专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2006074227A3 HIGHLY ANTIPROLIFERATIVE, LOW-CALCEMIC, ANALOGS OF THE HORMONE 1a, 25-DIHYDROXYVITAMIN D3 WITH CARBONYL SIDE CHAINS 审中-公开
标题翻译：具有羰基侧链的激素1a，25-二羟维生素D3的高度抗增殖的低剂量类似物
公开(公告)号：WO2006074227A3
公开(公告)日：2006-09-28
申请号：PCT/US2006000183
申请日：2006-01-03
申请人： UNIV JOHNS HOPKINS , POSNER GARY H , SINISHTAJ SANDRA , SUH BYUNG CHUL , KIM HYUNG JIN , LEE S H TONY , ZHANG ZHIYU , JEON HEUNG BAE , KAHRAMAN MEHMET , LI HONGBIN , PETERSEN KIMBERLY
发明人： POSNER GARY H , SINISHTAJ SANDRA , SUH BYUNG CHUL , KIM HYUNG JIN , LEE S H TONY , ZHANG ZHIYU , JEON HEUNG BAE , KAHRAMAN MEHMET , LI HONGBIN , PETERSEN KIMBERLY
IPC分类号： A61K31/593 , C07C401/00
CPC分类号： C07C401/00
摘要： The present invention discloses a series of new carbonyl side chain anlogs of calcitriol (I). Unexpectedly, several of these ketone analogs, such as the 24- and 25-tert-butyl ketones, amides, hydroxymate esters and a hetero atom ketones even though lacking the classical side-chain tertiary hydroxyl group, are considerably more antiproliferative in vitro than the hormone calcitriol (I) even at physiologically relevant low nanomolar concentrations and are less calcemic than calcitriol (I) in vivo.
摘要翻译：本发明公开了一系列新的钙三醇（I）的羰基侧链数据。出乎意料的是，这些酮类似物中的几种，例如24-和25-叔丁基酮，酰胺，羟基酯和杂原子酮（即使缺乏经典的侧链叔羟基），在体外比体外抗增殖要好得多即使在生理学相关的低纳摩尔浓度下，激素钙三醇（I）也比体内钙三醇（I）低。

2. 发明申请

WO2004054968A3 25-SO2-SUBSTITUTED ANALOGS OF 1ALPHA, 25-DIHYDROXYVITAMIN D3 (CALCITRIOL) 审中-公开
标题翻译： 25-SO2取代的1ALPHA，25-二羟基维生素D3（CALCITRIOL）的模拟物
公开(公告)号：WO2004054968A3
公开(公告)日：2004-10-21
申请号：PCT/CA0301926
申请日：2003-12-18
申请人： UNIV JOHNS HOPKINS , 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： A61K31/59 , A61P35/00 , C07C401/00 , A61K31/593
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 lalpha,25-dihydroxyvitamin D3, 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 lalpha,25-dihydroxyvitamin D3, for example, cell-proliferative disorders.
摘要翻译：本发明提供了新型的α，25-二羟基维生素D 3的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。

