cas 151982-51-3, 4-BROMO-2-FLUOROBENZOYL CHLORIDE

Articles about 151982-51-3Total 51 be found

Article title
Article abstract
Author
Journal number and time
Download

Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu4 positive allosteric modulators that mitigate CYP1A2 induction liability
Previous reports from our laboratory disclosed the structure and activity of a novel 1H-pyrazolo[4,3-b]pyridine-3-amine scaffold (VU8506) which showed excellent potency, selectivity and in vivo efficacy in preclinical rodent models of Parkinson's disease.
Engers, Darren W.,Bollinger, Sean R.,Engers, Julie L.,Panarese, Joseph D.,Breiner, Megan M.,Gregro, Alison,Blobaum, Anna L.,Bronson, Joanne J.,Wu, Yong-Jin,Macor, John E.,Rodriguez, Alice L.,Zamorano, Rocio,Conn, P. Jeffrey,Lindsley, Craig W.,Niswender, Colleen M.,Hopkins, Corey R.
p. 2641 - 2646
(2018)
Read Online

PIPERAZINE SUBSTITUTED AZAPINE DERIVATIVES AND USES THEREOF
The present disclosure relates to compounds of Formula (I) and (II): and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for modulating H1 and 5-HT2A receptors and are to be used in the treatment of sleep disorders, such as sleep fragmentation, disturbed sleep/arousals, and arousal threshold.
-
Paragraph 0980-0982

(2021/04/23)

Method for synthesizing high-purity tert-butyl 2-fluoro-4-bromobenzoate
The invention discloses a method for synthesizing high-purity tert-butyl 2-fluoro-4-bromobenzoate, which comprises the following steps: synthesizing a compound 2-fluorine-4-bromobenzoyl chloride from 2-fluorine-4-bromobenzoic acid, then synthesizing the t
-
Paragraph 0027

(2021/08/19)

Structure-activity relationships of agonists for the orphan G protein-coupled receptor GPR27
GPR27 belongs, with GPR85 and GPR173, to a small subfamily of three receptors called “Super-Conserved Receptors Expressed in the Brain” (SREB). It has been postulated to participate in key physiological processes such as neuronal plasticity, energy metabolism, and pancreatic β-cell insulin secretion and regulation. Recently, we reported the first selective GPR27 agonist, 2,4-dichloro-N-(4-(N-phenylsulfamoyl)phenyl)benzamide (I, pEC50 6.34, Emax 100%). Here, we describe the synthesis and structure-activity relationships of a series of new derivatives and analogs of I. All products were evaluated for their ability to activate GPR27 in an arrestin recruitment assay. As a result, agonists were identified with a broad range of efficacies including partial and full agonists, showing higher efficacies than the lead compound I. The most potent agonist was 4-chloro-2,5-difluoro-N-(4-(N-phenylsulfamoyl)phenyl)benzamide (7y, pEC50 6.85, Emax 37%), and the agonists with higher efficacies were 4-chloro-2-methyl-N-(4-(N-phenylsulfamoyl)phenyl)benzamide (7p, pEC50 6.04, Emax 123%), and 2-bromo-4-chloro-N-(4-(N-phenylsulfamoyl)phenyl)benzamide (7r, pEC50 5.99, Emax 123%). Docking studies predicted the putative binding site and interactions of agonist 7p with GPR27. Selected potent agonists were found to be soluble and devoid of cellular toxicity within the range of their pharmacological activity. Therefore, they represent important new tools to further characterize the (patho)physiological roles of GPR27.
Blavier, Jeremy,Charles, Ma?lle,Hanson, Julien,Kronenberger, Thales,Laschet, Céline,Müller, Christa E.,Pillaiyar, Thanigaimalai,Rosato, Francesca,Wozniak, Monika
(2021/08/27)

CRYSTALLINE HYDRATE OF A JAK INHIBITOR COMPOUND
Provided herein is a crystalline hydrate of the compound of formula 1: Also provides herein are pharmaceutical compositions comprising such crystalline hydrate, methods of using such crystalline hydrate to treat respiratory diseases, and processes useful
-
Paragraph 0177-0178

(2021/09/03)

NOVEL HETEROAROMATIC COMPOUNDS EXHIBITING ANTIFUNGAL ACTIVITY AND THEIR METHOD OF USE
Pharmaceutical compositions of the invention comprise herteroaromatic compounds having a disease-modifying action in the treatment of fungal infections and diseases associated with fungal infection.
-
Paragraph 0820-0821

