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| Number | Title | Issue Date |
| 8168615 | Prodrugs of piperazine and substituted piperidine antiviral agents This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R | 05/01/2012 |
| 8163719 | Regulators of the hedgehog pathway, compositions and uses related thereto The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway,... | 04/24/2012 |
| 8163718 | Nucleoside analogues containing phosphonate or phosphonamide groups Novel compounds having structure (1) wherein Z, is N or CH to form a purine, Y, R1, R2′ and R2 are defined in the specification, are provided for use in the treatment of tumors and ... | 04/24/2012 |
| 8138164 | HCV NS3 protease inhibitors The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. ... | 03/20/2012 |
| 8093229 | Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs as HSP90-inhibitors Alkynyl pyrrolo [2,3-d] pyrimidines of Formula I are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents used in the treatment and prevention of various HSP90 mediated disorders. Methods of synthesis and use of such compound... | 01/10/2012 |
| 8088754 | Anti-proliferative compounds, compositions, and methods of use thereof Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV, wherein: Y1A and Y1B are independently Y1... | 01/03/2012 |
| 8063028 | Heterocyclic antiviral compounds Compounds of formula I, wherein R1, R2, R3, X1, X2 and Ar, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment... | 11/22/2011 |
| 7871991 | Phosphonate analogs of HIV inhibitor compounds The invention is related to phosphorus substituted anti-viral inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such... | 01/18/2011 |
| 7803788 | Prodrugs of phosphonate nucoleotide analogues A novel method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a) having substituent groups as defined herein. Compositions of t... | 09/28/2010 |
| 7723319 | Acyclic nucleoside phosphonate derivatives, salts thereof and process for the preparation of the same The present invention relates to an acyclic nucleoside phosphonate derivative which is useful as an antiviral agent (particularly, against hepatitis B virus), pharmaceutically acceptable salts, stereoisomers, and a process for the preparation thereof. ... | 05/25/2010 |
| 7625881 | Prodrugs of Aadenosine receptor antagonists Disclosed are prodrugs of A2B adenosine receptor antagonists, having the following structure and their use in treating mammals for various disease states. ... | 12/01/2009 |
| 7608603 | Substituted pyrazolo[3,4-D]pyrimidines as p38 MAP kinase inhibitors Compounds of formula Ia, Ib, Ic, Id, Ie, If, Ig or Ih: wherein X and Y are nitrogen or one of X and Y is nitrogen and the other is CRg, and W, D, E, R4, R5, R6... | 10/27/2009 |
| 7605147 | Acyclic nucleoside phosphonate derivatives, salts thereof and process for the preparation of the same The present invention relates to an acyclic nucleoside phosphonate derivative represented by the following formula (1): in which represents single bond or double bond, R1, R2, R3, R7 | 10/20/2009 |
| 7579332 | Nucleobase phosphonate analogs for antiviral treatment The invention provides compounds with activity against infectious diseases. The compounds of the invention may inhibit retroviral reverse transcriptases and thus inhibit the replication, of the virus. The compounds of the invention may be useful for treating human p... | 08/25/2009 |
| 7563781 | Triazolopyrimidine derivatives The invention relates to the discovery of triazolopyrimidine derivatives of formula (I), which have been found to exhibit inhibitory activity against the serine-tyrosine and tyrosine kinases. ... | 07/21/2009 |
| 7553825 | Anti-proliferative compounds, compositions, and methods of use thereof Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV, wherein: Y1A and Y1B are independently Y1... | 06/30/2009 |
| 7544672 | Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs as HSP90-inhibitors Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents used in the treatment and prevention of various HSP90 mediated disorders. Methods of synthesis and use of such com... | 06/09/2009 |
| 7528121 | Phosphonooxy quinazoline derivatives and their pharmaceutical use Quinazoline derivatives of formula (I) wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy. ... | 05/05/2009 |
| 7494984 | Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors The invention encompasses a series of bicyclic heterocyclic compounds of Formula I which are inhibitors of 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... | 02/24/2009 |
