like activity in stimulating intestinal calcium transport and bone mobilization and in promoting the calcification of rachitic bone.

62. 发明授权

US5616759A Cyclohexylidene compounds 失效
标题翻译：环亚己基化合物
公开(公告)号：US5616759A
公开(公告)日：1997-04-01
申请号：US441966
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 , C07F9/02
CPC分类号： C07F7/1856 , C07C401/00 , C07F9/532 , Y02P20/55
摘要： Cyclohexylidene compounds of the structure: ##STR1## where X.sup.1 and X.sup.2, which may be the same or different, is hydrogen or a hydroxy-protecting group, and Y is --POPh.sub.2, or --PO (OAlkyl).sub.2, or --SO.sub.2 Ar, or --Si(Alkyl).sub.3. The compounds are used as intermediates in the preparation of 19-nor-vitamin D compounds.
摘要翻译：结构的环亚己基化合物：其中X1和X2可以相同或不同，是氢或羟基保护基，Y是-POPh2或-PO（O烷基）2或-SO2Ar，或 -Si（烷基）3。该化合物用作制备19-维生素D化合物的中间体。

63. 发明授权

US5597932A Intermediate for the preparation of 19-nor vitamin D compounds 失效
标题翻译：用于制备19-维生素D化合物的中间体
公开(公告)号：US5597932A
公开(公告)日：1997-01-28
申请号：US442508
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 , C07D309/00 , C07C47/28
CPC分类号： C07F7/1856 , C07C401/00 , C07F9/532 , Y02P20/55
摘要： The invention is drawn to a compound having the following formula ##STR1## in which X.sup.1 and X.sup.2, which may be the same or different, represent hydrogen or a hydroxy-protecting group, X.sup.4 is hydrogen, A is selected from --COOAlkyl and CH.sub.2 OH, and B is a hydroxy group, or A and B, when taken together, represent an oxo group. These compounds are useful as intermediates in the production of 19-nor vitamin D derivatives.
摘要翻译：本发明涉及具有下式的化合物，其中X 1和X 2可以相同或不同，表示氢或羟基保护基，X 4是氢，A选自-COOA烷基和CH 2 OH，并且B是羟基，或者A和B一起表示氧基。这些化合物可用作生产19-维生素D衍生物的中间体。

64. 发明授权

US5581006A 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：US5581006A
公开(公告)日：1996-12-03
申请号：US441991
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 , C07F9/02 , C07C317/00
CPC分类号： C07F7/1856 , C07C401/00 , C07F9/532 , Y02P20/55
摘要： A convergent synthesis of 19-nor-vitamin D compounds, specifically 19-nor-1.alpha.,25-dihydroxyvitamin D.sub.3, is disclosed. The synthesis can also readily be utilized for preparing other 1.alpha.-hydroxylated 19-nor-vitamin D compounds. The key step in the synthesis is a suitable application of Lythgoe's procedure i.e. a Horner-Wittig reaction of the lithium anion of a phosphine oxide with a Windaus Grundmann ketone to give, after any necessary deprotection, the desired 19-nor-vitamin D compound.
摘要翻译：公开了19-维生素D化合物，特别是19-nor-1α，25-二羟基维生素D3的会聚合成。合成还可以容易地用于制备其它1α-羟基化的19-维生素D化合物。合成中的关键步骤是Lythgoe方法的合适应用，即氧化膦锂的阴离子与Windaus Grundmann酮的Horner-Wittig反应，在任何必需的脱保护后，得到所需的19-维生素D化合物。

65. 发明授权

US5260290A Homologated vitamin D.sub.2 compounds and the corresponding 1.alpha.-hydroxylated derivatives 失效
标题翻译：同系维生素D2化合物和相应的1α-羟基化衍生物
公开(公告)号：US5260290A
公开(公告)日：1993-11-09
申请号：US654746
申请日：1991-02-13
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 , C07J71/00 , C07J172/00
CPC分类号： C07C401/00 , C07J71/0042
摘要： The invention provides new 24, 26, and/or 27 homologated vitamin D.sub.2 compounds, such as 26,27-dihomo-1.alpha.-hydroxyvitamin D.sub.2, 26,27-dihomo-1.alpha.-hydroxy-24-epi-vitamin D.sub.2, 26,27-dihomo-1.alpha.,25-dihydroxy-24-epi-vitamin D.sub.2 and certain hydroxy-protected derivatives thereof. The new epi compounds in particular exhibit a distinctive activity pattern comprising high potency in stimulating intestinal calcium transport and little or no activity in inducing bone calcium mobilization or the differentiation of undifferentiated cells in culture, thereby evincing utility in the treatment of diseases characterized by loss of bone mass. In contrast, the natural form exhibits no activity in either mobilizing calcium from bone or stimulating intestinal calcium transport. A process for preparing such compounds is also disclosed.
摘要翻译：本发明提供新的24,26和/或27个同系的维生素D 2化合物，例如26,27-二氢-1α-羟基维生素D 2，26,27-二羟基-α-羟基-24-表维生物D2,26 ，27-二高-1α，25-二羟基-24-表维生物D 2及其某些羟基保护的衍生物。新的epi化合物特别表现出独特的活性模式，其包括在刺激肠钙运输中具有高效力，并且在诱导骨钙动员或培养中未分化细胞的分化中几乎没有或没有活性，从而显示用于治疗以失去骨质量相比之下，天然形式在从骨中移动钙或刺激肠钙运输方面没有表现出任何活性。还公开了制备这种化合物的方法。

