Patents
Literature
Hiro is an intelligent assistant for R&D personnel, combined with Patent DNA, to facilitate innovative research.
Hiro

2007 results about "Pyrazine" patented technology

Pyrazine is a heterocyclic aromatic organic compound with the chemical formula C₄H₄N₂. Pyrazine is a symmetrical molecule with point group D₂ₕ. Pyrazine is less basic than pyridine, pyridazine and pyrimidine.

SUBSTITUTED SPIROPYRIDO[1,2-a]PYRAZINE DERIVATIVE AND PHARMACEUTICAL USE OF SAME AS HIV INTEGRASE INHIBITOR

[Summary][Problem] Provided is a substituted spiropyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof, which is useful as an anti-HIV agent.[Solving Means] The present invention relates to a compound represented by the following formula [I] or [II] or a pharmaceutically acceptable salt thereof:wherein each symbol is as defined in the specification.
Owner:JAPAN TOBACCO INC

Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton's tyrosine kinase by such compounds

Compounds of Formula I-a and all pharmaceutically-acceptable forms thereof, are described herein. The variables R1, R2, R3, Z1, Q, and A shown in Formula I-a are defined herein. Pharmaceutical compositions containing one or more compounds of Formula I-a, or a pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein. Methods of treating patients suffering from certain diseases responsive to inhibition of tyrosine kinase activity are also given. In certain embodiments the diseases are responsive to inhibition of Btk activity and / or B-cell proliferation. Such methods comprise administering to such patients an amount of a compound of Formula I-a effective to reduce signs or symptoms of the disease. These diseases include cancer, an autoimmune and / or inflammatory disease, or an acute inflammatory reaction. Thus methods of treatment include administering a sufficient amount of a compound or salt as provided herein to decrease the symptoms or slow the progression of these diseases. Other embodiments include methods of treating other animals, including livestock and domesticated companion animals, suffering from a disease responsive to inhibition of kinase activity. Methods of treatment include administering a compound of Formula I-a as a single active agent or administering a compound of Formula I-a in combination with one or more other therapeutic agent. A method for determining the presence of Btk in a sample, comprising contacting the sample with a compound or form thereof of Formula I-a under conditions that permit detection of Btk activity, detecting a level of Btk activity in the sample, and therefrom determining the presence or absence of Btk in the sample.
Owner:GILEAD CONNENTICUT INC

Method for Preparing Flavorful and Aromatic Compounds

The invention provides a method of preparing a purified, pyrazine-containing aqueous composition by mixing a reducing sugar, a base, and an amino acid in water to produce a mixture; heating the mixture for a time and under conditions conducive to Maillard reactions such that a flavorful and aromatic aqueous solution is formed, the aqueous solution comprising a plurality of pyrazines and a first 4-methylimidazole concentration; distilling the aqueous solution to produce an aqueous distillate comprising a plurality of pyrazines and having a second 4-methylimidazole concentration lower than the first 4-methylimidazole concentration; and collecting the aqueous distillate. The invention also includes flavorful and aromatic aqueous compositions formed by this inventive method, as well as tobacco products (e.g., smokable materials, smoking articles, and smokeless tobacco) incorporating the flavorful and aromatic composition.
Owner:R J REYNOLDS TOBACCO COMPANY

Compounds useful as inhibitors of atr kinase

The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I:wherein the variables are as defined herein.
Owner:VERTEX PHARMA INC

Nicotinamide acids, amides, and their mimetics active as inhibitors of PDE4 isozymes

Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: wherein j is 0 or 1, k is 0 or 1, m is 0, 1, or 2; n is 1 or 2; A is selected from the partial Formulas: where q is 1, 2, or 3, W3 is -O-; -N(R9)-; or -OC(=O)-; R7 is selected from -H; -(C1-C6) alkyl, -(C2-C6) alkenyl, or -(C2-C6) alkynyl substituted by 0 to 3 substituents R10; -(CH2)u-(C3-C7) cycloalkyl where u is 0, 1 or 2, substituted by 0 to 3 R10; and phenyl or benzyl substituted by 0 to 3 R14; R8 is tetrazol-5-yl; 1,2,4-triazol-3-yl; 1,2,4-triazol-3-on-5-yl; 1,2,3-triazol-5-yl; imidazol-2-yl; imidazol-4-yl; imidazolidin-2-on-4-yl; 1,3,4-oxadiazolyl; 1,3,4-oxadiazol-2-on-5-yl; 1,2,4-oxadiazol-3-yl; 1,2,4-oxadiazol-5-on-3-yl; 1,2,4-oxadiazol-5-yl; 1,2,4-oxadiazol-3-on-5-yl; 1,2,5-thiadiazolyl; 1,3,4-thiadiazolyl; morpholinyl; parathiazinyl; oxazolyl; isoxazolyl; thiazolyl; isothiazolyl; pyrrolyl; pyrazolyl; succinimidyl; glutarimidyl; pyrrolidonyl; 2-piperidonyl; 2-pyridonyl; 4-pyridonyl; pyridazin-3-onyl; pyridyl; pyrimidinyl; pyrazinyl; pyridazinyl; indolyl; indolinyl; isoindolinyl; benzo[b]furanyl; 2,3-dihydrobenzofuranyl; 1,3-dihydroisobenzofuranyl; 2H-1-benzopyranyl; 2-H-chromenyl; chromanyl; benzothienyl; 1H-indazolyl; benzimidazolyl; benzoxazolyl; benzisoxazolyl; benzothiazolyl; benzotriazolyl; benzotriazinyl; phthalazinyl; 1,8-naphthyridinyl; quinolinyl; isoquinolinyl; quinazolinyl; quinoxalinyl; pyrazolo[3,4-d]pyrimidinyl; pyrimido[4,5-d]pyrimidinyl; imidazo[1,2-a]pyridinyl; pyridopyridinyl; pteridinyl; or 1H-purinyl; or A is selected from phosphorous and sulfur acid groups; W is -O-; -S(=O)t-, where t is 0, 1, or 2; or -N(R3)-; Y is =C(R1a)-, or -[N<custom-character file="US20020111495A1-20020815-P00900.TIF" wi="20" he="20" id="custom-character-00001" / >(O)k] where k is 0 or 1; R4, R5 and R6 are (1) -H; provided that R5 and R6 are not both -H at the same time, -F; -Cl; -(C2-C4) alkynyl; -R16; -OR16; -S(=O)pR16; -C(=O)R16, -C(=O)OR16, -C(=O)OR<highlight><sup
Owner:PFIZER INC

