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1. 发明申请

US20070254857A1 2Alpha-Methyl-19-Nor-(20S)-1Alpha-Hydroxy-Bishomopregnacalciferol and Its Uses 有权
标题翻译： 2Aα-甲基-19-诺 - （20S）-1α-羟基 - 二高钙孕激素及其用途
公开(公告)号：US20070254857A1
公开(公告)日：2007-11-01
申请号：US11775074
申请日：2007-07-09
申请人： Hector DeLuca , Rafal Sicinski , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Rafal Sicinski , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , A61P11/06 , A61P17/06 , A61P19/02 , A61P3/00 , A61P3/10 , A61P35/00 , A61P35/02 , C07C401/00
CPC分类号： C07C401/00 , C07F7/1804
摘要： This invention discloses 2α-methyl-19-nor-(20S)-vitamin D analogs, and specifically 2α-methyl-19-nor-(20S)-1α-hydroxy-bishomopregnacalciferol and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
摘要翻译：本发明公开了2α-甲基-19-去甲 - （20S） - 维生素D类似物，特别是2α-甲基-19-去 - （20S）-1α-羟基 - 双代孕代孕甾醇及其药物用途。该化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面表现出显着的活性，从而证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如皱纹，松弛皮肤，皮肤干燥，皮脂分泌不足。该化合物也具有很少（如果有的话）钙活性，因此可用于治疗人体中的自身免疫性疾病或炎性疾病以及肾性骨营养不良。该化合物也可用于治疗或预防肥胖症。

2. 发明申请

US20060148769A1 (20S)-1alpha-hydroxy-2alpha-methyl and 2beta-methyl-19-nor-vitamin D3 and their uses 审中-公开
公开(公告)号：US20060148769A1
公开(公告)日：2006-07-06
申请号：US11374782
申请日：2006-03-14
申请人： Hector DeLuca , Rafal Sicinski , Pawel Grzywacz
发明人： Hector DeLuca , Rafal Sicinski , Pawel Grzywacz
IPC分类号： A61K31/59
CPC分类号： C07C49/433 , A61K31/593 , C07C49/443
摘要： This invention discloses (20S)-1α-hydroxy-2α-methyl-19-nor-vitamin D3 and (20S)-1α-hydroxy-2β-methyl-19-nor-vitamin D3 and pharmaceutical uses therefor. These compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. These compounds also have very significant calcemic activity and therefore may be used to treat immune disorders in humans as well as metabolic bone diseases such as osteoporosis.

3. 发明申请

US20050159397A1 (20S)-1alpha-hydroxy-2alpha-methyl and 2beta-methyl-19-nor-vitamin D3 and their uses 有权
标题翻译：（20S）-1α-羟基-2α-甲基和2b-甲基-19-维生素D3及其用途
公开(公告)号：US20050159397A1
公开(公告)日：2005-07-21
申请号：US11037876
申请日：2005-01-18
申请人： Hector DeLuca , Rafal Sicinski , Pawel Grzywacz
发明人： Hector DeLuca , Rafal Sicinski , Pawel Grzywacz
IPC分类号： A61K31/593 , A61P1/04 , A61P3/10 , A61P11/06 , A61P17/06 , A61P17/16 , A61P19/02 , A61P19/08 , A61P19/10 , A61P25/00 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/06 , C07C49/443 , A61K31/59
CPC分类号： C07C49/433 , A61K31/593 , C07C49/443
摘要： This invention discloses (20S)-1α-hydroxy-2α-methyl-19-nor-vitamin D3 and (20S)-1α-hydroxy-2β-methyl-19-nor-vitamin D3 and pharmaceutical uses therefor. These compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. These compounds also have very significant calcemic activity and therefore may be used to treat immune disorders in humans as well as metabolic bone diseases such as osteoporosis.
摘要翻译：本发明公开了（20S）-1α-羟基-2α-甲基-19-去甲维生素D 3和（20S）-1α-羟基-2β-甲基-19-去甲维生素D _{3 及其制药用途。这些化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面表现出显着的活性，从而证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如皱纹，松弛皮肤，皮肤干燥，皮脂分泌不足。这些化合物还具有非常显着的钙血活性，因此可用于治疗人类的免疫疾病以及代谢性骨疾病如骨质疏松症。}

