专利号:US-12384788-B2 优先权日:2019-09-13 标 题 :1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine derivatives and related compounds as LRRK2, NUAK1 and/or TYK2 kinase modulators for the treatment of e.g. autoimmune disease 发明人:KOESTLER ROLAND; TASSEL JEAN; THORMANN MICHAEL; YEHIA NASSER; TREML ANDREAS; ALMSTETTER MICHAEL 权利人:ORIGENIS GMBH 摘要:The present invention relates to compounds of formula (I) that are capable of modulating, e.g., inhibiting or activating, one or more kinases, especially LRRK2 and/or NUAK1 and/or TYK2 or mutants thereof. The compounds are useful for treating diseases, such as autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, Alzheimer's disease, Parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 40 to 146; examples 1 to 63; compounds 1 to 248; tables 1 to 3). Preferred compounds are e.g. 1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine derivatives and related compounds. An exemplary compound is e.g. 5-(2,6-difluorophenyl)-8-methoxy-1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine (example 49). (Formula (II):
专利号:US-7169932-B2 优先权日:2001-06-11 标题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses, material for their synthesis 发明人:KUCERA DAVID JOHN; SCOTT ROBERT WILLIAM 权利人:PFIZER 摘要:Compounds of the formula: n nwhere the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.
专利号:US-5403845-A 优先权日:1991-08-27 标 题:Muscarinic agonists 发明人:DUNBAR PHILIP G; DURANT GRAHAM J; HOSS WAYNE P; MESSER JR WILLIAM S 权利人:UNIV TOLEDO 摘要:Substituted 1,4,5,6 -tetrahydropyrimidine compositions, substituted 1,2,3,6 -tetrahydropyrimidine compositions and substituted 3,4,5,6 -tetrahydropyridine compositions are disclosed. They are useful for stimulating muscarinic receptors including, for example, treating the symptoms of cognitive disorders, especially impaired memory, which are associated with decreased acetylcholine synthesis and cholinergic cell degeneration.