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51. 发明授权

US4271170A Pyridine derivatives 失效
公开(公告)号：US4271170A
公开(公告)日：1981-06-02
申请号：US105672
申请日：1979-12-20
申请人： Tadao Tanouchi , Masanori Kawamura , Masaki Hayashi
发明人： Tadao Tanouchi , Masanori Kawamura , Masaki Hayashi
IPC分类号： C07D213/18 , C07D213/30 , C07D213/48 , C07D213/55 , C07D213/57 , A61K31/44 , C07D409/06
CPC分类号： C07D213/30 , C07D213/18 , C07D213/48 , C07D213/55 , C07D213/57 , Y10S514/826
摘要： The pyridine derivatives of the general formula: ##STR1## [wherein A represents an alkylene group containing from 1 to 5 carbon atoms unsubstituted or substituted by a hydroxy group, B represents a single bond, or an oxygen or sulphur atom, or an alkylene group containing from 1 to 5 carbon atoms, D represents a single bond, or an alkylene group containing from 1 to 5 carbon atoms, R represents a grouping of the formula: ##STR2## (in which R.sup.6 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms), Z represents a single bond, or an ethynylene group, or a grouping of the formula: ##STR3## in which R.sup.2 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, R.sup.3 represents a hydrogen, bromine or chlorine atom, or an alkyl group containing from 1 to 4 carbom atoms; the symbol represents a single or double bond, the carbon atom attached to R.sup.2 binds to B, and the carbon atom attached to R.sup.3 binds to D, R.sup.1 represents a hydroxy group, or a grouping of the formula: --COOR.sup.4 or --COSR.sup.4, in which R.sup.4 represents a hydrogen atom, or an alkyl group containing from 1 to 12 carbon atoms, or an aralkyl group containing from 7 to 13 carbon atoms, or a cycloalkyl group containing from 4 to 7 carbon atoms unsubstituted or substituted by at least one alkyl group containing from 1 to 4 carbon atoms, or a phenyl unsubstituted or substituted by at least one halogen atom, trifluoromethyl group, alkyl or alkoxy or alkylthio group containing from 1 to 4 carbon atoms, nitro or phenyl group, R.sup.5 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, with the proviso that, when B represents an oxygen or sulphur atom, Z represents a single bond and D represents an alkylene group containing from 1 to 5 carbon atoms], and non-toxic acid addition salts thereof and, when R.sup.1 represents a carboxy or thiocarboxy group, non-toxic salts thereof, possess a strong inhibitory activity on thromboxane synthetase from rabbit platelet microsomes, and are useful as therapeutically active agents in the prevention or treatment of inflammation, hypertension, thrombus, cerebral apoplexy, asthma, myocardial infarction, cardiostenosis, cerebral infarction and acute cardiac death.

52. 发明授权

US11980621B2 Gonadotropin-releasing hormone antagonist dosing regimens for the treatment of endometriosis 有权
公开(公告)号：US11980621B2
公开(公告)日：2024-05-14
申请号：US16619776
申请日：2018-06-05
申请人： ObsEva S.A.
发明人： Ernest Loumaye , Jean-Pierre Gotteland
IPC分类号： A61K31/519 , A61K38/09 , A61P15/00
CPC分类号： A61K31/519 , A61K38/09 , A61P15/00
摘要： The invention provides methods of treating endometriosis in a patient by administration of a gonadotropin-releasing hormone (GnRH) antagonist, for instance, according to dosing regimens predicated on the patient's level of anti-Müllerian hormone (AMH) or β17-estradiol (E2).

53. 发明申请

US20220257624A1 COMPOSITIONS AND METHODS FOR TREATING METABOLIC DISEASE 有权
公开(公告)号：US20220257624A1
公开(公告)日：2022-08-18
申请号：US17614055
申请日：2020-06-01
申请人： AVOLYNT , KISSEI PHARMACEUTICAL CO., LTD.
发明人： Wiliam Owen WILKISON , Bentley CHEATHAM , James Trinca GREEN , Yoshikazu FUJIMORI
IPC分类号： A61K31/706 , A61K31/7056 , A61K31/7012 , A61P3/10
摘要： The invention described herein relates to oral dosage form therapies for treating metabolic disorders using combinations of inhibitors of SGLT1 and SGLT2. In such dosage forms, SGLT1 is effective in the intestinal lumen, and is either not absorbed, or poorly absorbed, while the SGLT2 inhibitor inhibits sugar reabsorption in the kidney by inhibiting SGLT2 activity. Metabolic disorders treated by combined SGLT1 and SGLT2 oral dosage forms include disorders associated with abnormal accumulation of liver lipids, which may also be copresent with hyperglycemia. Combinations of SGLT1 and SGLT2 inhibitors are contemplated herein, particularly combinations

