专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US5616609A Carcinostatic compound and production thereof 失效
标题翻译：致癌化合物及其生产
公开(公告)号：US5616609A
公开(公告)日：1997-04-01
申请号：US185964
申请日：1994-02-08
申请人： Tetsuro Ikekawa , Nobuo Ikekawa
发明人： Tetsuro Ikekawa , Nobuo Ikekawa
IPC分类号： C07D493/22 , A61K31/335
CPC分类号： C07D493/22
摘要： Described are stelleramacrin A and stelleramacrin B represented by the following formulas (I) and (II), respectively: ##STR1## a process for the preparation thereof; and anticancer agents containing either of them as an active ingredient.Therapeutics for solid cancer, said therapeutics containing either of gnidimacrin or pimelea factor P.sub.2 as an active ingredient, are also described.
摘要翻译： PCT No.PCT / JP92 / 01017 Sec。 371日期1994年2月8日 102（e）日期1994年2月8日PCT提交1992年8月7日PCT公布。公开号WO93 / 03039 日期：1993年2月18日描述了分别由下式（I）和（II）表示的星形花粉rin素A和石粉rin rin rin;：：>>>>>>>>>>>>>>>>> 和含有它们中任一种作为活性成分的抗癌剂。还描述了用于固体癌症的治疗剂，所述治疗剂含有格尼法克林或双黄单胞菌因子P2作为活性成分。

2. 发明授权

US4832875A Vitamin D.sub.3 derivative 失效
标题翻译：维生素D3衍生物
公开(公告)号：US4832875A
公开(公告)日：1989-05-23
申请号：US80512
申请日：1987-07-08
申请人： Nobuo Ikekawa
发明人： Nobuo Ikekawa
IPC分类号： C07C401/00
CPC分类号： C07C401/00
摘要： This invention provides 1.alpha.,25-dihydroxy-24a,24a-difluoro-24-homovitamin D.sub.3 and a process for its production. This compound has strong vitamin D activity and low toxicity and is useful for preventing and treating calcium pathobolism, osteoporosis, etc.

3. 发明授权

US4305880A Process for preparing 24-fluoro-25-hydroxycholecalciferol 失效
标题翻译：制备24-氟-25-羟基胆钙化甾醇的方法
公开(公告)号：US4305880A
公开(公告)日：1981-12-15
申请号：US189513
申请日：1980-09-22
申请人： Hector F. DeLuca , Yoko Tanaka , Nobuo Ikekawa , Yoshiro Kobayashi
发明人： Hector F. DeLuca , Yoko Tanaka , Nobuo Ikekawa , Yoshiro Kobayashi
IPC分类号： C07J9/00
CPC分类号： C07J9/00 , C07J9/005
摘要： The invention provides a new derivative of vitamin D.sub.3, 24-fluoro-25-hydroxycholecalciferol.The compound is characterized by vitamin D-like activity in its ability to increase intestinal calcium transport, increase serum calcium and inorganic phosphorous concentration and to prevent the development of rickets. It would find ready application as a substitute for vitamin D.sub.3 and in the treatment of disease states evincing calcium-phosphorous imbalance and which are nonresponsive to vitamin D.sub.3 therapy.
摘要翻译：本发明提供维生素D3，24-氟-25-羟基胆钙化甾醇的新衍生物。该化合物的特征在于维生素D样活性增加肠钙运输能力，增加血清钙和无机磷浓度，并防止r the病的发展。它可以作为维生素D3的替代品和治疗表现出钙磷不平衡的疾病状态，并且对维生素D3治疗无反应。

