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Patent No. 5443036

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Class 544/265 - Chalcogen bonded directly to ring carbon of the purine ring system


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein chalcogen (i.e., oxygen, sulfur, selenium,
No. of patents: 279
Last issue date: 02/14/2012


1              
NumberTitleIssue Date
81149942′ and 3′-substituted cyclobutyl nucleoside analogs for the treatment viral infections and abnormal cellular proliferation
Provided are cyclobutyl nucleosides and methods for their use in treatment of infections including Retroviridae (including HIV), Hepadnaviridae (including HBV), or Flaviviridae (including BVDV and HCV) infection, or conditions related to abnormal cellular proliferat...
02/14/2012
7750153Process for the preparation of didanosine using novel intermediates
The present invention relates to novel crystalline alkali metal and alkaline earth metal salts of 2′,3′-dideoxy-2′,3′-didehydroinosine. The present invention also provides a novel process for preparation of didanosine in high yield and purity using novel int...
07/06/2010
7439240Purine-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
7439359Small molecule compositions for binding to hsp90
Structural differences in binding pockets of members of the HSP90 family can be exploited to achieve differential degradation of kinases and other signaling proteins through the use of designed small molecules which interact with the N-terminal binding pocket with a...
10/21/2008
73938552,2-bis-(hydroxymethyl)cyclopropylidenemethyl-purines and pyrimidines as antiviral agents
Compounds which are active against viruses have the following formulas: wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (...
07/01/2008
7388002Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
Compounds represented by the formula: A is (CH2)nR2, —CH═CH2, CH2—CH═CH2, O(CH2)nR2, CH(OH)CH3, CH(OH)...
06/17/2008
7358235Analogs of nitrobenzylthioinosine
Analogs or derivatives of nitrobenzylthioinosine compounds. The use of these new analogs of nitrobenzylthioinosine and methods for the treatment of pain and various other indications using these analogs of nitrobenzylthioinosine as well as pharmaceutical composition...
04/15/2008
7351827Substituted oxetanes, method of making, and method of use thereof
Oxetane-containing nucleosides, particularly non-reducing psiconucleoside oxetanes are described herein. Therapeutic application of these oxetane compounds toward the treatment of nucleoside analog related disorders such as disorders involving cellular proliferation...
04/01/2008
7335654Phosphodiesterase 4 inhibitors
PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein. ...
02/26/2008
7307166Oxpurine nucleosides and their congeners, and acyl, derivatives thereof, for improvement of hematopoiesis
The invention relates to certain oxypurine nucleosides, congeners of such oxypurine nucleosides, and acyl derivatives thereof, and compositions which contain at least one of these compounds. The invention also relates to methods of treating or preventing hematopoiet...
12/11/2007
7285558Pyrazolo[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
7256196Purine cytokine inhibitors
The present invention relates to 2,8,9-substituted purines which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions c...
08/14/2007
7253154Substituted thiazolopyrimidines as xanthine oxidase inhibitors
The invention relates to compounds of the following formula (I) or their salts: in which R1 represents OR4 or others, in which R4 is an alkyl group having 1-8 carbon atoms which m...
08/07/2007
7241890Purine analogs having HSP90-inhibiting activity
Novel purine compounds of Formula I. and tautomers, pharmaceutically acceptable salts, and prodrugs thereof, wherein X is S, S(O), or S(O)2; and O is selected from alkyl, cycloalkyl, arylalkyl, aryl, h...
07/10/2007
7211668PNA 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
7176312Kinase inhibitor scaffolds and methods for their preparation
General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, bor...
02/13/2007
7129239Purine compounds 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. ...
10/31/2006
7109330Purine inhibitors of cyclin dependent kinase 2 and IκB-α
Compounds of the following formula are provided: In the Formula (I), R1 is —X—R1′; in which R1′ is optionally substituted lower alkyl, optionally substituted aryl, optiona...
09/19/2006
RE39112Purine derivatives and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes
The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonist action. A purine compound represented by the formula (I), its pharmacologically...
05/30/2006
RE390564-Azasteroids for treatment of hyperandrogenic conditions
Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5α-reductase inhibitory activity. These compounds inhibit 5α-reductase type 1 and type 2. The compounds of structural Formula...
04/04/2006
6991902Nucleobase heterocyclic combinatorialization
