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| Number | Title | Issue Date |
| 4939261 | N-substituted butyramide derivatives useful for treatment of conditions responsive to inhibition of enkephalinase Disclosed are compounds of the formula ##STR1## wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, ... | 07/03/1990 |
| 4935536 | Protecting groups for asparagine and glutamine in peptide synthesis Trialkoxybenzyl (Taob) protected asparagine and glutamine, a method of synthesis and a method of use are provided. The Taob protected Asn and Gln have the following formulae: ##STR1## wherein Z is an alkyl group having from 1 to 10 carbon atoms; X an... | 06/19/1990 |
| 4933367 | Carboxylic acid derivatives, processes for the preparation thereof, the use thereof, and pharmaceutical compositions which contain these compounds This invention relates to carboxylic acid derivatives and their use thereof. The compounds are useful in treatment of various diseases such as diabetes, prediabetic conditions, adipositas ailments or atherosclerosis.... | 06/12/1990 |
| 4929751 | Vinyl tricarbonyl compounds and methods of making the same A vinyl tricarbonyl compound of the formula ##STR1## or its monohydrate of the formula ##STR2## wherein R1 is a hydrogen, halogen, unsubstituted or substituted C1 to C30 alkyl, unsubstituted or substituted aryl, ... | 05/29/1990 |
| 4923888 | Butenoic acid amides, their salts, and pharmaceutical compositions containing them The present invention relates to novel compounds of the general formula (I), ##STR1## wherein R stands for hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy or C1-4 acylamino group; R1 means hydrogen or a carboxyl... | 05/08/1990 |
| 4918095 | Compositions with antibiotic activity and their use The compound N-[(1S,2R)-fluoromethyl-2-hydroxy-2-(4-methylsulphonyl-phenyl)-ethyl]-2-pr openamide and the derivatives thereof in which the hydroxy in 2 position is esterified by a mono or dicarboxylic acid or by an aminoacid are described. Such compou... | 04/17/1990 |
| 4916252 | Process for preparing optically active alcohol A process for preparing an optically active alcohol is disclosed, which comprises asymmetrically hydrogenating a 1,3-diketone in the presence of a ruthenium-optically active phosphine complex as a catalyst. The resulting alcohol has high optical purity.... | 04/10/1990 |
| 4914227 | Certain intermediate 3-carbamoyloxyalkyl propiolic acid derivatives A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##ST... | 04/03/1990 |
| 4912221 | Chiral 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid and precursors and preparation thereof The instant invention relates to optically pure, L-(S)forms of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid compounds and their method of preparation from optionally pure L-phenylalanine precursor compounds and their preparation utilizing novel in sit... | 03/27/1990 |
| 4898977 | Processes for the preparation of 5-amino-4-hydroxyvaleric acid derivatives The invention relates to novel processes and intermediates for the preparation of 5-amino-4-hydroxyvaleric acid derivatives of the formula ##STR1## in which R1 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower... | 02/06/1990 |
| 4895842 | Phenylalanine derivative and proteinase inhibitor A phenylalanine derivative having the formula (I): ##STR1## where R1 and R2 are independently hydrogen provided that both R1 and R2 are not hydrogen at the same time; C1 -C8 alkyl which may... | 01/23/1990 |
| 4894437 | Novel renin inhibiting polypeptide analogs containing S-aryl-D- or L- or DL-cysteinyl, 3-(arylthio)lactic acid or 3-(arylthio)alkyl moieties The present invention provides novel renin-inhibiting peptides of the formula X-A6 -B5 -C8 -D9 -E10 -F11 -G12 -H13 -I14 -Z, wherein X and Z are terminal groups, ... | 01/16/1990 |
| 4879403 | Process for the preparation of cis, endo-2-azabicyclo-[3.3.0]-octane-3-carboxylic acids Compounds of the formula I ##STR1## in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R1 denotes hydrogen, allyl, vinyl or a side-chain o... | 11/07/1989 |
