Heterocyclic Compounds

Matches 201 - 250 out of 809	< 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 >

Document	Document Title
WO1999051238A9	SEMI-SYNTHETIC ECTEINASCIDINS The present invention is directed to several newly prepared semi-synthetic ecteinascidin (Et) species, designated herein as Et 757, Boc-Et 729, Iso-Et 743, Et 875, and Et 1560. The physical properties of these compounds, their preparatio...
WO/1999/061414A1	NOVEL SUBSTITUTED GUANIDINE DERIVATIVES AND PROCESS FOR PRODUCING THE SAME Compounds represented by general formula (1) which are useful as remedies and preventives for diseases caused by acceleration in the sodium/proton exchange system, wherein R¿1?, R¿2?, R¿3?, R¿4? and R¿5? represent each hydrogen, alk...
WO/1999/051570A1	ANION-COMPLEXING COMPOUND, METHOD OF PREPARING THE SAME, AN ION-SELECTIVE MEMBRANE AND A SENSOR PROVIDED WITH SUCH A COMPOUND OR MEMBRANE Disclosed is an anion-complexing compound (I) wherein R1 and A represent an aromatic 6-ring, Y' represents a -NHC(X)NH-group, and Y' represents a rest selected from the group -NHC(X')-, -C(X')NH- and -NHC(X')NH-, wherein X and X', indepe...
WO/1999/043670A1	BENZYLPIPERAZINYL- AND BENZYLPIPERIDINYL ETHANONE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS DOPAMINE D¿4? RECEPTOR ANTAGONISTS Disclosed are compounds of formula (I) or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH; R¿1?, R¿2? and R¿3? represents hydrogen, halogen, hydroxy, alkoxy, alkyl, triflu...
WO/1999/036403A1	NOVEL DOPAMINE RE-UPTAKE INHIBITORS AND METHODS OF SYNTHESIZING AND USING THE SAME The invention comprises dopamine re-uptake inhibitors, and methods of making and using such inhibitors. The inhibitors include methylphenidate, $i(threo-)methylphenidate, and analogs thereof.
WO/1999/032451A1	AZEPINE OR LARGER MEDIUM RING DERIVATIVES AND THEIR USE AS PHARMACEUTICALS Selected novel azepine and larger medium ring compounds are effective for prophylaxis and treatment of inflammation, tissue degradation and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutical...
WO/1999/020599A1	PHARMACEUTICALLY ACTIVE COMPOUNDS AND METHODS OF USE The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the inv...
WO/1999/009991A1	NOVEL AMIDE DERIVATIVES Disclosed are the novel compounds represented by structural Formula (I), wherein A is a lipophilic group comprising an aliphatic bridging group, B is a lipophilic group, D is a group having at least one amino or substituted amino group a...
WO/1999/002514A2	EPOTHILONE DERIVATIVES The present invention relates to compounds of formula (V).
WO/1999/000362A1	SYNTHESIS OF AMINOCARBONYL SUBSTITUTED LACTAMS The invention relates to an efficient and facile method for the preparation of substituted lactams represented by general formula (I), wherein n can be zero or an integer of one or more; and R, R?1¿, and R?2¿ are independently selected...
WO/1998/054152A1	AZACYCLOOCTANE AND HEPTANE DERIVATIVES, THEIR PREPARATION AND USEIN THERAPY The present invention discloses compounds of formula (1) or (2), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycl...
WO/1998/052925A1	ANALOGS OF DUOCARMYCIN AND CC-1065 Analogs and derivatives of duocarmycin and CC-1065 are provided. The compounds have use as antitumor antibiotics and as cell toxicity agents. The compounds have sequences specific DNA alkylating activity.
WO/1998/051298A1	ARYLSUBSTITUTED PIPERAZINES USEFUL IN THE TREATEMENT OF BENIGN PROSTATIC HYPERLASIA This invention relates to a series of arylsubstituted piperazines, of Formula (I), pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the...
