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| Number | Title | Issue Date |
| 8158796 | Process for the preparation of Rho-kinase inhibitor compounds The present invention is directed to practical high-yielding synthetic processes to prepare compounds of general Formula III, IV, V, VII, VIII, IX, X, XII, XIV, and XV. Such compounds are useful as final products or can be used as intermediates and be further modifi... | 04/17/2012 |
| 7429667 | Phenylamino isothiazole carboxamidines as MEK inhibitors The invention concerns compounds which inhibit MEK and which have activity as anti-neoplastic agents. These compounds include N-substituted-3-hydroxy-5-arylamino-isothiazole-4-carboxamidines. Also included are the tautomeric isothiazol-3(2H)-ones. ... | 09/30/2008 |
| 7157468 | Pyrazole derivatives This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R1 to R4, n W, X and Y are defined in the descript... | 01/02/2007 |
| 7053112 | Imidazolidinedione analogs useful as anticoagulants and antithrombotics A compound is disclosed, which is useful in treating a mammal having a disease-state characterized by thrombotic activity. The compound is of the following formula: wherein A, B, R1 | 05/30/2006 |
| 7030150 | Benzimidazole compounds and antiviral uses thereof The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion associated events such as viral transmission, reduce viral load or o... | 04/18/2006 |
| 6855717 | Tetrahydroisoquinoline derivatives as modulators of dopamine D3 receptors Compounds of formula (I): wherein: R2 represents a hydrogen atom or a C1-4alkyl group; q is 1 or 2; A represents a ... | 02/15/2005 |
| 6849617 | Tissue factor antagonists and methods of use thereof The invention includes pharmaceutically active compounds and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for treating or prophylaxis of undesired thrombo... | 02/01/2005 |
| 6825213 | β3-adrenoreceptor agonists, agonist compositions and methods of using The invention provides β3-adrenoreceptor agonists, pharmaceutical compositions comprising β3-adrenoreceptor agonist compounds, and methods of using such compounds for stimulating, regulating or modulating metabolism of fats in adipose tissue ... | 11/30/2004 |
| 6770657 | Compounds The invention relates to novel isoquinolines and their use as anticonvulsant and in the treatment of a variety of disorders. ... | 08/03/2004 |
| 6730783 | Process for preparing aminoguanidines and alkoxyguanidines as protease inhibitors Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra | 05/04/2004 |
| 6638931 | Aminoguanidines and alkoxyguanidines as protease inhibitors Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: ##STR1## wherein X is O or NR9 and R1 -R4, R6 -R9, R11, R12, Ra, Rb, R | 10/28/2003 |
| 6602867 | Triazole compounds with dopamine-D3-receptor affinity Triazole compounds of the following formula ##STR1## where R1, R2, A and B have the meanings given in the description are described. The compounds according to the invention possess a high affinity for the dopamine D3 rece... | 08/05/2003 |
| 6602864 | Sulfonic acid or sulfonylamino N-(heteroaralkyl)-azaheterocyclylamide compounds The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibit... | 08/05/2003 |
| 6596752 | Inhibitors of 댔댡 mediated cell adhesion The present invention relates to small molecules according to the formula [I]: ##STR1## which are potent inhibitors of 댔ଲ.sub.1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing | 07/22/2003 |
| 6562828 | Amidine compounds A compound of the formula [I] ##STR1## wherein R1, R2 and R3 are the same or different and each is hydrogen atom, ##STR2## wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof. T... | 05/13/2003 |
| 6541632 | Process for producing heterocyclic nitriles A carbocyclic or heterocyclic compound, ammonia and an oxygen-containing gas are subjected to fluid catalytic reaction in vapor phase in the presence of a catalyst containing alkali metal to produce an aromatic or heterocyclic nitrile. The use of the cata... | 04/01/2003 |
| 6518310 | Aminoguanidines and alkoxyguanidines as protease inhibitors Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: ##STR1## wherein X is O or NR9 and R1 -R4, R6 -R9, R11, R12, Ra, Rb, R | 02/11/2003 |
| 6504031 | Naphthamidine urokinase inhibitors Compounds having the formula: ##STR1## are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions, methods for the preparation of urokinase-inhibitors, and ... | 01/07/2003 |
| 6500823 | Unsaturated hydroximic acid derivatives as per abstract inhibitors ##STR1## The object of the invention consists of novel unsaturated hydroximic acid derivatives, the process for their preparation and as active substance such as compounds containing pharmaceutical compositions. The novel compounds possess valuable pharma... | 12/31/2002 |
| 6495692 | Helium-neon excitable reticulocyte dyes derivable from halolepidines A method for synthesizing dyes excitable by a helium-neon laser (excitable at 633 nm) from hololepidines, e. G., 7-halolepidine, which dyes are suitable for the detection and enumeration of reticulocytes in human blood samples. In another aspect, this inv... | 12/17/2002 |
| 6492401 | N-[(substituted five-membered di- or triaza diunsaturated ring)carbonyl] guanidine derivatives for the treatment of ischemia NHE-1 inhibitors, methods of using such NHE-1 inhibitors and pharmaceutical compositions containing such NHE-1 inhibitors. The NHE-1 inhibitors are useful for the reduction of tissue damage resulting from tissue ischemia.... | 12/10/2002 |
