Class 544/262 - The other cyclo in the bicyclo ring system is five-membered

Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein a five-membered ring is the other cyclo
No. of patents: 237
Last issue date: 10/21/2008

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Number	Title	Issue Date
7439240	Purine-or pyrrolol[2,3-d]pyrimidine-2-carbonitiles for treating diseases associated with cysteine protease activity The present invention therefore provides a compound of formula (I) and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases ...	10/21/2008
7439246	Fused heterocyclic kinase inhibitors In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful...	10/21/2008
7439345	Supramolecular pairing system, its preparation and use The invention relates to conjugates including at least one linker, a biomolecule coupled to the linker, and cyclohexane derivatives of the following formula: and oligomers thereof. ...	10/21/2008
7435731	Substituted pyrazolo[3,4-d]pyrimadines and methods of using the same Compounds of the formula Ia or Ib: wherein A, B, X, Y, Z, W, k, R1, R2, R3, R4 and R5 are those defined herein, and compositions comprising the same. The present invent...	10/14/2008
7425630	Processes for preparing pyrazolo[3,4-d]pyrimidine ethers The present invention relates to processes for preparing pyrazolo[3,4-d]pyrimidine ether compounds that are modulators of glucose metabolism and therefore useful in the treatment of metabolic disorders such as diabetes and obesity. ...	09/16/2008
7407962	Heteroaryl compounds useful as inhibitors or protein kinases The present invention provides compounds that are inhibitors of protein kinase, particularly inhibitors of ERK2, GSK3, PKA, CDK2 protein kinases, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmac...	08/05/2008
7405220	Pyrazolopyrimidines Novel pyrazolopyrimidines of formula (I): are discussed. These pyrazolopyrimidines are capable of inhibiting the activity of cyclin-dependent kinases, most particularly cyclin-dependent kinase 1 (Cdk1), cyclin-dependent kin...	07/29/2008
7384952	Pyrazolopyrimidine compound and a process for preparing the same The present invention provides a novel pyrazolopyrimidine compound of the formula [I]: wherein R′ is (A) a substituted aryl group, (B) an optionally substituted nitrogen-containing aliphatic heteromonocyclic group, (C) a substituted cyclo-lower alkyl group, (D) an...	06/10/2008
RE40332	Fungicidal trifluoromethylalkylamino-triazolopyrimidines The novel compounds of formula I: wherein (R1, R2, Hal and L1 through L5 are defined in the specification) show selective fungicidal activity. The new compounds may be processed with ca...	05/20/2008
7351826	Aryl acid pyrimidinyl methyl amides, pyridazinyl methyl amides and related compounds The invention provides compounds of Formula (I) that bind to GABAA receptors. In the above formula, variables are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly...	04/01/2008
7339054	Process for preparing branched ribonucleosides from 1,2-anhydroribofuranose intermediates A process is provided for the preparation of branched-chain ribonucleosides of formula (I): from the 1,2-anhydroderivatives of formula (II). wherein PG is a hydroxyl protecting gr...	03/04/2008
7332497	Pyrazolopyrimidines as therapeutic agents The present invention provides compounds of Formula I, including pharmaceutically acceptable salts and/or prodrugs thereof, where G, Ra, R2, and R3 are defined as described herein...	02/19/2008
7314871	2-phenyl substituted imidazotriazinones as phosphodiesterase inhibitors, for treatment of hypertension The application claims a method for treating hypertension by administering an effective amount of a compound of the formula (I) wherein the variable groups are as defined in the specification and claims. These 2-...	01/01/2008
7291640	Substituted triazole derivatives as oxytocin antagonists The present invention relates to a class of substituted 1,2,4-triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety ...	11/06/2007
7285558	Pyrazolo[3,4-d]pyrimidines inhibiting infections Compounds having the general formula and pharmaceutical compositions containing them, and their use in the treatment or prophylaxis of H. pylori infection. ...	10/23/2007
7268141	Xanthine phosphodiesterase V inhibitors A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders:	09/11/2007
7268128	1,3,5-trisubstituted-5-phenyl and 5-pyridyl pyrazolopyrimidinone derivatives having PDE7 inhibiting action Pyrazolopyrimidinone derivatives expressed by the following general formula (IA) or (IB): where the symbols are as disclosed in the specification, are provided as desired compounds. These compounds selectively in...	09/11/2007
7268133	Cannabinoid receptor ligands and uses thereof Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein ...	09/11/2007