3. 发明申请

WO03018545B1 24-SULFUR-SUBSTITUTED ANALOGS OF 1 ALPHA ,25-DIHYDROXY VITAMIN D3 审中-公开
标题翻译： 1α，25-二羟基维生素D3的24-硫取代的类似物
公开(公告)号：WO03018545B1
公开(公告)日：2003-07-31
申请号：PCT/CA0201294
申请日：2002-08-22
申请人： UNIV JOHNS HOPKINS , CYTOCHROMA INC , POSNER GARY H , CRAWFORD KENNETH R , YANG HONG WOON , WHITE JAY A , JONES GLENVILLE , SUH BYUNG-CHUL , JEON HEUNGBAE , HATCHER MARK
发明人： POSNER GARY H , CRAWFORD KENNETH R , YANG HONG WOON , WHITE JAY A , JONES GLENVILLE , SUH BYUNG-CHUL , JEON HEUNGBAE , HATCHER MARK
IPC分类号： A61K45/00 , A61K31/593 , A61P5/00 , A61P11/00 , A61P13/08 , A61P15/00 , A61P17/00 , A61P17/06 , A61P19/00 , A61P19/10 , A61P35/00 , A61P43/00 , C07C401/00 , A61K31/59
CPC分类号： C07C401/00
摘要： The present invention provides novel C24-aryl sulfone analogs of 1 alpha ,25-dihydroxy vitamin D3 of formula (I) : wherein R -R have the meanings given in the description, x is 0-2; and represents a single or a double bond, 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 1 alpha ,25-dihydroxy vitamin D3, for example, cell-proliferative disorders.
摘要翻译：本发明提供式（I）的1α，25-二羟基维生素D 3的新型C 24 - 芳基砜类似物：其中R 1 -R 7具有在说明书中给出的含义，x是0-2; 并表示单键或双键，包含这些化合物的组合物以及使用这些化合物作为CYP24的选择性抑制剂的方法。具体而言，本发明化合物可用于治疗受益于调节1α，25-二羟基维生素D3水平（例如细胞增殖性疾病）的疾病。

4. 发明申请

WO2007067333A3 TRIOXANE DIMERS HAVING HIGH ANTICANCER AND LONG-LASTING ANTIMALARIAL ACTIVITIES 审中-公开
标题翻译：具有高反应性和长寿命抗生素活性的三氧化二TIES
公开(公告)号：WO2007067333A3
公开(公告)日：2008-01-31
申请号：PCT/US2006044845
申请日：2006-11-17
申请人： UNIV JOHNS HOPKINS , US GOV HEALTH & HUMAN SERV , POSNER GARY H , PAIK IKHYEON , BORSTNIK KRISTINA , CHANG WONSUK , SINISHTAJ SANDRA , MAIO WILLIAM ANTHONY , D ANGELO JOHN GAETANO , WOODARD LAUREN ELAINE , KALINDA ALVIN SOLOMAN , USERA AIMEE R , HESS LINDSEY CATHERINE , ROSENTHAL ANDREW SCOTT , OH SEONGHO , BAEGE ASTRID C
发明人： POSNER GARY H , PAIK IKHYEON , BORSTNIK KRISTINA , CHANG WONSUK , SINISHTAJ SANDRA , MAIO WILLIAM ANTHONY , D ANGELO JOHN GAETANO , WOODARD LAUREN ELAINE , KALINDA ALVIN SOLOMAN , USERA AIMEE R , HESS LINDSEY CATHERINE , ROSENTHAL ANDREW SCOTT , OH SEONGHO , BAEGE ASTRID C
IPC分类号： A01N43/02 , A61K31/335
CPC分类号： C07D493/14 , A61K47/55 , C07D493/18 , C07D493/22
摘要： The invention provides novel trioxane dimers having formulae III, IV or V: methods for their preparation, pharmaceutical compositions containing these compounds, and methods for treating cancer and/or malaria using these compounds and compositions.
摘要翻译：本发明提供具有式III，IV或V的新型三恶烷二聚体：其制备方法，含有这些化合物的药物组合物，以及使用这些化合物和组合物治疗癌症和/或疟疾的方法。

5. 发明申请

WO2006113990B1 LOW-CALCEMIC 16,23-DIENE 25-OXIME ANALOGS OF 1a ,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：WO2006113990B1
公开(公告)日：2007-04-26
申请号：PCT/CA2006000657
申请日：2006-04-25
申请人： CYTOCHROMA INC , UNIV JOHNS HOPKINS , SAHA UTTAM , POSNER GARY H , KAHRAMAN MEHMET
发明人： SAHA UTTAM , POSNER GARY H , KAHRAMAN MEHMET
IPC分类号： C07C401/00 , A61K31/59
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。

