专利号:US-9512096-B2 优先权日:2011-12-22 标题 :Synthesis of amine substituted 4,5,6,7-tetrahydrobenzothiazole compounds 发明人:CHEN WEIRONG; HUMORA MICHAEL; KWOK DAW-LONG ALBERT; KIESMAN WILLIAM F; IRDAM ERWIN AYANDRA 权利人:KNOPP BIOSCIENCES LLC; KNOPP BIOSCIENCES LLP 摘要:The present invention is related to an improved process for the preparation of amino-substituted 4,5,6,7-tetrahydrobenzothiazole compounds of formula I, such as the compound 2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention further relates to an improved synthesis of (R)-2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention also relates to the methods and intermediates associated with the synthetic process.
专利号:US-2008125354-A1 优先权日:2005-11-21 标题 :Selective inhibition of matrix metalloproteinases 发明人:FIELDS GREGG B; HAMMER ROBERT 权利人:UNIV FLORIDA ATLANTIC; UNIV LOUISIANA STATE 摘要:Synthetic triple-helical peptides (THPs) are used for the design and synthesis of triple-helical transition state analog inhibitors. These inhibitors feature a phosphonate ester or phosphinic moiety in place of the scissle bond. These groups inhibit MMPs, and methods been developed for their convenient incorporation within a peptide sequence by solid-phase methods.
专利号:US-8519148-B2 优先权日:2007-03-14 标题 :Synthesis of chirally purified substituted benzothiazole diamines 发明人:RAJE PRASAD; GADIKOTA RAJENDRAKUMAR REDDY; CHEN JIAN-XIE; LAPINA OLGA V; MCCALL JOHN M 权利人:RAJE PRASAD; GADIKOTA RAJENDRAKUMAR REDDY; CHEN JIAN-XIE; LAPINA OLGA V; MCCALL JOHN M; KNOPP NEUROSCIENCES INC 摘要:Methods for preparing chirally purified substituted 4,5,6,7-tetrahydro-benzothiazole diamines such as, for example, (6R)2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole and purifying a dominant enantiomer of substituted 4,5,6,7-tetrahydro-benzothiazole diamines from entantiomerically enriched mixtures of substituted 4,5,6,7-tetrahydro-benzothiazole diamines are provided herein.
专利号:US-2013079526-A1 优先权日:2010-03-03 标题:Synthesis of Chirally Purified Substituted Benzothiazole Diamines 发明人:GREENFIELD SCOTT JEFFREY; GIBB CAMERON SEATH; GADIKOTA RAJENDRA KUMAR REDDY 权利人:GREENFIELD SCOTT JEFFREY; GIBB CAMERON SEATH; GADIKOTA RAJENDRA KUMAR REDDY; KNOPP NEUROSCIENCES INC 摘要:Methods for preparing chirally purified substituted 4,5,6,7-tetrahydro-benzothiazole diamines such as, for example, (6R)2-amino-4,5,6,7-tetrahydro- 6 -(propylamino)benzothiazole and purifying a dominant enantiomer of substituted 4,5,6,7-tetrahydro-benzothiazole diamines from entantiomerically enriched mixtures of substituted 4,5,6,7-tetrahydro-benzothiazole diamines are provided herein.
专利号:US-12201669-B2 优先权日:2021-03-11 标 题:Small molecule suppressors of APOE gene expression and cerebral vascular amyloid pathology 发明人:TSAI LI-HUEI; BLANCHARD JOEL 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present disclosure provides methods of inhibiting amyloid synthesis in a subject using small molecule inhibitors. The invention also includes methods of treating disease associated with amyloid synthesis, such as Alzheimer's disease. The small molecule inhibitors disclosed herein are compounds which are non-immunosuppressant cyclosporin including the pharmaceutically acceptable salts thereof.
专利号:US-8883831-B2 优先权日:2008-11-05 标题 :Compositions and methods for minimizing or reversing agonist-induced desensitization 发明人:BEAR DAVID M; KESSLER ROBERT M 权利人:PHARMORX THERAPEUTICS INC 摘要:Methods and compositions are provided for preventing or reversing loss of the therapeutic effect of a drug, where the loss is associated with the repeated administration of the drug to a patient. The method includes administering to the patient a dopamine receptor agonist or partial agonist or a drug that increases the extracellular level of dopamine by enhancing release of dopamine, decreasing the removal of dopamine from the extracellular space, enhancing the synthesis of dopamine within the brain, or decreasing metabolic degradation of dopamine; and also administering to the patient an opioid receptor antagonist in an ultra-low dose amount, wherein the ultra-low dose amount is effective to prevent or reverse loss of therapeutic effects associated with the repeated administration of the drug to the patient. The methods are useful for various treatments, including treating Parkinson's Disease, Restless Leg Syndrome, depression, schizophrenia, psychostimulant drug abuse, or attention deficit disorder.
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合成参考文献
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