CAS: 28289-54-5; Mptp

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23007-85-4 186347-72-8 38025-45-5

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📜苯基锂置于盐酸体系中,化学反应 4.0H,反应生成1-甲基-4-苯基-1,2,3,6-四氢吡啶
参考文献:Synthesis And Toxicity Toward Nigrostriatal Dopamine Neurons Of 1-Methyl-4-Phenyl-1,2,3,6-Tetrahydropyridine (Mptp) Analogs
标题:Synthesis And Toxicity Toward Nigrostriatal Dopamine Neurons Of 1-Methyl-4-Phenyl-1,2,3,6-Tetrahydropyridine (Mptp) Analogs
摘要:Six Compounds Having Structural Features In Common With 1-Methyl-4-Phenyl-1,2,3,6-Tetrahydropyridine (Mptp) Were Synthesized And Tested In Mice For The Ability To Produce A Prolonged Decrease In Nigrostriatal Dopamine (Da) And Da Metabolites. The Compounds That Were Prepared And Tested Include The Ester Elimination Products Of The Analgetic Drugs Alpha-Prodine And Trimeperidine. None Of The Compounds In This Study,Except For Mptp,Produced Significant Neurotoxic Effects In The Mouse Model. The Study Shows That Minor Changes In The Tetrahydropyridine Ring Of Mptp Result In A Marked Decrease In Neurotoxicity.
Doi:10.1021/jm00153A019

专利信息

专利号:US-8546532-B2
优先权日:2008-04-17
标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders
发明人：BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS
权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC
摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.

专利号:US-8569265-B2
优先权日:2011-05-06
标题:Deuterated analogs of (4S)-4-ethyl-4-hydroxy-11-[2- (trimethylsilyl)ethyl]-1H-pyrano[3′, 4′:6,7] indolizino [1,2-b]quinoline-3,14(4H, 12H)-dione and methods of use thereof
发明人：CHEN XINGHAI; HUANG QIULI; KOCHAT HARRY; MALAKHOV ANDREY; HAUSHEER FREDERICK H
权利人:CHEN XINGHAI; HUANG QIULI; KOCHAT HARRY; MALAKHOV ANDREY; HAUSHEER FREDERICK H; BIONUMERIK PHARMACEUTICALS INC
摘要:The present invention discloses: (i) two novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (ii) methods of synthesis of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (iii) pharmaceutically-acceptable formulations comprising said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents; and (iv) methods of administration of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof.

专利号:US-2005085555-A1
优先权日:1997-08-21
标 题:Composition, synthesis and therapeutic applications of polyamines
发明人：MURPHY MICHAEL A; MALACHOWSKI MITCHELL R
摘要:This invention relates to a process of synthesis and composition of open chain (ring), closed ring, linear branched and or substituted polyamines, polyamine derived tyrosine phosphatase inhibitors and PPAR partial agonists/partial antagonists via a series of substitution reactions and optimizing the bioavailability and biological activities of the compounds. Polyamines prevent the toxicty of neutoxins and diabetogenic toxins including paraquat, methyphenyl pyridine radical, rotenone, diazoxide, streptozotocin and alloxan. These polyamines can be to treat neurological, cardiovascular, endocrine acquired and inherited mitochondrial DNA damage diseases and other disorders in mammalian subjects, and more specifically to the therapy of Parkinson's disease, Alzheimer's disease, Lou Gehrig's disease, Binswanger's disease, Olivopontine Cerebellar Degeneration, Lewy Body disease, Diabetes, Stroke, Atherosclerosis, Myocardial Ischemia, Cardiomyopathy, Nephropathy, Ischemia, Glaucoma, Presbycussis, Cancer, Osteoporosis, Rheumatoid Arthritis, Inflammatory Bowel Disease, Multiple Sclerosis and as Antidotes to Toxin Exposure.

专利号:US-9980971-B2
优先权日:2006-07-11
标 题:Methods of synthesis and/or purification of diaminophenothiazinium compounds
发明人：WISCHIK CLAUDE MICHEL; STOREY JOHN MERVYN DAVID; MARSHALL COLIN; SINCLAIR JAMES PETER; BADDELEY THOMAS CRAVEN
权利人:WISTA LAB LTD
摘要:Disclosed are methods of synthesis and/or purification of certain 3,7-diamino-phenothiazin-5-ium compounds (“diaminophenothiazinium compoundsâ€?) including Methylthioninium Chloride (MTC) (Methylene Blue), and the resulting high purity characterized by a purity greater than 98%, and very low levels of heavy metals and organic impurities Azure A, B, C and MVB. Also disclosed are methods of treatment of a tauopathy or methemoglobinemia in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of the high-purity diaminophenothiazinium compound.

专利号:US-9950033-B2
优先权日:2012-02-29
标 题:Use of engrailed proteins for increasing dopamine synthesis by dopaminergic neurons
发明人：PROCHIANTZ ALAIN; MOYA KENNETH; JOSHI RAJIV
权利人:PROCHIANTZ ALAIN; MOYA KENNETH; JOSHI RAJIV; CENTRE NAT RECH SCIENT; COLLEGE FRANCE
摘要:The invention relates to the use of an Engrailed protein as a medicament for increasing dopamine synthesis by dopaminergic neurons, in particular in the management of conditions associated with a decrease of dopamine levels without loss of dopaminergic neurons.

专利号:US-11472777-B2
优先权日:2015-09-14
标题:Piperazine and piperidine derivatives, their synthesis and use thereof in inhibiting VDAC oligomerization, apoptosis and mitochondria dysfunction
发明人：SHOSHAN-BARMATZ VARDA; LEV GRUZMAN ARIE
权利人:NAT INST BIOTECHNOLOGY NEGEV LTD
摘要:Provided herein piperazine and piperidine derivatives, their synthesis and use thereof in inhibiting VDAC oligomerization, apoptosis and mitochondria dysfunction. Also provided methods of treatment of diseases associated with said processes, e.g. Alzheimer's and Parkinson's diseases.