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1. 发明申请

WO2007117544A3 CARNITINE CONJUGATES OF ADAMANTANAMINES AND NERAMEXANE DERIVATIVES AS DUEL PRODRUGS FOR VARIOUS USES 审中-公开
标题翻译：作为多种用途的胶原蛋白的新戊酰胺和NERAMEXANE衍生物的卡尼宁
公开(公告)号：WO2007117544A3
公开(公告)日：2008-09-04
申请号：PCT/US2007008477
申请日：2007-04-04
申请人： SSV THERAPEUTICS INC , GOEL OM P
发明人： GOEL OM P
IPC分类号： A61K31/21 , A61K31/16 , A61K31/215 , A61K31/24 , C07C69/608 , C07C69/612 , C07C69/616 , C07C235/34
CPC分类号： C07C233/06 , C07C237/04 , C07C2601/14 , C07C2603/74
摘要： This invention concerns compounds of adamantanamines and neramexane, including their pharmaceutical ly-acceptable salts, diesterioisomers, and formulations for treating Alzheimer's related dementias, depression, AIDS related dementias, as antivirals, inflammatory diseases such as rheumatoid arthritis, and cerebral ischemia, hyperlipidemia, and diabetes.
摘要翻译：本发明涉及金刚烷胺和奈拉美生的化合物，包括其药学上可接受的盐，二酯异构体和用于治疗阿尔茨海默病相关的痴呆症，抑郁症，艾滋病相关的痴呆症，作为抗病毒剂，炎性疾病如类风湿性关节炎和脑缺血，高脂血症和糖尿病。

2. 发明申请

WO2008018877A1 CARNITINE CONJUGATES AS DUAL PRODRUGS, METHODS OF PRODUCTION AND USES THEREOF 审中-公开
标题翻译： CARNITINE作为双重原料，其生产方法及其用途
公开(公告)号：WO2008018877A1
公开(公告)日：2008-02-14
申请号：PCT/US2006/031362
申请日：2006-08-11
申请人： SSV THERAPEUTICS, INC. , GOEL, Om, P.
发明人： GOEL, Om, P.
IPC分类号： A61K31/205
CPC分类号： A61K31/205
摘要： The present invention discloses novel dual prodrug compounds of formula (1), methods for their preparation and intermediates in their syntheses, formula (1): wherein A is a single bond, -0-, or -CH 2 -; m and n vary independently and are an integer from 1 to 15; p and q vary from 0 to an integer from 1 to 4; B is a single bond or -CR 3 R 4 ; D is formula (2): or formula (3): and X is halogen; R 1 to R 4 are various substituents selected to optimize the physiochemical and biological properties such as, lipophilicity, bioavailability, and pharmacokinetics of compounds of Formula 1; and R 1 and R 2 or R 3 and R 4 may optionally be tethered together to form a 3- to 7-membered alicyclic ring. These compounds are useful for the treatment of various infections, metabolic, cardiovascular and neurological disorders.
摘要翻译：本发明公开了式（1）的新型双重前药化合物，其制备方法及其合成中间体，式（1）：其中A为单键，-O-或-CH 2 > - ; m和n独立地是1〜15的整数; p和q从0变化到1到4的整数; B是单键或-CR 3 S 4 S 4。 D为式（2）：或式（3）：X为卤素; R 1至R 4是选择用于优化式1化合物的物理化学和生物学性质如亲脂性，生物利用度和药代动力学的各种取代基; 且R 1和R 2或R 3和R 4和R 4可任选地连接在一起以形成3- 至7元脂环。这些化合物可用于治疗各种感染，代谢，心血管和神经障碍。

