公开(公告)号：US08304443B2

公开(公告)日：2012-11-06

申请号：US12569324

申请日：2009-09-29

申请人： Seiji Nakano ,  Akifumi Morimoto ,  Yasuhiro Wada

发明人： Seiji Nakano ,  Akifumi Morimoto ,  Yasuhiro Wada

IPC分类号： A61K31/415 ,  C07D231/56

CPC分类号： C07D231/56

摘要： Compounds represented by the Formula (A-1) and the Formula (1) or salt thereof are provided. The compounds represented by the Formula (A-1) and the Formula (1) or salt thereof have a β3 adrenergic receptor agonist activity, and therefore are useful as an agent for the prevention and treatment of diabetes, obesity, hyperlipidemia, depression, biliary stone, a disorder derived from hyperactivity of biliary tract, a disorder derived from hyperactivity of digestive tract, interstitial cystitis, overactive bladder, urinary incontinence or a disorder derived from decreased tear secretion, etc.

摘要翻译： 提供由式（A-1）和式（1）表示的化合物或其盐。 由式（A-1）和式（1）表示的化合物或其盐具有β-肾上腺素能受体激动剂活性，因此可用作预防和治疗糖尿病，肥胖症，高脂血症，抑郁症的药剂 ，胆石，一种源于胆道多动症的病症，源自消化道多动症，间质性膀胱炎，膀胱过度活动，尿失禁或由泪液分泌减少引起的疾病等疾病。

公开(公告)号：US20120252881A1

公开(公告)日：2012-10-04

申请号：US13498771

申请日：2010-10-01

申请人： Takahiro Ochiya ,  Ryou-u Takahashi

发明人： Takahiro Ochiya ,  Ryou-u Takahashi

IPC分类号： A61K31/7088 ,  A61P35/00 ,  A61K31/713

CPC分类号： A61K31/7088 ,  A61K31/713 ,  C12N15/113 ,  C12N2310/141 ,  C12N2330/10 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/136 ,  C12Q2600/178

摘要： The present invention provides a therapeutic agent for a tumor, particularly a therapeutic agent for drug-resistant cancer, an agent for suppression or prophylaxis of tumor metastasis, and an agent for suppression or prophylaxis of cancer recurrence, containing a nucleic acid containing miR27b or a nucleotide having a nucleotide sequence having an identity of 70% or more with the nucleotide sequence shown by SEQ ID NO: 1 and having a function equivalent to miR27b.

摘要翻译： 本发明提供了一种用于肿瘤的治疗剂，特别是耐药性癌症的治疗剂，抑制或预防肿瘤转移的药剂，以及抑制或预防癌症复发的药物，其含有含有miR27b或 具有与SEQ ID NO：1所示的核苷酸序列同一性为70％以上且具有与miR27b相当的功能的核苷酸序列的核苷酸。

公开(公告)号：US20120252729A1

公开(公告)日：2012-10-04

申请号：US13395000

申请日：2010-09-08

申请人： Shinichiro Shirae ,  Yasuo Nakamura ,  Yuiko Oya ,  Yoshihide Nozaki ,  Nobuyuki Kobayashi ,  Tatsuhiko Kuroda ,  Hiroki Kato ,  Masashi Serada ,  Kazuyoshi Hori

发明人： Shinichiro Shirae ,  Yasuo Nakamura ,  Yuiko Oya ,  Yoshihide Nozaki ,  Nobuyuki Kobayashi ,  Tatsuhiko Kuroda ,  Hiroki Kato ,  Masashi Serada ,  Kazuyoshi Hori

IPC分类号： A61K38/29 ,  C07K14/635 ,  A61P19/10

CPC分类号： A61K38/29 ,  A61K33/10 ,  A61K45/06 ,  A61K2300/00

摘要： A method of treating osteoporosis by PTH that has excellent safety and high efficacy is disclosed, along with a method for inhibiting/preventing bone fractures by PTH that has excellent safety, as well as providing a drug to do this. A drug containing PTH as the active ingredient is disclosed, characterized in that a unit dose of PTH of 100 to 200 units is administered weekly in the above method.

