摘要:
[Problems to be Solved] To provide a novel compound having antiviral activity, especially inhibitory activity against HIV integrase, a pharmaceutical composition, especially anti-HIV drug, containing the same. [Means to Solve the Problem] A compound of the formula: (wherein: R1 is optionally substituted aralkyl; R2 and R3 are each independently hydrogen, optionally substituted alkyl, optionally substituted amino, optionally substituted alkenyl or optionally substituted alkoxy (provided that each substituent for “optionally substituted” is a noncyclic group); R4 is hydrogen, optionally substituted carboxy, optionally substituted formylamino, optionally substituted carbamoyl, optionally substituted amino (provided that a substituent on amino in “optionally substituted formylamino”, “optionally substituted carbamoyl” and “optionally substituted amino” may form an optionally-substituted N-atom containing heterocyclic ring together with an adjacent N atom), optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, or optionally substituted heteroaryl) or a salt thereof.
摘要翻译:[待解决的问题]提供具有抗病毒活性,特别是针对HIV整合酶的抑制活性的新型化合物,含有该化合物的药物组合物,特别是抗HIV药物。 解决问题的方法下式化合物:其中:R 1为任选取代的芳烷基; R 2和R 3各自独立地为氢,任选取代的烷基,任选取代的氨基,任选取代的烯基或任选取代的烷氧基(条件是每个取代基 对于“任选取代的”是非环基团); R 4是氢,任选取代的羧基,任选取代的甲酰氨基,任选取代的氨基甲酰基,任选取代的氨基(条件是“任选取代的甲酰氨基” “任选取代的氨基”可以与相邻的N原子一起形成任选取代的含有N原子的杂环,任选取代的烷基,任选取代的烯基,任选取代的芳基或任选取代的杂芳基)或其盐。
摘要:
A compound having HIV Integrase Inhibitory activity of the formula: (wherein: R1 is optionally substituted aralkyl; R2 and R3 are each independently hydrogen, optionally substituted alkyl, optionally substituted amino, optionally substituted alkenyl or optionally substituted alkoxy (provided that each substituent for “optionally substituted” is a noncyclic group); R4 is hydrogen, optionally substituted carboxy, optionally substituted formylamino, optionally substituted carbamoyl, optionally substituted amino (provided that a substituent on amino in “optionally substituted formylamino”, “optionally substituted carbamoyl” and “optionally substituted amino” may form an optionally-substituted N-atom containing heterocyclic ring together with an adjacent N atom), optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, or optionally substituted heteroaryl) or a salt thereof.
摘要翻译:具有下式的HIV整合酶抑制活性的化合物:其中:R 1为任选取代的芳烷基; R 2和R 3各自独立地为氢,任选取代的烷基,任选取代的氨基,任选取代的烯基或任选取代的烷氧基(条件是每个取代基为“ 任选取代的“是非环基团); R 4是氢,任选取代的羧基,任选取代的甲酰氨基,任选取代的氨基甲酰基,任选取代的氨基(条件是在”任选取代的甲酰氨基“中的氨基上的取代基,”任选取代的氨基甲酰基“ 取代的氨基“可以与相邻的N原子一起形成任选取代的含有N原子的杂环,任选取代的烷基,任选取代的烯基,任选取代的芳基或任选取代的杂芳基)或其盐。
摘要:
An echo removing apparatus that can remove an echo appropriately if the produced sound volume becomes large although the configuration is simple is provided. A control section 17 switches the operations of an echo suppressor 14 and an echo canceller 15 in response to the volume value input from a volume operation section 18. If the volume value is large, the echo suppressor 14 is operated and an echo is suppressed reliably. If the volume value is small, the echo canceller 15 is operated and double talk is enabled.
