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1. 发明授权

US08349818B2 Method of preventing Type 1 diabetes 有权
标题翻译：预防1型糖尿病的方法
公开(公告)号：US08349818B2
公开(公告)日：2013-01-08
申请号：US12909253
申请日：2010-10-21
申请人： Hector F. DeLuca , Jamie Nehring , Ehren N. Rudolph , Lori Plum
发明人： Hector F. DeLuca , Jamie Nehring , Ehren N. Rudolph , Lori Plum
IPC分类号： A61K31/59
CPC分类号： A61K31/593
摘要： The invention relates to novel methods of using 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D3 or 2-methylene-19-nor-20(S)-1,25-dihydroxyvitamin D3 to prevent Type 1 diabetes in a subject at risk of developing Type 1 diabetes without causing hypercalcemia in the subject.
摘要翻译：本发明涉及使用2α-甲基-19-nor-20（S）-1α，25-二羟基维生素D 3或2-亚甲基-19-去甲基-2（S）-1,2-二羟基维生素D 3来防止类型 1型糖尿病患有发生1型糖尿病的风险，而不会导致该受试者的高钙血症。

2. 发明申请

US20110124609A1 Method of Preventing Type I Diabetes 有权
标题翻译：预防I型糖尿病的方法
公开(公告)号：US20110124609A1
公开(公告)日：2011-05-26
申请号：US12909253
申请日：2010-10-21
申请人： Hector F. DeLuca , Jamie Nehring , Ehren N. Rudolph , Lori Plum
发明人： Hector F. DeLuca , Jamie Nehring , Ehren N. Rudolph , Lori Plum
IPC分类号： A61K31/593 , A61P3/10
CPC分类号： A61K31/593
摘要： The invention relates to novel methods of using 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D3 or 2-methylene-19-nor-20(S)-1,25-dihydroxyvitamin D3 to prevent Type 1 diabetes in a subject at risk of developing Type 1 diabetes without causing hypercalcemia in the subject.
摘要翻译：本发明涉及使用2α-甲基-19-nor-20（S）-1α，25-二羟基维生素D 3或2-亚甲基-19-去甲基-2（S）-1,2-二羟基维生素D 3来防止类型 1型糖尿病患有发生1型糖尿病的风险，而不会导致该受试者的高钙血症。

3. 发明授权

US08114393B2 Methods and compositions for phosphate binding 有权
标题翻译：用于磷酸盐结合的方法和组合物
公开(公告)号：US08114393B2
公开(公告)日：2012-02-14
申请号：US11974254
申请日：2007-10-12
申请人： Hector F. DeLuca , Katarzyna M. Barycka , Lori Plum , Julia Zella , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Katarzyna M. Barycka , Lori Plum , Julia Zella , Margaret Clagett-Dame
IPC分类号： A61K31/785
CPC分类号： A61K31/785 , C07C59/265 , C07C211/14 , C08G73/0206 , C08L101/005
摘要： The present invention provides improved methods and compositions for therapeutically controlling and/or reducing serum phosphate levels in animals and mammalian patients. The methods comprise administering to the patient an amount of a dendrimer composition effective to prevent absorption of substantial amounts of phosphate from the patient's GI tract. In a preferred version, a dose of between 2.5 and 15 grams per day is effective to prevent over 80% of phosphate present in the patient's GI tract from being absorbed. The dendrimer composition may comprise a hydrocitrate, hydrochloride, hydrobromide, hydroacetate or hydroanionic form.
摘要翻译：本发明提供用于治疗和/或降低动物和哺乳动物患者血清磷酸盐水平的改进方法和组合物。所述方法包括向患者施用一定量的有效防止从患者胃肠道吸收大量磷酸盐的树枝状大分子组合物。在优选的方案中，每日2.5至15克的剂量对于预防患者胃肠道中存在的超过80％的磷酸盐被吸收是有效的。树枝状聚合物组合物可以包含氢化柠檬酸盐，盐酸盐，氢溴酸盐，乙酸氢盐或水阴离子形式。

