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| Number | Title | Issue Date |
| 7141594 | Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particula... | 11/28/2006 |
| 6927036 | Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof Disclosed is a method for synthesizing 1-(acyloxy)-alkyl derivatives of primary or secondary amine drugs from 1-acyl-alkyl derivatives of primary or secondary amine drugs, which typically proceeds stereospecifically, in high yield, does not require the use of activa... | 08/09/2005 |
| 6673822 | Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, mor... | 01/06/2004 |
| 6645950 | Benzimidazole vascular damaging agents Vascular damaging agents composed of substituted 5(6)-substituted benzimidazole-2-carbamates are provided. These agents are useful in the preparation of medicaments for the treatment of diseases involving neovascularisation, particularly for the treatment... | 11/11/2003 |
| 6613743 | Sulfonamide inhibitors of aspartyl protease The present invention relates to a novel class of sulfonamides of formula I which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and phy... | 09/02/2003 |
| 6562964 | Heterocyclic compounds as inhibitors of rotamase enzymes Compounds of the formula (I): ##STR1## wherein A, Y, R, X, R1, R2, R3 and R4 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal r... | 05/13/2003 |
| 6482843 | Compounds and methods for use thereof in the treatment of cancer or viral infections Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm blooded animals by administration of these compounds. Such compounds may be used in combination with a c... | 11/19/2002 |
| 5919792 | Integrin antagonists This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are v댣 antagonists, ... | 07/06/1999 |
| 5821242 | Anti-viral compounds The present application provides a series of benzimidazole compounds which inhibit the growth of picornaviruses, such as rhinoviruses, enteroviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus and flaviviruses such as... | 10/13/1998 |
| 5693661 | Anti-viral compounds Certain vinyl acetylene benzimidazole compounds which inhibit the growth of picornaviruses, such as rhinoviruses, enteroviruses, cardioviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus.... | 12/02/1997 |
| 5475005 | Benzimidazole anthelmintic agents Benzimidazole anthelmintic agents of the formula (I) and their non-toxic salts, wherein R1, which is in the 5(6)-position, is either H or certain stated substituents, "alk" is a methylene or ethylene group; R2 is cyano, C1... | 12/12/1995 |
| 5459155 | Benzimidazole anthelmintic agents This invention is directed to anthelmintic benzimidazole compounds of formula (IA) or (IB) ##STR1## or non-toxic salts thereof, wherein R, which in the compounds (IA) is in the 5- or 6- position, is H, benzoyl, styryl, phenyloxy, phenylthio, phe... | 10/17/1995 |
| 5304604 | Hydroxamic acid collagenase inhibotors Compounds of general formula I: ##STR1## wherein: R1 represents a hydrogen atom or a C1 -C6 alkyl, C1 -C6 alkenyl, phenyl, phenyl(C1 -C6)alkyl, C1 -C6 ... | 04/19/1994 |
| 5023337 | Chemical process for the preparation of pharmaceutically active compounds The present invention is directed to the preparation of benzimidazole derivatives of the formula (I), ##STR1## wherein A=stands for S, SO or SO2, R1 =stands for C1-4 alkyl group, R2 =stands for C1-4 a... | 06/11/1991 |
| 4948891 | Benzamide protease inhibitors Compounds of the formula ##STR1## where Het is a heterocyclic group, n is an integer of 0 to 2 and R1 is hydrogen or lower alkyl are protease inhibitors useful as anti-plasmin and anti-thrombin agents.... | 08/14/1990 |
| 4940800 | Beazimidazole compounds active as inhibitors of the cholesterol biosynthesis The compounds of formula ##STR1## wherein R, R1, R2, R3, and R4 have the meanings given in the specification, are described. The compounds of formula I are active as inhibitors of the enzyme HMG-CoA reducta... | 07/10/1990 |
