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Class 544/277 - Nitrogen attached directly or indirectly to the purine ring system by nonionic bonding


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein nitrogen is attached directly or indirectly
No. of patents: 642
Last issue date: 05/22/2012


1                      
NumberTitleIssue Date
8183370Process for the preparation of abacavir
Process for removal of the amino protective group of a N-acylated {(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-cyclopent-2-enyl}methanol of formula (II) where R═H or a (C1-C4)-alkyl, using an inorganic base in a mixture of water an...
05/22/2012
8097723Process for the preparation of abacavir
Process for the preparation of abacavir, or its salts or its solvates comprising the step of reacting a compound (IV) where R1 is a (C1-C4)-alkyl radical with anhydrous hydrochloric acid/(C1-C6)-alcohol, and the...
01/17/2012
8058430Biologically active aphrocallistin compounds
The subject invention provides novel compositions of biologically active compounds which can advantageously be used in blocking cellular proliferation and/or treatment of cancer. Exemplified are: ...
11/15/2011
7834181Small-molecule Hsp90 inhibitors
Hsp90 inhibitors are provided having the formula: with a 2′,4′,5′-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4′ and...
11/16/2010
7790884Acylaminopiperidine compound
To provide a compound which has an excellent activity to modulate the functions of CCR4 or TARC and/or MDC and can be used for the prevention and/or treatment of various inflammatory diseases, allergic diseases, autoimmune diseases and the like. An acylaminop...
09/07/2010
7601835Preparation of famciclovir and other purine derivatives
Purine derivatives of formula I, substituted at the 9-position, are prepared from a chloro substituted purine starting material, first making an alkyl substitution at the 9-position, then forming the desired esterified side chain, reducing this and hydrogenating the...
10/13/2009
7557209Process for the preparation of (1S,4R)-cis-4-[2-amino-6-chloro-9H-purin-9-yl]-2-cyclopentene-1-methanol
The present invention relates to a process for preparing a chloropurine compound of formula (I) ...
07/07/2009
7473780Drying process for preparing crystalline solid famciclovir
The present invention provides a drying process for preparing crystalline solid famciclovir form I comprising the steps of: i) preparing a wet crystalline form of famciclovir; ii) drying the wet crystalline form of famciclovir at a temperature of below 50° C. until...
01/06/2009
74562822-amino-9-(2-substituted ethyl)purines and preparing methods for 9-[4-acetoxy-3-(acetoxymethyl)but-1-yl]-2-aminopurine using the same
The present invention relates to a new compound of 2-amino-9-(2-substituted ethyl)purine and an effective method for preparing 9-[4-acetoxy-3-(acetoxymethyl)but-1-yl]-2-aminopurin (famciclovir) using the same. The 2-amino-9-(2-substituted ethyl)purine according to t...
11/25/2008
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
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
7432274Acyclic nucleoside derivatives
Methods and novel intermediates for the preparation of and the treatment with acyclic nucleoside derivatives of the formula: where one of R1 and R2 is an amino acid acyl group ...
10/07/2008
7429595Acyl and sulfonyl derivatives of 6,9-disubstituted 2-(trans-1,4-diaminocyclohexyl)-purines and their use as antiproliferative agents
The present invention is directed to acyl and sulfonyl derivatives of 6,9-disubstituted 2-(trans-1,4 -diaminocyclohexyl)-purines of the formula where Z is selected from the group consisting of —S(O)2—, and ...
09/30/2008
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
7375224Adenine modified silica-based catalyst, a process for the preparation and use there for the production of cyclic carbonates
The present invention provides an adenine modified solid, ordered, mesoporous, bifunctional, organo-inorganic silica-based catalyst, its method of preparation and also a process for the production of cyclic carbonates of the formula hereinbelow
05/20/2008
7371857Synthesis for hydroxyalkylated heterocyclic bases
A hydroxyalkylated heterocyclic base is prepared by reacting a heterocyclic base with an alkylene carbonate in dimethylacetamide as a solvent, wherein the hydroxyalkylated heterocyclic base is isolated from the solvent using isopropanol or tert-butylmethylether....
05/13/2008
7355043Preparation of purines
A process for the preparation of a compound of formula (A) wherein: X is hydrogen or hydroxy, chloro, C1-6 alkoxy or pheny C1-6 alkoxy; and Ra and Rb are hydrogen, or acyl or phosphate derivatives thereof, which process co...