| 6476226 | Isoxazoline fibrinogen receptor antagonists This invention relates to novel isoxazolines and isoxazoles of formula (I): ##STR1## or a pharmaceutically acceptable salt or prodrug form thereof. The invention relates to novel isoxazolines which are useful as antagonists of the platelet glycoprotein II... | 11/05/2002 |
| 6472404 | HIV protease inhibitors The present invention discloses novel isoquinoline carboxamide derivatives which are HIV protease inhibitors or prodrugs thereof, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the co... | 10/29/2002 |
| 6413990 | Arylsulphonamide-substituted benzimidazoles having tryptase-inhibiting activity Bezimidazole derivatives of general formula (I) ##STR1## having tryptase-inhibitory activity. Exemplary are: N-{2-[2-(4-amidinophenyl)-ethyl]-1-methyl-benzimidazol-5-yl}-N-diethylamino ethyl-(4-ethoxycarbonyl-benzenesulphonamide)-hydrochloride, N-{2-[2-(4-amidi... | 07/02/2002 |
| 6365584 | Arylysulphonamide-substituted benzimidazoles having tryptase-inhibiting activity Arylsulphonamide-substituted benzimidazole derivatives of formula (I) ##STR1## having tryptase-inhibiting activity. Exemplary are: 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethylaminoethyl)-benzenesu lphonylamino]-benzimidazole; 1-Methyl-2-[2-(4-amidinop... | 04/02/2002 |
| 6344466 | Benzamide and sulfonamide substitued aminoguanidines and alkoxyguanidines as protease inhibitors The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: ##STR1## wherein X is O or NH, L is --O-- or --SO2 --, and R1 -R4, R9 -R19, Ra... | 02/05/2002 |
| 6331640 | Diaminopropionic acid derivatives A compound of formula 1a ##STR1## which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.... | 12/18/2001 |
| 6323215 | Neurotrophic tetrahydroisoquinolines and tetrahydrothienopyridines, and related compositions and methods This invention provides compounds having the following general structure: ##STR1## This invention also provides pharmaceutical compositions comprising same and methods of using these compositions to treat and prevent disorders characterized by neuronal da... | 11/27/2001 |
| 6303782 | Process for preparing benzylnitriles A process is described for preparing an aromatic compound substituted by a tertiary nitrile of Formula (1.0.0): ##STR1## comprising treating a substituted aromatic compound of Formula (2.0.0): ##STR2## with a secondary nitrile of Formula (3.0.0): ##S... | 10/16/2001 |
| 6288071 | 1-ethylene-2-alkylene-1,4-cyclohexadiene pesticides Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.... | 09/11/2001 |
| 6281227 | Sulfonic acid sulfonylamino n-(heteroaralkyl)-azaheterocyclylamide compounds The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibit... | 08/28/2001 |
| 6262123 | Ortho-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them Ortho-substituted benzoylguanidines of the formula I ##STR1## in which R(1) to R(4) have the meanings given in the claims, are suitable, as antiarrhythmic pharmaceuticals having a cardioprotective component, for the prophylaxis and treatment of infarction... | 07/17/2001 |
| 6235778 | Aminoguanidines and alkoxyguanidines as protease inhibitors Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: ##STR1## wherein X is O or NR9 and R1 14 R4, R6 -R9, R11, R12, Ra, Rb, R | 05/22/2001 |
| 6201006 | Aromatic amidine derivatives useful as selective thrombin inhibitors The present invention relates to a novel thrombin inhibitor which is effective even when orally administered. More specifically, the present invention relates to an aromatic amidine derivative represented by formula (I) and the salts thereof, which show p... | 03/13/2001 |
| 6166030 | Compounds There are provided novel compounds of formula (I) ##STR1## wherein R1 represents a 2-thienyl or 3-thienyl ring and R2 represents C 1 to 4 alkyl and optical isomers and racemates thereof and pharmaceutically acceptable salts ther... | 12/26/2000 |
| 6117874 | Benzopyran and benzo-fused compounds, their preparation and their use as leukotriene B4 (LTB4 ) antagonists This invention relates to novel benzopyran and other benzo-fused leukotriene B4 (LTB4) antagonists and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds, and to a method of using ... | 09/12/2000 |
| 6040314 | Bicyclic isothiourea derivatives useful in therapy There are provided novel compounds of formula I ##STR1## wherein D represents alkyl C1 to 6; T represents a C3-5 saturated or unsaturated alkylene chain substituted by --(CH2)m -- NXY; --O--(CH2)z --N... | 03/21/2000 |
| 6034097 | Isoquinolines useful as analgesics The present invention is directed to compounds that act as analgesics and that have the structure of formula (I): ##STR1## wherein; Z is ##STR2## wherein, n is 1 or 2, and R0 is C6-12 aryl or C7-8 aralkyl; o... | 03/07/2000 |
| 6011063 | Ortho-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them Ortho-substituted benzoylguanidines of the formula I ##STR1## in which R(1) to R(5) have the meanings given in the claims, are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and for infarct trea... | 01/04/2000 |
| 5977074 | Inhibitors of ଲ-amyloid protein production This invention relates to compounds and pharmaceutical compositions, and methods for inhibiting or preventing the amyloid protein deposits in the brain which are associated with Alzheimer's disease and aged Down's syndrome patients. More particularly, it ... | 11/02/1999 |
