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1. 发明申请

WO1987003281A1 PROPANE-1,3-DIOL DERIVATIVES, A METHOD FOR THEIR PRODUCTION AND A PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：丙-1,3-二醇衍生物，其生产方法和药物组合物
公开(公告)号：WO1987003281A1
公开(公告)日：1987-06-04
申请号：PCT/DK1986000128
申请日：1986-11-20
申请人： LEO PHARMACEUTICAL PRODUCTS LTD. A/S , GRUE-SORENSEN, Gunnar , NIELSEN, Christian, Kaergaard
发明人： LEO PHARMACEUTICAL PRODUCTS LTD. A/S
IPC分类号： C07C93/04
CPC分类号： C07D277/24 , C07C271/06 , C07C333/02
摘要： A derivative of 2-methylenepropane-1,3-diol of general formula (I), where O-A and O-A , which can be the same or different, each represents O, O-C(O), O-C(O)NH, O-C(S)NH or O-C(O)O, R represents an alkyl or alkenyl group of 10 - 22 carbon atoms, n is an integer from 1 to 11, B represents a quaternary ammonium group, either NR R R , or N(Het), where R , R and R are similar or different alkyl groups of 1 - 4 carbon atoms, or two or all of R , R and R may be incorporated into a cyclic or bicyclic structure, which may contain additional hetero atoms; X means the anion of a pharmaceutically acceptable inorganic or organic acid; and R and R are the same or different, and represent hydrogen or alkyl groups of 1 - 4 carbon atoms. The present compounds have been shown to possess a PAF antagonistic effect and an inhibitory effect on the growth of tumor cells, and are thus valuable in the human and veterinary practice as platelet aggregation inhibitors, anti-thrombotic agents, anti-asthmatic agents, anti-allergic agents, anti-inflammatory agents, anti-hypotensive agents, anti-ulcer agents, anti-psoriatic agents, anti-graft rejection agents, anti-conception agents and anti-tumor agents.
摘要翻译：通式（I）的2-亚甲基丙烷-1,3-二醇的衍生物，其中OA 1和OA 2可以相同或不同，各自表示O，OC（O），OC（O ）NH，OC（S）NH或OC（O）O，R 1表示10-22个碳原子的烷基或烯基，n是1至11的整数，B +表示季铵基 NR 4 R 5 R 6或N（Het），其中R 4，R 5和R 6是相同或不同的1-4个碳原子的烷基，或 R 4，R 5和R 6中的两个或全部可以并入环状或双环结构，其可以含有另外的杂原子; 是指药学上可接受的无机酸或有机酸的阴离子; R 2和R 3相同或不同，代表氢或1-4个碳原子的烷基。本发明化合物已被证明具有PAF拮抗作用和对肿瘤细胞生长的抑制作用，因此在人和兽医学实践中作为血小板聚集抑制剂，抗血栓形成剂，抗哮喘药，抗 - 过敏剂，抗炎剂，抗低血压剂，抗溃疡剂，抗牛皮癣剂，抗移植物排斥剂，抗受孕剂和抗肿瘤剂。

2. 发明申请

WO1997037972A1 NOVEL VITAMIN D ANALOGUES 审中-公开
标题翻译：新维生素D类似物
公开(公告)号：WO1997037972A1
公开(公告)日：1997-10-16
申请号：PCT/DK1997000128
申请日：1997-03-21
申请人： LEO PHARMACEUTICAL PRODUCTS LTD. A/S (LOVENS KEMISKE FABRIK PRODUKTIONSAKTIESELSKAB) , GRUE-SORENSEN, Gunnar
发明人： LEO PHARMACEUTICAL PRODUCTS LTD. A/S (LOVENS KEMISKE FABRIK PRODUKTIONSAKTIESELSKAB)
IPC分类号： C07C401/00
CPC分类号： C07C401/00
摘要： The present invention relates to compounds of formula (I) in which Q stands for a C1-C8 hydrocarbylene diradical, R stands for hydrogen or C1-C6 hydrocarbyl, or two R groups, taken together with the carbon atom bearing the hydroxy group can form a C3-C8 carbocyclic ring. The compounds show antiinflammatory and immunomodulating effects as well as strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells.
摘要翻译：本发明涉及式（I）化合物，其中Q代表C1-C8亚烃基双基，R代表氢或C1-C6烃基，或两个R基团与带有羟基的碳原子一起形成一个C3-C8碳环。这些化合物显示出抗炎和免疫调节作用，以及在诱导分化和抑制某些细胞的不期望的增殖方面具有很强的活性。

