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| Number | Title | Issue Date |
| 8188091 | Tetrahydroquinazoline compounds and their use in preparing medicaments for treating and preventing virosis The present invention relates to a compound of formula (I) or isomers thereof, or pharmaceutically acceptable salts or hydrates thereof. The present invention further relates to processes for the preparation of the compounds of formula (I) and optical isomers, and t... | 05/29/2012 |
| 8183245 | Pyrazine substituted pyrrolopyridines as inhibitors of JAK and PDK1 The present invention relates to pyrazine substituted pyrrolopyridines having formula (I) useful as inhibitors of JAK kinases (JAK1, JAK2, JAK3 and/or TYK2) and/or PDK1 and for the treatment of myeloproliferative disorders ... | 05/22/2012 |
| 8178539 | Substituted 3,4,6,7-tetrahydro-5-1,2a,4a,8-tetraazacyclopenta[]phenalenes and methods Substituted 3,4,6,7-tetrahydro-5H-1,2a,4a,8-tetraazacyclopenta[cd]phenalene-9-amines, pharmaceutical compositions containing the compounds or salts thereof, intermediates, methods of making the compounds or salts thereof, and methods of use of these compounds or sal... | 05/15/2012 |
| 8168641 | Aspartyl protease inhibitors Disclosed are compounds of formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 | 05/01/2012 |
| 8153638 | Metabotropic glutamate-receptor-potentiating isoindolones Compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the description, processes for th... | 04/10/2012 |
| 8148380 | Antibacterial amide and sulfonamide substituted heterocyclic urea compounds The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided. ... | 04/03/2012 |
| 8138193 | Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases Novel fused pyrazine compounds are disclosed that have a formula represented by the following: with Z, R1, R2, R8 and R9 as defined in the written description. The compounds may b... | 03/20/2012 |
| 8133895 | Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases Novel fused pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of c... | 03/13/2012 |
| 8129394 | Heteroaryl-substituted imidazole compounds and uses thereof Novel imidazole compounds of the general formula are disclosed, wherein R1 and R2 comprise heteroaryl groups. These compounds and compositions containing them are useful in met... | 03/06/2012 |
| 8119643 | Benzoimidazolyl-pyrazine compounds for inflammation and immune-related uses Biologically active chemical compounds, namely benzoimidazolyl-pyrazine derivatives and structurally related compounds, are disclosed herein. Such compounds include those represented by structural formula (II): and as descr... | 02/21/2012 |
| 8119644 | Thiadiazole-substituted arylamides as P2X3 and P2X2/3 antagonists Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted thiadiazolyl, and R2, R3, R4, R5, R6, R... | 02/21/2012 |
| 8106059 | Substituted pyrazines that inhibit protease cathepsin S and HCV replication The present invention is directed to compounds of formula I, below, that have the dual property of acting as cathepsin S inhibitors and of inhibiting HCV replication. Such compounds are therefore useful in treating disease states that include hepatitis C, Alzheimer'... | 01/31/2012 |
| 8101620 | Heterocyclic sulfonamides Provided is a compound of the following formula: wherein: R3 is an aryl or heteroaryl group, which is optionally substituted with a halogen, lower alkoxy, aryl or heteroaryl gro... | 01/24/2012 |
| 8080551 | HIV inhibiting pyrimidines derivatives HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhi... | 12/20/2011 |
| 8071605 | Piperidine compounds for use in the treatment of bacterial infections Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described. ... | 12/06/2011 |
| 8058278 | Methods of enhancing mucosal hydration and mucosal clearance by treatment with sodium channel blockers and osmolytes The present invention relates to methods and compositions for treating diseases ameliorated by increased mucociliary clearance and mucosal hydration by administering an effective amount of a sodium channel blocker as defined herein and an osmolyte to a subject to a ... | 11/15/2011 |
| 8053438 | Pyrazine compounds as phosphodiesterase 10 inhibitors Pyrazine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bip... | 11/08/2011 |
| 8039475 | Co-crystals and pharmaceutical compositions comprising the same The invention relates to compositions and co-crystals each comprising (1S,3aR,6aS)-2-[(2S)-2-[[(2S)-2-Cyclohexyl-2-(pyrazine-2-carbonylamino)acetyl]amino]-3,3-dimethylbutanoyl]-N-[(3S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl]-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c... | 10/18/2011 |
