专利号:US-6413957-B1 优先权日:1998-04-21 标题:Methods of inhibiting cell proliferation using indeno [1,2-c]pyrazol-4-ones 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W 权利人:BRISTOL MYERS SUIBB PHARMA COM 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:WO-02076965-A1 优先权日:2001-03-23 标 题 :Non peptide mimetics based on the active sequence s42fllr46 of the thrombin receptor for the treatment of thrombosis and cancer 发明人:MATSOUKAS JOHN; MARAGOUDAKIS MICHAEL; VLAHAKOS DEMETRIOS; ALEXOPOULOS KOSTAS 权利人:MATSOUKAS JOHN; MARAGOUDAKIS MICHAEL; VLAHAKOS DEMETRIOS; ALEXOPOULOS KOSTAS 摘要:The invention relates to novel non peptide compounds (mimetics) based on a thrombin receptor sequence and novel methods for the synthesis of these compounds. These compounds act as agonists or antagonists in a variety of cells including endothelial cells, blood platelets, vascular smooth muscle cells and tumor cells. They are useful in the treatment of thrombosis an cardiovascular diseases and modulation of angiogenesis for cancer treatment or wound healing.
专利号:US-7250435-B2 优先权日:1999-10-20 标 题:Acylsemicarbazides as cyclin dependent kinase inhibitors useful as anti-cancer and anti-proliferative agents 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; VIDWANS ANUP P; YUE EDDY 权利人:BRISTOL MYERS SQUIBB PHARMA CO 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n nthat are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G.n n This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:US-6407103-B2 优先权日:1998-04-21 标 题:Indeno [1,2-c] pyrazol-4-ones and their uses 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W 权利人:BRISTOL MYERS SQUIBB PHARMA CO 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I):that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-9 and their regulatory subunits know as cyclins A-H.This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:US-6593356-B2 优先权日:1999-10-20 标 题 :Acylsemicarbazides as cyclin dependent kinase inhibitors useful as anti-cancer and anti-proliferative agents 发明人:NUGIEL DAVID; CARINI DAVID; DIMEO SUSAN; VIDWANS ANUP; YUE EDDY 权利人:BRISTOL MYERS SQUIBB PHARMA CO 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I):that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G.This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:WO-2023071601-A1 优先权日:2021-10-28 标题:Desloratadine derivative, preparation method therefor and application thereof 发明人:YAO CHEN 权利人:TIANJIN NEWSUN INVEST DEVELOPMENT CO LTD 摘要:Disclosed in the present application is a compound as represented by formula (A), wherein-R is-R' or -Y-(CH 2 ) n -R', Y is O or NH, n is 1, 2, 3, 4, 5 or 6, and -R' is diethylamino, pyrrolidinyl, piperazinyl, N-morpholinyl, bis(2-methoxyethyl)amino or 4-methylpiperazinyl. Also disclosed are a synthesis method for the compound shown, and use of the compound shown in the preparation of drugs for relieving or treating or preventing allergy and related symptoms thereof.
参考文献:10.1007/bf02510054 摘要:Marek ÉM, Smirnova TA, Kochetova NF. Methods of gas chromatography in chemico-pharmaceutical industry. Part II. determination of the parent compound and impurities in 1-amino-4-methylpiperazine. Pharmaceutical Chemistry Journal. 1999 May;33(5):283–5. doi: 10.1007/bf02510054.