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1. 发明授权

US08754067B2 22-haloacetoxy-homopregnacalciferol analogs and their uses 有权
标题翻译： 22-卤代乙酰氧基 - 同孕孕甾醇类似物及其用途
公开(公告)号：US08754067B2
公开(公告)日：2014-06-17
申请号：US13294524
申请日：2011-11-11
申请人： Hector F. DeLuca , Rafal Barycki , Lori A. Plum
发明人： Hector F. DeLuca , Rafal Barycki , Lori A. Plum
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , C07C2601/14 , C07C2602/24 , C07F7/1804
摘要： This invention discloses 22-haloacetoxy-homopregnacalciferol analogs and specifically 22-bromoacetoxy-homopregnacalciferol and pharmaceutical uses therefor. This compound exhibits relatively little calcemic activity and does not promote cellular differentiation off HL-60 leukemia cells, but rather kills the cells. This cell death activity is found in small cell lung carcinoma also, but not in prostate cancer cells. This compound thus causes specific cell death in the absence of changes in calcium levels and without general toxicity in an animal. Therefore it might serve as a useful therapy for treatment of some forms of cancer, such as leukemia and lung cancer.
摘要翻译：本发明公开了22-卤代乙酰氧基 - 孕代孕甾醇类似物，特别是22-溴代乙酰氧基 - 孕代孕甾醇和其药物用途。该化合物显示相对较少的钙血症活性，并且不促进HL-60白血病细胞的细胞分化，而是杀死细胞。这种细胞死亡活动也存在于小细胞肺癌中，但不在前列腺癌细胞中发现。因此，该化合物在没有钙水平的变化并且在动物中没有一般毒性的情况下引起特异性细胞死亡。因此，它可能是治疗某些形式的癌症（如白血病和肺癌）的有用治疗方法。

2. 发明授权

US08575136B2 2-methylene-1α-hydroxy-18,19,21-trinorvitamin D3 analogs and uses thereof 有权
标题翻译： 2-亚甲基-1α-羟基-18,19,21-三维生素D3类似物及其用途
公开(公告)号：US08575136B2
公开(公告)日：2013-11-05
申请号：US11697414
申请日：2007-04-06
申请人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame , Rafal Barycki
发明人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame , Rafal Barycki
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： Compounds of formula I are provided where X1 and X2 are independently selected from H or hydroxy protecting groups. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
摘要翻译：提供式I化合物，其中X 1和X 2独立地选自H或羟基保护基。这些化合物用于制备药物组合物，并且可用于治疗各种生物学条件。

3. 发明授权

US08445468B2 (20S,22E)-2-methylene-19-nor-22-ene-1α,25-dihydroxyvitamin D3 有权
标题翻译：（20S，22E）-2-亚甲基-19-去甲-22-烯-1α，25-二羟基维生素D 3
公开(公告)号：US08445468B2
公开(公告)日：2013-05-21
申请号：US12895390
申请日：2010-09-30
申请人： Hector F. DeLuca , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/593 , C07C401/00
CPC分类号： C07C401/00
摘要： This invention discloses (20S,22E)-2-methylene-19-nor-22-ene-1α,25-dihydroxyvitamin D3 analogs, and specifically(20S,22E)-2-methylene-19-nor-22-ene-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits significant vitamin D receptor binding activity and transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent, especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
摘要翻译：本发明公开了（20S，22E）-2-亚甲基-19-去甲-22-烯-1α，25-二羟基维生素D 3类似物，特别是（20S，22E）-2-亚甲基-19-去甲-22-烯-1α ，25-二羟基维生素D3及其药物用途。该化合物表现出显着的维生素D受体结合活性和转录活性，以及阻止未分化细胞增殖并诱导其分化为单核细胞的显着活性，因此证明其用作抗癌剂，特别是用于治疗或预防白血病，结肠癌，乳腺癌，皮肤癌或前列腺癌。

