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11. 发明申请

WO2006105796A1 NOVEL INDOLINONE DERIVATIVES 审中-公开
标题翻译：新的吲哚啉酮衍生物
公开(公告)号：WO2006105796A1
公开(公告)日：2006-10-12
申请号：PCT/DK2006/000199
申请日：2006-04-07
申请人： LEO PHARMA A/S , DUVOLD, Laetitia, Maud, Elysa , HAVEZ, Sophie, Elisbeth , BINDERUP, Ernst, Torndal , ANDERSEN, Grith, Krøyer
发明人： DUVOLD, Laetitia, Maud, Elysa , HAVEZ, Sophie, Elisbeth , BINDERUP, Ernst, Torndal , ANDERSEN, Grith, Krøyer
IPC分类号： C07D209/34 , C07D401/14 , C07D401/12 , C07D405/14 , A61K31/40 , A61P29/00
CPC分类号： C07D401/14 , C07D209/34 , C07D401/12 , C07D405/14
摘要： The invention relates to novel indolinone derivatives of formula (I), wherein X, R1, R2, R3, R4, R5, Re, Ri', Ri , FV/ R4'/ FV and R6' are as shown herein, as well as their use in the treatment of inflammatory autoimmune diseases, in particular by administration via the oral route.
摘要翻译：本发明涉及式（I）的新的吲哚啉酮衍生物，其中X，R 1，R 2，R 3，R 4，R 5，R 6，R'，R 1，R F，R 4'/ FV和R 6'如本文所示，它们用于治疗炎性自身免疫性疾病，特别是通过口服途径给药。

12. 发明申请

WO2003097602A1 CYANOGUANIDINE PRODUGS 审中-公开
公开(公告)号：WO2003097602A1
公开(公告)日：2003-11-27
申请号：PCT/DK2003/000319
申请日：2003-05-15
申请人： LEO PHARMA A/S , BINDERUP, Ernst, Torndal
发明人： BINDERUP, Ernst, Torndal
IPC分类号： C07D213/02
CPC分类号： C07D213/75
摘要： Pyridyl cyanoguanidine compounds according to formula I wherein A, R 1 , R 2 , R 5 , R 6 , X 1 , X 2 , X 3 , X 4, Y 1 , Y 2 , Y 3 , Y 4 and n are as indicated in the description are useful as produgs in human and veterinary therapy of poliferative disease such as cancers.
摘要翻译：其中A，R 1，R 2，R 5，R 6，X 1，X 2，X 3，X 4，Y 1，Y 2，Y 3，Y 4和n如说明书中所示的式I的吡啶基氰基胍化合物可用作人和兽医疗法的复发性疾病如癌症。

13. 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。

14. 发明申请

WO1991000271A1 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：WO1991000271A1
公开(公告)日：1991-01-10
申请号：PCT/DK1990000156
申请日：1990-06-19
申请人： LEO PHARMACEUTICAL PRODUCTS LTD. A/S (LOVENS ... , CALVERLEY, Martin, John , 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 present invention relates to compounds of formula (I), in which formula, n is 0 or 1, m is 0 or an integer from 1-7, R and R (which may be the same or different) stand for hydrogen or C1-C8-hydrocarbyl, or, taken together with the carbon bearing the hydroxyl group (starred in formula I), R and R can form a saturated or unsaturated C3-C8 carbocyclic ring. In addition, R and/or R and/or one of the m carbons designatedby the " DEG " may be optionally substituted with a hydroxyl group or one or more chlorine or fluorine atom(s); and finally one of the carbons designated " DEG " may optionally be substituted by one or two C1-C2 alkyl group(s); and derivatives of the compounds of formula I in which one or more hydroxy have been transformed into -O-acyl or -O-glycosyl or phosphate ester groups; such masked groups being hydrolyzable in vivo. The present compounds find use in both the human and veterinary practice in the treatment and prophylaxis of autoimmune diseases (including diabetes mellitus), hypertension, acne, alopecia, skin ageing, imbalance in the imune system, inflammatory diseases such as rheumatoid arthritis and asthma as well as diseases characterized by abnormal cell differentiation and/or cell proliferation, such as e.g. psoriasis and cancer.
摘要翻译：本发明涉及式（I）化合物，其中n为0或1，m为0或1-7的整数，R 1和R 2（其可以相同或不同））代表氢或C 1 -C 8烃基，或者与带有羟基（式I化合物）的碳一起，R 1和R 2可以形成饱和或不饱和的C 3 -C 8碳环。此外，R 1和/或R 2和/或由“DEG”指定的m个碳之一可以任选被羟基或一个或多个氯或氟原子取代; 最后称为“DEG”的一个碳可以任选地被一个或两个C 1 -C 2烷基取代; 和其中一个或多个羟基已转化为-O-酰基或-O-糖基或磷酸酯基团的式I化合物的衍生物; 这种掩蔽基团在体内可水解。本发明化合物在人和兽医学实践中都可用于治疗和预防自身免疫性疾病（包括糖尿病），高血压，痤疮，脱发，皮肤老化，免疫系统失衡，类风湿性关节炎和哮喘等炎性疾病以及以异常细胞分化和/或细胞增殖为特征的疾病，例如，牛皮癣和癌症。

15. 发明申请

WO1986000902A1 DERIVATIVES OF METHYLENE-BISPHOSPHONIC ACID, PROCESS FOR THEIR PREPARATION AND A PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：甲基二磷酸的衍生物，其制备方法和药物组合物
公开(公告)号：WO1986000902A1
公开(公告)日：1986-02-13
申请号：PCT/DK1985000071
申请日：1985-07-25
申请人： LEO PHARMACEUTICAL PRODUCTS LTD. A/S , BINDERUP, Ernst, Torndal
发明人： LEO PHARMACEUTICAL PRODUCTS LTD. A/S
IPC分类号： C07F09/38
CPC分类号： C07F9/386
摘要： Hitherto unknown compounds of formula (I) in which R1 is a straight or branched, saturated or unsaturated aliphatic or alicyclic C1-C10 hydrocarbon radical, an aryl or an aryl-C1-C4-alkyl radical, R1 if desired being unsubstituted or substituted with straight or branched C1-C4-alkyl, amino, C1-C4-alkylamino, di-(C1-C4-alkyl)-amino, carboxy, C1-C4-alkoxycarbonyl, hydroxy, C1-C4-alkoxy, phenoxy, mercapto, C1-C4-alkylthio, phenylthio, halogen, trifluoromethyl; R2 stands for hydrogen, C1-C8-alkyl, aryl-C1-C4-alkyl or halogen; X is O or S and n is an integer from 0 to 2; with the proviso that R2 cannot be hydrogen or methyl if n=0 and R1 is methyl. The compounds of the invention are valuable in the human and veterinary practice.
摘要翻译：迄今未知的式（I）化合物，其中R 1是直链或支链，饱和或不饱和的脂族或脂环族C 1 -C 10烃基，芳基或芳基-C 1 -C 4烷基，如果需要，R 1是未取代的或被直链或支链C 1 -C 4 - 烷基，氨基，C 1 -C 4烷基氨基，二 - （C 1 -C 4 - 烷基） - 氨基，羧基，C 1 -C 4烷氧基羰基，羟基，C 1 -C 4 - 烷氧基，苯氧基，巯基，C 1 -C 1-4 - 烷硫基，苯硫基，卤素，三氟甲基; R2代表氢，C1-C8-烷基，芳基-C1-C4-烷基或卤素; X是O或S，n是0至2的整数; 条件是如果n = 0，R 2不能为氢或甲基，并且R 1为甲基。本发明的化合物在人和兽医学实践中是有价值的。

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