- BENZOXAZEPIN COMPOUNDS SELECTIVE FOR PI3K P110 DELTA AND METHODS OF USE
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Benzoxazepin Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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- QUINAZOLINAMIDE DERIVATIVES
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Novel quinazolinamide derivatives of the formula (I), in which R1-R5 and X have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the in
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Page/Page column 41
(2011/10/13)
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- Design and synthesis of cyclic sulfonamides and sulfamates as new calcium sensing receptor agonists
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The design, synthesis and calcimimetic properties of various cyclic sulfonamides and sulfamates are described. The latter were prepared from the corresponding o-alkenylarenesulfonamides via copper- or rhodium-catalyzed intramolecular aziridination. The si
- Kiefer, Lionel,Gorojankina, Tatiana,Dauban, Philippe,Faure, Hélène,Ruat, Martial,Dodd, Robert H.
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scheme or table
p. 7483 - 7487
(2011/02/21)
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- Selective angiotensin II AT2 receptor agonists: Benzamide structure-activity relationships
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In the investigation of the structure-activity relationship of nonpeptide AT2 receptor agonists, a series of substituted benzamide analogues of the selective nonpeptide AT2 receptor agonist M024 have been synthesised. In a second ser
- Wallinder, Charlotta,Botros, Milad,Rosenstr?m, Ulrika,Guimond, Marie-Odile,Beaudry, Hélène,Nyberg, Fred,Gallo-Payet, Nicole,Hallberg, Anders,Alterman, Mathias
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p. 6841 - 6849
(2008/12/22)
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- THIOUREAS AS FACTOR Xa INHIBITORS
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The present invention is directed to compounds represented by Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
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Page/Page column 45
(2010/11/08)
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- 5-AMIDINO-2-HYDROXYBENZENESULFONAMIDE DERIVATIVES, MEDICINAL COMPOSITIONS CONTAINING THE SAME, MEDICINAL USE THEREOF AND INTERMEDIATES IN THE PRODUCTION THEREOF
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The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, an optionally substituted lower alkenyl group, a cycloalkyl group or a lower acyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom or a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same and an intermediate thereof. These compounds are useful as preventives or remedies for various diseases such as brain infarction, cerebral thrombosis, cerebral embolism, TIA, cerebral vascular jerk, Alzheimer's diseases, myocardial infarction, heart attack, heart failure, thrombosis, pulmonary infarction and pulmonary embolism.
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- Inhibitors of factor Xa
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Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
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Page column 200
(2010/02/05)
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- ISOXAZOLINE, ISOTHIAZOLINE AND PYRAZOLINE FACTOR Xa INHIBITORS
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Isoxazolines, isothiazolines and pyrazolines which are inhibitors of Factor Xa, pharmaceutical compositions containing these compounds, and methods of using these compounds as anticoagulant agents for treatment and prevention of thromboembolic disorders.
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Page/Page column 15-16
(2010/02/06)
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- OXYGEN OR SULFUR CONTAINING 5-MEMBERED HETEROAROMATICS AS FACTOR Xa INHIBITORS
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The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula (I), or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is O or S and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.
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- Factor xa inhibitors with aryl-amidines and derivatives, and prodrugs thereof
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The present invention relates to a compound with aryl-amidines, particularly amidinoaryl-cyclopropanes, amidinoarylmethyl-pyrroles, amidinoaryl-benzenes, amidinoaryl-pyridines, or amindonoaryl-alanines, represented by formula (1), a pharmaceutically acceptable salt, a prodrug, a hydrate, a solvate or an isomer thereof, which are inhibitors of coagulation enzyme, factor Xa (FXa). The present invention also relates to a pharmaceutical composition containing the compound, and a method of using the same as an anticoagulant agent for treatment and prevention of thrombosis disorders.
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- Inhibitors of factor Xa
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Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
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- Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P1 structure-activity relationships of the substituted 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides
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Based on DuPont Pharmaceuticals' monobenzamidine lead structure SN429, we have designed the biphenyl 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides as a novel series of non-basic factor Xa inhibitors. We have discovered that the displacement of the benzamidine moiety with substituted 2-naphthyl structures not only results in highly potent factor Xa inhibitors, but also significantly increases their enzyme specificity and oral bioavailability.
- Jia, Zhaozhong J.,Wu, Yanhong,Huang, Wenrong,Goldman, Erick,Zhang, Penglie,Woolfrey, John,Wong, Paul,Huang, Brian,Sinha, Uma,Park, Gary,Reed, Andrea,Scarborough, Robert M.,Zhu, Bing-Yan
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p. 1651 - 1655
(2007/10/03)
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- Phenyl-isoxazoles as factor XA Inhibitors
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The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is O or S and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.
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- Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors1
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A series of potent and selective factor Xa inhibitors was synthesized using various readily available amino acids as central templates. The most potent compound displays IC50 of 3 nM.
- Su, Ting,Wu, Yanhong,Doughan, Brandon,Jia, Zhaozhong J.,Woolfrey, John,Huang, Brian,Wong, Paul,Park, Gary,Sinha, Uma,Scarborough, Robert M.,Zhu, Bing-yan
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p. 2947 - 2950
(2007/10/03)
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- 6-membered aromatics as factor Xa inhibitors
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The present application describes 6-membered aromatics of formula I: or pharmaceutically acceptable salt forms thereof, wherein D may be CH2NH2 or C(=NH)NH2, which are useful as inhibitors of factor Xa.
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- ISOXAZOLINE, ISOTHIAZOLINE AND PYRAZOLINE FACTOR XA INHIBITORS
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Isoxazolines, isothiazolines and pyrazolines which are inhibitors of Factor Xa, pharmaceutical compositions containing these compounds, and methods of using these compounds as anticoagulant agents for treatment and prevention of thromboembolic disorders. The compounds can be represented by the formula: STR1 where X is O, S or NR 15.
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- PYRAZOLE DERIVATIVES AS ANGIOTENSIN II ANTAGONISTS
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Compounds of general formula I and their salts and solvates are angiotensin II receptor antagonists and as such are useful in the treatment of hypertension, congestive heart failure and elevated intraocular pressure. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.
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- SUBSTITUTED 1,2,4-TRIAZOLIN-3-ONE COMPOUNDS BEARING ACIDIC FUNCTIONAL GROUPS AS BALANCED ANGIOTENSIN II ANTAGONISTS
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Novel substituted 1,2,4-triazolin-3-ones of the formula (I) are useful as angiotensin II antagonists. STR1
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- SUBSTITUTED PYRAZOLES, COMPOSITIONS AND USE
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Substituted pyrazole compounds are angiotensin II antagonists and therefore useful in the treatment of hypertension, and related cardiovascular disorders and ocular hypertension. These compounds have the general formula I: STR1
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- Angiotensin-II receptor blocking, heterocycle substituted imidazoles
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Novel heterocycle substituted imidazoles of Formula (I), which are useful as angiotensin-II antagonists, are disclosed: STR1
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