4. 发明申请

US20090004133A1 Methods and compositions for phosphate binding 有权
标题翻译：用于磷酸盐结合的方法和组合物
公开(公告)号：US20090004133A1
公开(公告)日：2009-01-01
申请号：US11974254
申请日：2007-10-12
申请人： Hector F. DeLuca , Katarzyna M. Barycka , Lori Plum , Julia Zella , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Katarzyna M. Barycka , Lori Plum , Julia Zella , Margaret Clagett-Dame
IPC分类号： A61K31/785 , C08G73/02
CPC分类号： A61K31/785 , C07C59/265 , C07C211/14 , C08G73/0206 , C08L101/005
摘要： The present invention provides improved methods and compositions for therapeutically controlling and/or reducing serum phosphate levels in animals and mammalian patients. The methods comprise administering to the patient an amount of a dendrimer composition effective to prevent absorption of substantial amounts of phosphate from the patient's GI tract. In a preferred version, a dose of between 2.5 and 15 grams per day is effective to prevent over 80% of phosphate present in the patient's GI tract from being absorbed. The dendrimer composition may comprise a hydrocitrate, hydrochloride, hydrobromide, hydroacetate or hydroanionic form.
摘要翻译：本发明提供用于治疗和/或降低动物和哺乳动物患者血清磷酸盐水平的改进方法和组合物。所述方法包括向患者施用一定量的有效防止从患者胃肠道吸收大量磷酸盐的树枝状大分子组合物。在优选的方案中，每日2.5至15克的剂量对于预防患者胃肠道中存在的超过80％的磷酸盐被吸收是有效的。树枝状聚合物组合物可以包含氢化柠檬酸盐，盐酸盐，氢溴酸盐，乙酸氢盐或水阴离子形式。

5. 发明申请

US20110034426A1 Method of Preventing Renal Disease and Treating Symptoms Thereof 审中-公开
标题翻译：预防肾脏疾病和治疗症状的方法
公开(公告)号：US20110034426A1
公开(公告)日：2011-02-10
申请号：US12845173
申请日：2010-07-28
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori Plum
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori Plum
IPC分类号： A61K31/59 , A61P13/12
CPC分类号： A61K31/593
摘要： The invention relates to novel methods of using 2-methylene-19-nor-20(S)-1,25-dihydroxyvitamin D3 to prevent renal disease, particularly Lupus nephritis, in a subject at risk of developing renal disease. Methods of preventing symptoms of renal disease, such as proteinuria, splenomegaly or glomerular damage are also provided. Methods of treating symptoms of renal disease, including proteinuria and splenomegaly, are also provided.
摘要翻译：本发明涉及使用2-亚甲基-19-去甲基-20（S）-1,2,5-二羟基维生素D 3以防止发生肾脏疾病风险的受试者的肾脏疾病，特别是狼疮性肾炎的新方法。还提供了预防肾病症状的方法，例如蛋白尿，脾肿大或肾小球损伤。还提供了治疗肾病症状的方法，包括蛋白尿和脾肿大。

6. 发明授权

US10479764B2 2-methylene-(22E)-25-hexanoyl-24-oxo-26,27-cyclo-22-dehydro-19-nor-vitamin D analogs 有权
公开(公告)号：US10479764B2
公开(公告)日：2019-11-19
申请号：US13533018
申请日：2012-06-26
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Rafal Barycki
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Rafal Barycki
IPC分类号： C07C401/00 , A61K31/593
摘要： This invention discloses 2-methylene-(22E)-25-hexanoyl-24-oxo-26,27-cyclo-22-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-(22E)-25-hexanoyl-24-oxo-26,27-cyclo-22-dehydro-19-nor-1α-hydroxyvitamin 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 low activity in vivo on bone calcium mobilization, 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.

7. 发明授权

US08993547B2 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-维生素D类似物及其用途
公开(公告)号：US08993547B2
公开(公告)日：2015-03-31
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： A61K31/59 , C07C401/00 , C07F9/02 , C07F9/53 , A61K31/593
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。

