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公开(公告)号：EP2308886B1
公开(公告)日：2016-12-07
申请号：EP09766724.0
申请日：2009-06-19
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公开(公告)号：EP1314427A1
公开(公告)日：2003-05-28
申请号：EP01956911.0
申请日：2001-08-16
IPC分类号： A61K31/593 , A61P19/10 , A61P3/02
CPC分类号： A61K31/593
摘要： The object of the present invention is to provide a therapeutic agent for osteoporosis with a good bone mass-increasing effect, but almost no blood calcium-increasing effect.
The present invention provides a therapeutic agent for osteoporosis which comprises, as an active ingredient, a compound of Formula (1):
wherein
R 1 and R 2 each represent a hydrogen atom or a methyl group,
R 3 represents a C 1 -C 4 alkyl group which may be substituted with a fluorine atom,
m represents an integer of 0 to 3, and
A represents -CH 2 -CH 2 -, -CH=CH- or -C≡C-.摘要翻译： 本发明的目的是提供骨质疏松症的治疗剂，具有良好的骨量增加效果，但几乎没有血钙增加作用。 本发明提供骨质疏松症治疗剂，其包含作为活性成分的式（1）化合物：其中R 1和R 2各自表示氢原子或甲基，R 3表示C 1 -C 4烷基 其可以被氟原子取代，m表示0〜3的整数，A表示-CH 2 -CH 2 - ， - CH = CH-或-C。
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3.发明公开CRYSTALLINE FORMS OF (1S,3'R,4'S,5'S,6'R)-6-[(4-ETHYLPHENYL)METHYL]-3',4',5',6'-TETRAHYDRO-6'- (HYDROXYMETHYL)SPIRO[ISOBENZOFURAN-1(3H) 2'-[2H]PYRAN]-3',4',5'-TRIOL 审中-公开（1S，3'R，4'S，5'S，6'R）-6 - [（4-乙基苯基）甲基] -3'，4'，5'，6'-四氢-6' - （羟基甲基） SPIRO [异苯并呋喃-1（3H）2' - [2H]吡喃] -3'，4'，5'-三醇
公开(公告)号：EP3170834A1
公开(公告)日：2017-05-24
申请号：EP16202285.9
申请日：2009-06-19
IPC分类号： C07H19/01 , C07H1/00 , C07D493/10
摘要： The present invention relates to crystalline forms of the compound represented by Formula (XI), which is useful for preventing or treating diabetes.
摘要翻译： 本发明涉及由式（XI）表示的化合物的结晶形式，其可用于预防或治疗糖尿病。
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公开(公告)号：EP4036100A1
公开(公告)日：2022-08-03
申请号：EP22155547.7
申请日：2009-06-19
发明人： MURAKATA, Masatoshi , IKEDA, Takuma , KIMURA, Nobuaki , KAWASE, Akira , NAGASE, Masahiro , YAMAMOTO, Keisuke , TAKATA, Noriyuki , YOSHIZAKI, Shinichi , TAKANO, Koji
IPC分类号： C07H19/01 , C07H1/00 , C07D493/10 , A61P3/10
摘要： The present invention relates to compounds represented by Formulas (IVb) and (VI):
and to a process for preparing a compound represented by Formula (I) using compound (IVb):-
5.发明授权METHOD FOR PRODUCING VITAMIN D DERIVATIVE UTILIZING PHOTOREACTION 有权METHOD FOR PRODUCTION维生素D衍生物使用光响应
公开(公告)号：EP1961740B1
公开(公告)日：2013-04-24
申请号：EP06833694.0
申请日：2006-11-30
发明人： KAWASE, Akira , KATO, Yasuharu , KINOSHITA, Kazutomo , KITOH, Yasushi , IKEDA, Takuma , HANEISHI, Tsuyoshi , MARUYAMA, Noriaki , KOBAYASHI, Mio
IPC分类号： C07C401/00 , C07J41/00 , C07J71/00
CPC分类号： C07C401/00 , C07J41/00 , C07J71/00
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公开(公告)号：EP2308886A1
公开(公告)日：2011-04-13
申请号：EP09766724.0
申请日：2009-06-19
发明人： MURAKATA, Masatoshi , IKEDA, Takuma , KIMURA, Nobuaki , KAWASE, Akira , NAGASE, Masahiro , YAMAMOTO, Keisuke , TAKATA, Noriyuki , YOSHIZAKI, Shinichi , TAKANO, Koji
IPC分类号： C07H19/01 , A61K31/7048 , A61P3/10 , C07H7/04 , C07H23/00
摘要： The present invention provides a process for preparing a spiroketal derivative, via an intermediate represented by Formula (VI):
wherein variable groups and numbers are as defined in the specification, which can be produced from dihalobenzene derivatives in one pot reaction.摘要翻译： 本发明提供了经由式（VI）代表的中间体制备螺缩酮衍生物的方法：其中可变基团和数量如说明书中所定义，其可以由一卤代苯衍生物在一锅反应中制备。
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公开(公告)号：EP1061070B1
公开(公告)日：2008-07-16
申请号：EP99905280.6
申请日：1999-02-23
IPC分类号： C07C401/00 , C07C35/32 , C07C49/443 , C07C43/178 , C07C33/44 , C07F7/18 , A61K31/59
CPC分类号： C07C401/00 , C07C33/44 , C07C35/32 , C07C2601/14 , C07C2602/24 , C07F7/1856 , Y02P20/55
摘要： Vitamin D derivatives having general formula (1) which are hydroxylated at the 24-position and considered as one of metabolites of physiologically active vitamin D derivatives substituted at the 2β-position wherein R1, R2, R3 and R4 are the same or different and each represents hydrogen or a protective group; X and Y represent each H or OR5, provided that Y is OR5 when X is H, and Y is H when X is OR5 (wherein R5 represents hydrogen or a protective group, or R1 and R5 may together form a vicinal-diol protective group); synthesis intermediates useful in synthesizing these vitamin D derivatives; and medicinal compositions containing these vitamin D derivatives.
