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1.发明授权VITAMIN D-DERIVATE MIT SUBSTITUENTEN AN C-25, VERFAHREN ZU IHRER HERSTELLUNG, ZWISCHENPRODUKTE UND DIE VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN 失效在C-25，产生，中间体和使用用于生产药物的方法用的取代基维生素D衍生物
公开(公告)号：EP0832063B1
公开(公告)日：2000-02-23
申请号：EP96915001.0
申请日：1996-04-30
发明人： KIRSCH, Gerald , STEINMEYER, Andreas , NEEF, Günter , SCHWARZ, Katica , THIEROFF-EKERDT, Ruth , WIESINGER, Herbert , MENRAD, Andreas , HABEREY, Martin
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00
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2.发明授权23-OXA-DERIVATE IN DER VITAMIN-D-REIHE, VERFAHREN ZU IHRER HERSTELLUNG, DIESE DERIVATE ENTHALTENDE PHARMAZEUTISCHE PRÄPARATE SOWIE DEREN VERWENDUNG ALS ARZNEIMITTEL 失效中的维生素D系列23 OXA衍生物，METHOD FOR PRODUCING这些衍生物药物制剂和它们作为药物
公开(公告)号：EP0639179B1
公开(公告)日：1996-05-29
申请号：EP92903336.3
申请日：1992-01-20
发明人： NEEF, Günter , STEINMEYER, Andreas , KIRSCH, Gerald , SCHWARZ, Katica , HABEREY, Martin , THIEROFF-EKERDT, Ruth , RACH, Petra
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00
摘要： The invention concerns 23-oxa derivatives of vitamins of the D-series, the derivatives having the formula (I), in which R?1, R2 and R4¿, independently of each other, may be a hydrogen atom or an acyl group with 1-9 carbon atoms; each R3 may be a hydrogen atom or a straight-chain or branched-chain alkyl group with 1-4 carbon atoms; and x is an alkylene residue-(CH¿2?)n-in which n =1, 2 or 3, neither of the R?3¿ groups being methyl or propyl when n = 1. The invention also concerns a method of preparing such derivatives. The compounds have a proliferation inhibiting and cell differentiating effect and are suitable for the production of medicaments.
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公开(公告)号：EP0413006A1
公开(公告)日：1991-02-20
申请号：EP90902143.0
申请日：1990-01-29
CPC分类号： C07D295/185 , C07C235/06
摘要： Emploi de dérivés d'acide carboxylique d'hydroxyalkane de formule générale (I), où n représente un nombre compris entre 7 et 18, R1 est un atome d'hydrogène ou un groupe acyle avec 16 atomes de carbone au maximum et R2 et R3 représentent chacun des groupes alkyle avec 8 atomes de carbone au maximum ou ensemble représentent un groupe alkylène avec 4 à 8 atomes de carbone, éventuellement interrompu par un atome d'oxygène ou un atome d'azote, pour fabriquer un médicament destiné au traitement topique de maladies de la peau et des muqueuses.
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4.发明公开NEUE VITAMIN D-DERIVATE MIT SUBSTITUENTEN AN C-25, VERFAHREN ZU IHRER HERSTELLUNG, ZWISCHENPRODUKTE UND DIE VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN 失效在C-25，生产，中间体用于制造药物的方法和使用带有取代基NEW维生素D衍生物
公开(公告)号：EP0832063A1
公开(公告)日：1998-04-01
申请号：EP96915001.0
申请日：1996-04-30
发明人： KIRSCH, Gerald , STEINMEYER, Andreas , NEEF, Günter , SCHWARZ, Katica , THIEROFF-EKERDT, Ruth , WIESINGER, Herbert , MENRAD, Andreas , HABEREY, Martin
CPC分类号： C07C401/00
摘要： The invention concerns novel vitamin D derivatives with C-25 substituents of general formula (I). The invention also concerns a process for their preparation and their use in preparing medicaments.
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5.发明授权22-EN-25-OXA-DERIVATE IN DER VITAMIN D-REIHE, VERFAHREN ZU IHRER HERSTELLUNG, DIESE DERIVATE ENTHALTENEN PHARMAZEUTISCHE PRÄPARATE SOWIE DEREN VERWENDUNG ALS ARZNEIMITTEL 失效中的维生素D系列22-EN-25-OXA衍生物，制备这些衍生物的方法所含药物制剂和它们作为药物
公开(公告)号：EP0649405B1
公开(公告)日：1997-03-26
申请号：EP93915800.2
申请日：1993-06-30
发明人： STEINMEYER, Andreas , KIRSCH, Gerald , NEEF, Günter , SCHWARZ, Katica , THIEROFF-EKERDT, Ruth , WIESINGER, Herbert , HABEREY, Martin
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07F7/1852 , C07C401/00
摘要： The invention concerns 22-ene-25-oxa derivatives of the vitamin D series of general formula (I), in which R?1, R2 and R4¿, independently of each other, may each be a hydrogen atom, an alkanoyl group with 1 to 9 carbon atoms or an aroyl group; each R3 may be a hydrogen atom, a straight-chain or branched-chain alkyl group with 1 to 4 carbon atoms or a trifluoromethyl group, or the two R¿3? groups, together with the tertiary carbon atom to which they are attached, may form a saturated or unsaturated 3-, 4-, 5- or 6-membered carboxyclic or heterocyclic ring; and X is an alkylene group of the formula -(CH2)n- in which n = 1, 2 or 3. The invention also concerns a method of preparing such derivatives and their pharmaceutical use in the treatment of hyperproliferative diseases.