(2021/12/28)

Hit-to-Lead Optimization of Benzoxazepinoindazoles As Human African Trypanosomiasis Therapeutics
Human African trypanosomiasis (HAT) is a neglected tropical disease caused by infection with either of two subspecies of the parasite Trypanosoma brucei. Due to a lack of economic incentive to develop new drugs, current treatments have severe limitations in terms of safety, efficacy, and ease of administration. In an effort to develop new HAT therapeutics, we report the structure-activity relationships around T. brucei for a series of benzoxazepinoindazoles previously identified through a high-throughput screen of human kinase inhibitors, and the subsequent in vivo experiments for HAT. We identified compound 18, which showed an improved kinase selectivity profile and acceptable pharmacokinetic parameters, as a promising lead. Although treatment with 18 cured 60% of mice in a systemic model of HAT, the compound was unable to clear parasitemia in a CNS model of the disease. We also report the results of cross-screening these compounds against T. cruzi, L. donovani, and S. mansoni.
Klug, Dana M.,Tschiegg, Laura,Diaz, Rosario,Rojas-Barros, Domingo,Perez-Moreno, Guiomar,Ceballos, Gloria,García-Hernández, Raquel,Martinez-Martinez, Maria Santos,Manzano, Pilar,Ruiz, Luis Miguel,Caffrey, Conor R.,Gamarro, Francisco,Pacanowska, Dolores Gonzalez,Ferrins, Lori,Navarro, Miguel,Pollastri, Michael P.
p. 2527 - 2546
(2019/11/28)

PROCESS FOR PREPARING JAK INHIBITORS AND INTERMEDIATES THEREOF
The invention is directed to a process for preparing compounds which are useful as intermediates for the preparation of medicinal agents having inhibitory activity for JAK.
-
Paragraph 0101; 0102

(2020/03/23)

DIMETHYL AMINO AZETIDINE AMIDES AS JAK INHIBITORS
The invention provides compounds of formula (I): where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions compris
-
Paragraph 0146-0147

(2020/03/23)

Discovery of methoxy-naphthyl linked N-(1-benzylpiperidine) benzamide as a blood-brain permeable dual inhibitor of acetylcholinesterase and butyrylcholinesterase
The cholinesterase enzymes play a vital role in maintaining balanced levels of the neurotransmitter acetylcholine in the central nervous system. However, the overexpression of these enzymes results in hampered neurotransmission. Both the major forms of cholinesterase enzymes viz. acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) play a crucial role in blocking neurotransmission; therefore, in recent years, a strategy of dual cholinesterase inhibition is being explored. Herein, we developed an energy-optimized e-pharmacophore hypothesis AHHPRR from AChE-donepezil complex and screened a set of 15 scaffolds that were designed imaginarily. The ligand with N-(1-benzylpyridinium) benzamide framework has shown the highest fitness and volume score, which was chosen for synthesis and validation. A series of pyridinium benzamides were synthesized and screened for cholinesterase inhibition that led to the identification of 7b, a naphthalene containing N-(1-benzylpiperidine) benzamide as a potent dual AChE and BChE inhibitor with IC50 values of 0.176, and 0.47 μM, respectively. The kinetic study indicated that 7b inhibits AChE in a non-competitive manner with Ki value of 0.21 μM, and BChE in a mixed-fashion with Ki of 0.15 μM. The observed mode of inhibition was corroborated with molecular docking studies. The MD simulation studies pointed out that both AChE and BChE undergo low conformational changes in complex with 7b. The benzamide 7b displayed high BBB permeability in PAMPA assay, which indicates its potential for further exploration in preclinical studies for Alzheimer's disease.
Abdullaha, Mohd,Bharate, Sandip B.,Nuthakki, Vijay K.
(2020/09/18)

NON-FUSED THIOPHENE DERIVATIVES AND THEIR USES
The present invention relates to a new class of non-fused thiophene derivatives and their uses for treating diseases such as infection, cancer, metabolic diseases, cardiovascular diseases, iron storage disorders and inflammatory disorders.
-
Page/Page column 104-105

(2019/08/29)