WO/1998/051702A1	METHODS AND COMPOSITIONS FOR DESTRUCTION OF SELECTED PROTEINS Compounds having an ansamycin antibiotic, or other moiety which binds to hsp90, coupled to a targeting moiety which binds specifically to a protein, receptor or marker can provide effective targeted delivery of the ansamycin antibiotic l...
WO/1998/035941A1	NEW BENZOLACTAM DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME Compounds represented by general formula (I) or pharmacologically acceptable salts thereof, or hydrates of both, (wherein R?1� and R?2� are each independently a hydrogen atom, a halogen atom, etc.; R?3� is a lower alkyl group which...
WO/1998/030551A1	MACROCYCLIC INHIBITORS OF MATRIX METALLOPROTEINASES AND TNF$g(a) SECRETION Macrocyclic compounds of formula (I) are potent inhibitors of matrix metalloproteinase and are useful in the treatment of diseases in which matrix metalloproteinase play a role. Also disclosed are matrix metalloproteinase inhibiting comp...
WO/1998/023594A1	CYTOTRIENINS, PROCESS FOR PREPARING THE SAME, AND ANTITUMOR AGENT An antitumor agent comprising cytotrienin (I), (II), (III), or (IV) as the active ingredient, characterized by being produced by culturing a bacterium capable of producing cytotrienin (I), (II), (III), or (IV) represented by general form...
WO/1997/047625A1	TRICYCLIC BENZAZEPINE VASOPRESSIN ANTAGONISTS Tricyclic compounds of general formula (I) as defined herein which exhibit antagonist activity at V1 and/or V2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases character...
WO/1997/032860A1	BENZODIAZONINE DERIVATIVES BINDING TO CHOLECYSTOKININ OR GASTRIN RECEPTORS Compounds of formula (I), wherein one of U and V is -CHR2-, and the other of U and V is selected from -N(COR4)-, -CH(COR4)-,-N(SO2R4)- and -CH(SO2R4)-, in which R2 is H, -COOR5, -CONR6R7 or -COR7 and R4 is H, C1 to C6 hydrocarbyl (in whi...
WO/1997/030054A1	PHARMACEUTICALLY ACTIVE COMPOUNDS AND METHODS OF USE The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof, 1,2,3,4-tetrahydroisoquinolinyl, benz[cd]indol...
WO/1997/009328A1	PHENYLOXAZOLIDINONES HAVING A C-C BOND TO 4-8 MEMBERED HETEROCYCLIC RINGS A compound of formula (I), or pharmaceutical acceptable salts thereof wherein X is NR1, S(O)g, or O; R1 is H, C1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R1 is -(CH2)h-aryl, -COR1-1, -COOR1-2, -CO-(CH2)h-COR1-1...
WO/1997/003978A1	NOVEL HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF PAIN AND USE THEREOF Polycyclic alkaloids of formula (I), wherein R1 is H, C1-6 alkyl, or C6-12 aryl optionally substituted with polar groups; R2 and R3 are independently H, OH, C1-6 alkyl, -C(NH)-NH2, a positively charged group, or C7-13 aralkyl optionally ...
WO/1997/003979A1	POLYCYCLIC ALCALOID-DERIVATIVES AS NMDA-RECEPTOR ANTAGONISTS Polycyclic alkaloids of formula (I), wherein R1 is H, C1-6 alkyl, or C6-12 aryl optionally substituted with polar groups; R2 abd R3 are independently H, OH, C1-6 alkyl, -C(NH)-NH2, a positively charged group, or C7-13 aralkyl optionally ...
WO/1996/034525A1	INDUCEMENT OF THERMOTOLERANCE WITH BENZOQUINONOID ANSAMYCINS Thermotolerant phenotypes are developed in cells, tissues, organs and organisms by the administration of benzoquinonoid ansamycins such as herbimycin A and any of various analogs. The general stress tolerance resulting from this induceme...