4. 发明授权

US4022891A Novel 1.alpha.,24-dihydroxycholecalciferol compositions, novel precursors thereof, and processes for preparing them 失效
标题翻译：新型1 {60,24-二羟基胆钙化甾醇组合物，其新型前体及其制备方法
公开(公告)号：US4022891A
公开(公告)日：1977-05-10
申请号：US583115
申请日：1975-06-02
申请人： Toru Takeshita , Yoshinobu Hashimoto , Hiroyuki Kawashima , Sachio Ishimoto , Nobuo Ikekawa , Masuo Morisaki
发明人： Toru Takeshita , Yoshinobu Hashimoto , Hiroyuki Kawashima , Sachio Ishimoto , Nobuo Ikekawa , Masuo Morisaki
IPC分类号： A23K1/16 , C07J9/00 , C07J71/00 , A61K31/59
CPC分类号： C07J9/00 , A23K20/174 , C07J71/001 , Y02P20/55
摘要： Novel 1.alpha., 24-dihydroxycholecalciferol and derivatives thereof which are useful with reduced side-effects for the treatment of abnormal metabolism of calcium and phosphorus caused by liver failure, renal failure, gastrointestinal tract failure and parathyroid failure, and related bone diseases. Preparation of the novel 1.alpha., 24-dihydroxycholecalciferol and their derivatives starts from 1.alpha., 24-dihydroxycholesterol prepared by reacting 1.alpha., 2.alpha.-epoxy-24-keto-cholesta-4,6-dien-3-one with an alkali metal and a proton donor in the presence of liquid ammonia or a liquid amine. Reaction of the 1.alpha., 24-dihydroxycholesterol with an allylic brominating agent, followed by contacting with a dehydrobrominating agent, affords 1.alpha.,3.beta., 24-trihydroxycholesta-5,7-diene derivative, which can then be converted to 1.alpha., 24-dihydroxycholocalciferol by ultraviolet irradiation in a organic solvent, followed by isomerization. Processes are also provided for separating 1.alpha., 24-dihydroxycholesterol into an (S)-epimer and an (R)-epimer, and also for separating at least one of 1.alpha., 3.beta., 24(S)-and 1.alpha., 3.beta., 24(R)-trihydroxycholesta-5,7-dienes from trihydroxycholesta-4,6-diene.
摘要翻译：用于治疗由肝衰竭，肾衰竭，胃肠道衰竭和甲状旁腺功能衰竭引起的钙和磷的异常代谢的副作用的新型1α，24-二羟基胆钙化甾醇及其衍生物以及相关的骨疾病。 1α，24-二羟基胆钙化甾醇及其衍生物的制备从1α，24-二羟基胆固醇开始，其通过使1α，2α-环氧-24-酮 - 胆甾烯-4,6-二烯-3-酮与碱金属和质子供体在液态氨或液态胺存在下进行。 1α，24-二羟基胆固醇与烯丙基溴化剂的反应，然后与脱氢溴化剂接触，得到1α，3β，24-三羟基胆甾-5,7-二烯衍生物，然后将其转化为1α，通过紫外线照射在有机溶剂中进行异构化，得到24-二羟基胆钙化甾醇。还提供了用于将1α，24-二羟基胆固醇分离成（S） - 对映体和（R） - 对映体的方法，还用于分离1α，3β，24（S） - 和1α， 3β，24（R） - 三羟基胆甾-5,7-二烯的三羟基胆甾-4,6-二烯。

5. 发明授权

US5278155A Fluorine-containing vitamin D.sub.3 analogues and cell differentiation-inducing agent containing the same 失效
标题翻译：含氟维生素D3类似物和含有其的细胞分化诱导剂
公开(公告)号：US5278155A
公开(公告)日：1994-01-11
申请号：US710394
申请日：1991-06-05
申请人： Nobuo Ikekawa , Yoshiro Kobayashi , Yoko Tanaka , Tadashi Eguchi
发明人： Nobuo Ikekawa , Yoshiro Kobayashi , Yoko Tanaka , Tadashi Eguchi
IPC分类号： A61K31/59 , A61P3/02 , C07C401/00 , C07J9/00 , C07J31/00 , C07J7/00
CPC分类号： C07C401/00 , C07J31/006 , C07J9/00 , Y02P20/55
摘要： Fluorine-containing vitamin D.sub.3 analogues of the formula [I]: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen atom, a chemically inactive hydroxy-protecting group, an acyl having 2 to 8 carbon atoms or an alkyl having 1 to 8 carbon atoms, and n is an integer of 4 to 6, which have excellent pharmacological activities, particularly anti-tumor activity owing to differentiation-inducing activity and are useful for the prophylaxis and treatment of various tumors and intermediates therefore.
摘要翻译：具有式[I]的含氟维生素D3类似物：其中R1，R2和R3独立地是氢原子，化学惰性的羟基保护基，具有2-8个碳原子的酰基或具有 1〜8个碳原子，n为4〜6的整数，由于分化诱导活性，具有优异的药理活性，特别是抗肿瘤活性，因此可用于预防和治疗各种肿瘤及中间体。

6. 发明授权

US4959097A 23-Phenylsteroids 失效
标题翻译： 23-苯基类固醇
公开(公告)号：US4959097A
公开(公告)日：1990-09-25
申请号：US416926
申请日：1989-10-04
申请人： Sei-ichi Hayashi , Tadashi Hohjoh , Atsuhiko Shida , Nobuo Ikekawa
发明人： Sei-ichi Hayashi , Tadashi Hohjoh , Atsuhiko Shida , Nobuo Ikekawa
IPC分类号： A01N43/22 , A01N45/00 , C07J9/00 , C07J71/00 , C07J73/00
CPC分类号： A01N43/22 , A01N45/00 , C07J71/0026 , C07J73/003 , C07J9/00
摘要： Disclosed herein is a novel steroids represented by the formula (1): ##STR1## wherein Z represents ##STR2## n is integer of 1 to 3, R represents hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy or --CO.sub.2 R', wherein R' represents hydrogen, alkali metal or lower alkyl, andR.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent hydrogen or acyl, respectively.The compound of the formula (1) of the present invention exhibits high durability as well as excellent plant growth regulation.