Method for synthesizing enzalutamide intermediate
The invention discloses a method for synthesizing an enzalutamide intermediate. The method is characterized by comprising the following steps: adding 4-bromo-2-fluorobenzoic acid and sulfoxide chloride into an organic solvent, evacuating and introducing nitrogen, and carrying out a reaction at a temperature of 80-100 DEG C; evaporating the solvent to dryness so as to obtain 4-bromo-2-fluorobenzoylchloride after the reaction ends, adding the organic solvent into the 4-bromo-2-fluorobenzoyl chloride, slowly adding an aqueous solution of methylamine to regulate the pH value of the reaction solution to be 8-9, and continuing to carry out the reaction; extracting with the organic solvent after the reaction ends, collecting the organic phase, and evaporating the solvent to dryness, thereby obtaining the 4-bromo-2-fluoro-N-methylbenzamide. According to the method disclosed by the invention, the 4-bromo-2-fluorobenzoic acid and 2-aminoisobutyric acid are taken as the raw materials, the product is prepared by a substitution reaction under the actions of cuprous halide catalysis, ligand assistance and in the presence of an acid-binding agent, and the yield is 75%. However, by virtue of theoptimized conditions, cheap acetylacetone is screened as a ligand, and the cost is greatly reduced.
-
Paragraph 0022; 0028

(2019/04/04)

PROCESS FOR PREPARATION OF ENZALUTAMIDE USING NOVEL INTERMEDIATE
Process for preparation of Enzalutamide using novel intermediate Provided herein is a process for the preparation of a novel [4-cyano-3- (trifluoromethyl)phenyl]carbamodithioic acid and its use in preparation of Enzalutamide being cost effective with higher yield, higher HPLC purity with reduced impurities.
-
Page/Page column 27; 33; 34

(2019/06/17)

The compounds of structure containing conjugated zincon, its pharmaceutical composition and use thereof (by machine translation)
The present invention relates to compounds having a structure containing conjugated zincon, its pharmaceutical composition and use, and in particular relates to the general formula (I) or a salt thereof to the compound represented by the, pharmaceutical compositions thereof, and its as BTK inhibitors and/or B cell activation inhibitor, for the prevention or treatment B cell activity with abnormal and/or the use of the BTK-related diseases. The compounds of lymphoma, breast cancer, liver cancer, colon cancer, gastric cancer, such as lung cancer and cervical cancer cell has better lethal effect, note has potential for the treatment of cancer and self-immune diseases related to potential. (by machine translation)
-
Paragraph 0174; 0175

(2018/03/24)

BICYCLIC HYDROXAMIC ACIDS USEFUL AS INHIBITORS OF MAMMALIAN HISTONE DEACETYLASE ACTIVITY
A compound of formula (Ia) or (Ib) or a pharmaceutically acceptable salt thereof. The compound is an inhibitor of a histone deacetylase, and as such is useful in terepy, e.g. in the treatment of autoimmune disorders, mental disorders, neurodegenerative disorders, and hyperproliferative disorders.
-
Page/Page column 82

(2017/07/14)

Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB2 ligands by regioisomeric 1,3,4-oxadiazole ring
It has been reported that bioisosteric replacement of an 1,2,4-oxadiazole ring by an 1,3,4-oxadiazole ring leads to higher polarity, reduced metabolic degradation by human liver microsomes and reduced interaction with hERG channels. In a seven to eight st
Heimann, Dominik,Lueg, Corinna,De Vries, Henk,Frehland, Bastian,Schepmann, Dirk,Heitman, Laura H.,Wünsch, Bernhard
p. 1697 - 1705
(2017/08/22)

BTK INHIBITOR
Provided are a series of BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or prodrug thereof represented by formula (I), (II), (III) or (IV).
-
Paragraph 0306

(2017/11/16)

Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis
Bruton's tyrosine kinase (BTK) is a Tec family kinase with a well-defined role in the B cell receptor (BCR) pathway. It has become an attractive kinase target for selective B cell inhibition and for the treatment of B cell related diseases. We report a series of compounds based on 8-amino-imidazo[1,5-a]pyrazine that are potent reversible BTK inhibitors with excellent kinase selectivity. Selectivity is achieved through specific interactions of the ligand with the kinase hinge and driven by aminopyridine hydrogen bondings with Ser538 and Asp539, and by hydrophobic interaction of trifluoropyridine in the back pocket. These interactions are evident in the X-ray crystal structure of the lead compounds 1 and 3 in the complex with the BTK enzyme. Our lead compounds show desirable PK profiles and efficacy in the preclinical rat collagen induced arthritis model.
Liu, Jian,Guiadeen, Deodial,Krikorian, Arto,Gao, Xiaolei,Wang, James,Boga, Sobhana Babu,Alhassan, Abdul-Basit,Yu, Younong,Vaccaro, Henry,Liu, Shilan,Yang, Chundao,Wu, Hao,Cooper, Alan,De Man, Jos,Kaptein, Allard,Maloney, Kevin,Hornak, Viktor,Gao, Ying-Duo,Fischmann, Thierry O.,Raaijmakers, Hans,Vu-Pham, Diep,Presland, Jeremy,Mansueto, My,Xu, Zangwei,Leccese, Erica,Zhang-Hoover, Jie,Knemeyer, Ian,Garlisi, Charles G.,Bays, Nathan,Stivers, Peter,Brandish, Philip E.,Hicks, Alexandra,Kim, Ronald,Kozlowski, Joseph A.
p. 198 - 203
(2016/03/01)

