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| Number | Title | Issue Date |
| 7741479 | Urea inhibitors of MAP kinases The present invention is directed to a compound having the formula wherein R1, R2, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases such a... | 06/22/2010 |
| 7612200 | Inhibitors of protein kinases The present invention is directed to a compound having the formula wherein R1, R2, R3, R4, G, and Q are defined herein. The compounds of the present invention are useful as inhibi... | 11/03/2009 |
| 7598376 | Process for the preparation of [1,4,5]-oxadiazepine derivatives A process for the preparation of [1,4,5]-oxadiazepine derivatives by reaction of N,N′-diacyl-hydrazines with 2,2′-disubstituted diethyl ethers to form 4,5-diacyl-[1,4,5]-oxadiazepines and reaction of the latter compounds with a hydrohalic acid. ... | 10/06/2009 |
| 7589194 | Crystalline k-252b, sodium salt, methanolate pentahydrate A crystalline (9S-(9α,10β,12α))-2,3,9,10,11,12-hexahydro-10-hydroxy-10-(carboxylate)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3′,2′,1′-k1]pyrrolo[3,4-i][1,6]benzodiazocin-1-one methanolate pentahydrate and ways to make it are disclosed. ... | 09/15/2009 |
| 7585972 | Crystalline K-252α bis(tetrahydrofuranate) A crystalline (9S-(9α,10β,12α))-2,3,9,10,11,12-hexahydro-10-hydroxy-10-(methoxycarbonyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3′,2′,1′-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one bis(tetrahydrofuranate) and ways to make it are disclosed. ... | 09/08/2009 |
| 7407949 | Benzamide derivatives as oxytocin agonists and vasopressin antagonists Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds ... | 08/05/2008 |
| 7358239 | Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is... | 04/15/2008 |
| 7288650 | Cyclic substituted fused pyrrolocarbazoles and isoindolones The present invention is directed to cyclic substituted fused pyrrolocarbazoles and isoindolones. The invention also is directed to methods for making and using the cyclic substituted fused pyrrolocarbazoles and isoindolones. ... | 10/30/2007 |
| 7244843 | Modulators of serotonin receptors The present invention provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metab... | 07/17/2007 |
| 7238684 | Benzothiadiazepine derivatives, processes for their preparation and pharmaceutical compositions containing them The present invention relates to compounds of formula (I): wherein Rv, R1, R2, Rx, Ry, R3, R4, R5, R6, Rz and v are as defined within; pharmaceutically acce... | 07/03/2007 |
| 7192953 | Antibacterial agents Compounds of formula (I) have antibacterial activity; wherein Q represents a radical of formula —N(OH)CH(═O) or formula —C(═O)NH(OH); Y represents —C(═O)—, —C(═S)—, —S(═O)—, or —SO2—; R1 represents hydrogen, C... | 03/20/2007 |
| 7132416 | Benzothiazepine and benzothiazepine derivatives with ileal bile acid transport (IBAT) inhibotory activity for the treatment hyperlipidaemia The present invention relates to compounds of formula (I) wherein Rv, R1, R2, Rx, Ry, M, Rz, v, R3, R4, R5 and R6 are as defined within; pharmaceutically ac... | 11/07/2006 |
| 7074793 | Cyclic substituted fused pyrrolocarbazoles and isoindolones The present invention is directed to cyclic substituted fused pyrrolocarbazoles and isoindolones. The invention also is directed to methods for making and using the cyclic substituted fused pyrrolocarbazoles and isoindolones. ... | 07/11/2006 |
| 7060818 | Synthesis of macrocyclic tetraamido compounds and new metal insertion process An improved method of synthesizing a macrocyclic tetraamido compound includes protecting the amino portion of an amino carboxylic acid to form a protected amino carboxylic acid; exposing the protected amino carboxylic acid to a first solvent, preferably a hydrocarbo... | 06/13/2006 |
| 7038043 | Glycosylated indolocarbazole synthesis Indolocarbazoles are furanosylated (e.g., 7) with acetals (e.g., 8) or their open chain congeners (e.g., 9) under conditions known to promote acetal exchange or formation, such as protic or Lewis acids. Furanosylated indolocarbazoles (e.g., 1... | 05/02/2006 |
| 6921759 | Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention... | 07/26/2005 |
| 6875865 | Selected derivatives of K-252a Disclosed herein are selected indolocarbazole derivatives which are represented by the general formula: The compounds are useful for enhancing the function and/or survival of a trophic factor responsive cell. They inhibi... | 04/05/2005 |
| 6852714 | (Benzodioxan, benzofuran or benzopyran) derivatives having fundic relaxation properties The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6 | 02/08/2005 |
| 6844347 | Substituted 4-amino-2aryl-pyrimidines, their production and use and pharmaceutical preparations containing same The invention relates to compounds of formula I, in which R1, R2, R3 and R4 have the meanings given in the claims. Said compounds are valuable active ingredients for the trea... | 01/18/2005 |
| 6806266 | Staurosporin derivatives The present invention provides an antitumor agent comprising a staurosporin derivative or a pharmaceutically acceptable salt thereof, as an active ingredient, which is represented by the general formula (I): wherein R | 10/19/2004 |
| 6723844 | Preparation of K-252a The present invention provides a process for the synthesis of K-252a and intermediates useful in the process. ... | 04/20/2004 |
