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JP5225856B2 |
The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, ph...
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JP5219323B2 |
This invention relates to compounds of the formula: ##STR00001## wherein: the substituent groups defined by R.sub.1, R.sub.2 are each independently selected of H, C(.dbd.O)R', C.sub.1 C.sub.18 alkyl, C.sub.2 C.sub.18 alkenyl, C.sub.2 C.s...
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JP2013508285A |
The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in tre...
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JP5147866B2 |
In its many embodiments, the present invention provides -substituted pyridazinone compounds as glucan synthase inhibitors, methods of preparing such compounds, pharmaceutical including one or more of such compounds, methods of preparing ...
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JP2013014622A |
To provide pyridazinone derivatives useful as glucan synthase inhibitors.In its many embodiments, the present invention provides: substituted pyridazinone compounds as glucan synthase inhibitors; methods of preparing such compounds; phar...
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JP5085935B2 |
The present invention is directed to a process of reducing the particle size of a crude beta- or gamma-quinacridone pigment in a crystal phase, while maintaining the crystal phase, comprising the steps of: combining a milling composition...
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JP2012177130A |
To provide an environmentally friendly process that does not produce large amounts of waste in the milling or recrystatlization and that allows the reduction in particle size in two isomorphous crystal phases (β and γ crystal phases) o...
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JP5008812B2 |
Antitumor compounds have the five membered fused ring ecteinascidin structure of the formula (XIV). The present compounds lack a 1,4-bridging group as found in the ecteinascidins. They have at the C-1 position a substituent selected from...
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JP4942900B2 |
A process step in the manufacture of an ecteinascidin compound comprising deprotecting a compound of formula (A) by removing both protecting groups in a single step to give an alpha aminolactone of formula (35), wherein ProtNH is an amin...
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JP4840594B2 |
This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen ato...
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JP2011518836A |
The present invention relates to macrocyclic compounds of Formula I: or pharmaceutically acceptable salts thereof or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and...
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JP4684552B2 |
Derivatives of ecteinascidin 736 are provided.
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JP4653950B2 |
The present invention provides a compound of the general formula Ia : wherein R 2 , R 4 , R 5 are each independently selected of H, C(=O)R', C(=O)OR', P=O(OR') 2 , substituted or unsubstituted C 1 -C 18 alkyl, substituted or unsubstitute...
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JP2011026331A |
To provide new compounds having most suitable characteristics of cytotoxicity and selectivity to tumor, decreased in systemic toxicity and improved in pharmacokinetic properties.There are provided derivatives of ecteinascidin 736 of gene...
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JP4599801B2 |
To obtain a new thia/oxaporphyrin-based compound having optical or electric function. The thiaporphyrin-based compound, the dithiaporphyrin-based compound, the oxaporphyrin-based compound, the dioxaporphyrin-based compound and the oxathi...
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JP4583598B2 |
The purification and structure elucidation of several products of the metabolism of Et 743 by human cytochrome CYP3A4 have been accomplished. These compounds are abbreviated herein as "ETM" followed by a numeric value which represents th...
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JP2010215656A |
To provide related structures having the same or higher level antitumor activities than conspicuous antitumor activities of the ecteinascidin (Et) 743 compound.Compounds having structural formula of the figure have the same or higher lev...
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JP4492348B2 |
A quinoxalinone derivative of the formula (I): or a pharmaceutically acceptable salt or ester thereof, wherein; X is NH, S or the like; Y is O or the like; the partial structure is, for example, the formula: B1, B2, ....., Bn-1 and Bn, (...
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JP4445136B2 |
Methods are provided for preparing a compound with a fused ring structure of formula (XIV) which comprises one or more reactions starting from a 21-cyano compound of formula (XVI) where typically; R1 is an amidomethylene group or an acyl...
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JP4443043B2 |
The present application is directed to several newly prepared semi-synthetic ecteinascidin (Et) species, designated herein as Boc-Et 729, Et 875, and Et 1560. The physical properties of these compounds, their preparation and bioactivitie...
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JP2010065030A |
To provide a therapeutic agent for arrhythmia.A benzopyran derivative is represented by formula (I) or (II) [wherein, R1 and R2 together mean C=O or the like, or together mean cycloalkyl or heterocyclyl such as pyran or piperidine with c...
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JP4435561B2 |
The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO2; R1, R2, R3 and R4 are independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, halogen,...
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JP4435325B2 |
A class of novel tricyclics is disclosed of the formula (I) wherein; A is phenil or pyridyl wherein the nitrogen is at the 5-, 6-, 7- or 8-position; one of B or D is nitrogen and the other is carbon; Z is cyclohexenyl, phenyl, pyridyl, w...
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JP4425995B2 |
The present invention is directed to a synthetic process for the formation of ecteinascidin compounds and related structures, such as the saframycins. In one particularly preferred embodiment, the present invention provides a synthetic r...