4. 发明申请

US20050043281A1 2-Ethyl and 2-ethylidene-19-nor-vitamin D compounds 有权
标题翻译： 2-乙基和2-亚乙基-19-去甲维生素D化合物
公开(公告)号：US20050043281A1
公开(公告)日：2005-02-24
申请号：US10957483
申请日：2004-10-01
申请人： Hector DeLuca , Rafal Sicinski
发明人： Hector DeLuca , Rafal Sicinski
IPC分类号： A61K31/593 , A61K31/59 , A61P1/00 , A61P3/10 , A61P5/18 , A61P7/00 , A61P9/10 , A61P9/12 , A61P13/08 , A61P15/00 , A61P17/00 , A61P17/06 , A61P17/14 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/00 , A61P29/00 , A61P35/02 , A61P37/06 , C07C401/00
CPC分类号： A61K31/59 , A61K31/593 , C07C401/00 , Y10S514/824 , Y10S514/861 , Y10S514/863 , Y10S514/866 , Y10S514/903
摘要： Biologically active 19-nor vitamin D analogs substituted at C-2 in the A-ring with an ethylidene or an ethyl group. These compounds have preferential activity on mobilizing calcium from bone and either high or normal intestinal calcium transport activity which allows their in vivo administration for the treatment of metabolic bone diseases where bone loss is a major concern. These compounds are also characterized by high cell differentiation activity.
摘要翻译：在A环中用亚乙基或乙基取代C-2的生物活性的19-或维生素D类似物。这些化合物具有从骨骼中移动钙以及高或正常的钙运输活性的优先活性，其允许其体内施用以治疗骨质流失是主要关注的代谢性骨疾病。这些化合物的特征还在于高细胞分化活性。

5. 发明申请

US20070112077A1 Des-C,D analogs of 1alpha,25-dihydroxy-19-norvitamin D3 有权
标题翻译： 1α，25-二羟基-19-去甲维生素D3的Des-C，D类似物
公开(公告)号：US20070112077A1
公开(公告)日：2007-05-17
申请号：US11512705
申请日：2006-08-30
申请人： Hector DeLuca , Katarzyna Plonska-Ocypa , Rafal Sicinski , Pawel Grzywacz , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Katarzyna Plonska-Ocypa , Rafal Sicinski , Pawel Grzywacz , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/045
CPC分类号： C07C401/00 , C07B2200/07 , C07C35/17 , C07C45/292 , C07C45/30 , C07C47/19 , C07C403/08 , C07C2601/14 , C07F7/1804 , Y02P20/55
摘要： Des-C,D 2-methylene-19-norvitamin D3 analogs are provided including compounds of formula 1, in which R1 is a straight or branched chain alkyl or alkylene group having from 8 to 27 carbons and bearing an Oy3 group; and y1, y2 and y3 are independently selected from H or hydroxy-protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
摘要翻译：提供了包含式1化合物的Des-C，D 2 - 亚甲基-19-去甲维生素D 3 N 3类似物，其中R 1是直链或支链烷基或亚烷基具有8至27个碳并具有Oy 3+基团的基团; 且y 1，y 2和y 3独立地选自H或羟基保护基。这样的化合物可用于制备药物组合物，并且可用于治疗各种生物学条件。

6. 发明申请

US20070088008A1 2-Ethyl and 2-ethylidene-19-nor-vitamin D compounds 有权
标题翻译： 2-乙基和2-亚乙基-19-去甲维生素D化合物
公开(公告)号：US20070088008A1
公开(公告)日：2007-04-19
申请号：US11603721
申请日：2006-11-22
申请人： Hector DeLuca , Rafal Sicinski
发明人： Hector DeLuca , Rafal Sicinski
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： A61K31/59 , A61K31/593 , C07C401/00 , Y10S514/824 , Y10S514/861 , Y10S514/863 , Y10S514/866 , Y10S514/903
摘要： Biologically active 19-nor vitamin D analogs substituted at C-2 in the A-ring with an ethylidene or an ethyl group. These compounds have preferential activity on mobilizing calcium from bone and either high or normal intestinal calcium transport activity which allows their in vivo administration for the treatment of metabolic bone diseases where bone loss is a major concern. These compounds are also characterized by high cell differentiation activity.
摘要翻译：在A环中用亚乙基或乙基取代C-2的生物活性的19-或维生素D类似物。这些化合物具有从骨骼中移动钙以及高或正常的钙运输活性的优先活性，其允许其体内施用以治疗骨质流失是主要关注的代谢性骨疾病。这些化合物的特征还在于高细胞分化活性。

7. 发明申请

US20060293291A1 2-Propylidene-19-nor-vitamin d compounds 审中-公开
标题翻译： 2-亚丙基-19-去甲维生素d化合物
公开(公告)号：US20060293291A1
公开(公告)日：2006-12-28
申请号：US10544163
申请日：2004-04-09
申请人： Hector DeLuca , Rafal Sicinski , Agnieszka Glebocka , Lori Plum
发明人： Hector DeLuca , Rafal Sicinski , Agnieszka Glebocka , Lori Plum
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , C07F7/1804 , Y02P20/55
摘要： 2-propylidene-19-nor-vitamin D compounds are disclosed as well as pharmaceutical uses for these compounds and methods of synthesizing these compounds. These compounds are characterized by high bone calcium mobilization activity and high intestinal calcium transport activity. This results in novel therapeutic agents for the treatment and prophylaxis of diseases where bone formation is desired, particularly osteoporosis, as well as autoimmune diseases such as multiple sclerosis, diabetes mellitus and lupus. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis. These compounds also increase both breaking strength and crushing strength of bones evidencing use in conjunction with bone replacement surgery such as hip and knee replacements.
摘要翻译：公开了2-亚丙基-19-去甲维生素D化合物以及这些化合物的药物用途和合成这些化合物的方法。这些化合物的特征在于高钙钙动员活性和高钙运输活性。这导致用于治疗和预防需要骨形成的疾病，特别是骨质疏松症以及自身免疫性疾病如多发性硬化，糖尿病和狼疮的新型治疗剂。这些化合物在阻止未分化细胞的增殖并诱导其分化成单核细胞方面也表现出显着的活性，因此证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣。这些化合物还增加骨骼的断裂强度和破碎强度，证明与骨替代手术（例如髋关节和膝盖置换）结合使用。

