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102 results about "Impromidine" patented technology

Impromidine (INN) is a highly potent and specific histamine H₂ receptor agonist. It has been used diagnostically as a gastric secretion indicator.

3H-[1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES

The invention relates to 3H-[1,2,3]triazolo[4,5-d]pyrimidine compounds of the Formula 1:or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
Owner:WYETH LLC

Pyridine-2,4-dicarboxylic acid diamides and pyrimidine-4,6-dicarboxylic acid diamides and the use thereof for selectively inhibiting collagenases

Abstract of Disclosure Pyridine-2,4-dicarboxylic acid diamides and pyrimidine-4,6-dicarboxylic acid diamides of formula I. These compounds are found to possess the property of selectively inhibiting collagenase (MMP). They may therefore be useful in prophylaxis and therapy of diseases whose course involves an increased activity of matrix metalloproteinase 13.
Owner:SANOFI AVENTIS DEUT GMBH

Fused pyrimidines and substituted quinazolines as inhibitors of p97

A group of fused two ring pyrimidine compounds having a heterocycles substituent at the 2 position and a substituted amine at the 4 position as well as optional aliphatic, functional and / or aromatic components substituted at other positions of the pyrimidine and other ring are disclosed. In addition a group of quinazoline compounds having similar substituents at the 2 and 4 positions as well as at other positions are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity.
Owner:EIKON THERAPEUTICS INC

4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as jak-2 modulators and pharmaceutical compositions containing them

This invention relates to certain pyrimidine derivative inhibitors of JAK-2, having Formula (I): wherein D, E, L, Z, R<1>, R<2>, R<25>, and n1 are as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof.
Owner:EXELIXIS INC

Protein tyrosine kinase modulators and methods of use

Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and / or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative,and methods of treatment for diseases associated with protein kinase enzymatic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed.
Owner:BETTA PHARM CO LTD

Phosphoinositide 3-kinase (P13K) inhibitor, pharmaceutical composition containing P13K inhibitor, and application of phosphoinositide kinase inhibitor and pharmaceutical composition

The invention discloses a phosphoinositide 3-kinase (P13K) inhibitor, a pharmaceutical composition containing the P13K inhibitor, and application of the P13K inhibitor and the pharmaceutical composition. The P13K inhibitor comprises a pyrimidine compound and a stereoisomer / hydrate / pharmaceutically-acceptable salt thereof. The pyrimidine compound has a general formula I of which the structure is shown in the specification. The P13K inhibitor and the pharmaceutical composition containing the same can be used for inhibiting PI3 Ks and treating proliferative diseases on which the PI3 Ks act. According to the invention, high-effectiveness and high-selectivity inhibitors for treating proliferative diseases on which PI3Ks act can be provided.
Owner:SUN YAT SEN UNIV

Protein tyrosine kinase modulators and methods of use

Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and / or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative, and methods of treatment for diseases associated with protein kinase enzymatic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed.
Owner:BETTA PHARM CO LTD

Novel synthetic agonists of toll-like receptors containing CG dinucleotide modifications

InactiveUS20080279785A1Allow flexibilityModulate immune responseOrganic active ingredientsPeptide/protein ingredientsPurineCG-dinucleotide
The invention relates to the therapeutic use of oligonucleotides as immune modulatory agents in immunotherapy applications. More particularly, the invention provides immune modulatory oligonucleotide compositions for use in methods for generating an immune response or for treating a patient in need of immune modulation. The immune modulatory oligonucleotides of the invention preferably comprise novel pyrimidines and purines.
Owner:IDERA PHARMA INC

2-amino-3,4-dihydro-pyrido[3,4-d]pyrimidine derivatives useful as inhibitors of beta-secretase (BACE)

The present invention is directed to novel 2-amino-3,4-dihydro-pyrido[3,4-d]pyrimidine derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of β-secretase, also known as β-site cleaving enzyme and BACE, BACE1, Asp2 and memapsin2.
Owner:JANSSEN PHARMA NV

Process for the preparation of tri-substituted pyridine and tri-substituted pyrimidine derivatives useful as gdir agonists

