Class 514/267 - Tricyclo ring system having 1,3-diazine as one of the cyclos

Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the 1,3-diazine is a part of a tricyclo
No. of patents: 589
Last issue date: 05/22/2012

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Number	Title	Issue Date
8183250	Potent PARP inhibitors The present invention relates to 1H-benzimidazole-4-carboxamides of formula (I), their preparation, and their use as inhibitors of the enzyme poly(ADP-ribose)polymerase for the preparation of drugs. ...	05/22/2012
8158638	Pyrazolopyrimidine derivative Problem to be Solved To provide a novel compound inhibiting the effect of HSP90, in particular a novel compound inhibiting the function of HSP90 as a chaperone protein and having antitumor activity. Solution The present invention provides a pyra...	04/17/2012
8148388	2,4 (4,6) pyrimidine derivatives The present invention is drawn to 2,4 (4,6) pyrimidine derived macrocyclcs, pharmaceutical compositions thereof, and methods of making said compounds. The compounds disclosed herein are inhibitors of EGF receptor tyrosine kinases and are useful for treating cell pro...	04/03/2012
8129398	HIV integrase inhibitors The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also enco...	03/06/2012
8063056	Anti-cancer cyclopenta []quinazonline compounds Cyclopenta[g]quinazolines of the formula (I):— wherein: A is a group OR or NR0R1 wherein R0 and R1 are each independently hydrogen C1-4	11/22/2011
8058285	Substituted pyrido [3′, 2′: 4, 5] thieno [3, 2-D] pyrimidines and pyrido [3′, 2′: 4, 5] furo [3, 2-D] pyrimidines used as inhibitors of the PDE-4 and/or the release of TNF-ALPHA The invention relates to compounds of general formula (I); 1a, 1 b, 1 c and 1 d. The invention also relates to a method for the production thereof, pharmaceutical preparations containing said compounds and/or physiologically compatible salts thereof which can be pro...	11/15/2011
8039478	Purinone derivatives as HM74A agonists The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease. ...	10/18/2011
8030321	Benzofuro- and benzothienopyrimidine modulators of the histamine Hreceptor Benzofuro- and benzothienopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H	10/04/2011
8026246	Aurora kinase inhibitors for inhibiting mitotic progression The present invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides potent inhibitors of Aurora A kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment...	09/27/2011
8022078	Pyrimidine classical cannabinoid compounds and related methods of use Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors. ...	09/20/2011
8017619	Compositions useful as inhibitors of protein kinases The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositi...	09/13/2011
7998967	Methotrexate adjuvants to reduce toxicity and methods for using the same Methods are provided for using methotrexate (MTX) in which reduced host toxicity is observed. Aspects of the methods include administering to a subject an effective amount of MTX in conjunction with a MTX toxicity-reducing adjuvant, such as a 2,2′-anhydropyrimidin...	08/16/2011
7989464	mGluR1 antagonists as therapeutic agents In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as se...	08/02/2011
7964608	Tricyclic compounds as modulators of TNF-α synthesis The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-alpha or by PDE4, including but not limited to rheumatoid arthritis....	06/21/2011
7960400	Tricyclic compounds having cytostatic and/or cytotoxic activity and methods of use thereof The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are usef...	06/14/2011
7947697	8-(3-pentylamino)-2-methyl-3-(2-chloro-4-methoxyphenyl)-6,7-dihydro-5H-cyclopenta[d] pyrazolo[1,5-a]pyrimidine methanesulfonate as a CRF antagonist 8-(3-pentylamino)-2-methyl-3-(2-chloro-4-methoxyphenyl)-6,7-dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidine methanesulfonate of the structural formula (I) has Corticotropin Releasing Factor (CRF) antagonist activity and i...	05/24/2011
7910597	Substituted quinazolines This invention relates to the discovery of 3- and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myelo...	03/22/2011
7902205	Purinone derivatives as HM74A agonists The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease. ...	03/08/2011
7863284	Anti-cancer cyclopenta[G]quinazoline compounds Cyclopenta[g]quinazolines of the formula (I): —wherein: A is a group OR or NR0R1 wherein R0 and R1 are each independently hydrogen C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 ...	01/04/2011
7863285	Purinone derivatives as HM74A agonists The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease. ...	01/04/2011
7851478	Agent for preventing and/or treating movement disorder For example, an agent for preventing and/or treating movement disorder comprising, as an active ingredient, a triazolopyrimidine derivative having an adenosine A2A receptor antagonistic action, which is represented by the following formula (I):	12/14/2010