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JP4382164B2 |
Five new nucleophile substituted ecteinascidin compounds were isolated from extracts of Exteinascidia turbinata and designated Et 802, Et 788, Et 760, Et 858 and Et 815. Three new N-oxides were also obtained and designated Et 717, Et 775...
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JP4364305B2 |
Novel compounds, formulations and methods of treating patients with cancer are provided for in this invention. The compounds are derivatives of camptothecin, and specifically relate to compounds having novel substitutions at the C-7 posi...
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JP4334194B2 |
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JP2009108107A |
To provide new crystalline forms of clopidogrel hydrogensulfate and the amorphous form thereof.There are provided new crystalline forms III, IV, V and VI of clopidogrel hydrogensulfate, the amorphous form thereof, their pharmaceutical co...
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JP2009519224A |
The present invention relates to HDAC inhibitor derivatives, particularly derivatives of the free thiol of metabolites of the HDAC inhibitor FK228, pharmaceutical compositions thereof, and to methods of using such derivatives and pharmac...
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JP4246488B2 |
Compounds of general structural formula (I), and use of the compounds or salts or solvates thereof as therapeutic agents, are disclosed
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JP2009512662A |
The present invention concerns an intermediate of the following formula I in which R 1 and R 2 represent independently of each other a C 1 -C 12 alkyl group, a (C 1 -C 12 alkoxy)carbonyl group, optionally substituted by one, two or three...
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JP4208469B2 |
Intermediates (I) for the total synthesis of ecteinascidin compounds are new having the 10 membered ring structure of ecteinascidins with a 4-position thioether group and trichloroethoxycarbonyl (Troc) substituent as R 2in the 12-N posit...
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JP4164028B2 |
A compound of Formula Ior a pharmaceutically acceptable salt thereof, or a tautomer thereof, wherein G1, G2, and B are as defined in the application, are selective inhibitors of MMP-13. The compounds are useful for treating diseases medi...
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JPWO2006088191A1 |
The present invention provides a eugenic derivative represented by the general formula (I) or a salt thereof, or a hydrate or solvate thereof, which exhibits antiviral activity against viruses such as hepatitis C virus.(In the formula, R...
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JP2008514688A |
We have found anti-inflammatory activity in the ecteinascidin compounds. Such compounds have been widely described, and may have the following general formula (I), wherein: R5 is OH, alkoxy or alkanoyloxy; R6 is hydrogen, alkyl, alkenyl,...
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JP4066223B2 |
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JP2008505862A |
The present invention relates to the use of ecteinascidin 743 in patients having certain levels of molecular markers who can predict the outcome of chemotherapy, in particular in patients having low levels of BRCA1 expression.
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JP3973906B2 |
The present invention relates to a combination comprising component (a) being a compound of formula I, and component (b), being, at least one other drug useful in the treatment of arrhythmias and / or at least one other drug useful in th...
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JP2007204486A |
To provide a novel intermediate compound useful as an intermediate of a compound particularly used for treating cardiac arrhythmia. The compound of formula XLII, a salt or a solvate thereof is useful as the intermediate for preparing the...
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JP2007513961A |
The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form,...
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JP2006342182A |
To provide a intermediate for producing oxabispidine compounds useful as antiarrhythmics and its production method.There is provided epoxy compounds shown by general formula (XLII), wherein R1a expresses an aryl sulfonyl group or the lik...
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JP2006523704A |
The present invention is directed to compounds of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, thes...
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JP3787809B2 |
To provide a method for forming a 7 membered oxathiazepine ring in high yield by controlling a three-dimensional structure. This method for synthesizing an oxathiazepine ring is to synthesize a compound having an oxathiazepine ring expre...
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JP2002510633A5 |
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JP2006515350A |
A compound of formula (I): wherein: represents benzo or pyrido, optionally fused in the 2-3, 3-4 or 4-5 position to a phenyl, (C4-C8)cycloalkyl or heterocyclic group, which may be optionally substituted, W represents X-Y or Y-X, wherein:...
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JP2006511551A |
Aminocyanopyridine compounds are described which are capable of inhibiting mitogen activated protein kinase-activated protein kinase-2. Pharmaceutical compositions and kits are also described, which include an anminocyanopyridine MK-2 in...
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JP2006507255A |
The present invention provides compounds and methods for treatment of viral diseases and cancer.
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JP2006502238A |
A method for manufacturing hydrogen sulphate (alpha S) of the alpha-(2-chlorophenyl)-6,7dihydrothieno[3,2-c]pyridine-5(4H)
-acetic acid methyl ester (clopidogrel hydrogen sulphate) of formula I, in crystalline Form I, wherein the compoun...
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JP2005336088A |
To provide a new bioactive substance having activities for inhibiting MRSA and VRE.The thiazole-based compound is represented by formula A (wherein, R is a group represented by formula B or an amino group). The compound has the anti-MRSA...
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JP2005523275A |
The present invention provides compounds of formula: wherein R a and R b together with the carbon to which they are attached form a group of formula: where each X 1 is independently selected from hydrogen or substituted or unsubstituted ...
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