公开(公告)号：US4891364A

公开(公告)日：1990-01-02

申请号：US211096

申请日：1988-06-13

申请人： Noboru Kubodera ,  Katsuhito Miyamoto ,  Kiyoshige Ochi ,  Isao Matsunaga ,  Eigoro Murayama

发明人： Noboru Kubodera ,  Katsuhito Miyamoto ,  Kiyoshige Ochi ,  Isao Matsunaga ,  Eigoro Murayama

IPC分类号： C07C401/00 ,  C07J7/00 ,  C07J41/00 ,  C07J51/00 ,  C07J71/00

CPC分类号： C07J7/002 ,  C07C401/00 ,  C07J41/005 ,  C07J51/00 ,  C07J7/007 ,  C07J71/0042

摘要： Vitamin D derivatives of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 which may be the same or different each represents a hydrogen atom or a hydroxyl group; X is an oxygen atom, the group of the formula OR.sub.4 (where R.sub.4 is either a hydrogen atom or a lower alkyl having 4 to 6 carbon atoms that may or may not be substituted by a hydroxyl group), or the group of the formula=N-OR.sub.5 (where R.sub.5 is either a hydrogen atom or a lower alkyl group having 1 to 5 carbon atoms that may or may not be substituted by a hydroxyl group, an amino group or a lower alkylamino group having 1 to 3 carbon atoms), provided that the carbon atom at 20-position is linked to X by a single bond when X is the group of the formula OR.sub.4, and by a double bond in other cases, and a process for preparing the derivatives are disclosed.The derivatives have both the immunoregulating action and the ability to induce differentiation in tumor cells and hence are useful as medicines such as antiallergic agents, antirheumatic agents and antitumor agents.

摘要翻译： 其中R1，R2和R3可以相同或不同的维生素D衍生物表示氢原子或羟基; X是氧原子，式OR4（其中R4是氢原子或具有4-6个碳原子的低级烷基，可以被羟基取代或不被羟基取代）的基团，或式= N-OR5（其中R5为氢原子或碳原子数1〜5的低级烷基，可以被羟基，氨基或碳原子数1〜3的低级烷基氨基取代） 条件是当X是式OR4的基团时，20位上的碳原子通过单键与X连接，并且在其它情况下通过双键，并且公开了制备衍生物的方法。 所述衍生物具有免疫调节作用和在肿瘤细胞中诱导分化的能力，因此可用作药物如抗过敏剂，抗风湿剂和抗肿瘤剂。

公开(公告)号：US5051526A

公开(公告)日：1991-09-24

申请号：US527806

申请日：1990-05-24

申请人： Susumu Funakoshi ,  Eigoro Murayama

发明人： Susumu Funakoshi ,  Eigoro Murayama

IPC分类号： C07C271/24 ,  C07C51/00 ,  C07C59/90 ,  C07C67/00 ,  C07C227/00 ,  C07C227/06 ,  C07C229/34 ,  C07C237/22 ,  C07C239/00 ,  C07C251/40 ,  C07C271/12 ,  C07C271/22 ,  C07K1/00 ,  C07K1/04 ,  C07K1/06 ,  C07K5/117 ,  C07K7/06 ,  C07K7/16 ,  C07K14/575 ,  C08G69/06 ,  C08G69/28 ,  C08G69/30

CPC分类号： C07C229/34 ,  C07C251/40 ,  C07C271/22 ,  C07C59/90 ,  C07K1/003 ,  C07K1/042 ,  C07C2103/18

摘要： Novel benzhydrylamine derivatives represented by general formulas (I) and (II) are useful as reaction reagents for the solid-phase synthesis of polypeptide amides making use of 9-fluorenylmethyloxycarbonyl group ("Fmoc"). An intermediate for these derivatives represented by the general formula (III) is also disclosed: ##STR1## where R.sub.1 and R.sub.2 each independently represents a C.sub.1-3 lower alkyl; n is an integer of 1-4; l is 1 or 2; and m is 1 or 2.