Mixtures of chemical compounds are provided having antibacterial and other utility. The mixtures are formed, preferably in solution phase, from the reaction of a purine or pyrimiding heterocyclic scaffold with a set of related chemical substituients, optionally thro...
01/31/2006
6974815Hexahydro-benzimidazolone compounds useful as anti-inflammatory agents
The present invention is directed to compounds having the formula (I): useful in treating inflammatory and immune diseases, in which K is O or S; Q is —C(═O)— or optionally substituted C1-4alkylene; Ar...
12/13/2005
6962921Dementia remedies containing 2-aryl-8-oxodihydropurine derivatives as the active ingredient
Medicines for treatment or prevention of dementia comprising 2-aryl-8-oxodihydropurine derivatives of the formula (I): wherein W is H, C1-6 alkyl, halogen, C1-6 alkoxy, or the like; X is H, C...
11/08/2005
6949535Inhibitors of human phosphatidyl-inositol 3-kinase delta
Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ ac...
09/27/2005
6949640Method for synthesizing 2-chloro-9-(2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine
2-Chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin-9-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofuranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy...
09/27/2005
6936602Benzazepine derivatives, process for the preparation of the same and uses thereof
Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which...
08/30/2005
6919455Purine derivative dihydrate, drugs containing the same as the active ingredient and intermediate in the production thereof
A compound represented by the following formula (I), or a salt thereof: where X is a halogen atom or a group represented by —S—(CH2)n—A, —SO—(CH2)m—B, —SO2...
07/19/2005
6919332N-substituted-heteroaryloxy-aryloxy-pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to N-substituted-heteroaryloxy-aryloxy-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, and R1 are as defined in the specification, and to pharmac...
07/19/2005
6906190Inhibitors for de novo-RNA polymerases and methods of identifying targets for same
A polymerase inhibitor has first moiety coupled to a second moiety via an optional linker in which the first moiety binds to an initiation nucleotide binding site of a polymerase and forms at least two hydrogen bonds with an RNA template strand that is associated wi...
06/14/2005
6897201Compositions and methods for the treatment of glaucoma or ocular hypertension
The present invention is directed to a method of reducing intraocular pressure. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a nucleoside 5′-pyrophosphate pyranoside or analogue, which is defined by...
05/24/2005
6894045Tetrahydropurinones and derivatives thereof as corticotropin releasing factor receptor ligands
Compounds provided herein are novel substituted tetrahydropurinones of Formula (I): wherein R3 is aryl substituted with 0-5 XAr or heteroaryl substituted with 0-4 XhAr. Such compounds a...
05/17/2005
6893815Nucleobase heterocyclic combinatorialization
Mixtures of chemical compounds are provided having antibacterial and other utility. The mixtures are formed, preferably in solution phase, from the reaction of a purine or pyrimiding heterocyclic scaffold with a set of related chemical substituients, optionally thro...
05/17/2005
6867298Copper-catalyzed formation of carbon-heteroatom and carbon-carbon bonds
The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or a...
03/15/2005
6864254Inhibitor for 20-hete-yielding enzyme
An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular dis...
03/08/2005
6855821Processes for preparing 1,3-dioxolane nucleosides
Disclosed are novel processes for preparing 1,3-dioxolane nucleosides of general formula I and II: wherein B is a purine or pyrimidine base or an analog or derivative thereof. The invention also provides intermediates ...
02/15/2005
6849660Antimicrobial biaryl compounds
Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1′ is —C(O)NR5R5′
02/01/2005
6849735Methods of synthesis for 9-substituted hypoxanthine derivatives
An improved method of synthesis of a 9-substituted hypoxanthine derivative comprises the steps of: (1) reacting aminocyanacetamide with triethyl orthoformate to form an imidoester derivative of aminocyanacetamide; (2) forming a compound having a reactive amino group...
02/01/2005
6800620Inhibitors of human phosphatidylinositol 3-kinase delta
Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ ac...
10/05/2004
67908412-hydroxymethylcyclopropylidenemethylpurines and -pyrimidines as antiviral agents
Compounds which are active against viruses have the following Formulas: wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopu...
09/14/2004
6790958Purine inhibitors of cyclin dependent kinase 2 & IKBA
Compounds of the following formula are provided: wherein: R1 is —X—R1′; in which R1′ is alkyl, cycloalkyl, aryl, aralkyl, hetaryl, or heterocyclyl, all of which are optiona...
09/14/2004
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