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1. 发明授权

US4806654A Processes for the preparation of benzo(chalcogeno)(4,3,2-cd)indazoles and intermediates thereof 失效
标题翻译：制备苯并（硫族基）（4,3,2-cd）吲唑的方法及其中间体
公开(公告)号：US4806654A
公开(公告)日：1989-02-21
申请号：US149103
申请日：1988-02-11
申请人： Vladimir G. Beylin , Om P. Goel , Anthony D. Sercel , Howard D. H. Showalter
发明人： Vladimir G. Beylin , Om P. Goel , Anthony D. Sercel , Howard D. H. Showalter
IPC分类号： C07D491/048 , A61K31/415 , A61P31/04 , A61P35/02 , C07D495/04 , C07D495/06 , C07D513/08 , C07D517/08 , C07D491/06
CPC分类号： C07D495/06
摘要： Improved processes for producing substituted benzo(chalcogeno)[4,3,2-cd] indazoles. The processes produce compounds in higher yields and of greater purity by using a novel sequence of acylation chemistry and easily removed protecting groups. The compounds produced have antibacterial, antifungal, antileukemic, and antitumor activity.

2. 发明授权

US4689423A Process for the preparation of 2,3,4,5-tetrafluorobenzoyl acetates 失效
标题翻译：制备2,3,4,5-四氟苯甲酰基乙酸酯的方法
公开(公告)号：US4689423A
公开(公告)日：1987-08-25
申请号：US846695
申请日：1986-04-01
申请人： Vladimir G. Beylin , Om P. Goel
发明人： Vladimir G. Beylin , Om P. Goel
IPC分类号： C07C69/738 , C07C67/14
CPC分类号： C07C67/14
摘要： An improved process for the preparation of methyl 2,3,4,5-tetrafluorobenzoylacetate is described. The process is for intermediates that lead to trifluoroquinolinic acids which in turn are used to produce antibacterial agents of the difluoro quinolinecarboxylic acid type. The process runs at room temperature, uses a safe and inexpensive base, and can be conveniently scaled up for manufacturing purposes.

3. 发明授权

US4672129A Process for preparing substituted anthra[1,9-cd]pyrazol-6(2H)-ones 失效
标题翻译：制备取代的蒽[1,9-cd]吡唑-6（2H） - 酮的方法
公开(公告)号：US4672129A
公开(公告)日：1987-06-09
申请号：US859673
申请日：1986-05-05
申请人： Vladimir G. Beylin , Om P. Goel , H.D. Hollis Showalter
发明人： Vladimir G. Beylin , Om P. Goel , H.D. Hollis Showalter
IPC分类号： C07D231/54
CPC分类号： C07D231/54 , Y02P20/55
摘要： An improved process for producing anthra[1,9-cd]-pyrazol-6(2H)-ones from 1,4-dichloro-5,8-disubstituted 9,10-anthracenediones. The process produces higher yields by using a new combination of protecting groups on the compounds which allows for easier and cleaner chromatographic resolution. The compounds produced have antibacterial, antifungal, antileukemic, and antitumor activity.
摘要翻译：从1,4-二氯-5,8-二取代的9,10-蒽二酸生产蒽[1,9-cd] - 吡唑-6-（2H）酮的改进方法。该方法通过使用化合物上的保护基团的新组合产生更高的产率，其允许更容易和更清洁的色谱分辨率。所生产的化合物具有抗菌，抗真菌，抗白血病和抗肿瘤活性。

4. 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。

5. 发明授权

US07977511B2 Carnitine conjugates of adamantanamines and neramexane derivatives as dual prodrugs for various uses 失效
标题翻译：金刚烷胺和奈拉美生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：US07977511B2
公开(公告)日：2011-07-12
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： C07C321/00
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。

6. 发明申请

US20080188444A1 Methods of treating various diseases using carnitine conjugates as dual prodrugs 有权
公开(公告)号：US20080188444A1
公开(公告)日：2008-08-07
申请号：US11980846
申请日：2007-10-31
申请人： Om P. Goel
发明人： Om P. Goel
IPC分类号： A61K31/66 , A61K31/21 , A61P3/00
CPC分类号： A61K31/24 , A61K31/21 , A61K31/522 , A61K31/66 , C07C229/22
摘要： The present invention discloses uses for treating various diseases with novel dual prodrug compounds of Formula 1, wherein A is selected from the group consisting of a single bond, —O—, or —CH2—; m and n vary independently and are an integer from 1 to 15; p and q vary independently from 0 to 1; B is —CR3R4; D is selected from the group consisting of —CO2R5, —OR6, —OCOR7, —SO3R8, —SO2NH2, —OPO(OR9)(OR10), —OPO(OR9)(NH2), —OPO(OR9)—O—PO(OR10)(OR11), wherein R1 to R4 are independently selected from C1-C6 alkyl; and R5 to R11 are independently selected from the group consisting of hydrogen; C1-C6 alkyl; C3-C6 cycloalkyl; C2-C6 alkenyl; C6 alkynyl; C5-C10 aryl unsubstituted or substituted with C1-C6 alkyl, hydroxyl, C1-C6 alkoxyl, 1,3-dioxolanyl, cyano, halo, nitro, trihaloalkyl, carboxyl, C1-C6 acyl, C1-C6 hydroxyalkyl, amino, C1-C6 alkylamino, C1-C6 dialkylamino, C1-C6 acylamino, C1-C6 alkoxylcarbonyl; C5-C6 arylalkyl unsubstituted or substituted with C1-C6 alkyl, hydroxyl, C1-C6 alkoxyl, 1,3-dioxolanyl, cyano, halo, trihaloalkyl, carboxyl, C1-C6 acyl, C1-C6 hydroxyalkyl, amino, C1-C6 alkylamino, C1-C6 dialkylamino, C1-C6 alkoxylcarbonyl; C1-C6 carboxyalkyl; C1-C6 acylamino; C1-C6 sulfonatoalkyl; C1-C6 sulfamylalkyl; and C1-C6 phosphonatoalkyl. The various terms in Formula 1 are selected to optimize the physiochemical and biological properties such as, lipophilicity, bioavailability, and pharmacokinetics of compounds of Formula 1. There compounds are useful for the treatment of various metabolic, cardiovascular and neurological disorders.

