cas 885693-20-9, TERT-BUTYL 5-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)-3,6-DIHYDROPYRIDINE-1(2H)-CARBOXYLATE

Articles about 885693-20-9Total 19 be found

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Multigram Synthesis of Heterabicyclo[n.1.0]alkan-1-yl Trifluoroborates
An approach to the synthesis of oxa- and azabicyclo[n.1.0]alkan-1-yl trifluoroborates on a multigram scale was developed. Two synthetic strategies were evaluated: the first based on the lithiation–borylation of the corresponding 2-bromoallyl derivatives, and the other relying on regioselective hydroboration of the appropriate hetera-substituted enynes. The second method appeared to be more efficient in terms of scalability and substrate scope. Further steps included ring closing-metathesis, mild palladium-catalyzed cyclopropanation with diazomethane, and reaction with KHF2 and furnished the title compounds in up to 50 g scale in a single run (10–41 % overall yield, 4–5 steps).
Kleban, Ihor,Krokhmaliuk, Yevhen,Reut, Sofiia,Shuvakin, Serhii,Pendyukh, Vyacheslav V.,Khyzhan, Oleksandr I.,Yarmoliuk, Dmytro S.,Tymtsunik, Andriy V.,Rassukana, Yuliya V.,Grygorenko, Oleksandr O.
p. 6551 - 6560
(2020/09/17)

Sodium channel blockers (by machine translation)
The invention belongs to the field of medicines, and particularly relates to a compound shown as a formula (I). A pharmaceutical composition comprising the compound, a pharmaceutically acceptable salt, a solvate or an isomer thereof, a pharmaceutically ac
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Paragraph 0364; 0369-0371

(2020/11/05)

Triazolo[1,5-a]pyrimidine Phosphodiesterase 2A Inhibitors: Structure and Free-Energy Perturbation-Guided Exploration
We describe the hit-To-lead exploration of a [1,2,4]triazolo[1,5-A]pyrimidine phosphodiesterase 2A (PDE2A) inhibitor arising from high-Throughput screening. X-ray crystallography enabled structure-guided design, leading to the identification of preferred substructural components. Further rounds of optimization used relative binding free-energy calculations to prioritize different substituents from the large accessible chemical space. The free-energy perturbation (FEP) calculations were performed for 265 putative PDE2A inhibitors, and 100 compounds were synthesized representing a relatively large prospective application providing unexpectedly active molecules with IC50′s from 2340 to 0.89 nM. Lead compound 46 originating from the FEP calculations showed PDE2A inhibition IC50 of 1.3 ± 0.39 nM, a 100-fold selectivity versus other PDE enzymes, clean cytochrome P450 profile, in vivo target occupancy, and promise for further lead optimization.
Tresadern, Gary,Velter, Ingrid,Trabanco, Andrés A.,Van Den Keybus, Frans,MacDonald, Gregor J.,Somers, Marijke V. F.,Vanhoof, Greet,Leonard, Philip M.,Lamers, Marieke B. A. C.,Van Roosbroeck, Yves E. M.,Buijnsters, Peter J. J. A.
p. 12887 - 12910
(2020/11/13)

gem-Difluorocyclopropanation of Alkenyl Trifluoroborates with the CF3SiMe3–NaI System
Difluorocyclopropanation of alkenyl trifluoroborates using TMSCF3–NaI system was reported for the first time. The developed method allowed preparation of monocyclic, spiro- and fused-bicyclic gem-difluorocyclopropanes bearing additional functio
Grygorenko, Oleksandr O.,Hryshchuk, Oleksandr V.,Kuchkovska, Yuliya O.,Tymtsunik, Andriy V.,Varenyk, Anatolii O.,Yurov, Yevhen
supporting information
p. 2217 - 2224
(2020/04/29)

Preparation method of N-substituted-tetrahydropyridine-3/4-boric acid/ester
The invention discloses a preparation method of N-substituted tetrahydropyridine-3/4-boric acid/ester, and belongs to the technical field of organic boric acid chemistry. The method comprises the following steps: carrying out a reaction on pyridine-3/4-boric acid/ester and a halide to form a quaternary salt, and reducing the quaternary salt with sodium/potassium borohydride in an aprotic solvent to generate N-substituted-tetrahydropyridine-3/4-boric acid/ester. According to the method, easily-synthesized pyridine-3/4-boric acid/ester is used as a raw material, the product can be obtained through two continuous steps, and the reaction selectivity is high, so that the defect that palladium-catalyzed coupling or ultralow temperature is needed when substituted piperidone is adopted as a raw material is overcome, the method is verified on the hectogram scale, and a concise and efficient synthesis path is provided for preparation of the compound.
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Paragraph 0041-0043

(2020/04/22)

CHEMOKINE RECEPTOR MODULATORS AND USES THEREOF
Disclosed herein, inter alia, are compounds and methods of use thereof for the modulation of chemokine receptor activity.
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Paragraph 1625-1626

(2018/05/03)

ANTI-AMYLOID COMPOUNDS CONTAINING BENZOFURAZAN
In general, among other things, compounds of Formula I are provided: in which R11 is e.g., 4-(pyrrolidin-1-yl)piperidin-1-yl, N-methyl-3-(pyrrolidin-1-yl)propan-1-amino, N1,N1,N3-trimethylpropane-1,3-diamino, N,N-dimethylpiperidin-4-amino, 3-(pyrrolidin-1-ylmethyl)azetidin-1-yl, 3-(pyrrolidin-1-ylmethanon)azetidin-1-yl, or 3-(morpholin-1-ylmethyl)azetidin-1-yl; R13 is, e.g., phenyl optionally substituted with one or more substituents; and R12 and R14 are each independently hydrogen or alkyl. Methods of treatment are also provided.
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(2017/07/14)

