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| Number | Title | Issue Date |
| 5227380 | Pharmaceutical compositions and methods employing camptothecins A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase I and show an... | 07/13/1993 |
| 5190947 | Codeine salt of a substituted carboxylic acid, its use and pharmaceutical compositions thereof The invention relates to the codeine salt of [2-[(2,6-dichlorophenyl)-amino]-phenyl]-acetic acid of formula ##STR1## to processes for the preparation thereof, to pharmaceutical compositions comprising that salt, and to its use as an analgesic drug. C... | 03/02/1993 |
| 5180722 | 10,11-methylenedioxy-20(RS)-camptothecin and 10,11-methylenedioxy-20(S)-camptothecin analogs A camptothecin analog having the structure shown below: ##STR1## where Z is H or C1-8 alkyl and R is NO2, NH2, N3, hydrogen, halogen, COOH, OH, O--C1-3 alkyl, SH, S--C1-3 alkyl, CN, CH... | 01/19/1993 |
| 5180824 | 6-azido-2-fluoropurine, useful in the synthesis of nucleosides This invention pertains to novel methods of synthesizing fludarabine, fludarabine phosphate and related nucleoside pharmacologic agents utilizing 6-azido-2-fluoropurine as a novel intermediate. In particular this invention pertains to a synthesis of fludarabin... | 01/19/1993 |
| 5179084 | Antiviral phosphoric acid esters of oxetanocins The present invention relates to phosphoric acid esters of oxetanocins having an antiviral activity which are represented by general formula (I): ##STR1## wherein R1 represents a phosphoric acid ester residue, X represents hydrogen, hydrox... | 01/12/1993 |
| 5175290 | 8-(oxo-substituted cycloalkyl)xanthines 1,3-Substituted-8-(oxo-substituted cycloalkyl)xanthines and pharmaceutically acceptable salts of such compounds are disclosed. Preferred compounds include the cis and trans isomers of 1,3-dipropyl-8-(3-hydroxycyclopentyl)xanthine and the cis and trans ... | 12/29/1992 |
| 5175291 | Process for preparing 1,3-dipropyl-8-(3-oxocyclopentyl)-xanthine A process for preparing 1,3-dipropyl-8-(3-oxocyclopentyl)-xanthine.... | 12/29/1992 |
| 5175288 | Process for preparing purine derivatives and intermediates thereof A process for preparing pharmaceutically active compounds of formula (A): ##STR1## wherein X is hydrogen, hydroxy, chloro, C1-6 alkoxy or phenyl C1-6 alkoxy; and Ra and Rb are hydrogen, or acyl or phosphate... | 12/29/1992 |
| 5166198 | Antiviral phosphonylalkoxy purines A compound of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein R1 is hydroxy or amino; R2 is hydrogen or amino; R3 is hydrogen, hydroxymethyl or acyloxymethyl; R4 is hydrogen or (when R | 11/24/1992 |
| 5164390 | 6-substituted purinyl piperazine derivatives 6-substituted purinyl piperazine derivatives and a method of synthesis for the derivatives are described. The 6-substituted purinyl piperazine derivatives are useful as cardiotonic agents and antiarrhythmic agents.... | 11/17/1992 |
| 5155098 | N-heteroaryl-purin-6-amines, and pharmaceutical compositions and methods employing them This invention relates to a N-heteroaryl-purin-6-amine of the formula ##STR1## where R1 is hydrogen, lower alkyl, and arylloweralkyl; R2 and R3 are independently hydrogen, lower alkyl or R2 and R3 ... | 10/13/1992 |
| 5151430 | Specific 17ଲ-thiobenzoyl-4-aza-5-androst-1-en-3-ones as antiandrogen agents Specific 17ଲ-thiobenzoyl-4-aza-5-androst-1-en-3-ones as antiandrogenic agents of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl and R2 is phenyl substituted with one or more of: --SH, --SC1 ... | 09/29/1992 |
| 5151429 | 17ଲ-acyl-4-aza-5-androst-1-ene-3-ones as 5 reductase inhibitors 17ଲ-Acyl-4-aza-5-androst-1-en-3-ones of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl and R2 is a monovalent radical selected from straight and branched chain alkyl of from 1-12 carbons, or monocyclic ... | 09/29/1992 |
| 5151518 | N-arylation of isatins A process for the N-arylation of isatins with organo bismuth reagents is disclosed.... | 09/29/1992 |