| 4874864 | Benzamide protease inhibitors Compounds of the formula ##STR1## where HET is a heterocyclic group, n is an integer of 0 to 2 and R1 is hydrogen or lower alkyl are protease inhibitors use as anti-plasmin and anti-thrombin agents.... | 10/17/1989 |
| 4675413 | Process for the preparation of benzimidazole-thiol A new process is disclosed for preparing a compound of the formula (I) ##STR1## wherein R is C1 to C5 alkyl; which comprises reducing a compound of the formula (II) ##STR2## or salt thereof wherein A is --SO2 X, ... | 06/23/1987 |
| 4656290 | Process for preparing thio, dithio or carbonyl compounds A process is disclosed for the preparation of compounds of the Formula I wherein X is thio, dithio or carbonyl and R and R1 are defined hereinbelow which comprises reducing a compound of the Formula II wherein A is chlorosulfonyl or a group of the Formul... | 04/07/1987 |
| 4639463 | Substituted phenylsulfonyloxybenzimidazolecarbamates and anthelmintic compositions New phenylsulfonyloxybenzimidazolecarbamates of the formula ##STR1## are described, as are processes for their preparation. The new compounds have anthelmintic activity, including, in particular, against liver flukes.... | 01/27/1987 |
| 4628087 | Process for the preparation of pharmacologically active compounds containing a sulfoxide group Process for the preparation of pharmacologically active compounds containing a sulfoxide group by oxidation of a thioether with hypochlorite in an alkaline medium at a pH higher than 10 and at a temperature comprised between 0° and 40° C.... | 12/09/1986 |
| 4599428 | Process for the preparation of 5(6)-thio substituted benzimidazoles A process is disclosed for the preparation of a compound of the formula (XI) ##STR1## or a salt thereof, wherein R1 is hydrogen, halogen, C1 to C4 alkyl, C1 to C3 alkoxy, or trifluoromethyl; R | 07/08/1986 |
| 4487936 | Preparation of alkylthiobenzimidazoles The invention concerns a new process for the preparation of biologically active 2-[(alkoxycarbonyl)amino]-5-(alkylthio)-1H-benzimidazoles of the formula (V) ##STR1## wherein R and R1 independently stand for alkyl having 1 to 3 carbon ... | 12/11/1984 |
| 4473697 | Production of thiocyanato benzimidazoles A new process is disclosed for the preparation of a compound of the formula (VIII) ##STR1## wherein R1 is hydrogen, halogen, C1-4 alkyl, C1-3 alkoxy, or trifluoromethyl; R5 is amino or C1-4 alkox... | 09/25/1984 |
| 4454065 | Oligopeptide prodrugs Prodrugs are described whose structures have a oligopeptide chain which is substituted by a nucleophilic chemotherapeutic residue at the -position. The products have increased cell membrane permeability and beneficial physico-chemical properties.... | 06/12/1984 |
| 4420487 | Diuretic and antihypertensive benzimidazoles The invention relates to compounds which exhibit diuretic and antihypertensive properties and have the following structures: ##STR1## or pharmaceutically acceptable salts thereof, wherein: X=halogen or trifluoromethyl Y1 and Y2 ... | 12/13/1983 |
| 4368328 | Process for preparing alkylthiobenzimidazoles The invention concerns a new process for the preparation of biologically active 2-[(alkoxycarbonyl)amino]-5-(alkylthio)-1H-benzimidazoles of the general formula (V) ##STR1## wherein R and R1 independently stand for alkyl having 1 to 3 carb... | 01/11/1983 |
| 4303666 | 5-Phenylseleno-2-benzimidazole carbamates The invention relates to novel 5-phenylseleno-2-benzimidazolecarbamate derivatives, for example methyl 5-phenylseleno-2-benzimidazole-carbamate, which possess useful anthelmintic and/or fasciolicidal activity, and processes for the manufacture of the nove... | 12/01/1981 |
