cas 847818-71-7, 1-(2-Methoxyethyl)-4-(4,4,5,5-tetraMethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

Articles about 847818-71-7Total 32 be found

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AMINOPYRIDINE COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF
The present invention discloses an aminopyridine compounds, a preparation method and use thereof, particularly the aminopyridine compounds of formula (I), pharmaceutical compositions containing the same, the method for preparing the same and the use thereof in the prophylaxis or treatment of an adenosine A2a receptor related disease.
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Paragraph 0269-0271; 0275-0277

(2021/11/04)

AMINOPYRAZINE COMPOUNDS AS HPK1 INHIBITOR AND THE USE THEREOF
Disclosed herein is an aminopyrazine compound of Formula (I), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions comprising thereof. Also disclosed is a method of treating HPK1 related disorders or diseases by using the compound disclosed herein.
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Page/Page column 94; 116

(2021/02/26)

MAP4K4 INHIBITORS
This invention relates to compounds that may be useful as inhibitors of Mitogen-activated Protein Kinase Kinase Kinase Kinase-4 (MAP4K4). The invention also relates to the use of these compounds, for example in a method of treatmentof cardiac conditions.In particular, the present invention relates to compounds of formula (I):
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Paragraph 00281-00283

(2020/07/05)

N-(AZAARYL)CYCLOLACTAM-1-CARBOXAMIDE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
An N-(azaaryl)cyclolactam-1-carboxamide derivative having a structure of formula (I), a preparation method therefor, and a use thereof are disclosed in the application. Each substituent are defined in the specification and claims. The series of compounds of the application can be widely applied in the preparation of drugs for treating cancer, tumor, autoimmune disease, metabolic disease or metastatic disease, particularly for treating ovarian cancer, pancreatic cancer, prostate cancer, breast cancer, cervical cancer, glioblastoma, multiple myeloma, metabolic disease, neurodegenerative disease, primary tumor site metastasis or osseous metastasis cancer, and are expected to be developed into a new generation of CSF-1R inhibitor drugs.
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Paragraph 0143; 0144; 0145

(2020/03/23)

CARBOXYLIC ACID AROMATIC AMIDES AS ANTAGONISTS OF BRADYKININ B1 RECEPTOR
The present invention relates to carboxylic acid aromatic amides compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing
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Page/Page column 142

(2018/07/29)

Structure-based design and synthesis of 1H-pyrazolo[3,4-d]pyrimidin-4-amino derivatives as Janus kinase 3 inhibitors
Janus kinases (JAKs) regulate various inflammatory and immune responses and are targets for the treatment of inflammatory and immune diseases. Here we report the discovery and optimization of 1H-pyrazolo[3,4-d]pyrimidin-4-amino as covalent JAK3 inhibitors that exploit a unique cysteine (Cys909) residue in JAK3. Our optimization study gave compound 12a, which exhibited potent JAK3 inhibitory activity (IC50 of 6.2 nM) as well as excellent JAK kinase selectivity (>60-fold). In cellular assay, 12a exhibited potent immunomodulating effect on IL-2-stimulated T cell proliferation (IC50 of 9.4 μM). Further, compound 12a showed efficacy in delayed hypersensitivity assay. The data supports the further investigation of these compounds as novel JAKs inhibitors.
Yin, Yuan,Chen, Cheng-Juan,Yu, Ru-Nan,Wang, Zhi-Jian,Zhang, Tian-Tai,Zhang, Da-Yong
p. 4774 - 4786
(2018/08/24)

Preparation and application of novel purine analogue JAK (janus kinase) inhibitor
The invention provides medicine for preventing, treating and/or relieving autoimmunity diseases such as Psoriasis, rheumatoid arthritis, inflammatory enteritis diseases, sjogren's syndrome, behcet's diseases, multiple sclerosis and systemic lupus erythematosus. The medicine has excellent JAK inhibitory activity. The invention also provides a medically acceptable composition containing the compoundand a method for preparing the compound.
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Paragraph 0159; 0161; 0162; 0164

(2018/09/21)