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8.发明授权VITAMIN D DERIVATIVES POSSESSING A 22-OXA OR 22-THIA ATOM, A C17-SIDE CHAIN SUBSTITUTED BY AN ACID, ESTER OR AMIDE GROUP AND A 16(17)-DOUBLE BOND 有权WITH A 22-氧杂或22硫杂原子，氧，酯或酰胺含有取代C17-侧链和16（17） - 双键维生素D衍生物
公开(公告)号：EP1295871B1
公开(公告)日：2011-05-18
申请号：EP01938659.8
申请日：2001-06-14
IPC分类号： C07C401/00 , C07D295/185 , C07J7/00 , C07J9/00 , A61K31/592 , A61K31/593 , A61P3/02 , A61P17/00 , C07F7/18
CPC分类号： C07D295/185 , A61K31/592 , A61K31/593 , C07C235/06 , C07C401/00 , C07C2601/14 , C07C2602/24 , C07F7/1856 , C07J7/00 , C07J9/00 , Y02P20/55
摘要： Provided are vitamin D derivatives which exhibit excellent physiologic activities suitable for drugs, particularly remedies for dermatoses such as psoriasis, and are lowered in the calcium increasing activity. The derivatives are represented by the general formula (1): (1) wherein X is oxygen or sulfur; m is a number of 1 to 3; R1 and R2 are each hydrogen or alkyl; R4 and R5 are each hydrogen, hydroxyl, or the like; R3 is YR8 or the like; R6 is hydrogen or the like; and R7 is hydrogen or the like.
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9.发明公开METHOD FOR PRODUCING VITAMIN D DERIVATIVE UTILIZING PHOTOREACTION 有权METHOD FOR PRODUCTION维生素D衍生物使用光响应
公开(公告)号：EP1961740A1
公开(公告)日：2008-08-27
申请号：EP06833694.0
申请日：2006-11-30
发明人： KAWASE, Akira , KATO, Yasuharu , KINOSHITA, Kazutomo , KITOH, Yasushi , IKEDA, Takuma , HANEISHI, Tsuyoshi , MARUYAMA, Noriaki , KOBAYASHI, Mio
IPC分类号： C07C401/00 , C07J41/00 , C07J71/00
CPC分类号： C07C401/00 , C07J41/00 , C07J71/00
摘要： There are provided a novel process for producing [{(5Z,7E)-(1S,3R,20S)-1,3-dihydroxy-9,10-secopregna-5,7,10(19),16-tetraen-20-yl}oxy]-N-(2,2,3,3,3-pentafluoropropyl)acetamide, which process is characterized by irradiating a compound represented by the formula:
with UV to ring-open the compound, and then isomerizing the resulting compound; an intermediate useful for carrying out the process; and a process for producing the intermediate.摘要翻译： 本发明提供一种新颖的制造方法[{（5Z，7E） - （1S，3R，20S）-1,3-二羟基-9,10-断孕甾-5,7,10（19），16-四烯20 用UV到开环的化合物，然后异构化所得的：基}氧基] -N-（2,2,3,3,3-五氟丙基）乙酰胺该方法的通过照射由下式表示的化合物，其特征 化合物; 在用于实施过程中间有用; 及其制造中间体的方法。
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10.发明公开
公开(公告)号：EP1955999A1
公开(公告)日：2008-08-13
申请号：EP06842818.4
申请日：2006-12-04
发明人： OGASAWARA, Kunio , EMURA, Takashi , KAWASE, Akira , TAKANO, Koji , YAMAMOTO, Keisuke , KATO, Yoshiaki
IPC分类号： C07C401/00 , C07C33/44 , C07C231/12 , C07C235/06 , C07B61/00
CPC分类号： C07C33/44 , C07C235/06 , C07C401/00 , C07C2602/24 , C07D301/26 , C07D303/08
摘要： There are provided a novel process for producing [{(5Z,7E)-(1S,3R,20S)-1,3-dihydroxy-9,10-secopregna-5,7,10(19),16-tetraen-20-yl}oxy]-N-(2,2,3,3,3-pentafluoropropyl)acetamide, which process is shown in the following reaction scheme:
an intermediate useful for carrying out the process, and a process for producing the intermediate.摘要翻译： 本发明提供一种新颖的制造方法[{（5Z，7E） - （1S，3R，20S）-1,3-二羟基-9,10-断孕甾-5,7,10（19），16-四烯20 基}氧基] -N-（2,2,3,3,3-五氟丙基）乙酰胺哪个方法在以下反应方案所示：有用的中间体用于实施该方法，和用于制备该中间体的方法。
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