| 7476661 | Regulators of the hedgehog pathway, compositions and uses related thereto The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway,... | 01/13/2009 |
| 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 |
| 7435739 | Substituted pyrrolopyrimidines useful in the treatment of cancer The invention relates to compounds of the formula 1 or a pharmaceutically acceptable salt, prodrug or hydrates thereof, wherein X, L, R1, R2, R3 and R4 are as defined herein. The ... | 10/14/2008 |
| 7429596 | 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof This invention generally relates to pyrazolo pyrimidine derivatives useful as inhibitors of short chain dehydrogenase/reductase (SDR) family of NAD(P)(H) dependent oxido-reductases. The invention further relates to pharmaceutical compositions and methods of preventi... | 09/30/2008 |
| 7429574 | 4-heterocyclo-pyrrolo[2,3d] pyrimidine compositions and their use Novel deazapurines are disclosed which are useful for the treatment of adenosine receptor stimulated diseases. ... | 09/30/2008 |
| 7419969 | HIV integrase inhibitors: cyclic pyrimidinone compounds The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates us... | 09/02/2008 |
| 7417036 | Crystal form of adefovir dipivoxil and its preparation A new crystal form of adefovir dipivoxil {9-[2-[bis(pivaloyloxy)-methoxy]-phosphinyl]-methoxyl]-ethyl]-adenime} and its composition is disclosed, as is a method to prepare the crystal comprising placing adefovir dipivoxil in a round bottom flask, adding organic solv... | 08/26/2008 |
| 7390791 | Prodrugs of phosphonate nucleotide analogues A novel method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a) having substituent groups as defined herein. Compositions of t... | 06/24/2008 |
| 7388002 | Nucleosides, 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 |
| 7371857 | Synthesis 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 |
| 7368437 | Bicyclic heterocycles, processes for their preparation and their use as herbicides and pharmaceutical agents Methods and compounds for inhibiting the enzymes adenosine monophosphate deaminase or adenoside deaminase are provided. Such methods and compounds are useful in agriculture, horticulture and/or pharmacology as, for example, active compounds for crop protection or ph... | 05/06/2008 |
| 7358250 | Pyrrolo[2,3-d]pyrimidines that modulate ACK1 activity Compounds that modulate the action of ACK1 and LCK, and related compositions methods for treating ACK1- and LCK-mediated diseases are described. In one aspect, the compounds have the general structure: where the values of t... | 04/15/2008 |
| 7338966 | Substituted oxindole derivatives as tyrosine kinase inhibitors The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alt... | 03/04/2008 |
| 7323449 | Thionucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase The present invention provides thionucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependen... | 01/29/2008 |
| 7312204 | Insecticides The present invention relates to insecticidal mixtures of chloronicotinyl insecticides of the formula (I) in which R1 represents C1-C5-alkyl, R2 | 12/25/2007 |
| 7300924 | Anti-infective phosphonate analogs The invention is related to phosphorus substituted anti-infective compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compou... | 11/27/2007 |
| 7285543 | Purine inhibitors of fructose-1,6-bisphosphatase Novel purine compounds of Formula 1, pharmaceutically acceptable prodrugs and salts thereof, and their use as fructose 1,6-bisphosphatase inhibitors ... | 10/23/2007 |
| 7253154 | Substituted 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 |
| 7241887 | 3-azabicyclo[3.2.1]octane derivatives The subject invention relates to 3-azabicyclo[3.2.1]octane derivatives, pharmaceutical compositions comprising such derivatives and methods of using such derivatives to treat disease states, disorders and conditions mediated by opioid receptors. The subject inventio... | 07/10/2007 |
| 7238679 | Heterocycles and uses thereof Compounds of the following formula are disclosed: wherein RB is a substituted or unsubstituted aryl or heteroaryl moiety; at least one of RU and RL is a phosphorus-containing moie... | 07/03/2007 |
| 7235538 | Heterocyclic compounds, which are inhibitors of the enzyme DPP-IV The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, which are of formula I wherein each n is one or two independently and R1, R2, R3 | 06/26/2007 |