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Organic compounds -- part of the class 532-570 series

20130116430 - Novel nicotinamide derivative or salt thereof: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group,... Agent: Fujifilm Corporation

20130116431 - Novel hsp90 inhibitor: Disclosed is a triazole derivative(s) represented by the general formula (1) below or a pharmacologically acceptable salt(s) thereof. Also disclosed are a prodrug(s) of such a triazole derivative(s) and an HSP90 inhibitor(s) containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom,... Agent: Nippon Kayaku Kabushiki Kaisha

20130116432 - Modified macromolecule: The present invention relates to a macromolecule having a controlled terminal group stoichiometry, the macromolecule including a surface layer, at least one subsurface layer and at least two terminal groups including: a first terminal group which is a residue of a pharmaceutically active agent, a derivative thereof or precursor therefor;... Agent: Starpharma Pty Ltd

20130116433 - Process for the production of etravirine: A novel process for the preparation of Etravirine comprises the condensing of ethyl cyanoacetate with N-cyanophenylguanidine to obtain an —OH compound of formula (II), which is further converted to a leaving group of formula (III). The compound of formula (III) is optionally protected and brominated to yield compound of formula... Agent:

20130109852 - Process for making thienopyrimidine compounds: The invention provides processes of preparing, separating, and purifying PI3K inhibitor, Formula I and II compounds, and novel intermediates for preparing Formula I and II compounds.... Agent: Genentech, Inc.

20130109853 - Preparation method of 5-[[2(r)-[1(r)-[3,5-bis(trifluoromethyl) phenyl]ethoxy]-3(s)-4-fluorophenyl-4-morpholinyl]methyl]-1,2-dihydro-3h-1,2,4-triazole-3-one: Disclosed is a synthesis method of a compound of formula 1,5-[[2(R)-[1(R)-[3,5-bis(trifluoromethyl)phenyl]ethoxyl]-3(S)-4-fluorophenyl-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazole-3-one (i.e. aprepitant), which comprises cyclizing a compound of formula 4 in a solvent, wherein R is C1-C5 alkyl. The intermediate for preparing aprepitant is also disclosed. The present method is especially suitable for industrial production of aprepitant.... Agent:

20130109854 - Novel methods for preparation of (+)-1-ethyl-4-[2-(4-morpholinyl)ethyl)-3,3-diphenyl-2-pyrrolidinone and salts thereof: The present invention includes a method of preparing a composition comprising (+)-doxapram or a salt thereof, wherein the composition is essentially free of (−)-doxapram or a salt thereof.... Agent: Galleon Pharmaceuticals, Inc.

20130109855 - Modular synthesis of graphene nanoribbons and graphene substructures from oligo-alkynes: A method for the synthesis of carbon-based structures, particularly graphene substructures and ribbons, from oligo- and poly-alkyne starting materials.... Agent: The Florida State University Research Foundation, Inc.

20130109856 - Novel process for the preparation of acylguanidines and acylthioureas: m

20130102778 - Process for the preparation of isoxazolyl- methoxy nicotinic acids: P

20130102779 - Substituted tetracycline compounds:

20130102780 - Transition metal-catalyzed processes for the preparation of n-allyl compounds and use thereof: The present disclosure provides processes for the N-dealkylation of tertiary amines and the use of transition metal catalysts to prepare tertiary N-allyl amine derivatives and secondary amine derivatives thereof. The tertiary amines can be alkaloids and, more particularly, the tertiary amines can be opioids. In specific embodiments, the present disclosure... Agent: Rhodes Technologies

20130102781 - Methods of making cocrystals: Disclosed are processes for preparing cocrystals, including processes for scaling up of cocrystal formation, as well as scalable processes for preparing cocrystals. Also disclosed are processes for scaled-up preparation of pterostilbene, progesterone, p-coumaric, and minoxidil cocrystals. Minoxidil cocrystals, such as minoxidil:benzoic acid 1:1 monohydrate cocrystals are also disclosed herein.... Agent: Aptuit (west Lafayette), LLC

20130102782 - Processes and intermediates for producing azaindoles: The present invention relates to processes and intermediates for the preparation of compounds useful as inhibitors of Janus kinases (JAK).... Agent: Vertex Pharmaceuticals Incorporated

20130102783 - Substituted diketopiperazines and their use as oxytocin antagonists: e

20130096301 - Kinase inhibitors and method of treating cancer with same: The present invention is directed to novel synthetic methods for preparing a spiro cyclopropyl indolinone compound represented by Structural Formula (A): (A) or its pharmaceutically acceptable salt thereof. Also included are synthetic intermediates described herein.... Agent: University Health Network

20130096302 - Pyrrolopyrazines and pyrazolopyrazines useful as inhibitors of protein kinases: The present invention relates to compounds useful as inhibitors of Aurora protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.... Agent:

20130096303 - Process for the preparation of hmg-coa reductase inhibitors and intermediates thereof: The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvastatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R2—N—O—R1 moiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for... Agent:

20130096304 - Nilotinib hcl crystalline forms: Crystalline forms of Nilotinib HCl are described.... Agent: Teva Pharmaceutical Industries Ltd.

20130096305 - Deuterated hiv attachment inhibitors: Deuterated piperazine and piperidine HIV attachment inhibitor compounds are set forth. The present invention provides compounds of Formula I, the pharmaceutically acceptable salts and/or solvates (e.g., hydrates) thereof, their pharmaceutical formulations, and their use in patients suffering from or susceptible to a virus such as HIV. The compounds of Formula... Agent: Bristol-myers Squibb Company