摘要翻译： 公开了一种通过PTH治疗骨质疏松症的方法，其具有优异的安全性和高效力，以及通过PTH抑制/预防骨折的方法，其具有优异的安全性，以及提供药物。 公开了含有PTH作为活性成分的药物，其特征在于，以上述方法每周施用100〜200单位的PTH单位剂量。

公开(公告)号：US20120225909A1

公开(公告)日：2012-09-06

申请号：US13498524

申请日：2010-09-30

申请人： Yasuhiro Wada ,  Akifumi Morimoto

发明人： Yasuhiro Wada ,  Akifumi Morimoto

IPC分类号： A61K31/416 ,  C07D231/56 ,  C07D409/12 ,  C07D401/12 ,  A61K31/422 ,  C07D403/12 ,  C07D417/12 ,  A61K31/427 ,  C07D413/12 ,  A61P13/10 ,  A61K31/4439

CPC分类号： C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： [Objective] To provide a drug that selectively stimulates the β3-adrenergic receptors, particularly a drug capable of preferentially stimulating the β3-adrenergic receptors over the α1-adrenergic receptors. This drug can be used in the treatment and prevention of diabetes, obesity, hyperlipidemia, depression, cholelithiasis, diseases caused by biliary hyperkinesia, diseases caused by hyperfunction of the gastrointestinal tract, interstitial cystitis, overactive bladder or urinary incontinence, diseases associated with decreased lacrimation, and the like.[Solution] Indazole analogs represented by the general formula (I) or a salt thereof. Drugs that contains these indazole analogs or a salt thereof as the active ingredient.

摘要翻译： [目的]提供一种选择性刺激肾上腺素能受体的药物，特别是能够优先刺激α1-肾上腺素能受体的β-肾上腺素能受体的药物。 该药物可用于治疗和预防糖尿病，肥胖症，高脂血症，抑郁症，胆石病，胆汁性运动障碍引起的疾病，由胃肠道功能亢进引起的疾病，间质性膀胱炎，膀胱过度活动或尿失禁，与流泪相关的疾病 ，等等。 [溶液]由通式（I）表示的吲唑类似物或其盐。 含有这些吲唑类似物或其盐作为活性成分的药物。

公开(公告)号：US20120015925A1

公开(公告)日：2012-01-19

申请号：US13108394

申请日：2011-05-16

申请人： Takehiko SASAHARA ,  Mitsunobu MOHRI ,  Ken-ichi KASAHARA

发明人： Takehiko SASAHARA ,  Mitsunobu MOHRI ,  Ken-ichi KASAHARA

IPC分类号： A61K31/397 ,  A61K31/38 ,  A61K31/4025 ,  A61K31/4535 ,  A61K31/5377 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/541 ,  A61K31/55 ,  A61K31/439 ,  A61K31/4995 ,  A61K31/40 ,  A61K31/47 ,  A61P9/00 ,  A61P3/06 ,  A61K31/554

CPC分类号： C07D285/36 ,  C07D337/08

摘要： A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided. A benzothiazepine or benzothiepine compound represented by the following formula (1A) having a thioamide bond and a quaternary ammonium substituent:

摘要翻译： 可用作治疗剂和高脂血症预防剂的药物，以及用作治疗剂的药物和与胆汁郁积相关的肝病，特别是原发性胆汁性肝硬化和原发性硬化性胆管炎的预防剂，以及可用作治疗剂的药物 提供了用于肥胖，脂肪肝和脂肪性肝炎的药剂和预防剂。 由具有硫代酰胺键和季铵取代基的下式（1A）表示的苯并硫氮杂或苯并噻吩类化合物：

公开(公告)号：US20110172154A1

公开(公告)日：2011-07-14

申请号：US12940380

申请日：2010-11-05

申请人： Toshinori ISHIZUYA ,  Tatsuhiko KURODA

发明人： Toshinori ISHIZUYA ,  Tatsuhiko KURODA

IPC分类号： A61K38/29 ,  A61P19/02

CPC分类号： A61K38/29

摘要： [Object] To provide a medicine that is extremely useful for preventing and/or treating and/or limiting exacerbation of human knee osteoarthritis.[Means of Achievement] A medicine characterized in comprising a parathyroid hormone (PTH) or a PTH derivative as an active ingredient for preventing and/or treating and/or limiting exacerbation of human knee osteoarthritis.

