Class 544/284 - Additional nitrogen containing unsaturated hetero ring (e.g., thiazole, etc.)

Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds having, in addition to the bicyclo ring system,
No. of patents: 705
Last issue date: 01/10/2012

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Number	Title	Issue Date
RE43098	Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such ki...	01/10/2012
8071768	Alkylquinoline and alkylquinazoline kinase modulators The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula I: wherein R1, R2, R3, B, Z, G, Q and X are as defined herein, the use of such compounds as protein tyro...	12/06/2011
8058431	Fluorescent double stranded DNA binding dyes Disclosed is a fluorescent dye comprising a benzothiazolium moiety and a pyrimidinium moiety connected by a mono-methine bridge, characterized in that (i) the 2-position of the pyrimidine carries a substituent which starts with a C-atom and (ii) the 5- and 6- positi...	11/15/2011
7977480	Synthesis of paliperidone A 9-hydroxy or 9-acyloxy group can be added to a pyridopyrimidinone ring structure by a process comprising acylating a compound of formula (5) under Vilsmeier-Haack or Friedel-Crafts conditions to form a compound (6); and transforming with a peroxo-compound to obtai...	07/12/2011
7872125	Phenylalanine derivatives Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin. ...	01/18/2011
7645878	Process for preparing quinazoline Rho-kinase inhibitors and intermediates thereof A process for the preparation of various quinazoline compounds which are useful as Rho-Kinase inhibitors, and thus having utility in the treatment of hypertension and other indications. ...	01/12/2010
7488823	Cyanoguanidines and cyanoamidines as ErbB2 and EGFR inhibitors Cyanoguanidine quinazoline and cyanoamidine quinazolamine derivatives that are useful in the treatment of hyperproliferative diseases are disclosed. Methods of treating hyperproliferative diseases in mammals are also disclosed. ...	02/10/2009
7439249	Inhibitors of phosphatases The present invention relates to compounds that inhibit phosphatases, compositions thereof, and methods of using those compounds and compositions for treating diseases. ...	10/21/2008
7429597	Substituted nitrogen-containing heterobicycles, the preparation thereof and their use as pharmaceutical compositions The present invention relates to new substituted nitrogen-containing heterobicyclic compounds of general formula wherein B, X1 to X3 and R1 to R5 are defined as in claim 1,...	09/30/2008
7427681	Pyrazole compounds useful as protein kinase inhibitors This invention describes novel pyrazole compounds of formula II: wherein Z1 is nitrogen or CR8; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, whe...	09/23/2008
7417041	Imidazopyrimidines as transforming growth factor (TGF) inhibitors Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of tran...	08/26/2008
7410975	Small molecule toll-like receptor (TLR) antagonists The invention provides methods and compositions useful for modulating signaling through Toll-like receptors. The methods involve contacting a TLR-expressing cell with a small molecule having a core structure including at least two rings. Certain of the compounds are...	08/12/2008
7407946	Quinazoline compounds Quinazoline derivatives of formula (I) wherein A is 5-membered heteroaryl containing a sulphur atom and optionally containing one or more nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.	08/05/2008
7402585	Substituted quinazoline derivatives as inhibitors of aurora kinases The invention provides quinazoline derivatives of formula (I): in the preparation of a medicament for use in the inhibition of Aurora kinase and also novel quinazoline derivatives, processes for their preparation, pharamceutical compositions containing them and thei...	07/22/2008
7390815	Pyrazole compounds useful as protein kinase inhibitors This invention describes novel pyrazole compounds of formula II: wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, and R2, R2′, R...	06/24/2008
7381730	3-arylquinazoline derivatives as selective estrogen receptor beta modulators Novel quinazoline derivatives possessing activity as estrogen receptor beta (ERβ) modulators are provided which have the general formula I wherein X is O or S; A and B ar...	06/03/2008
7378422	Inhibitors of serine proteases, particularly HCV NS3-NS4A protease The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents....	05/27/2008
7378522	Quinoline, isoquinoline and phthalazine derivatives as antagonists of the gonadotropin-releasing hormone The invention relates to new quinoline, isoquinoline and phthalazine derivatives as antagonists of the gonadotropin-releasing hormone. ...	05/27/2008
