公开(公告)号：US20090118264A1

公开(公告)日：2009-05-07

申请号：US12318248

申请日：2008-12-23

申请人： Ryozo Nagai ,  Ichiro Manabe ,  Takayuki Shindo ,  Hiroshi Iwata ,  Koichi Shudo ,  Hiroyuki Kagechika

发明人： Ryozo Nagai ,  Ichiro Manabe ,  Takayuki Shindo ,  Hiroshi Iwata ,  Koichi Shudo ,  Hiroyuki Kagechika

IPC分类号： A61K31/551 ,  A61K31/4164 ,  A61K31/39 ,  A61K31/4439 ,  A61P9/10

CPC分类号： A61K31/551

摘要： Methods of use of medicaments having neovascularization promoting action, which medicaments comprise a retinoid antagonist such as 4-(5H-7,8,9,10-tetrahydro-5,7,7,10,10-pentamethylbenzo[e]naphtho[2,3-b][1-,4]diazepin-13-yl)benzoic acid as an active ingredient.

摘要翻译： 使用具有新血管形成促进作用的药物的方法，该药物包含类视黄醇拮抗剂如4-（5H-7,8,9,10-四氢-5,7,7,10,10-五甲基苯并[e]萘并[2 ，3-b] [1-，4]二氮杂-13-基）苯甲酸作为活性成分。

公开(公告)号：US20070161105A1

公开(公告)日：2007-07-12

申请号：US10549816

申请日：2004-03-17

申请人： Makoto Asashima ,  Tatsuo Hamazaki ,  Hiroyuki Kagechika ,  Koichi Shudo

发明人： Makoto Asashima ,  Tatsuo Hamazaki ,  Hiroyuki Kagechika ,  Koichi Shudo

IPC分类号： C12N5/06 ,  C12N5/08

CPC分类号： C12N5/0062 ,  C12N2501/385 ,  C12N2501/999 ,  C12N2506/00

摘要： A method for forming an organ and/or tissue from undifferentiated cells derived from a vertebrate animal in vitro, which comprises the step of culturing the undifferentiated cells derived from a vertebrate animal in the presence of a retinoic acid X receptor ligand (e.g., a retinoic acid X receptor agonist or antagonist), and a method for forming a pancreas from undifferentiated cells derived from a vertebrate animal in vitro or a method for forming a tissue having morphology and function of a pancreas from undifferentiated cells derived from a vertebrate in vitro, which comprises the step of culturing the undifferentiated cells derived from a vertebrate animal in the presence of a retinoic acid receptor ligand, together with activin, that does not substantially bind to the retinoic acid receptor subtype γ.

摘要翻译： 一种用于从体外衍生自脊椎动物的未分化细胞形成器官和/或组织的方法，其包括在视黄酸X受体配体（例如，视黄酸）存在下培养源自脊椎动物的未分化细胞的步骤 酸X受体激动剂或拮抗剂）以及从体外衍生自脊椎动物的未分化细胞形成胰腺的方法或用于从体外衍生自脊椎动物的未分化细胞形成具有胰腺形态和功能的组织的方法，其中 包括在视黄酸受体配体存在下培养来源于脊椎动物的未分化细胞以及基本上不与维甲酸受体亚型γ结合的激活素的步骤。

公开(公告)号：US20090270612A1

公开(公告)日：2009-10-29

申请号：US12065994

申请日：2006-09-04

申请人： Nobuyuki Udagawa ,  Midori Nakamura ,  Hiroyuki Kagechika

发明人： Nobuyuki Udagawa ,  Midori Nakamura ,  Hiroyuki Kagechika

IPC分类号： C07D243/10

CPC分类号： A61K31/5513

摘要： It is an object of the present invention to provide a novel therapeutic agent for osteoporosis.HX531 is utilized, which is synthesized as a retinoid X receptor antagonist and has an activity in inhibiting a differentiation into adipocytes. Furthermore, any dosage form containing HX531 as an effective component can be used.

