- Novel indazole derivatives, and use thereof
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The present invention refers to novel indazole derivatives, or pharmaceutically acceptable salts; and including DYRK1A DYRK1B active ingredient (Dual non-specificity tyrosine phosphorylation in a non-regulated kinase 1a) or a pharmaceutical composition for preventing or treating related disorders are disclosed. (by machine translation)
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- The impact of binding site waters on the activity/selectivity trade-off of Janus kinase 2 (JAK2) inhibitors
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Structure based optimization of B39, an indazole-based low micromolar JAK2 virtual screening hit is reported. Analysing the effect of certain modifications on the activity and selectivity of the analogues suggested that these parameters are influenced by
- Egyed, Attila,Bajusz, Dávid,Keser?, Gy?rgy M.
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p. 1497 - 1508
(2019/03/05)
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- BENZAMIDE OR BENZAMINE COMPOUNDS USEFUL AS ANTICANCER AGENTS FOR THE TREATMENT OF HUMAN CANCERS
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The described invention provides small molecule anti-cancer compounds for treating tumors that respond to cholesterol biosynthesis inhibition. The compounds selectively inhibit the cholesterol biosynthetic pathway in tumor-derived cancer cells, but do not
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Paragraph 0772; 0873; 0774
(2017/01/26)
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- SELECTIVE HETEROCYCLIC SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS
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Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
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Paragraph 0242; 0243
(2015/11/18)
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- NOVEL OXADIAZOLE COMPOUNDS
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Novel oxadiazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions as agonists or antagonists of the S1P family of G protein-coupled receptors for treating diseases associated with modulation o
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- PIPERAZINYL DERIVATIVES USEFUL AS MODULATORS OF THE NEUROPEPTIDE Y2 RECEPTOR
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The present invention is directed to piperidinyl and piperazinyl derivatives of formula (I) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of
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Page/Page column 112
(2009/07/18)
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- COMPOUNDS
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The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
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Page/Page column 44
(2009/12/05)
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- Compounds and methods for F labelled agents
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This invention relates to novel compounds suitable for or already radiolabeled with 18F, methods of making such compounds and use of such compounds for diagnostic imaging. Such labeled compounds are characterized by Formula 11, wherein the subs
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- Thymidine analogs for imaging
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The present invention relates to nucleoside analogues and more particularly to labelled nucleoside analogues of formula (I). It has been found new thymidine analogues can be stably labelled with a detectable label moiety. Further the present invention rel
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Page/Page column 18-19
(2008/06/13)
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- COMPOUNDS AND METHODS FOR 18F LABELED AGENTS
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The present invention relates to novel compounds suitable for or already radiolabeled with 18F, methods of making such compounds and use of such compounds for diagnostic imaging. Such labeled compounds are characterized by Formula II, wherein the substituents G, Q, L, Y and U have the meaning as defined in the specification and claims.
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Page/Page column 74-75; 86-87
(2010/11/30)
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- Dual aromatase-steroid sulfatase inhibitors
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By introducting the steroid sulfatase inhibitory pharmacophore into aromatase inhibitor 1 (YM511), two series of single agent dual aromatase-sulfatase inhibitors (DASIs) were generated. The best DASIs in'vitro (JEG-3 cells) are 5, (IC50(aromatase) = 0.82 nM; IC 50(sulfatase) = 39 nM), and 14, (IC50(aromatase) = 0.77 nM; IC50(sulfatase) = 590 nM). X-ray crystallography of 5, and docking studies of selected compounds into an aromatase homology model and the steroid sulfatase crystal structure are presented. Both 5 and 14 inhibit aromatase and sulfatase in PMSG pretreated adult female Wistar rats potently 3 h after a single oral 10 mg/kg dose. Almost complete dual inhibition is observed for 5 but the levels were reduced to 85% (aromatase) and 72% (sulfatase) after 24 h. DASI 5 did not inhibit aldosterone synthesis. The development of a potent and selective DASI should allow the therapeutic potential of dual aromatase-sulfatase inhibition in hormone-dependent breast cancer to be assessed.
- Woo, L. W. Lawrence,Bubert, Christian,Sutcliffe, Oliver-B.,Smith, Andrew,Chander, Surinder K.,Mahon, Mary F.,Purohit, Atul,Reed, Michael J.,Potter, Barry V. L.
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p. 3540 - 3560
(2008/02/09)
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- (3,4-DISUBSTITUTED)PROPANOIC CARBOXYLATES AS S1P (EDG) RECEPTOR AGONISTS
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The present invention encompasses compounds of Formula A: A as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.