8. 发明授权

US08987235B2 N-cyclopropyl-(20R)-2-methylene-19,26,27-trinor-25-aza-vitamin D analogs and their uses 有权
标题翻译： N-环丙基 - （20R）-2-亚甲基-19,26,27-三硝基-25-氮杂 - 维生素D类似物及其用途
公开(公告)号：US08987235B2
公开(公告)日：2015-03-24
申请号：US13473259
申请日：2012-05-16
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Grazia Chiellini
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Grazia Chiellini
IPC分类号： A61K31/59 , C07C401/00 , C07C211/03 , C07C271/24 , C07C215/42 , C07C225/10 , C07F7/18
CPC分类号： C07C401/00 , C07C215/42 , C07C225/10 , C07C271/24 , C07C2601/02 , C07C2601/14 , C07C2602/24 , C07F7/1804
摘要： This invention discloses N-cyclopropyl-(20R)-2-methylene-19,26,27-trinor-25-aza-vitamin D analogs, and specifically N-cyclopropyl-(20R)-2-methylene-19,26,27-trinor-25-aza-1α-hydroxyvitamin D3 and pharmaceutical uses therefor. This compound exhibits 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 leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
摘要翻译：本发明公开了N-环丙基 - （20R）-2-亚甲基-19,26,27-三硝基-25-氮杂 - 维生素D类似物，特别是N-环丙基 - （20R）-2-亚甲基-19,26,27 - 紫霉素-25-氮杂-1α-羟基维生素D3及其药物用途。该化合物在阻止未分化细胞的增殖和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明显的活性，从而证明其用作抗癌剂，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。

9. 发明授权

US08609643B2 2-methylene-(20S,25R)-19,26-dinor-vitamin D analogs 有权
标题翻译： 2-二甲基 - （20S，25R）-19,26-二 - 维生素D类似物
公开(公告)号：US08609643B2
公开(公告)日：2013-12-17
申请号：US12343586
申请日：2008-12-24
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Grazia Chiellini , Pawel Grzywacz
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Grazia Chiellini , Pawel Grzywacz
IPC分类号： A61K31/593 , C07C401/00 , A61P17/06 , A61P1/00 , A61P17/00 , A61P37/00
CPC分类号： C07C401/00
摘要： This invention discloses 2-methylene-(20S,25R)-19,26-dinor-vitamin D analogs, and specifically 2-methylene-(20S,25R)-19,26-dinor-1α,25-dihydroxyvitamin D3, 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2-亚甲基 - （20S，25R）-19,26-二 - 维生素D类似物，特别是2-亚甲基 - （20S，25R）-19,26-二牛-1al，25-二羟基维生素D3和药物用它。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。

10. 发明授权

US08404666B2 2-substituted-1α,25-dihydroxy-19,26,27-trinor vitamin D analogs and uses thereof 有权
标题翻译： 2-取代-1α，25-二羟基-19,26,27-三核维生素D类似物及其用途
公开(公告)号：US08404666B2
公开(公告)日：2013-03-26
申请号：US11697434
申请日：2007-04-06
申请人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame , Pawel Grzywacz
发明人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame , Pawel Grzywacz
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： Compounds of formula I, II or III are provided where X1, X2 and X3 are independently selected from H and hydroxy protecting groups and R1 and R2 are independently selected from H or straight or branched chain alkyl groups having from 1 to 8 carbon atoms, straight or branched chain alkenyl groups having from 2 to 8 carbon atoms, straight or branched chain hydroxy-substituted alkyl groups having from 1 to 8 carbon atoms, or straight and branched chain hydroxy-substituted alkenyl groups having from 2 to 8 carbon atoms; and R3 is independently selected from straight or branched chain alkyl groups having from 1 to 8 carbon atoms, straight or branched chain alkenyl groups having from 2 to 8 carbon atoms, straight or branched chain hydroxy-substituted alkyl groups having from 1 to 8 carbon atoms, or straight and branched chain hydroxy-substituted alkenyl groups having from 2 to 8 carbon atoms. 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，II或III的化合物，其中X 1，X 2和X 3独立地选自H和羟基保护基，R 1和R 2独立地选自H或具有1至8个碳原子的直链或支链烷基，直链或具有2至8个碳原子的支链烯基，具有1至8个碳原子的直链或支链羟基取代的烷基，或具有2至8个碳原子的直链和支链羟基取代的烯基; 并且R 3独立地选自具有1至8个碳原子的直链或支链烷基，具有2至8个碳原子的直链或支链烯基，具有1至8个碳原子的直链或支链羟基取代的烷基或具有2至8个碳原子的直链和支链羟基取代的烯基。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。

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