| 4879398 | Process for producing 2,6-disubstituted tyrosine A process for making 2,6-disubstituted tyrosine by the noble metal coupling of a disubstituted aromatic halide or diazonium salt with an amino-protected 2-aminoacrylic acid to form a (Z)-ଲ-(disubstituted phenyl)--acylaminoacrylate, and asymme... | 11/07/1989 |
| 4876399 | Taxols, their preparation and intermediates thereof The present invention is directed to novel taxols useful as a chemotherapeutic agent. Moreover, the present invention is directed to the process of preparing taxols and various intermediates in said process. A key intermediate is this process is 2,5-dihyd... | 10/24/1989 |
| 4876343 | Process for statine and statine analogs An improved process for the preparation of statine, the phenyl analog of statine, the cyclohexyl analog of statine and derivatives thereof is described, as well as other valuable intermediates used in the process.... | 10/24/1989 |
| 4873253 | Phenylalanine derivative and proteinase inhibitor A phenylalanine derivative having the formula (I): ##STR1## wherein A represents ##STR2## B represents ##STR3## wherein m is 0, 1, or 2 and n is 3, 4, or 5; X represents (a) hydroxy, (b) nitro, (c) amino, (d) phenoxy which may be subs... | 10/10/1989 |
| 4871870 | Immunomodulators and method of making same A compound having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein A is an amino acid identifying group; B is a hydrogen atom, an alkyl group having 1-5, inclusive, carbon atoms, or an aralkyl group having 6-12, inclusive, ... | 10/03/1989 |
| 4870182 | 4-Hydroxy-quinoline-3-carboxylic A process for the preparation of a compound of the formula ##STR1## in which Y is a nitrile group, an ester group COOR1 or an acid amide CONR2 R3, R1, R2 and R3 each independently is hydrog... | 09/26/1989 |
| 4866197 | Production of N-((2-alkoxy-6-methoxy-5-(trifluoromethyl)-1-naphthalenyl)carbonyl)-N-me thylglycine esters Process for the production of N-[[2-alkoxy-6-methoxy-5-(trifluoromethyl)-1-naphthalenyl]carbonyl]-N-meth ylglycine esters and intermediates for their production. Said esters are themselves intermediates for the manufacture of compounds which inhibit a... | 09/12/1989 |
| 4859233 | 2,3,6-trichlorobenzohydroxamic acid derivatives Disclosed are herbicidal compounds of the general formula I; ##STR1## wherein A is O-alkylene of 1 to 5 carbon atoms, O-alkenylene of 3 to 6 carbon atoms in which the unsaturation is non-adjacent the oxygen atom thereof or NH-alkylene in which the al... | 08/22/1989 |
| 4851443 | Carboxylic acid amides, compositions and medical use thereof Amide derivatives of non-steroidal anti-inflammatory carboxylic acids which have anti-inflammatory activity in their own right as well as being effective as pro-drugs of the carboxylic acids.... | 07/25/1989 |
| 4843062 | N-acyl-N-napthoylglycines as aldose reductase inhibitors Disclosed herein are N-acyl-N-napthoylglycines and methods of their preparation. The N-acyl-N-napthoylglycines are novel aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.... | 06/27/1989 |
| 4837353 | Dopamine-ଲ-hydroxylase inhibitors 2-(N-Phenylakyl-N-formyl)amino-3-hydroxy-2-propenoic acids are intermediates for mercaptoimidazolecarboxylic acids which are dopamine-ଲ-hydroxylase inhibitors.... | 06/06/1989 |
| 4831190 | Trifluorohydroxyaromatic acid and preparation thereof There are disclosed 2,4,5-Trifluoro-3-hydroxybenzoic acid represented by the following formula (I): ##STR1## and a salt thereof and a process for preparing the same. Further, there is disclosed a process for preparing 3,5,6-trifluoro-4-hydroxyphthali... | 05/16/1989 |
| 4829090 | Chrysene derivatives The present invention relates to compounds of formula (I) or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; ... | 05/09/1989 |
| 4822818 | Bicycle compounds, their production and use New bicyclic compounds, inclusive of salts thereof, of the formula: ##STR1## wherein R1 and R2 are the same or different and each represents hydrogen, hydroxyl or lower alkoxy, R3 is hydrogen or lower alkyl, R4 | 04/18/1989 |