7262192	Substituted pyrazolo[4,3-d]pyrimidines and their use as PDE-5 inhibitors The present invention comprises a class of 5,7-diaminopyrazolo[4,3-d]pyrimidine compounds. These compounds are useful as phosphodiesterase type 5 inhibitors. The present invention further comprises compositions containing the compounds use of the compounds and compo...	08/28/2007
7259157	N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain. ...	08/21/2007
7259165	Heterocyclyl-3-sulfonylazaindole or-azaindazole derivatives as 5-hydroxytryptamine-6 ligands The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor. ...	08/21/2007
7230100	Stereoselective method for the preparation of nucleosides A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A): wherein R1 is a pyrimidine base or a pharmaceutically acceptable derivative thereof and Q is oxygen, c...	06/12/2007
7217710	Substituted pyrazolopyrimidines Pyrazolo-pyrimidine derivatives are described herein. The described invention also includes methods of making such derivatives as well as methods of using the same in the treatment of diseases. ...	05/15/2007
7211668	PNA monomer and precursor This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers:	05/01/2007
7176311	Process for preparing pharmaceutically active compounds A process for the preparation of Compounds of the formula (1): wherein R1, R2, R4 and R13 are as defined or a pharmaceutically or veterinarily acceptable salt or polymo...	02/13/2007
7173039	Protein kinase inhibitors Disclosed are compounds which inhibit or modulate the activity of protein kinases and pharmaceutical compositions containing such compounds. The disclosed compound contain two or more ligand moieties covalently linked together by one or more linking groups. Such com...	02/06/2007
7148350	Compounds in the form of homodimeric or heterodimeric pro-drugs; process for obtaining these pro-drugs and their acceptable pharmaceutical salts and use of compounds in the treatment of phosphodiesterases-mediated diseases or dysfunction The present invention describes new homo or heterodimer prodrugs wherein both active monomeric units are compounds of the formula: where R1 and R2 are each independently —H, —C1–C...	12/12/2006
7148228	Pyrazolopyrimidines and related analogs as HSP90-inhibitors A compound represented by Formula I, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof: wherein: R1 is halogen, —OR1...	12/12/2006
7141669	Cannabiniod receptor ligands and uses thereof Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein ...	11/28/2006
7135493	HDAC inhibitor A compound having the following formula (I): wherein R1 is N-containing heterocyclic ring optionally substituted with one or more suitable substituent(s), ...	11/14/2006
7135486	Substituted 2-thio-3,5-dicyano-4-aryl-6-aminopyridines and the use thereof This application relates to compounds of formula (I), wherein R1, R2, R3, and R4 are defined as recited in the claims, or a tautomer, salt, hyd...	11/14/2006
7132426	Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto The present invention relates to certain fused aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or trea...	11/07/2006
7122540	2-Phenyl substituted imidazotriazinones as phosphodiesterase inhibitors The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizi...	10/17/2006
7101884	Tyrosine kinase inhibitors The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogen...	09/05/2006
7087754	Pyrazolo[3,4-d]pyrimidine derivatives and their use as purinergic receptor antagonists Use of a compound of formula (I): wherein R1 is selected from alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NR6R7, NR5COR6, NR5CONR6R7, NR5CO2	08/08/2006
7074929	Certain alkylene diamine-substituted heterocycles This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula II, IV, V, VII–IX and X...	07/11/2006
7067660	Process for the preparation of pyrazolopyrimidinones There is provided a process for the production a compound of general formula I: wherein A, R1, R2, R3 and R4 have meanings given in the description, which process compr...	06/27/2006
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
7060823	5-aminoalkyl-pyrazolo[4,3-d]pyrimidines with a phosphodiesterase v-inhibiting effect The present invention relates to 5-aminomethylpyrazolo[4,3-d]pyrimidines of the general formula (I) in which the radicals R1 to R6 have the meaning indicated in the text. The compounds show ...	06/13/2006
7041667	CCR5 modulators Compounds of Formula 1 [Region α]—[Region β]—[Region γ]—[Region δ] (1) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and m...	05/09/2006

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Class 544/262 - The other cyclo in the bicyclo ring system is five-membered