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WO/2013/190497A2 |
The invention provides pharmaceutical compositions and methods for treatment of an inflammatory disease of the lung caused by inhalation of a toxic agent or an irritant, more particularly, chlorine inhalational lung injury, as well as ce...
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WO/2013/179052A1 |
The present invention relates to methods of synthesising aziridines including isotopically labelled aziridines, said methods comprising contacting an imine or one or more precursors thereof with a diazo compound in the presence of a phos...
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WO/2013/116715A1 |
Methods and intermediates useful for preparing a compound of formula I and salts thereof.
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WO/2013/103973A1 |
This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compunds as at le...
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WO/2013/081549A1 |
The invention relates to a method for preparing 2H-azirine carboxylic esters. More specifically, the invention relates to a method for preparing 2H-azirine carboxylic esters starting from α-diazo-β-keto oxime ethers in the presence of ...
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WO/2013/061340A1 |
The present invention discloses high yielding enantioselective process for synthesis of Oseltamivir from readily available starting material, cis-1,4-butene diol.The process features incorporation of chirality using sharpless asymmetric ...
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WO/2012/072036A1 |
Disclosed are intermediates of Sitagliptin, a preparation process thereof, and a process for synthesizing Sitagliptin using these intermediates. Sitagliptin is synthesized by using chiral amino compounds as a raw material, without having...
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WO/2011/087664A1 |
Described is a pre-adhesive, curable composition comprising an acid-functional (meth)acrylate copolymer and a novel (meth)acryloyl-aziridine crosslinking agent, which when crosslinked provides a pressure-sensitive adhesive composition.
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WO/2011/070459A1 |
The present invention relates to a novel manufacturing process and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially rennin inhibitors such as Aliskiren. The invention describes a preparation of...
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WO/2011/035064A2 |
Homogenous and heterogenous catalysts comprising 1,2,4-triazole ligands and transition metals are described. The catalysts can be used to catalyze the oxidation of hydrocarbons and other reactions. In particular, the catalysts can be use...
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WO/2010/114291A2 |
The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention is able to reduce preparation costs by using low cost reagents on reaction and is able to be used...
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WO/2010/104645A1 |
A crosslinkable, pre-adhesive composition is described comprising an acid- functional (meth)acrylate copolymer and an aziridine crosslinking agent, which when crosslinked provides a pressure-sensitive adhesive and pressure-sensitive adhe...
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WO/2010/099206A2 |
A process for the asymmetric aziridination of an alkene comprising treating the alkene with a sulfonyl azide, preferably trichloroethoxysulfonyl azide, in the presence of a cobalt(II) porphyrin.
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WO/2010/065355A1 |
A photoactive compound that is the Michael addition reaction product of an aziridine compound and a photoinitiator-functional (meth)acrylate is described. The compound can be used to crosslink (meth)acrylic polymers via a hydrogen abstra...
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WO/2010/055887A1 |
A novel β-(trifluoromethyl)vinyldiaryl sulfonium salt represented by general formula (I), which can be used for simple syntheses of various useful compounds each containing a trifluoromethyl group, or the like. (In formula (I), R1 and R...
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WO/2010/041748A1 |
Disclosed is a prophylactic or therapeutic agent for diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, heart failure, cardiomyopathy, myocardial ischemia, cer...
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WO/2010/018154A1 |
The present invention relates to a process for the production of (3aR, 4S, 7aR)-4-hydroxy-4-m-tolylethynyl-octahydro-indole-1-carboxyli
c acid methyl ester (I), of carbamic acid (2-chloroethyl)(3-oxocyclohexyl)-alkyl ester enantiomers (I...
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WO/2009/146032A2 |
Cobalt(II) complex of P1 [Co(P1)], a new porphyrin that was designed on the basis of potential hydrogen bonding interactions in the metal-nitrene intermediate, is a highly active catalyst for olefin aziridination with azides. The [Co(P1)...
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WO/2009/096907A1 |
The invention relates to a process for making an aziridine, wherein an aldehyde, a nitroso compound and a Michael acceptor are reacted in the presence of an N-heterocyclic carbene (NHC) catalyst.
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WO/2009/078813A1 |
A process is provided for the synthesis of 4,5-diamino cyclohexene carboxylate ester (1): or a pharmaceutically acceptable salt thereof. R1 - R3 are a silyl-, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. R...
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WO/2008/155355A1 |
The invention relates to a method for synthesizing an N-unsubstituted or N-substituted aziridine of the formula (III), wherein an olefin of the formula (I), in which R1 to R5 independently of one another represent hydrogen, linear or bra...
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WO/2008/083729A1 |
The present invention relates to novel compounds suitable for or already radiolabeled with 18F, methods of making such compounds and use of such compounds for diagnostic imaging.
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WO/2008/046232A1 |
The present invention relates to unprotected amino aldehydes and applications for same. More particularly, the present invention relates to novel aziridine aldehydes and processes for preparing these novel compounds. The invention also r...
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WO/2008/024892A2 |
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11...