WO/1996/033175A1	CYCLIC AMIDINO AGENTS USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS The current invention discloses amidino derivatives of formula (I) useful as nitric oxide synthase inhibitors wherein R1 is selected from the group consisting of cycloalkyl, heterocyclyl and aryl, which may optionally be substituted; L i...
WO/1996/016059A1	6-METHOXY-1H-BENZOTRIAZOLE-5-CARBOXAMIDE DERIVATIVES, PROCESS FOR PRODUCING THE SAME, AND MEDICINAL COMPOSITION CONTAINING THE SAME A 6-methoxy-1H-benzotriazole-5-carboxamide derivative represented by general formula (I) or pharmacologically acceptable acid-addition salts thereof, a process for producing the same, a medicinal composition containing a compound of form...
WO/1996/014844A1	CYCLIC AMIDINE ANALOGS AS INHIBITORS OF NITRIC OXIDE SYNTHASE Disclosed herein are the heterocyclic compounds and pharmaceutically acceptable salts thereof which have been found to be useful in the treatment of nitric oxide synthase mediated diseases and disorders.
WO/1996/015114A1	COMPOUNDS UCF116 Compounds UCF116 represented by general formula (I) and having activities as antibacterial and antitumor drugs, thus being useful as such, wherein Q1 represents formula (II) etc., and Q2 represents formula (III) etc.
WO/1996/013478A1	MONO- OR POLYENIC CARBOXYLIC ACID DERIVATIVE Novel retinoid-related compounds that can substitute for retinoic acid as preventives or remedies for various diseases and compounds that are antagonistic to retinoids, i.e., heterocyclic compounds represented by the general formula (1-I...
WO/1996/011192A1	LTA4 HYDROLASE INHIBITORS The present invention provides compounds of the formula Ar1-Q-Ar2-Y-R-Z and pharmaceutically acceptable salts thereof wherein Ar1 and Ar2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety...
WO/1996/009299A1	DRUGS TO IMPROVED SYNAPTIC TRANSMISSION Peripherally administered Brefeldin A and its analogs and derivatives are used to enhance learning and reverse memory dysfunction through induced long term potentiation in hippocampal tissues.
WO/1996/008250A1	FIBRINOGEN RECEPTOR ANTAGONISTS Fibrinogen receptor antagonists having formula (I) for example (a).
WO/1995/023788A1	IMPROVED PROCESS FOR THE ACYLATION OF LACTAMS High quality acyl lactams are prepared by reacting a lactam, an anhydride of a carboxylic acid, and an acylating acid, preferably in the presence of a base catalyst. The process affords acyl lactams in high yield and at lower reaction te...
WO/1995/021614A1	NEW PROTEIN TRAFFICKING INHIBITORS Novel compounds related structurally to Brefeldin A useful as antiviral, antifungal, antiproliferative, immunosuppressive and detoxifying agents as well as pharmaceutical compositions and methods based thereon are disclosed.
WO/1995/011231A1	AMIDINO DERIVATIVES USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS The current invention discloses useful pharmaceutical compositions containing amidino derivatives of formula (I) as nitric oxide synthase inhibitors.
WO/1995/003289A1	BENZO-FUSED LACTAMS PROMOTE RELEASE OF GROWTH HORMONE There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production...
WO/1995/001342A1	ANSAMYCIN DERIVATIVES AS ANTIONCOGENE AND ANTICANCER AGENTS A compound of formula (I) and pharmaceutically acceptable salts and prodrugs thereof wherein R1, R2, R3, R4, R5 and R6 are as defined below, methods and intermediates useful in the preparation thereof, pharmaceutical compositions thereof...
WO/1994/008578A2	TUMORICIDAL ACTIVITY OF BENZOQUINONOID ANSAMYCINS AGAINST PROSTATE CANCER AND PRIMITIVE NEURAL MALIGNANCIES The invention provides methods and compositions for treating selected human malignancies including use of certain ansamycin benzoquinones.
