- Preparation method 4 -chloro - 7H - pyrrolo [2, 3 - d] pyrimid -5 - carbonitrile
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The invention discloses a preparation method of 4 -chloro - 7H - pyrrolo [2, 3 - d] pyrimid -5 - carbonitrile which firstly utilizes phosphorus oxychloride and N, N - dimethyl formamide to prepare a vinol Michael reagent and 4 - chlorine - 7H - pyrrolo [2, 3 - d] pyrimidine to generate 4 -chloro - 7H - pyrrolo [2, 3 - d] pyrimidine -5 - formaldehyde. , 4 - Chloro - 7H - pyrrolo [2, 3 - d] pyrimidine -5 - formaldehyde is trioximated with hydroxylamine hydrochloride under the action of a base to obtain 4 -chloro - 7H - pyrrolo [2, 3 - d] pyrimidine -5 - formaldehyde oxime. The reaction of 4 - chloro - 7H - pyrrolo [2, 3 - d] pyrimid -5 - methanal oxime under the action of a dehydrating reagent generates 4 - chloro - 7H - pyrrolo [2, 3 - d] pyrimid -5 - carbonitrile. The raw materials adopted by the method are cheap and easily available, the synthesis method is simple to operate, the reaction conditions are mild, requirements on equipment are low, and the method is suitable for industrial large-scale production.
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Paragraph 0035; 0042-0044; 0045; 0052-0054; 0055; 0061-0063
(2021/09/08)
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- HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
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Paragraph 00942
(2013/03/26)
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- HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
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Page/Page column 81-82
(2012/05/21)
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- ASK1 INHIBITING PYRROLOPYRIMIDINE DERIVATIVES
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This invention relates to pyrrolopyrimidine derivatives of formula (I): where R1, X, p, R4, R2and R3are as defined herein, and their use as pharmaceuticals.
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Page/Page column 12; 44
(2012/06/30)
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- CHEMICAL COMPOUNDS, COMPOSITIONS AND METHODS FOR KINASE MODULATION
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Chemical compounds that modulate kinase activity, including PI3 kinase activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
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Page/Page column 110-111
(2011/12/04)
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- NEW ANTIVIRAL MODIFIED NUCLEOSIDES
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This invention relates to novel compounds that have various medicinal applications, e.g. for the treatment and/or prevention of viral infections.
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Page/Page column 96
(2010/04/03)
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- Heterocyclic Compounds Useful as RAF Kinase Inhibitors
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The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
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Page/Page column 25
(2009/01/24)
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- AMINE DERIVATIVES USEFUL AS ANTICANCER AGENTS
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The invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein: A is a moiety of formula (Il) and to pharmaceutically acceptable salts and solvates thereof, wherein X, Z, D, E, V, W, Y, R1, R2, R5, R6, L, and u are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula I to a patient in need thereof, and to compositions for treating such disorders which contain the compounds of formula (I). The invention also relates to methods of making the compounds of formula (I).
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Page/Page column 83
(2010/11/30)
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- Monocyclic-7H-pyrrolo[2,3-d]pyrimidine compounds, compositions, and methods of use
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Novel pyrrolo[2,3-d]pyrimidine compounds useful as inhibitors of the enzyme protein tyrosine kinases such as Janus Kinase 3 as well as immunosuppressive agents for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, Leukemia and other autoimmune diseases are described.
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Page/Page column 28
(2008/06/13)
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- Heterocyclic ring-fused pyrimidine derivatives
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The present invention relates to heterocyclic ring-fused pyrimidine derivatives of formula (I) or stereoisomers, pharmaceutically acceptable salts or prodrugs thereof, wherein Z and Y are as defined in the specification. Compounds of formula (I) are useful in the treatment of hyperproliferative diseases, such as cancers and acnes, in mammals:
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