摘要翻译： 本发明的目的是提供一种用于骨质疏松症的新型治疗剂。 使用HX531，其被合成为类视色素X受体拮抗剂，并且具有抑制分化成脂肪细胞的活性。 此外，可以使用含有HX531作为有效成分的任何剂型。

公开(公告)号：US07259187B2

公开(公告)日：2007-08-21

申请号：US10450836

申请日：2001-12-18

申请人： Hiroyuki Kagechika

发明人： Hiroyuki Kagechika

IPC分类号： A61K31/18 ,  C07C303/00

CPC分类号： C07D333/74 ,  C07C17/266 ,  C07C45/62 ,  C07C45/63 ,  C07C45/64 ,  C07C45/65 ,  C07C45/673 ,  C07C45/68 ,  C07C45/71 ,  C07C49/683 ,  C07C49/747 ,  C07C49/753 ,  C07C225/20 ,  C07C225/22 ,  C07C233/32 ,  C07C233/76 ,  C07C245/10 ,  C07C275/28 ,  C07C275/38 ,  C07C311/20 ,  C07C2601/18 ,  C07C2602/10 ,  C07D307/46 ,  C07D333/22 ,  C07C25/22 ,  C07C49/717

摘要： Tropolone derivatives represented by the formula (I), which have retinoid actions and are useful as active ingredients of medicaments [R1 to R4 represent hydrogen atom, an alkyl group, or an alkoxyl group; the ring represented by Ar represents an aryl ring or a heteroaryl ring; X represents a single bond, —N═N—, —CON(R5)—, —(C═C)nCON(R6)—, —N(R7)CON(R8)—, —SO2N(R9)—, —N(R10)— (R5 to R9 represent hydrogen atom or an alkyl group, n represents 1 to 3, R10 represents hydrogen atom, an alkyl group, or an acyl group), an alkylene group, an aryldiyl group, or a heterocyclic diyl group; Y represents hydrogen atom, —OR11 (R11 represents hydrogen atom, an alkyl group, or an acyl group), —NHR12 (R12 represents hydrogen atom, an alkyl group, an acyl group, or amino group), or a halogen atom

摘要翻译： 具有类视黄醇作用并可用作药物的活性成分的式（I）表示的替罗非隆衍生物代表氢原子，烷基， 或烷氧基; 由Ar表示的环表示芳基环或杂芳基环; X表示单键-NN-，-CON（R 5） - ， - （CC）n CON（R 6） - ，-N（R 7）CON（R 8） - ，-SO 2 N（R 9） - ， - （R 10） - （R 5至R 9）表示氢原子或烷基，n表示1〜3， R 10表示氢原子，烷基或酰基），亚烷基，芳基二基或杂环二基; Y表示氢原子，-OR 11（R 11表示氢原子，烷基或酰基），-NHR 12（ R 12表示氢原子，烷基，酰基或氨基）或卤素原子

公开(公告)号：US06869959B1

公开(公告)日：2005-03-22

申请号：US09926407

申请日：2000-04-26

申请人： Hiroyuki Kagechika

发明人： Hiroyuki Kagechika

IPC分类号： A61K31/505 ,  A61P3/10 ,  C07D239/42

CPC分类号： C07D239/42 ,  A61K31/505

摘要： Compounds or salts thereof represented by the formula (I) wherein R1 represents hydrogen atom, a C1-6 alkyl group, a C1-6 alkenyl group, or an acyl group, R2 and R3 represent hydrogen atom or a C1-6 alkyl group, or adjacent R2 and R3 may combine to form 5- to 7-membered ring, R4 represents hydrogen atom, hydroxyl group, a C1-6 alkoxyl group, a C1-6 alkyl group, HAr represents a heteroaryl-diyl group consisting of a 5-membered or 6-membered ring containing 1 to 3 hetero atoms, R5 represents hydrogen atom or a C1-6 alkyl group. The compounds or the salts thereof have retinoid-like physiological activities or controlling activity on physiological activities of retinoid.

摘要翻译： 由式（I）表示的化合物或其盐，其中R 1表示氢原子，C 1-6烷基，C 1-6链烯基或酰基，R 2和R 3表示氢 原子或C 1-6烷基，或相邻的R 2和R 3可以结合形成5-至7-元环，R 4表示氢原子，羟基，C 1-6烷氧基， C 1-6烷基，HAr表示由含有1至3个杂原子的5元或6元环组成的杂芳基 - 二基，R 5表示氢原子或C 1-6烷基。 化合物或其盐具有类视黄醇样生理活性或控制类视黄醇生理活性的活性。

公开(公告)号：US07314639B2

公开(公告)日：2008-01-01

申请号：US10344690

申请日：2001-08-31

申请人： Hiroyuki Kagechika ,  Hiroo Nagano

发明人： Hiroyuki Kagechika ,  Hiroo Nagano

IPC分类号： A61K9/14

CPC分类号： C07C233/65 ,  C07C231/24 ,  C07C2602/10 ,  C07C235/84

摘要： A method for preparing a crystal of 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]benzoic acid having a single endothermic peak approximately at 233° C. in differential scanning calorimetry, which comprises the step of recrystallizing a crystal of 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]benzoic acid from a mixture of water and ethanol. The method enables selective preparation of type-II crystals which are stable against physical impact. The resulting crystals are free from highly toxic hexane as a residual solvent, and preferably used as an active ingredient of pharmaceuticals.

