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| Number | Title | Issue Date |
| 4620001 | Chemical methods and intermediates for preparing substituted pyrimidinones A series of chemical reactions starting from the condensation of uracil with an acid stable heterocyclic aldehyde in an acid medium produces biologically active end products which are 2-heterocyclylmethylthioethylamino-5-heterocyclylmethyl-4-pyrimidinones... | 10/28/1986 |
| 4588740 | Pharmaceutical methods using 4-aminoalkyl-2(3H)-indolones A series of pharmaceutical compositions which contain 4-aminoalkyl-2(3H)-indolones has been demonstrated to have D2 -agonist activity useful for treating congestive heart failure and hypertension. A representative ingredient of the compositions... | 05/13/1986 |
| 4584381 | 5-(Nitro or halogen)-3-(alkyl)-2-(aminoalkyl)pyridines Compounds of the formula: ##STR1## where R1 is halogen or nitro; R2 is C1-4 alkyl; and R3 is a C1-3 alkylene group are intermediates to 2-(3,5-disubstituted pyridyl-alkyl amino)-5-pyridylmethyl-4... | 04/22/1986 |
| 4584384 | Nitro pyrroles 3-Nitro-2-substituted aminopyrroles are histamine H2 -receptor antagonists. The 2-position substituent is a fully-unsaturated heterocyclyl alkyl group preferably with alkyl group interrupted by sulfur or oxygen. The 4- and 5-positions of the py... | 04/22/1986 |
| 4579972 | Intermediates for preparing secondary amines New intermediates and processes for preparing 6-halo-7,8-dihydroxy-1-(p-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepi nes involve the reaction of a p-methoxyphenylglyoxal, lower alkyl hemimercaptal with a 2-chloro-3,4-dimethoxyphenethylamine, followed b... | 04/01/1986 |
| 4578388 | Unsymmetrical guanidino, thioureido, isothioureido and nitromethyleneamino derivatives The compounds are C2 -C8 straight chain alkanes terminally substituted, symmetrically or unsymmetrically, by N-(N'-substituted guanidino), N-(N',N"-disubstituted guanidino). N-(N'-substituted thioureido), N-(nitromethylene amidino) o... | 03/25/1986 |
| 4578459 | Heterocyclic alkylaminoheterocycles Heterocyclic compounds which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A specific compound of this invention is 2-[2-(4-methyl-5-imidazolylmethylthio)ethylamino]-4-pyrimidone.... | 03/25/1986 |
| 4576937 | 7 -D-Mandelamido-3(1-sulfomethyltetrazol-5-yl)thiomethyl-3-cephem-4-carboxy lic acid monosodium salt A new cephalosporin compound, 7-D-mandelamido-3-(1-sulfomethyltetrazol-5-yl) thiomethyl-3-cephem-4-carbo xylic acid monosodium salt, having unique antibacterial activity and advantageously high stability, is disclosed. Pharmaceutical compositions comp... | 03/18/1986 |
| 4574126 | Pyridine derivatives histamine H2 -antagonists This invention relates to 2-pyridine derivatives substituted in the 4-position with a dialkylamino- or piperidinyl- or pyrrolidinylalkyl group. The compounds have histamine H2 -antagonist activity.... | 03/04/1986 |
| 4571398 | Cytosine derivatives having histamine H2 -antagonist activity This invention relates to cytosine derivatives which have histamine H2 -antagonist activity. A specific compound of this invention is 4-[3-(3-(piperidinomethyl)phenoxy)propylamino]-pyrimidin-2-thione.... | 02/18/1986 |
| 4569996 | Process for preparing substituted pyrimidinones This invention provides a process for the preparation of pyrimidinone compounds with a group R2 CH(OH)-- at the 5-position thereof, wherein R2 is an optionally substituted acid-stable 5- or 6-membered nitrogen-containing heteroaryl g... | 02/11/1986 |
| 4567176 | 4H-Imidazol-4-ones and their pharmaceutical use This invention relates to Mannich-furyl(thienyl, pyridyl or phenyl) alkylaminoimidazolinones which have histamine H2 -antagonist activity. A specific compound of this invention is 2-[2-(5-dimethylaminomethylfuran-2-ylmethylthio)-ethylamino]-1-m... | 01/28/1986 |