| 4816598 | 4-Amino-butanoic acid derivatives The invention relates to 4-amino-butanoic acid derivatives of general formula: ##STR1## in which: M represents an alkali metal atom, R represents a protected amino group, R1 represents a labile group, R2 represents hydrogen, a branch... | 03/28/1989 |
| 4814484 | Thyronine derivatives The invention relates to new thyronine derivatives of the formula ##STR1## in which n is 1-6, R denotes hydroxyl, alkyl or aryl, R1 and R2 are identical or different and denote iodine or hydrogen, and R3 denotes hydro... | 03/21/1989 |
| 4814485 | 4-aminobutanoic acid derivatives, process of preparation and use thereof The invention relates to new (4S)-4-aminobutanoic acid derivatives of general formula: ##STR1## in which: R represents an N-protective group, R1 represents hydrogen, an alkali metal atom such as lithium, sodium or potassium or a liabile gr... | 03/21/1989 |
| 4797496 | Process for the preparation of pyrrolidone derivatives Process for preparing pyrrolidinone derivatives of (1) ##STR1## in which R is hydrogen, alkyl or acyl characterized in that a compound of (2) ##STR2## wherein R1 is hydrogen and R2 is benzyl or substituted benzyl, or R... | 01/10/1989 |
| 4791216 | Para ethyl amino phenol pharmaceutical compounds There are provided paraethylamine phenol compounds of formula I, ##STR1## and pharmaceutically acceptable derivatives thereof. There are also described the use of the compounds of formula I as pharmaceuticals, methods for making the compounds and pha... | 12/13/1988 |
| 4783537 | -(aminoalkyl)-arylacetic acid derivatives Novel -aryl--(ω-aminoalkyl)--[hydroxy(aralkyl and cycloalkyl)]acetic acid derivatives and -aryl--(ω-aminoalkyl)-[alkanoyloxy(aralkyl and cycloalkyl)]acetic acid derivatives, such as N,N-dimethyl-2-(hydroxyp... | 11/08/1988 |
| 4783480 | 6-keto-prostaglandin E1 derivatives A 6-keto-prostaglandin E1 derivative of the formula: ##STR1## (wherein R1 represents an amino acid or amino alcohol residue, R2 represents a single bond or an alkylene group of from 1 to 4 carbon atoms, R3 ... | 11/08/1988 |
| 4778514 | N-acyl amino acid derivative and process for production and use thereof N-halogenophenoxyacetyl amino acid or ester thereof and salt thereof, a process for production thereof comprising acylation of amino acid or derivative thereof, a herbicidal composition comprising the compound, and a method for killing or controlling plan... | 10/18/1988 |
| 4777253 | Process for preparation of racemate and optically active ofloxacin and related derivatives A process for producing racemic or optically active compounds of the formula: ##STR1## wherein R1 is hydrogen, C1 to C6 alkyl or benzyl; and Z is amino or substituted amino. Also disclosed are intermediates useful in ... | 10/11/1988 |
| 4764619 | Optically active compounds, smectic liquid crystal compositions containing them and smectic liquid crystal display devices An optically active compound having the formula: ##STR1## wherein each of Z and Z' is a single bond, --COO--, --OCO--, --CH2 CH2 --, --OCH2 -- or --CH2 O--, R is an alkyl group having from 1 to 12 carbon at... | 08/16/1988 |
| 4755614 | Preparation of herbicides containing a phosphonate group from intermediate benzoxazines Preparation of intermediates for herbicides of formula ##STR1## by the reaction of organic phosphites with benzoxazines of formula in which Bzx denotes the radical of formula: ##STR2## X is a usual substituent of phenols n is an integer from 0 to 4 R... | 07/05/1988 |
| 4743691 | 2-halomethyl derivatives of 2-amino acids 2-(Fluoromethyl or chloromethyl)-2,5-diaminopentanoic acid, 2-(fluoromethyl or chloromethyl)-2,6-diaminohexanoic acid, and 2-fluoromethyl-2-amino-5-guanidinopentanoic acid, and certain derivatives thereof, are inhibitors of ornithine decarboxylase. Method... | 05/10/1988 |
| 4734120 | Dipeptides containing C-terminal phosphinothricin, a process for their preparation and their use for controlling undesirable plant growth Dipeptides containing C-terminal phosphinothricin of the formula ##STR1## in which phosphinothricin is attached to a--preferably natural--amino acids at the amino group are effective herbicides in the pre-emergence and post-emergence techniques. The ... | 03/29/1988 |