54. 发明授权

US10100030B2 Carboxymethyl piperidine derivative 有权
公开(公告)号：US10100030B2
公开(公告)日：2018-10-16
申请号：US15034808
申请日：2014-11-06
申请人： Kissei Pharmaceutical Co., Ltd.
发明人： Kazuo Shimizu , Takashi Miyagi , Kohsuke Ohno , Yasunori Ueno , Yusuke Onda , Hikaru Suzuki
IPC分类号： C07D401/04 , C07D413/14
摘要： The present invention provides a new compound which has NK1 receptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to carboxymethyl piperidine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. Wherein, ring A is a benzene ring or the like; ring B is a pyridine ring or the like; R1 is C1-6 alkyl or C1-6 alkoxy; R2 and R3 are a hydrogen atom or methyl; and n is an integral number from 0 to 5.

55. 发明授权

US10047139B2 Fc fusion high affinity IgE receptor α-chain 有权
公开(公告)号：US10047139B2
公开(公告)日：2018-08-14
申请号：US15552065
申请日：2016-02-19
申请人： Kissei Pharmaceutical Co., Ltd.
发明人： Takashi Sakamoto , Yoichi Inada , Kazumasa Yokoyama
IPC分类号： A61K39/00 , C07K14/735
摘要： Provided is an Fc fusion high affinity IgE receptor α-chain having excellent stability at low pH.An Fc fusion protein comprising: (i) a high affinity IgE receptor α-chain; and (ii) an Fc region of IgG1, wherein a linker fragment region between the (i) and the (ii) is the amino acid sequence shown in SEQ ID NO: 2.

56. 发明授权

US10016433B2 Salt of fused heterocyclic derivative and crystal thereof 有权
公开(公告)号：US10016433B2
公开(公告)日：2018-07-10
申请号：US15647911
申请日：2017-07-12
申请人： KISSEI PHARMACEUTICAL CO., LTD.
发明人： Kazumichi Jo , Hideki Takeuchi
IPC分类号： A61K31/519 , A61P15/00 , A61P15/08 , A61P5/06 , A61P5/08 , C07D495/04 , A61K31/14 , A61K9/00
CPC分类号： A61K31/519 , A61K9/0053 , A61K31/14 , C07B2200/13 , C07D495/04
摘要： The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt having excellent solubility and storage stability.

57. 发明申请

US20180147189A1 ADMINISTRATION REGIMEN FOR THERAPEUTIC AGENTS FOR ATAXIA IN SPINOCEREBELLAR DEGENERATION 审中-公开
公开(公告)号：US20180147189A1
公开(公告)日：2018-05-31
申请号：US15736400
申请日：2015-06-26
申请人： KISSEI PHARMACEUTICAL CO., LTD.
发明人： Yoshitaka Shimizu , Hitoshi Yamano , Yuji Kiyono , Tomoyuki Ijiro
IPC分类号： A61K31/427 , A61P25/14
CPC分类号： A61K31/427 , A61P25/14
摘要： The present invention is directed to provide excellent pharmaceutical compositions for the treatment of ataxia in spinocerebellar degeneration with which the risk of side effects caused by elevation of thyroid hormone levels is reduced. The present invention relates to a pharmaceutical composition for treatment of ataxia in spinocerebellar degeneration including, as an active ingredient, a daily dose of 1.6 mg to 3.2 mg of rovatirelin or 1.6 mg to 3.2 mg of pharmacologically acceptable salt of rovatirelin as being calculated as a free form, wherein the pharmaceutical composition is administered once daily. The pharmaceutical compositions of the present invention are particularly useful as therapeutic agents for ataxia in SCD.

