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| Number | Title | Issue Date |
| 8080654 | Macrocyclic quinoxaline compounds as HCV NS3 protease inhibitors The present invention relates to macrocyclic a compound of formula (I) and its use as inhibitors of the hepatitis C virus (HCV) NS3 protease, and in treating or preventing HCV infections. ... | 12/20/2011 |
| 7202256 | Proline CCI-779, production of and uses therefor, and two-step enzymatic synthesis of proline CCI-779 and CCI-779 Methods for the synthesis of CCI-779 and proline-CCI-779 are described, including a method involving lipase-catalyzed acetylation of 42-hydroxy of rapamycin with a vinyl ester of 2,2-bis(hydroxymethyl) propionic acid in an organic solvent followed by deprotection. A... | 04/10/2007 |
| 7202246 | Spiro-rifamycin derivatives targeting RNA polymerase Compounds of the current invention relate to rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. More specifically, compounds of the current invention relate to a series of novel spiro rifamycin derivati... | 04/10/2007 |
| 7022720 | Synthetic diazonamides as novel anti-mitotic agents The application discloses novel synthetic compounds, modeled after unique toxins extracted from the marine invertebrate Diazona angulata useful in the treatment abnormal cell mitosis. The application also discloses novel methods for synthesis of these compoun... | 04/04/2006 |
| 6946482 | Motilide compounds Motilide compounds having the formula (I), wherein R1, R2, R3, and R4 are as defined herein, and methods for their preparation and use in the treatment of diseases or conditi... | 09/20/2005 |
| 6878820 | Streptogramin derivatives, their preparation and compositions containing them The present invention relates to group A streptogramin derivatives of general formula (I) and processes for preparing the same: which has particularly advantageous antibacterial activity. ... | 04/12/2005 |
| 6610722 | Inhibitors of prenyl-protein transferase The present invention is directed to peptidomimetic macrocyclic compounds that inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds ... | 08/26/2003 |
| 6596717 | Streptogramin derivatives, their preparation and compositions which contain them Group A streptogramin derivatives of formula (I) and salts thereof: ##STR1## and Group A streptogramin derivatives of formula (III) and salts thereof: ##STR2## as well as processes for preparing such streptogramins, and pharmaceutical compositions compris... | 07/22/2003 |
| 6569854 | Streptogramin derivatives, their preparation and compositions containing them Group A streptogramin derivatives of general formula (I) in which: R1 represents a halogen atom or an azido or thiocyanato radical, R2 represents a hydrogen atom or a methyl or ethyl radical, R3 represents a hydrogen atom, or the residue... | 05/27/2003 |
| 6562852 | Streptogramin derivatives, their preparation and compositions which contain them Group A streptogramin derivatives of formula (I) and salts thereof: ##STR1## Group A streptogramin derivatives of formula (II) and salts thereof: ##STR2## and Group A streptogramin derivatives of formula (III) and salts thereof: ##STR3## as well as proces... | 05/13/2003 |
| 6410534 | Inhibitors of prenyl-protein transferase The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds... | 06/25/2002 |
| 6025350 | C-4" substituted macrolide antibiotics This invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are potent antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infec... | 02/15/2000 |
| 5952320 | Macrocyclic inhibitors of matrix metalloproteinases and TNF secretion Macrocyclic compounds of formula ##STR1## are potent inhibitors of matrix metalloproteinase and are useful in the treatment of diseases in which matrix metalloproteinase play a role. Also disclosed are matrix metalloproteinase inhibiting compositions... | 09/14/1999 |
| 5925649 | Ascomycins The invention provides novel ascomycins bearing one or more physiologically hydrolyzable and acceptable oxycarbonyl moieties or carboxy moieties, such compounds being found useful as pharmaceuticals, especially in the treatment of asthma an dermatitis. Me... | 07/20/1999 |