摘要翻译： 提供一种对预防和/或治疗和/或限制人膝关节骨性关节炎恶化非常有用的药物。 [成就手段]一种药物，其特征在于包含甲状旁腺激素（PTH）或PTH衍生物作为活性成分，用于预防和/或治疗和/或限制人膝关节骨性关节炎的加重。

公开(公告)号：US20110171139A1

公开(公告)日：2011-07-14

申请号：US13005954

申请日：2011-01-13

申请人： Benson M. Fong

发明人： Benson M. Fong

IPC分类号： A61K31/5513 ,  A61K9/12 ,  A61P11/00

CPC分类号： A61K31/192 ,  A61K31/137 ,  A61K31/22 ,  A61K31/343 ,  A61K31/353 ,  A61K31/366 ,  A61K31/401 ,  A61K31/4409 ,  A61K31/455 ,  A61K31/506 ,  A61K31/519 ,  A61K31/551 ,  A61K31/554 ,  A61K31/5578 ,  A61K45/06 ,  A61K2300/00

摘要： Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and/or preventing pulmonary arterial hypertension and/or stable angina. More particularly, aspects of the present invention are related to therapeutic combinations comprising a Rho-kinase inhibitor, such as fasudil, and one or more additional compounds selected from the group consisting of prostacyclins, such as iloprost, endothelin receptor antagonists, PDE inhibitors, calcium channel blockers, 5-HT2A antagonists, such as sarpogrelate, selective serotonin reuptake inhibitors, such as fluoxetine, statins, and vascular remodeling modulators, such as Gleevec.

摘要翻译： 本发明的优选实施方案涉及用于治疗和/或预防肺动脉高压和/或稳定性心绞痛的新型治疗药物组合和方法。 更具体地，本发明的方面涉及包含Rho-激酶抑制剂如法舒地尔和一种或多种选自前列环素，例如伊洛前列素，内皮素受体拮抗剂，PDE抑制剂，钙 通道阻断剂，5-HT2A拮抗剂，如卡波格雷特，选择性5-羟色胺再摄取抑制剂，如氟西汀，他汀类药物和血管重建调节剂，如格列卫。

公开(公告)号：US07964613B2

公开(公告)日：2011-06-21

申请号：US12071921

申请日：2008-02-27

申请人： Koki Matsubara ,  Atsushi Iesato ,  Akifumi Oomura ,  Koh Kawasaki ,  Rintaro Yamada ,  Minoru Seto

发明人： Koki Matsubara ,  Atsushi Iesato ,  Akifumi Oomura ,  Koh Kawasaki ,  Rintaro Yamada ,  Minoru Seto

IPC分类号： A01N43/42 ,  A01N43/00 ,  A61K31/47 ,  A61K31/00 ,  C07D217/00 ,  C07D217/22

CPC分类号： A61K31/55 ,  A61K31/47 ,  C07D401/12

摘要： A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; G1 represents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; G2 represents a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; G3 represents hydrogen atom, a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkoxycarbonyl group, an acyl group, an acyloxy group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; Y represents a single bond, or —C(R3)(R4)— (R3 and R4 represent hydrogen atom, or an alkyl group, or alkylene groups which combine together to form a saturated hydrocarbon ring group); G4 represents hydroxyl group (Y is a single group), or —N(R1)(R2) (R1 and R2 represent hydrogen atom, an alkyl group, an aralkyl group, an alkenyl group, an alkynyl group, a saturated heterocyclic group, an alkylsulfonyl group, an acyl group, or an amidino group); G5 is a substituent on a ring-constituting carbon atom of A, and represents hydrogen atom, fluorine atom, or an alkyl group] or a salt thereof, or a derivative thereof that is a prodrug, which potently inhibits Rho kinase.

摘要翻译： 由式（1）表示的化合物[A表示含氮饱和环; m表示0〜2的整数。 n表示1〜4的整数， G1表示氢原子，氯原子，羟基，烷氧基或氨基; G 2表示卤素原子，羟基，氰基，羧基，烷基，烯基，炔基，烷氧基，烷硫基，氨基，烷基亚磺酰基，烷基磺酰基或芳基 组; G3表示氢原子，卤素原子，羟基，氰基，羧基，烷基，烯基，炔基，烷氧基，烷硫基，氨基，烷氧基羰基，酰基， 酰氧基，烷基亚磺酰基，烷基磺酰基或芳基; Y表示单键，或-C（R3）（R4） - （R3和R4表示氢原子，或烷基或结合在一起形成饱和烃环基的亚烷基）; G4表示羟基（Y为单一基团）或-N（R1）（R2）（R1和R2表示氢原子，烷基，芳烷基，烯基，炔基，饱和杂环基， 烷基磺酰基，酰基或脒基）; G5是A的环构成碳原子上的取代基，代表氢原子，氟原子或烷基，或其盐，或其作为前体药物的衍生物，其有效抑制Rho激酶。