| 5144034 | Process for the synthesis of cyclopentene derivatives of purines This invention relates to a new process for preparing certain optically active cyclopentene derivatives and novel intermediates used in this process. In particular, the invention concerns the synthesis of the 1'R-cis isomer of carbovir, (1'R-cis)-2-a... | 09/01/1992 |
| 5142051 | N-phosphonylmethoxyalkyl derivatives of pyrimidine and purine bases and a therapeutical composition therefrom with antiviral activity This invention relates to new nucleotide analogues and solves the technical problem of their use as biologically active compounds. The subject of this invention are N-(2-phosphonylmethoxyethyl) and N-(3-hydroxy-2-phosphonylmethoxypropyl) derivatives of py... | 08/25/1992 |
| 5138057 | Chemical process for the preparation of purine derivatives A process for the preparation of a compound of formula (I) ##STR1## which process comprises reacting a compound of formula (II): ##STR2## wherein the amino group is optionally protected, with a side chain intermediate of formula (III): ##ST... | 08/11/1992 |
| 5138063 | 17ଲ-methoxycarbonyl-4-aza-androsten-1-en-3-ones 17ଲ-Acyl-4-aza-5-androst-1-in-3-ones of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl R2 is methoxy, a monovalent radical selected from straight and branched chain alkyl of from 1-12 carbons, or m... | 08/11/1992 |
| 5127934 | Stabilized compositions comprising isothiazolones and epoxides Organic stabilizers are used to stabilize various materials which are normally unstable neat or in solution. These compositions exhibit bactericidal, fungicidal and algaecidal properties.... | 07/07/1992 |
| 5126347 | Isomeric dideoxynuclesides Isomeric derivatives of 2',3'-dideoxyadenosine and 2',3'-dideoxyguanosine wherein the adenine or guanine base is attached to the 1' position of the iso-dideoxysugar residue by the 9-N position, the novel intermediates used in the synthesis of these compou... | 06/30/1992 |
| 5126452 | Synthesis of purine substituted cyclopentene derivatives This invention relates to new process for preparing certain optically active purine substituted cyclopentene derivatives and novel intermediates used in this process. In particular, the invention concerns the synthesis of the 1R-cis isomer of carbovir, ... | 06/30/1992 |
| 5122606 | 10,11-methylenedioxy camptothecins The invention relates to a method of producing 20(S)-camptothecin, 20(R)-camptothecin and analogs thereof. The method involves the resolution of an mixture of enantiomers of an intermediate lactone.... | 06/16/1992 |
| 5122526 | Camptothecin and analogs thereof and pharmaceutical compositions and method using them A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase I and show an... | 06/16/1992 |
| 5122607 | Racemic and optically active octahydro-indolo(2,3-a) tetrahydropyranyl (2,3-c) quinolizine diester derivatives and process for preparing the same New intermediate compounds are disclosed of the formula I, ##STR1## wherein R1 and R2 are independently alkyl having 1 to 4 carbon atoms, or acid-addition salts thereof of formula Ib, ##STR2## wherein X represents an acid r... | 06/16/1992 |
| 5120742 | 17 ଲ-acyl-4-aza-5 -androst-1-ene-3-ones as 5 -reductase inhibitors 17ଲ-Acyl-4-aza-5-Androst-1-end-3-ones of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl and R3 is cycloalkyl of from 4-8 carbons; and pharmaceutical formulation of the above compounds are active as test... | 06/09/1992 |
| 5116831 | Aminoalkyl-substituted cycloalkylamine platinum (II) complexes Square-planar four-coordinate complexes of cis-platinum (II) with neutral bidentate aminoalkyl-substituted cycloalkylamine ligands and bromo-, chloro-, iodo-, nitrato-, oxalato-, or malanato-ligands possess antimicrobial activity as well as activity again... | 05/26/1992 |
| 5112970 | Water-soluble triphendioxazine compounds and precursors thereof containing sulfonyl groups, processes for their preparation and the use of the triphendioxazines as dyestuffs Water-soluble triphendioxazine compounds of the formula (1) with quaternary ammonium groups ##STR1## in which the substituents are defined in claim 1. The compounds (1) have fiber-reactive dyestuff properties and dye, for example, cellulose fiber ... | 05/12/1992 |