| 5786350 | 36-derivatives of rifamycins and their use as antimicrobial agents Rifamycin antibiotic derivatives of formulae (I) and (Ia) bearing at the position 36 a substituent selected from (C1 -C8)alkyl, halo, hydroxy, (C1 -C4)acyloxy, (C1-C.sub.4)alkoxy, (C1 -C | 07/28/1998 |
| 5538961 | Macrocyclic lactam prokinetic agents Macrocylic lactam compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein A is selected from ##STR2## also disclosed are synthetic processes and intermediates useful in the preparation of the compounds of the inv... | 07/23/1996 |
| 5523401 | Macrocyclic lactam prokinetic agents Macrocylic lactam compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein A is selected from ##STR2## also disclosed are synthetic processes and intermediates useful in the preparation of the compounds of the inv... | 06/04/1996 |
| 5378837 | Process for preparing 2'-(diethylamino)rifamycin P (P/DEA) The present invention relates to a new one-pot process for preparing 2'-(diethylamino)rifamycin P and its 25-desacetyl derivative which consists in cyclizing 3-bromorifamycin S or its 25-desacetyl derivative, dissolved in dimethylformamide, with 1,1-dieth... | 01/03/1995 |
| 5290772 | Immunosuppressant agent Described is a process for producing an immunosuppressant, "demethimmunomycin" (L-683,7411) a C-31 demethylated analog of L-683,590 under fermentation conditions utilizing the microorganism, Actinoplanacete sp, (Merck Culture Collection MA 6559) ATCC No. ... | 03/01/1994 |
| 5185365 | Insect deterrent azamcrolides The insect deterrent azamacrolide ##STR1## and other insect deterrent azamacrolides have been recovered from droplets formed at the ends of pupal hairs of the Mexican bean beetle Epilachna varivestis or synthesized from (I).... | 02/09/1993 |
| 5180718 | Acyl derivatives of oxazolorifamycins The invention relates to novel acyl derivatives of rifamycins of the formula ##STR1## and the salts thereof, in which the structural elements --A1 --A2 --, --A3 --A4 -- and --A5 --A6 -... | 01/19/1993 |
| 5095108 | Non-solvated crystalline form "A" of 3-(4-cynnamyl-1-piperazinyl)iminomethylrifamycine SV and a method of its production The non-solvated crystalline form "A" of 3-(-4-cynnamyl-1-piperazinyl)-iminomethylrifamycine SV finds application in the therapeutical practice. It represents a crystalline substance with absorption maximum of the infrared spectrum at 1644, 1585, 1340, 13... | 03/10/1992 |
| 4987139 | FK-520 microbial transformation product Described is a new immunosuppressant, L-687,795, a C-13, C-15, C-31 trisdemethylated, ring rearranged derivative of L-683,590, produced under fermentation conditions utilizing the microorganism, Actinoplanacete sp. (Merck Culture Collection MA 6559) ATCC ... | 01/22/1991 |
| 4983602 | 3'-hydroxybenzoxazinorifamycin derivative, process for preparing the same and antibacterial agent containing the same A rifamycin derivative having the formula (I): ##STR1## wherein A is a group having the formula: ##STR2## in which R1 is an alkyl group having 4 or 5 carbon atoms or an alkenyl group having 3 to 5 carbon atoms, or a group having the f... | 01/08/1991 |
| 4975372 | Microbial transformation product of L-683,590 Described is a new immunosuppressant, L-685,487, a monodemethylated rearranged derivative of L-683,590, produced under fermentation conditions utilizing the microorganism, unidentified Actinomycete (Merck Cultrue Collection MA 6474) ATCC No. 53828. The ma... | 12/04/1990 |
| 4965261 | Substituted benzoxazinorifamycin derivative and antibacterial agent containing the same A rifamycin derivative having the formula (I): ##STR1## wherein R1 is hydrogen atom, methyl group or ethyl group, R2 is an alkyl group having 1 to 4 carbon atoms, and A is a group having the formula: ##STR2## in which ... | 10/23/1990 |
| 4880789 | 2'-Substituted-4-deoxy-thiazolo(5,4-c)-rifamycin SV derivatives The present invention concerns new 2'-substituted-4-deoxy-thiazolo[5,4-c]rifamycin SV derivatives having antibacterial activity. These compounds are compounds obtained by chemical modification of thiazolo[5,4-c]rifamycin SV.... | 11/14/1989 |