3. 发明申请

WO1994014766A1 NOVEL VITAMIN D ANALOGUES 审中-公开
标题翻译：新维生素D类似物
公开(公告)号：WO1994014766A1
公开(公告)日：1994-07-07
申请号：PCT/DK1993000425
申请日：1993-12-17
申请人： LEO PHARMACEUTICAL PRODUCTS LTD. A/S (LOVENS ... , GRUE-SORENSEN, Gunnar , OTTOSEN, Erik, Rytter
发明人： LEO PHARMACEUTICAL PRODUCTS LTD. A/S (LOVENS ...
IPC分类号： C07C401/00
CPC分类号： C07C401/00
摘要： The present invention relates to compounds of formula (I) in which formula Y is sulfur, S(O), or S(O)2; R stands for C1-C3 alkyl, or (a) can form a C3-C8 carbocyclic ring, Q is a C1-C8 hydrocarbylene diradical; and derivatives thereof. The compounds show antiinflammatroy and immunomodulating effects as well as strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells.
摘要翻译：本发明涉及式（I）化合物，其中式Y为硫，S（O）或S（O）2; R代表C 1 -C 3烷基，或（a）可以形成C 3 -C 8碳环，Q是C 1 -C 8亚烷基双基; 及其衍生物。这些化合物显示抗炎和免疫调节作用，以及在诱导分化和抑制某些细胞的不期望的增殖方面具有很强的活性。

4. 发明申请

WO1995002577A1 NOVEL VITAMIN D ANALOGUES 审中-公开
标题翻译：新维生素D类似物
公开(公告)号：WO1995002577A1
公开(公告)日：1995-01-26
申请号：PCT/DK1994000271
申请日：1994-07-01
申请人： LEO PHARMACEUTICAL PRODUCTS LTD. A/S (LOVENS KEMISKE FABRIK PRODUKTIONSAKTIESELSKAB) , GRUE-SORENSEN, Gunnar
发明人： LEO PHARMACEUTICAL PRODUCTS LTD. A/S (LOVENS KEMISKE FABRIK PRODUKTIONSAKTIESELSKAB)
IPC分类号： C07C401/00
CPC分类号： C07C401/00
摘要： The present invention relates to compounds of formula (I) in which formula X is hydrogen or hydroxy; R and R , which may be the same or different, stand for hydrogen or C1-C4 hydrocarbyl; or R and R , taken together with the carbon atom bearing the group X, can form a C3-C8 carbocyclic ring; Q is a single bond or a C1-C4 hydrocarbylene diradical; R , R and/or Q may be optionally substituted with one or more fluorine atoms; and prodrugs of formula (I) in which one or more of the hydroxy groups are masked as groups which can be reconverted to hydroxy groups in vivo. The compounds show antiinflammatory and immunomodulating effects as well as strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells.
摘要翻译：本发明涉及式（I）化合物，其中式X为氢或羟基; R 1和R 2可以相同或不同，代表氢或C 1 -C 4烃基; 或R 1和R 2与带有基团X的碳原子一起可以形成C 3 -C 8碳环; Q是单键或C1-C4亚烃基双基; R 1，R 2和/或Q可任选被一个或多个氟原子取代; 和式（I）的前药，其中一个或多个羟基被掩蔽为可在体内再转化为羟基的基团。这些化合物显示出抗炎和免疫调节作用，以及在诱导分化和抑制某些细胞的不期望的增殖方面具有很强的活性。

