- Synthesis, Antibacterial and Anthelmintic Activity of Novel 3-(3-Pyridyl)-oxazolidinone-5-methyl Ester Derivatives
-
In this study, a series of 3-(3-pyridyl)-oxazolidone-5-methyl ester derivatives was synthesized and characterized by1H NMR,13C NMR, and LC-MS. The conducted screening antibacterial studies of the new 3-(3-pyridyl)-oxazolidone-5-methyl ester derivatives established that the methyl sulfonic acid esters have broad activity spectrum towards Staphylococcus aureus, Streptococcus pneu-moniae, Bacillus subtilis and Staphylococcus epidermidis. Among them, compound 12e has the most potent activity, with an MIC of 16 μg/mL against B.subtilis, and could reduce the instantaneous growth rate of bacteria. Furthermore, molecular docking studies were also simulated for compound 12e to predict the specific binding mode of this compound. In addition, anthelmintic activity of these compounds was also evaluated against adult Indian earthworms (Pheretima posthuman). The results showed that compound 11b had the best effect. These results above can provide experimental ref-erence for the development of novel antibacterial and anthelmintic drugs.
- Chen, Jia-Yi,Jin, Bo,Sheng, Zun-Lai,Sun, Meng-Qing,Yang, Hong-Liang
-
-
- COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
-
This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said che
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Page/Page column 241
(2021/07/10)
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- SMALL MOLECULE INHIBITORS OF GALECTIN-3
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The present disclosure relates to compounds of Formula (I), which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions. (Formula (I))
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Page/Page column 26-27
(2021/11/20)
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- TARGETED PROTEIN DEGRADATION
-
This invention provides pharmaceutical protein degraders and E3 ubiquitin ligase binders for therapeutic applications as described further herein.
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Page/Page column 327
(2020/07/14)
-
- Seeking potent anti-tubercular agents: Design and synthesis of substituted-: N -(6-(4-(pyrazine-2-carbonyl)piperazine/homopiperazine-1-yl)pyridin-3-yl)benzamide derivatives as anti-tubercular agents
-
Pyrazinamide is an important first-line drug used in shortening TB therapy. In our current work, a series of novel substituted-N-(6-(4-(pyrazine-2-carbonyl)piperazine/homopiperazine-1-yl)pyridin-3-yl)benzamide derivatives were designed, synthesized, and evaluated for their anti-tubercular activity against Mycobacterium tuberculosis H37Ra. Among the tested compounds, five compounds (6a, 6e, 6h, 6j and 6k) from Series-I and one compound (7e) from Series-II exhibited significant activity against Mycobacterium tuberculosis H37Ra with 50% inhibitory concentrations (IC50) ranging from 1.35 to 2.18 μM. To evaluate the efficacy of these compounds, we examined their IC90 values. Five of the most active compounds were found to be more active with IC90s ranging from 3.73 to 4.00 μM and one compound (6e) showed an IC90 of 40.32 μM. Moreover, single crystals were developed for 6d, 6f and 6n. In addition, most active compounds were evaluated for their cytotoxicity on HEK-293 (human embryonic kidney) cells. Our results indicate that the compounds are nontoxic to human cells. The molecular interactions of the derivatised conjugates in docking studies reveal their suitability for further development.
- Aggarwal, Himanshu,Calster, Kevin Van,Cappoen, Davie,Chandra Sekhar, Kondapalli Venkata Gowri,De Voogt, Linda,Ghosh, Balaram,Murugesan, Sankaranarayanan,Nandikolla, Adinarayana,Srinivasarao, Singireddi,Suresh, Amaroju
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p. 12272 - 12288
(2020/04/20)
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- 5-HETEROARYL SUBSTITUTED INDAZOLE-3-CARBOXAMIDES AND PREPARATION AND USE THEREOF
-
Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., tendinopathy, dermatitis, psoriasis, morphea, ichthyosis, Raynaud's syndrome, Darier's disease, scleroderma, cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.
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-
- HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Heterocyclic compounds as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
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-
Paragraph 0459-0461
(2019/04/25)
-
- N-heteroarylsulfonamide derivative, and preparation and application of same
-
The invention provides an N-heteroarylsulfonamide derivative, and preparation and an application of same. The derivative includes pharmaceutically acceptable salts and solvates thereof; a test provesthat the N-heteroarylsulfonamide derivative allows specific combination and inhibit or reduce the activity of potassium pathway Kv1.3, so that the derivative can be used for treating autoimmune diseases, caused by abnormal activation of the potassium pathway Kv1.3, of human or animal. An inhibitor in the invention also includes a medicinal composition of the compound. The invention also provides amethod for preparing the compound. The derivative has the general formula as the specification.
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Paragraph 0184; 0185; 0186; 0187
(2019/05/15)
-
- N/O-LINKED DEGRONS AND DEGRONIMERS FOR PROTEIN DEGRADATION
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This invention provides Degronimers that have E3 Ubiquitin Ligase targeting moieties (Degrons) that can be linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation. The invention also provides Degrons that can be used to treat disorders mediated by cereblon or an Ikaros family protein, and methods of use and compositions thereof as well as methods for their preparation.