04/08/2008
7351807Cyanine-sulfenates for dual phototherapy
Dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions. The compounds comprise sulfenates having the formula, t,0080 where E is selected from the group consisting of somatostatin receptor binding molecules, heat se...
04/01/2008
7342021Phosphodiesterase 4 inhibitors
PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein. ...
03/11/2008
7338774Method for determining activity of cell cycle regulatory factor and method for diagnosing cancer using the same
A method for determining the activity of a cell cycle regulatory factor comprising the steps of: preparing a sample for measuring a cyclin-dependent kinase/cyclin complex from living cells; reacting adenosine 5′-...
03/04/2008
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
7332486Phosphodiesterase 4 inhibitors
PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein. ...
02/19/2008
7321035Process for producing 2,6-dihalogenopurine
A process for conveniently and efficiently preparing a 2,6-dihalogenopurine using an inexpensive starting material. A process for preparing a 2,6-dihalogenopurine, comprising treating a 2-amino-6-halogenopurine having a protective group at 7th position or...
01/22/2008
7319101COMT inhibitors for the treatment of depression and impaired cognition
The present invention relates to compounds of formula I wherein R1 is as defined in the specification and to esters thereof which are hydrolyzable under physiological conditions and to the ph...
01/15/2008
73148712-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
7312326Fluorescent labeled nucleotide derivatives
Fluorescent labeled reporter compounds having a modified cyanine dye that is coupled to a nucleotide derivative through a linker are disclosed. The compounds are useful for nucleic acid sequence analysis. The fluorescent labeled reporter compounds are ring-locked cy...
12/25/2007
7309497Injectable pharmaceutical composition for systematic administration of pharmacologically active ingredients
The invention relates to novel pharmaceutical compositions for the systemic administration of pharmacologically active ingredients. The invention relates in particular to an injectable pharmaceutical composition comprising (a) a pharmacologically active ingredient i...
12/18/2007
7300923Partial and full agonists of A1 adenosine receptors
Disclosed are syntheses suitable for large scale manufacture of novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infa...
11/27/2007
7291623Compounds that interact with kinases
A method of inhibiting or effecting the activity of protein kinase activity which comprises contacting a protein kinase with a compound of formula (I) being a derivative of a furanose or pyranose form of a monosaccharide, or a pharmaceutically acceptable salt thereo...
11/06/2007
7279483Famciclovir monohydrate
Famciclovir monohydrate and its pharmaceutical use. ...
10/09/2007
7279482Heterocyclic compound based on N-substituted adenine, methods, of their preparation, their use for preparation of drugs, cosmetic preparations and growth regulators, pharmaceutical preparations, cosmetic preparations and growth regulators containing these compounds
Heterocyclic derivatives based on N6-substituted adenine of, e.g.,a formula: wherein R2 is hydrogen, R6 is R6′-X, X is —NH—, and R6′ is substituted phenyl or substituted benzyl. The derivatives...
10/09/2007
7273864Compositions and methods for inducing osteogenesis
The present invention provides compositions and methods for differentiating and transdifferentiating mammalian cells into cells of an osteoblast lineage, using compounds of the following formula: wherein R4 ...
09/25/2007
7273869Inhibitors of Akt activity
The present invention is directed to compounds comprising a ring-fused quinoxalinyl moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this inven...
09/25/2007
7271157Aadenosine receptor agonists
Disclosed is a synthesis suitable for large scale manufacture of novel compounds that are partial and full A1 adenosine receptor agonist having the structure of Formula I: wherein R is optionally subst...
09/18/2007
7265111Adenosine analogues and their use as pharmaceutical agents
The present invention relates to compounds according to the general formula (I) wherein X is selected from the group consisting of wherein n and p are indepe...
09/04/2007
7262176Adenosine A receptor agonists
Disclosed are novel compounds that are A3 adenosine receptor agonists, useful for treating various disease states, including cancer, cardiac ischemia, leukopenia, and neutropennia. ...
08/28/2007
7259157N-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
7259159Guanidino derivatives as inhibitors of cell adhesion
The present invention relates to acylguanidino derivatives of formula (I), in which R1, R2, R3, A, B, X, Y and n have the meanings indicated in claim 1, their physiologically tolerable salts and their prodrugs. The compounds o...
08/21/2007
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
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