| 6677450 | Topoisomerase inhibitors The present invention relates to novel N12, N13-bridged sugar derivatives of indolylopyrrolocarbazoles and pharmaceutical formulations thereof which exhibit topoisomerase-I activity and are useful in inhibiting the proliferation of tumor cells.... | 01/13/2004 |
| 6660729 | Particle-forming compositions containing fused pyrrolocarbazoles A non-aqueous, particle-forming, fused pyrrolocarbazole-containing composition is disclosed. Upon contact with an aqueous medium, the particle-forming composition spontaneously disperses into suspended particles, thereby forming a stable suspension that p... | 12/09/2003 |
| 6635637 | Cyclic oxyguanidine protease inhibitors Cyclic oxyguanidine compounds, including compounds of Formulae I and II: ##STR1## wherein R1, R3 -R6, R21 -R26, L, Y, Z, and A are set forth in the specification, as well as hydrates, solvates or phar... | 10/21/2003 |
| 6624157 | Thiadioxobenzodiazepine inhibitors of farnesyl protein transferase Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formulas ##STR1## and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and solvate... | 09/23/2003 |
| 6552187 | Process for the preparation of herbicidal derivatives ##STR1## A process for the preparation of compounds of formula (I), which process comprises reacting a compound of formula (II), in an inert organic solvent, optionally in the presence of a base, with a compound of formula (IV), (IVa) or (IVb), and option... | 04/22/2003 |
| 6509334 | Cyclocarbamate derivatives as progesterone receptor modulators This invention provides compounds of Formula (I): ##STR1## wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 ... | 01/21/2003 |
| 6503898 | Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A repr... | 01/07/2003 |
| 6500818 | Naphthalenecarboxamides as tachykinin receptor antagonists Compounds having the following formula ##STR1## wherein L, M, R2, R3, R4, R5, R6, R7, X1 and X2 are as defined in the specification, pharmaceutically-acceptable salt t... | 12/31/2002 |
| 6476016 | Cyclic oxyguanidine pyrazinones as protease inhibitors Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: ##STR1## wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically ... | 11/05/2002 |
| 6472385 | Compositions and methods to enhance cancer chemotherapy in p53 defective tumors Compositions which abrogate DNA damage induced cell cycle arrest thereby enhancing the cell killing activity of DNA damaging anticancer agents for use in the treatment of cancer, and in particular, p53 defective cancers are provided.... | 10/29/2002 |
| 6451787 | Remedies for ocular diseases Use of the compound represented by general formula (I) for remedies of and protection against eye diseases is disclosed. General formula (I): ##STR1## (wherein, R1 and R2 independently represent a lower alkyl group, R3 and... | 09/17/2002 |
| 6410480 | Herbicidally active 3-hydroxy-4-aryl-5-oxopyrazoline derivatives The present invention relates to novel herbicidally active 3-hydroxy-4-aryl-5-oxopyrazoline derivatives, to processes for their preparation, to compositions which comprise these compounds and may additionally comprise safeners, and to the use of these com... | 06/25/2002 |
| 6359129 | Amino acid-derived, 7-membered cyclic sulfamides and methods of synthesizing the same New sulfamide compounds and methods of forming those compounds are provided. The inventive methods comprise subjecting a template opened-ring sulfamide compound to a ring-closing metathesis reaction in the presence of a Grubbs catalyst to yield a heterocy... | 03/19/2002 |
| 6225306 | Biphenyl derivatives and drug composition A biphenyl derivative represented by the following general formula (1) and a pharmaceutically acceptable salt thereof: ##STR1## [In the formula (1), A represents a single bond, --CH2 --, --CO--, --CS-- or --SO2 --; B represents a sin... | 05/01/2001 |
| 6200968 | Particle-forming compositions containing fused pyrrolocarbazoles A non-aqueous, particle-forming, fused pyrrolocarbazole-containing composition is disclosed. Upon contact with an aqueous medium, the particle-forming composition spontaneously disperses into suspended particles, thereby forming a stable suspension that p... | 03/13/2001 |
| 6197955 | Production of staurosporine derivative using acid isomerization A staurosporine derivative with anti-cancer activity and anti-bacterial activity is produced by acidifying a solution containing staurosporine to isomerize staurosporine to its desired derivative, whereby the derivative is recovered from the acidified sol... | 03/06/2001 |
| 6156746 | 1,2,5-benzothiadiazepine-1,1-dioxides with n-2 imidazolylalkyl substituents Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formula ##STR1## and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and sol... | 12/05/2000 |
| 6127401 | Bridged indenopyrrolocarbazoles The present invention is directed to novel fused aryl and heteroaryl bridged indenopyrrolocarbazoles which are useful, inter alia, as therapeutic agents. The invention is also directed to methods for making and using the bridged indenopyrrolocarbazoles.... | 10/03/2000 |
| 6127359 | Bicyclic fibrinogen antagonists Compounds of the formula: ##STR1## wherein A1 to A5 form a seven-membered ring containing one optionally substituted nitrogen atom and one heteroatom selected from oxygen and nitrogen; D1 to D4 form a subst... | 10/03/2000 |