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Page/Page column 323; 324
(2019/01/10)
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- METHODS OF USING INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/B-CATENIN SIGNALING PATHWAY INHIBITORS
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This disclosure features the use of one or more indazole-3-carboxamide compounds or salts or analogs thereof, in the treatment of one or more diseases or conditions independently selected from the group consisting of a tendinopathy, dermatitis, psoriasis, morphea, ichthyosis, Raynaud's syndrome, and Darier's disease; and/or for promoting wound healing. The methods include administering to a subject (e.g., a subject in need thereof) a therapeutically effective amount of one or more indazole-3-carboxamide compounds or salts or analogs thereof as described anywhere herein.
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Paragraph 0351; 0352
(2018/05/16)
-
- 5-SUBSTITUTED INDAZOLE-3-CARBOXAMIDES AND PREPARATION AND USE THEREOF
-
Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, fibrotic disorders, cartilage (chondral) defects, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, and neurological conditions/disorders/diseases linked to overexpression of DYRK1A.
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Paragraph 1294; 1295
(2015/11/09)
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- HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS AS INHIBITORS OF BTK ACTIVITY
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Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X, X, and Xare N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I foranddiagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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-
Paragraph 0753; 0754
(2015/11/16)
-
- Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors
-
The structure-activity relationship studies of a novel series of carboxylic acid derivatives of pyridine-carboxamides as DGAT-1 inhibitors is described. The optimization of the initial lead compound 6 based on in vitro and in vivo activity led to the disc
- Ting, Pauline C.,Lee, Joe F.,Zorn, Nicolas,Kim, Hyunjin M.,Aslanian, Robert G.,Lin, Mingxiang,Smith, Michelle,Walker, Scott S.,Cook, John,Van Heek, Margaret,Lachowicz, Jean
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p. 985 - 988
(2013/03/13)
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- Design and synthesis of novel antifungal triazole derivatives with good activity and water solubility
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In order to find novel antifungal agents with good activity and aqueous solubility, a series of SYN-2869 analogues containing a pyridine ring were synthesized and evaluated for their in vitro antifungal activity and water solubility. The results indicated that some compounds showed potent activity against six pathogenic fungi. In particular, the analogue 17a having an isobutyl substitution on the triazolone exhibited significant broad spectrum antifungal activity. In addition, the water solubility of compound 17a was sufficiently improved over SYN-2869.
- Cao, Xu-Feng,Chu, Wen-Jing,Cao, Yong-Bing,Yang, Yu-She
-
p. 303 - 306
(2013/07/04)
-
- INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/B-CATENIN SIGNALING PATHWAY INHIBITORS
-
lndazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole-3- carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
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-
Paragraph 00319
(2013/03/28)
-
- Identification of 2-aminooxazole amides as acyl-CoA: Diacylglycerol acyltransferase 1 (DGAT1) inhibitors through scaffold hopping strategy
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A scaffold hopping strategy was successfully applied in discovering 2-aminooxazole amides as potent DGAT1 inhibitors for the treatment of dyslipidemia. Further optimization in potency and PK properties resulted in a lead series with oral in vivo efficacy in a mouse postprandial triglyceridemia (PPTG) assay.
- Kim, Hyunjin M.,Smith, Michelle D.,Kim, Jae-Hun,Caplen, Mary Ann,Chan, Tin Yau,McKittrick, Brian A.,Cook, John A.,Van Heek, Margaret,Lachowicz, Jean
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p. 6410 - 6414
(2013/11/19)
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- SUBSTITUTED AMIDE DERIVATIVES AS DGAT-1 INHIBITORS
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Described herein are compounds of formula I. The compounds of formula I act as DGAT-1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
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Page/Page column 62
(2012/03/11)
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- Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability
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To improve antifungal activities, water solubility and bioavailability, a series of novel analogues of itraconazole-containing pyridine rings were designed and synthesized. Their antifungal activities were evaluated in vitro against six clinically important fungi by measuring the minimal inhibitory concentrations (MICs). Most of the compounds showed more potent antifungal activities than that of itraconazole. In particular, the analogues 30d, 30c, 31c, and 36d exhibited much higher solubility and bioavailability than that of itraconazole. The bioavailability of 36d (42.2%) was five times higher than that of itraconazole (8%) and was negative for genetic toxicology in the Ames test.
