摘要:
The object aims to find a novel pharmacological activity of a novel 1,2,3,4-tetrahydroquinoxaline derivative which contains, as a substituent, a phenyl group having a sulfonic acid ester structure introduced therein. A compound represented by general formula (1) or a salt thereof is useful as a glucocorticoid receptor agonist, particularly as a therapeutic agent for diseases against which a glucocorticoid receptor agonist (e.g., a steroid) is believed to be effective, such as inflammatory bone/joint diseases, inflammatory ophthalmic diseases (inflammatory ophthalmic diseases in the anterior or posterior segment of an eye). R1 represents a group represented by general formula (2a), (3a), (4a) or (5a); R2 represents a lower alkyl group which may have a substituent, a lower cycloalkyl group which may have a substituent, or the like; R3 represents a lower alkyl group; R4, R5, R6 or R7 represent a halogen atom, a lower alkyl group which may have a substituent, a hydroxy group, a lower alkoxy group which may have a substituent, or the like; and m, n, p or q represents a number of 0, 1 or 2.
摘要翻译:本发明的目的在于找到引入其中具有磺酸酯结构的苯基作为取代基的新的1,2,3,4-四氢喹喔啉衍生物的新药理活性。 由通式(1)表示的化合物或其盐可用作糖皮质激素受体激动剂,特别是作为糖皮质激素受体激动剂(例如类固醇)被认为有效的疾病的治疗剂,例如炎性骨 /关节疾病,炎症性眼部疾病(眼睛前部或后部的炎症性眼部疾病)。 R1表示通式(2a),(3a),(4a)或(5a)表示的基团。 R 2表示可以具有取代基的低级烷基,可以具有取代基的低级环烷基等。 R3表示低级烷基; R4,R5,R6或R7表示卤素原子,可以具有取代基的低级烷基,羟基,可以具有取代基的低级烷氧基等; m,n,p或q表示0,1或2的数。
摘要:
A polypeptide according to the present invention includes: an altered polypeptide obtained by altering an ArgRS, a CysRS, a MetRS, a GlnRS, a GluRS, a LysRS, a TyrRS, or a TrpRS so that an unnatural amino acid is recognized; and an editing polypeptide derived from a PheRS, a LeuRS, an IleRS, a ValRS, an AlaRS, a ProRS, or a ThrRS, the editing polypeptide having been either inserted between a Rossman-fold N domain and a Rossman-fold C domain that exist in the altered polypeptide, or bound to an N terminal of the altered polypeptide. Thus provided are a new aaRS that exhibits high substrate specificity to an unnatural amino acid and a technique that involves the use of such an aaRS.
摘要:
A base sequence detection apparatus is provided with a channel formed on a base sequence detection chip. Working electrodes are formed along the channel and include a probe immobilized thereon, counter electrodes are formed on the inner surface of the channel and, reference electrodes are formed on the inner surface of the channel. An introduction port introduces solution or air from the upstream side of the channel, a delivery port delivers the solution or air in the channel, and the sample is injected into the channel through a sample injection port.
摘要:
An engine cooling structure for a water cooled engine includes water pump and a thermostat. The water pump pumps coolant to a water jacket of the engine. The water pump and thermostat are provided on a cover member installed on an outside of a crankcase of the engine, and a coolant passage, which communicates with the water jacket through the water pump from the thermostat, is integrally formed in the cover member, so as to obtain arrangement of the cooling structure that is efficient in terms of space. The engine cooling structure increases the degree of freedom of layout around a cylinder head by keeping the projection amount on a side of the cylinder head small, simplifies the piping construction, and reduces the number of assembly steps.
摘要:
A thermostat mounting structure capable of reliably positioning an embedded thermostat and ensuring high sealability. A coolant channel is formed in a casing. An embedding hole is formed in the casing across the coolant channel. A thermostat includes a cylindrical valve body with a surrounding wall having an entry aperture and an exit aperture. A valving element for advancing and retracting to open and close the entry aperture and the exit aperture. The thermostat is inserted into the embedding hole so that both apertures face the coolant channel. A cover member for covering the embedding hole via a circular rubber seal seated in a groove of the cover member and for fixing the thermostat. A positioning structure for positioning the thermostat to a side of the cover member.
摘要:
A two-step self-servowriting process first writes an intermediate pattern based on a reference pattern, and then writes a final pattern based on the intermediate pattern, wherein the reference pattern can be a printed media or a spiral pattern. Such an approach can be utilized to reduce the noise/runout, eliminate timing eccentricity, and increase the sample rate of the final pattern. This description is not intended to be a complete description of, or limit the scope of, the invention. Other features, aspects, and objects of the invention can be obtained from a review of the specification, the figures, and the claims.
摘要:
A fuel injection device is installed in a cylinder head of an internal combustion engine in such a manner that a fuel injection port thereof faces a curved intake passage formed in the cylinder head. Fuel is injected from the fuel injection device directly toward a wall surface of the intake passage without aiming at an intake port.
摘要:
A two-cycle engine includes a cylinder block having at least one pair of first and second cylinders, the first and second cylinders having a pair of first and second exhaust ports, respectively. A pair of first and second pistons are received respectively in the first and second cylinders for reciprocal movement therealong, each of the exhaust ports being selectively closed and opened by a respective one of the pistons during the movement thereof along a respective one of the cylinders. The first and second pistons are operatively connected to a crankshaft in such a manner that the first and second pistons are reciprocable 180.degree. out of phase along the respective cylinders. A final portion of the duration of opening of one of the exhaust ports overlaps an initial portion of the duration of opening of the other. An exhaust passage has a communicating portion communicating the first and second exhaust ports with each other adjacent thereto.