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6.发明授权
公开(公告)号：EP0663902B1
公开(公告)日：1998-03-11
申请号：EP93922944.9
申请日：1993-10-06
发明人： STEINMEYER, Andreas , KIRSCH, Gerald , NEEF, Günter , SCHWARZ, Katica , THIEROFF-EKERDT, Ruth , WIESINGER, Herbert , HABEREY, Martin
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00
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7.发明公开
公开(公告)号：EP0663902A1
公开(公告)日：1995-07-26
申请号：EP93922944.0
申请日：1993-10-06
发明人： STEINMEYER, Andreas , KIRSCH, Gerald , NEEF, Günter , SCHWARZ, Katica , THIEROFF-EKERDT, Ruth , WIESINGER, Herbert , HABEREY, Martin
CPC分类号： C07C401/00
摘要： Described are the new 25-carboxylic acid derivatives of general formula (I), R?19 and R19a¿ each denoting a hydrogen atom or in common an exocyclic methyl group, R?21 and R21a¿ independently of each other denoting a hydrogen atom, a chlorine or fluorine atom, an alkyl group with 1-4 carbon atoms, in common a methylene group, a 3-7 membered, saturated or unsaturated carbocyclic ring in common with the quaternary 20 carbon atom, Y preferably denoting a derivatized carboxyl residue, with the other substituents as indicated in the description, and a method of producing them. The new compounds possess vitamin D activity as well as anti-proliferative and cell-differentiating action and can be used in the manufacture of medicines.
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8.发明公开22-EN-25-OXA-DERIVATE IN DER VITAMIN D-REIHE, VERFAHREN ZU IHRER HERSTELLUNG, DIESE DERIVATE ENTHALTENEN PHARMAZEUTISCHE PRÄPARATE SOWIE DEREN VERWENDUNG ALS ARZNEIMITTEL 失效中的维生素D系列22-EN-25-OXA衍生物，制备这些衍生物的方法所含药物制剂和它们作为药物。
公开(公告)号：EP0649405A1
公开(公告)日：1995-04-26
申请号：EP93915800.0
申请日：1993-06-30
发明人： STEINMEYER, Andreas , KIRSCH, Gerald , NEEF, Günter , SCHWARZ, Katica , THIEROFF-EKERDT, Ruth , WIESINGER, Herbert , HABEREY, Martin
CPC分类号： C07F7/1852 , C07C401/00
摘要： The invention concerns 22-ene-25-oxa derivatives of the vitamin D series of general formula (I), in which R1, R2 and R4, independently of each other, may each be a hydrogen atom, an alkanoyl group with 1 to 9 carbon atoms or an aroyl group; each R3 may be a hydrogen atom, a straight-chain or branched-chain alkyl group with 1 to 4 carbon atoms or a trifluoromethyl group, or the two R3 groups, together with the tertiary carbon atom to which they are attached, may form a saturated or unsaturated 3-, 4-, 5- or 6-membered carboxyclic or heterocyclic ring; and X is an alkylene group of the formula -(CH2)n- in which n = 1, 2 or 3. The invention also concerns a method of preparing such derivatives and their pharmaceutical use in the treatment of hyperproliferative diseases.
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9.发明公开23-OXA-DERIVATE IN DER VITAMIN-D-REIHE, VERFAHREN ZU IHRER HERSTELLUNG, DIESE DERIVATE ENTHALTENDE PHARMAZEUTISCHE PRÄPARATE SOWIE DEREN VERWENDUNG ALS ARZNEIMITTEL 失效中的维生素D系列23-OXA衍生物，方法用于生产这些衍生物的药物制剂及其使用药物。
公开(公告)号：EP0639179A1
公开(公告)日：1995-02-22
申请号：EP92903336.0
申请日：1992-01-20
发明人： NEEF, Günter , STEINMEYER, Andreas , KIRSCH, Gerald , SCHWARZ, Katica , HABEREY, Martin , THIEROFF-EKERDT, Ruth , RACH, Petra
CPC分类号： C07C401/00
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公开(公告)号：EP0413006B1
公开(公告)日：1994-10-19
申请号：EP90902143.8
申请日：1990-01-29
IPC分类号： C07C235/06 , C07D295/18 , C07D265/30 , A61K31/16 , A61K31/40 , A61K31/535
CPC分类号： C07D295/185 , C07C235/06
摘要： Use of hydroxyalkane carboxylic acid derivatives of formula general (I), where n stands for a number from 7 to 18, R1 is a hydrogen atom or an acyl group with not more than 16 carbon atoms and R2 and R3 each stand for alkyl groups with not more than 8 carbon atoms or together stand for an alkylene group with 4 to 8 carbon atoms possibly interrupted by an oxygen atom or a nitrogen atom, to manufacture a drug for topical treatment of diseases of the skin and mucous membranes.
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