796729-03-8Relevant academic research and scientific papers
Focal adhesion kinase inhibitor and use
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Paragraph 0372; 0384; 0385, (2019/01/08)
The invention belongs to the field of medicines, relates to a focal adhesion kinase inhibitor and use, in particular relates to a novel focal adhesion kinase inhibitor compound, or stereoisomers, geometric isomers, tautomers, oxynitrides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, further relates to the use of the compound and pharmaceutical compositions as medicines, in particular the use of the compound and pharmaceutical compositions in manufacture of medicines for treatment or prevention of cancer, pulmonary hypertension, and pathological angiogenesis-related diseases.
BIARYL COMPOUNDS USEFUL FOR THE TREATMENT OF HUMAN DISEASES IN ONCOLOGY, NEUROLOGY AND IMMUNOLOGY
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Paragraph 0546, (2015/06/25)
The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.
8-FLUOROPHTHALAZIN-1(2H)-ONE COMPOUNDS
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Paragraph 0581, (2013/05/21)
8-Fluorophthalazin-1(2h)-one compounds of Formula II where one or two of X1, X2, and X3 are N, are provided, 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 II for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
PYRAZOLE COMPOUNDS FOR CONTROLLING INVERTEBRATE PESTS
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Page/Page column 88, (2010/04/27)
The present invention relates to a method for controlling invertebrate pests which method comprises treating the pests, their food supply, their habitat or their breeding ground or a plant, seed, soil, area, material or environment in which the pests are growing or may grow, or the materials, plants, seeds, soils, surfaces or spaces to be protected from pest attack or infestation with a pesticidally effective amount of a pyrazole compound of formulae I or II or a salt or an N-oxide thereof, wherein A is a pyrazole radical of the formulae A1 or A2, wherein # denotes the binding; D is a 5- or 6-membered heterocyclic radical fused to the pyrazole moiety; Rp1, Rp2 and Rpx are H, halogen, CN, NO2, C1-C10-alkyl, C2-C10- alkenyl, C2-C10-alkynyl, etc.; n is 0 to 4; or two radicals Rpx bound to the same ring- member may form an oxo substituent, or two radicals Rpx bound to adjacent ring- members may form a 3- to 7-membered fused cyclic radical; B is N or CR4, wherein R4 is H, halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, etc.; X1 is S, O or NR1a, wherein R1a is H, C1-C10-alkyl, etc.; X2 is O2a, NR2bR2c or S(O)mR2d, wherein m is 0, 1 or 2; R2a is C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, etc.; R2b, R2c are H, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, etc.; R2d is C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, etc.; R1 is H, CN, C1-C10-alkyl, C1-C10-haloalkyl, C3-C10-cycloalkyl, etc.; R2, R3 and R5 are H, halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, etc.; to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material comprising at least one compound of formulae I or II, to a method for treating or protecting an animal from infestation or infection by parasites, to novel pyrazole compounds of formulae I or Il and agricultural composition containing those compounds.
Selective hydrolysis of ethyl 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole-2- carboxylate and ethyl 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole-3-carboxylate as a key step in the large-scale synthesis of bicyclic heteroaryl carboxyaldehydes
Nikitenko,Winkley,Zeldis,Kremer,Chan,Strong,Jennings,Jirkovsky,Blum,Khafizova,Grosu,Venkatesan
, p. 712 - 716 (2012/12/22)
The isomeric mixture of ethyl 5,6-dihydro-4H-pyrrolo[1,2-b]-pyrazole-2- and -3-carboxylates (14 and 15), derived from a proline meso-ionic synthon, demonstrated remarkably different stabilities towards alkaline hydrolysis. On that basis, a non-chromatographic, highly efficient method for their large-scale separation was developed. The desired isomer 14 was converted into 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole-2-carbaldehyde, a key intermediate in the synthesis of bicyclic heteroaryl-substituted 6-alkylidene penems.
Process for synthesizing beta-lactamase inhibitor intermediates
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Page 14-15, (2008/06/13)
There is provided a process for the preparation of bicyclicheteroaryl carboxaldehydes having the structural Formula I where X and Y are defined in the specification The bicyclic heteroaryl carboxaldehydes are useful as intermediates in the preparation of β-lactamase inhibitors.
Pyrazolopyrimidine derivatives
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Page 59, (2010/01/31)
The present invention provides a compound of formula (I): where Q is a group of formula: These compounds inhibit cyclic guanosine 3',5'-monophosphate phosphodiesterases (cGMP PDEs). More notably, the compounds are potent and selective inhibitors of the type 5 cyclic guanosine 3',5'-monophosphate phosphodiesterases and have utility therefore in a variety of therapeutic areas. In particular, the present compounds are of value for the curative or prophylactic treatment of mammalian sexual disorders.
