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| Number | Title | Issue Date |
| 7179907 | Antibiotic compounds The present invention provides methods for identifying (3-amino-2-oxo-azetidin-1-yl) acetic acid derivatives with anti-PBP2a activity. The method involves the selection of RNA biocatalysts that promote the formation of (3-amino-2-oxo-azetidin-1-yl) acetic acid deriv... | 02/20/2007 |
| 7129350 | Coupling process and intermediates useful for preparing cephalosporins A process for the preparation of 3-cyclic-ether-substituted cephalosporins of formula I wherein the group CO2R1 is a carboxylic acid or a carboxylate salt and R2 has the formula: ... | 10/31/2006 |
| 7045515 | β-lactam compounds process for reproducing the same and serum cholesterol-lowering agents containing the same Novel β-lactam compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof which are useful as serum cholesterol-lowering agents: (I) wherein A1, A3 and ... | 05/16/2006 |
| 6900312 | Thiazole-substituted β-lactams The present discovery consists in new thiazole-substituted β-lactams of general formula (I), as well as the method for their preparation. R1, R2, R3, R4, R5, R6, R7, and R8 are, independently from each other, a hydrogen... | 05/31/2005 |
| 6730782 | Carbamoyl substituted β-lactams Taxane derivatives having an amino substituted C13 side chain. ... | 05/04/2004 |
| 6569847 | Substituted azetidin-2-ones as cysteine protease inhibitors This invention relates to substituted azetidin-2-ones and to pharmaceutical compositions containing such compounds. Their use in medicine as inhibitors of cysteine proteases, particularly the cathepsins is also described. The invention includes a compound... | 05/27/2003 |
| 6562962 | Preparation of substituted isoserine esters using metal alkoxides and ଲ-lactams A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal alkoxide is reacted with a ଲ-lactam.... | 05/13/2003 |
| 6407228 | Method for the preparation of ଲ-lactam compound A simple and efficient method is proposed for the preparation of a ଲ-lactam compound such as 1-phenyl-4-ethoxy-2-azetidinone which can be produced by mixing an isocyanate compound such as phenyl isocyanate and a vinyl ether compound such as ethyl vi... | 06/18/2002 |
| 6310201 | ଲ-lactams, methods for the preparation of taxanes, and sidechain-bearing taxanes Novel ଲ-lactams finding utility as intermediates in the preparation of sidechain-bearing taxes such as tall and tall derivatives. The present invention also relates to novel methods of coupling ଲ-lactams to form such sidechain-bearing taxes, a... | 10/30/2001 |
| 6239125 | Azetidinone derivatives for the treatment of HCMV infections A compound of formula 1: ##STR1## wherein Y is S or O; R1 is C1-6 alkyl; (C0-6 alkyl)aryl; (C0-6 alkyl)Het; or R1 is an amino acid analog or dipeptide analog of the formula: ##STR2## wherein R2 ... | 05/29/2001 |
| 6221860 | Beta-lactam inhibitors of CoA-IT This invention relates to methods for treating diseases or disorders mediated by lipid inflammatory mediators, arachidonic acid, its metabolites and/or platelet activating factor (PAF), which method comprises administration to a mammal in need thereof of ... | 04/24/2001 |
| 6194569 | Efficient process for the preparation of [S-(R,S)]-N-[1,3-benzodioxol-5-yl)butyl]-3,3-diethyl-2[4-[4-methyl-1-piper azinyl)carbonyl]phenoxy]-4-oxo-1-azetidine carboxamide, a human leukocyte elastase inhibitor Processes for the preparation of [S-(R,S)]-N-[1,3-benzodioxol-5-yl)butyl]-3,3-diethyl-2[4-[4-methyl-1-piper azinyl)carbonyl]phenoxy]-4-oxo-l-azetidine carboxamide, a useful inhibitor of human leukocyte elastase (HLE), are described. The process including ... | 02/27/2001 |
| 6187916 | Process for the preparation of taxane derivatives and ଲ-lactam intermediates therefor A process for the preparation of a taxane derivative of the formula ##STR1## in which R2 represents an RO--, RS-- or RR'N-- in which R represents an unsubstituted or substituted straight chain or branched alkyl, alkenyl or alkynyl, or cycloalky... | 02/13/2001 |