4. 发明申请

US20120322775A1 3-Desoxy-2-Methylene-19-Nor-Vitamin D Analogs and Their Uses 有权
标题翻译： 3-脱氧-2-亚甲基-19-不维生素D类似物及其用途
公开(公告)号：US20120322775A1
公开(公告)日：2012-12-20
申请号：US13495548
申请日：2012-06-13
申请人： Hector F. DeLuca , Lori A. Plum , Rafal R. Sicinski , Izabela Sibilska , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Lori A. Plum , Rafal R. Sicinski , Izabela Sibilska , Margaret Clagett-Dame
IPC分类号： A61K31/593 , A61P35/00 , C07F9/53 , A61P19/10 , A61P19/08 , C07C401/00 , A61P35/02
CPC分类号： C07F9/5325 , A61K31/593 , C07C401/00 , C07C2601/14 , C07C2602/24 , C07F9/53
摘要： This invention discloses 3-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-3-desoxy-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3 and (20R)-3-desoxy-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3 as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to monocytes thus evidencing use as anti-cancer agents especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also exhibit relatively high calcemic activity evidencing use in the treatment of bone diseases.
摘要翻译：本发明公开了3-脱氧-2-亚甲基-19-去甲维生素D类似物，特别是（20S）-3-脱氧-2-亚甲基-1α，25-二羟基-19-去甲维生素D3和（20R） - 3-脱氧-2-亚甲基-1α，25-二羟基-19-去甲维生素D3以及其用途。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相对较高的结合活性和显着的活性，从而证明其用作抗癌剂，特别是用于治疗或预防骨肉瘤，白血病，结肠癌，乳腺癌，皮肤癌或前列腺癌。这些化合物还表现出相对较高的钙摄取活性，其用于治疗骨疾病。

5. 发明授权

US08217023B2 19-nor-vitamin D analogs with 1,2- or 3,2-cyclopentene ring 有权
标题翻译：具有1,2-或3,2环戊烯环的19-维生素D类似物
公开(公告)号：US08217023B2
公开(公告)日：2012-07-10
申请号：US12895540
申请日：2010-09-30
申请人： Hector F. DeLuca , Agnieszka Glebocka , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski
发明人： Hector F. DeLuca , Agnieszka Glebocka , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00
摘要： 19-nor-vitamin D analogs having an additional cyclopentene ring connecting carbon 1 and carbon 2, or connecting carbon 3 and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit selective in vitro activities, making them therapeutic agents for the treatment or prophylaxis of some types of cancers, particularly leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
摘要翻译：描述了具有连接碳1和碳2的附加环戊烯环或者连接类似物的A环的碳3和碳-2的19-维生素D类似物以及药用。这些化合物显示出选择性的体外活性，使其成为治疗或预防某些类型癌症，特别是白血病，结肠癌，乳腺癌，皮肤癌或前列腺癌的治疗剂。

6. 发明申请

US20120157418A1 2-Methylene-19-Nor-Vitamin D Analogs and Their Uses 有权
标题翻译： 2-亚甲基-19-维生素D类似物及其用途
公开(公告)号：US20120157418A1
公开(公告)日：2012-06-21
申请号：US13278846
申请日：2011-10-21
申请人： Hector F. DeLuca , Izabela Sibilska , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski , Katarzyna M. Barycka , Katarzyna Plonska-Ocypa , Rafal Barycki
发明人： Hector F. DeLuca , Izabela Sibilska , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski , Katarzyna M. Barycka , Katarzyna Plonska-Ocypa , Rafal Barycki
IPC分类号： A61K31/593 , C07F7/18 , C07F9/53 , A61P35/02 , A61P19/08 , A61P19/10 , C07C401/00 , A61P35/00
CPC分类号： C07C401/00 , C07F7/1804 , C07F9/5325
摘要： This invention discloses 2-methylene-19-nor-vitamin D analogs, and specifically (20S)-25-hydroxy-2-methylene-19-nor-vitamin D3 and (20R)-25-hydroxy-2-methylene-19-nor-vitamin D3, as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. Although these compounds have relatively low calcemic activities they may also be useful in the treatment of bone diseases due to their ability to act as prodrugs in vivo.
摘要翻译：本发明公开了2-亚甲基-19-去甲维生素D类似物，特别是（20S）-25-羟基-2-亚甲基-19-去甲维生素D3和（20R）-25-羟基-2-亚甲基-19- 维生素D3，以及其用途。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相对较高的结合活性和显着的活性，从而证明其用作抗癌剂，特别是用于治疗或预防骨肉瘤，白血病，结肠癌，乳腺癌，皮肤癌或前列腺癌。虽然这些化合物具有相对较低的血钙活性，但是由于它们在体内作为前药的能力，它们也可用于治疗骨骼疾病。

7. 发明申请

US20110086824A1 (20S,22E)-2-Methylene-19-Nor-22-Ene-1Alpha,25-Dihydroxyvitamin D3 有权
标题翻译：（20S，22E）-2-亚甲基-19-壬-22-Ene-1Alpha，25-二羟基维生素D 3
公开(公告)号：US20110086824A1
公开(公告)日：2011-04-14
申请号：US12895390
申请日：2010-09-30
申请人： Hector F. DeLuca , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/593 , C07C35/21 , A61P35/00
CPC分类号： C07C401/00
摘要： This invention discloses (20S,22E)-2-methylene-19-nor-22-ene-1α,25-dihydroxyvitamin D3 analogs, and specifically(20S,22E)-2-methylene-19-nor-22-ene-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits significant vitamin D receptor binding activity and transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent, especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
摘要翻译：本发明公开了（20S，22E）-2-亚甲基-19-去甲-22-烯-1α，25-二羟基维生素D3类似物，特别是（20S，22E）-2-亚甲基-19-去甲-22-烯-1α ，25-二羟基维生素D3及其药物用途。该化合物表现出显着的维生素D受体结合活性和转录活性，以及阻止未分化细胞增殖并诱导其分化为单核细胞的显着活性，因此证明其用作抗癌剂，特别是用于治疗或预防白血病，结肠癌，乳腺癌，皮肤癌或前列腺癌。