AN IMPROVED PROCESS FOR THE PREPARATION OF ENZALUTAMIDE
The present application relates to an improved process for preparation of Enzalutamide (I). The present application also relates to an improved process for the preparation of substantially pure Enzalutamide (I) having purity of greater than 99.5%. The present application also relates to a novel process for the preparation of Enzalutamide intermediate useful in the industrially viable synthesis of Enzalutamide.
-
Page/Page column 14; 15

(2016/04/26)

A "one-pot synthesis" method of synthesizing graciousness mixed Lu An
The invention provides a one-pot method for synthetizing enzalutamide and belongs to the field of medicinal chemical synthesis. The method comprises the following steps: firstly, carrying out copper-catalyzed Buchwald reaction on N-methyl-4-bromo-2-fluoro-benzamide and 2-methyl alanine, adding halogenated hydrocarbon, reacting to generate ester, finally adding a key intermediate 4-isothiocyano-2-(trifluoromethyl) cyanophenyl and carrying out bucherer-Bergs reaction to generate the enzalutamide. The method is simple in operation and high in product yield and has the advantages that the intermediate products are not needed to be separated and directly reacted, so that the process flow cycle is shortened; the final product is easy to separate and purify.
-
Paragraph 0017; 0022-0024

(2017/03/14)

HETEROARYL PYRIDONE AND AZA-PYRIDONE AMIDE COMPOUNDS
Heteroaryl pyridone and aza-pyridone amide compounds of Formula (I) are provided, and various substituents including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
-
Page/Page column 106

(2015/01/16)

AMIDE COMPOUND AND USE THEREOF FOR PEST CONTROL
A fused heterocyclic compound represented by formula (1) has an excellent pest control effect. (In the formula, R1 represents a C1-C6 chain hydrocarbon group which may have one or more atoms or groups selected from group X, or the like; R2, R3,
-
Paragraph 0543

(2015/05/06)

FLAP MODULATORS
The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, R2, R3, R3′, L, W, and V are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention
-
Paragraph 0179

(2015/11/03)

NOVEL COMPOUNDS AND COMPOSITIONS FOR INHIBITION OF FASN
The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
-
Page/Page column 257

(2014/10/18)

HIGHLY SELECTIVE C-MET INHIBITORS AS ANTICANCER AGENTS
Disclosed are novel nitrogen-containing, heterocyclic, c-Met inhibitor compounds, processes for their preparation and formulations thereof. The compounds are useful as therapeutical agents for the inhibition, regulation, and control of c-Met kinase signal pathway, and useful for treating in a subject a cell proliferative disorder or disorders mediated by c-Met.
-
Page/Page column 9-10

(2014/03/25)

Synthesis of derivatives of the keto-pyrrolyl-difluorophenol scaffold: Some structural aspects for aldose reductase inhibitory activity and selectivity
Seven novel ARIs (3a-c, 4a-c and 5) were synthesized with the implementation of an optimized and, partially, selective synthetic procedure, via a Friedel-Crafts acylation reaction. The synthesized ARIs have values of IC50ALR2 ranging
Kotsampasakou, Eleni,Demopoulos, Vassilis J.
p. 869 - 873
(2013/03/13)

NEW ARYL-BENZOCYCLOALKYL AMIDE DERIVATIVES
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1, A2 and n are as described herein, compositions including the compounds and methods of using the compounds.
-
Paragraph 0322-0323

(2013/03/26)

1, 2, 4-TRIAZOLONE DERIVATIVE
The present invention provides a 1,2,4-triazolone derivative represented by Formula (1A) having an antagonistic activity on the arginine-vasopressin 1b receptor or a pharmaceutically acceptable salt thereof and provides a pharmaceutical composition comprising the compound or the salt as an active ingredient, in particular, a therapeutic or preventive agent exhibiting favorable pharmacokinetics in a disease such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, or alopecia.
-
Paragraph 0524

