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1. 发明申请

WO2004054968A2 25-SO2-SUBSITUTED ANALOGS OF 1α,25-DIHYDROXYVITAMIN D3 审中-公开
标题翻译： 1α，25-二羟基维生素D3的25-SO 2取代的模拟物
公开(公告)号：WO2004054968A2
公开(公告)日：2004-07-01
申请号：PCT/CA2003/001926
申请日：2003-12-18
申请人： JOHNS HOPKINS UNIVERSITY , CYTOCHROMA INC. , POSNER, Gary, H. , LEE, Jae, Kyoo , WANG, Qiang , CRAWFORD, Kenneth, R. , YANG, Hong, Woon , SILVERMAN, Steven, M. , SUH, Byung-Chul , WHITE, Jay, A. , JONES, Glenville , SAHA, Uttam , JEON, Heung, Bae
发明人： POSNER, Gary, H. , LEE, Jae, Kyoo , WANG, Qiang , CRAWFORD, Kenneth, R. , YANG, Hong, Woon , SILVERMAN, Steven, M. , SUH, Byung-Chul , WHITE, Jay, A. , JONES, Glenville , SAHA, Uttam , JEON, Heung, Bae
IPC分类号： C07C401/00
CPC分类号： C07C401/00 , C07B2200/07 , C07C2601/02 , C07C2601/04
摘要： The present invention provides novel D-ring and side-chain analogs of lα,25dihydroxyvitamin D 3 , compositions comprising these compounds and methods of using these compounds as selective inhibitors of CYP24. In particular, the compounds of the invention are useful for treating diseases which benefit from a modulation of the levels of lα,25-dihydroxyvitamin D 3 , for example, cell-proliferative disorders.
摘要翻译：本发明提供了Lalpha，25二羟基维生素D 3的新型D环和侧链类似物，包含这些化合物的组合物和使用这些化合物作为CYP24选择性抑制剂的方法。特别地，本发明的化合物可用于治疗受益于调节Lalpha，25-二羟基维生素D3水平的疾病，例如细胞增殖性疾病。

2. 发明申请

WO2006113990A2 LOW-CALCEMIC 16,23-DIENE 25-OXIME ANALOGS OF 1α ,25-DIHYDROXY VITAMIN D3 审中-公开
标题翻译： 1a，25-二羟基维生素D3的低钙16,23-二烯25-氧化物模拟物
公开(公告)号：WO2006113990A2
公开(公告)日：2006-11-02
申请号：PCT/CA2006/000657
申请日：2006-04-25
申请人： CYTOCHROMA INC. , JOHNS HOPKINS UNIVERSITY , SAHA, Uttam , POSNER, Gary, H. , KAHRAMAN, Mehmet
发明人： SAHA, Uttam , POSNER, Gary, H. , KAHRAMAN, Mehmet
CPC分类号： C07C401/00
摘要： The present invention provides novel 16,23-diene 25-oxime ether analogs of 1 ,25-dihydroxy vitamin D3, compositions comprising these compounds and methods of using these compounds as inhibitors of CYP24. In particular, the novel compound of the invention are useful for treating diseases which benefit from a modulation of the levels of 1 ,25-dihydroxy vitamin D3, for example, cell-proliferative disorders.
摘要翻译：本发明提供1,25-二羟基维生素D3的新型16,23-二烯25-肟醚类似物，包含这些化合物的组合物和使用这些化合物作为CYP24抑制剂的方法。特别地，本发明的新化合物可用于治疗受益于调节1,25-二羟维生素D3水平的疾病，例如细胞增殖性疾病。

3. 发明申请

WO2003106411A1 24-SULFOXIMINE VITAMIN D3 COMPOUNDS 审中-公开
标题翻译： 24-SULFOXIMINE维生素D3化合物
公开(公告)号：WO2003106411A1
公开(公告)日：2003-12-24
申请号：PCT/CA2003/000851
申请日：2003-06-13
申请人： JOHNS HOPKINS UNIVERSITY , CYTOCHROMA INC. , KAHRAMAN, Mehmet , POSNER, Gary, H. , SAHA, Uttam
发明人： KAHRAMAN, Mehmet , POSNER, Gary, H. , SAHA, Uttam
IPC分类号： C07C401/00
CPC分类号： C07C401/00
摘要： The present invention provides novel sulfoximine compounds, compositions comprising these compounds and methods of using these compounds as inhibitors of CYP24. In particular, the compounds of the invention are useful for treating diseases which benefit from a modulation of the levels of 1α,25-dihydroxy vitamin D 3 , for example, cell-proliferative disorders.
摘要翻译：本发明提供新的磺酰亚胺化合物，包含这些化合物的组合物和使用这些化合物作为CYP24抑制剂的方法。特别地，本发明的化合物可用于治疗受益于调节1α，25-二羟维生素D3水平的疾病，例如细胞增殖性疾病。

