- DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE
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Disclosed herein are novel bifunctional compounds formed by conjugating BTK inhibitor moieties with E3 ligase Ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof.
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Paragraph 0567-0569
(2021/09/17)
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- RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.
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- Preparation method for synthesizing 1-tert-butyloxycarbonyl -4-(4- carboxyphenyl) piperidine (by machine translation)
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The preparation method 1 - of synthesizing)-tert-butyloxycarbonyl - 4 4 4 4 4-carboxyphenyl, piperidine comprises the following steps: reacting dibromobenzene or iodobromide as raw material, with N - Boc - 4 - piperidone to obtain the target product 2, with intermediate 3, and preparing intermediate 3 by hydrogenation or hydrogenation to obtain the target product through intermediate 4, preparation intermediate 3 and carrying out hydrogenation reaction with the carbon dioxide to obtain the target product, which is, suitable for industrial production 4, in large, scale 5. by using common reagent, raw material cost, and the reaction is carried out with carbon dioxide. (by machine translation)
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Paragraph 0070-0072
(2020/05/05)
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- INHIBITORS OF ACTIVIN RECEPTOR-LIKE KINASE
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Described herein are compounds that inhibit ALK2 and its mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
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Page/Page column 278; 279
(2017/11/10)
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- METALLO-BETA-LACTAMASE INHIBITORS
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The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
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Paragraph 0336
(2016/12/01)
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- METALLO-BETA-LACTAMASE INHIBITORS
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The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
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Page/Page column 56
(2017/04/04)
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- HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS AND COMBINATIONS THEREOF
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Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.
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Page/Page column 100
(2015/07/07)
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- METALLO-BETA-LACTAMASE INHIBITORS
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The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
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Page/Page column 53; 54
(2015/08/06)
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- HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS
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Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds.
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Page/Page column 85
(2014/01/18)
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- Imidazopyridine-based fatty acid synthase inhibitors that show anti-HCV activity and in vivo target modulation
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Potent imidazopyridine-based inhibitors of fatty acid synthase (FASN) are described. The compounds are shown to have antiviral (HCV replicon) activities that track with their biochemical activities. The most potent analogue (compound 19) also inhibits rat FASN and inhibits de novo palmitate synthesis in vitro (cell-based) as well as in vivo.
- Oslob, Johan D.,Johnson, Russell J.,Cai, Haiying,Feng, Shirley Q.,Hu, Lily,Kosaka, Yuko,Lai, Julie,Sivaraja, Mohanram,Tep, Samnang,Yang, Hanbiao,Zaharia, Cristiana A.,Evanchik, Marc J.,McDowell, Robert S.
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supporting information
p. 113 - 117
(2013/02/26)
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- Synthesis and SAR study of diphenylbutylpiperidines as cell autophagy inducers
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A novel series of diphenylbutylpiperidines as autophagy inducers was described and extensive SAR studies resulted in derivatives (15d-e, 15i-j) with 10-fold greater activity than the lead compounds 1 and 2. Meanwhile, a new synthetic route to diphenylbutyl bromide (6) from bromobenzene and γ-butyrolactone was also reported here.
- Chen, Gang,Xia, Hongguang,Cai, Yu,Ma, Dawei,Yuan, Junying,Yuan, Chengye
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scheme or table
p. 234 - 239
(2011/02/26)
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- DIPHENYLBUTYPIPERIDINE AUTOPHAGY INDUCERS
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Autophagy inducing compounds, methods of their preparation and use, and kits containg said compounds are disclosed herein.
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Page/Page column 7; 84-85
(2011/12/02)
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- DIAZACARBAZOLES AND METHODS OF USE
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The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chkl) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
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Page/Page column 127
(2010/01/07)
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- INHIBITORS OF THE BMP SIGNALING PATHWAY
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The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation.
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Page/Page column 82-83
(2009/10/22)
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- HETEROCYCLIC COMPOUNDS AND USE THEREOF AS ERK INHIBITORS
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Disclosed are the ERK inhibitors of formula 1.0: [Formula (1.0)] and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
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Page/Page column 226
(2009/01/23)
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- Synthesis and structure-activity relationships of piperidine-based melanin-concentrating hormone receptor 1 antagonists
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Isosteric replacement of the urea group of lead compound 1 led to novel substituted piperidine phenylamide analogues. SAR on the electron-induced effects of various linkers as well as substituents on the phenyl rings and the piperidine nitrogen has been investigated. Many single-digit nanomolar MCH R1 antagonists have been identified from this series.
- Wu, Wen-Lian,Burnett, Duane A.,Spring, Richard,Qiang, Li,Sasikumar, Thavalakulamgara K.,Domalski, Martin S.,Greenlee, William J.,O'Neill, Kim,Hawes, Brian E.
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p. 3668 - 3673
(2007/10/03)
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- 2-Substituted benzimidazole piperidines analogs as selective melanin concentrating hormone receptor antagonists for the treatment of obesity and related disorders
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The present invention discloses compounds of formula I wherein Ar, Y, m, n, R1 and R4 are herein defined, said compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
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Page/Page column 33-34; 26
(2008/06/13)
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- Design and synthesis of orally active inhibitors of TNF synthesis as anti-rheumatoid arthritis drugs
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A novel series of TNF inhibitors was identified based on the screening of existing MMP inhibitor libraries. Further SAR optimization led to the discovery of a novel lead compound. Its synthesis, efficacy in experimental animal models, and pharmacokinetic
- Chen, Jian Jeffrey,Dewdney, Nolan,Lin, Xiaohong,Martin, Robert L.,Walker, Keith A. M.,Huang, Jane,Chu, Frances,Eugui, Elsie,Mirkovich, Anna,Kim, Yong,Sarma, Keshab,Arzeno, Humberto,Van Wart, Harold E.
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p. 3951 - 3954
(2007/10/03)
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- Hydroxamic acid derivatives as matrix metalloprotease (MMP) inhibitors
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Compounds of formula (I):or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diseases.
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- Fibrinogen receptor antagonists
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Novel fibrinogen receptor antagonists of the formula: are provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.
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