Benzoimidazolyl-pyrazine compounds for inflammation and immune-related uses

The invention relates to compounds of structural formula (I) or (III): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein ring A, X1, X2, X3, X5, R1, R4, Y, Z, L, m and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
Owner:SYNTA PHARMA CORP

(indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)-pyrazines for treating rho kinase-mediated diseases and conditions

Methods for using (indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)-pyrazines are disclosed herein to treat rho kinase-mediated diseases or rho kinase-mediated conditions, including controlling intraocular pressure and treating glaucoma, are disclosed. Ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma, and additionally useful for controlling intraocular pressure, the compositions comprising an effective amount of (indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)-pyrazines, are disclosed herein.
Owner:ALCON RES LTD

Compounds useful as inhibitors of atr kinase

The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I:wherein the variables are as defined herein.
Owner:VERTEX PHARMA INC

Novel imidazopyrazines as cyclin dependent kinase inhibitors

In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
Owner:MERCK SHARP & DOHME CORP

Compounds useful as inhibitors of atr kinase

The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I:wherein the variables are as defined herein.
Owner:VERTEX PHARMA INC

Compounds useful as inhibitors of atr kinase

The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I:wherein the variables are as defined herein.
Owner:VERTEX PHARMA INC

Pyrazine derivatives, process for manufacture and use thereof

The present invention provides pyrazine derivatives of formula Iand pharmaceutically acceptable salts thereof, wherein the designation of R1, R2, R3 and R4 is provided herein. The invention also provides syntheses for preparation of such compounds. The invention further provides methods of use of these compounds and pharmaceutical compositions containing them for treatment and / or prevention of diseases and for manufacture of medicaments. These compounds and pharmaceutical compositions have antioxidative and thrombolytic effects, and thus can be used for the treatment and / or prevention of cerebral stroke caused by ischemia, and used for manufacture of medicaments for the treatment and / or prevention of nervous system diseases caused by excessive amount of radicals and / or thrombosis, infectious diseases, metabolic system diseases, cardiovascular and cerebrovascular diseases, and age-related degenerative diseases.
Owner:JINAN UNIVERSITY

Oral Care Compositions With Improved Flavor

Oral care compositions having improved taste, said compositions comprising: a carrier material; from about 0.001 to about 10%, by weight of the composition, of an oral care component selected from metal salts, antimicrobial agents, bad breath reduction agents, bleaching agents, surfactants, or a combination thereof; and from about 0.0001 to about 1%, by weight of the composition, of a TRPA1 agonist selected from vanillin esters; benzoate esters; hydroxybenzoate derivatives; methoxy benzoate derivatives; hydroxybutanedioate derivatives; benzamidobenzoate derivatives; methylpropanoate derivatives; phenyl acetate derivatives; hex-3-enoate derivatives; 2-(furan-2-ylmethylsulfanyl)-3-methylpyrazine; phenylmethoxymethylbenzene; (2R)-2-azaniumyl-3-[(2R)-2-azaniumyl-3-oxido-3-oxopropyl]disulfanylpropanoate; (3E)-2-hydroxy-4,8-dimethylnona-3,7-dienal; (2R)-2-azaniumyl-3-[(2S)-2-azaniumyl-3-oxido-3-oxopropyl]disulfanylpropanoate; (3Z)-3-butylidene-2-benzofuran-1-one; 3-methyl-N-(3-methylbutyl)butan-1-imine; 2-(furan-2-ylmethyldisulfanylmethyl)furan; and combinations thereof. Uses thereof and methods of improving the taste of an oral care composition.
Owner:THE PROCTER & GAMBLE COMPANY

Compounds useful as inhibitors of ATR kinase

The present disclosure relates to pyrazine compounds of formula I:wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.
Owner:VERTEX PHARMA INC

Compounds useful as inhibitors of ATR kinase

The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula IV:wherein the variables are as defined herein.
Owner:VERTEX PHARMA INC

Substituted imidazolopyrazine and triazolopyrazine derivatives: gabaa receptor ligands

Compounds of Formula (1) are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, R5, R6, R7, R8, and Ar in the above Formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals, and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
Owner:NEUROGEN

Cyclic pyrazinoylguanidine sodium channel blockers

The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.
Owner:PARION SCI DURHAM NC

Pyrrolopyrazines and pyrazolopyrazines useful as inhibitors of protein kinases

InactiveUS20060258662A1Avoid cell deathTreat and prevent reperfusion/ischemiaBiocideSenses disorderPyrazineBiochemistry
The present invention relates to compounds useful as inhibitors of Aurora protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
Owner:VERTEX PHARMA INC
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products