- Synthesis method of arylcyclobutane compound
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The present invention discloses a method for synthesizing an arylcyclobutane compound to 1eq phenylacetonitrile and 1.1eq 1-bromo-3-chloropropane as raw material, N,N- dimethylacetamide as a solvent, plus 2.5eq sodium hydride, under the protection of iner
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Paragraph 0033-0037; 0058-0061
(2022/01/10)
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- Iridium-Catalyzed Enantioselective C(sp3)–H Borylation of Cyclobutanes
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We herein report the first example of iridium-catalyzed enantioselective C(sp3)–H borylation of cyclobutanes using benzoxazoline as the directing group. The combination of a chiral bidentate boryl ligand and an iridium precursor has found to effectively catalyze C(sp3)–H borylation to afford a variety of cyclobutylboronates with good to excellent enantioselectivities. We also demonstrate the synthetic utility of the current method by converting the stereogenic C—B bond to other functionalities.
- Chen, Xiang,Chen, Lili,Zhao, Hongliang,Gao, Qian,Shen, Zhenlu,Xu, Senmiao
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supporting information
p. 1533 - 1537
(2020/09/09)
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- COMPOUNDS AND THEIR METHODS OF USE
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The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.
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Page/Page column 169-170
(2018/06/12)
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- ARYL HETEROCYCLIC PIPERIDINONE FORMYL PEPTIDE 2 RECEPTOR AND FORMYL PEPTIDE 1 RECEPTOR AGONISTS
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The disclosure relates to compounds of formula (I), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPRl) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the tr
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Page/Page column 22; 23
(2019/01/06)
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- Oxadiazole Amine Derivative Compounds as Histone Deacetylase 6 Inhibitor, and the Pharmaceutical Composition Comprising the same
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The present invention relates to a novel compound having an activity of inhibiting histone deacetylase 6 (HDAC6), an optical isomer thereof or a pharmaceutically acceptable salt thereof, a use thereof for preparation of a drug for treatment, a pharmaceutical composition comprising the same, a treatment method using the composition, and a method for preparing the same. The novel compound, an optical isomer thereof or a pharmaceutically acceptable salt thereof according to the present invention has an activity of inhibiting histone deacetylase 6 (HDAC6), and is effective for preventing or treating HDAC6-related diseases, including infectious diseases; neoplasm; endocrine, nutritional and metabolic diseases; mental and behavior disorders; nerve disorders; eye and adnexa diseases; cardiovascular diseases; respiratory diseases; digestive organ diseases; skin and subcutaneous tissue diseases; musculoskeletal and connective tissue diseases; or congenital malformation, deformation and chromosomal abnormality.COPYRIGHT KIPO 2017
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Paragraph 1332-1335
(2017/07/18)
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- Synthesis, SAR, and series evolution of novel oxadiazole-containing 5-lipoxygenase activating protein inhibitors: Discovery of 2-[4-(3-{(R)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]- N, N -dimethyl-acetamide (BI 665915)
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The synthesis, structure-activity relationship (SAR), and evolution of a novel series of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitors are described. The use of structure-guided drug design techniques provided compounds that demonstrated excellent FLAP binding potency (IC50 4 synthesis in human whole blood (IC50 4 production.
- Takahashi, Hidenori,Riether, Doris,Bartolozzi, Alessandra,Bosanac, Todd,Berger, Valentina,Binetti, Ralph,Broadwater, John,Chen, Zhidong,Crux, Rebecca,De Lombaert, Stéphane,Dave, Rajvee,Dines, Jonathon A.,Fadra-Khan, Tazmeen,Flegg, Adam,Garrigou, Michael,Hao, Ming-Hong,Huber, John,Hutzler, J. Matthew,Kerr, Steven,Kotey, Adrian,Liu, Weimin,Lo, Ho Yin,Loke, Pui Leng,Mahaney, Paige E.,Morwick, Tina M.,Napier, Spencer,Olague, Alan,Pack, Edward,Padyana, Anil K.,Thomson, David S.,Tye, Heather,Wu, Lifen,Zindell, Renee M.,Abeywardane, Asitha,Simpson, Thomas
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p. 1669 - 1690
(2015/04/21)
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- ANTITUMOR EFFECT POTENTIATOR COMPOSED OF IMIDAZOOXAZINE COMPOUND
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An antitumor effect potentiator for potentiating one or more other antitumor agents, comprising, as an active ingredient, an imidazooxazine compound represented by Formula (I), or a pharmaceutically acceptable salt thereof, wherein A, B, C, and D represen
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Paragraph 0169
(2015/05/19)
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- Identification of A Novel Small-Molecule Binding Site of the Fat Mass and Obesity Associated Protein (FTO)
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N-(5-Chloro-2,4-dihydroxyphenyl)-1-phenylcyclobutanecarboxamide (N-CDPCB, 1a) is found to be an inhibitor of the fat mass and obesity associated protein (FTO). The crystal structure of human FTO with 1a reveals a novel binding site for the FTO inhibitor and defines the molecular basis for recognition by FTO of the inhibitor. The identification of the new binding site offers new opportunities for further development of selective and potent inhibitors of FTO, which is expected to provide information concerning novel therapeutic targets for treatment of obesity or obesity-associated diseases.