| 5112818 | 2-(2-cyclopropylpyrrolidin-4-ylthio)carbapenhem derivatives A compound of the formula: ##STR1## wherein R1 is a hydrogen atom or a methyl group, each of R2 and R3 which may be the same or different, is a hydrogen atom or a lower alkyl group, or R2 and R3 ... | 05/12/1992 |
| 5112975 | Preparation of noroxymorphone from morphine 3,17-(diethoxycarbonyl)normorphine, which may be prepared by reaction of morphine with ethyl chloroformate, is converted to 3,17-(diethoxycarbonyl)normorphinone, a novel compound, by oxidation. The novel normorphinone derivative is converted to 3,17-... | 05/12/1992 |
| 5110818 | Anticonvulsive substituted-9-benzyl-9H-purines The invention relates to novel 9H-purine derivatives, especially to the novel substituted 9-benzyl-9H-purines of the general formula ##STR1## in which Ph is a phenyl radical substituted by halogen, R1 is hydrogen or a free amino group or a... | 05/05/1992 |
| 5110926 | Process for the preparation of a carbocyclic nucleoside analogue A process is described for the preparation of carbocyclic guanosine from aristeromycin in a multi-step procedure, the final step of which is the hydrolysis of a compound of the formula ##STR1## wherein R1 represents a C1-6 alkyl... | 05/05/1992 |
| 5110932 | Polysubstituted aryl acridinium esters The present invention relates to novel acridinium esters which are useful as luminescent labels in specific binding assays such as immunoassays or nucleic acid hybridization assays. More particularly, polysubstituted aryl acridinium esters are highly stab... | 05/05/1992 |
| 5109003 | Method for the treatment of peptic ulcer disease Therapeutic agents for the treatment of peptic ulcer disease, containing as active ingredient, at least one compound of the general formula I ##STR1## wherein one of R1 and R3 is ##STR2## (wherein m is 1-5, R4 re... | 04/28/1992 |
| 5108994 | Antiviral purine derivatives Compounds of formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein R1 is hydroxy or amino; R2 is hydrogen or amino; R3 is hydrogen, hydroxymethyl or acyloxymethyl; R4 is a group of formula: ... | 04/28/1992 |
| 5104892 | Substituted benzimidazole derivatives possessing Class III antiarrhythmic activity This invention relates to N-heteroalkyl-substituted 1-aryloxy-2-propanolamine and proplyamine derivatives possessing anti-arrhythmic activity, to pharmaceutical compositions and to method for production thereof.... | 04/14/1992 |
| 5100881 | N-(23-vincristinoyl) and N-(5'-noranhydro-23-vinblastinoyl) compounds of 1-aminomethylphosphonic acid useful for the treatment of neoplastic diseases The invention relates to the compounds of general formula I: ##STR1## in which: R1 represents a hydrogen atom, a linear or branched alkyl radical containing from 1 to 6 carbon atoms, a linear or branched alkenyl radical containing from 2 t... | 03/31/1992 |
| 5098908 | 17ଲ-hydroxybenzoyl-4-aza-5-androst-1-en-3-ones as testosterone reductase inhibitors Novel 17ଲ-hydroxybenzoyl-4-aza-5-androst-1-en-3-ones as tetosterone reductase inhibitors of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethy and R2 is phenyl substituted with one or more of: --OH, --OFC | 03/24/1992 |
| 5093337 | Substituted derivatives of 20,21-dinoreburnamenine, their use as medicaments and the pharmaceutical compositions containing them The invention concerns compounds of formula (I); ##STR1## in which R1, R2 and R3, identical or different, stand for hydrogen, halogen, alkyl or alkoxy (C1-5), hydroxy, trifluoromethyl, nitro, amino, alkylam... | 03/03/1992 |
| 5091431 | Phosphodiesterase inhibitors Compounds having an optionally-substituted purine derivative portion and a carbobicyclic or heterobicyclic portion, which compounds are useful as phosphodiesterase inhibitors, are disclosed. Also disclosed are intermediates, methods for making the inhibit... | 02/25/1992 |
| 5084574 | Dehydrogenation process A process for dehydrogenating a compound of the formula ##STR1## which comprises reacting the compound with a silylating agent in the presence of a quinone to introduce a Ɗ1 double bond.... | 01/28/1992 |