| 4564363 | Delayed action assembly A device for effecting the delayed release of an active ingredient comprises a container and, within, a dispersible unit of ingredient, a removable closure and a electrical control circuit for removal of said closure at a designated time to release the ac... | 01/14/1986 |
| 4558128 | 2-Substituted alkylaminopyrimidones The compounds are isoureas and isothioureas which have an O- or S- alkylpyrimidone substituent and which are histamine H2 -antagonists and antiinflammatory agents. A specific compound of this invention is 2-[5-(O-isoureido)pentylamino]-5-(6-met... | 12/10/1985 |
| 4554287 | Antihypertensive 7-[2-(dialkylamino)ethyl]-4-hydroxy-1,3-benzimidazol-2-ones 7-[2-Dialkylamino)ethyl]-4-hydroxy-1,3-benzimidazol-2-ones are prepared by oxidative cyclization of a urea, followed by removal of protective groups. The compounds are D2 -agonists and, thereby, have anti-hypertensive activity. A species of the... | 11/19/1985 |
| 4554284 | 7-(2-Aminoethyl)-1,3-benzthia- or oxa-zol-2(3H)-ones Certain aminoethyl substituted 1,3-benzthiazol- and 1,3-benzoxazol-2(3H)-ones are D2 -dopamine agonists. These compounds are prepared by reacting an appropriate o-aminophenol or thiophenol with phosgene.... | 11/19/1985 |
| 4551466 | Pyridyl-2-oxy-propyl-1H-1,2,4-triazole-3,5-diamines This invention relates to diaminotriazole derivatives in which one amino group is substituted by a 4-dialkylamino- or piperidinyl- or pyrolidinylmethyl pyrid-2-yloxypropyl group. The compounds have histamine H2 -antagonist activity. One specifi... | 11/05/1985 |
| 4548940 | Pyridylaminoalkylaminopyrimidones useful as histamine H1 -antagonists Pyridine derivatives are disclosed which are useful as histamine H1 -antagonists.... | 10/22/1985 |
| 4547512 | 2-(Imidazolyl alkylamino)-3-carboxy(or hydroxy)-pyridines This invention relates to 2-amino-3-hydroxy, and 3-carboxy pyridine derivatives, in which the amino group is substituted by a methylthioethyl, butyl or oxypropyl group bearing a terminal heterocyclic group. The compounds have histamine H2 -anta... | 10/15/1985 |
| 4547506 | 2-Pyridylaminoakylamino-4-pyrimidones useful as histamine H1 -antagonists Pyridine derivatives are disclosed which are useful as histamine H1 -antagonists.... | 10/15/1985 |
| 4543349 | Basic heptapeptide vasopressin antagonists Certain cyclic vasopressin-like peptides, which have an ω-amino- or guanidinoalkyl substituent attached to the cysteine in the 6-position of the ring, have vasopressin antagonist activity. A species of this series of new compounds is [1-(ଲ-mer... | 09/24/1985 |
| 4542124 | Octapeptide vasopressin antagonists Certain octapeptides, which have structures characterized by being a six unit cyclic peptide ring with a dipeptide tail which lacks a glycine unit at position 9, have potent vasopressin antagonist activity. The compounds here claimed are in general charac... | 09/17/1985 |
| 4540699 | N-Substituted pyridinones having histamine H2 -antagonist activity This invention relates to N-substituted pyridinone compounds which have histamine H2 -antagonist activity. A specific compound of this invention is 2-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-5-(1-methyl-2-oxopyridin -4-ylmethyl)pyrim... | 09/10/1985 |
| 4540819 | Process for preparing secondary amines New intermediates and processes for preparing 6-halo-7,8-dihydroxy-1-(p-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepi nes involve the reaction of a p-methoxyphenylglyoxal, lower alkyl hemimercaptal with a 2-chloro-3,4-dimethoxyphenethylamine, followed b... | 09/10/1985 |
| 4539207 | Pyrimidine compounds The compounds are substituted pyrimidine compounds which are histamine H2 -antagonists. A specific compound of the present invention is 2-[2-(5-dimethylaminomethyl)-2-furylmethylthio)ethylamino]-5-(3-pyridylmet hyl)-4-pyrimidone.... | 09/03/1985 |
| 4537779 | Pharmacologically active compounds Heterocyclic compounds which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A specific compound of this invention is 2-[2-(4-methyl-5-imidazolylmethylthio)ethylamino]-4-pyrimidone.... | 08/27/1985 |