- He, Wu,Zhou, Bin,Liu, Weijia,Zhang, Meizi,Shen, Zhenhua,Han, Zhifu,Jiang, Qingwei,Yang, Qinghua,Song, Chuanjun,Wang, Ruiyong,Niu, Tianhui,Han, Shengna,Zhang, Lirong,Wu, Jie,Guo, Feima,Zhao, Renbin,Yu, Wenquan,Chai, Jijie,Chang, Junbiao
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p. 7341 - 7348
(2015/10/05)
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- PROCESS OF PREPARING 3-(3-(4-(1-AMINOCYCLOBUTYL)PHENYL)-5-PHENYL-3H-IMIDAZO[4,5-B]PYRIDIN-2-YL)PYRIDIN-2-AMINE
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The present invention is directed to a processes for the synthesis of 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine:
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Paragraph 0169; 0170
(2015/11/03)
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- NOVEL IMIDAZO-OXAZINE COMPOUND OR SALT THEREOF
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The present invention provides an imidazooxazine compound represented by Formula (I) or a salt thereof, wherein A, B, C, and D are as defined in the specification.
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Paragraph 0247-0249
(2014/02/15)
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- Direct lactonization of 2-arylacetic acids through Pd(II)-catalyzed C-H activation/C-O formation
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Palladium-catalyzed direct lactonization of 2-arylacetic acids through a reaction sequence that includes C-H activation/C-O formation is reported. This method provides a concise and efficient pathway to synthesize fully functionalized benzofuranone derivatives, which are highly relevant to bioactive natural and synthetic products.
- Yang, Mingyu,Jiang, Xingyu,Shi, Wen-Juan,Zhu, Qi-Lei,Shi, Zhang-Jie
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supporting information
p. 690 - 693
(2013/04/10)
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- HETEROCYCLIC COMPOUNDS AS INHIBITORS OF LEUKOTRIENE PRODUCTION
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The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R7, A and HET are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes
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Paragraph 0263; 0264
(2013/08/14)
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- IL-23 ANTAGONISTS FOR TREATMENT OR PREVENTION OF SKIN RASH ASSOCIATED WITH TREATMENT WITH P13K/AKT PATHWAY INHIBITORS
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The present invention provides methods for use of interleukin-23 (IL-23) antagonists to treat or prevent skin rash associated with treatment with PI3K/AKT pathway inhibitors, such as treatment of cancer.
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Paragraph 00177
(2013/03/26)
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- OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION
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The present invention relates to compound of formula (I) and pharmaceutically acceptable salt thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
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Page/Page column 95
(2012/03/26)
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- BIARYLAMIDE INHIBITORS OF LEUKOTRIENE PRODUCTION
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The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, R1a, R1b, R2, R3, R4a and R4b are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
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Page/Page column 79
(2012/06/30)
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- INHIBITORS OF AKT ACTIVITY
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The instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
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Page/Page column 183-184
(2010/10/03)
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- Inhibitors of Akt activity
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The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
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Page/Page column 59
(2008/12/06)
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- BENZIMIDAZOLE DERIVATIVES USEFUL IN TREATMENT OF VALLINOID RECE TOR TRPVL RELATED DISORDERS
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The claimed invention provides benzimidazole derivatives antagonists of VRl, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds of Formula I may be used in the treatment of osteoarthritis,
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Page/Page column 78-79
(2008/06/13)
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