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| Number | Title | Issue Date |
| 6258819 | Substituted 2(4-piperidyl)-4(3H)-quinazolinones and 2-(4-piperidyl)-4(3H)-azaquinazolinones This invention relates to compounds which are generally alpha1A/B -receptor antagonists and which are represented by Formula I: ##STR1## wherein the substituents are as defined in the specification; or pharmaceutically acceptable salts, hydrate... | 07/10/2001 |
| 6251912 | Substituted quinazoline derivatives This invention provides compounds of formula 1 having the structure ##STR1## wherein: X, R1, R2, R3, R4, Z, X, and n are as defined hereinbefore in the specification, which are useful as antineoplastic agents an... | 06/26/2001 |
| 6239129 | Cyano-indole serotonin-reuptake inhibitor compounds Compound of formula (I): ##STR1## wherein: R1 and R2 each independently of the other represents hydrogen or alkyl, A represents alkylene, alkenylene or alkynylene, G1 represents ##STR2## wherein R3 and R4 | 05/29/2001 |
| 6225318 | 4-aminoquinazolone derivatives This invention relates to certain 4-aminoquinazoline derivatives of the formula ##STR1## and their pharmaceutically acceptable salts wherein R1, Q1, m, n, and Z are defined as in the specification. The compounds of formula I and ... | 05/01/2001 |
| 6214832 | Bis-piperidinyl-pyrimidin-2-ones as alpha 1a adrenergic receptor antagonists Pyrimidinone, oxazolidinone, and (alkyl)aryl derivatives, their synthesis, and their use as alpha 1a adrenergic receptor antagonists are disclosed. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are... | 04/10/2001 |
| 6211196 | Benzyloxy-substituted, fused N-heterocycles, processes for their preparation, and their use as bradykinin receptor antagonists Benzyloxy-substituted, fused N-heterocycles, because of their ability to act as bradykinin receptor antagonists, have been found to be useful as therapeutics for the treatment and prevention of liver cirrhosis or Alzheimer's disease. This application desc... | 04/03/2001 |
| 6211189 | Amino-spiro-quinazoline compounds There are provided novel compounds of formula (I) ##STR1## wherein A represents an aromatic carbocyclic ring or a 5- or 6-membered heterocyclic aromatic ring containing 1 to 3 heteroatoms which may be the same or different and are selected from O, N and S... | 04/03/2001 |
| 6204267 | Methods of modulating serine/thereonine protein kinase function with quinazoline-based compounds The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with quinazoline-based compounds. The methods incorporate cells that express a serine/threonine protein kinase, such as RAF. In additi... | 03/20/2001 |
| 6187923 | Process for the synthesis of quinazolinones The present invention provides a process for synthesizing a compound or a library of compounds of Formula 1A and 1B: ##STR1##... | 02/13/2001 |
| 6187788 | Condensed-ring thiophene derivatives, their production and use A gonadotropin-releasing hormone antagonistic composition, which comprises an optionally substituted condensed-bicyclic compound consisting of a homo or hetero 5 to 7 membered ring and a homo or hetero 5 to 7 membered ring is effective as a propylactic or... | 02/13/2001 |
| 6184377 | Compositions containing N-amino- and N-hydroxy-quinazolinones and methods for preparing libraries thereof The present invention is directed to certain N-amino- and N-hydroxy-quinazolinone compounds and synthetic methods for synthesis thereof, which compounds may find use in combinatorial libraries. More specifically, the invention is directed to the synthesis... | 02/06/2001 |
| 6184226 | Quinazoline derivatives as inhibitors of P-38 The invention describes compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof and the pharmaceutically acceptable salts thereof wherein each R2 is independently a noninterfering substituent; m is an integer of 0-4; Z is CH o... | 02/06/2001 |
| 6180637 | 1,2,5-trisubstituted 1,2-dihydroindazol-3-ones having anti-asthmatic, anti-allergic, anti-inflammatory, immunomodulating and neuroprotective action, process for their preparation and their use as medicaments The invention relates to 1,2,5-trisubstituted 1,2-dihydroindazol-3-ones of formula (I) ##STR1## wherein X is --SO2 --, --SO--, --(CH2)p --, --(CH2)p --O--, --(CH2)p --(C.dbd.O)--... | 01/30/2001 |
| 6166205 | 2-Aryl-4-(1-[4-heteroaryl]piperazin-1-yl)methylimidazoles: dopamine . D.sub4 receptor subtype ligands Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof wherein: Ra represents ##STR2## where X, Y and Z are the same or different and represent CH or nitrogen; R1 R | 12/26/2000 |
| 6156772 | Antagonists of gonadotropin releasing hormone There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both m... | 12/05/2000 |
| 6153617 | Irreversible bicyclic inhibitors of tyrosine kinases The invention provides compounds of Formula I ##STR1## that are irreversible inhibitors of tyrosine kinases. Also provided is a method of treating cancer, restenosis, atherosclerosis, endometriosis, and psoriasis and a pharmaceutical composition that... | 11/28/2000 |
| 6150532 | Modulators of proteins with phosphotyrosine recognition units The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human an... | 11/21/2000 |
| 6150370 | 1,3-diheterocyclic metalloprotease inhibitors Disclosed are compounds which are inhibitors of metalloproteases having the following structure: ##STR1## where Ar, W, X, Y, Z, R1 and R2 have the meanings described in the specification and optical isomers, diastereomers, and e... | 11/21/2000 |