7. 发明授权

US4886544A 23-phenylbrassinosteroids 失效
标题翻译： 23-苯基疱疹素类固醇
公开(公告)号：US4886544A
公开(公告)日：1989-12-12
申请号：US163526
申请日：1988-03-03
申请人： Sei-ichi Hayashi , Tadashi Hohjoh , Atsuhiko Shida , Nobuo Ikekawa
发明人： Sei-ichi Hayashi , Tadashi Hohjoh , Atsuhiko Shida , Nobuo Ikekawa
IPC分类号： A01N43/22 , A01N45/00 , C07J9/00 , C07J71/00 , C07J73/00
CPC分类号： A01N43/22 , A01N45/00 , C07J71/0026 , C07J73/003 , C07J9/00
摘要： Disclosed herein is a novel steroids represented by the formula (1): ##STR1## wherein Z represents ##STR2## n is integer of 1 to 3, R represents hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy or --CO.sub.2 R', wherein R' represents hydrogen, alkali metal or lower alkyl, andR.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent hydrogen or acyl, respectively.The compound of the formula (1) of the present invention exhibits high durability as well as excellent plant growth regulation.

8. 发明授权

US4619920A 26,26,26,27,27-pentafluoro-1.alpha.-hydroxy-27-methoxyvitamin D.sub.3 失效
标题翻译： 26,26,26,27,27-五氟-1α-羟基-27-甲氧基维生素D3
公开(公告)号：US4619920A
公开(公告)日：1986-10-28
申请号：US776342
申请日：1985-09-16
申请人： Hector F. DeLuca , Nobuo Ikekawa , Yoshiro Kobayashi , Yoko Tanaka
发明人： Hector F. DeLuca , Nobuo Ikekawa , Yoshiro Kobayashi , Yoko Tanaka
IPC分类号： C07J1/00 , C07C67/00 , C07C401/00 , C07J9/00
CPC分类号： C07C401/00 , C07J9/00
摘要： The invention provides a new derivative of vitamin D.sub.3, 26,26,26,27,27-pentafluoro-1.alpha.-hydroxy-27-methoxy-cholecalciferol and a process for preparing the same.The compound is characterized by some vitamin D-like activity except that it exhibits negligible activity in mobilizing bone. This characteristic indicates that the compound would find ready application in the treatment of disease or physiological states which evince loss of bone mass and application in other situations where metabolic calcium imbalances are found.
摘要翻译：本发明提供维生素D3,26,26,26,27,27-五氟-1α-羟基-27-甲氧基胆钙化甾醇的新衍生物及其制备方法。该化合物的特征在于一些维生素D样活性，除了它在动员骨中显示出可忽略的活性。该特征表明该化合物可用于治疗疾病或生理状态，这些疾病或生理状态证明骨质量的损失和在发现代谢钙不平衡的其他情况下的应用。

9. 发明授权

US4594192A 2.alpha.-fluorovitamin D.sub.3 失效
标题翻译： 2α-氟维生素D3
公开(公告)号：US4594192A
公开(公告)日：1986-06-10
申请号：US713941
申请日：1985-03-20
申请人： Hector F. DeLuca , Yoko Tanaka , Nobuo Ikekawa , Yoshiro Kobayashi
发明人： Hector F. DeLuca , Yoko Tanaka , Nobuo Ikekawa , Yoshiro Kobayashi
IPC分类号： C07C401/00 , C07J9/00
CPC分类号： C07J9/00 , C07C401/00
摘要： The invention provides new derivatives of vitamin D.sub.3, 2.alpha.-fluorovitamin D.sub.3 and the acylates thereof.The compounds are characterized by vitamin D-like activity in their ability to increase intestinal calcium transport and serum calcium indicating their ready application as substitutes for vitamin D.
摘要翻译：本发明提供维生素D3,2α-氟维生素D3及其酰化物的新衍生物。这些化合物的特征在于维生素D样活性能够增加肠钙运输和血清钙，表明它们作为维生素D替代品的适用。

10. 发明授权

US4502991A 23,23-Difluoro-1.alpha.,25-dihydroxy-vitamin D.sub.3 失效
标题翻译： 23,23-二氟-1α，25-二羟基维生素D3
公开(公告)号：US4502991A
公开(公告)日：1985-03-05
申请号：US524268
申请日：1983-08-18
申请人： Hector F. DeLuca , Yoko Tanaka , Nobuo Ikekawa , Yoshiro Kobayashi
发明人： Hector F. DeLuca , Yoko Tanaka , Nobuo Ikekawa , Yoshiro Kobayashi
IPC分类号： C07C67/00 , C07C401/00 , C07J9/00 , C07J17/00 , C07J31/00 , C07J53/00 , C12P7/02
CPC分类号： C07J31/006 , C07C401/00 , C07J17/00 , C07J53/002 , C07J9/00 , C07J9/005 , C12P7/02
摘要： The invention provides a new derivative of vitamin D, 23,23-difluoro-1,25-dihydroxycholecalciferol.The compound is characterized by vitamin D-like activity as evidenced by its ability to increase intestinal calcium transport. It is further characterized by its resistance to hydroxylation at C-23, which is recognized as an essential metabolic step to the inactivation of vitamin D, and therefore should provide vitamin D-like activity of greater time duration.
摘要翻译：本发明提供维生素D，23,23-二氟-1,25-二羟基胆钙化甾醇的新衍生物。该化合物的特征在于维生素D样活性，其证据是其增加肠钙运输的能力。其进一步特征在于其在C-23处的抗羟化反应，其被认为是维生素D失活的基本代谢步骤，因此应提供更长时间的维生素D样活性。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式