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| Number | Title | Issue Date |
| 8026375 | Transition metal catalyzed synthesis of N-aminoindoles The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; R6; A1; A2; A3; A4, Q, T and J have the meanings indicated in the claims. The presen... | 09/27/2011 |
| 7754894 | Crystalline sulfonamide-containing indole compound and process for preparing the same A crystalline form of N-(3-cyano-4-methyl-1H-indol-7-yl)-3-cyanobenzenesulfonamide having a diffraction peak at a diffraction angle (2θ±0.2°) of 19.1° in a powder X-ray diffraction. ... | 07/13/2010 |
| 7429610 | Analogs of indole-3-carbinol metabolites as chemotherapeutic and chemopreventive agents Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particula... | 09/30/2008 |
| 7405300 | Substituted indoles as inhibitors of poly (ADP-ribose) polymerase (PARP) The present invention relates to a series of substituted indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. Th... | 07/29/2008 |
| 7368605 | Variously substituted derivatives of guanidine, and their use as medicines with anti-diabetes and/or anti-obesity activity Formula (I) compounds are described where the groups are as identified in the text, and their use as medicines, particularly as anti-diabetes, serum glucose-lowering and anti-obesity agents. They are useful for the prophyla... | 05/06/2008 |
| 7342038 | Substituted diphenyl indanone, indane and indole compounds and analogues thereof useful for the treatment or prevention of diseases characterized by abnormal cell proliferation The present invention provides substituted 3,3-diphenyl indole compounds, as well as analogues thereof, which are specific potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a ther... | 03/11/2008 |
| 7338966 | Substituted oxindole derivatives as tyrosine kinase inhibitors The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alt... | 03/04/2008 |
| 7314887 | Thrombopoietin activity modulating compounds and methods Disclosed herein are compounds of Formula (I), (II), and (III) pharmaceutical compositions comprising the same, methods of modulating the activity a thrombopoietin receptor using the same, methods of identifying ... | 01/01/2008 |
| 7265130 | NPY Y5 antagonist The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, ... | 09/04/2007 |
| 7241799 | Cannabimimetic indole derivatives Cannabimimetic indole derivatives are presented which have preferentially high affinities for one of the cannabinoid CB1 or CB2 receptor sites. The improved receptor affinity makes these analogs therapeutically useful as medications in individuals and animals. ... | 07/10/2007 |
| 7176312 | Kinase inhibitor scaffolds and methods for their preparation General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, bor... | 02/13/2007 |
| 7166635 | 3-imino-2-indolones for the treatment of depression and/or anxiety This invention is directed to indolone derivatives which are selective antagonists for the GalR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically accepta... | 01/23/2007 |
| 7153881 | Compounds acting as melanocortin receptor ligands The present invention provides novel compounds and use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: Wherein X and Y are independently chosen from O, N, S and (CH2 | 12/26/2006 |
| 7141674 | Anti-inflammatory compounds This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: ... | 11/28/2006 |
| 7112682 | Process for the preparation of N-amino substituted heterocyclic compounds An improved process for the preparation of N-amino nitrogen heterocyclic compounds is disclosed and claimed. In an embodiment of this invention, a compound of the formula (VI) is prepared starting from the corresponding indole derivative by way of N-amination and su... | 09/26/2006 |
| 7081470 | Use of GALR3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods This invention is directed to indolone derivatives which are antagonists for the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrie... | 07/25/2006 |
| 7078427 | Analogs of indole-3-carbinol metabolites as chemotherapeutic and chemopreventive agents Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particula... | 07/18/2006 |
| 7078429 | Substituted 3-carbonyl-1H-indol-1-yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) Substituted 3-carbonyl-1H-indol-1-yl acetic acid derivatives of formula I are provided: wherein: R1, R2, R3, R4 and R5 are as defined herein which are useful a... | 07/18/2006 |
| 7071217 | Substituted oxindole derivatives as tyrosine kinase inhibitors The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alt... | 07/04/2006 |
