摘要:
Compounds of the formula ##STR1## wherein W, Ar.sup.1, Ar.sup.2 and Ar.sup.3 are defined as below; and the pharmaceutically acceptable salts of such compounds. These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.
摘要:
Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of the formula I ##STR1## and the pharmaceutically-acceptable salts thereof, wherein Ar.sup.1 and Ar.sup.2 are each independently aryl or substituted aryl; R.sup.1 is alkyl having from 1 to 6 carbon atoms;R.sup.2 is hydrogen or alkyl having from 1 to 6 carbon atoms;and either X and Y are taken separately and they are each, independently, hydrogen, dialkylphosphoryl having 2 to carbon atoms, alkyl having from 1 to 6 carbon atoms, alkenyl having from 2 to 6 carbon atoms or alkynyl having from 2 to 6 carbon atoms; or X and Y are taken together and they represent a hydrocarbon chain having 3, 4, or 5 carbon atoms, optionally containing up to 2 double bonds and optionally having 1 or 2 substituents selected from oxo, hydroxy and alkyl having from 1 to 6 carbon atoms; or Y is methoxy when X is ethyl; provided that when X and Y are taken together they are attached to adjacent carbon atoms; and provided that if either X or Y is hydrogen, then the other one must be alkenyl or alkynyl; and provided that when Y is methoxy and X is ethyl, then Y is at the 4-position and X is at the 5-position, Ar.sup.1 or Ar.sup.2 must each be phenyl, R.sup.1 is methyl and R.sup.2 is hydrogen.
摘要:
A compound of the formula: or a pharmaceutically acceptable salt thereof, wherein R1 is unsubstituted, mono-, di- or tri-substituted (C3-C11)cycloalkyl or (C3-C11)cycloalkenyl or the like, A is unsubstituted (C1-C7)alkyl or (C2-C5)alkenyl, hydroxy-(C1-C4)alkyl, (C1-C4)alkoxy-(C═O), or unsubstituted, mono-, di- or tri-substituted aryl, or aromatic-heterocyclic or the like, M is a covalent bond O, S, NH or the like, Y is 4- to 12-membered bicyclic-carbocyclic rings or 4- to 12-membered bicyclic-heterocyclic rings, or 5- to 17 membered spirocarbocyclic rings or 5- to 17-membered spiroheterocyclic rings or the like, Z1, Z2, Z3 and Z4 are hydrogen or the like, is disclosed. These compounds have ORL1-receptor agonist activity, and are thus useful as analgesics or the like in mammalian subjects.
摘要:
A compound of the formula (I) or a salt, prodrug or solvate thereof, wherein R1 and R2 groups are all hydrogen; A is a benzofuzed azahetero ring; W1—W2 is CH2—CH2; X1—X1 is CH2—CH2; and Z is methylene or carbonyl; or the like, is a ligand for ORL1-receptor and are useful for treating or preventing pain, a CNS disorder or the like in mammalian subjects.
摘要翻译:式(I)化合物或其盐,前药或溶剂合物,其中R 1和R 2均为氢; A是苯并呋喃氮杂环; W 1 -W 2是CH 2 -CH 2; X 1 -X 1是CH 2 -CH 2; Z是亚甲基或羰基; 等等是ORL1-受体的配体,可用于治疗或预防哺乳动物受试者的疼痛,CNS病症等。
摘要:
The present invention provides a headstock of a polishing machine, having a simple structure and capable of tracing a pad surface. The headstock of the present invention is formed of a spindle, a holder plate, a spherical bearing, and a plate spring. The holder plate is connected to a lower end portion of the spindle via the spherical bearing and the plate spring. A workpiece is attached to the lower surface of the holder plate. The spherical bearing has a center of tilting movement on a rotation axis of the spindle. The holder plate has a balance plate. The center of gravity of the holder plate including the balance plate coincides with the center of tilting movement of the spherical bearing. The plate spring has an axisymmetric shape. More specifically, the plate spring has an opening portion at the center and a plurality of arm portions extending to the outer periphery in the diameter direction. The plate spring is connected to the lower end of the spindle by use of first fitting holes which are formed along the inner periphery, and the plate spring is also attached to the holder plate by use of second fitting holes which are formed in the distal end of the plate spring. The first and second fitting holes are respectively located on small- and large-diameter circles which are concentrically arranged around the rotation axis of the spindle.
摘要:
This invention provides a compound of the following formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein R is hydrogen, C.sub.1 -C.sub.5 alkyl or an O-protecting group; B is a dircet bond, C.sub.1 -C.sub.5 alkylene or C.sub.2 -C.sub.5 alkenylene; R.sup.1 is C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.5 alkenyl or C.sub.3 -C.sub.7 cycloalkyl-C.sub.1 -C.sub.3 alkyl; R.sup.2 is hydroxy or C.sub.1 -C.sub.5 alkoxy; R.sup.3 is hydrogen, hydroxy or C.sub.1 -C.sub.5 alkoxy; and R.sup.4 is hydrogen, phenyl or heteroaryl selected from furyl, thienyl and pyrrolyl, the phenyl and heteroaryl being optionally substituted by one to five substitutents selected from halo, hydroxy, C.sub.1 -C.sub.3 allyl, C.sub.1 -C.sub.3 alkoxy and C.sub.2 -C.sub.5 alkenyl. These compounds and pharmaceutical compositions containing such compounds are useful as analgesic, antiinflammatory, diuretic, anesthetic or neuroprotective agents, or an agent for stroke or treatment of functional bowel diseases such as abdominal pain, for the treatment of a mammalian subject, especially a human subject.
摘要:
A facsimile apparatus which carries out ringing of a telephone first for calling, and transmits a voice message informing of "absence" and "facsimile receivable" to a calling station when offhook is not detected during a predetermined period. The facsimile apparatus also transmits a called station identification signal CED after a silence interval of about 5 seconds. When the calling station onhooks a handset during the period of ringing of the telephone by judging that the called station is absent, a fee for a telephone call will not be charged. Furthermore, by setting the silence interval, the CED signal after the voice message is prevented from being heard by the calling station.
摘要:
Certain 6-aryl- or 6-heteroaryl- alkylaminobenzoxazolones, and their pharmaceutically-acceptable salts, are dual inhibitors of lipoxygenase and cyclooxygenase enzymes, and so are useful as antiallergy and antiinflammatory agents.
摘要:
Compounds of the formula ##STR1## where Y is alkyl, aryl or heterocyclic, n is 1-7, R is hydrogen, alkyl, aralkyl or carboxymethyl, R.sub.1 is acetoxy, thiophenoxy, hydrogen, halo, alkyl, alkoxy or trifluoromethyl, R.sub.2 is hydrogen, alkyl or alkanoyl and X is C.dbd.O, CH.sub.2, NH, O or S as antiallergy and antiinflammatory agents.
摘要:
A compound of formula: R1 and R2 are independently C1-C4 alkyl; or R1 and R2, taken together with the carbon atom to which they are attached, form a mono-, bi-, tri- or spiro-cyclic group having 3 to 13 carbon atoms, wherein the cyclic group is optionally substituted by one to five substituents; A is (C1-C3)alkyl, phenyl, benzyl or the like; R is hydrogen, (C1-C3)alkyl, amino-(C1-C6)alkyl, heterocyclic-(C1-C3)alkyl wherein the heterocyclic is optionally substituted by amino, ((C1-C4)alkyl)-Z—(C1-C6)alkyl wherein Z is OC(═O) or the like; and X is (C1-C3)alkyl, phenyl or the like. These compounds are useful as ORL1-receptor agonists, and useful as analgesics or the like in mammalian subjects.