Did You Know...
...that several people are credited with the invention of the flush toilet? Most people have heard of Thomas Crapper (1837-1910), the sanitary engineer who invented the valve-and-siphon arrangement that made the modern toilet possible. Another claimant to "the throne" was British inventor Alexander Cumming who patented a toilet in 1775. Then there's a nameless Minoan (a native of ancient Crete) who lived 4,000 years ago who supposedly was ahead of his time and created the first flush toilet!
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| Number | Title | Issue Date |
| 8173807 | Pyridine, pyrimidine and pyrazine derivatives as GPCR agonists Compounds of formula (I): R1-A-V—B—R2, wherein V is phenyl or a 6-membered heteroaryl ring containing up to three N-atoms, or pharmaceutically acceptable salts thereof, are agonists of GPR116 and are useful for the treatment of obesity, and... | 05/08/2012 |
| 8124763 | Process for the synthesis of 5-(methyl-1-imidazol-1-yl)-3-(trifluoromethyl)-benzeneamine The present invention provides a new method of making compounds of formula (I): wherein R1 is mono- or polysubstituted aryl; R2 is hydrogen, lower alkyl or aryl; and ... | 02/28/2012 |
| 7982037 | Pyrazole compounds useful as protein kinase inhibitors This invention describes novel pyrazole compounds of formula IIIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyc... | 07/19/2011 |
| 7872129 | Compositions useful as inhibitors of GSK-3 The present invention provides a compound of formula I: or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK3 mammalian protein kinase. The i... | 01/18/2011 |
| 7803940 | Heteromonocyclic compound or a salt thereof having strong antihypertensive action, insulin sensitizing activity and the like production thereof and use thereof for prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases A compound represented by the formula (I): wherein R1 is an oxo group, ═N—R or the like; a group represented by the formula: ... | 09/28/2010 |
| 7442795 | Triazole compounds useful in therapy A compound of formula (I), or a pharmaceutically acceptable derivative, wherein A, B, V, W, X, Y, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof. ... | 10/28/2008 |
| 7439240 | Purine-or pyrrolol[2,3-d]pyrimidine-2-carbonitiles for treating diseases associated with cysteine protease activity The present invention therefore provides a compound of formula (I) and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases ... | 10/21/2008 |
| 7429593 | Utilities of amide compounds Compounds having an activity to enhance the expression of apoAI are provided, which are used as medicaments. Compounds of formula (I): in which ring A and Ar1 are independently a monocyclic or bicyclic aro... | 09/30/2008 |
| 7419984 | Pyrimidines and uses thereof The invention relates to pyrimidines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase β (LPAAT-β) activity and/or proliferation of cells such as tumor-cells. ... | 09/02/2008 |
| 7414060 | Pyridine-2-carboxyamide derivatives The invention relates to compounds of formula I: wherein R1 to R3 are as defined in the specification, to processes for their preparation, to pharmaceutical compositions containing them, and to methods... | 08/19/2008 |
| 7414059 | Pyrazolyl and imidazolyl pyrimidines as CRF antagonists Compounds of the formula (I): and pharmaceutically acceptable salts or prodrugs thereof, wherein X, Y, Z and R1 are as defined herein. The invention also provides methods for preparing, compositions comprising, a... | 08/19/2008 |
| 7410973 | 4-amino-substituted pyrimidine derivatives The present invention relates to novel 4-amino-substituted pyrimidine derivatives which stimulate soluble guanylate cyclase, to processes for the preparation thereof, and to the use thereof for producing medicaments, in particular medicaments for the treatment of ce... | 08/12/2008 |
| 7390815 | Pyrazole compounds useful as protein kinase inhibitors This invention describes novel pyrazole compounds of formula II: wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, and R2, R2′, R... | 06/24/2008 |
| 7335654 | Phosphodiesterase 4 inhibitors PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein. ... | 02/26/2008 |
| 7320975 | 2-(2-pyridyl)-5-phenyl-6-aminopyrimidine, method and intermediate products for the production and use thereof for combating noxious fungi The invention relates to 2-(2-pyridyl)-5-phenyl-6-aminopyrimidines of formula I, wherein the substitutes and the index have the following meaning: R1 represents halogen, hydroxy, hyano, hxo, nitro, amino, mercapto, alkyl, halogenalkyl, alkenyl, alkinyl, c... | 01/22/2008 |
| 7317016 | Methods of treating medical conditions using sulfonate-substituted pyrazolopyridine derivatives This invention relates to methods of treatment of cardiovascular disorders, thromboembolic disorders, inflammation, and disorders of the central nervous system using pyrazol pyridine derivatives of formula (I) wh... | 01/08/2008 |
| 7309704 | Heteroaryl urea neuropeptide Y Y5 receptor antagonists The present invention relates to compounds represented by the structural Formula I: or a pharmaceutically acceptable salt thereof, which are useful for the treatment of metabolic and eating disorders such as obes... | 12/18/2007 |
| 7294627 | Chemical compounds Compounds of formula (I) in which R1, R2, R3 and R4, have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorde... | 11/13/2007 |
