- 4-Anilino-pyrimidine, novel aldosterone synthase (CYP11B2) inhibitors bearing pyrimidine structures
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2,2,2-Trifluoro-1-{4-[(4-fluorophenyl)amino]pyrimidin-5-yl}-1-[1-(methylsulfonyl)piperidin-4-yl]ethanol 1 was identified as a novel potent aldosterone synthase inhibitor. Despite large species differences, compound 1 inhibits both human and rodent CYP11B2 in a nano-molar range.
- Meguro, Masaki,Miyauchi, Satoru,Kanao, Yukiko,Naito, Satoru,Suzuki, Kanae,Inoue, Shinichi,Yamada, Keisuke,Homma, Tsuyoshi,Chiba, Kiyoshi,Nara, Futoshi,Furuzono, Shinji
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Read Online
- Intramolecular Metal-Free N?N Bond Formation with Heteroaromatic Amines: Mild Access to Fused-Triazapentalene Derivatives
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Formation of N?N bonds may offer an original approach to various nitrogen-containing heterocycles with numerous applications. For this purpose, we found that readily available heteroaromatic amines are appropriate substrates for providing an efficient and innovative approach for the formation of N?N bonds in the presence of iodine (III) reagent in very mild conditions. This method makes it possible to synthesize nitrogen rich triazapentalene derivatives exhibiting fluorescent properties, inaccessible with existing approaches.
- Daniel, Matthieu,Hiebel, Marie-Aude,Guillaumet, Gérald,Pasquinet, Eric,Suzenet, Franck
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supporting information
p. 1525 - 1529
(2020/02/05)
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- Hetero-aromatic compound and its use in medicine
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The invention provides a hetero-aromatic compound or a stereisomer, geometric isomer, tautomer, despinner, nitrogen oxide, hydrate, solvate, metabolite, metabolism precursor and pharmaceutically acceptable salt or prodrug thereof, which is used for treating proliferative diseases. The invention also discloses a pharmaceutical composition containing the compound and an application of the compound or pharmaceutical composition thereof in preparation of a medicine for treating proliferative diseases.
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Paragraph 0989; 0992-0993
(2019/07/04)
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- PYRROLOTRIAZINONE DERIVATIVES AS PI3K INHIBITORS
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New pyrrolotriazinone derivatives having the chemical structure of formula (I), are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks)
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Page/Page column 139; 140
(2014/05/07)
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- Aurora kinase modulators and method of use
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The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R1- are defined herein, and synthetic intermediates, which
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Page/Page column 47
(2008/06/13)
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- Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors
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Anilinoalkynylpyrimidines were prepared and evaluated as dual EGFR/ErbB2 kinase inhibitors. A preference was found for substituted phenyl and heteroaromatic rings attached to the alkyne. In addition, the presence of a potential hydrogen bond donor appende
- Waterson, Alex G.,Stevens, Kirk L.,Reno, Michael J.,Zhang, Yue-Mei,Boros, Eric E.,Bouvier, Frederic,Rastagar, Abdullah,Uehling, David E.,Dickerson, Scott H.,Reep, Bryan,McDonald, Octerloney B.,Wood, Edgar R.,Rusnak, David W.,Alligood, Krystal J.,Rudolph, Sharon K.
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p. 2419 - 2422
(2007/10/03)
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- CHEMICAL COMPOUNDS
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The present invention discloses pyrimidine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such pyrimidine derivatives are useful in the treat
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Page/Page column 44
(2010/02/10)
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- STEROID SPARING AGENTS AND METHODS OF USING SAME
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This invention relates generally to the use of a steroid sparing agent for the preparation of a medicament for the treatment of inflammatory bowel diseases (IBD), asthma, multiple sclerosis (MS), rheumatoid arthritis (RA), graft versus host disease (GVHD), host versus graft disease, and various spondyloarthropathies, comprising administering a steroid sparing immunoglobulin or small molecule composition to a patient in need thereof. The invention also relates generally to combination therapies for the treatment of these conditions.
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Page/Page column 527; 553; 554; 556
(2010/02/14)
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- 3-(Heteroaryal) alanine derivatives-inhibitors of leukocyte adhesion mediated by VLA-4
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Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
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- CONDENSED HETEROAROMATIC RING SYSTEMS. VII. SYNTHESIS OF THIENOPYRIDINES, THIENOPYRIMIDINES, AND FUROPYRIDINES FROM o-SUBSTITUTED N-HETEROARYLACETYLENES
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The cross-coupling reaction of 2-chloro-3-iodo- and 4-chloro-3iodopyridines with phenylacetylene in the presence of dichlorobis(triphenylphosphine)palladium occured at the 3-position.The 3-ethynylpyridines containing an adjacent chloro group were converti
- Sakamoto, Takao,Kondo, Yoshinori,Watanabe, Ryo,Yamanaka, Hiroshi
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p. 2719 - 2724
(2007/10/02)
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