3. 发明申请

WO2008103421A1 ADAMANTANAMINES AND NERAMEXANE SALTS OF THIOMOLYBDIC AND THIOTUNGSTIC ACIDS 审中-公开
标题翻译：三羟甲基氨基甲酸和十二烷酸的盐酸铵
公开(公告)号：WO2008103421A1
公开(公告)日：2008-08-28
申请号：PCT/US2008/002308
申请日：2008-02-21
申请人： SSV THERAPEUTICS, INC. , GOEL, Om, P.
发明人： GOEL, Om, P.
IPC分类号： A01N55/02 , A61K31/28
CPC分类号： C07C211/63 , C07C2601/14 , C07C2603/74
摘要： This invention concerns adamantanamines (e.g. memantine, amantadine, and rimantadine) and neramexane salts of thiomolybdic and thiotungstic acids, including their preparation and pharmaceutical compositions, as dual acting drugs. These salts are used to treat or potentially arrest the neurodegenerative pathophysiology, clinical signs and symptoms of dementia of the Alzheimer's type, Parkinson's, Huntington's, AIDS-related dementia and Schizophrenia and its cognitive deficits. Additional uses of these derivatives include antiviral activity. The novel compositions of the present invention appear particularly useful in enhancing the therapeutic benefits of copper-sequestering tetrathiomolybdates in treating elevated copper-induced toxicities in neurologically presenting Wilson's disease, and in treating diseases of the inflammatory etiology and abnormal copper biochemistry, such as tumor angiogenesis, liver cirrhosis, hepatitis, pulmonary fibrosis and other fibrotic diseases, cardiovascular disease, cerebral ischemia, renal anemia, rheumatoid arthritis, diabetes, obesity, gastrointestinal disorders, and eye diseases such as glaucoma, proliferative diabetic retinopathy, and age related macular degeneration. These compounds have excellent stability and aqueous solubility for good oral bioavailability.
摘要翻译：本发明涉及硫代钼酸和硫代酸的金刚烷胺（例如美金刚，金刚烷胺和金刚乙胺）和奈拉美生盐，包括它们的制备和药物组合物，作为双作用药物。这些盐用于治疗或潜在地阻止阿尔茨海默氏症，帕金森氏症，亨廷顿舞蹈症，艾滋病相关性痴呆和精神分裂症及其认知缺陷的神经变性病理生理学，临床症状和痴呆症状。这些衍生物的其它用途包括抗病毒活性。本发明的新型组合物特别可用于增强铜螯合四硫钼酸盐在治疗神经性呈现威尔逊氏症中升高的铜诱导毒性以及治疗炎性病因学和异常铜生物化学疾病如肿瘤血管生成中的治疗益处，肝硬化，肝炎，肺纤维化等纤维化疾病，心血管疾病，脑缺血，肾性贫血，类风湿性关节炎，糖尿病，肥胖症，胃肠道疾病和眼部疾病如青光眼，增殖性糖尿病性视网膜病变和年龄相关性黄斑变性。这些化合物具有优异的稳定性和水溶性，以获得良好的口服生物利用度。

4. 发明申请

WO2008100418A1 ZINC COMPLEXES OF NATURAL AMINO ACIDS FOR TREATING ELEVATED COPPER CAUSED TOXICITIES 审中-公开
标题翻译：自然氨基酸的锌化合物用于治疗高胆固醇引起的毒性
公开(公告)号：WO2008100418A1
公开(公告)日：2008-08-21
申请号：PCT/US2008/001674
申请日：2008-02-08
申请人： SSV THERAPEUTICS, INC. , GOEL, Om, P.
发明人： GOEL, Om, P.
IPC分类号： A61K31/315
CPC分类号： A61K31/315 , A61K9/0095 , A61K9/4858 , C07C229/08 , C07C229/26 , C07C279/14 , C07D207/16 , C07D209/20 , C07D233/64
摘要： The present invention relates to formulations of zinc complexes of natural amino acids, especially L-arginine, L-lysine, L-ornithine, and other natural amino acids, in a molar ratio of about 1 :2 (metal :amino acid), and compositions thereof. These pharmaceutical compositions offer better tolerated and faster acting regimens than common zinc salts (i.e., acetate, sulfate, etc.) for long term maintenance therapy of diseases caused by abnormal elevated copper levels, such as in Wilson's disease, inflammatory and fibrotic diseases and Alzheimer's disease.
摘要翻译：本发明涉及摩尔比约为1:2（金属：氨基酸）的天然氨基酸，特别是L-精氨酸，L-赖氨酸，L-鸟氨酸和其他天然氨基酸的锌络合物的配方，以及的组合物。这些药物组合物比普通锌盐（即乙酸盐，硫酸盐等）具有更好的耐受性和更快速的作用方案，用于长期维持治疗由异常升高的铜水平引起的疾病，如威尔逊病，炎症和纤维化疾病和阿尔茨海默病疾病。

5. 发明申请

WO2007117544A2 CARNITINE CONJUGATES OF ADAMANTANAMINES AND NERAMEXANE DERIVATIVES AS DUEL PRODRUGS FOR VARIOUS USES 审中-公开
标题翻译：作为多种用途的胶原蛋白的新戊酰胺和NERAMEXANE衍生物的卡尼宁
公开(公告)号：WO2007117544A2
公开(公告)日：2007-10-18
申请号：PCT/US2007/008477
申请日：2007-04-04
申请人： SSV THERAPEUTICS, INC. , GOEL, Om, P.
发明人： GOEL, Om, P.
IPC分类号： C07C237/14
CPC分类号： C07C233/06 , C07C237/04 , C07C2601/14 , C07C2603/74
摘要： This invention concerns compounds of adamantanamines and neramexane, including their pharmaceutical ly-acceptable salts, diesterioisomers, and formulations for treating Alzheimer's related dementias, depression, AIDS related dementias, as antivirals, inflammatory diseases such as rheumatoid arthritis, and cerebral ischemia, hyperlipidemia, and diabetes.
摘要翻译：本发明涉及金刚烷胺和奈拉美生的化合物，包括其药学上可接受的盐，二酯异构体和用于治疗阿尔茨海默病相关的痴呆症，抑郁症，艾滋病相关的痴呆症，作为抗病毒剂，炎性疾病如类风湿性关节炎和脑缺血，高脂血症和糖尿病。

