摘要:
Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein Q.sup.1 is halo substituted phenyl; naphthyl; indolyl; benzthiophenyl; benzofuranyl; benzyl; or fluorenyl; . . is an optional covalent bond;one of X and Y is H and the other is hydroxy or C.sub.1-6 alkoxy, or X and Y are together .dbd.0 or .dbd.NOR.sup.5 ;R.sup.1 and R.sup.2 are H; C.sub.1-6 alkyl optionally substituted by hydroxy, cyano, COR.sup.c, CO.sub.2 R.sup.c, CONR.sup.c R.sup.d, or NR.sup.c R.sup.d (where R.sup.c and R.sup.d are H, C.sub.1-6 alkyl or phenyl(C.sub.0-4 alkyl) optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo and trifluoromethyl); phenyl(C.sub.1-4 alkyl) (optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo or trifluoromethyl); COR.sup.c ; CO.sub.2 R.sup.c ; CONR.sup.c R.sup.d ; COC.sub.1-6 alkylNR.sup.c R.sup.d ; CONR.sup.c COOR.sup.d ; or SO.sub.2 R.sup.c ;R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; andR.sup.4 is phenyl optionally substituted by C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, OR.sup.a, SR.sup.a, SOR.sup.a, NR.sup.a R.sup.b, NR.sup.a COR.sup.b, NR.sup.a CO.sub.2 R.sup.b, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b, where R.sup.a and R.sup.b are H, C.sub.1-6 alkyl, phenyl or trifluoromethyl; are tachykinin antagonists.
摘要翻译:式(I)化合物及其盐和前药其中Q 1是卤素取代的苯基; 萘基; 吲哚基 苯硫酚 苯并呋喃基 苄基; 或芴基; 。 。 。 是可选的共价键; X和Y之一是H,另一个是羟基或C 1-6烷氧基,或X和Y一起= 0或= NOR5; R1和R2是H; 任选被羟基,氰基,CORc,CO2Rc,CONRcRd或NRcRd取代的C 1-6烷基(其中R c和R d为H,任选被C 1-6烷基,C 1-6烷氧基,卤素和三氟甲基取代的C 1-6烷基或苯基(C 0-4烷基) ); 苯基(C 1-4烷基)(任选被C 1-6烷基,C 1-6烷氧基,卤素或三氟甲基取代); CORC; CO2Rc; CONRcRd; COC 1-6烷基NR c R d; CONRcCOORd; 或SO2Rc; R3是H,C1-6烷基或C2-6烯基; R4是任选被C 1-6烷基,C 2-6烯基,C 2-6炔基,卤素,氰基,硝基,三氟甲基,三甲基甲硅烷基,OR a,SR a,SOR a,NR a R b,NR a COR b,NR a CO 2 R b,CO 2 R a或CONR a R b任意取代的苯基,其中R a和R b是 H,C 1-6烷基,苯基或三氟甲基; 速激肽拮抗剂。
摘要:
Compounds of formula (I), wherein Q.sup.1 represents an aryl group; the dotted line represents an optional covalent bond; one of X and Y represents H and the other represents hydroxy or C.sub.1-6 alkoxy, or X and Y together form a group .dbd.O or .dbd.NOR.sup.5 where R.sup.5 is H or C.sub.1-6 alkyl; Z represents O, S or NR.sup.2, where R.sup.2 is H or C.sub.1-6 alkyl; W represents a bond or a saturated or unsaturated hydrocarbon chain of 1, 2, 3, 4, 5 or 6 carbon atoms; R.sup.1 represents H or C.sub.1-6 alkyl. R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; R.sup.4 represents an optionally substituted phenyl group; and R.sup.6 represents a specified amino group or an optionally substituted aromatic or non-aromatic azacyclic or azabicyclic group; and salts and prodrugs are tachykinin receptor antagonists.