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WO/2007/007828A1 |
Disclosed is a novel compound useful as a production intermediate for benzylamine derivatives. Also disclosed is a method for producing such a compound. Specifically disclosed is a method for producing an ethylenediamine derivative repre...
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WO/2006/109146A2 |
The present invention relates to novel heterocyclic derivatives of formula (I) and their pharmaceutically acceptable salts, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, ...
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WO/2006/003795A1 |
A process which comprises using a stable Ru(salen)(CO) complex represented by the general formula (I) or an enantiomer thereof as the catalyst and by which optically active aziridines and amines can be produced enantioselectively with a ...
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WO/2005/117865A1 |
The present invention relates to compounds of formula (I) wherein A, R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositi...
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WO/2005/094818A1 |
The invention provides novel inhibitors of IAP that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula (I) in which X1 and X2 are independently O or S; L is a bond or -C(X3)-, -C(X3)...
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WO/2005/054194A1 |
A method for the synthesis of a compound of formula (I) as a mixture of enantiomers, formula (I) (wherein R1 is H or an acid protective group and H+A- indicates an optional acid with which the compound of formula (I) may form an ammonium...
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WO/2005/042471A1 |
The present invention relates to novel nitrophenyl mustard and nitrophenylaziridine alcohols, to their corresponding phosphates, to their use as targeted cytotoxic agents; as bioreductive drugs in hypoxic tumours, and to their use in cel...
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WO/2005/016264A2 |
Diamine derivatives of quinones, and related compounds, including salts thereof, that modulate the levels of gene expression in cellular systems, such as cancer cells, are disclosed, along with methods for preparing such compounds and de...
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WO/2005/002570A1 |
The invention features a method for inactivating parasites in biological compositions. The method includes contacting the biological composition with an aziridino compound under parasite inactivating conditions.
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WO/2004/080944A1 |
The invention provides a mufti-step process for preparing 1,2-diamino compounds of formula wherein R1, R1, R2’ RTand R3 have the meaning given in the specification and pharmaceutically acceptable addition salts thereof, from 1,2-epoxid...
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WO/2004/050617A1 |
The invention relates to a composition consisting of at least one polyfunctional aziridine compound and 1,4-diazabicyclo[2.2.2]octane, and to a method for producing the same. The invention also relates to the use of said composition as a...
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WO/2004/050613A2 |
This invention provides 2-substituted-propenamide derivatives and their compositions for the treament of hepatitis B virus and/or hepatitis D virus.
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WO/2004/050623A1 |
Methods of making substituted phenylalkynes of formula (I).
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WO/2004/020429A1 |
A method for stereoselective chemical synthesis, includes the steps of: (A) reacting a nucleophile and a chiral or prochiral cyclic substrate, said substrate comprising a carbocycle or a heterocycle having a reactive center susceptible t...
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WO/2003/093512A1 |
This invention relates to methods and compositions for the modification of nucleic acids.
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WO/2003/089476A1 |
There is disclosed a cross-linked hyaluronate compound obtained by reacting a sodium hyaluronate compound with a polyfunctional aziridine compound as a cross-linking agent. The polyfunctional aziridine compound was added to hyaluronan of...
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WO/2003/066806A2 |
Methods are provided for treatment of diseases. The methods include preventing or inhibiting transcription and/or replication of a nucleic acid molecule by administering to a subject in need of such treatment an effective amount of one o...
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WO/2003/053918A2 |
The invention relates to a method for producing perfluoroalkane sulfonic acid esters and their subsequent conversion into salts, in addition to the use of the produced compounds in electrolytes and batteries, capacitors, supercapacitors ...
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WO/2003/053919A1 |
The present invention relates to compounds of formula (I) wherein A?1¿, A?2¿, A?3¿, A?4¿, A?5¿, A?6¿, A?7¿, A?8¿, A?9¿, A?10¿, U, V, W, m, n and p are as defined in the description and claims, and pharmaceutically acceptable sa...
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WO/2003/050099A1 |
Substituted phenylalkynes of formula (l), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
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WO/2003/045906A2 |
The present invention provides a process for producing an aziridine-1-carboxamide of the formula: (I) from an aziridine of the formula: (II) and an isocyanate of the formula R5-N&equals C&equals O, where R?1¿, R?2¿, R?3¿, R?4¿ and R?...
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WO/2003/025017A1 |
A crystalline composition comprising a crystal of the IL-6 receptor I chain is provided. Also provided are methods of using the crystal and related structural information to screen for and design compounds that interact with IL-6R, or va...
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WO/2002/026705A2 |
The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one s...
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WO/2002/026750A2 |
Disclosed are substantially enantiomerically pure bis-phosphine compounds comprising a substantially enantiomerically pure chiral backbone linking two phosphine residues wherein one of the phosphine residues has three phosphorus-carbon b...
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WO/2002/024636A2 |
N-Benzoyl arylsulfonamides having the formula (I) are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.
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WO/2002/012184A1 |
The invention relates to (D)- or (L)-alpha-amino acids and their derivatives comprising phenylalanine or homophenylalanine having formula (I) or (II) and a process for the preparation thereof by stereoselective synthesis from aziridine h...
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