| 8030316 | Malate salt of (2R)-methyl-1-{3-[2-(3-pyridinyloxy)ethoxy]-2-pyrazinyl}piperazine The present invention relates to a process for the preparation of compounds which are therapeutically active in the central nervous system. In one aspect, the invention relates to a process for the preparation of compounds of the general formula (I): | 10/04/2011 |
| 8012983 | Substituted triazolopyrazines useful for the treatment of degenerative and inflammatory diseases Novel [1.2.4]triazolo[1,5-a]pyrazine and imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the... | 09/06/2011 |
| 8008306 | Quinoline compounds To provide a novel LXRβ agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused ... | 08/30/2011 |
| 7994177 | Therapeutic agents useful for treating pain The present invention discloses a compound of formula: where Ar1, Ar2, X, Z1, Z2, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “... | 08/09/2011 |
| 7977340 | Antibacterial compositions Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioethe... | 07/12/2011 |
| 7973043 | Combination therapy for depression, prevention of suicide, and various medical and psychiatric conditions The present invention relates to a new method of treatment for persons meeting diagnoses for major depressive disorder, or other unipolar (non-bipolar, non-psychotic and non-treatment resistant) depression. The method comprises administering a combination of two cat... | 07/05/2011 |
| 7964606 | Therapeutic agents useful for treating pain The present invention discloses compounds of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Phenylene Compound”); composi... | 06/21/2011 |
| RE42375 | Quinoxalinyl macrocyclic hepatitis C serine protease inhibitors The present invention relates to compounds of Formula I or II, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS... | 05/17/2011 |
| 7935706 | Nitrogen-containing heterocycle derivatives substituted with cyclic group It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: ... | 05/03/2011 |
| 7928109 | Sulfonyl amide derivatives for the treatment of abnormal cell growth The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell gr... | 04/19/2011 |
| 7915263 | Aminopyridine derivatives having aurora A selective inhibitory action The present invention relates to a compound of formula I: wherein: R1 is a hydrogen atom, F, CN, etc.; R1′ is a hydrogen atom or lower alkyl which may be substituted; R2 is O, S, SO, SO... | 03/29/2011 |
| 7910592 | CETP inhibitors Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of... | 03/22/2011 |
| 7902200 | Chemical compounds The invention relates to a novel group of compounds of Formula (I) or a salt thereof: wherein R1, A and HET-1 are as described in the specification, which may be useful in the treatment or prevention of a disease... | 03/08/2011 |
| 7902201 | Isoxazolo-pyrazine derivatives The invention relates to isoxazolo-pyrazine derivatives and their pharmaceutically acceptable salts having affinity and selectivity for the GABA A α5 receptor binding site, their manufacture, and pharmaceutical compositions containing them. The compounds of the pre... | 03/08/2011 |
| 7897606 | 5,6-di-substituted oxadiazolopyrazines and thiadiazolopyrazines as CXC-chemokine receptor ligands Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof. The compounds are useful for the treatment of chemokine-mediated diseases such as COPD. ... | 03/01/2011 |
| 7888364 | Pyridyl inhibitors of hedgehog signalling The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R... | 02/15/2011 |
| 7875618 | Substituted imidazo[1,5-a]quinoxalines useful as inhibitors of phosphodiesterase 10 for the treatment of neurological and other disorders The invention relates to imidazo[1,5-a]quinoxaline derivatives having Formula IIa: to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compou... | 01/25/2011 |
| 7812027 | Substitued [1,2,4]triazolo[1,5-a]pyrazines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzym... | 10/12/2010 |
| 7812026 | Imidazole derivatives having a positive allosteric GABAreceptor modulator effect and methods of use The present invention relates to novel imidazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for... | 10/12/2010 |
| 7795267 | Bicyclic piperazine compound having TGR23 antagonistic activity The present invention provides a compound represented by the formula: wherein R1 is —(C═O)—NR7R8 or —(C═O)—OR6, R2 is a hydrocarbon... | 09/14/2010 |
| 7790728 | Pyrazine derivatives useful as adenosine receptor antagonists The present disclosure relates to a compound of formula (I) wherein: A is an optionally substituted monocyclic or polycyclic aryl or heteroaryl group; B is an optionally substituted monocy... | 09/07/2010 |
| 7786130 | Pyridones useful as inhibitors of kinases The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, o... | 08/31/2010 |