摘要:
Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein Q.sup.1 is halo substituted phenyl; naphthyl; indolyl; benzthiophenyl; benzofuranyl; benzyl; or fluorenyl; . . is an optional covalent bond;one of X and Y is H and the other is hydroxy or C.sub.1-6 alkoxy, or X and Y are together .dbd.O or .dbd.NOR.sup.5 ;R.sup.1 and R.sup.2 are H; C.sub.1-6 alkyl optionally substituted by hydroxy, cyano, COR.sup.c, CO.sub.2 R.sup.c, CONR.sup.c R.sup.d, or NR.sup.c R.sup.d (where R.sup.c and R.sup.d are H, C.sub.1-6 alkyl or phenyl(C.sub.0-4 alkyl) optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo and trifluoromethyl); phenyl(C.sub.1-4 alkyl) (optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo or trifluoromethyl); COR.sup.c ; CO.sub.2 R.sup.c ; CONR.sup.c R.sup.d ; COC.sub.1-6 alkylNR.sup.c R.sup.d ; CONR.sup.c COOR.sup.d ; or SO.sub.2 R.sup.c ;R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; andR.sup.4 is phenyl optionally substituted by C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, OR.sup.a, SR.sup.a, SOR.sup.a, NR.sup.a R.sup.b, NR.sup.a COR.sup.b, NR.sup.a CO.sub.2 R.sup.b, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b, where R.sup.a and R.sup.b are H, C.sub.1-6 alkyl, phenyl or trifluoromethyl; are tachykinin antagonists.
摘要翻译:式(I)化合物及其盐和前药其中Q 1是卤素取代的苯基; 萘基; 吲哚基 苯硫酚 苯并呋喃基 苄基; 或芴基; 。 。 。 是一个可选的共价键; X和Y之一是H,另一个是羟基或C 1-6烷氧基,或X和Y一起= O或= NOR 5; R1和R2是H; 任选被羟基,氰基,CORc,CO2Rc,CONRcRd或NRcRd取代的C 1-6烷基(其中R c和R d为H,任选被C 1-6烷基,C 1-6烷氧基,卤素和三氟甲基取代的C 1-6烷基或苯基(C 0-4烷基) ); 苯基(C 1-4烷基)(任选被C 1-6烷基,C 1-6烷氧基,卤素或三氟甲基取代); CORC; CO2Rc; CONRcRd; COC 1-6烷基NR c R d; CONRcCOORd; 或SO2Rc; R3是H,C1-6烷基或C2-6烯基; R4是任选被C 1-6烷基,C 2-6烯基,C 2-6炔基,卤素,氰基,硝基,三氟甲基,三甲基甲硅烷基,OR a,SR a,SOR a,NR a R b,NR a COR b,NR a CO 2 R b,CO 2 R a或CONR a R b任意取代的苯基,其中R a和R b是 H,C 1-6烷基,苯基或三氟甲基; 速激肽拮抗剂。
摘要:
Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要:
A mixture of carbon-containing fibers, such as mesophase or isotropic pitch fibers, a suitable matrix material, such as a milled pitch is compressed while resistively heating the mixture to form a carbonized composite material. Preferably, the carbonized material has a density of at least about 1.30 g/cm3. Preferably, the composite material is formed in less than ten minutes. This is a significantly shorter time than for conventional processes, which typically take several days and achieve a lower density material. A treating component may be impregnated into the composite. Consequently, carbon composite materials having final densities of about 1.6-1.8 g/cm3 or higher are readily achieved with one or two infiltration cycles using a pitch or other carbonaceous material to fill voids in the composite and rebaking.
摘要翻译:将含碳纤维如中间相或各向同性沥青纤维,合适的基质材料如研磨沥青的混合物压缩,同时电阻加热混合物以形成碳化复合材料。 优选地,碳化材料具有至少约1.30g / cm 3的密度。 优选地,复合材料在不到10分钟内形成。 这比通常需要几天并实现较低密度材料的常规工艺明显更短的时间。 处理组分可以浸渍到复合材料中。 因此,通过使用沥青或其它碳质材料填充复合材料中的空隙并进行重新粘合,可以通过一次或两次渗透循环,容易地实现最终密度为约1.6-1.8g / cm 3或更高的碳复合材料。
摘要:
Benzenepolycarboxylic acid esters, preferably phthalate or isophthalate acid esters are used as plasticizers in carbon/pitch mixes used in the production of extruded carbon and graphite electrodes.
摘要:
Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要:
A high coking value pitch prepared from coal tar distillate and has a low softening point and a high carbon value while containing substantially no quinoline insolubles is disclosed. The pitch can be used as an impregnant or binder for producing carbon and graphite articles.
摘要:
Electrode joint for threadably joining two abutting carbon upper and lower electrode sections is provided with a locking pin releasably held in an upper electrode section which when released engages a groove in a lower electrode section.
摘要:
Compounds of Formula (I) are useful inhibitors of anaplastic lymphoma kinase. Compounds of Formula (I) have the following structure: where the definitions of the variables are provided herein.