8. 发明申请

US20110082122A1 19-Nor-Vitamin D Analogs With 1,2- or 3,2-Cyclopentene Ring 有权
标题翻译： 19-维生素D类似物与1,2-或3,2环戊烯环
公开(公告)号：US20110082122A1
公开(公告)日：2011-04-07
申请号：US12895540
申请日：2010-09-30
申请人： Hector F. DeLuca , Agnieszka Glebocka , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski
发明人： Hector F. DeLuca , Agnieszka Glebocka , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski
IPC分类号： A61K31/59 , C07C49/633 , C07F7/08 , C07C35/23 , A61P35/00 , A61P35/02
CPC分类号： C07C401/00
摘要： 19-nor-vitamin D analogs having an additional cyclopentene ring connecting carbon 1 and carbon 2, or connecting carbon 3 and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit selective in vitro activities, making them therapeutic agents for the treatment or prophylaxis of some types of cancers, particularly leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
摘要翻译：描述了具有连接碳1和碳2的附加环戊烯环或者连接类似物的A环的碳3和碳-2的19-维生素D类似物以及药用。这些化合物显示出选择性的体外活性，使其成为治疗或预防某些类型癌症，特别是白血病，结肠癌，乳腺癌，皮肤癌或前列腺癌的治疗剂。

9. 发明授权

US07888339B2 2-methylene-20(21)-dehydro-19-nor-vitamin D analogs 有权
标题翻译： 2-亚甲基-20（21） - 脱氢-19-去甲维生素D类似物
公开(公告)号：US07888339B2
公开(公告)日：2011-02-15
申请号：US12171056
申请日：2008-07-10
申请人： Hector F. DeLuca , Bulli Padmaja Tadi , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Bulli Padmaja Tadi , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00
摘要： This invention discloses 2-methylene-20(21)-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-20(21)-dehydro-19-nor-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits relatively high transcription activity as well as 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 shows lower activity in vivo on bone calcium mobilization and similar in vivo intestinal calcium transport activity compared to the native hormone 1α,25-dihydroxyvitamin D3, 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2-亚甲基-20（21） - 脱氢-19-去甲维生素D类似物，特别是2-亚甲基-20（21） - 脱氢-19-去甲-17α-二羟基维生素D 3及其药物用途。该化合物显示相对较高的转录活性以及阻止未分化细胞增殖并诱导其分化为单核细胞的明显活性，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，皮肤松弛，皮肤干燥和皮脂分泌不足。与天然激素1α，25-二羟基维生素D3相比，该化合物在骨钙动员和体内肠钙运输活性方面的体内活性也较低，因此可用于治疗人体以及肾脏中的自身免疫疾病或炎性疾病骨营养不良。该化合物也可用于治疗或预防肥胖症。

10. 发明授权

US07879829B2 19-nor-vitamin D analogs with 1,2-dihydrofuran ring 有权
标题翻译： 19-维生素D类似物与1,2-二氢呋喃环
公开(公告)号：US07879829B2
公开(公告)日：2011-02-01
申请号：US12171103
申请日：2008-07-10
申请人： Hector F. DeLuca , Agnieszka Glebocka , Katarzyna Sokolowska , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Agnieszka Glebocka , Katarzyna Sokolowska , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07C401/00 , C07D317/00
CPC分类号： C07D307/79
摘要： 19-nor-vitamin D analogs having an additional dihydrofuran ring connecting the 1α-oxygen and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit selective in vitro and in vivo activities, making them therapeutic agents for the treatment or prophylaxis of autoimmune diseases, some types of cancers, secondary hyperparathyroidism, psoriasis, or other skin diseases.
摘要翻译：描述了具有连接类似物的A环的1α-氧和碳-2的另外的二氢呋喃环的19-维生素D类似物和药物用途。这些化合物表现出选择性的体外和体内活性，使其成为治疗或预防自身免疫性疾病，某些类型的癌症，继发性甲状旁腺功能亢进，银屑病或其它皮肤疾病的治疗剂。

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