- Urea-substituted alkynyl pyrimidine or urea-substituted alkynyl pyridine compound as well as composition and application thereof
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The invention relates to urea-substituted alkynyl pyrimidine or urea-substituted alkynyl pyridine compounds with a formula (I) or pharmaceutically acceptable salts, isomers, solvates, crystals or prodrugs thereof, pharmaceutical compositions containing the compounds, and applications of the compounds or compositions in drug preparation. The medicine can be used as kinase inhibitors such as ABL, ABL-T315I, KIT, VEGFR-2 and the like for treating related diseases.
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Paragraph 0089-0091
(2021/02/10)
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- NITROGENOUS HETEROCYCLIC DERIVATIVES AND THEIR APPLICATION IN DRUGS
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The invention relates to the field of medicine, discloses new nitrogen heterocyclic derivatives, preparation method thereof and as medicament in particular as the treatment and prevention of treating tissue fibrosis of the medicament. The invention also discloses a pharmaceutically acceptable compound of the present invention comprise a pharmaceutical composition and methods for using the composition for the treatment of the human or animal tissue fibrosis of diseases, in particular for treating the human or animal renal interstitial fibrosis, glomerular sclerosis, hepatic fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, skin fibrosis, after the operation of adhering, benign prostate hypertrophy, bone-myocardial, scleroderma, multiple sclerosis, pancreas fibrosis, liver cirrhosis, myosarcoma, neurofibromatosis, interstitial pulmonary fibrosis, diabetic nephropathy, Alzheimer's disease or vascular fibrosis disease in use. (by machine translation)
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Page/Page column 121
(2018/06/01)
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- Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT
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In modern cancer therapy, the use of small organic molecules against receptor tyrosine kinases (RTKs) has been shown to be a valuable strategy. The association of cancer cells with dysregulated signaling pathways linked to RTKs represents a key element in
- Kaitsiotou, Helena,Keul, Marina,Hardick, Julia,Mühlenberg, Thomas,Ketzer, Julia,Ehrt, Christiane,Krüll, Jasmin,Medda, Federico,Koch, Oliver,Giordanetto, Fabrizio,Bauer, Sebastian,Rauh, Daniel
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p. 8801 - 8815
(2017/11/15)
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- Nitrogenous Heterocyclic Derivatives And Their Application In Drugs
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The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.
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Paragraph 0504
(2015/03/31)
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- NITROGENOUS HETEROCYCLIC DERIVATIVES AND THEIR APPLICATION IN DRUGS
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The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.
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Paragraph 00260
(2014/02/15)
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- SUBSTITUTED PYRAZOLYL-BASED CARBOXAMIDE AND UREA DERIVATIVES BEARING A PHENYL MOIETY SUBSTITUTED WITH AN O-CONTAINING GROUP AS VANILLOID RECEPTOR LIGANDS
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The invention relates to substituted pyrazolyl-based carboxamide and urea derivatives of formula (Q) as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Page/Page column 124; 125; 126
(2013/05/23)
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- Aryl or N-heteroaryl Substituted Methanesulfonamide Derivatives as Vanilloid Receptor Ligands
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The invention relates to aryl or N-heteroaryl substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Paragraph 0544; 0545
(2013/04/10)
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- Substituted Methanesulfonamide Derivatives as Vanilloid Receptor Ligands
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The invention relates to substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseas
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Paragraph 0359-0360; 0370-0371; 0375-0376; 0380-0381
(2013/04/10)
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- ARYL OR N-HETEROARYL SUBSTITUTED METHANESULFONAMIDE DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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The invention relates to aryl or N-heteroaryl substituted methanesulfonamide derivatives of Formula (I) as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Page/Page column 79
(2013/04/13)
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- SUBSTITUTED METHANESULFONAMIDE DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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The invention relates to substituted methanesulfonamide derivatives as vanilloid receptor ligands of formula (I), to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and