(2013/08/14)

Analogues of fenarimol are potent inhibitors of trypanosoma cruzi and are efficacious in a murine model of chagas disease
We report the discovery of nontoxic fungicide fenarimol (1) as an inhibitor of Trypanosoma cruzi (T. cruzi), the causative agent of Chagas disease, and the results of structure-activity investigations leading to potent analogues with low nM IC50s in a T. cruzi whole cell in vitro assay. Lead compounds suppressed blood parasitemia to virtually undetectable levels after once daily oral dosing in mouse models of T. cruzi infection. Compounds are chemically tractable, allowing rapid optimization of target biological activity and drug characteristics. Chemical and biological studies undertaken in the development of the fenarimol series toward the goal of delivering a new drug candidate for Chagas disease are reported.
Keenan, Martine,Abbott, Michael J.,Alexander, Paul W.,Armstrong, Tanya,Best, Wayne M.,Berven, Bradley,Botero, Adriana,Chaplin, Jason H.,Charman, Susan A.,Chatelain, Eric,Von Geldern, Thomas W.,Kerfoot, Maria,Khong, Andrea,Nguyen, Tien,McManus, Joshua D.,Morizzi, Julia,Ryan, Eileen,Scandale, Ivan,Thompson, R. Andrew,Wang, Sen Z.,White, Karen L.
supporting information; experimental part
p. 4189 - 4204
(2012/07/27)

ANTINEOPLASTIC DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
The disclosure concerns heterobicyclic compounds of general formula (I) and acid addition salts, hydrates and solvates thereof, as well as enantiomers, diastereoisomers and mixtures thereof. Methods for preparing the compounds, pharmaceutical compositions, and methods of treatment also are disclosed.
-
Page/Page column 19

(2011/10/19)

PROCESSES FOR THE SYNTHESIS OF DIARYLTHIOHYDANTOIN AND DIARYLHYDANTOIN COMPOUNDS
Processes are provided for the synthesis of diarylthiohydantoin and diarylhydantoin compounds, such as compounds of the formula: wherein X, Y1, Y2, R1, and R2 are as defined herein. Medicinal products containing the same find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.
-
Page/Page column 43

(2011/09/30)

HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES
The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases
-
Page/Page column 30

(2010/03/31)

Analogues of morphanthridine and the tear gas dibenz[ b, f ][1,4]oxazepine (CR) as extremely potent activators of the human transient receptor potential ankyrin 1 (TRPA1) channel
The TRPA1 channel can be considered as a key biological sensor to irritant chemicals. In this paper, the discovery of 11H-dibenz[b,e]azepines (morphanthridines) and dibenz[b,f][1,4]oxazepines is described as extremely potent agonists of the TRPA1 receptor. This has led to the discovery that most of the known tear gases are potent TRPA1 activators. The synthesis and biological activity of a number of substituted morphanthridines and dibenz[b,f][1,4]oxazepines have given insight into the SAR around this class of TRPA1 agonists, with EC50 values ranging from 1 μM to 0.1 nM. Compounds 6 and 32 can be considered as the most potent TRPA1 agonists known to date, with 6 now being used successfully as a screening tool in the discovery of TRPA1 antagonists. The use of ligands such as 6 and 32 as pharmacological tools may contribute to the basic knowledge of the TRPA1 channel and advance the development of TRPA1 antagonists as potential treatment for conditions involving TRPA1 activation, including asthma and pain.
Gijsen, Harrie J. M.,Berthelot, Didier,Zaja, Mirko,Br?ne, Bert,Geuens, Ivo,Mercken, Marc
scheme or table
p. 7011 - 7020
(2010/11/18)

VIRAL POLYMERASE INHIBITORS
The present application provides compounds of formula I wherein X, Y, R2, n, R5 and R6 are defined herein, useful as inhibitors of the hepatitis C virus NS5B polymerase The present application also provides pharmaceutical
-
Page/Page column 85

(2010/04/27)

VIRAL POLYMERASE INHIBITORS
Compounds of formula I: wherein X, R2, R3, R3a, R3b,R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
-
Page/Page column 56

(2009/07/18)

VIRAL POLYMERASE INHIBITORS
Compound of Formula I: wherein, R2, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase
-
Page/Page column 70

(2009/04/25)

DIBENZOAZEPINE AND DIBENZOOXAZEPINE TRPA1 AGONISTS
The present invention is related to novel tricyclic compounds of formula (I) having TRPA1 receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use as pharmacologi
-
Page/Page column 16-17