| 4859661 | Alkyl-substituted benzoxazinorifamycin derivative, process for preparing the same and antibacterial agent containing the same A novel rifamycin derivative having the formula (I): ##STR1## wherein X1 is an alkyl group with 1 to 6 carbon atoms or a cycloalkyl group with 3 to 8 carbon atoms; X2 is a hydrogen atom or an alkyl group with 1 to 4 carbon atoms... | 08/22/1989 |
| 4774237 | Expellants of phytopathogenic microbes The present invention provides expellants of phytopothogenic microbes comprising rifamycins, which have excellent in prevention of disease in plants with little adverse influence to human body and environments.... | 09/27/1988 |
| 4690919 | Benzoxazinorifamycin derivative, process for preparing the same and antibacterial agent containing the same A novel rifamycin derivative having the general formula (I): ##STR1## or salts thereof, a process for preparing the same and antibacterial agents containing the same as an effective component. The rifamycin derivative of the present invention having the g... | 09/01/1987 |
| 4557866 | Process for the synthesis of pyrido-imidazo rifamycins A new process for the synthesis of pyrido-imidazo-rifamycins of formula ##STR1## wherein R is hydrogen or acetyl, R1 and R2 independently represent hydrogen, (C1-4)-alkyl, benzyloxy, mono- or di-(C1-3)-alky... | 12/10/1985 |
| 4341785 | Imidazo-rifamycin derivatives with antibacterial utility New rifamicyn derivatives of the following general formula ##STR1## wherein: A may be the structure ##STR2## --x-- is a chemical bond or nil; R is hydrogen or acetyl R1 and R2 independently represent hydrogen, (C1-4) ... | 07/27/1982 |
| 4305941 | Rifamycin XII derivatives, their preparation and anti-bacterial compositions thereof Novel rifamycin derivatives having the formula: ##STR1## wherein Y is --H or --COCH3 ; R1 and R2 may be linear or branched alkyl having from 1 to 7 carbon atoms and alkenyl having 3 or 4 carbon atoms R2 may... | 12/15/1981 |
| 4234485 | Process for preparing 4-desoxy-thiazolo[5,4-c]rifamycin derivatives Novel 4-desoxy-thiazole[5,4-c]rifamycin derivatives of formula I ##STR1## wherein R stands for a group --OR1, --NR2 R3 or --NHCOR4 wherein R1 represents alkyl, alkenyl, alkynyl, cycloalkyl, aryl ... | 11/18/1980 |
| 4226765 | Novel rifamycin compounds of high antibiotic activity Novel rifamycin compounds of high antibiotic activity. Such compounds are obtained by reacting 3-amino-4-deoxo-4-imino-rifamycin S with aldehydes.... | 10/07/1980 |
| 4217276 | Rifamycin compounds Rifamycin compounds having high antibacterial activity, consisting of powder colored from yellow to orange. Such compounds are provided by reacting 3-amino-rifamycin S with an aldehyde of formula X--CHO in the presence of a reducing agent and in an organi... | 08/12/1980 |
| 4212873 | 4-Desoxy-thiazolo[5,4-c]rifamycin derivatives and their use as antimicrobial agents Novel 4-desoxy-thiazolo[5,4-c]rifamycin derivatives of formula I ##STR1## wherein R stands for a group --OR1, --NR2 R3 or --NHCOR4 wherein R1 represents alkyl, alkenyl, alkynyl, cycloalkyl, aryl ... | 07/15/1980 |
| 4174320 | Process for the preparation of rifampicin The present invention provides a process for the preparation of rifampicin, wherein rifamycin S is reacted in an aprotic dipolar solvent with a 1,3,5-trisubstituted hexahydro-1,3,5-triazine at a temperature from 20° to 100° C. followed by reaction with ... | 11/13/1979 |
| 4169834 | Rifamycin derivatives A process for preparing 4-deoxy-thiazolo[5,4-c]rifamycin SV derivatives of the following general formula ##STR1## wherein R represents hydrogen or a straight or branched alkyl chain containing from 1 to 10 carbon atoms, R1 is selected from... | 10/02/1979 |
| 4165317 | Rifamycin compounds Rifamycin compounds having high antibacterial activity, comprising powder of yellow-orange color. Such compounds are obtained by reacting 3-aminosubstituted-4-desoxo-4-imino rifamycin S with aldehydes of formula X--CHO.... | 08/21/1979 |