| 4299837 | Anthelmintic benzimidazole-carbamates Benzimidazole-carbamates endowed wth anthelmintic activity, and substituted in position 5(6) by a diene chain bound to the position 5(6) by an oxygen or sulphur atom optionally oxidized, are described. The processes for their preparation, the intermediates the... | 11/10/1981 |
| 4287199 | Benzimidazolylcarbamic acid esters substituted on the benzenoid nucleus by an oxy or thio substituent The invention relates to 2-benzimidazolylcarbamic acid esters, substituted on the benzenoid nucleus by an aminoalkoxy, aminoalkylthio, an aminoalkylsulphinyl or an aminoalkylsulphonyl grouping. The invention also includes methods for making the compounds ... | 09/01/1981 |
| 4259344 | Sulfur-containing benzimidazole derivatives A process for the preparation of anthelmintic compounds of the formula: ##STR1## wherein R1 is hydrogen or --COOR; R5 is C1 to C4 alkyl; R2 is halogen, alkyl, trifluoromethyl, alkoxy, aryloxy, or aralkoxy;... | 03/31/1981 |
| 4258198 | 5-Cycloalkyl thio- and oxy-2-carbalkoxyaminobenzimidazoles New anthelmintic compounds, compositions and methods of use are described utilizing 5-cycloalkylthio and oxy-2-carbalkoxyaminobenzimidazole. Methods of preparation involve the reaction of 4-cycloalkylthio- or oxy-o-phenylenediamine with methyl cyanocarbam... | 03/24/1981 |
| 4182893 | Anthelmintic benzimidazol-carbamates Benzimidazol(2)methylcarbamates substituted in position 5(6) are disclosed, together with a method for preparing them, and use thereof in suitable form for combatting intestinal, pulmonary and hepatic parasites, particularly Helminthes, in animals.... | 01/08/1980 |
| 4174400 | Anthelmintic benzimidazoles Benzimidazole compounds are disclosed which are substituted at the 2-position with a loweralkoxy carbonylamino group and at the 5-position with a halogenated loweralkenyl group or a halogenated loweralkoxy, loweralkylthio, loweralkylsulfinyl or loweralkyl... | 11/13/1979 |
| 4167569 | Pyrimido[1,2-a ]benzimidazole derivatives The invention concerns 3,4-dihydropyrimido [1,2-a]benzimidazole derivatives bearing one or more substituents at positions 6, 7, 8 or 9; processes for their preparation and manufacture; and pharmaceutical compositions thereof. The compounds inhibit the agg... | 09/11/1979 |
| 4156006 | Vinyl sulfide derivatives of benzimidazoles Vinyl sulfide derivatives of benzimidazoles are provided having the structure ##STR1## wherein R is lower alkyl or phenyl-lower alkyl, R1 is lower alkyl, R2 is hydrogen or lower alkyl, or R1 and R2 may be t... | 05/22/1979 |
| 4152522 | Process for the preparation of 2-benzimidazole carbamates A process for preparing 2-benzimidazole carbamate compounds by condensing an alkyl cyano carbamate with an o-phenylenediamine produced by reacting an ortho-nitro-aniline with thiocyanogen followed by replacement of the cyanide with an alkyl group and then... | 05/01/1979 |
| 4145431 | Method of treating helminthiasis by parenteral administration of sulfide- and sulfoxide-derivatives of benzimidazoles A method is provided for treating or inhibiting helminthiasis by parenterally or topically administering sulfide or sulfoxide derivatives of benzimidazoles having the structure ##STR1## wherein R1 is lower alkyl or phenyl-lower alkyl, R | 03/20/1979 |
| 4145433 | Method of treating helminthiasis by parenteral administration of sulfoxide derivatives of benzimidazoles A method is provided for treating or inhibiting helminthiasis by parenterally or topically administering sulfoxide derivatives of benzimidazoles having the structure ##STR1## wherein R1 is lower alkyl or phenyl-lower alkyl, R2 a... | 03/20/1979 |
| 4138493 | 2,2-Dihalo-1(3)-lower alkyl-cyclopropylalkylthio benzimidazole derivatives, compositions thereof and method of use in treating tapeworms and whipworms Benzimidazole derivatives are provided having the structure ##STR1## wherein R1 is lower alkyl or phenyl-lower alkyl, R2 and R3 are the same or different and are hydrogen or lower alkyl, R4 is lower alkyl o... | 02/06/1979 |