6. 发明申请

WO2006113990A3 LOW-CALCEMIC 16,23-DIENE 25-OXIME ANALOGS OF 1a ,25-DIHYDROXY VITAMIN D3 审中-公开
标题翻译： 1a，25-二羟基维生素D3的低含量16,23-二烯25-肟类似物
公开(公告)号：WO2006113990A3
公开(公告)日：2007-02-22
申请号：PCT/CA2006000657
申请日：2006-04-25
申请人： CYTOCHROMA INC , UNIV JOHNS HOPKINS , SAHA UTTAM , POSNER GARY H , KAHRAMAN MEHMET
发明人： SAHA UTTAM , POSNER GARY H , KAHRAMAN MEHMET
IPC分类号： C07C401/00 , A61K31/59
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D 3的新型16,23-二烯25-肟醚类似物，包含这些化合物的组合物以及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1,25-二羟基维生素D3水平（例如细胞增殖性疾病）的疾病。

7. 发明申请

WO2008131267A3 LOW CALCEMIC, HIGHLY ANTIPROLIFERATIVE, ANALOGS OF CALCITRIOL 审中-公开
标题翻译：低钙化，高抗微生物药物，模拟药物
公开(公告)号：WO2008131267A3
公开(公告)日：2009-01-15
申请号：PCT/US2008060885
申请日：2008-04-18
申请人： UNIV JOHNS HOPKINS , POSNER GARY H , PETERSEN KIMBERLY S , HESS LINDSEY C , GENNA DOUGLAS T , BORELLA SCOTT
发明人： POSNER GARY H , PETERSEN KIMBERLY S , HESS LINDSEY C , GENNA DOUGLAS T , BORELLA SCOTT
IPC分类号： C07C401/00 , A61K31/59 , A61P17/00 , A61P35/00
CPC分类号： C07C401/00 , C07C2601/14 , C07C2601/16 , C07C2602/24 , C07D307/42
摘要： The disclosure provides compounds, compositions and methods using these compounds and compositions to stimulate the differentiation of cells and inhibit excessive cell proliferation of certain cells, including cancer cells and skin cells, which may be useful in the treatment of diseases characterized by abnormal cell proliferation and/or cell differentiation such as leukemia, myelofibrosis and psoriasis without the well known effect on calcium metabolism, which gives rise to hypercalcemia.
摘要翻译：本公开提供使用这些化合物和组合物刺激细胞分化并抑制某些细胞（包括癌细胞和皮肤细胞）的过度细胞增殖的化合物，组合物和方法，其可用于治疗以异常细胞增殖为特征的疾病， /或细胞分化例如白血病，骨髓纤维化和牛皮癣，而没有众所周知的对钙代谢的作用，其引起高钙血症。

8. 发明申请

WO0051554A3 REGULATING SKIN APPEARANCE AND COMPOSITION WITH A FLUORINATED VITAMIN D3 ANALOG COMPOUND 审中-公开
标题翻译：用荧光维生素D3模拟化合物调节皮肤外观和组成
公开(公告)号：WO0051554A3
公开(公告)日：2001-01-11
申请号：PCT/US0005414
申请日：2000-03-01
申请人： UNIV JOHNS HOPKINS , BISSETT DONALD LYNN , POSNER GARY H , LEE JAE KYOO , WANG QIANG , TREJO AMY VIOLET
发明人： BISSETT DONALD LYNN , POSNER GARY H , LEE JAE KYOO , WANG QIANG , TREJO AMY VIOLET
IPC分类号： A61K8/67 , A61Q19/08 , A61K7/48
CPC分类号： A61Q19/08 , A61K8/67
摘要： The present invention relates to topical skin care compositions and methods of their use. Such compositions comprise a fluorinated vitamin D3 analog which is useful for regulating skin condition, especially for regulating the signs of skin aging.
摘要翻译：本发明涉及局部皮肤护理组合物及其使用方法。这样的组合物包含氟化维生素D3类似物，其可用于调节皮肤状况，特别是用于调节皮肤老化的迹象。

9. 发明申请

WO2011088209A3 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：WO2011088209A3
公开(公告)日：2015-09-03
申请号：PCT/US2011021129
申请日：2011-01-13
申请人： CYTOCHROMA INC , UNIV JOHNS HOPKINS , 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 , A61K31/59 , A61K31/592 , A61K31/593 , A61P17/06 , A61P19/10 , A61P35/00 , C07C317/10 , C07C381/10
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。前药可以被设计为具有一种或多种有益的性质，例如CYP24酶的选择性抑制，低钙血症活性和抗增殖活性。具体来说，这些前药是活性维生素D类似物的1-脱氧激素。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，特别是作为前药治疗和/或预防疾病。

