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| Number | Title | Issue Date |
| 8450305 | Macrocyclic compounds useful as inhibitors of kinases and HSP90 Disclosed are macrocyclic compounds of formulae I-V, which are analogs of the pochonin resorcylic acid lactones, and processes for the preparation of the compounds. The compounds disclosed are useful as inhibitors of kinases and Heat Shock Protein 90 (HSP 90). Also ... | 05/28/2013 |
| 7514425 | Short-acting sedative hypnotic agents for anesthesia and sedation The invention provides compounds compositions and methods useful for inducing or maintaining general anesthesia or sedation in mammals. ... | 04/07/2009 |
| 7405209 | Protease inhibitors The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such co... | 07/29/2008 |
| 7351703 | Sulfonylamino carboxylic acid N-arylamides as guanylate cyclase activators The present invention relates to compounds of the formula I in which A1, A2, R2 and R3 have the meanings indicated in the claims, which are valuable pharmaceutical active compound... | 04/01/2008 |
| 7351702 | Caspase inhibitors and uses thereof This invention provides compounds of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; next to R3 represents a... | 04/01/2008 |
| 7285547 | Amidinophenylalanine derivatives as thrombin inhibitors The compounds of the formula (formula 1) and pharmaceutically acceptable salts thereof and a process for preparing the same and pharmaceutical compositions containing the same are described wherein the substituents have the meaning as specified in the description. T... | 10/23/2007 |
| 7217838 | Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme The present invention relates to compounds that are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-in... | 05/15/2007 |
| 7160874 | Phenylalanine derivatives Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin. ... | 01/09/2007 |
| 7071184 | Protease inhibitors The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel int... | 07/04/2006 |
| 7018979 | Method for using potassium channel agonists for delivering a medicant to an abnormal brain region and/or a malignant tumor Disclosed are methods of selectively delivering a medicant to an abnormal brain region and/or to a malignant tumor in a mammalian subject, including a human. A medicant is administered simultaneously or substantially simultaneously with a potassium channel agonist (... | 03/28/2006 |
| 6992081 | Compounds to treat Alzheimer's disease The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) useful in treating Alzheimer's disease and other similar diseases. ... | 01/31/2006 |
| 6953789 | Thiol compounds, their production and use The present invention provides a compound represented by Formula: wherein ring A and ring B may be same or different and each is an optionally substituted homocyclic or heterocyclic ring and the like, each R1 | 10/11/2005 |
| 6951860 | Calcium channel blockers The invention involves the identification of a family of compounds which block calcium channels. The compounds can be formulated in pharmaceutical carriers and administered to subjects. The compounds are useful for treating disorders associated with calcium channel ... | 10/04/2005 |
| 6906059 | Pharmaceutical composition with protective action against oxidative/toxic substances, especially cardiotoxic substances The use of benzazepin-N-acetic acid derivatives which contain an oxo group in the a position to the nitrogen atom and are substituted in the 3 position by a 1-(carboxyalkyl)-cyclopentyl-carbonyl-amino radical, and of their salts and biolabile esters, for the prophyl... | 06/14/2005 |
| 6887864 | Azepane derivatives This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their ... | 05/03/2005 |
| 6887866 | Short-acting sedative hypnotic agents for anesthesia and sedation The invention provides compounds compositions and methods useful for inducing or maintaining general anesthesia or sedation in mammals. ... | 05/03/2005 |
| 6855706 | Phenylalanine derivatives Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α 4 integrin. They are used as therapeutic agents for various diseases concerning α 4 integrin. ... | 02/15/2005 |
| 6710179 | Compounds with analgesic effect Compounds of general formula (I) wherein m is 0 or 1, and n is 1 or 2; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprisi... | 03/23/2004 |
| 6579889 | Substituted isonipecotyl derivatives as inhibitors of cell adhesion Compounds of Formula I are antagonists of VLA-4 and/or 댔ଲ.sub.7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical ... | 06/17/2003 |
| 6534536 | Alkylsulfonamido heterocyclic thrombin inhibitors Alkylsulfonamido heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein G is ##STR2## wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; R is hydrogen, hydroxyalkyl, aminoalkyl, alkyl, cycloalkyl, amidoalkyl, ... | 03/18/2003 |