| 7071206 | Agents for treating neurodegenerative disorders Compounds and methods of using these compounds to treat neurodegenerative diseases, especially Alzheimer's disease, are provided. The compounds that are provided for the treatment of neurodegenerative diseases can be represented by a general formula (I): | 07/04/2006 |
| 7030123 | Indole derivatives with vascular damaging activity The invention provides a compound of Formula (I). Wherein R1, R2, R3, R10 and R11 have the meanings given in the description. Such compounds are predicted to cause the selective destruction of tumour vasculature. They ... | 04/18/2006 |
| 6969729 | Use of isatin derivatives as ion channel activating agents The present invention relates to ion channel activating agents. More particularly, the present invention relates to a particular class of chemical compounds that has proven useful as openers of SKCa and IKCa channels. In further aspects, the present invention relate... | 11/29/2005 |
| 6958416 | Valproyltaurinamide derivatives as anticonvulsant amd CNS active agents The invention relates to derivatives of valproyltaurinamide of formula (I) in which R1 and R2 are independently hydrogen, a C1-C6-alkyl group, an arylalkyl group or an aryl group. The derivatives are especially useful for ... | 10/25/2005 |
| 6900236 | Cannabimimetic indole derivatives Novel cannabimimetic indole derivatives are presented which have preferential high affinities for one of the cannabinoid CB1 CB2 receptor sites. The improved receptor affinity makes these analogs therapeutically useful as medications in individuals and animals for t... | 05/31/2005 |
| 6825352 | Preparation and use of ortho-sulfonamido arylhydroxamic acids as matrix metalloproteinase inhibitors Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs. ... | 11/30/2004 |
| 6723848 | Method for producing benzo annelated heterocycles Process for the preparation of benzo-fused heterocycles of general formula I: in which X, R1, R2, R3, R4, R5 and n are as defined in claim 1, by reacting tetrahydrob... | 04/20/2004 |
| 6677353 | Substituted N-phenyl-N-heteroaralkyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating... | 01/13/2004 |
| 6586459 | Antithrombotic agents This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well a... | 07/01/2003 |
| 6583145 | Thio-oxindole derivatives This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: ##STR1## wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a... | 06/24/2003 |
| 6583173 | Antithrombotic agents This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well a... | 06/24/2003 |
| 6545152 | R-isomers of nonnucleoside inhibitors Novel chiral derivitaves of non-nucleoside inhibitors (NNI), particularly R-isomers of halopyridyl and thiazoyl thiourea compounds are provided as potent inhibitors of reverse transcriptase (RT), and particularly of retroviral RT, most particularly HIV RT... | 04/08/2003 |
| 6541503 | Substituted oxindole derivatives as protein tyrosine kinase and as protein serine/threonine kinase inhibitors Compounds of formula (I): wherein X is N, CH, CCF3, or C(C1-12 aliphatic); R4 is sulfonic acid, C1-12 aliphatic-sulfonyl, sulfonyl-C1-12 aliphatic, C1-12 aliphatic-sulfonyl-C1-6 ... | 04/01/2003 |
| 6534535 | Inhibitors of factor Xa Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds of formula (I) below: ##STR1## are useful in vitro or in vivo for preventing or treating coagulation disorders.... | 03/18/2003 |
| 6518291 | Inhibitors of IMPDH enzyme The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly... | 02/11/2003 |
| 6512125 | Preparation of 1H-indol-1-amines The synthesis of memory enhancing, analgetic, and antidepressant N-alkyl-N-pyridinyl-1H-indol-1-armines is described.... | 01/28/2003 |
| 6509369 | Anti-inflammatory compounds This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: ##STR1##... | 01/21/2003 |
| 6500854 | Chondrongenesis promotors and indolin-2-one derivatives A chondrogenesis promoter comprising as an active ingredient a compound represented by general formula (I) or a salt thereof: ##STR1## wherein R1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, etc.; R2 represen... | 12/31/2002 |
| 6500855 | Thrombin or factor Xa inhibitors This invention relates generally to inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention o... | 12/31/2002 |
| 6498176 | 3-(anilinomethylene) oxindoles as protein tyrosine kinase and protein serine/threonine kinase inhibitors ##STR1## Compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, D, X, Y and Z have the meaning as defined in the claims exhibit protein tyrosine kinase and protein serin/threonine kinase inhibitory activity.... | 12/24/2002 |
| 6458803 | Substituted N-phenyl-N-heteroaralkyl aminoalcohol compounds for inhibiting cholesteryl ester transfer protein activity The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating... | 10/01/2002 |