8. 发明申请

US20060079692A1 Synthesis of indole thiazole compounds as ligands for the Ah receptor 有权
公开(公告)号：US20060079692A1
公开(公告)日：2006-04-13
申请号：US11286537
申请日：2005-11-23
申请人： Hector DeLuca , Pawel Grzywacz , Rafal Sicinski
发明人： Hector DeLuca , Pawel Grzywacz , Rafal Sicinski
IPC分类号： C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D403/06 , C07D209/12 , C07D413/06 , C07D417/06
摘要： A method of synthesizing aromatic ketone compositions of formula I comprising the step of introducing a double bond into the 5 membered ring of the 4,5-dihydro-1,3-azoles moiety of formula II is disclosed. A method of synthesizing aromatic ketone compositions of formula I comprising the step of ring synthesis of the tetrahydro-1,3-azoles of formula XI is also disclosed.

9. 发明申请

US20080032956A1 2-Ethyl and 2-Ethylidene-19-Nor-Vitamin D Compounds 有权
标题翻译： 2-乙基和2-亚乙基-19-维生素D化合物
公开(公告)号：US20080032956A1
公开(公告)日：2008-02-07
申请号：US11839586
申请日：2007-08-16
申请人： Hector DeLuca , Rafal Sicinski
发明人： Hector DeLuca , Rafal Sicinski
IPC分类号： A61K31/593 , A61P17/00
CPC分类号： A61K31/59 , A61K31/593 , C07C401/00 , Y10S514/824 , Y10S514/861 , Y10S514/863 , Y10S514/866 , Y10S514/903
摘要： Biologically active 19-nor vitamin D analogs substituted at C-2 in the A-ring with an ethylidene or an ethyl group. These compounds have preferential activity on mobilizing calcium from bone and either high or normal intestinal calcium transport activity which allows their in vivo administration for the treatment of metabolic bone diseases where bone loss is a major concern. These compounds are also characterized by high cell differentiation activity.
摘要翻译：在A环中用亚乙基或乙基取代C-2的生物活性的19-或维生素D类似物。这些化合物具有从骨骼中移动钙以及高或正常的钙运输活性的优先活性，其允许其体内施用以治疗骨质流失是主要关注的代谢性骨疾病。这些化合物的特征还在于高细胞分化活性。

10. 发明申请

US20070213546A1 2-Propylidene-19-nor-vitamin D compounds 有权
标题翻译： 2-异丙基-19-去甲维生素D化合物
公开(公告)号：US20070213546A1
公开(公告)日：2007-09-13
申请号：US11750172
申请日：2007-05-17
申请人： Hector DeLuca , Rafal Sicinski , Agnieszka Glebocka , Lori Plum
发明人： Hector DeLuca , Rafal Sicinski , Agnieszka Glebocka , Lori Plum
IPC分类号： C07C49/543 , C07C401/00
CPC分类号： C07C401/00 , C07F7/1804 , Y02P20/55
摘要： 2-propylidene-19-nor-vitamin D compounds are disclosed as well as pharmaceutical uses for these compounds and methods of synthesizing these compounds. These compounds are characterized by high bone calcium mobilization activity and high intestinal calcium transport activity. This results in novel therapeutic agents for the treatment and prophylaxis of diseases where bone formation is desired, particularly osteoporosis, as well as autoimmune diseases such as multiple sclerosis, diabetes mellitus and lupus. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis. These compounds also increase both breaking strength and crushing strength of bones evidencing use in conjunction with bone replacement surgery such as hip and knee replacements.
摘要翻译：公开了2-亚丙基-19-去甲维生素D化合物以及这些化合物的药物用途和合成这些化合物的方法。这些化合物的特征在于高钙钙动员活性和高钙运输活性。这导致用于治疗和预防需要骨形成的疾病，特别是骨质疏松症以及自身免疫性疾病如多发性硬化，糖尿病和狼疮的新型治疗剂。这些化合物在阻止未分化细胞的增殖并诱导其分化成单核细胞方面也表现出显着的活性，因此证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣。这些化合物还增加骨骼的断裂强度和破碎强度，证明与骨替代手术（例如髋关节和膝盖置换）结合使用。

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