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| Number | Title | Issue Date |
| 7202370 | Semi-synthesis of taxane intermediates from 9-dihydro-13-acetylbaccatin III A method is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel from 9-dihydro-13-acetylbaccatin III. The preparation of a suitably protected baccatin III backbone from 9-dihydro-13-acetylbaccatin III, and th... | 04/10/2007 |
| 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 |
| 6890921 | Arylsubstituted piperazines useful in the treatment of benign prostatic hyperplasia This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibi... | 05/10/2005 |
| 6730782 | Carbamoyl substituted β-lactams Taxane derivatives having an amino substituted C13 side chain. ... | 05/04/2004 |
| 6602864 | Sulfonic acid or sulfonylamino N-(heteroaralkyl)-azaheterocyclylamide compounds The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibit... | 08/05/2003 |
| 6544976 | Neurotrophic 2-azetidinecarboxylic acid derivatives, and related compositions and methods This invention provides compounds having the following general structure: ##STR1## This invention also provides pharmaceutical compositions comprising same and methods of using these compositions to treat and prevent disorders characterized by neuronal da... | 04/08/2003 |
| 6403789 | Method of halogenating hydroxyl group A halogenating agent of the formula (1) and a method of halogenating hydroxyl group ##STR1## wherein R1 and R2 are the same or different and are each ethyl, propyl, isopropyl, butyl, isobutyl or allyl; X is chlorine atom or bromine ... | 06/11/2002 |
| 6395895 | Butenyl substituted ଲ-lactams Taxane derivatives having a 3' butenyl substituted C13 side chain.... | 05/28/2002 |
| 6335324 | Beta lactam compounds and their use as inhibitors of tryptase Compounds of the formulas: ##STR1## are disclosed. These compounds inhibit tryptase as well as other enzyme systems or are selective tryptase inhibitors and are useful as antiinflammatory agents particularly in the treatment of chronic asthma.... | 01/01/2002 |
| 6281227 | Sulfonic acid sulfonylamino n-(heteroaralkyl)-azaheterocyclylamide compounds The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibit... | 08/28/2001 |
| 6225463 | Synthesis of new ଲ-lactams The object of the present invention is the development of new chiral auxiliaries for improved ଲ-lactam formation that control both the diastereoselectivity of ଲ-lactam formation and which can be removed without destruction of the sensitive aze... | 05/01/2001 |
| 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 |
| 6214841 | Antithrombotic compound This application relates to a novel compound of formula (I) (or a pharmaceutically acceptable salt thereof) as defined herein, processes and Intermediates for its preparation, pharmaceutical formulations comprising the novel compound of formula (I), and t... | 04/10/2001 |
| 6194567 | Halogenating agent and process for halogenating hydroxyl group A halogenating agent of the formula (1) and a method of halogenating hydroxyl group ##STR1## wherein R1 and R2 are the same or different and are each ethyl, propyl, isopropyl, butyl, isobutyl or allyl; X is chlorine atom or bromine ... | 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 |
| 6174879 | Aminocyclohexylesters and uses thereof Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and com... | 01/16/2001 |
| 6071915 | Arylsubstituted piperazines useful in the treatment of benign prostatic hyperplasia This invention relates to a series of arylsubstituted piperazines, of Formula I ##STR1## pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &... | 06/06/2000 |
| 6054579 | Synthesis of substituted lactams The invention relates to an efficient and facile method for the preparation of substituted lactams, as described herein. The method comprises reacting a difunctional component containing an activated carbon, an amine capable of forming an imine with the a... | 04/25/2000 |
| 6051678 | Copolymers containing N-vinyllactam derivatives, preparation methods thereof and photoresists therefrom Copolymers containing N-vinyllactam derivatives protected at 3-position are provided and represented by the following formula. The copolymers are used as a photoresist material suitable for deep uv process so that high sensitivity and resolution can be ob... | 04/18/2000 |
