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7612200 |
Inhibitors of protein kinases
The present invention is directed to a compound having the formula
wherein R 1 , R 2 , R 3 , R 4 , G, and Q are defined herein. The compounds of the present invention are useful as inhibitors...
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7608420 |
Process for the recovery of staurosporine from a fermentation broth
Staurosporine of the formula (I) is recovered from a fermentation broth in a process comprising an ultrafiltration and a diafiltration step.
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7598376 |
Process for the preparation of [1,4,5]-oxadiazepine derivatives
A process for the preparation of [1,4,5]-oxadiazepine derivatives by reaction of N,N′-diacyl-hydrazines with 2,2′-disubstituted diethyl ethers to form 4,5-diacyl-[1,4,5]-oxadiazepines and...
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7589194 |
Crystalline k-252b, sodium salt, methanolate pentahydrate
A crystalline (9S-(9α,10β,12α))-2,3,9,10,11,12-hexahydro-10-hydroxy-10-
(carboxylate)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3′,
2′,1′-k1]pyrrolo[3,4-i][1,6]benzodiazocin-1-one...
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7585972 |
Crystalline K-252α bis(tetrahydrofuranate)
A crystalline (9S-(9α,10β,12α))-2,3,9,10,11,12-hexahydro-10-hydroxy-10-
(methoxycarbonyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3
′,2′,1′-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one...
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7569517 |
4-biphenyl-substituted pyrazolidin-3 5-diones pesticide agent and/or microbicide and/or herbicide
The invention relates to novel 4-biphenyl-substituted 4-substituted pyrazolidine-3,5-diones of the formula (I)
in which
A, D, G, W, X, Y and Z are as defined above, to processes and...
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7482337 |
Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
Disclosed are substituted xanthines of general formula
wherein R 1 to R 4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts...
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7407949 |
Benzamide derivatives as oxytocin agonists and vasopressin antagonists
Novel compounds according to general formula 1, wherein G 1 is NR 5 R 6 or a fused polycyclic group that are specific OT receptor agonists and/or V 1a receptor antagonists. Pharmaceutical...
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7358239 |
Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z...
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7244843 |
Modulators of serotonin receptors
The present invention provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders...
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7238684 |
Benzothiadiazepine derivatives, processes for their preparation and pharmaceutical compositions containing them
The present invention relates to compounds of formula (I): wherein R v , R 1 , R 2 , R x , R y , R 3 , R 4 , R 5 , R 6 , R z and v are as defined within; pharmaceutically acceptable salts,...
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7192953 |
Antibacterial agents
Compounds of formula (I) have antibacterial activity; wherein Q represents a radical of formula —N(OH)CH(═O) or formula —C(═O)NH(OH); Y represents —C(═O)—, —C(═S)—,...
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7132416 |
Benzothiazepine and benzothiazepine derivatives with ileal bile acid transport (IBAT) inhibotory activity for the treatment hyperlipidaemia
The present invention relates to compounds of formula (I) wherein R v , R 1 , R 2 , R x , R y , M, R z , v, R 3 , R 4 , R 5 and R 6 are as defined within; pharmaceutically acceptable salts,...
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7060818 |
Synthesis of macrocyclic tetraamido compounds and new metal insertion process
An improved method of synthesizing a macrocyclic tetraamido compound includes protecting the amino portion of an amino carboxylic acid to form a protected amino carboxylic acid; exposing the...
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7038043 |
Glycosylated indolocarbazole synthesis
Indolocarbazoles are furanosylated (e.g., 7 ) with acetals (e.g., 8 ) or their open chain congeners (e.g., 9 ) under conditions known to promote acetal exchange or formation, such as protic or...
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6921759 |
Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors
Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV...
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6875865 |
Selected derivatives of K-252a
Disclosed herein are selected indolocarbazole derivatives which are represented by the general formula:
The compounds are useful for enhancing the function and/or survival of a trophic factor...
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6852714 |
(Benzodioxan, benzofuran or benzopyran) derivatives having fundic relaxation properties
The present invention of compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk 1 ...
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6844347 |
Substituted 4-amino-2aryl-pyrimidines, their production and use and pharmaceutical preparations containing same
The invention relates to compounds of formula I,
in which R 1 , R 2 , R 3 and R 4 have the meanings given in the claims. Said compounds are valuable active ingredients for the treatment and...
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6806266 |
Staurosporin derivatives
The present invention provides an antitumor agent comprising a staurosporin derivative or a pharmaceutically acceptable salt thereof, as an active ingredient, which is represented by the general...
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6723844 |
Preparation of K-252a
The present invention provides a process for the synthesis of K-252a and intermediates useful in the process.
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6677450 |
Topoisomerase inhibitors
The present invention relates to novel N12, N13-bridged sugar derivatives of indolylopyrrolocarbazoles and pharmaceutical formulations thereof which exhibit topoisomerase-I activity and are useful...
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6660729 |
Particle-forming compositions containing fused pyrrolocarbazoles
A non-aqueous, particle-forming, fused pyrrolocarbazole-containing composition is disclosed. Upon contact with an aqueous medium, the particle-forming composition spontaneously disperses into...
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6635637 |
Cyclic oxyguanidine protease inhibitors
Cyclic oxyguanidine compounds, including compounds of Formulae I and II: wherein R 1 , R 3 -R 6 , R 21 -R 26 , L, Y, Z, and A are set forth in the specification, as well as hydrates, solvates or...
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6624157 |
Thiadioxobenzodiazepine inhibitors of farnesyl protein transferase
Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formulas and their enantiomers, diastereomers, and their...
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6552187 |
Process for the preparation of herbicidal derivatives
A process for the preparation of compounds of formula (I), which process comprises reacting a compound of formula (II), in an inert organic solvent, optionally in the presence of a base, with a...