7820684	Pharmaceutical formulations comprising salts of a protein kinase inhibitor and methods of using same The present invention relates to pharmaceutical formulations comprising the protein kinase inhibitor, MP470, and methods of using same in treating conditions involving undesirable cell proliferation, such as cancer. ...	10/26/2010
7807688	Tri-heterocyclic compounds and a pharmaceutical comprising them as an active ingredient Tri-heterocyclic compound of formula (I) wherein each of W, X and Y is carbon or nitrogen; each of U and Z is CR2, NR13, nitrogen, oxygen, sulfur etc.; A ring is carbocyclic ring, heterocyclic ring; R	10/05/2010
7807687	Pyrido[3,2-h]quinazolines and/or 5,6-dihydro derivatives thereof, a method for the production thereof and doped organic semiconductor material containing these The present invention relates to pyrido[3,2-h]quinazolines and/or 5,6-dihydro derivatives thereof, methods for their production and doped organic semiconductor material which use such quinazolines. ...	10/05/2010
7763629	Tetrahydropteridines useful as inhibitors of protein kinases The present invention relates to compounds useful as inhibitors of protein kinase, represented by Structural Formula (I): wherein the variables in Structural Formula (I) are as described herein. The invention also provides ...	07/27/2010
7759356	Arylindenopyridines and arylindenopyrimidines and related therapeutic and prophylactic methods This invention provides novel arylindenopyridines and arylindenopyrimidines of the formula: wherein R1, R2, R3, R4, and X are as defined above, and pharmaceutical compositions com...	07/20/2010
7754730	Arylindenopyridines and arylindenopyrimidines and related therapeutic and prophylactic methods This invention provides novel arylindenopyridines and arylindenopyrimidines of the formula: wherein R1, R2, R3, R4, and X are as defined above, and pharmaceutical compositions com...	07/13/2010
7750017	Heterocycles This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly hyperproliferative diseases such as cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the t...	07/06/2010
7741333	Quinazoline derivatives, their preparation, their use, and medicaments comprising them The present invention relates to a quinazoline derivative having the general formula (A): in which R1, R2, X, Y and Z are indicated in the description and the claims, the use of the compounds of the ge...	06/22/2010
7723343	Adenosine Areceptor antagonists The present invention provides compounds of the formula wherein R1 and R2 have meaning as defined herein in the specification. The compounds of formula (I) are adenosine A2A receptor antagon...	05/25/2010
7713985	Adenosine Areceptor antagonists Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein: X1 and X2 are 1-3 substituents independently selected from the group...	05/11/2010
7709492	Pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A receptor antagonists Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, furanyl, thienyl, pyridyl, pyridyl N-oxide, oxazolyl or...	05/04/2010
7705006	Anti-cancer cyclopenta[g]quinazoline compounds Cyclopenta[g]quinazolines of the formula (I): wherein: A is a group OR or NR0R1 wherein R0 and R1 are each independently hydrogen C1-4 alkyl, C1-4 alkenyl, C1-4 alkynyl, C1-4 hyd...	04/27/2010
7700609	Compositions useful as inhibitors of protein kinases The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositi...	04/20/2010
7691869	Pyrrolotriazolopyrimidine derivatives, pharmaceutical compositions containing them and methods of treating conditions and diseases mediated by the adenosine Areceptor activity The present invention provides compounds of the formula wherein R1 and R2 have meaning as defined herein in the specification. The compounds of formula (I) are adenosine A2A receptor antagon...	04/06/2010
7691868	Thiazolyl-dihydro-quinazoline Disclosed are thiazolyl-dihydro-quinazolines of general formula (I) wherein the groups R1 to R4 have the meanings given in the claims and specification, the isomers thereof, and processes for preparing...	04/06/2010
7615560	Thienopyrimidines as cooling agents Use of a compound of formula (I) where R1 is a C4-6 alkylene linkage optionally substituted by a C1-4alkyl group; R2 is ═NH, —NH2 or —OH; R3 is C1-5 alkyl optionally terminated by a h...	11/10/2009
7598259	mGluR1 antagonists as therapeutic agents In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as se...	10/06/2009
7579356	Thia-tetraazaacenaphthylene kinase inhibitors The present invention is directed to novel thia-tetraazaacenaphthylene compounds of Formula (I): and pharmaceutically acceptable forms thereof and their synthesis and use as inhibitors of ATP-protein kinase interactions.	08/25/2009
7576091	Thiazolo-, oxazalo and imidazolo-quinazoline compounds capable of inhibiting protein kinases A compound of formula 1, or a pharmaceutically acceptable salt thereof, wherein: X is S, O, or NH; “a” is a single bond; or “a” is a double bond and one of R3 and R4, and one of R5 a...	08/18/2009

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Class 514/267 - Tricyclo ring system having 1,3-diazine as one of the cyclos