| 6013791 | Process for the preparation of 4-(formylthio)-azetidin-2-one derivatives and penem derivatives A process for the preparation of a compound of formula (IVA) which process comprises subjecting a compound of formula (V), where R is an ester-forming group or carboxy-protecting group, and X and Y are hydrogen or halogen provided that at least one of X o... | 01/11/2000 |
| 5892036 | Process for the preparation of 2-bromo- and 2-nitroxy derivatives of 3-bromo- and 3,3-dibromo-4-oxo-azetidines The invention relates to novel 2-bromo- and 2-nitroxy derivatives of 3-,bromo- and 3-dibromo-4-oxo-azetidines, to processes for the preparation thereof and to the use thereof. According to the invention 2-bromo- and 2-nitroxy derivatives of 3-bromo- and 3... | 04/06/1999 |
| 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 |
| 5770729 | Ozonide reducing agent The present invention provides an ozonide reducing agent for use in the ozonolysis reaction of an organic compound, the ozonide reducing agent finding wide applications, and being safe and inexpensive from a commercial viewpoint and easy to treat for disp... | 06/23/1998 |
| 5760219 | Pyridyl substituted B-lactam compounds Pyridyl substituted ଲ-lactam compounds used in preparing taxane derivatives having a 3' pyridyl substituted C13 side chain.... | 06/02/1998 |
| 5750680 | N-vinyllactam derivatives and polymer thereof N-vinyllactam derivatives protected at the 3-position are provided and represented by the following formula (I). These are polymerized into homo- and copolymers for use in microlithography of semiconductor manufacture. The polymers are used as a photoresi... | 05/12/1998 |
| 5691356 | Disubstituted heterocyclic thrombin inhibitors Disubstituted heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein G is ##STR2## wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; p is 0, 1 or 2, Q is a single bond or ##STR3## and Z... | 11/25/1997 |
| 5670638 | 2-bromo- and 2-nitroxy derivatives of 3-bromo- and 3,3-dibromo-4-oxo-azetidines, and preparation The azetidines of the present invention have the formula I ##STR1## wherein R1 is hydrogen or bromine, R2 is hydrogen or bromine, wherein at least one of R1 or R2 is bromine, R3 is hydrogen; Me2 | 09/23/1997 |
| 5583146 | Heterocyclic thrombin inhibitors Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R1, R2, R3, G, Gx, R6', Ra, Xa, R6, Rb, R3, p, Q, A and R4 are as defined... | 12/10/1996 |
| 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 |
| 5561146 | Modified guanidino and amidino thrombin inhibitors Thrombin inhibitors are provided which have the formula ##STR1## wherein Z is a thrombin inhibitor substructure containing distal and proximal binding site residues; and R1 is cyano, hydroxyl, alkoxy, amino, aminoalkyl or nitro.... | 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 |
| 5475011 | Anti-tumor compounds, pharmaceutical compositions, methods for preparation thereof and for treatment The present invention is directed to novel taxanes useful as chemotherapeutic agents or their precursors. Processes for preparing the novel taxanes include coupling reactions, in the presence of a base, of baccatin of formula (III) or (IV) ##STR1## ... | 12/12/1995 |
| 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 |
| 5423998 | Peroxy carboxylic amino-derivatives Amino-derivative (poly)peroxycarboxylic acids which have the formula: ##STR1## wherein the symbols have the following meanings: R, R1, and R2, which may be equal to or different from one another, represent hydrogen atoms, alkyl ... | 06/13/1995 |
| 5314886 | N-substituted lactams useful as cholecystokinin antagonists This invention relates to novel N-substituted lactams having the following formula ##STR1## useful in the treatment and prevention of Cholecystokinin (CCK) related disorders of the gastrointestinal, central nervous and appetite regulatory system... | 05/24/1994 |
| 5300638 | Asymmetric synthesis of taxol side chain The present invention relates to a process for the preparation of (3R, 4S)-3-hydroxy-4-phenyl-2-azetidinone derivatives which are useful intermediates in the synthesis of taxol from baccatin III, said process comprises reacting an acyloxyacetyl halide wit... | 04/05/1994 |
| 5175315 | Method for preparation of taxol using ଲ-lactam 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... | 12/29/1992 |
| 4975441 | Lactams, their synthesis and use in cosmetic compositions A composition suitable for topical application to mammalian skin or hair for inducing, maintaining or increasing hair growth comprises: (i) a chemical inhibitor of glycosidase activity chosen from lactams having the structure: ##STR1## where A1... | 12/04/1990 |