摘要:
It was found that the compound having a binding activity to the cannabinoid type 2 receptor represented by the formula (I): wherein R1 is a group represented by the formula: —Y1—Y2—Y3—Ra wherein Y1 is single bond or the like; Y2 is —C(═O)—NH— or the like; Y3 is optionally substituted aryl or the like; R2 is hydrogen or the like; R3 is alkyl or the like; R4 is alkyl or the like; R5 is optionally substituted alkyl or the like; or R3 and R4 taken together with the adjacent atom form cyclic group or the like.
摘要:
A music session support method which enables each of players in a music session which is performed via a network to immediately recognize whether or not the other players are in the state of being able to participate in the session. A session support apparatus 10 transmits sets of status information indicative of whether or not each of players is in a state of being able to participate in a session, and player identification information which identifies the players, to each of session terminals 20. Each of the session terminals 20 which have received the sets of status information and player identification information causes a touch display 24 thereof to display the status information for each of the players. The session support apparatus 10 acquires a set of status transition information indicating that a player of at least one of the session terminals 20 in which the detecting device has detected the performance preparatory operation has gone into the state of being able to participate in a session, and player identification information for a session terminal 20, from the session terminal 20. The session support apparatus 10 transmits the acquired set of status transition information and player identification information to the session terminals 20. Each of the session terminals 20 updates contents displayed on the touch display 24 thereof, based upon the status transition information and player identification information transmitted from the session support apparatus 10.
摘要:
Disclosed is a 2'-deoxy-5-fluorouridine derivative of the formula ##STR1## wherein one of R.sub.1 and R.sub.2 is a benzyl group which may optionally have substituent selected from the group consisting of C.sub.1 -C.sub.6 alkyl group, C.sub.1 -C.sub.6 alkoxy group, C.sub.1 -C.sub.3 halogenated alkyl group, halogen atom, hydroxyl group and nitro group on the phenyl ring, and the other constitutes an amino acid residue, or a salt thereof. The compounds are useful for treating cancer.
摘要:
An internal combustion engine includes a crank shaft having a crank web, a crank pin on one end of the crank web, and a weight on an opposite end of the crank web, a crank case supporting the crank shaft therein, a cylinder, a piston reciprocally fitted in the cylinder, a rod coupled to the piston by a piston pin and connecting the piston to the crank pin for reciprocally moving the piston in the cylinder, the crank case having an opening and extending obliquely to axes of the crank shaft and the cylinder. The cylinder has an end corresponding to a bottom dead center of the piston and having a first recess opening toward the opening, the first recess being of a size allowing the piston pin to pass therethrough when the piston is in the bottom dead center. The weight on the crank web has on one side a second recess of a shape defining with the end of the cylinder a space allowing the piston as disconnected from the rod to pass therethrough.
摘要:
The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect.A pharmaceutical composition having an analgesic effect or an improving effect of urination disorder comprising a compound of the formula (I): wherein Rh and Rj are taken together to form a bond; Ra and Rb and/or Rd and Re are taken together to form oxo or the like; Rc is hydrogen, substituted or unsubstituted alkyl or the like; Rf is —(CR4aR4b)n—R2; R4a and R4b are hydrogen, substituted or unsubstituted alkyl or the like; R2 is substituted or unsubstituted cycloalkyl or the like; n is an integer of 1 to 4; —Rg is —X—R3; —X— is —O—, —S— or the like; R3 is substituted or unsubstituted cycloalkyl or the like, or its pharmaceutically acceptable salt or a solvate thereof.
摘要:
This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid β protein.
摘要:
It was found that the compound having a binding activity to the cannabinoid type 2 receptor represented by the formula (I): wherein R1 is a group represented by the formula: —Y1—Y2—Y3—Ra wherein Y1 is single bond or the like; Y2 is —C(═O)—NH— or the like; Y3 is optionally substituted aryl or the like; R2 is hydrogen or the like; R3 is alkyl or the like; R4 is alkyl or the like; R5 is optionally substituted alkyl or the like; or R3 and R4 taken together with the adjacent atom form cyclic group or the like.