摘要翻译： 具有大约233℃的单一吸热峰的4 - [（5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基）氨基甲酰基]苯甲酸的结晶的方法 在差示扫描量热法中，其包括从4 - [（5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基）氨基甲酰基]苯甲酸的结晶重结晶步骤 水和乙醇。 该方法能够选择性制备对物理冲击稳定的II型晶体。 所得结晶不含作为残留溶剂的高毒性己烷，优选用作药物的有效成分。

公开(公告)号：US07084133B2

公开(公告)日：2006-08-01

申请号：US10470268

申请日：2002-02-08

申请人： Hiroyuki Kagechika

发明人： Hiroyuki Kagechika

IPC分类号： A61K31/69

CPC分类号： A61K31/69 ,  C07F5/027

摘要： A compound represented by the following general formula (I), wherein R1 represents a hydroxy-substituted alkyl group, a hydroxy-substituted alkenyl group, a hydroxy-substituted arylalkyl group (said arylalkyl group may have a substituent on the aryl ring), or a hydroxy-substituted arylalkenyl group (said arylalkenyl group may have a substituent on the aryl ring); X represents a dicarba-closo-dodecaborane-diyl group; R2 represents a hydroxy-substituted alkyl group or a hydroxy-substituted alkoxyalkyl group, or a salt thereof, which is useful as an agent exerting vitamin D actions or an agent for enhancing vitamin D actions R1—X—R2.

摘要翻译： 由以下通式（I）表示的化合物，其中R 1表示羟基取代的烷基，羟基取代的烯基，羟基取代的芳烷基（所述芳烷基可以具有 芳基环上的取代基）或羟基取代的芳基烯基（所述芳基烯基可以在芳基环上具有取代基）; X表示二碳 - 十六碳烷 - 二基; R 2表示羟基取代的烷基或羟基取代的烷氧基烷基或其盐，其可用作施用维生素D作用的试剂或用于增强维生素D作用的试剂 -line-formula description =“In-line Formulas”end =“lead”？> R＆lt; 1＆lt; -XR＆lt; 2＆lt; 2＆lt;＆lt; in-line-formula description =“In “公式”end =“tail”？>

公开(公告)号：US06458782B1

公开(公告)日：2002-10-01

申请号：US09555508

申请日：2000-09-01

申请人： Hiroyuki Kagechika ,  Yuichi Hashimoto ,  Hideji Fujii ,  Yoshiaki Yonekawa ,  Hisao Ekimoto

发明人： Hiroyuki Kagechika ,  Yuichi Hashimoto ,  Hideji Fujii ,  Yoshiaki Yonekawa ,  Hisao Ekimoto

IPC分类号： A61K3155

CPC分类号： C07D243/24 ,  A61K31/5513 ,  A61K31/553 ,  A61K31/554 ,  Y10S514/866

摘要： Medicaments comprising a compound represented by the following formulas: wherein, R1 represents hydrogen atom or a C1-6 alkyl group; R2 and R3 represent hydrogen atom or a C1-6 alkyl group, or R2 and R3 may combine together with the carbon atoms of the phenyl ring to which R2 and R3 bind to represent a 5- or 6-membered ring; R4 represents hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxyl group etc.; R5 represents hydrogen atom, a C1-6 alkyl group, or an aryl-substituted C1-6 alkyl group; R6 represents hydrogen atom or a C1-6 alkyl group; X represents —NR7—, —NO—, —O— etc. in which R7 represents hydrogen atom, a C1-6 alkyl group etc.; and Y represents a phenylene group or a pyridinediyl group, which are useful for preventive and therapeutic treatments of diabetes and complications of diabetes.

摘要翻译： 药物，其含有下述式表示的化合物：其中，R1表示氢原子或C1-6烷基; R2和R3表示氢原子或C1-6烷基，或R2和R3可以与R2和R3结合的苯环的碳原子一起形成5-或6-元环; R4表示氢原子，C1-6烷基，C1-6烷氧基等; R5表示氢原子，C1-6烷基或芳基取代的C1-6烷基; R6表示氢原子或C1-6烷基; X表示-NR7-，-NO-，-O-等，其中R7表示氢原子，C1-6烷基等; Y代表亚苯基或吡啶二基，可用于预防和治疗糖尿病和糖尿病并发症。