公开(公告)号：US07943337B2

公开(公告)日：2011-05-17

申请号：US12506695

申请日：2009-07-21

申请人： Takeshi Matsuoka ,  Shinji Koga ,  Takuji Kouzuma

发明人： Takeshi Matsuoka ,  Shinji Koga ,  Takuji Kouzuma

IPC分类号： C12Q1/26 ,  C12Q1/37

CPC分类号： C12N9/0004 ,  C12N9/50 ,  C12Q1/37 ,  C12R1/01 ,  C12R1/07 ,  G01N33/66 ,  G01N33/723 ,  G01N2333/95

摘要： There is provided a method for specifically determining a glycated β-chain N-terminal of glycated hemoglobin using enzymes without a separation operation, and a determination reagent kit therefor. A protease that cleaves a glycated amino acid and/or a glycated peptide from a glycated β-chain N-terminal without substantially cleaving a glycated amino acid or a glycated peptide from a glycated α-chain N-terminal of glycated hemoglobin or a fragment thereof is screened. The method of specifically determining a glycated β-chain N-terminal of glycated hemoglobin and the determination reagent kit are provided by using the protease obtained by the screening method. According to the present invention, a glycated β-chain N-terminal of glycated hemoglobin can specifically be determined without a separation operation.

摘要翻译： 提供了使用不分离操作的酶来特异性测定糖化血红蛋白的糖基化和N-末端的N-末端的方法及其测定试剂盒。 一种蛋白酶，其从糖基化连接的N-末端切割糖基化氨基酸和/或糖化肽，而不从糖化血红蛋白的糖基化α-链N-末端切割糖基化氨基酸或糖化肽 被筛选。 通过使用通过筛选方法获得的蛋白酶提供了特异性测定糖化血红蛋白的糖基化和连结的N-末端的方法和测定试剂盒。 根据本发明，可以在没有分离操作的情况下，具体地确定糖化血红蛋白的糖基化和连结的N-末端。

公开(公告)号：US07935720B2

公开(公告)日：2011-05-03

申请号：US12898367

申请日：2010-10-05

申请人： Motoshi Shoda

发明人： Motoshi Shoda

IPC分类号： A61K31/416 ,  C07D231/56

CPC分类号： C07D231/56

摘要： In the case of using 3-[3-amino-4-(indan-2-yloxy)-5-(1-methyl-1H-indazol-5-yl)phenyl]propionic acid, methyl 3-[4-(indan-2-yloxy)-3-(1-methyl-1H-indazol-5-yl)-5-nitrophenyl]propionate, or methyl 3-[3-amino-4-(indan-2-yloxy)-5-(1-methyl-1H-indazol-5-yl)phenyl]propionate as a medicine, more preferable aspects or improved methods are provided.Crystals of any compound among 3-[3-amino-4-(indan-2-yloxy)-5-(1-methyl-1H-indazol-5-yl)phenyl]propionic acid, methyl 3-[4-(indan-2-yloxy)-3-(1-methyl-1H-indazol-5-yl)-5-nitrophenyl]propionate, and methyl 3-[3-amino-4-(indan-2-yloxy)-5-(1-methyl-1H-indazol-5-yl)phenyl]propionate, and methods of producing the same are provided.

摘要翻译： 在使用3- [3-氨基-4-（茚满-2-基氧基）-5-（1-甲基-1H-吲唑-5-基）苯基]丙酸的情况下，使用3- [4-（茚满） -2-氧基）-3-（1-甲基-1H-吲唑-5-基）-5-硝基苯基]丙酸乙酯或3- [3-氨基-4-（茚满-2-基氧基）-5-（ 1-甲基-1H-吲唑-5-基）苯基]丙酸乙酯，更优选的方案或改进的方法。 3- [3-氨基-4-（茚满-2-基氧基）-5-（1-甲基-1H-吲唑-5-基）苯基]丙酸，3- [4-（茚满酮）的任何化合物的晶体 -2-基氧基）-3-（1-甲基-1H-吲唑-5-基）-5-硝基苯基]丙酸甲酯和3- [3-氨基-4-（茚满-2-基氧基）-5-（ 1-甲基-1H-吲唑-5-基）苯基]丙酸乙酯及其制备方法。