| 6150352 | Antagonists of gonadotropin releasing hormone There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related conditions in both men and wom... | 11/21/2000 |
| 6136971 | Preparation of sulfonamides The present invention provides a process for preparing 1,2-diheteroethylene sulfonamide of the formula: ##STR1## by reacting a pyrimidine monohalide of the formula: ##STR2## with a mono-protected 1,2-diheteroethylene anion of the formula M1... | 10/24/2000 |
| 6127375 | 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinthiones useful as HIV reverse transcriptase inhibitors The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinthiones of formula I: ##STR1## or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV ... | 10/03/2000 |
| 6127374 | Irreversible inhibitors of tyrosine kinases This invention provides irreversible inhibitors of tyrosine kinases having for formula ##STR1## which compounds are useful for treating cancer, restenosis, atherosclerosis, endometriosis and psoriasis.... | 10/03/2000 |
| 6124302 | 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones useful as HIV reverse transcriptase inhibitors The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones of formula I: ##STR1## or steroisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV ... | 09/26/2000 |
| 6114526 | Heterocyclic compounds, process for their preparation and pharmaceutical compositions containing them and their use in the treatment of diabetes and related diseases The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically accep... | 09/05/2000 |
| 6096761 | Esters of 3-hydroxy-piperidinemethanol derivatives The present invention of compounds of formula (I), ##STR1## a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 is C1-6 alkyloxy, C2-6 alke... | 08/01/2000 |
| 6093821 | Process for preparing steroid receptor modulator compounds Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions f... | 07/25/2000 |
| 6090944 | Alkanoic acid derivatives as v integrin receptor antagonists The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors v댣, �... | 07/18/2000 |
| 6080860 | Methods of making ureas and guanidines including, terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefor Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediate... | 06/27/2000 |
| 6077847 | Antagonists of gonadotropin releasing hormone There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both m... | 06/20/2000 |
| 6071921 | Chemical compounds The invention relates to quinazoline derivatives of the formula: ##STR1## [wherein: Y1 represents --O--, --S--, --CH2 --, --SO--, --SO2 --, --NR5 CO--, --CONR6 --, --SO2 NR7 --, ... | 06/06/2000 |
| 6066638 | Fungicidal pyrimidinones Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful as fungicides ##STR1## wherein W is O, S(O)n or NR5 ; n is 0, 1 or 2; Q is O or S; G is a fused phenyl, naphthalene, thiophe... | 05/23/2000 |
| 6060479 | Quinazoline-4-one AMPA antagonists The present invention relates to novel quinazolin-4-one derivatives of the formula I, as defined in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurodegenerative, psychotropic, and drug and a... | 05/09/2000 |
| 6057326 | Bicyclic 4-aralkylaminopyrimidine derivatives as tyrosine kinase inhibitors Novel and known bicyclic 4-aralkylaminopyrimidine derivatives of formula (I) wherein A is a benzene or imidazole ring; B is a benzene, tetralin, indane or 2-oxindole ring R is (C1 -C4)perfluoroalkyl, phenyl, phenyl-(C1 -C | 05/02/2000 |
| 6048864 | Quinolines and quinazolines useful in therapy Compounds of formula I, ##STR1## wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 and R3 independently represent H or C1-6 alkoxy (which is optionally su... | 04/11/2000 |
| 6030973 | Heterocyclic compounds having antidiabetic hypolipidemia and antihypertensive properties, process for their preparation and pharmaceutical compositions containing them The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their analogues, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharm... | 02/29/2000 |
| 6017919 | Compounds and pharmaceutical use thereof The compounds of the formula (I) ##STR1## wherein each symbol is as defined in the specification, pharmaceutically acceptable salts thereof and pharmaceutical use thereof. The Compound (I) and pharmaceutically acceptable salts thereof of the present ... | 01/25/2000 |
| 6011037 | Thiazole derivatives with phosphodiesterase-inhibiting action Compounds having the formula (I): ##STR1## wherein R1, R2, R3, R4, R5 and n have the meanings given in the description. The compounds of formula (I) are selective inhibitors of phosphodiesterase IV.... | 01/04/2000 |
| 6011045 | Vitronectin receptor antagonists, their preparation and their use The present invention relates to compounds of the formula I A--B--D--E--F--G (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds... | 01/04/2000 |
| 5998456 | Benzimidazole compounds containing 1,2,4-triazole ring, and compositions and methods of use containing the same Benzimidazole compounds represented by the formula set out below and analogs thereof, wherein Y represents a single bond or sulfur atom; Z represents oxygen atom, sulfur atom, or N--R4 ; R1 and R2 independently represent h... | 12/07/1999 |
| 5994544 | Steroid receptor modulator compounds and methods Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors and the method of preparing these compounds are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employin... | 11/30/1999 |
