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| Number | Title | Issue Date |
| 8178670 | Method of synthesizing tetrahydrobiopterin The present disclosure provides a method that efficiently produces (6R)-tetrahydrobiopterin of Formula I in high yield and purity. The method includes the step of hydrolyzing diacetylbiopterin to biopterin under basic conditions in a biphasic mixture comprising an o... | 05/15/2012 |
| 8044200 | Synthesis and purification of pteroic acid and conjugates thereof Methods for purifying pteroic acid, analogs of pteroic acid, and derivatives of pteroic acid are described. Methods for synthesizing and purifying conjugates of vitamins, including FITC conjugates of folic acid, folic acid analogs, and derivatives of folic acid and ... | 10/25/2011 |
| 7816525 | Process for the preparation of optically pure tetrahydropterins and derivatives, and specifically of optically pure tetrahydrofolic acid and derivatives thereof, by stereospecific hydrogenation Process for the preparation of tetrahydropterin and tetrahydropterin derivatives by hydrogenating pterin and pterin derivatives with hydrogen in the presence of a hydrogenating catalyst, in which the hydrogenation is carried out in a polar reaction medium and metal ... | 10/19/2010 |
| 7807831 | Dihydropteridione derivatives, process for their manufacture and their use as medicament Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes f... | 10/05/2010 |
| 7786299 | Methods for treating diseases or conditions using dihydropteridinone compounds Disclosed are new dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, intermediates and processes for... | 08/31/2010 |
| 7728134 | Hydrates and polymorphs of 4[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament Disclosed are hydrates and polymorphs of 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]Amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide: processes for preparing them and their use as pha... | 06/01/2010 |
| 7723517 | Dihydropteridione derivatives, process for their manufacture and their use as medicament Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes f... | 05/25/2010 |
| 7629460 | Dihydropteridione derivatives, process for their manufacture and their use as medicament Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes f... | 12/08/2009 |
| 7501513 | Immunosuppressive effects of pteridine derivatives This invention relates to a group of trisubstituted and tetrasubstituted pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydro-derivatives and enantiomers, possessing unexpectedly desirable pharmaceutical propert... | 03/10/2009 |
| 7439358 | Specific salt, anhydrous and crystalline form of a dihydropteridione derivative The present invention relates to a specific salt of a dihydropteridione derivative, namely the trihydrochloride salt of the compound N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pt... | 10/21/2008 |
| 7423038 | Compounds and compositions as protein kinase inhibitors The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or d... | 09/09/2008 |
| 7414053 | Dihydropteridione derivatives, process for their manufacture and their use as medicament Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes f... | 08/19/2008 |
| 7371753 | Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions Disclosed are new dihydropteridinones of general formula (I) wherein the groups R1 to R5, Ra to Rc, W, Q1 and Q2 have the meanings given in the claims and sp... | 05/13/2008 |
| 7332491 | Dihydropteridione derivatives, process for their manufacture and their use as medicament Disclosed are new dihydropteridinones of general formula (I) whereby the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and specificat... | 02/19/2008 |
| 7276506 | Immunosuppressive effects of pteridine derivatives This invention relates to a group of trisubstituted and tetrasubstituted pteridine derivatives, having the formula: wherein X represents an oxygen atom or a group with the formula NZ and wherein: R1 C | 10/02/2007 |
| 7241889 | 6-formyl-tetrahydropteridines, process for their manufacture and use thereof as medicaments Disclosed are 6-formyl-tetrahydropteridines of the formula (I) wherein the groups R1 to R6 have the meanings given in the claims and specification, the isomers thereof, methods of preparing ... | 07/10/2007 |
| 7232824 | Quinazoline derivatives as medicaments Quinazoline derivatives have the formula: or the pharmaceutically acceptable salts thereof; wherein each of Z5, Z6, Z7 and Z8 ... | 06/19/2007 |
| 7193082 | (6S)-5,6,7,8-tetrahydrofolic acid production process New process for the production of (6S)-5,6,7,8-tetrahydrofolic acid or derivatives thereof starting from the corresponding (6S, 6R) racemic mixture. The procedure comprises in the steps of adding an organic acid to a non-alkaline suspension of (6S,6R)-5,6,7,8-tetray... | 03/20/2007 |
| 7169778 | Pteridinones as kinase inhibitors Disclosed are compounds of Formulae (Ia), (Ib), (Ic), (Id) wherein: W is NH, S, SO, or SO2; R2 is (un)substituted aryl, (un)substituted heteroaryl, or (un)substituted carbocycle or heterocycle; Q is hydrogen or lower alkyl; R4 and R | 01/30/2007 |
| 7126001 | Class of cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof The present invention provides the compound having the formula: wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperid... | 10/24/2006 |