7368445	Fused pyrazole derivatives as TGF-β signal transduction inhibitors for the treatment of fibrosis and neoplasms The disclosed invention is directed to compounds of the formula: Formula (I) and methods of using these compounds. ...	05/06/2008
7368453	Quinazolinone compounds with reduced bioaccumulation A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the formula IA and IB. IA and IB have the fol...	05/06/2008
7348333	Cycloalkyl derivatives as inhibitors of bone resorption and vitronectin receptor antagonists There are described cycloalkyl derivatives of the formula (I) R1—Y-A-B-D-E-F-G (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds a...	03/25/2008
7348332	(3,4-dihydro-quinazolin-2-yl)-indan-1-yl-amines The present invention relates to compounds of formula wherein R1, R2, and n are as defined herein and to pharmaceutically acceptable acid addition salts thereof.	03/25/2008
7342022	Compounds in the treatment of dementia related diseases, Alzheimer's Disease and conditions associated with glycogen synthase kinase-3 The present invention relates to new compounds of formula I wherein R1, R2, R3, n, m are defined as in claim 1, a process for their preparation and new intermediates used in the preparation thereof, pharmaceutical formulations contai...	03/11/2008
7332493	Substituted bicyclic derivatives for the treatment of abnormal cell growth The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R3, R4, R5, R11, m a...	02/19/2008
7332483	Amide derivatives The invention concerns amide derivatives of Formula (Ia) wherein X is —NHCO— or —CONH—; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-2; R2 is a group su...	02/19/2008
7329664	Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with ...	02/12/2008
7329655	Nitrogenous heterocyclic compounds The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to ...	02/12/2008
7329749	Piperazinylcarbonylquinolines and -isoquinolines Compound of the formula (I) in which R1, R2 and alk are as defined in Claim 1, are potent 5-HT2A antagonist and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkins...	02/12/2008
7329665	Quinazolinone derivative An optically active form of the quinazolinone derivatives represented by the general formula (1): [wherein Y represents a phenyl group or C2-C7 alkyl group; E represents —CH═ or nitrogen atom; and R represent...	02/12/2008
7326712	Substituted tricyclic compounds as protein kinase inhibitors Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including ...	02/05/2008
7312209	Acridone inhibitors of IMPDH enzyme Compounds having the formula (I), wherein R3 is selected from H, OH and NH2; R30 is selected from ═O and ═S; W is —C(═O)—, —S(═O)—, or —S(O)2—; or W...	12/25/2007
7312214	1, 1-disubstituted cycloalkyl derivatives as factor Xa inhibitors The present application describes 1,1-disubstituted cycloalkyl compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa. ...	12/25/2007
7304059	Substituted quinazolin-4-ylamine analogues Substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activati...	12/04/2007
7294634	Methods and compositions utilizing quinazolinones Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity ...	11/13/2007
7279481	Quinoline and quinazoline derivatives having affinity for 5HT1-type receptors Compounds of formula (I) and pharmaceutically acceptable salts thereof are provided: wherein R1, m, X, R2, n, W, p, Y, Z, R3, R4, R5 and q have the meanings ...	10/09/2007
7273936	Oxazole and thiazole compounds as transforming growth factor (TGF) inhibitors Novel oxazole and thiazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of tran...	09/25/2007
7271179	Inhibitors of JAK protein kinase The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, ...	09/18/2007
7268230	Quinazoline compounds The invention relates to compounds of the formula (I): wherein ring C is as defined herein, for example indolyl, indazolyl or azaindolyl; Z is —O—, —NH— or —S—; n is 0-5; m is 0-3; R1 and R2 are defined herein including groups: (i) ...	09/11/2007
7268142	Tetrahydroisoquinolinyl derivatives of quinazoline and isoquinoline The invention pertains to substituted quinazoline and isoquinoline compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE-10. The invention also relates to in...	09/11/2007
7265125	Neuropeptide Y antagonists Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity. ...	09/04/2007

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Class 544/284 - Additional nitrogen containing unsaturated hetero ring (e.g., thiazole, etc.)