摘要:
[Problems] A useful compound which can be used as a pharmaceutical, in particular, an agent for treating peripheral arterial occlusive disease is provided.[Means for Solution] The present inventors have conducted extensive studies on EP4 receptor agonists, and as a result, have found that a novel pyridone compound, in which a group having an acidic group is substituted at the 1-position of the pyridone ring, the 6-position is bonded with an aromatic ring group via a linking part, and the linking part contains a nitrogen atom, has an excellent EP4 receptor agonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor agonistic action, it is useful as a pharmaceutical, in particular, as an agent for treating peripheral arterial occlusive disease.
摘要:
[Solving Means] The present inventors have conducted extensive studies on an EP4 receptor agonist, and as a result, found that a novel pyridone compound characterized in that the 1-position in the pyridone ring is substituted with a group having an acidic group such as a carboxyl group and the 6-position is bonded with an aromatic ring group via lower alkyl, lower alkylene, ether, or thioether, has an excellent EP4 receptor agonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor agonistic action and a blood flow increasing action in the hindlimb of a rat, it is useful as a pharmaceutical, in particular, an agent for treating peripheral arterial occlusive disease.
摘要:
[Problem] To provide a compound having excellent platelet aggregation inhibitory activity.[Means for Resolution] It was found that quinolone derivatives characterized in that these have lower alkyl, cycloalkyl or the like at the 1-position; —N(R0)C(O)-lower alkylene-CO2R0, lower alkylene-CO2R0, lower alkenylene-CO2R0, —O-lower alkylene-CO2R0, —O-(lower alkylene which may be substituted with —CO2R0)-aryl or —O-lower alkenylene-CO2R0 (wherein R0 is H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof, has excellent P2Y12 inhibitory activity. In addition, it was confirmed that these quinolone derivatives also have excellent platelet aggregation inhibitory activity. Based on the above, these quinolone derivatives or pharmaceutically acceptable salts thereof are useful as platelet aggregation inhibitors.
摘要翻译:提供具有优异血小板聚集抑制活性的化合物。 [解决方法]发现喹诺酮衍生物的特征在于它们在1-位具有低级烷基,环烷基等; -N(R 0)C(O) - 低级亚烷基-CO 2 R 0,低级亚烷基-CO 2 R 0,低级亚烯基-CO 2 R O,-O-低级亚烷基-CO 2 R O,-O-(可被-CO 2 R 0取代的低级亚烷基) - 芳基或 O-低级亚烯基-CO 2 R 0(其中R 0是H或低级烷基)在3-位; 6位卤素; 分别被具有7位具有环结构的取代基取代的氨基或其药学上可接受的盐具有优异的P2Y12抑制活性。 此外,证实这些喹诺酮衍生物也具有优异的血小板聚集抑制活性。 基于上述,这些喹诺酮衍生物或其药学上可接受的盐可用作血小板聚集抑制剂。
摘要:
Disclosed are quinolone derivatives characterized in that these have lower alkyl, cycloalkyl or the like at the 1-position; —N(R0)C(O)-lower alkylene-CO2R0, lower alkylene-CO2R0, lower alkenylene-CO2R0, —O-lower alkylene-CO2R0, —O-(lower alkylene which may be substituted with —CO2R0)-aryl or —O-lower alkenylene-CO2R0 (wherein R0 is H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof, has excellent P2Y12 inhibitory activity. The quinolone derivatives have excellent platelet aggregation inhibitory activity. A method of using the compounds is also disclosed.
摘要翻译:公开了喹诺酮衍生物,其特征在于它们在1-位具有低级烷基,环烷基等; -N(R 0)C(O) - 低级亚烷基-CO 2 R 0,低级亚烷基-CO 2 R 0,低级亚烯基-CO 2 R O,-O-低级亚烷基-CO 2 R O,-O-(可被-CO 2 R 0取代的低级亚烷基) - 芳基或 O-低级亚烯基-CO 2 R 0(其中R 0是H或低级烷基)在3-位; 6位卤素; 分别被具有7位具有环结构的取代基取代的氨基或其药学上可接受的盐具有优异的P2Y12抑制活性。 喹诺酮衍生物具有优异的血小板聚集抑制活性。 还公开了使用该化合物的方法。
摘要:
Provided are quinolone derivatives having a lower alkyl or cycloalkyl at the 1-position; —N(R0)C(O)-lower alkylene-CO2R0, lower alkylene-CO2R0, lower alkenylene-CO2R0, —O-lower alkylene-CO2R0, —O-(lower alkylene which may be substituted with —CO2R0)-aryl or —O-lower alkenylene-CO2R0 (wherein R0 is H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof. Pharmaceutical composition containing the quinolone derivatives and methods of using the compositions are provided.