6. 发明公开

EP2117315A1 ADAMANTANAMINES AND NERAMEXANE SALTS OF THIOMOLYBDIC AND THIOTUNGSTIC ACIDS 审中-公开
标题翻译：硫代乙酰胺和硫代酸的鸟嘌呤胺和Neramxane盐
公开(公告)号：EP2117315A1
公开(公告)日：2009-11-18
申请号：EP08725898.4
申请日：2008-02-21
申请人： SSV Therapeutics, Inc.
发明人： GOEL, Om, P.
IPC分类号： A01N55/02 , A61K31/28
CPC分类号： C07C211/63 , C07C2601/14 , C07C2603/74
摘要： This invention concerns adamantanamines (e.g. memantine, amantadine, and rimantadine) and neramexane salts of thiomolybdic and thiotungstic acids, including their preparation and pharmaceutical compositions, as dual acting drugs. These salts are used to treat or potentially arrest the neurodegenerative pathophysiology, clinical signs and symptoms of dementia of the Alzheimer's type, Parkinson's, Huntington's, AIDS-related dementia and Schizophrenia and its cognitive deficits. Additional uses of these derivatives include antiviral activity. The novel compositions of the present invention appear particularly useful in enhancing the therapeutic benefits of copper-sequestering tetrathiomolybdates in treating elevated copper-induced toxicities in neurologically presenting Wilson's disease, and in treating diseases of the inflammatory etiology and abnormal copper biochemistry, such as tumor angiogenesis, liver cirrhosis, hepatitis, pulmonary fibrosis and other fibrotic diseases, cardiovascular disease, cerebral ischemia, renal anemia, rheumatoid arthritis, diabetes, obesity, gastrointestinal disorders, and eye diseases such as glaucoma, proliferative diabetic retinopathy, and age related macular degeneration. These compounds have excellent stability and aqueous solubility for good oral bioavailability.
摘要翻译：本发明涉及作为双作用药物的金刚胺（例如美金刚胺，金刚烷胺和金刚乙胺）和硫代钼酸和硫代钨酸的奈拉美生盐，包括它们的制剂和药物组合物。这些盐用于治疗或潜在地抑制阿尔茨海默型，帕金森氏病，亨廷顿舞蹈病，AIDS相关性痴呆和精神分裂症及其认知缺陷的痴呆的神经变性病理生理学，临床体征和症状。这些衍生物的其他用途包括抗病毒活性。本发明的新型组合物似乎特别有用于增强铜螯合四硫代钼酸盐在治疗神经学呈现的威尔逊氏病中铜诱导的毒性升高以及治疗炎性病因学和异常铜生物化学疾病如肿瘤血管生成，肝硬化，肝炎，肺纤维化和其他纤维化疾病，心血管疾病，脑缺血，肾性贫血，类风湿性关节炎，糖尿病，肥胖症，胃肠疾病和眼病例如青光眼，增殖性糖尿病视网膜病和年龄相关性黄斑变性。这些化合物具有优异的稳定性和水溶性，具有良好的口服生物利用度

7. 发明授权

US08247398B2 Zinc complexes of natural amino acids for treating elevated copper caused toxicities 有权
标题翻译：用于治疗升高的铜的天然氨基酸锌络合物引起毒性
公开(公告)号：US08247398B2
公开(公告)日：2012-08-21
申请号：US11707329
申请日：2007-02-17
申请人： Om P. Goel
发明人： Om P. Goel
IPC分类号： A01N55/02 , A01N43/76 , A61K31/41
CPC分类号： A61K31/315 , A61K9/0095 , A61K9/4858 , C07C229/08 , C07C229/26 , C07C279/14 , C07D207/16 , C07D209/20 , C07D233/64
摘要： The present invention relates to the use of zinc complexes of natural amino acids, especially L-arginine, L-lysine, L-ornithine, and other natural amino acids, in a molar ratio of about 1:2 (metal:amino acid), and formulations thereof. These pharmaceutical compositions offer better tolerated and faster acting regimens than common zinc salts (i.e., acetate, sulfate, etc.) for long term maintenance therapy of diseases caused by abnormal elevated copper levels, such as in Wilson's disease, inflammatory and fibrotic diseases and Alzheimer's disease.
摘要翻译：本发明涉及天然氨基酸锌配合物，特别是L-精氨酸，L-赖氨酸，L-鸟氨酸等天然氨基酸，其摩尔比为约1:2（金属：氨基酸），及其制剂。这些药物组合物比普通锌盐（即乙酸盐，硫酸盐等）具有更好的耐受性和更快速的作用方案，用于长期维持治疗由异常升高的铜水平引起的疾病，如威尔逊病，炎症和纤维化疾病和阿尔茨海默病疾病。