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Page/Page column 65; 66
(2013/04/13)
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- Amine Substituted Methanesulfonamide Derivatives as Vanilloid Receptor Ligands
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The invention relates to amine substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Paragraph 0515; 0516; 0627; 0628; 0637
(2013/04/10)
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- AMINE SUBSTITUTED METHANESULFONAMIDE DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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The invention relates to amine substituted methanesulfonamide derivatives of formula (I) as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Page/Page column 61
(2013/04/13)
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- SUBSTITUTED PYRAZOLYL-BASED CARBOXAMIDE AND UREA DERIVATIVES BEARING A PHENYL MOIETY SUBSTITUTED WITH AN N-CONTAINING GROUP AS VANILLOID RECEPTOR LIGANDS
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The invention relates to substituted pyrazolyl-based carboxamide and urea derivatives of formula (R) bearing a phenyl moiety substituted with an N-containing group as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Page/Page column 76; 80; 82
(2013/05/23)
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- Dihydroindolone compounds, a process for their preparation and pharmaceutical compositions containing them
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Compounds of formula (I): wherein: m and n represent 1 or 2,A represents a pyrrolyl group,X represents a C(O), S(O) or SO2 group,R1 and R2 represent an alkyl group or, together with the nitrogen atom carrying them, form a heterocyclic group,R3 and R4, together with the atoms carrying them, form a heterocyclic group,R5 represents a hydrogen atom or an alkyl group,R6 represents a hydrogen atom or a halogen atom. Medicinal products containing the same which are useful in treating cancer.
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Page/Page column 23
(2011/02/26)
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- (R)-3-(N,N-DIMETHYLAMINO)PYRROLIDINE DERIVATIVES
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(R)-3-(N,N-Dimethyiamino)pyrrolidine derivatives of formula (I), wherein the meaning for Cy1 is as disclosed in the description. These compounds are useful as JAK3 kinase inhibitors
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Page/Page column 68
(2010/04/27)
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- HETEROCYCLIC DERIVATIVE HAVING INHIBITORY ACTIVITY ON TYPE-I 11 -HYDROXYSTEROID DEHYDROGENASE
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Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein X is O or S, a broken line and a wavy line represent the presence or the absence of a bond, (i) when a broken line represents the presence of a bond, a wavy line represents the absence of a bond, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, (ii) when a broken line represents the absence of a bond, a wavy line represents the presence of a bond, R1 and R4 are each independently hydrogen, halogen or the like, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, and R5 and R6 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like.
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Page/Page column 123
(2010/08/07)
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- PIPERAZINYL DERIVATIVES USEFUL IN THE TREATMENT OF GPR38 RECEPTOR MEDIATED DISEASES
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The invention relates to compounds of formula (I), processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or disorders which are mediated via the GPR38 receptor.
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Page/Page column 70
(2008/06/13)
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- N-[4-(1,1'-biphenylyl)methyl]-4-(4-thiomorpholinylmethyl) benzenamines, a new class of synthetic antituberculosis agents active against Mycobacterium avium
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Various N-derivatives of 4-(4-thiomorpholinyl)aniline and 4-(4- thiomorpholinylmethyl)aniline were synthesized and tested for in vitro antibacterial activities against Mycobacterium avium CIP 103317 and other mycobacteria including M. tuberculosis CIP 103471. Appropriate substituents were introduced at the nitrogen of aniline portion in order to exploit their potential antimycobacterial activities. Only derivatives with the biphenylylmethyl group bound to the 4-(4-thiomorpholinylmethyl)aniline moiety were found to possess appreciable antibacterial activities against atypical mycobacteria and M. tuberculosis. Several compounds (7c-g and 7j) were two and sixteen times more potent than azithromycin and isoniazid, respectively, in the in vitro assays against M. avium.
- Mai, Antonello,Sbardella, Gianluca,Artico, Marino,Massa, Silvio,Lampis, Giorgio,Deidda, Delia,Pompeit, Raffaello
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p. 149 - 161
(2007/10/03)
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