| 7291622 | Medical uses of carbamate-substituted pyrazolo-pyridine derivatives This invention relates to methods for treating sexual dysfunction, by administering a compound of the formula wherein R1 is H or a di-C1-6-alkylaminocarbonyl radical, and R2 is a ... | 11/06/2007 |
| 7253174 | N-heterocyclic inhibitors of TNF-α expression N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of production, pharm... | 08/07/2007 |
| 7226927 | Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators of caspases and inducers of apoptosis and the use thereof The present invention is directed to substituted 2-aryl-4-arylaminopyrimidine and analogs thereof, represented by the general Formula I: wherein A, Ar1, Ar2, R1 and R3 ... | 06/05/2007 |
| 7205306 | Substituted pyrazinones, pyridines and pyrimidines as corticotropin releasing factor ligands Compounds provided herein are novel substituted pyrazinones, pyridines and pyrimidines of Formula (I) and (II): Such compounds are particularly useful as CRF receptor ligands, and hence, in the treatment of vario... | 04/17/2007 |
| 7189729 | Methods and compositions as protein kinase inhibitors The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or d... | 03/13/2007 |
| 7173037 | Carbamate-substituted pyrazolopyridines The present invention relates to compounds which stimulate soluble guanylate cyclase, to the preparation thereof and to the use thereof as medicaments, in particular as medicaments for the treatment of cardiovascular disorders and/or sexual dysfunction. ... | 02/06/2007 |
| 7157580 | Aminopyrimidine and aminopyridine anti-inflammation agents Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided herein ... | 01/02/2007 |
| 7153860 | 5-Phenylpyrimidines, methods and intermediate products for the production thereof and use of the same for controlling pathogenic fungi The invention relates to 5-phenylpyrimidine of formula (I) wherein the substituents have the following designations: R1 represents a five to ten-membered saturated, partially unsaturated or aromatic monocyclic or bicyclic heterocycle which contains betwee... | 12/26/2006 |
| 7135474 | Derivatives of 2-(1-benzyl-1H-pyrazolo(3,4-B)pyridine-3-yl)-5(-4-pyridinyl)l-4-pyrimidinamines and the use thereof as quanylate cyclase stimulators This application relates to compounds of the formula (I) in which R1 is chlorine, cyano, trifluoromethyl or methoxy and R2 is hydrogen or flurorine; or R1 | 11/14/2006 |
| 7115597 | Tyrosine kinase inhibitors The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogen... | 10/03/2006 |
| 7115599 | Sulfonamide-substituted pyrazolopyridine compounds This invention relates to compounds of the formula in which R1, R2, and R3 are as defined in the claims, to a process for preparing such compounds, to pharmaceutical compositions ... | 10/03/2006 |
| 7112589 | Cysteine protease inhibitors with 2-cyano-4-amino-pyrimidine structure and cathepsin k inhibitory activity for the treatment of inflammations and other diseases The invention provides compounds of formula I or a pharmaceutically acceptable salt or ester thereof (I), wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions ... | 09/26/2006 |
| 7105523 | Carbamate-substituted pyrazolopyridine-derivatives This invention relates to compounds of the formula wherein R1 is H or a di-C1-6-alkylaminocarbonyl raical, and R2 is a radical of the formula —O—C(X)—NR3R4 w... | 09/12/2006 |
| 7091343 | Compositions useful as inhibitors of protein kinases The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, ... | 08/15/2006 |
| 7091198 | 2,5-disubstituted pyrimidine derivatives The present invention relates to novel 2,5-disubstituted pyrimidine derivatives which stimulate soluble guanylate cyclase, to processes for the preparation thereof, and to the use thereof for producing medicaments, in particular medicaments for the treatment of cent... | 08/15/2006 |
| 7087616 | Pyrazolyl pyrimidines This invention relates to novel pyrazolylpyrimidines of the formula in which R1, R2, X, n, Y, Z and R have the meanings given in the disclosure, to a plurality of processes for preparing the... | 08/08/2006 |
| 7067522 | 2,4,DI (hetero-) arylamino (-oxy)-5-substituted pyrimidines as antineoplastic agents Pyrimidine derivatives of formula (I) wherein Q1, Q2, G and R1 are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compos... | 06/27/2006 |
| 7053089 | N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain. ... | 05/30/2006 |
| 7034019 | Prodrugs of HIV replication inhibiting pyrimidines The present invention concerns compounds of formula (A1)(A2)N—R1 (I),the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is sub... | 04/25/2006 |
| 7034031 | Modulators of TNF-α signaling The present invention provides compounds which are modulators of TNF-α signaling and methods of use thereof for treating a patient having a TNF-α mediated condition. The compounds can be represented by the following structural formulas: | 04/25/2006 |
| 7015228 | 4-amino-2-(2-pyridyl)pyrimidines as microbicidal active substances Compounds of formula wherein R1 and R2 are each independently of the other hydrogen; unsubstituted or mono- or poly-halo-substituted C1–C20alkyl, C1... | 03/21/2006 |
| 7005433 | Heteroaryl, heterocyclic and aryl compounds which inhibit leukocyte adhesion mediated by VLA-4 Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, su... | 02/28/2006 |