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6500818 |
Naphthalenecarboxamides as tachykinin receptor antagonists
Compounds having the following formula wherein L, M, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X 1 and X 2 are as defined in the specification, pharmaceutically-acceptable salt thereof, useful for...
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6472385 |
Compositions and methods to enhance cancer chemotherapy in p53 defective tumors
Compositions which abrogate DNA damage induced cell cycle arrest thereby enhancing the cell killing activity of DNA damaging anticancer agents for use in the treatment of cancer, and in particular,...
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6451787 |
Remedies for ocular diseases
Use of the compound represented by general formula (I) for remedies of and protection against eye diseases is disclosed. General formula (I): (wherein, R 1 and R 2 independently represent a...
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RE37781 |
Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors
This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of...
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6410480 |
Herbicidally active 3-hydroxy-4-aryl-5-oxopyrazoline derivatives
The present invention relates to novel herbicidally active 3-hydroxy-4-aryl-5-oxopyrazoline derivatives, to processes for their preparation, to compositions which comprise these compounds and may...
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6359129 |
Amino acid-derived, 7-membered cyclic sulfamides and methods of synthesizing the same
New sulfamide compounds and methods of forming those compounds are provided. The inventive methods comprise subjecting a template opened-ring sulfamide compound to a ring-closing metathesis...
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6225306 |
Biphenyl derivatives and drug composition
A biphenyl derivative represented by the following general formula (1) and a pharmaceutically acceptable salt thereof: ##STR1## [In the formula (1), A represents a single bond, --CH 2 --, --CO--,...
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6197955 |
Production of staurosporine derivative using acid isomerization
A staurosporine derivative with anti-cancer activity and anti-bacterial activity is produced by acidifying a solution containing staurosporine to isomerize staurosporine to its desired derivative,...
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6156746 |
1,2,5-benzothiadiazepine-1,1-dioxides with n-2 imidazolylalkyl substituents
Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formula ##STR1## and their enantiomers, diastereomers, and their...
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6080758 |
Benzenesulfonamide derivatives as bradykinin antagonists
The present invention relates to compounds selected from the group consisting of the compounds of formula (I): ##STR1## X is a halogen atom, A is --CH 2 --, --CH(OH)--, --CH(NH--COCH 3 )-- or S, R...
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5882544 |
Polycyclic iminooxadiazinediones from (cyclo)aliphatic 1,4-diisocyanates
The present invention relates to polycyclic iminooxadiazinediones A corresponding to formula I ##STR1## The present invention also relates to mixtures of these polycyclic iminooxadiazinediones with...
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5827846 |
Carbazole derivatives as agents against multi-drug resistance
The utility of known and novel staurosporin derivatives of formula I ##STR1## wherein R 1 is formyl, an aliphatic hydrocarbon radical having up to 29 carbon atoms that is unsubstituted or...
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5780461 |
Therapeutic treatment of cancer with Protein Kinase C inhibitors
This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## The invention further provides the preparation, pharmaceutical formulations and the methods of use...
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5760222 |
Thiadiazole dioxide derived oxaziridines as bleaching compounds
Bleaches, a method for bleaching substrates using these materials and detergent compositions containing same are reported. The bleaches are thiadiazole dioxide derived mono- and di- oxaziridines....
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5760028 |
Integrin receptor antagonists
This invention relates to novel heterocycles including 3- 1- 3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-
(benzylo xycarbonylamino)propionic acid, which are useful as antagonists of...
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5756494 |
Protein kinase inhibitors for treatment of neurological disorders
The invention features novel derivatives of K-252a, as well as novel bis-N-substituted derivatives of staurosporine. The invention also features a method for treating diseased neuronal cells...
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5698691 |
Condensed cyclic compounds and their use
Disclosed is a squalene synthetase inhibitor which comprises the compound represented by the formula ##STR1## wherein R 1 is hydrogen or an optionally substituted hydrocarbon group; R 2 is...
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5674867 |
Indolocarbazole derivatives and therapeutic method for stimulating megakaicyocyte production
The present invention relates to therapeutic agents for thrombocytopenia which contain an indolocarbazole derivative represented by the formula (I) given below or a pharmaceutically acceptable salt...
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5668271 |
Indolopyrrolocarbazole derivatives
Indolopyrrocarbazole derivatives represented by formula (I) and the pharmaceutically acceptable salts thereof have excellent antitumor activity as evidenced by their in vitro proliferation...
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5654427 |
Indolocarbazole derivatives to treat a pathological condition of the prostate
The invention features a method of treating a pathological condition of the prostate gland, e.g., benign prostatic hypertrophy or prostate cancer, in a mammal, said method comprising administering...
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5621100 |
K-252a derivatives for treatment of neurological disorders
The invention features novel derivatives of K-252a, as well as novel bis-N-substituted derivatives of staurosporine. The invention also features a method for treating diseased neuronal cells...
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5618809 |
Indolocarbazoles from saccharothrix aerocolonigenes copiosa subsp. nov SCC 1951 ATCC 53856
N-alkanoyl derivatives of staurospodne represented by the formula I ##STR1## wherein R a and R b are each H or ##STR2## wherein R 1 and R 2 are independently H or --OH or --OCH 3 and R 3 is...
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5605898 |
Anellated triazole compounds
Disclosed are novel anellated triazole compounds of formula, in which R A , m, n, X--X, V, W and Q have the meaning stated in the specification; a method of their preapartion; and their use as...
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5604219 |
Indolocarbazole derivatives that stimulate platelet production
Disclosed is an indolocarbazole derivative represented by the following formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## [wherein R 1 represents substituted or unsubstituted...
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