| 4537891 | 2-(3,5-Substituted-2-pyridylalkylamino)-5-benzyl-4-pyrimidones 3,5-Disubstituted-2-pyridylalkylamino-5-optionally substituted benzyl-4-pyrimidones having histamine H1 -antagonist activity are disclosed.... | 08/27/1985 |
| 4537890 | 2-(3,5-Substituted-2-pyridylalkylamino)-5-oxopyridylmethyl-4-pyrimidones useful as histamine H1 -antagonists Pyridone derivatives useful as histamine H1 -antagonists are disclosed.... | 08/27/1985 |
| 4535163 | 2-Aminoalkyl-pyridine derivatives The invention provides 2-(3,5-disubstituted pyridylalkyl amino)-5-pyridylmethyl-4-pyrimidone derivatives which are useful as histamine H1 -antagonists.... | 08/13/1985 |
| 4532246 | 2-(2-Pyridylaminoalkylamino)-4-pyrimidones Pyridine derivatives are disclosed which are useful as histamine H1 -antagonists.... | 07/30/1985 |
| 4532252 | 3,5-Substituted-2-pyridylalkylamino compounds having histamine H1 -antagonist activity 3,5-Substituted-2-pyridylalkylamino derivatives are disclosed which are useful as histamine H1 -antagonists.... | 07/30/1985 |
| 4528371 | Process for preparing 6-(2-hydroxyphenyl)-3-pyridazinone A process for preparing 6-(2-hydroxyphenyl)-3-pyridazinone which comprises reacting 2-hydroxyacetophenone with glyoxylic acid under alkaline conditions, adjusting the pH of the reaction mixture to give a mixture within a pH range of about pH 4.0-9.5 and w... | 07/09/1985 |
| 4526974 | Synthesis of 2-pyridylalkylamines The invention provides a process for preparing 2-pyridylalkylamines by reacting an alkali metal derivative of a 2-methylpyridine with a haloalkylamine. The compounds are useful as intermediates in the preparation of compounds having histamine H1 | 07/02/1985 |
| 4525477 | 2-Thiazolyl, isothiazolyl, oxazolyl and isoxazolyl alkylamino-3-nitro-heterocyclic compounds 2,3-Unsaturated nitrogen-containing heterocyclic compounds with a 3-nitro group and a 2-heterocyclyl alkylamino group. The alkyl group of 2-position substituents is preferably interrupted by sulfur or oxygen. The compounds of the invention are preferably ... | 06/25/1985 |
| 4523015 | Process and nitroaminopyrimidone intermediates for histamine H2 -antagonists A process for making substituted 2-aminopyrimidones which are histamine H2 -antagonists which comprises reacting a 2-nitroaminopyrimidone with a heteroarylalkylamine, heteroarylalkylthioalkylamine, or heteroarylalkoxyalkylamine. One particular ... | 06/11/1985 |
| 4521418 | Guanidinothiazolyl derivatives The compounds are guanidinothiazolyl derivatives which are histamine H2 -antagonists. A specific compound of the present invention is 2-[2-(2-guanidino-4-thiazolylmethylthio)ethylamino]-5-(6-methyl-3-pyridylm ethyl)-4-pyrimidone.... | 06/04/1985 |
| 4521625 | Dioxocyclobutene compounds 1-(Hydroxypropylamino)-2-aminocyclobut-1-ene-3,4-dione compounds are disclosed as useful intermediates in the preparation of histamine H2 -antagonists.... | 06/04/1985 |
| 4515952 | Synthesis of 2-pyridylalkylamines substituted on the pyridyl ring by bromine The invention provides a process for preparing 2-pyridylalkylamines, substituted in one of the 3- or 5-positions by bromo and in the other by C1-4 alkyl, by reacting an appropriate C1-4 alkyl substituted 2-pyridylalkylamine with an e... | 05/07/1985 |
| 4514394 | Anti-hypertensive use of 1-(4'-branched alkylsulfonylphenyl)-6-chloro-7,8-dihydroxy-2,3,4,5-tetrahydro-1H-3-benz azepines 6-Chloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines whose structures have an isopropylsulfonyl, isopropylthio, isobutylsulfonyl or isobutylthio group substituted at the 4-position of the 1-phenyl substituent have potent renal dopaminergic... | 04/30/1985 |
| 4507320 | Dopaminergic agonist N,N-di-n-propyl-4-hydroxy-3-methanesulfonamidophenethylamine N,N-Di-n-propyl-4-hydroxy-3-methanesulfonamidophenethylamine is a potent, selective presynaptic dopaminergic agonist. The compound is prepared by N-sulfonylation of an optionally O-protected derivative of 3-amino-4-hydroxy-N,N-di-n-propylphenethylamine, f... | 03/26/1985 |
