136866-33-6Relevant articles and documents
N-[ 4 - (1H-pyrazolo [3,4-b] pyrazin-6-yl)-phenyl]-sulfamide and their use as medicaments
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Paragraph 0341; 0343; 0344, (2016/10/09)
The invention relates to N-[4-(1H-pyrazolo[3,4-b] pyrazine-6-yl)-phenyl]-sulfonamides of a formula I. In the formula I, Ar, R1, R2 and n have meanings as shown in the claims. The compounds of the formula I are compounds which are valuable, have pharmacological activity and can adjust the activity of protein kinase, particularly the activity of serum and glucocorticoid induced kinase (SGK), and more particularly the activity of serum and glucocorticoid induced kinase isoform (SGK-1, SGK1). The compounds are suitable for treating diseases with inappropriate activity of the SGK, such as degenerative joint diseases or inflammatory process such as osteoarthritis or rheumatism. The invention also relates to a method for preparing the compounds of the formula I, an application of the compounds serving as the medicines and medicine compositions containing the compounds.
Discovery of N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as highly active and selective SGK1 inhibitors
Halland, Nis,Schmidt, Friedemann,Weiss, Tilo,Saas, Joachim,Li, Ziyu,Czech, J?rg,Dreyer, Matthias,Hofmeister, Armin,Mertsch, Katharina,Dietz, Uwe,Strübing, Carsten,Nazare, Marc
supporting information, p. 73 - 78 (2015/01/30)
From a virtual screening starting point, inhibitors of the serum and glucocorticoid regulated kinase 1 were developed through a combination of classical medicinal chemistry and library approaches. This resulted in highly active small molecules with nanomolar activity and a good overall in vitro and ADME profile. Furthermore, the compounds exhibited unusually high kinase and off-target selectivity due to their rigid structure. (Chemical Presented).
N-[ 4-(1H-pypazolo [3, 4-b] aminopyrazine-6-yl)-phenyl]-and its use as a chemical acylsulfonamide
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Paragraph 0134, (2017/01/02)
PROBLEM TO BE SOLVED: To provide a compound effective for the treatment of diseases due to the inadequacy of serum and glucocorticoid adjustment kinase (SGK) activities, for instance, degenerative arthropathy or inflammatory process, e.g., osteoarthritis or rheumatism, to provide its use as a drug, and to provide a pharmaceutical composition containing the same. SOLUTION: The compound is represented by formula I ( wherein, Ar is selected from the group consisting of phenyl and five- or six-membered monocyclic aromatic heterocyclic rings each containing a ring heteroatom selected from the group consisting of nitrogen, oxygen and sulfur; R1 is H, amino or the like; R2 is a halogen atom, alkyl or the like; and n is 0, 1 or 2). COPYRIGHT: (C)2013,JPOandINPIT
N-[4-(1h-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides and their use as pharmaceuticals
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Paragraph 0130, (2013/03/28)
The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS
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Page/Page column 93, (2013/04/10)
The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula (I), (R2)n wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS
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Page/Page column 92, (2013/04/10)
The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]- sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS
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Paragraph 0325, (2013/03/28)
The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them
Metalation of diazines IV. Lithiation of sym-disubstituted pyrazines
Turck, A.,Trohay, D.,Mojovic, L.,Ple, N.,Queguiner, G
, p. 301 - 310 (2007/10/02)
Conditions for the metalation of 2,6-dichloro- and 2-6-dimethoxy-pyrazine are defined and the lithio-derivatives are shown to react with some electrophiles.A convenient synthesis of a diazaxanthone from the lithio-derivative of the dichloro-compund is des
