- ADENOSINE RECEPTOR BINDING COMPOUNDS
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The present invention relates to pharmaceutical compounds and compositions of Formula (I) and methods of treatment using the compounds and compositions, especially for the treatment and/or prevention of a proliferation disorder, such as cancer. Compounds of Formula (I) as further described herein are shown modulators of the adenosine A2A receptor and exhibit antiproliferative activity. Accordingly, these compounds are useful to treat proliferative disorders such as cancer, and other adenosine receptor-related conditions including an inflammatory disease, renal disease, diabetes, vascular disease, lung disease, or an autoimmune disease.
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Paragraph 00648-00649
(2020/02/06)
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- Synthesis of 2-Pyridinemethyl Ester Derivatives from Aldehydes and 2-Alkylheterocycle N-Oxides via Copper-Catalyzed Tandem Oxidative Coupling-Rearrangement
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Successful benzylic C(sp3)-H acyloxylation of 2-alkylpyridine, 2-alkylpyrazine, and 2-alkylthiazole compounds was achieved using simple aldehydes. This was carried out via a copper-catalyzed tandem reaction, involving oxidative esterification followed by O-atom transfer of the resultant high yield formed Boekelheide intermediate. The method enables the preparation of functional heterocycles and the desymmetrization of 2,6-dialkylpyridines for efficient synthesis of dissymmetric pincer ligands, thus offering a new life for more practical Boekelheide rearrangement.
- Wang, Chang-Sheng,Roisnel, Thierry,Dixneuf, Pierre H.,Soulé, Jean-Fran?ois
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supporting information
p. 6720 - 6723
(2017/12/26)
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- NOVEL COMPOUND, ORGANIC CATION TRANSPORTER 3 DETECTION AGENT, AND ORGANIC CATION TRANSPORTER 3 ACTIVITY INHIBITOR
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[Problem] The present invention addresses the problem of providing a novel compound. The present invention also addresses the problem of providing an OCT3 detection agent or an OCT3 activity inhibitor, which comprises the novel compound. [Solution] A compound represented by formula (A), a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof. ????????R1-R2-R3-R4?????(A)
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- SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS beta-SECRETASE INHIBITORS
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The present invention is directed to substituted imidazo[1,2-a]pyridine derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit beta-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which BACE is involved.
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Page/Page column 45-47
(2010/11/17)
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- Metallo-controlled dynamic molecular tweezers: Design, synthesis, and self-assembly by metal-ion coordination
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The introduction of controllable dynamic features into synthetic receptors represents a step towards "smart" adaptive nanodevices. We report herein our studies on the construction of dynamic molecular tweezers in which the binding of a substrate is allost
- Ulrich, Sebastien,Petitjean, Anne,Lehn, Jean-Marie
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p. 1913 - 1928
(2011/01/10)
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- SELECTIVE INHIBITORS AGAINST Cdk4 AND Cdk6 HAVING AMINOTHIAZOLE SKELETON
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The present invention relates to a compound represented by Formula [I]: wherein X is O, S, NH or CH 2 ; Y 1 , Y 2 , Y 3 , Y 4 and Y 5 , which may be identical or different, are each CH or N; however, at least one of Y 1 , Y 2 , Y 3 , Y 4 and Y 5 is N; Z 1 and Z 2 , which may be identical or different, are each CH or N; n is an integer from 1 to 3; R 1 is a C 3 -C 8 cycloalkyl group, a C 6 -C 10 aryl group, an aliphatic heterocyclic ring or an aromatic heterocyclic ring, or a bicyclic aliphatic saturated hydrocarbon group; R 2 and R 3 , which may be identical or different, are each a hydrogen atom, a lower alkyl group, a lower alkenyl group, a C 3 -C 8 cycloalkyl group, a C 6 -C 10 aryl group, an aromatic heterocyclic ring, or the like; and R 4 is a hydrogen atom, a lower alkyl group, a C 3 -C 6 cycloalkyl group or the like, or a pharmaceutically acceptable salt or ester thereof, and a selective inhibitor against Cdk4 and/or Cdk6 or an anticancer agent containing the compound or a pharmaceutically acceptable salt or ester thereof.
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Page/Page column 89
(2010/11/25)
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- NOVEL COMPOUNDS OF AMINO SULFONYL DERIVATIVES
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The present invention relates to compounds with formula (I) or a pharmaceutically acceptable salt thereof: (I);wherein; T is a (4 to 10)-membered heterocyclyl and wherein R1, R2 and R3 are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of the 11-β-hsd-1 enzyme.