PYRAZOLOPYRIMIDINE DERIVATIVES
The present invention covers Pyrazolopyrimidine compounds of general formula (I), in which n, o, X, Y, R, Q, R1, R2, R3 and R4 are as defined herein, methods of preparing said compounds, intermediate compounds u
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Page/Page column 115

(2017/11/10)

Fused imidazole derivative having IDO/TDO inhibition activity and having structure represented by formula (I), preparation method and applications thereof
The present invention relates to a fused imidazole derivative having IDO/TDO inhibition activity and having a structure represented by a formula (I), a preparation method and applications thereof. According to the present invention, the series of the fused imidazole derivatives have high IDO/TDO inhibition activity, can be widely used for treating or preventing cancers or tumors, viral infections, depression, neurodegenerative disorders, trauma, age-related cataract, organ transplant rejections or autoimmune diseases, can further be used to inhibit the immune suppression of patients, and are expected to be developed into the new generation of the immunosuppressive agent. The formula (I) is defined in the specification.
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Paragraph 0474; 0475; 0476; 0477

(2017/11/18)

Compounds used as JAK inhibitor, and use of compounds
The invention provides compounds used as a JAK inhibitor, and a use of the compounds, and concretely provides compounds (represented by formula (I)) with JAK inhibition activity or a stereoisomer, a geometric isomer, a tautomer, a racemate, a nitrogen oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and a medicinal composition including the compounds. The invention also discloses a use of the compounds or the medicinal composition thereof in the preparation of medicines used for treating autoimmune diseases or proliferative diseases.
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Paragraph 0418; 0419; 0420; 0421; 0424

(2017/08/27)

HETEROARYL COMPOUNDS AND PHARMACEUTICAL APPLICATIONS THEREOF
The present invention provides herein is a heteroaryl compound or a stereoisomer, a geometric isomer, a tautomer, a racemate, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, as well as a pharmaceutical composition containing the compound disclosed herein. The present invention also provides herein is use of the compound or the pharmaceutical composition thereof disclosed herein in the manufacture of a medicine for treating autoimmune diseases or proliferative diseases.
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Paragraph 00517

(2016/01/25)

AROMATIC HETEROCYCLIC DERIVATIVE AND PHARMACEUTICAL
The main purpose of the invention is to provide a novel aromatic heterocyclic derivative or a pharmaceutically acceptable salt thereof. Examples of the invention include aromatic heterocyclic derivatives represented by general formula [1] and pharmaceutically acceptable salts thereof. In formula [1], R1 represents phenyl optionally substituted with one or two groups selected from the group consisting of halogens ,as well as alkyls and alkoxys optionally substituted by halogens; R2 represents a hydrogen, an alkyl, cycloalkyl, or alkoxy optionally substituted by a halogen, or a heteroaryl optionally substituted by an alkyl; X represents CR3, and Y represents N or CR4, or X represents N, and Y represents CR4; and Z represents CR5 or N.
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Paragraph 0123; 0124

(2015/04/15)

HISTONE DEMETHYLASE INHIBITORS
The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like
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Paragraph 00179

(2014/10/04)

PHARMACOLOGICALLY ACTIVE COMPOUNDS
The present invention relates to compounds of formula (II) wherein X, Y, R2, R3, R4 and Ar are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1 – also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
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Paragraph 00416-00418

(2014/03/26)

SUBSTITUTED PYRIDOPYRAZINES AS NOVEL SYK INHIBITORS
Provided are pyridopyrazine compounds of formula (1), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, R4 and m are as defined in the specification.
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Paragraph 0166; 0167

(2014/05/08)

AMIDE, UREA OR SULFONE AMIDE LINKED BENZOTHIAZOLE INHIBITORS OF ENDOTHELIAL LIPASE
The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
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Paragraph 00223

(2014/02/15)

Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia
We report the discovery of a series of imidazo[1,2-a]pyrazine derivatives as novel inhibitors of phosphodiesterase 10A (PDE10A). In a high-throughput screening campaign we identified the imidazopyrazine derivative 1, a PDE10A inhibitor with limited select
Bartolomé-Nebreda, José Manuel,Delgado, Francisca,Martín-Martín, María Luz,Martínez-Viturro, Carlos M.,Pastor, Joaquín,Tong, Han Min,Iturrino, Laura,Macdonald, Gregor J.,Sanderson, Wendy,Megens, Anton,Langlois, Xavier,Somers, Marijke,Vanhoof, Greet,Conde-Ceide, Susana
p. 4196 - 4212
(2014/06/09)

FURO [3, 2 - B] - AND THIENO [3, 2 - B] PYRIDINE DERIVATIVES AS TBK1 AND IKK INHIBITORS
Compounds of the formula (I) in which R1, R2 and X have the meanings indicated in Claim 1, are inhibitors of TBK1 and ΙΚΚε and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.
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Page/Page column 82; 83

(2013/08/28)

Tetrahydroquinoline Derivatives And Their Pharmaceutical Use
Tetrahydroquinoline compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
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Page/Page column 48

(2012/08/28)

SUBSTITUTED PYRIDOPYRAZINES AS NOVEL SYK INHIBITORS
Provided are certain pyridopyrazine compounds, pharmaceutical compositions thereof and methods of use therefor.
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Page/Page column 35-36

(2013/02/27)

IMIDAZO[1,2-a]PYRAZINE DERIVATIVES AND THEIR USE FOR THE PREVENTION OR TREATMENT OF NEUROLOGICAL, PSYCHIATRIC AND METABOLIC DISORDERS AND DISEASES
The present invention relates to novel imidazo[1,2-a]pyrazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
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Page/Page column 46

(2013/02/28)

IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS
The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
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Page/Page column 95

(2011/05/11)

IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS
The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
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Page/Page column 42

(2011/11/12)

TETRAHYDROQUINOLINE DERIVATIVES AND THEIR PHARMACEUTICAL USE
Tetrahydroquinoline compounds of Formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
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Page/Page column 106-107

(2011/06/11)

IMIDAZO [1, 2 -A] PYRAZINE DERIVATIVES AND THEIR USE FOR THE PREVENTION OR TREATMENT OF NEUROLOGICAL, PSYCHIATRIC AND METABOLIC DISORDERS AND DISEASES
The present invention relates to novel imidazo[1,2-a]pyrazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
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Page/Page column 95-96

(2011/10/05)

cMET INHIBITORS
Compounds of the following formula are provided for use with cMET: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
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Page/Page column 154

(2010/04/03)

4, 6-DISUBSTITUTED 2-AMINO-PYRIMIDINES AS HISTAMINE H4 RECEPTOR MODULATORS
The present invention relates to substituted heterocyclic compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine H4 receptor inhibitors/antagonists useful in the treatment of histamine H4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.
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Page/Page column 169

(2010/07/09)

BENZOXAZINONE DERIVATIVES ACTING AS BETA2-ADRENORECEPTOR AGONIST FOR THE TREATMENT OF RESPIRATORY DISORDERS
The present invention provides a compound of formula (I), wherein W, R1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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Page/Page column 147-148

(2010/01/12)

KINASE INHIBITOR COMPOUNDS
Pyridine and pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.
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Page/Page column 48

(2008/12/07)

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
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Page/Page column 58-59

(2009/01/24)

FUSED HETEROCYCLIC DERIVATIVES AND METHODS OF USE
Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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Page/Page column 112-113

(2010/11/29)

Synthesis of pinacol esters of 1-alkyl-1H-pyrazol-5-yl- and 1-alkyl-1H-pyrazol-4-ylboronic acids
Starting from 1H-pyrazol, a wide number of 1-alkyl-1H-pyrazol-4-yl and 1-alkyl-1H-pyrazol-5-ylboronic acids and their pinacol esters were synthesized and characterized. The key step in the described methodology is the regioselective lithiation of the pyrazole ring. The synthesized pinacolates are stable under prolonged storage and can be used as convenient reagents in organic synthesis.
Ivachtchenko, Alexandre V.,Kravchenko, Dmitry V.,Zheludeva, Valentina I.,Pershin, Dmitry G.
p. 931 - 939
(2007/10/03)