InactiveUS20100113479A1Inadequate glucose toleranceBiocideOrganic active ingredientsDiabetes mellitusD-Glucose
The present invention is directed to novel processes for the preparation of tri-substituted pyridine and tri-substituted pyrimidine derivatives, useful as glucose dependent insulinotropic receptor agonist, for the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.
Owner:ARENA PHARMA

Pyrimidine Derivatives and Their Use as P2Y12 Receptor Antagonists

The invention relates to 4-aminocarbonyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and / or prevention and / or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.
Owner:IDORSIA PHARM LTD

Ligands for aggregated tau molecules

Provided are certain benzothiazole, imidazothiazole, imidazopyrimidine and imidazopyridine compounds, including, for example: formula (I) and pharmaceutically and physiologically acceptable salts, hydrates, and solvates thereof. Such compounds can be used as diagnostic ligands or labels of tau protein and PHF.
Owner:WISTA LAB LTD

4-amino-3-(imidazolyl)-pyrazolo[3,4-d]pyrimidines

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are 4-amino-3-imidazoyl-pyrazolo[3,4-d]pyrimidine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
Owner:CHEMOCENTRYX INC

Sulfoximine-substituted pyrimidines as CDK-and/or VEGF inhibitors, their production and use as pharmaceutical agents

The present invention relates to pyrimidine derivatives of formula (I), which are useful as inhibitors of cyclin-dependent kinases and VEGF receptor tyrosine kinases. The present invention also relates to a method for preparing the derivative and its use as a medicine for treating various diseases.
Owner:BAYER IP GMBH

Thienopyrimidine and furopyrimidine derivative, its preparation method and application in medicines

The invention discloses a thienopyrimidine and furopyrimidine derivative, its preparation method and its application in medicines. The derivative is a compound shown as general formula I, general formula II, general formula III or general formula IV. The thienopyrimidine and furopyrimidine pyrimidine derivative provided in the invention has an obvious EGFR (epidermal growth factor receptor) inhibitory activity, and some of the compounds also have an obvious inhibitory activity on VEGFR (vascular endothelial growth factor receptor), so that the thienopyrimidine and furopyrimidine pyrimidine derivative can be expected to be developed into tyrosine kinase EGFR or / and VEGFR inhibitors, which can be used for preparation of drugs preventing or treating diseases related to EGFR and / or VEGFR. Therefore, the derivative provided in the invention provides a new development direction and approach for developing novel tyrosine kinase inhibitor drugs that have low resistance or can alleviate early inhibitor resistance, and has wide application prospect and medicinal value.
Owner:JIANGSU DESANO PHARMA

Pyrazolo 1,5-a pyrimidine derivatives

InactiveCN100482665CGood kinase inhibitory activityOrganic active ingredientsSenses disorderImmunologic disordersDisease
The Pyrazolo[1,5-a]pyrimidine derivatives represented by formula I and their pharmaceutically acceptable salts exhibit excellent kinase inhibiting activity. Drugs comprising the compounds as effective ingredients are therefore expected to be useful as therapeutic or prophylactic agents for a protein kinase mediated disorder in which kinase is implicated, such as inflammatory disease, autoimmune disease, destructive bone disorder, cancer and / or tumour growth.
Owner:TEIJIN PHARMA CO LTD

Quinazoline, pyridopyrimidine or pyrimidopyrimidine derivative epidermal growth factor inhibitor and preparing method and application thereof

The invention discloses a selectivity inhibitor of a clinical mutant of EGFR protein tyrosine kinase. The selectivity inhibitor of the clinical mutant of EGFR protein tyrosine kinase has a structure which is shown in the formula (1) (The formula (1) is defined in the description), and is a double aromatic nucleus template compound containing quinazoline, pyridopyrimidine or pyrimidopyrimidine. The invention further discloses a preparing method of the compound and an application of the compound as the selectivity inhibitor of the clinical mutant of EGFR protein tyrosine kinase, especially an inhibiting effect of the compound in a T790M-variation EGFR and an application in treating diseases such as renal carcinoma, lung cancer, prostate gland cancer, pancreatic cancer, breast cancer and spongiocytoma, wherein the diseases are related to overexpression of the epidermal growth factor receptor EGFR.
Owner:NANJING LEIKEXING BIOTECH CO LTD
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