4. 发明申请

WO2011088209A2 1-DEOXY ANALOGS OF VITAMIN D-RELATED COMPOUNDS 审中-公开
标题翻译：维生素D相关化合物的1-去氧模拟物
公开(公告)号：WO2011088209A2
公开(公告)日：2011-07-21
申请号：PCT/US2011/021129
申请日：2011-01-13
申请人： CYTOCHROMA INC. , JOHNS HOPKINS UNIVERSITY , POSNER, Gary, H. , HESS, Lindsey, C. , KALINDA, Alvin, S. , SLACK, Rachel, D. , SAHA, Uttam , PETKOVICH, P., Martin
发明人： POSNER, Gary, H. , HESS, Lindsey, C. , KALINDA, Alvin, S. , SLACK, Rachel, D. , SAHA, Uttam , PETKOVICH, P., Martin
IPC分类号： C07C251/40 , C07C317/10 , C07C381/10 , A61K31/59 , A61K31/592 , A61K31/593 , A61P17/06 , A61P19/10 , A61P35/00
CPC分类号： A61K45/06 , A61K31/593 , C07C401/00 , C07C2601/14 , C07C2602/24
摘要： This present disclosure is directed to novel prodrugs of activated vitamin D3 compounds. The prodrugs can be designed to have one or more beneficial properties, such as selective inhibition of the enzyme CYP24, low calcemic activity, and anti-proliferative activity. Specifically, these prodrugs are 1-deoxy prohormones of active Vitamin D analogs, e.g. analogs of calcitriol. This disclosure is also directed to pharmaceutical and diagnostic compositions containing the prodrugs of the invention, and to their medical use, particularly as prodrugs in the treatment and/or prevention of diseases.
摘要翻译：本公开内容涉及活化的维生素D3化合物的新型前药。前药可以设计成具有一种或多种有益的性质，例如选择性抑制酶CYP24，低钙血症活性和抗增殖活性。具体地，这些前药是活性维生素D类似物的1-脱氧激素，例如，骨化三醇的类似物。本公开还涉及含有本发明前药的药物和诊断组合物及其医疗用途，特别是用于治疗和/或预防疾病的前药。

5. 发明申请

WO2009111873A1 STABILIZED 1,25-DIHYDROXYVITAMIN D2 AND METHOD OF MAKING SAME 审中-公开
标题翻译：稳定的1,25-二羟基维生素D2及其制备方法
公开(公告)号：WO2009111873A1
公开(公告)日：2009-09-17
申请号：PCT/CA2009/000291
申请日：2009-03-12
申请人： CYTOCHROMA, INC. , SAHA, Uttam
发明人： SAHA, Uttam
IPC分类号： C07C401/00 , A61K31/592
CPC分类号： C07C401/00 , A61K31/592 , A61K45/06
摘要： A stabilized 1,25 -dihydroxy vitamin D 2 composition, free of methyl formate, which is particularly well suited for pharmaceutical formulations, pharmaceutical formulations of the 1,25 -dihydroxyvitamin D 2 composition, and a method of making the purified composition by purifying a crude 1,25 -dihydroxy vitamin D 2 from acetone/water, are disclosed. The stabilized 1,25 -dihydroxy vitamin D 2 is characterized by a reduced rate of degradation on heat challenge and during prolonged storage and exhibits excellent storage stability when formulated in a pharmaceutical dosage form, e.g., a soft gelatin capsule.
摘要翻译：稳定的1,25-二羟基维生素D2组合物，不含甲酸甲酯，其特别适用于药物制剂，1,25-二羟基维生素D 2组合物的药物制剂，以及通过纯化粗制物1制备纯化的组合物的方法，丙酮/水中的25-二羟基维生素D 2。稳定的1,25-二羟基维生素D 2的特征在于在热攻击和延长储存期间降低的降解速率，并且当配制成药物剂型，例如软明胶胶囊时，其表现出优异的储存稳定性。

6. 发明申请

WO2010083613A1 PHOSPHATE MANAGEMENT WITH SMALL MOLECULES 审中-公开
标题翻译：磷酸盐管理与小分子
公开(公告)号：WO2010083613A1
公开(公告)日：2010-07-29
申请号：PCT/CA2010/000111
申请日：2010-01-26
申请人： CYTOCHROMA INC. , SAHA, Uttam , HELVIG, Christian, F. , PETKOVICH, P., Martin
发明人： SAHA, Uttam , HELVIG, Christian, F. , PETKOVICH, P., Martin
IPC分类号： A61K31/66 , A61K31/661 , A61K31/662 , A61K31/675 , A61P3/12
CPC分类号： A61K31/66 , A61K31/662 , A61K31/663 , A61K31/675 , A61K45/06 , A61K2300/00
摘要： This invention relates to methods and small molecules having a phosphate group that can be used to inhibit phosphate transport and to treat or prevent diseases that are related to disorders in the maintenance of normal serum phosphate levels.
摘要翻译：本发明涉及具有磷酸基团的方法和小分子，其可用于抑制磷酸盐转运并且治疗或预防与维持正常血清磷酸盐水平的疾病有关的疾病。