| 6071899 | Azetidinone derivatives for the treatment of atherosclerosis Azetidinone derivatives of formula (I) in which R1 and R2, which may be the same or different, is each selected from hydrogen or C.sub.(1-8) alkyl; R3 is C.sub.(1-8) alkyl or C.sub.(3-8) cycloalkyl each of which may be opt... | 06/06/2000 |
| 6008347 | N-substituted 2-azetidinones The present invention provides novel cis-N-iminomethyl-3,4-disubstituted-2-azetidinones, and their use in the preparation of N-acyl-2-azetidinones, intermediates in the semi-synthesis of taxol and taxol derivatives.... | 12/28/1999 |
| 5998612 | Antibiotic synthesis A method of preparing intermediates for carbapenem antibiotics characterized by treating a N-deprotected acetoxy conpound of the formula: ##STR1## in the presence of a Lewis acid or a silylating agent to yeild an intermediate; and cyclizing the inter... | 12/07/1999 |
| 5990102 | Substituted azetidin-2-ones for treatment of atherosclerosis Compounds of formula (I) in which R1 and R2, which may be the same or different, is each selected from hydrogen, halogen or C.sub.(1-8) alkyl; R3 is aryl or aryl C.sub.(1-4) alkyl which may be optionally substituted; X is ... | 11/23/1999 |
| 5952321 | Substituted azetidinones as anti-inflammatory and antidegenerative agents New substituted azetidinones of the general Formula (I) which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described, wherein n is... | 09/14/1999 |
| 5916887 | 4-substituted-3-(2-amino-2-cycloalkyl methyl)-acetamido azetidin-2-one derivatives as cysteine proteinase regulators In accordance with the present invention, there are provided 4-substituted-3-(2-amino-2-cycloalkyl methyl)-acetamido azetidin-2-one derivatives of the formula: ##STR1## wherein n is 1, 2 or 3; in which R1, R2 and R3 a... | 06/29/1999 |
| 5866691 | Lactam nucleic acids Novel ଲ-lactam monomers bearing various functional groups are prepared. The novel ଲ-lactam monomers can be joined into oligomeric compounds such as via preferred phosphate linkages including phosphodiester and phosphorothioate linkages. Useful... | 02/02/1999 |
| 5843939 | Derivatives of 3-bromo- and 3,3-dibromo-4-oxo-1-azetidines, processes for the preparation thereof and their use 3-Bromo- and 3,3-dibromo-4-oxo-1-azetidines of the formula I ##STR1## wherein R1 is hydrogen or bromo, R2 is hydrogen or bromo, R3 is hydrogen, ##STR2## wherein R4 is hydrogen, methyl, benzyl or some other ... | 12/01/1998 |
| 5808056 | Process for preparing substituted azetidinones The present invention relates to the process for the preparation of the substituted azetidinone having the formula: ##STR1## comprising a convergent synthesis wherein the azetidinone portion of the molecule is coupled to the lower benzodioxole portio... | 09/15/1998 |
| 5728827 | Process for the synthesis of azetidinones This invention provides a process for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, particularly for azetidinones substituted in the C-3 and C-4 positions and optionally substituted at the rin... | 03/17/1998 |
| 5688785 | Substituted azetidinone compounds useful as hypocholesterolemic agents Substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar1 is aryl or R3 -substituted aryl; Ar2 is aryl or R4 -substituted aryl; R... | 11/18/1997 |
| 5633246 | Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents Sulfur-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar1 is aryl, R10 -substituted aryl or heteroaryl; Ar2 is aryl or R4 -subs... | 05/27/1997 |
| 5624920 | Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents Sulfur-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar1 is aryl or R10 -substituted aryl; Ar2 is aryl or R4 -substituted aryl... | 04/29/1997 |
| 5591737 | Substituted azetidinones as anti-inflammatory and antidegenerative agents New substituted azetidinones of the general Formula (I) which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described. ##STR1## wherein R4 is (a) ##STR2## or... | 01/07/1997 |