(2009/07/17)

QUINOXALINE DERIVATIVES AS INHIBITORS OF THE TYROSINE KINASE ACTIVITY OF JANUS KINASES
The present invention relates to quinoxaline compound of the formula (I): wherein R1 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R7; R2 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R8; R3, R4, R5 and R6 are each independently hydrogen or R9; and R7, R8 and R9 are each independently selected from organic and inorganic substituents, their use in therapy of diseases, in particular diseases mediated by the tyrosine kinase activity of Janus kinases, including JAK-2 and JAK-3 kinases
-
Page/Page column 31-32

(2009/01/24)

Hydrogenation on palladium-containing granulated catalysts 3. Synthesis of aminobenzimidazoles by catalytic hydrogenation of dinitroanilines
Efficient hydrogenation of o-aminonitrobenzenes on palladium-containing granulated carbon catalysts in carboxylic acid solutions was accompanied by cyclization into aminobenzimidazoles. A simple hydrogenation reactor with a fixed gauze holding a reusable granulated catalyst was designed. Acylated and sulfonylated 4(7)-aminobenzimidazoles were obtained. In terms of electronic and geometrical parameters, they are close analogs of biologically active imidazo[1,5,4-e,f ][1,5]benzodiazepines.
Elkin,Tolkacheva,Chernysheva,Karmanova,Konyushkin,Semenov
p. 1216 - 1226
(2008/09/19)

Novel 5α-reductase inhibitors: Synthesis, structure-activity studies, and pharmacokinetic profile of phenoxybenzoylphenyl acetic acids
Novel substituted benzoyl benzoic acids and phenylacetic acids 1-14 have been synthesized and evaluated for inhibition of rat and human steroid 5α-reductase isozymes 1 and 2, The compounds turned out to be potent and selective human type 2 enzyme inhibitors, exhibiting IC50 values in the nanomolar range. The phenylacetic acid derivatives were more potent than the analogous benzoic acids. Bromination in the 4-position of the phenoxy moiety led to the strongest inhibitor in this class (12; IC50 = 5 nM), which was equipotent to finasteride. Since oral absorption is essential for a potential drug, 12 was further examined. In the parallel artificial membrane permeation assay (PAMPA) it turned out to be a good permeator, whereas it was a medium permeator in Caco2 cells. After oral administration (40 mg/kg) to rats a high bioavailability and a biological half-life of 5.5 h were observed, making it a promising candidate for clinical evaluation.
Salem, Ola I. A.,Frotscher, Martin,Scherer, Christiane,Neugebauer, Alexander,Biemel, Klaus,Streiber, Martina,Maas, Ruth,Hartmann, Rolf W.
p. 748 - 759
(2007/10/03)

Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
-
Page/Page column 43

(2008/06/13)

OXAZOLE DERIVATIVES AS HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES
The present invention discloses novel aryl oxazole compounds of Formula I (I), or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing and using such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. Formula I (I) or a pharmaceutically acceptable salt thereof, wherein: m is independenlly at each occurrence 1, 2, or 3, Z independently represents carbon (substituted with hydrogen or the optional substituents indicated herein) or nitrogen, provided that when Z is nitrogen then R6 is not attached to Z; R1 and R2 are independently -(C1-C7) alkyl(optionally substituted with one to three halogens), or R1 and R2 and the nitrogen to which they are attached form an azetidinyl ring, a pyrrolidinyl ring, or a piperidinyl ring, wherein further the azetidinyl, pyrrolidinyl, or piperidinyl ring so formed may be optionally substituted one to three times with R5; R6 is independently at each occurrence -H, -halogen, or -CH3.
-
Page/Page column 56

(2008/06/13)

NOVEL COMPOUNDS
Novel Compounds The invention relates to substituted acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
-
Page/Page column 52

(2010/10/20)

PYRROLIDINE DERIVATIVES AS HISTAMINE RECEPTORS LIGANDS
The present invention relates to pyrrolidine derivatives of formula (I) having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.
-
Page/Page column 33

(2010/11/08)

METHYLENE DIPIPERIDINE DERIVATIVES
The present invention relates to novel methylene dipiperidine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.
-
Page/Page column 18-19

(2010/11/30)

HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES
The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods and intermediates for preparing such compounds. In anot
-
Page/Page column 27

(2010/11/24)

CHEMICAL COMPOUNDS
The present invention relates to novel compounds with a variety of therapeutic uses, more particularly novel substituted cyclic alkylidene compounds that are particularly useful for selective estrogen receptor modulation.
-
Page/Page column 78