公开(公告)号：US4965405A

公开(公告)日：1990-10-23

申请号：US316167

申请日：1989-02-27

申请人： Susumu Funakoshi ,  Eigoro Murayama

发明人： Susumu Funakoshi ,  Eigoro Murayama

IPC分类号： C07C271/24 ,  C07C51/00 ,  C07C59/90 ,  C07C67/00 ,  C07C227/00 ,  C07C227/06 ,  C07C229/34 ,  C07C237/22 ,  C07C239/00 ,  C07C251/40 ,  C07C271/12 ,  C07C271/22 ,  C07K1/00 ,  C07K1/04 ,  C07K1/06 ,  C07K5/117 ,  C07K7/06 ,  C07K7/16 ,  C07K14/575 ,  C08G69/06 ,  C08G69/28 ,  C08G69/30

CPC分类号： C07C229/34 ,  C07C251/40 ,  C07C271/22 ,  C07C59/90 ,  C07K1/003 ,  C07K1/042 ,  C07C2103/18

摘要： Novel benzhydrylamine derivatives represented by general formulas (I) and (II) are useful as reaction reagents for the solid-phase synthesis of polypeptide amides making use of 9-fluorenylmethyloxycarbonyl group ("Fmoc"). An intermediate for these derivatives represented by the general formula (III) is also disclosed: ##STR1## where R.sub.1 and R.sub.2 each independently represents a C.sub.1 -C.sub.3 lower alkyl; n is an integer of 1-4; l is 1 or 2; and m is 1 or 2.

公开(公告)号：US4666634A

公开(公告)日：1987-05-19

申请号：US800320

申请日：1985-11-20

申请人： Katsuhito Miyamoto ,  Noboru Kubodera ,  Kiyoshige Ochi ,  Isao Matsunaga ,  Eigoro Murayama

发明人： Katsuhito Miyamoto ,  Noboru Kubodera ,  Kiyoshige Ochi ,  Isao Matsunaga ,  Eigoro Murayama

IPC分类号： A61K31/59 ,  A61P3/00 ,  A61P3/02 ,  A61P3/14 ,  C07C67/00 ,  C07C401/00 ,  C07J9/00 ,  C07J41/00 ,  C07J71/00

CPC分类号： C07J71/0042 ,  C07C401/00 ,  C07J41/0011 ,  C07J41/0027 ,  C07J71/001 ,  C07J9/00

摘要： A 1.alpha.-hydroxy vitamin D.sub.3 derivative of the formula: ##STR1## where R.sub.1 is a hydroxyl group, an amino group or the group: OR' (where R' is a lower alkyl group having 1 to 7 carbon atoms that may or may not be substituted by a hydroxyl group, a halogen atom, a cyano group, a lower alkoxy group having 1 to 3 carbon atoms, an amino group, or an acylamino group); R.sub.2 is a hydrogen atom or a hydroxyl group), and a process for preparing the same are disclosed.The compound represented by the formula above has the calcium control action and the ability to induce differentiation in tumor cells and, therefore, are useful as an antitumor agents and a medicine for treating calcium dysbolism-caused diseases.

摘要翻译： 1α-羟基维生素D3衍生物，其结构式如下：其中R1是羟基，氨基或基团：OR'（其中R'是具有1至7个碳原子的低级烷基，可以或可以 不被羟基，卤素原子，氰基，具有1至3个碳原子的低级烷氧基，氨基或酰氨基取代）; R2是氢原子或羟基），以及其制备方法。 由上式表示的化合物具有钙控制作用和诱导肿瘤细胞分化的能力，因此可用作抗肿瘤剂和用于治疗钙异常引起的疾病的药物。

公开(公告)号：US5831000A

公开(公告)日：1998-11-03

申请号：US322386

申请日：1994-10-12

申请人： Eigoro Murayama ,  Tohru Hoshi

发明人： Eigoro Murayama ,  Tohru Hoshi

IPC分类号： A61K38/00 ,  A61K38/23 ,  C07K7/00 ,  C07K14/585 ,  C07K19/00

CPC分类号： C07K14/585 ,  A61K38/00 ,  C07K2319/00 ,  C07K2319/75

摘要： The improved hybrid calcitonin has a peptide segment in human calcitonin and a peptide segment in calcitonin derived from animals other than humans, such as eel, salmon and chicken. Each of the human or human analog calcitonins and the calcitonins derived from animals other than humans may be either native calcitonin or an analog thereof. The hybrid calcitonin has the outstanding advantage that it exhibits biological activities as strong as eel, salmon and chicken calcitonin while causing no side effects including nausea, disorders in the functions of the digestive tract or antigenicity.

摘要翻译： 改进的混合降钙素在人降钙素中具有肽段，并且衍生自除人之外的动物（例如鳗鱼，鲑鱼和鸡）的降钙素的肽段。 源自人以外的动物的人或人类模拟降钙素和降钙素各自可以是天然降钙素或其类似物。 混合降钙素具有突出的优点，即其表现出与鳗鱼，鲑鱼和鸡降钙素一样强的生物活性，同时不引起恶心，消化道功能紊乱或抗原性的副作用。