66. 发明授权

US5250523A Side chain unsaturated 1.alpha.-hydroxyvitanim D homologs 失效
标题翻译：侧链不饱和1α-羟基维生素D同系物
公开(公告)号：US5250523A
公开(公告)日：1993-10-05
申请号：US481993
申请日：1990-02-14
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 , A61K31/59 , C07J172/00 , C07J175/00
CPC分类号： C07C401/00
摘要： This invention provides novel vitamin D-related compounds characterized by extended unsaturated side chain structures. Such compounds exhibit increased activity in arresting the proliferation and promoting the differentiation of malignant cells with only minimal calcemic activity and thus represents new therapeutic agents applicable and uniquely useful in differentiation therapy of malignant diseases. The activity characteristics of these compounds provide the basis of a method for the treatment of neoplastic diseases, specifically leukemoid diseases.
摘要翻译：本发明提供了以延展不饱和侧链结构为特征的新型维生素D相关化合物。这样的化合物在抑制增殖和促进恶性细胞的分化方面表现出增加的活性，仅具有最小的血钙活性，因此代表了适用于在恶性疾病的分化治疗中独特有用的新治疗剂。这些化合物的活性特征提供了治疗肿瘤疾病，特别是白血病的方法的基础。

67. 发明授权

US5237110A 19-nor-vitamin D compounds 失效
标题翻译： 19-NOR-VITAMIN D化合物
公开(公告)号：US5237110A
公开(公告)日：1993-08-17
申请号：US481354
申请日：1990-02-16
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.

68. 发明授权

US4973584A Novel 1.alpha.-hydroxyvitamin D.sub.2 epimer and derivatives 失效
标题翻译：新型1α-羟基维生素D2差向异构体及其衍生物
公开(公告)号：US4973584A
公开(公告)日：1990-11-27
申请号：US321254
申请日：1989-03-09
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： A61K31/59 , A61K31/592 , A61P3/02 , A61P3/14 , A61P19/10 , A61P43/00 , C07C401/00
CPC分类号： C07C401/00
摘要： The invention provides a new vitamin D.sub.2 compound, 1.alpha.-hydroxy-24-epi-vitamin D.sub.2 and certain hydroxy-protected derivatives thereof. The new compound exhibits a distinctive activity pattern comprising high potency in stimulating intestinal calcium transport and little or no activity in inducing bone calcium mobilization or the differentiation of undifferentiated cells in culture, thereby evincing utility in the treatment of diseases characterized by loss of bone mass.

69. 发明授权

US4927815A Compounds effective in inducing cell differentiation and process for preparing same 失效
标题翻译：有效诱导细胞分化的化合物及其制备方法
公开(公告)号：US4927815A
公开(公告)日：1990-05-22
申请号：US187680
申请日：1988-04-29
申请人： Hector F. DeLuca , Heinrich K. Schnoes , Kato L. Perlman , Andrzej Kutner
发明人： Hector F. DeLuca , Heinrich K. Schnoes , Kato L. Perlman , Andrzej Kutner
IPC分类号： A61K31/59 , A61P35/00 , C07C401/00 , C07F7/18
CPC分类号： C07C401/00
摘要： This invention provides novel side chain homologs of 1.alpha.,25-dihydroxyvitamin D.sub.3 which exhibit enhanced and highly selective activity in inducing differentiation of malignant cells. It also provides a general method of synthesis applicable to the preparation of a variety of vitamin D side chain analogs, and a method of treatment of neoplastic diseases which takes advantage of the selective differentiation activity of the new vitamin D homologs.
摘要翻译：本发明提供1α，25-二羟基维生素D3的新型侧链同源物，其在诱导恶性细胞分化中表现出增强的和高选择性的活性。它还提供适用于制备各种维生素D侧链类似物的一般合成方法，以及利用新维生素D同系物选择性分化活性的肿瘤疾病的治疗方法。

70. 发明授权

US4588716A Method for treating metabolic bone disease in mammals 失效
标题翻译：治疗哺乳动物代谢性骨病的方法
公开(公告)号：US4588716A
公开(公告)日：1986-05-13
申请号：US691824
申请日：1985-01-16
申请人： Hector F. DeLuca , Heinrich K. Schnoes
发明人： Hector F. DeLuca , Heinrich K. Schnoes
IPC分类号： C07C401/00 , C07D317/24 , C07J71/00 , A61K31/595 , A61K31/56 , A61K31/59
CPC分类号： C07C401/00 , C07D317/24 , C07J71/0042
摘要： A method for treating or preventing metabolic bone disease characterized by loss of bone mass in mammals by administering 24-epi-1.alpha.,25-dihydroxy vitamin D.sub.2 alone or in combinations thereof with bone mobilization-inducing vitamin D derivatives to said mammals.
摘要翻译：通过将24-epi-1α，25-二羟基维生素D2单独或与骨移动诱导维生素D衍生物组合施用于所述哺乳动物来治疗或预防代谢性骨疾病的方法，其特征在于哺乳动物的骨质量损失。

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