摘要翻译:提供在1-位具有低级烷基或环烷基的喹诺酮衍生物; -N(R 0)C(O) - 低级亚烷基-CO 2 R 0,低级亚烷基-CO 2 R 0,低级亚烯基-CO 2 R O,-O-低级亚烷基-CO 2 R O,-O-(可被-CO 2 R 0取代的低级亚烷基) - 芳基或 O-低级亚烯基-CO 2 R 0(其中R 0是H或低级烷基)在3-位; 6位卤素; 分别被具有7-位上的环结构的取代基取代的氨基或其药学上可接受的盐。 提供了含有喹诺酮衍生物的药物组合物和使用该组合物的方法。
摘要:
[Problem] To provide a compound which may be used in treating diseases in which a calcium sensing receptor (CaSR) is concerned, particularly hyperparathyroidism. [Means for Resolution] It was found that novel pyrrolidine derivatives which are characterized by the possession of aminomethyl group substituted with arylalkyl group or the like, or salts thereof, have excellent CaSR agonistic regulatory activity and also have excellent selectivity with CYP2D6 inhibitory activity having a possibility of causing drug interaction. Based on the above, these novel pyrrolidine derivatives are useful as therapeutic agents for treating diseases in which CaSR is concerned (hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like).
摘要:
[Problem]Provided is a compound, which exhibits a P2Y12 inhibitory action and is useful as a medical drug, particularly, as a platelet aggregation inhibitor.[Means for Solution]The inventors have eagerly investigated P2Y12 inhibitors. As a result, the inventors have found that a bicyclic heterocyclic compound such as quinazolinedione, isoquinolone, and the like having an amino group substituted with lower alkyl, cycloalkyl, or lower alkylene-cycloalkyl at the specific position exhibits an excellent platelet aggregation inhibitory action, thereby completing the present invention. Since the compound of the invention exhibits excellent P2Y12 inhibitory action and platelet aggregation inhibitory action, it is useful as a platelet aggregation inhibitor.
摘要:
[Problem] To provide a compound which may be used in treating diseases in which a calcium sensing receptor (CaSR) is concerned, particularly hyperparathyroidism.[Means for Resolution] It was found that novel pyrrolidine derivatives which are characterized by the possession of aminomethyl group substituted with arylalkyl group or the like, or salts thereof, have excellent CaSR agonistic regulatory activity and also have excellent selectivity with CYP2D6 inhibitory activity having a possibility of causing drug interaction. Based on the above, these novel pyrrolidine derivatives are useful as therapeutic agents for treating diseases in which CaSR is concerned (hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like).
摘要:
A charged particle beam writing method includes inputting design pattern data, virtually dividing a writing area to be written with the design pattern data into a plurality of small areas in a mesh-like manner, calculating a pattern density in each of the plurality of small areas based on the design pattern data, calculating a resizing amount for each pattern density in a case of irradiating a charged particle beam at an isofocal dose, resizing a dimension of the design pattern data in each of the plurality of small areas, based on the resizing amount in each of the plurality of small areas, and writing a resized design pattern on a target workpiece with the isofocal dose corresponding to the pattern density which was calculated before the resizing in each of the plurality of small areas.
摘要:
A charged particle beam writing apparatus includes an unit configured to irradiate a beam, a deflector configured to deflect the beam, a stage, on which a target is placed, configured to perform moving continuously, an lens configured to focus the beam onto the target, an unit configured to calculate a correction amount for correcting positional displacement of the beam on a surface of the target resulting from a first magnetic field caused by the lens and a second magnetic field caused by an eddy current generated by the first magnetic field and the moving of the stage, an unit configured to calculate a correction position where the positional displacement on the surface of the target has been corrected using the correction amount, and an unit configured to control the deflector so that the beam may be deflected onto the correction position.