8. 发明申请

US20090246267A1 Carnitine Conjugates of Adamantanamines and Neramexane Derivatives as Dual Prodrugs for Various Uses 失效
标题翻译：金刚烷胺和Neramexane衍生物的肉碱结合物作为各种用途的双重前药
公开(公告)号：US20090246267A1
公开(公告)日：2009-10-01
申请号：US11992907
申请日：2007-04-04
申请人： Om P. Goel
发明人： Om P. Goel
IPC分类号： A61K9/127 , C07C233/05 , A61K31/16 , C07C69/757 , A61K31/215 , A61P3/10
CPC分类号： C07C233/06 , C07C237/04 , C07C2601/14 , C07C2603/74
摘要： This invention concerns compounds of adamantanamines and neramexane, including their pharmaceutically-acceptable salts, diesterioisomers, and formulations for treating Alzheimer's related dementias, depression, AIDS related dementias, as antivirals, inflammatory diseases such as rheumatoid arthritis, and cerebral ischemia, hyperlipidemia, and diabetes.
摘要翻译：本发明涉及金刚烷胺和奈拉美生的化合物，包括其药学上可接受的盐，二酯异构体和用于治疗阿尔茨海默病相关的痴呆症，抑郁症，艾滋病相关的痴呆症，抗病毒剂，炎性疾病如类风湿性关节炎和脑缺血，高脂血症和糖尿病的制剂。

9. 发明申请

US20080200443A1 Zinc complexes of natural amino acids for treating elevated copper caused toxicities 有权
标题翻译：用于治疗升高的铜的天然氨基酸锌络合物引起毒性
公开(公告)号：US20080200443A1
公开(公告)日：2008-08-21
申请号：US11707329
申请日：2007-02-17
申请人： Om P. Goel
发明人： Om P. Goel
IPC分类号： A61K31/555 , A61P25/28 , A61P29/00
CPC分类号： A61K31/315 , A61K9/0095 , A61K9/4858 , C07C229/08 , C07C229/26 , C07C279/14 , C07D207/16 , C07D209/20 , C07D233/64
摘要： The present invention relates to the use of zinc complexes of natural amino acids, especially L-arginine, L-lysine, L-ornithine, and other natural amino acids, in a molar ratio of about 1:2 (metal:amino acid), and formulations thereof. These pharmaceutical compositions offer better tolerated and faster acting regimens than common zinc salts (i.e., acetate, sulfate, etc.) for long term maintenance therapy of diseases caused by abnormal elevated copper levels, such as in Wilson's disease, inflammatory and fibrotic diseases and Alzheimer's disease.
摘要翻译：本发明涉及天然氨基酸锌配合物，特别是L-精氨酸，L-赖氨酸，L-鸟氨酸等天然氨基酸，其摩尔比为约1:2（金属：氨基酸），及其制剂。这些药物组合物比普通锌盐（即乙酸盐，硫酸盐等）具有更好的耐受性和更快速的作用方案，用于长期维持治疗由异常升高的铜水平引起的疾病，如威尔逊病，炎症和纤维化疾病和阿尔茨海默病疾病。

10. 发明申请

US20110212166A1 CARNITINE CONJUGATES OF ADAMANTANAMINES DERIVATIVES AS DUAL PRODRUGS FOR VARIOUS USES 失效
标题翻译：亚胺丹衍生物作为各种用途的双重制剂的结合
公开(公告)号：US20110212166A1
公开(公告)日：2011-09-01
申请号：US13103053
申请日：2011-05-07
申请人： Om P. Goel
发明人： Om P. Goel
IPC分类号： A61K9/127 , A61K31/16 , C07C237/14 , A61P25/28 , A61P31/12 , A61P19/02 , A61P3/06 , A61P3/10 , C07C229/14 , A61K31/216
CPC分类号： C07C233/06 , C07C237/04 , C07C2601/14 , C07C2603/74
摘要： This invention concerns compounds of adamantanamines and neramexane, including their pharmaceutically-acceptable salts, diesterioisomers, and formulations for treating Alzheimer's related dementias, depression, AIDS related dementias, as antivirals, inflammatory diseases such as rheumatoid arthritis, and cerebral ischemia, hyperlipidemia, and diabetes.
摘要翻译：本发明涉及金刚烷胺和奈拉美生的化合物，包括其药学上可接受的盐，二酯异构体和用于治疗阿尔茨海默病相关的痴呆症，抑郁症，艾滋病相关的痴呆症，抗病毒剂，炎性疾病如类风湿性关节炎和脑缺血，高脂血症和糖尿病的制剂。

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