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- N-(PYRIDIN-2-YL)-SULFONAMIDE DERIVATIVES
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The present invention relates to novel compounds, to pharmaceutical compositions comprising the compounds described herein, their pharmaceutically acceptable salts, hydrates and solvates, as well as to the use of the compounds in medicine and for the prep
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Page/Page column 34
(2008/06/13)
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- 1, 3, 4-BENZOTRIAZEPIN-2-ONE SALTS AND THEIR USE AS CCK RECEPTOR LIGANDS
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This invention relates to pharmaceutically acceptable salts of compounds of formula (I) wherein: W is N or N+-O-; R2 is an optionally substituted C1 to C18 hydrocarbyl group wherein up to three C atoms may optionally be replaced by N, O and/or S atoms. R3 is -(CR11R12)m-X-(CR13R14)p-R9; m is 0, 1, 2, 3 or 4; p is 0, 1 or 2; X is a bond, -CR15=CR16-, -C≡C-, C(O)NH, NHC(O), C(O)NMe, NMeC(O), C(O)O, NHC(O)NH, NHC(O)O, OC(O)NH, NH, O, CO, SO2, SO2NH, C(O)NHNH, R9 is H ; C1 to C6 alkyl ; or phenyl, naphthyl, pyridyl, benzimidazolyl, indazolyl, quinolinyl, isoquinolinyl, tetrahydroisoquinolinyl, indolinyl, isoindolinyl, indolyl, isoindolyl or 2-pyridonyl substituted with -L-Q. R4 is an optionally substituted C1 to C18 hydrocarbyl group wherein up to three C atoms may optionally be replaced by N, O and/or S atoms ; and Such salts are useful, for example, for the treatment of gastrin related disorders.
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- Tyrosine kinase inhibitors
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The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
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- N-bromosuccinimide reactions of some heterocycles in the presence or absence of water: An overview of ring versus side chain bromination for the synthesis of important brominated heterocyclic synthons
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Reactions of various heterocycles 1-6 with N-bromosuccinimide in the presence or absence of water have been studied for side chain versus ring bromination to afford some new and important heterocyclic synthons. Interestingly, the N-bromosuccinimide reaction in the presence of perchloric acid, a new condition, affords exclusively the new dibromo aminopicoline 1f, which is not obtained by other presently studied methods.
- Goswami,Ghosh,Mukherjee,Avijit Kumar Adak,Ajit Kumar Mahapatra
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p. 173 - 178
(2007/10/03)
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- Synthesis of artificial receptors as potential candidates for recognition and binding of pterin analogs
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Open chain podands 2a-c and macrocycles 2d-e have been synthesized as potential candidates for 4-aminopterin recognition and binding, featuring H-bonding characteristics and 'stacking interaction' 2e. Preliminary binding studies between 6, 7, and 8 (simpler analogs of the above 2a-e) as 'hosts' and appropriate 'guests', showed that carbamates 2a and 2e are the most promising receptors for 4-aminopterin binding.
- Papadopoulou,Goswami,Hamilton
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p. 675 - 681
(2007/10/02)
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- Triazolopyridines. 14. Substitution Reactions of 7-AminoTriazoloPyridines
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Reaction between 7-aminotriazolopyridines 1 or 2 and sulphuric acid gives hydroxyalkylpyridines 3 and 4; bromination gives brominated pyridine 5 or triazolopyridine 6.The anions from 1 or 2 are ambient, acylating on N but alkylating on N or on C6; in the latter case triazolylalkenylcyanides 16 - 20 or the 6,6-dialkylated derivative 19 are obtained.An X-ray diffraction study has confirmed structure 19. Key Words: Aminotriazolopyridines; Ambident Anions; Alkylation/Acylation; Triazolylalkenyl Cyanides; X-ray Diffraction.
- Asensio, Amparo,Abarca, Belen,Jones, Gurnos,Hursthouse, Michael B.,Malik, K. M. Abdul
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p. 703 - 712
(2007/10/02)
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- HALOGUANIDINE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND METHOD OF USE
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Compounds useful for inhibiting gastric acid secretion and for the treatment of peptic ulcers caused or exacerbated by gastric acidity having the following formula (I): STR1 in which R 1 and R 2, are H, C 1-10 alkyl, C 3-8 cycloalkyl or cycloalkylalkyl in which the alkyl part is C 1-6 and the cycloalkyl part is C 3-8, each of the alkyl, cycloalkyl and cycloalkylalkyls being optionally substituted by one or more halogens selected from F, Cl and Br, provided that at least one of R 1 and R 2 is a halogen substituted alkyl, cycloalkyl or cycloalkylalkyl and provided that there is no halogen substituent on the carbon directly attached to the nitrogen; and X, m, Y, n and R 3 are as described in the specification; and the pharmaceutically-acceptable acid-addition salts thereof. Processes for producing compounds of formula (I), pharmaceutical compositions containing them, methods of utilizing such compositions and intermediates useful for synthesizing compounds of formula (I) are also described.
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