7. 发明授权

US5380925A Cyclic amino acids and derivatives thereof 失效
公开(公告)号：US5380925A
公开(公告)日：1995-01-10
申请号：US109797
申请日：1993-08-20
申请人： Vladimir Beylin , Huai G. Chen , Om P. Goel , Mark E. Marlatt , John G. Topliss
发明人： Vladimir Beylin , Huai G. Chen , Om P. Goel , Mark E. Marlatt , John G. Topliss
IPC分类号： C07D333/12 , A43B7/06 , A43B13/18 , A61K38/00 , C07B57/00 , C07C227/34 , C07C229/36 , C07C233/41 , C07C233/51 , C07C233/79 , C07C271/22 , C07D219/02 , C07D311/90 , C07D335/18 , C07D335/20 , C07D453/04 , C07C229/14 , C07B55/00 , C07C233/47 , C07D215/38
CPC分类号： C07C271/22 , C07C229/36 , C07C233/51 , C07D335/20 , A61K38/00 , C07C2103/32
摘要： Novel cyclic amino acids which are useful in preparing biologically active peptides as well as a process for the preparation of D and L enantiomers of the cyclic amino acids are described where an N-protected derivative of the racemic cyclic amino acid is treated with (-)cinchonidine and the resulting salt resolved into the desired enantiomers, as well as derivatives thereof and valuable intermediates used in the process.

8. 发明授权

US5264577A Cyclic amino acids and derivatives thereof 失效
标题翻译：环状氨基酸及其衍生物
公开(公告)号：US5264577A
公开(公告)日：1993-11-23
申请号：US872742
申请日：1992-04-22
申请人： Vladimir Beylin , Huai G. Chen , Om P. Goel , Mark E. Marlatt , John G. Topliss
发明人： Vladimir Beylin , Huai G. Chen , Om P. Goel , Mark E. Marlatt , John G. Topliss
IPC分类号： C07D333/12 , A43B7/06 , A43B13/18 , A61K38/00 , C07B57/00 , C07C227/34 , C07C229/36 , C07C233/41 , C07C233/51 , C07C233/79 , C07C271/22 , C07D219/02 , C07D311/90 , C07D335/18 , C07D335/20 , C07D453/04 , C07D453/02 , C07C231/20 , C07D311/82 , C07D335/12
CPC分类号： C07C271/22 , C07C229/36 , C07C233/51 , C07D335/20 , A61K38/00 , C07C2103/32
摘要： Novel cyclic amino acids which are useful in preparing biologically active peptides as well as a process for the preparation of D and L enantiomers of the cyclic amino acids are described where an N-protected derivative of the racemic cyclic amino acid is treated with (-)cinchonidine and the resulting salt resolved into the desired enantiomers, as well as derivatives thereof and valuable intermediates used in the process.
摘要翻译：描述了可用于制备生物活性肽的新型环状氨基酸以及制备环状氨基酸的D和L对映异构体的方法，其中外消旋环状氨基酸的N-保护的衍生物用（ - ）辛可尼定，所得盐分解成所需的对映异构体，以及其衍生物和在该方法中使用的有价值的中间体。

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. 发明授权

US5449778A Cyclic amino acids and derivatives thereof 失效
标题翻译：环状氨基酸及其衍生物
公开(公告)号：US5449778A
公开(公告)日：1995-09-12
申请号：US302290
申请日：1994-09-08
申请人： Vladimir Beylin , Huai G. Chen , Om P. Goel , Mark E. Marlatt , John G. Topliss
发明人： Vladimir Beylin , Huai G. Chen , Om P. Goel , Mark E. Marlatt , John G. Topliss
IPC分类号： C07D333/12 , A43B7/06 , A43B13/18 , A61K38/00 , C07B57/00 , C07C227/34 , C07C229/36 , C07C233/41 , C07C233/51 , C07C233/79 , C07C271/22 , C07D219/02 , C07D311/90 , C07D335/18 , C07D335/20 , C07D453/04 , C07D219/08 , C07D215/00
CPC分类号： C07C271/22 , C07C229/36 , C07C233/51 , C07D335/20 , A61K38/00 , C07C2103/32
摘要： Novel cyclic amino acids which are useful in preparing biologically active peptides as well as a process for the preparation of D and L enantiomers of the cyclic amino acids are described where an N-protected derivative of the racemic cyclic amino acid is treated with (-)cinchonidine and the resulting salt resolved into the desired enantiomers, as well as derivatives thereof and valuable intermediates used in the process.
摘要翻译：描述了可用于制备生物活性肽的新型环状氨基酸以及制备环状氨基酸的D和L对映异构体的方法，其中外消旋环状氨基酸的N-保护的衍生物用（ - ）辛可尼定，所得盐分解成所需的对映异构体，以及其衍生物和在该方法中使用的有价值的中间体。

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