- Liu, Yu,Liu, Zining,Cao, Xufeng,Liu, Xin,He, Huili,Yang, Yushe
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scheme or table
p. 4779 - 4783
(2011/09/20)
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- INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE
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The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (DGAT) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below:
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Page/Page column 66-67
(2011/04/18)
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- Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes
-
Diacylglycerol acyltransferase-1 (DGAT-1) is the enzyme that catalyzes the final and committed step of triglyceride formation, namely, the acylation of diacylglycerol with acyl coenzyme A. DGAT-1 deficient mice demonstrate resistance to weight gain on hig
- Qian, Yimin,Wertheimer, Stanley J.,Ahmad, Mushtaq,Cheung, Adrian Wai-Hing,Firooznia, Fariborz,Hamilton, Matthew M.,Hayden, Stuart,Li, Shiming,Marcopulos, Nicholas,McDermott, Lee,Tan, Jenny,Yun, Weiya,Guo, Liang,Pamidimukkala, Anjula,Chen, Yingsi,Huang, Kuo-Sen,Ramsey, Gwendolyn B.,Whittard, Toni,Conde-Knape, Karin,Taub, Rebecca,Rondinone, Cristina M.,Tilley, Jefferson,Bolin, David
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scheme or table
p. 2433 - 2446
(2011/06/17)
-
- Synthesis and solid state study of pyridine- and pyrimidine-based fragment libraries
-
A library of pyridines and pyrimidines has been synthesised in excellent yields employing microwave and flow chemistry methodologies. Work-up bottlenecks have been facilitated substantially by the use of supported reagents and many of the final compounds have been studied in the solid state by single crystal X-ray diffraction.
- Spencer, John,Patel, Hiren,Callear, Samantha K.,Coles, Simon J.,Deadman, John J.
-
supporting information; experimental part
p. 5905 - 5909
(2011/11/14)
-
- INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE
-
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below.
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Page/Page column 182
(2010/07/10)
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- THIAZOLE SULFONAMIDE AND OXAZOLE SULFONAMIDE KINASE INHIBITORS
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The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents
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Page/Page column 115
(2010/10/03)
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- THIAZOLE AND OXAZOLE KINASE INHIBITORS
-
The present invention provides thiazole and oxazole compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
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Page/Page column 149-150
(2009/04/25)
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- STEAROYL COA DESATURASE INHIBITORS
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The present invention relates to novel Stearoyl CoA desaturase (SCD) inhibitors and uses thereof for treating diseases, conditions and/or disorders modulated by a Stearoyl CoA desaturase enzyme. The SCD inihibitors have the formula (I) or a pharmaceutical
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Page/Page column 26-27
(2010/11/30)
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- DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS
-
Provided herein are compounds of the formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
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Page/Page column 47
(2009/01/20)
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- PYRROLIDINE DERIVATIVES AS ERK INHIBITORS
-
Disclosed are the ERK inhibitors of Formula (1.0): and the pharmaceutically acceptable salts 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 195
(2010/11/28)
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- UREA DERIVATIVE
-
The present invention relates to a urea derivative or a pharmacologically acceptable salt thereof having an excellent DGAT inhibitory effect. A urea derivative having the formula: [wherein R 1 is a C 6 -C 10 aryl group which may be independently mono- to pentasubstituted by a group selected from Substituent Group a or others; R 2 is a C 6 -C 10 aryl group which may be independently mono- to pentasubstituted by a group selected from Substituent Group a or others; E is a group having the formula (II) or the formula (III) (wherein R 3 is a hydrogen atom or others; R 4 and R 5 , which are the same or different, are a hydrogen atom or others; X and U, which are the same or different, are a group represented by the formula CH or others; m and n, which are the same or different, are 1 or another number) or others; and A is a group represented by the formula -NH-C(=O)- or others], or a pharmacologically acceptable salt thereof.
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Page/Page column 105
(2010/11/26)
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- KINASE INHIBITORS
-
The present invention provides kinase inhibitors of Formula (I). Wherein R1, R2, X and Z are as described herein, or a pharmaceutically acceptable salt thereof.
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Page/Page column 14
(2010/11/27)
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- COMPOUNDS
-
The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R1, n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
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Page/Page column 43
(2010/11/23)
-
- PIPERAZINE DERIVATIVES AS GLYT1 INHIBITORS
-
The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R1, n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
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Page/Page column 53
(2010/11/23)
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- HETEROCYCLIC TRIAZINES AS HYPOXIC SELECTIVE PROTEIN KINASE INHIBITORS
-
The invention relates to novel heterocyclic triazines which are useful as hypoxic selective cytotoxic agents that mediate and/or inhibit cell proliferation, for example, through the activity of protein kinases. The invention is further related to pharmaceutical compositions containing such compounds and compositions, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation by administering effective amounts of such compounds.
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Page/Page column 50
(2010/11/25)
-
- 2-(Pyridin-3-ylamino)-pyrido[2,3-D]pyrimidin-7-ones
-
This invention provides compounds of formula I: wherein R1, R2, R3, R4, and X1 are as defined in the specification. The 2-(pyridin-3-ylamino)-pyrido[2,3-d]pyrimidin-7-one compounds of formula I, which are inhibitors of cyclin-dependent kinases 2 and 4 (CDK2 and CDK4), are useful in treating cell proliferative disorders.
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Page/Page column 9; 12
(2008/06/13)
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- OXAZOLIDINONE DERIVATIVES AS ANTIBACTERIAL AGENTS
-
The present invention provides novel compounds of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmac
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-
-
- Bioisosteric bensamide derivatives and their use as apob-100 secretion inhibitors
-
The present invention relates to A compound of formula (I) wherein A, U, V, X, Z, R1, Y, R2 and R3 are defined in the description or a physiologically acceptable salt, solvate or derivative thereof, to compositions and pro
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Page/Page column 10
(2010/02/05)
-