58. 发明授权

US09718771B2 Aniline derivative, pharmaceutical composition containing same, and use thereof 有权
公开(公告)号：US09718771B2
公开(公告)日：2017-08-01
申请号：US15121522
申请日：2015-02-27
申请人： Kissei Pharmaceutical Co., Ltd.
发明人： Hitoshi Inoue , Kohsuke Ohno , Tetsuya Nakamura , Yusuke Ohsawa
IPC分类号： C07D205/04
CPC分类号： C07D205/04
摘要： A compound having an S1P1 receptor antagonistic activity. A compound represented by general formula (I): (in the formula, R1, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group or the like, R4 is a C1-6 alkyl group or the like, R5 is a C1-6 alkyl group or the like, R6 is a C1-6 alkyl group or the like, R7 is a hydrogen atom, a halogen atom, a C1-6 alkyl group or the like, R8 is a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group, a C1-6 alkoxy group or the like, and R9 is a hydrogen atom or a C1-6 alkyl group.) or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same, and use thereof. The compounds have an excellent S1P1 receptor antagonistic activity and are useful for the treatment or prevention of autoimmune diseases.

59. 发明授权

US09694027B2 Pyrazole derivative and use thereof for medical purposes 有权
公开(公告)号：US09694027B2
公开(公告)日：2017-07-04
申请号：US14995489
申请日：2016-01-14
申请人： KISSEI PHARMACEUTICAL CO. LTD.
发明人： Masayuki Isaji , Masaaki Takemura , Hidetoshi Isawa , Yukihiko Hotei , Itaru Miyashita
IPC分类号： A61K31/7056 , C07H17/02
CPC分类号： A61K31/7056 , C07H17/02
摘要： The present invention provides pyrazole derivatives, uses thereof for medical purposes and so on. More particularly, the present invention relates to pharmaceuticals useful for the prevention or treatment of constipation, which comprise as an active ingredient 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide, or a pharmaceutically acceptable salt thereof. The pharmaceuticals of the present invention exert an effect of increasing the frequency of bowel movement or the like, and are useful for the prevention or treatment of constipation.

60. 发明申请

US20160115119A1 alpha-SUBSTITUTED GLYCINAMIDE DERIVATIVE 有权
标题翻译： α-取代的甘氨酰胺衍生物
公开(公告)号：US20160115119A1
公开(公告)日：2016-04-28
申请号：US14889475
申请日：2014-05-07
申请人： KISSEI PHARMACEUTICAL CO., LTD.
发明人： Hideaki HIRASAWA , Naohiro KAWAMURA , Junichi KOBAYASHI
IPC分类号： C07C233/81 , C07D307/82 , C07D237/24 , C07D239/28 , C07D241/24 , C07D213/82 , C07D405/12
CPC分类号： C07C233/81 , C07C237/22 , C07C237/36 , C07C255/60 , C07C271/22 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D213/56 , C07D213/81 , C07D213/82 , C07D213/84 , C07D215/54 , C07D217/26 , C07D221/04 , C07D231/14 , C07D233/90 , C07D237/08 , C07D237/24 , C07D239/26 , C07D239/28 , C07D241/12 , C07D241/24 , C07D261/18 , C07D263/34 , C07D271/08 , C07D275/02 , C07D277/20 , C07D277/30 , C07D277/56 , C07D307/78 , C07D307/82 , C07D307/84 , C07D317/62 , C07D333/38 , C07D333/70 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： The present invention is to provide a novel α-substituted glycinamide derivative, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and a pharmaceutical use thereof.The present invention provides a compound represented by the general formula (I), which has TRPM8 inhibitory effects: [wherein A1 represents a C6-10 aryl and the like, A2 represents a C6-10 aryl and the like, X represents CH and the like, Y represents —CR1R2— and the like, R1 and R2 independently represent a hydrogen atom and the like, R3 and R4 independently represent a halogen atom and the like, n is 1 or 2], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing diseases or symptoms caused by hyperexcitability or disorder of afferent neurons.
摘要翻译：本发明提供一种新的α-取代的甘氨酰胺衍生物或其药学上可接受的盐，包含其的药物组合物及其药学用途。本发明提供具有TRPM8抑制作用的通式（I）表示的化合物：[其中，A1表示C6-10芳基等，A2表示C6-10芳基等，X表示CH， Y表示-CR1R2-等，R1和R2独立地表示氢原子等，R3和R4独立地表示卤素原子等，n为1或2]或其药学上可接受的盐。此外，本发明的化合物（I）可以用作治疗或预防由传入神经元的过度兴奋性或紊乱引起的疾病或症状的药剂。

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