摘要:
Compounds of the formula (I): (wherein A is an optionally substituted straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally intervened by oxygen or nitrogen atom; Ar1 is aryl or heteroaryl, any of which is optionally substituted; n is 0 or 1; R0 is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A; T, U, V and W are independently nitrogen atom or optionally substituted methine, and at least two of T, U, V and W are said methine group; X is —N(SO2R1)—, —N(COR2)— or —CO—; Y is —C(R3)(R4)—, —O— or —N(R5)—; Z is methine or nitrogen atom) exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, etc., sexual and reproductive dysfunctions, and gastro-intestinal motility disorder.
摘要:
An input signal is input via a first resistor to an inverting input terminal of an operational amplifier. A second resistor is provided on a feedback path between an output terminal and the inverting input terminal of the operational amplifier. A control voltage Vcnt output from the operational amplifier is input to a VCO. A frequency divider frequency-divides an output signal Sout of the VCO. A phase comparator compares an output signal from the frequency divider with a reference clock signal and outputs a voltage according to a phase difference. A loop filter removes a high-frequency component of an output voltage Vcp of the phase comparator and outputs the voltage to a non-inverting input terminal of the operational amplifier.
摘要:
In a frequency modulator, a VCO oscillates at a frequency according to a voltage applied to an input terminal. A divider divides an output signal of the VCO. A phase comparator compares the output of the divider with a reference clock signal and outputs a voltage corresponding to a phase difference. A loop filter is provided on a path leading from an output terminal of the phase comparator to the input terminal of the VCO, and the loop filter removes a high-frequency component of an output voltage of the phase comparator. A terminal for inputting a modulation signal is provided in the loop filter, separately from a terminal connected with the path leading from the output terminal of the phase comparator to the input terminal of the VCO.
摘要:
The invention provides the compounds represented by the formula (I) in which, R stands for a dihydroxy-substituted C1-C6 alkyl group, and Cy stands for an optionally substituted C6-C10 bi- or tri-cyclic aliphatic carbocyclic group. These compounds act as nociceptin receptor antagonist, and are useful, for example, as relievers against tolerance to narcotic analgesic, dependence on narcotic analgesic or addiction; analgesic enhancers; antiobestic or appetite suppressors; treating or prophylactic agents for cognitive impairment and dementia/amnesia; agents for treating developmental cognitive abnormality; remedy for schizophrenia; agents for treating neurodegenerative diseases; anti-depressant or treating agents for affective disorder; treating or prophylactic agents for diabetes insipidus; treating or prophylactic agents for polyuria; and remedy for hypotension and the like.
摘要:
The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc.The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要翻译:本发明涉及通式(I)的化合物:其中Ar1是任选取代的芳基或杂芳基; R 1是任选取代的低级烷基,低级烯基,低级炔基或环低级烷基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R2是氢原子,低级烷基,低级烯基或低级炔基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R3是氢原子或低级烷基; R4是氢原子,卤素原子,羟基,低级烷基或-N(R1k)R1m基团; T和U是氮原子或次甲基等。本发明的化合物具有优异的韦尔激酶抑制作用,因此可用于药物领域,特别是治疗各种癌症。
摘要:
The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要翻译:本发明涉及通式(I)的化合物:其中Ar1是任选取代的芳基或杂芳基; R 1是任选取代的低级烷基,低级烯基,低级炔基或环低级烷基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R2是氢原子,低级烷基,低级烯基或低级炔基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R3是氢原子或低级烷基; R4是氢原子,卤素原子,羟基,低级烷基或-N(R1k)R1m基团; T和U是氮原子或次甲基等。本发明的化合物具有优异的韦尔激酶抑制作用,因此可用于药物领域,特别是治疗各种癌症。
摘要:
The present invention is directed to compounds of generic formula (I) which are inhibitors of ephrin A4. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases regulated by the EphA4 RTK signaling, such as neurological and neurodegenerative disorders and cancer.
摘要:
The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要翻译:本发明涉及通式(I)的化合物:其中Ar1是任选取代的芳基或杂芳基; R 1是任选取代的低级烷基,低级烯基,低级炔基或环低级烷基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R2是氢原子,低级烷基,低级烯基或低级炔基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R3是氢原子或低级烷基; R4是氢原子,卤素原子,羟基,低级烷基或-N(R1k)R1m基团; T和U是氮原子或次甲基等。本发明的化合物具有优异的韦尔激酶抑制作用,因此可用于药物领域,特别是治疗各种癌症。
摘要:
The present invention relates to a compound represented by Formula [I]: wherein X is O, S, NH or CH2; Y1, Y2, Y3, Y4 and Y5, which may be identical or different, are each CH or N; however, at least one of Y1, Y2, Y3, Y4 and Y5 is N; Z1 and Z2, which may be identical or different, are each CH or N; n is an integer from 1 to 3; R1 is a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aliphatic heterocyclic ring or an aromatic heterocyclic ring, or a bicyclic aliphatic saturated hydrocarbon group; R2 and R3, which may be identical or different, are each a hydrogen atom, a lower alkyl group, a lower alkenyl group, a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aromatic heterocyclic ring, or the like; and R4 is a hydrogen atom, a lower alkyl group, a C3-C6 cycloalkyl group or the like, or a pharmaceutically acceptable salt or ester thereof, and a selective inhibitor against Cdk4 and/or Cdk6 or an anticancer agent containing the compound or a pharmaceutically acceptable salt or ester thereof.
摘要:
A blade plate 2 includes cutting edges 5 on both sides in a lateral direction Y. The cutting edges 5 extend along a longitudinal direction X. Each cutting edge 5 includes an arcuate distal cutting edge 8 and a main cutting edge 10. The distal cutting edges 8 are continuous via a distal joining portion 7. Each main cutting edge 10 extends from the corresponding distal cutting edge 8 via an intermediate joining portion 9 toward the proximal portion of the blade plate 2 to an cutting edge end portion 11. The width W8 between the distal cutting edges 8 of the cutting edges 5 gradually increases from the distal joining portion 7 toward the intermediate joining portions 9. The width W10 between the main cutting edges 10 of the cutting edges 5 gradually increases from the intermediate joining portions 9 toward the cutting edge ends 11. The width W11 between the cutting edge ends 11 of the cutting edges 5 is 2.0 mm or less.