10. 发明申请

WO2004028476A3 ARTEMISININ-DERIVED TRIOXANE DIMERS 审中-公开
标题翻译：阿司匹林衍生三溴二异氰酸酯
公开(公告)号：WO2004028476A3
公开(公告)日：2004-07-08
申请号：PCT/US0330612
申请日：2003-09-26
申请人： UNIV JOHNS HOPKINS , POSNER GARY H , SHAPIRO THERESA A , SUR SUROJIT , LABONTE TANZINA , BORSTNIK KRISTINA , PAIK IK-HYEON , MCRINER ANDRES J
发明人： POSNER GARY H , SHAPIRO THERESA A , SUR SUROJIT , LABONTE TANZINA , BORSTNIK KRISTINA , PAIK IK-HYEON , MCRINER ANDRES J
IPC分类号： A61K20060101 , A61K31/335 , A61K31/357 , C07D321/10 , C07D323/04 , C07D407/06 , C07D493/20 , C07D519/00
CPC分类号： C07D493/18
摘要： In only two steps and in 65% overall yield, natural trioxane artemisinin (I) was converted on gram scale into C-10carba trioxane dimer (3). This new, very stable dimer was then transformed easily in one additional step into four different dimers (4-7). Alcohol and diol dimers (4 and 5) and ketone dimer (7) are 10 times more antimalarially potent in vitro than artemisinin (I), and alcohol and diol dimers (4 and 5) are strongly inhibitory but not cytotoxic toward several human cancer cell lines. Water-soluble carboxylic acid derivatives (8a-10c and 12) were easily prepared from dimers (4-6); they are thermally stable even at 60°C for 24 hours, are more orally efficacious as antimalarials than either artelinic acid or sodium artesunate, and have potent and selective anticancer activities. Further derivitization of the alcohol dimers (4 and 17), diol dimer (5) and ketone (7) has produced a number of analogs also antimalarially active in vitro at sub-nanomolar concentrations (most notably: pyridine N-oxides (13, 15, 18, 23, 24 and 25), phosphoric acid triesters (26 and 27), sulfonamide (40) and cyclic carbonate (41)). In addition, dimers (13 and 19) are more efficacious (when administered both orally and i.v.) and less toxic (when administered intraperitoneally to mice as a single dose) than clinically-used sodium artesunate, thereby giving them a better antimalarial therapeutic index than sodium artesunate.
摘要翻译：只有两个步骤，65％的总产率，将天然三烷青蒿素（I）按克标度转化为C-10卡巴三恶烷二聚体（3）。然后将这种新的非常稳定的二聚体在一个额外的步骤中容易地转化成四种不同的二聚体（4-7）。醇和二醇二聚体（4和5）和酮二聚体（7）在体外比青蒿素（I）具有10倍的抗疟药效力，醇和二醇二聚体（4和5）是强烈抑制的，但对几种人类癌细胞没有细胞毒性线。水溶性羧酸衍生物（8a-10c和12）容易由二聚体（4-6）制备; 它们甚至在60℃下热稳定24小时，作为抗疟药物比阿特金酸或青蒿琥酯钠更具口服效力，并且具有有效和选择性的抗癌活性。醇二聚体（4和17），二醇二聚物（5）和酮（7）的进一步衍生产生了许多在亚纳摩尔浓度下体外抗疟活性的类似物（最引人注目的是：吡啶N-氧化物（13,15 ，18,23,24和25），磷酸三酯（26和27），磺酰胺（40）和环状碳酸酯（41））。此外，二聚体（13和19）比临床使用的青蒿琥酯钠更有效（当口服和静脉内施用）和毒性较小（当以单剂量腹膜内给予小鼠时），从而给予它们更好的抗疟治疗指数青蒿琥酯钠。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式