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Page/Page column 105
(2008/06/13)
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- Design and Synthesis of New Templates Derived from Pyrrolopyrimidine as Selective Multidrug-Resistance-Associated Protein Inhibitors in Multidrug Resistance
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In our continued effort to identify selective MRP1 modulators, we have developed two novel templates, 3 and 4, through rational drug design by identifying the key pharmacophore interaction at the 7-position of the pyrrolopyrimidine template 1. Further syn
- Wang, Shouming,Wan, Nan Chi,Harrison, John,Miller, Warren,Chuckowree, Irina,Sohal, Sukhjit,Hancox, Timothy C.,Baker, Stewart,Folkes, Adrian,Wilson, Francis,Thompson, Deanne,Cocks, Simon,Farmer, Hayley,Boyce, Anthony,Freathy, Caroline,Broadbridge, Jan,Scott, John,Depledge, Paul,Faint, Richard,Mistry, Prakash,Charlton, Peter
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p. 1339 - 1350
(2007/10/03)
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- PYRROLOPYRIMIDINE DERIVATIVES AS MODULATORS OF MULTI-DRUG RESISTANCE (MDR)
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A compound which is a pyrrolopyrimidine of formula (I) wherein R1 is selected from H, Cl-C6 alkyl which is unsubstituted or substituted, (CH2)nAr1, (CH2)pNR4R5, halogen and (CH2)pX; R2 is CH2)pArl; R3 is selected from H, Cl -C6 alkyl which is unsubstituted or substituted, (CH2)pZ and (CH2)pArl; P is an unsaturated 5, 6, or 7 membered carbocyclic or heterocyclic ring which is unsubstituted or substituted; R4 and R5 which are the same or different are selected from H, Cl -C6 alkyl which is unsubstituted or substituted, (CH2)nC3-C10 cycloalkyl, (CH2)nAr1 , and (CH2)nOR6, or R4 and R5 together with the nitrogen atom to which they are attached, form a saturated five or six membered nitrogen containing heterocyclic ring which may contain one extra heteroatom selected from 0, N and S and which is unsubstituted or substituted; R6 is selected from H, Cl -C6 alkyl which is unsubstituted or substituted, C3-C10 cycloalkyl, (CH2)nOC1-C6alkyl which is unsubstituted or substituted, (CH2)nO(CH2)nAr1 , (CH2)nCO2C1-C6,alkyl which is unsubstituted or substituted and (CH2)nAr1; X is selected from CN, azide, (CH2)nNHSO2R6 and (CH2)nNHCOR6; Z is selected from CN, CO2R6 and CONR4R5; Ar1 is the same or different when more than one is present within a given substituent group and is an unsaturated C6-C10 membered carbocylic group or an unsaturated 5-11 membered heterocycle, either of which is unsubstituted or substituted; p is an integer of 1 to 6; n is the same or different when more than one is present within a given substituent group and is 0 or an integer of 1 to 6; with the proviso that the pyrrolepyrimidine compound of formula (I) is other than 1-(4-benzyl-piperazin-1-yl)-9H-2,4,9-triaza-fluorene; and the pharmaceutically acceptable salts thereof, have activity as inhibitors of MRP (multidrug resistant protein) and may thus be used to modulate multidrug resistance, for instance in potentiating the cytotoxicity of a chemotherapeutic agent.
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- Bicyclic fibrinogen antagonists
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PCT No. PCT/US95/00248 Sec. 371 Date Jul. 3, 1996 Sec. 102(e) Date Jul. 3, 1996 PCT Filed Jan. 9, 1995 PCT Pub. No. WO96/18619 PCT Pub. Date Jul. 13, 1995Certain compounds within formula (I) are inhibitors of platelet aggregation: wherein A1 is NH or CH2;
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- An Alternate Enantiospecific Synthesis of Methyl (S)-7-tert-Butoxycarbonyl-2,3,4,5-Tetrahydro-4-Methyl-3-Oxo-1H-1,4-Benzodiazepine-2-Acetate
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An alternate enantiospecific synthesis of methyl (S)-7-tert-butoxycarbonyl-2,3,4,5-tetrahydro-4-methyl-3-oxo-1H-1,4-benzodiazepine-2-acetate (5) is reported.The key step, which involves an intermolecular displacement of the activated aryl fluoride (9) by L-aspartic acid β-mehtyl ester, proceeds without racemization.
- Ku, Thomas W.,Ali, Fadia E.,Bondinell, William E.,Erhard, Karl F.,Huffmann, William F.,et al.
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p. 3131 - 3134
(2007/10/03)
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