CAS: 89565-68-4; Rel-(1R,3R,5S)-8-Methyl-8-Azabicyclo[3.2.1]Octan-3-Yl 1H-Indole-3-Carboxylate

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CAS号59496-25-2 1H-吲哚-3-羰酰氯 | CAS号120-29-6 托品醇; 品托碱

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-9518034-B2
优先权日:2013-10-14
标题 :Synthesis of chiral enaminones, their derivatives, and bioactivity studies thereof
发明人：STOLTZ BRIAN M; DOUGHERTY DENNIS A; DUQUETTE DOUGLAS; DUFFY NOAH
权利人:CALIFORNIA INST OF TECHN
摘要:This invention provides enantioenriched heterocyclic enaminone compounds with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): n ncomprising treating a compound of formula (II):n n nwith a transition metal catalyst under alkylation conditions.

专利号:US-7576211-B2
优先权日:2004-09-30
标题 :Synthesis of thienopyridinone compounds and related intermediates
发明人：DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE
权利人:EPIX DELAWARE INC
摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

专利号:US-8734846-B2
优先权日:2008-06-16
标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
发明人：ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
权利人:BIND BIOSCIENCES INC
摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

专利号:US-2013035307-A1
优先权日:2010-01-26
标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
发明人：PRESTWICH GLENN D; KENNEDY THOMAS P
权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

专利号:US-12295961-B2
优先权日:2009-12-31
标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols
发明人：DHINGRA OM
权利人:MARIUS PHARMACEUTICALS INC
摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.