INHIBITORS OF BRUTON'S TYROSINE KINASE
Disclosed herein are compounds that inhibit Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
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Paragraph 00654

(2016/01/25)

Method for synthesizing N-substitute-1, 2, 3, 6-tetrahydropyridine-5-boric acid ester
The invention discloses a method for synthesizing N-substitute-1, 2, 3, 6-tetrahydropyridine-5-boric acid ester. According to the method, N-substitute-1, 2, 3, 6-tetrahydropyridine-5-carboxylic acid (ester) serves as the raw material, conducts addition with halogen and then is subjected to alkaline condition elimination to form alkenyl halide and then subjected to coupling with al boron ester under the condition of metal palladium catalyzation, and the N-substitute-1, 2, 3, 6-tetrahydropyridine-5-boric acid ester is obtained. According to the method, the obtained midbody alkenyl halide does not contain isomer, separation is easy to conduct, purity of an obtained product is high, and the method provides a simple way for synthesis of compounds of the type.
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Paragraph 0024

(2016/11/07)

Pyrimidin-4-one derivatives and their use in the treatment, amelioration or prevention of a viral disease
The present invention relates to a compound having the general formula II, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
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Paragraph 184

(2013/05/08)

SUBSTITUTED FUSED TRICYCLIC COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF
The present invention relates to substituted fused tricyclic compounds of formula (I) or (Ia), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by JAK activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders mediated by JAK activity. Such conditions include, but not limited to, arthritis, Alzheimer's disease, autoimmune thyroid disorders, cancer, diabetes, leukemia, T-cell prolymphocytic leukemia, lymphoma, myleoproliferation disorders, lupus, multiple myeloma, multiple sclerosis, osteoarthritis, sepsis, psoriatic arthritis, prostate cancer, T-cell autoimmune disease, inflammatory diseases, chronic and acute allograft transplant rejection, bone marrow transplant, stroke, asthma, chronic obstructive pulmonary disease, allergy, bronchitis, viral diseases, or Type I diabetes, complications from diabetes, rheumatoid arthritis, asthma, Crohn's disease, dry eye, uveitis, inflammatory bowel disease, organ transplant rejection, psoriasis and ulcerative colitis. The present disclosure also relates to process for the preparation of such compounds, and to pharmaceutical compositions containing them.
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Page/Page column 68-69

(2012/10/08)

BRUTON'S TYROSINE KINASE INHIBITORS
The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
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Page/Page column 122; 123

(2011/04/14)

HETEROARYLOXYHETEROCYCLYL COMPOUNDS AS PDE10 INHIBITORS
Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
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Page/Page column 85

(2011/12/02)

SUBSTITUTED PYRROLO[2,3-B]-PYRIDINES AND-PYRAZINES
Compounds of Formula I, as shown below and defined herein:(I) pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by Ron and/or Met.
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Page/Page column 47

(2010/07/10)

METHOD OF INHIBITING C-KIT KINASE
A method of reducing or inhibiting kinase activity of C-KIT in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to C-KIT using a compound of the present invention: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.
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Page/Page column 60

(2008/06/13)

METHOD OF INHIBITING FLT3 KINASE
A method of reducing or inhibiting kinase activity of FLT3 in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 using a compound of the present invention (I), or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.
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Page/Page column 115

(2010/11/27)

Methods for inhibiting protein kinases
The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim-1 kinase, and tyrosine kinase using imidazo[1,2-a]pyrazine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with protein kinases using such compounds.
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Page/Page column 180

(2010/11/27)

INHIBITORS OF C-FMS KINASE
The invention is directed to compounds of Formula (I): wherein A, X, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula (I), are also provided.
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Page/Page column 97

(2008/06/13)

SYNERGISTIC MODULATION OF FLT3 KINASE USING A FLT3 INHIBITOR AND A FARNESYL TRANSFERASE INHIBITOR
The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from compounds of Formula I′: Included within the present invention is both prophylactic and therapeutic methods for treating a subject at risk of (or susceptible to) developing a cell proliferative disorder or a disorder related to FLT3.
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Page/Page column 73

(2008/06/13)

Chemical Properties

Melting Point: 105 °C
Boiling Point: 348.007 °C at 760 mmHg
Flash Point:164.269 °C
Density: 1.055 g/cm³
Storage Temp.:Keep in dark place,Sealed in dry,Room Temperature
Refractive Index: 1.488
PKA: -1.17±0.40(Predicted)
PSA: 48.00000
LogP: 3.12290

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885693-20-9

Articles about 885693-20-9Total 19 be found

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Chemical Properties

Melting Point: 105 °C

Boiling Point: 348.007 °C at 760 mmHg

Flash Point:164.269 °C

Density: 1.055 g/cm³

Storage Temp.:Keep in dark place,Sealed in dry,Room Temperature

Refractive Index: 1.488

PKA: -1.17±0.40(Predicted)

PSA: 48.00000

LogP: 3.12290

Global suppliers and manufacturers of 885693-20-9total 66 suppliers on LookChem

Article Database

885693-20-9

Articles about 885693-20-9Total 19 be found

More Articles about upstream products of 885693-20-9

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Chemical Properties

Melting Point: 105 °C

Boiling Point: 348.007 °C at 760 mmHg

Flash Point:164.269 °C

Density: 1.055 g/cm3

Storage Temp.:Keep in dark place,Sealed in dry,Room Temperature

Refractive Index: 1.488

PKA: -1.17±0.40(Predicted)

PSA: 48.00000

LogP: 3.12290

Global suppliers and manufacturers of 885693-20-9total 66 suppliers on LookChem

Density: 1.055 g/cm³