(2008/06/13)

HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES
The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases
-
Page/Page column 51

(2008/06/13)

SUBSTITUTED PIPERIDINES AS HISTAMINE H3 RECEPTOR LIGANDS
The present invention relates to novel piperidine ether derivatives having affinity for the histamine H3 receptor, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.
-
Page/Page column 30-31

(2010/02/10)

NITROGENOUS FUSED?RING COMPOUND HAVING PYRAZOLYL GROUP AS SUBSTITUENT AND MEDICINAL COMPOSITION THEREOF
The present invention provides a compound having an excellent inhibitory action on activation of STAT6 and a pharmaceutical composition thereof. Inparticular, it provides a compound represented by the following formula (I), a salt thereof or a hydrate of them. In the formula, X represents a nitrogen-containing condensed aromatic heterocyclic group such as imidazo[1,2-a]pyridine, benzimidazole, quinazoline, quinoline, or 2,1-benzisoxazole and has (R4)n as substituent groups; Y represents a C3-8 cycloalkyl group, C4-8 cycloalkenyl group, 5- to 14-membered non-aromatic heterocyclic group, C6-14 aromatic hydrocarbon cyclic group or 5- to 14-membered aromatic heterocyclic group; n in (R4)n is 0, 1, 2 or 3, and Z groups independently represent (1) hydrogen atom, (2) amino group, (3) halogen atom, (4) hydroxyl group, (5) nitro group, (6) cyano group, (7) azido group, (8) formyl group, (9) hydroxyamino group, (10) sulfamoyl group, (11) guanodino group, (12) oxo group, (13) C2-6 alkenyl group, (14) C1-6 alkoxy group, (15) C1-6 alkylhydroxyamino group, (16) halogenated C1-6 alkyl group, (17) halogenated C2-6 alkenyl group, (18) (i) C3-7cycloalkyl group, (ii) C3-7cycloalkenyl group, (iii) 5- to 14-membered non-aromatic heterocyclic group, each of which may have one or more substituent groups Q, or (19) formula -M1-M2-M3, R1 represents (1) hydrogen atom, (2) halogen atom, (3) hydroxyl group, (4) nitro group, (5) cyano group, (6) halogenated C1-6 alkyl group, (7) C2-6 alkyl group substituted with a hydroxyl or cyano group, (8) C2-6 alkenyl group, or (9) formula -L1-L2-L3, and R2 represents a hydrogen atom or a protecting group; and R3 represents a hydrogen atom, halogen atom, cyano group, amino group, C1-4 alkyl group or halogenated C1-4 alkyl group.
-
Page 162

(2008/06/13)

Chemical Properties

Appearance/Colour :white to light yellow liquid or crystalline mass
Melting Point: 24-24.5 °C
Boiling Point: 236.873 °C at 760 mmHg
Flash Point:97.058 °C
Density: 1.743 g/cm³
Storage Temp.:under inert gas (nitrogen or Argon) at 2-8°C
Vapor Pressure: 0.0462mmHg at 25°C
Refractive Index: 1.5877
Sensitive: Lachrymatory
BRN: 6323925
PSA: 17.07000
LogP: 2.96720

Global suppliers and manufacturers of 151982-51-3total 51 suppliers on LookChem

Company Name
Business Type
Min Order
FOB Price
Main Products
Contact

Dayang Chem (Hangzhou) Co.,Ltd.
Business Type:Lab/Research institutions
Min Order:1 Kilogram
FOB Price:USD $ 3.0-3.0 / Kilogram
Main Products:994
Country:

Enke Pharma-tech Co.,Ltd. （Cangzhou, China ）
Business Type:Manufacturers
Min Order:1 Kilogram
FOB Price:USD $ 5.0-5.0 / Kilogram
Main Products:53
Country:

COLORCOM LTD.
Business Type:Manufacturers
Min Order:1 Metric Ton
FOB Price:No Data
Main Products:32
Country:

Chemwill Asia Co., Ltd.
Business Type:Manufacturers
Min Order:5 Kiloliter
FOB Price:USD $ 1.2-5.0 / Kiloliter
Main Products:56
Country:

Zhuozhou Wenxi import and Export Co., Ltd
Business Type:Trading Company
Min Order:1 Kilogram
FOB Price:USD $ 139.0-210.0 / Kilogram
Main Products:1
Country:

Triumph International Development Limilted
Business Type:Lab/Research institutions
Min Order:100 Metric Ton
FOB Price:No Data
Main Products:24
Country:

Hangzhou J&H Chemical Co., Ltd.
Business Type:Lab/Research institutions
Min Order:No Data
FOB Price:No Data
Main Products:46
Country:

Ality Chemical Corporation
Business Type:Other
Min Order:No Data
FOB Price:No Data
Main Products:165
Country:

Henan Tianfu Chemical Co., Ltd.
Business Type:Lab/Research institutions
Min Order:1 Metric Ton
FOB Price:USD $ 5000.0-5000.0 / Metric Ton
Main Products:67
Country:

Shanghai Minstar Chemical Co., Ltd
Business Type:Lab/Research institutions
Min Order:1 Gram
FOB Price:No Data
Main Products:120
Country:

TAIZHOU ZHENYU BIOTECHNOLOGY CO., LTD
Business Type:Lab/Research institutions
Min Order:1 Kilogram
FOB Price:USD $ 2.0-2.0 / Kilogram
Main Products:90
Country:

Hunan chemfish Pharmaceutical co.,Ltd
Business Type:Manufacturers
Min Order:No Data
FOB Price:No Data
Main Products:29
Country:

Changzhou Anchor Biological Technology Co., Ltd.
Business Type:Lab/Research institutions
Min Order:No Data
FOB Price:No Data
Main Products:30
Country:

Win-Win chemical Co.Ltd
Business Type:Lab/Research institutions
Min Order:No Data
FOB Price:No Data
Main Products:55
Country:

GIHI CHEMICALS CO.,LIMITED
Business Type:Lab/Research institutions
Min Order:No Data
FOB Price:No Data
Main Products:80
Country:

DB BIOTECH CO., LTD
Business Type:Trading Company
Min Order:No Data
FOB Price:No Data
Main Products:90
Country:

Henan Allgreen Chemical Co.,Ltd
Business Type:Manufacturers
Min Order:No Data
FOB Price:No Data
Main Products:34
Country:

Hubei Taiho Chemical Co.,LTD
Business Type:Manufacturers
Min Order:No Data
FOB Price:No Data
Main Products:1
Country:

Antimex Chemical Limied
Business Type:Lab/Research institutions
Min Order:No Data
FOB Price:No Data
Main Products:163
Country:

Hangzhou Ocean Chemical Co., Ltd.
Business Type:Lab/Research institutions
Min Order:No Data
FOB Price:No Data
Main Products:44
Country:

Post a RFQ

Cas No.:

Product Name:

Quantity:

Email:

Company name:

Valid Period:

Detailed Requirements:

Enter 15 to 2000 letters.Word count: 0 letters

Attach files(File Format: Jpeg, Jpg, Gif, Png, PDF, PPT, Zip, Rar,Word or Excel Maximum File Size: 3MB)

What can I do for you?
Get Best Price

Get Best Price for 151982-51-3

Article Database

151982-51-3

Articles about 151982-51-3Total 51 be found

More Articles about upstream products of 151982-51-3

More Articles about downstream products of 151982-51-3

Chemical Properties

Appearance/Colour :white to light yellow liquid or crystalline mass

Melting Point: 24-24.5 °C

Boiling Point: 236.873 °C at 760 mmHg

Flash Point:97.058 °C

Density: 1.743 g/cm³

Storage Temp.:under inert gas (nitrogen or Argon) at 2-8°C

Vapor Pressure: 0.0462mmHg at 25°C

Refractive Index: 1.5877

Sensitive: Lachrymatory

BRN: 6323925

PSA: 17.07000

LogP: 2.96720

Global suppliers and manufacturers of 151982-51-3total 51 suppliers on LookChem

Article Database

151982-51-3

Articles about 151982-51-3Total 51 be found

More Articles about upstream products of 151982-51-3

More Articles about downstream products of 151982-51-3

Chemical Properties

Appearance/Colour :white to light yellow liquid or crystalline mass

Melting Point: 24-24.5 °C

Boiling Point: 236.873 °C at 760 mmHg

Flash Point:97.058 °C

Density: 1.743 g/cm3

Storage Temp.:under inert gas (nitrogen or Argon) at 2-8°C

Vapor Pressure: 0.0462mmHg at 25°C

Refractive Index: 1.5877

Sensitive: Lachrymatory

BRN: 6323925

PSA: 17.07000

LogP: 2.96720

Global suppliers and manufacturers of 151982-51-3total 51 suppliers on LookChem

Density: 1.743 g/cm³