| 7115739 | Triazole compounds useful as protein kinase inhibitors This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 | 10/03/2006 |
| 7098216 | Thiazolopyrimidines useful as TNFα inhibitors The invention provides derivatives of thiazolo[4,5-d1]pyrimidine and their use as inhibitors of proinflammatory cytokines. ... | 08/29/2006 |
| 7067659 | Reactive oxygen generating enzyme inhibitor with nitric oxide bioactivity and uses thereof A reactive oxygen generating enzyme inhibitor with NO donor bioactivity, e.g., nitrated allopurinol, e.g., 1,5-bis(3-nitrooxypropyyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one is useful to treat heart failure, stable angina, ischemic disorder, ischemic reperfus... | 06/27/2006 |
| 6949643 | Thiazolopytimidines and their use as modulators of chemokine receptor activity The invention provides certain thiazolopyrimidine compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof: in which: A is a group of formula (a) or (b): processes and intermediates used in their preparation, pharmaceutical compositions cont... | 09/27/2005 |
| 6930101 | Thiazolopyrimidines useful as TNFα inhibitors The invention provides derivatives of thiazolo[4,5-dl]pyrimidine and their use as inhibitors of proinflammatory cytokines. ... | 08/16/2005 |
| 6906070 | Guanidine mimics as factor Xa inhibitors The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are use... | 06/14/2005 |
| 6875868 | Pteridine compounds for the treatment of psoriasis The invention provides pteridine compounds of formula (I), processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy. Formula (I) in which A is a group of formula (a) or (b). ... | 04/05/2005 |
| 6861422 | Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions The present invention relates to new dihydropteridinones of general formula (I): wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, proces... | 03/01/2005 |
| 6858731 | Process for the preparation of pure stereoisomers of tetrahydrofolic acid esters salts and tetrahydrofolic acid by fractionated crystallization of tetrahydrofolic acid esters salts A process for preparing and concentrating (6S,αS) or (6S,αR) tetrahydrofolic acid ester salts and (6S,αS) or (6S,αR) tetrahydrofolic acid, characterized by preparing or dissolving equimolar or concentrated mixtures of diastereomers of addition salts of tetrahydr... | 02/22/2005 |
| 6858612 | Use of tetrahydropteridine derivatives as no synthase inhibitors The present invention relates to the use of pteridine derivatives of the formula I in which X is O or NH and R4, for example, is hydrogen, phenyl or the radical R4a—CH2— and R4... | 02/22/2005 |
| 6849628 | Optically active compounds The present invention relates to the preparation of substantially pure diastereoisomers of derivatives of tetrahydrofolate and the use of such diastereoisomers. More particularly the present invention provides a process for the preparation of a desired substantially... | 02/01/2005 |
| 6787650 | Urea compounds, process for producing the same and use thereof A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substitu... | 09/07/2004 |
| 6784174 | Pyridine and pyrimidine derivatives and their use as inhibitors of cytokine mediated disease This invention concerns a bicyclic compound of Formula (I), wherein: G is N, CH or C(CN); ring X is a 5- or 6-membered fused heteroaryl ring which contains 1, 2, or 3 heteroatoms selected from oxygen, sulphur and nitrogen; m is 0-2; R1 is a group such as ... | 08/31/2004 |
| 6747016 | Substituted purine derivatives as inhibitors of cell adhesion The present invention relates to compounds of formula (I), in which B, D, E, G, X, Y, Z, R1, R2 and s have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable... | 06/08/2004 |
| 6740654 | Squaric acid derivatives Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L2 is a covalent bond or an atom or group —O—, —Sâ€... | 05/25/2004 |
| 6720304 | Conjugate comprising a folic acid antagonist and a carrier The invention relates to conjugates comprising a D-enantiomer of a folic acid antagonist and a carrier. Furthermore, the invention relates to the production of such conjugates as well as their use. ... | 04/13/2004 |
| 6596721 | Stable crystalline (6R) -tetrahydrofolic acid Pure and extremely stable crystalline (6R)-tetrahydrofolic acids, absolutely inert even when exposed to air and elevated temperature without stabilizers being added, are prepared by a crystallization process at a pH of ࣙ2.... | 07/22/2003 |
| 6521620 | Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family Described are heterocyclic pyrimidine derivatives and a method of inhibiting epidermal growth factor by treating, with an effective inhibiting amount, a mammal, in need thereof, a compound of the formula: ##STR1## where: at least two of A-E are nitrogen, ... | 02/18/2003 |
| 6511990 | Class of cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof The present invention provides the compound having the formula: ##STR1## wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkylox... | 01/28/2003 |
| 6500829 | Substantially pure diastereoisomers of tetrahydrofolate derivatives The present invention related to the preparation of substantially pure diastereoisomers of derivatives of tetrahydrofolate and the use of such diastereoisomers. More particularly the present invention provides a process for the preparation of a desired su... | 12/31/2002 |