WO/1994/006774A1	ANTI-INFLAMMATORY MACROLACTAM (CYCLAMENOL) The invention relates to the natural substance cyclamenol of formula (Ia), a process for producing it from micro-organisms of the actinomycetal order, especially the Streptomyces strain MHW 846, chemical derivatives thereof, and their us...
WO/1994/005634A1	BENZO-FUSED LACTAMS PROMOTE RELEASE OF GROWTH HORMONE There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production...
WO/1994/002447A1	HYDROXAMIC ACID DERIVATIVES AS METALLOPROTEINASE INHIBITORS Compounds of formula (I) have matrix metalloproteinase inhibitory activity, wherein R2 represents a group R6-A- wherein A represents a divalent straight or branched, saturated or unsaturated hydrocarbon chain of up to 6 C atoms which may...
WO/1994/002446A1	NATURAL AMINO ACID DERIVATIVES AS METALLOPROTEINASE INHIBITORS Compounds of Formula (I) wherein R2 represents a group R6-A- wherein A represents a divalent straight or branched, saturated or unsaturated hydrocarbon chain of up to 6 C atoms which may be interrupted by an O or S atom, and R6 represent...
WO/1994/001100A1	METHODS AND COMPOSITIONS FOR INHIBITING 5alpha-REDUCTASE ACTIVITY Disclosed is a novel class of antiandrogenic compounds including saturated and unsaturated fatty acids, their derivatives, and synthetic analogs, their method of synthesis, and their use in treating disorders associated with androgenic a...
WO/1993/016997A1	2,3,4,5-TETRAHYDRO-1H_-3-BENZAZEPINES HAVING ANTI-PSYCHOTIC ACTIVITY, AND SYNTHESIS OF alpha-SUBSTITUTED-ARYLACETAMIDES A novel process for the preparation of alpha-substituted arylacetamides wherein the substituent is an aromatic group or a 1-alkenyl or 1-cycloalkenyl group and wherein the nitrogen atom carries no hydrogen atoms comprises the reaction of...
WO/1993/014215A1	PROCESS AND USES FOR 4,5-DIHYDROGELDANAMYCIN AND ITS HYDROQUINONE A process for the fermentation and isolation of compounds (I) and (II), members of the ansamycin benzoquinone antibiotics family, having formulae (I) and (II), as well as the chemical synthesis of compound (II) from coumpound (I) are dis...
WO/1993/008192A1	AZABICYCLO ARYLACETYLENE AND ARYLENYNE OXIMES AS CHOLINERGIC AGENTS AND METHODS OF TREATMENT Pharmaceutically useful nitrogen containing cyclic oxime substituted compounds which are arylacetylene and arylenyne azabicyclo [2.2.1] oximes of formula (I) which are useful for alleviating pain and for treating cognitive decline are de...
WO/1993/004682A1	NOVEL 4-ARYLPIPERAZINES AND 4-ARYLPIPERIDINES Compounds of general formula (I) are disclosed as novel antipsychotic agents.
WO/1993/004684A1	NOVEL 4-ARYLPIPERAZINES AND 4-ARYLPIPERIDINES Compounds of the general formula (I) are disclosed as novel antipsychotic agents.
WO/1992/012133A2	ARTHROPODICIDAL CARBOXANILIDES Compounds of formula (I), wherein Q, X, R?1�, R?2�, R?9� and Z are as defined in the text, including compositions containing said compounds and a method for using them to control arthropods.
WO/1992/006079A1	FUSED RING ANALOGS OF NITROGEN CONTAINING NONAROMATIC HETEROCYCLES The present invention relates to novel fused ring analogs of nitrogen containing heterocycles, and specifically, to compounds of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, x, y, and z and m are defined as below. These novel com...

Matches 201 - 250 out of 809	< 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 >