5. 发明申请

WO1993019044A1 NOVEL VITAMIN D ANALOGUES 审中-公开
标题翻译：新维生素D类似物
公开(公告)号：WO1993019044A1
公开(公告)日：1993-09-30
申请号：PCT/DK1993000105
申请日：1993-03-23
申请人： LEO PHARMACEUTICAL PRODUCTS LTD. A/S (LOVENS ... , BRETTING, Claus, Aage, Svensgaard , GRUE-SORENSEN, Gunnar
发明人： LEO PHARMACEUTICAL PRODUCTS LTD. A/S (LOVENS ...
IPC分类号： C07C401/00
CPC分类号： C07C401/00
摘要： The invention relates to compounds of formula (I) in which formula X is hydrogen or hydroxy; R and R stand for hydrogen or a C1-C6 hydrocarbyl radical; or taken together with the carbon atom bearing the group X, can form a C3-C8 carbocyclic ring; R stands for hydrogen or a C1-C10 hydrocarbyl radical or for YR , in which Y stands for the radicals -CO-, -CO-O-, -CO-S-, -CS-, -CS-O-, -CS-S-, -SO- or -SO2-, and R stands for hydrogen or a C1-C10 hydrocarbyl radical; Q is a single bond or a C1-C8 hydrocarbylene diradical. R , R , R and/or Q may be optionally substitued with one or more deuterium or fluorine atoms. The compounds show an antiinflammatory and immunomodulating effect as well as strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells.
摘要翻译：本发明涉及式（I）化合物，其中式X为氢或羟基; R 1和R 2代表氢或C 1 -C 6烃基; 或与带有X基团的碳原子一起形成C 3 -C 8碳环; R 3代表氢或C 1 -C 10烃基或YR 4，其中Y代表基团-CO-，-CO-O-，-CO-S-，-CS-，-CS -O - ， - S-S-，-SO-或-SO 2 - ，R 4代表氢或C 1 -C 10烃基; Q是单键或C1-C8亚烃基双基。 R 1，R 2，R 3和/或Q可任选被一个或多个氘或氟原子取代。该化合物显示出抗炎和免疫调节作用，以及在诱导分化和抑制某些细胞的不期望的增殖方面具有很强的活性。

6. 发明申请

WO1991015475A1 NOVEL VITAMIN D ANALOGUES 审中-公开
标题翻译：新维生素D类似物
公开(公告)号：WO1991015475A1
公开(公告)日：1991-10-17
申请号：PCT/DK1991000091
申请日：1991-03-22
申请人： LEO PHARMACEUTICAL PRODUCTS LTD. A/S (LOVENS ... , CALVERLEY, Martin, John , GRUE-SORENSEN, Gunnar , BINDERUP, Ernst, Torndal
发明人： LEO PHARMACEUTICAL PRODUCTS LTD. A/S (LOVENS ...
IPC分类号： C07C401/00
CPC分类号： C07C401/00
摘要： The invention relates to compounds of formula (I) in which formula X is hydrogen or hydroxy; Y is oxygen or sulphur or oxidized sulphur (S(O) or S(O2)); R and R , which may be the same or different, stand for hydrogen or C1-C6 hydrocarbyl; or R and R , taken together with the carbon atom (starred in formula I) bearing the group X, can form a C3-C8 carbocyclic ring; Q is a C1-C8 hydrocarbylene diradical. R is hydrogen or C1-C6 hydrocarbyl. R , R and/or Q may be optionally substituted with one or more deuterium or fluorine atoms. n is 0 or 1. The present compounds, which find use both in the human and veterinary practice, show an antiinflammatory and immunomodulating effects as well as strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells, including cancer cells and skin cells.
摘要翻译：本发明涉及式（I）化合物，其中式X为氢或羟基; Y是氧或硫或氧化硫（S（O）或S（O 2））; R 1和R 2可以相同或不同，代表氢或C 1 -C 6烃基; 或R 1和R 2与带有基团X的碳原子（以式I表示的原子）一起可以形成C 3 -C 8碳环; Q是C1-C8亚烃基双基。 R 3是氢或C 1 -C 6烃基。 R 1，R 2和/或Q可任选被一个或多个氘或氟原子取代。 n是0或1.本发明化合物在人和兽医学实践中都有用，显示出抗炎和免疫调节作用，以及在诱导分化和抑制某些细胞（包括癌细胞和皮肤细胞）的不期望的增殖的强烈活性。

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