- Co(II)-Catalyzed Regioselective Pyridine C-H Coupling with Diazoacetates
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A Co(II)-catalyzed pyridyl C-H bond carbenoid insertion with α-diazoacetates has been realized. This transformation features a highly regioselective C-C bond formation at the C3-position of pyridines, providing an efficient access to diverse α-aryl-α-pyri
- Xie, Haisheng,Shao, Youxiang,Gui, Jiao,Lan, Jianyong,Liu, Zhipeng,Ke, Zhuofeng,Deng, Yuanfu,Jiang, Huanfeng,Zeng, Wei
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supporting information
(2019/05/08)
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- Inverting Conventional Chemoselectivity in Pd-Catalyzed Amine Arylations with Multiply Halogenated Pyridines
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A new catalyst system capable of selective chloride functionalization in the Pd-catalyzed amination of 3,2- and 5,2- Br/Cl-pyridines is reported. A reaction optimization strategy employing ligand parametrization led to the identification of 1,1′-bis[bis(dimethylamino)phosphino]ferrocene "DMAPF", a readily available yet previously unutilized diphosphine, as a uniquely effective ligand for this transformation.
- Keylor, Mitchell H.,Niemeyer, Zachary L.,Sigman, Matthew S.,Tan, Kian L.
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supporting information
p. 10613 - 10616
(2017/08/15)
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- NOVEL CHEMICAL COMPOUNDS (VARIANTS) AND THE USE THEREOF TO TREAT ONCOLOGICAL DISEASES
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The invention relates to novel chemical compounds of general formula I, in which L A , L B , L C , ring A, ring B, R A , R B , R C ,R D ,R E and R F have are defined in the description, and which are protein kinases inhibitors. The invention also relates
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Paragraph 0310; 0311
(2016/10/08)
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- TRIAZOLE COMPOUNDS AS T-TYPE CALCIUM CHANNEL BLOCKERS
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The invention relates to compounds of formula (I) wherein X, Y, R1, R2, (R4)n, and (R5)m are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium T-channel blockers.
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Page/Page column 49
(2016/04/09)
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- ALLOSTERIC MODULATORS OF THE CANNIBINOID 1 RECEPTOR
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The present technology relates to compounds and compositions of Formulas I, II, VII, and VIII, and methods using such compounds. The compounds and compositions described herein may be used in the treatment or prophylaxis of addiction, metabolic syndrome, obesity, and/or a CB1 receptor-medited disorder.
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Paragraph 0245
(2015/03/13)
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- PYRAZOLE COMPOUNDS AND THEIR USE AS T-TYPE CALCIUM CHANNEL BLOCKERS
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The invention relates to compounds of formula (I) Formula (I) wherein X, Y, R1, R2, (R4)n, and (R5)m are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium T-channel blockers.
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Page/Page column 88
(2015/12/24)
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- 5, 7-DIHYDRO- 6H-PYRIMIDO [ 5, 4-D] [ 1 ] BENZAZEPIN-6-THIONES AS PLK INHIBITORS
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This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
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Page/Page column 110
(2010/06/20)
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- BICYCLIC AROMATIC COMPOUNDS USEFUL AS INHIBITORS OF MITOGEN-ACTIVATED PROTEIN KINASE-ACTIVATED PROTEIN KINASE-2
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A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the groups R1-R6, A and Y are as defined in the specification, as inhibitors of (MK2 or MAPKAP kinase-2).
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Page/Page column 58
(2008/06/13)
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- Methods for the synthesis of 5,6,7,8-tetrahydro-1,8-naphthyridine fragments for αvβ3 integrin antagonists
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The preparation of 3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propan-1- amine 2a and 3-[(7R)-7-methyl-5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl]propan-1- amine 2b, key intermediates in the synthesis of αvβ 3 antagonists, is described. The syntheses rely on the efficient double Sonogashira reactions of 2,5-dibromopyridine 3 with acetylenic alcohols 4a/4b and protected propargylamines 10a-e followed by Chichibabin cyclizations of 3,3′-pyridine-2,5-diyldipropan-1-amines 9a/9b.
- Hartner, Frederick W.,Hsiao, Yi,Eng, Kan K.,Rivera, Nelo R.,Palucki, Michael,Tan, Lushi,Yasuda, Nobuyoshi,Hughes, David L.,Weissman, Steven,Zewge, Daniel,King, Tony,Tschaen, Dave,Volante
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p. 8723 - 8730
(2007/10/03)
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- BENZAMIDINE DERIVATIVES
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Benzamidine derivatives of the following formulae or analogs thereof, i. e., pharmaceutically acceptable salts thereof, are provided. These compounds or salts thereof have a blood-coagulation inhibiting effect based on an excellent effect of inhibiting the action of activated blood coagulation factor X, and they are useful as anticoagulants.
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