| 6506802 | Disulfide derivatives useful for treating allergic diseases Novel disulfide derivatives useful for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of systemic mastocytosis are disclosed. The disulfide derivative... | 01/14/2003 |
| 6495544 | Homoiminopiperidinyl hexanoic acid inhibitors of inducible nitric oxide synthase Homoiminopiperidinyl Hexanoic Acid derivatives and pharmaceutically acceptable salts thereof useful in the inhibition of the inducible isoform of nitric oxide synthase are disclosed.... | 12/17/2002 |
| 6486151 | N-oxides of heterocyclic esters, amides, thioesters, and ketones This invention relates to neurotrophic low molecular weight, small molecule N-oxides of heterocyclic esters amides, thioesters, and ketones having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with ... | 11/26/2002 |
| 6462073 | N-hydroxy-2-(alkyl, aryl, or heteroaryl sulfanyl, sulfinyl or sulfonyl)-3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenase... | 10/08/2002 |
| 6455520 | Benzamide derivatives and their use as cytokine inhibitors The invention concerns amide derivatives of formula (I) ##STR1## wherein R3 is (1-6C)alkyl or halogeno; m is 0-3, p is 0-2 and q is 0-4; each of R1 and R2 is a group such as hydroxy, halogeno, trifluoromethyl and cyano; R | 09/24/2002 |
| 6451824 | Sulfonylaminocarboxylic acids Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.... | 09/17/2002 |
| 6451817 | Alpha-substituted-1-benzyl-napthyls This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 1-benzyl-naphthyls which are -substituted with ether, thioether, amino, hydrazino, cyano or halo that are useful for the treatment of the various medica... | 09/17/2002 |
| 6403584 | Substituted nipecotyl derivatives as inhibitors of cell adhesion Compounds of Formula I are antagonists of VLA-4 and/or 댔ଲ.sub.7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical ... | 06/11/2002 |
| 6376468 | Protein:prenyl transferase inhibitors The invention pertains to novel peptide analogs suitable for inhibiting protein:prenyl transferases. As such they are therapeutically useful in e.g. inhibiting oncogenesis and other unwanted cell proliferation, and in supressing aberrant high signal trans... | 04/23/2002 |
| 6362174 | Reduced dipeptide analogues as calcium channel antagonitsts The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma. The nov... | 03/26/2002 |
| 6346547 | N-substituted amino acids, antioxidant pharmaceutical compositions containing n-substituted amino acids and methods for preventing cardiovascular diseases and/or preventing and/or treating antioxidant responsive diseases therewith Low-toxicity, highly-bioavailable, pharmaceutical antioxidant compositions for preferred oral administration to mammals are provided which have at least one amino acid-based compound of the general formula (I): A--N(Z)--CH(R1)C(O)--Q (I) wherein A ... | 02/12/2002 |
| 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 |
| 6335329 | Carboxylic acid substituted heterocycles, derivatives thereof and methods of use Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharm... | 01/01/2002 |
| 6316440 | Reduced dipeptide analogues as calcium channel antagonists ##STR1## The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma... | 11/13/2001 |
| 6291450 | Carboxylic acid substituted heterocycles, derivatives thereof and methods of use Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharm... | 09/18/2001 |
| 6251919 | Heterocyclic substituted aniline calcium channel blockers The present invention provides compounds that block calcium channels having the Formula I shown below. ##STR1## The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, epilepsy, ... | 06/26/2001 |
| 6251949 | Oxime derivatives, hydrazone derivatives and use thereof Compounds having fungicidal activities and represented by general formula (I) and salts and hydrates thereof ##STR1## wherein R1 represents an optionally substituted aryl, an optionally substituted alkyl or the like; R2 represents an... | 06/26/2001 |
| 6251892 | N-oxides of heterocyclic esters, amides, thioesters, and ketones This invention relates to neurotrophic low molecular weight, small molecule N-oxides of heterocyclic esters, amides, thioesters, and ketones having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with... | 06/26/2001 |
| 6191125 | Small molecule pipecolic acid derivative hair growth compositions and uses This invention relates to pharmaceutical compositions and methods for treating alopecia and promoting hair growth using pipecolic acid derivatives.... | 02/20/2001 |
| 6191144 | Method of using angiotensin converting enzyme inhibitor to stimulate angiogenesis The present invention is directed to the use of a group of ACE inhibitors to stimulate angiogenesis in mammals or in mammalian tissue in vitro. Specifically, the present invention is directed to inducing or enhancing angiogenesis through the administratio... | 02/20/2001 |