| 5585373 | 3-(7'-oxo-1'-aza-4'-oxabicyclo[3.2.0]-hept-3'-YL)propionic acid derivative as antitumor agent A derivative of 3-(7'-oxo-1'-aza-4'-oxabicyclo[3.2.0 ]hept-3'-yl)propionic acid represented by the formula ##STR1## wherein R1 is a hydrogen atom, a lower alkyl group optionally having one or more cycloalkyl groups, a lower acyl group, a b... | 12/17/1996 |
| 5580976 | Preparation of ଲ-lactam compounds, and intermediates therefor A process for preparing a ଲ-lactam compound of the formula (I): ##STR1## which comprises cyclization of an azetidinone derivative of the formula: ##STR2## is provided in which R1 is hydrogen, alkyl which is optionally substitute... | 12/03/1996 |
| 5574156 | ଲ-lactams used in preparing taxol A ଲ-lactam of the formula: ##STR1## wherein R1 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; R2 is hydrogen, alkyl, acyl, acetal, ethoxyethyl, or other hydroxyl protecting group; and R3 is aryl, substit... | 11/12/1996 |
| 5561227 | Process for the stereospecific synthesis of azetidinones This invention provides an improved process for producing azetidinones. More particularly, this invention provides the steps of producing an azetidinone represented by the formula I ##STR1## from a carboxylic acid R2 --D--CH2 CO... | 10/01/1996 |
| 5554746 | Lactam nucleic acids Novel ଲ-lactam monomers bearing various functional groups are prepared. The novel ଲ-lactam monomers can be joined into oligomeric compounds such as via preferred phosphate linkages including phosphodiester and phosphorothioate linkages. Useful... | 09/10/1996 |
| 5539103 | ଲ-lactams as taxol intermediates N-acylated ଲ-lactam compounds which are reacted with a metal alkoxide for preparing N-acyl, N-sulfonyl and phosphoryl substituted isoserine esters.... | 07/23/1996 |
| 5461045 | Fused benzeneoxyacetic acid derivatives A fused benzeneoxyacetic acid derivative of the formula: ##STR1## wherein ##STR2## is (i) ##STR3## (ii) ##STR4## (iii) ##STR5## or (iv) ##STR6## A is (i) ##STR7## or (ii) ##STR8## R1 | 10/24/1995 |
| 5453502 | 1,3,4 substituted and bicyclic derivatives of 2-azetidinones and processes for preparation thereof The invention provides 1,3,4 substituted and bicyclic derivatives of 2-azetidinones and processes therefor. These compounds are valuable intermediates useful in the preparation of 1-carba(dethia)cephalosporin antibiotics.... | 09/26/1995 |
| 5412092 | N-substituted 2-azetidinones Novel cis compound having the formula: ##STR1## wherein R1 is alkyl, haloalkyl, cycloalkyl, aryl or a carbohydrate derivative; X is O, N, S, C(O)O or a direct bond; and R2 is aryl, substituted aryl or heteroaryl are useful in th... | 05/02/1995 |
| 5348953 | Substituted azetidinones as anti-inflammatory and antidegenerative agents New substituted azetidinones of the general formula (I) which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described. ##STR1##... | 09/20/1994 |
| 5310899 | Process for the preparation of chiral 4-aryloxyazetidinones A process for preparing a single enantiomer of a 4-aryloxyazetidin-2-one derivative in optically pure form comprises reacting a hindered vinyl ester with chlorosulphonyl isocyanate; displacing the hindered acyloxy group with a phenolic derivative containi... | 05/10/1994 |
| 5250677 | Azetidin-2-one derivatives as serine protease inhibitors The present invention relates to new 3-guanidinoalkyl-2-azetidinones of the formula ##STR1## wherein: U and W can be the same or different and are selected from the group consisting of hydrogen and an amino protecting group; n is 1 to 3; X is a membe... | 10/05/1993 |
| 5250676 | Process for the preparation of 3-substituted-2-azetidinones Provided is a process for diastereoselectively preparing compounds of the formula ##STR1## which includes the step of subjecting a compound of the formula ##STR2## to a salt whose anion is a nucleophilic base whose conjugate acid has a pKa ... | 10/05/1993 |