7. 发明申请

WO2010060197A1 METHOD FOR SYNTHESIZING VITAMIN D ANALOGS 审中-公开
标题翻译：合成维生素D类似物的方法
公开(公告)号：WO2010060197A1
公开(公告)日：2010-06-03
申请号：PCT/CA2009/001687
申请日：2009-11-25
申请人： CYTOCHROMA INC. , SAHA, Uttam
发明人： SAHA, Uttam
IPC分类号： C07F9/53 , C07C401/00 , C07F7/18
CPC分类号： C07F7/188 , C07C401/00
摘要： Processes for preparing vitamin D 2 derivatives and intermediates to vitamin D 2 derivatives are disclosed. An improved photolysis process for the preparation of cis intermediate (I) from the trans starting material (II) are disclosed. Also disclosed is an improved process for the formation of a trans double bond at C 22 -C 23 of the vitamin D 2 derivative, which provides high selectivity of the desired trans double bond of compound (III) over the undesired cis double bond of compound (IIIA).
摘要翻译：公开了制备维生素D2衍生物和中间体维生素D 2衍生物的方法。公开了用于从反式起始原料（II）制备顺式中间体（I）的改进的光解方法。还公开了在维生素D 2衍生物的C22-C23上形成反式双键的改进方法，其提供化合物（III）的所需反式双键与化合物（IIIA）的不希望的顺式双键的高选择性，。

8. 发明申请

WO2008146130A1 PROCESS FOR PRODUCING PHOSPHINE OXIDE VITAMIN D PRECURSORS 审中-公开
标题翻译：生产氧化膦维生素D前体的方法
公开(公告)号：WO2008146130A1
公开(公告)日：2008-12-04
申请号：PCT/IB2008/001321
申请日：2008-05-23
申请人： CYTOCHROMA INC. , SAHA, Uttam
发明人： SAHA, Uttam
IPC分类号： C07F9/53
CPC分类号： C07F9/5316 , Y02P20/55
摘要： A process for producing a compound of the formula (structure of formula I ) (I) comprising reacting of a compound of the formula" (structure of formula 2) (2) with diphenyl phosphine oxide using a binary phase reaction mixture comprising diphenyl phosphine oxide in an organic solvent, a basic aqueous solution, and a phase transfer catalyst, to obtain the compound of formula (1), wherein Ph is phenyl, X 1 and X 2 are both hydrogen or X 1 and X 2 taken together is CH 2 , R 1 is a protecting group, R 2 is fluorine, hydrogen or OR3, wherein R 3 is a protecting group, and the squiggly line represents a bond that results in the adjacent double bond being m either the E or Z configuration, is disclosed.
摘要翻译：一种制备式（I）结构的化合物（I）的方法，包括使用包含二苯基氧化膦的二元相反应混合物使式（“式2”）（2）的化合物与二苯基氧化膦反应在有机溶剂，碱性水溶液和相转移催化剂中，得到式（1）化合物，其中Ph为苯基，X1和X2均为氢或X1，X2一起为CH2，R1为保护基基团，R 2是氟，氢或OR 3，其中R 3是保护基，并且波纹线表示导致相邻双键为E或Z构型的键。

9. 发明公开

EP1511725A1 24-SULFOXIMINE VITAMIN D sb 3 /sb COMPOUNDS 有权
标题翻译： 24个亚磺酰亚胺维生素D3衍生物
公开(公告)号：EP1511725A1
公开(公告)日：2005-03-09
申请号：EP03727105.3
申请日：2003-06-13
申请人： Johns Hopkins University , Cytochroma Inc.
发明人： KAHRAMAN, Mehmet , POSNER, Gary, H. , SAHA, Uttam
IPC分类号： C07C401/00 , A61K31/593
CPC分类号： C07C401/00
摘要： The present invention provides novel sulfoximine compounds, compositions comprising these compounds and methods of using these compounds as inhibitors of CYP24. In particular, the compounds of the invention are useful for treating diseases which benefit from a modulation of the levels of 1alpha,25-dihydroxy vitamin D3, for example, cell-proliferative disorders.

10. 发明授权

EP1511725B1 24-SULFOXIMINE VITAMIN D3 COMPOUNDS 有权
标题翻译： 24-SULFOXIMINE VITAMIN D3 DERIVATE
公开(公告)号：EP1511725B1
公开(公告)日：2012-02-01
申请号：EP03727105.3
申请日：2003-06-13
申请人： JOHNS HOPKINS UNIVERSITY , Cytochroma Inc.
发明人： KAHRAMAN, Mehmet , POSNER, Gary, H. , SAHA, Uttam
IPC分类号： C07C401/00 , A61K31/593
CPC分类号： C07C401/00
摘要： The present invention provides novel sulfoximine compounds, compositions comprising these compounds and methods of using these compounds as inhibitors of CYP24. In particular, the compounds of the invention are useful for treating diseases which benefit from a modulation of the levels of 1alpha,25-dihydroxy vitamin D3, for example, cell-proliferative disorders.

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