Abstract:
The invention provides valS polypeptides and DNA (RNA) encoding valS polypetides and methods for producing such polypeptides by recombinant techniques. Also provided are methods for utilizing valS polypeptides to screen for antibacterial compounds.
Abstract:
The invention provides hisS polypeptides and DNA (RNA) encoding hisS polypetides and methods for producing such polypeptides by recombinant techniques. Also provided are methods for utilizing hisS polypeptides to screen for antibacterial compounds.
Abstract:
The invention provides tRNA synthetase polypeptides and DNA (RNA) encoding tRNA synthetase polypetides and methods for producing such polypeptides by recombinant techniques. Also provided are methods for utilizing tRNA synthetase polypeptide for the protection against infection, particularly bacterial infections.
Abstract:
A container and closure combination wherein the closure comprises a skirt portion, the periphery of which has at least one rounded ramped portion adapted to cooperate with one or more corresponding rounded ramped portions on the container such that relative axial rotation of the container causes cooperation of the ramped portions and disengagement of the closure from the container.
Abstract:
The present invention provides novel indole and indoline derivatives according to formula (I) below, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments. The present indole and indoline derivatives are compounds of formula (I) or a salt thereof: ##STR1## in which R is a group of formula (i): ##STR2## in which P.sup.1 is a phenyl or a 5 to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur; and R.sup.1 and R.sup.2 are independently hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyC.sub.1-6 alkyl, acyl, nitro, trifluoromethyl, cyano, SR.sup.5, SOR.sup.5, SO.sub.2 R.sup.5, SO.sub.2 NR.sup.5 R.sup.6, CO.sub.2 R.sup.5, CONR.sup.5 R.sup.6, CONR.sup.5 (CH.sub.2).sub.x CO.sub.2 R.sup.6, NR.sup.5 R.sup.6, NR.sup.5 CO.sub.2 R.sup.6, CR.sup.5 =NOR.sup.6, where R.sup.5 and R.sup.6 are independently hydrogen or C.sub.1-6 alkyl and x is 1 to 3; or R is a group of formula (ii): ##STR3## in which P.sup.2 is phenyl or biphenyl; P.sub.3 is phenyl or a 5 to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur; A is a bond or a group (CH.sub.2).sub.p --R.sup.8 --(CH.sub.2).sub.q where R.sup.8 is oxygen, S(O).sub.m where m is 0 to 2, carbonyl, CO.sub.2 or CH.sub.2 and p and q are independently 0 to 3; and R.sup.1 and R.sup.2 are as defined above in formula (i); R.sup.3 is hydrogen, halogen, hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkoxy;n is 1 or 2; R.sup.4 is hydrogen or C.sub.1-6 alkyl; and B is --CHR.sup.9 CHR.sup.10 -- or --CR.sup.9 .dbd.CR.sup.10 -- where R.sup.9 and R.sup.10 are independently hydrogen or C.sub.1-6 alkyl. C.sub.1-6 alkyl groups, whether alone or as part of another group, may be straight chain or branched. The groups P.sub.1, P.sub.2, and P.sub.3 can be aromatic or saturated heterocyclic rings.
Abstract:
Use of a compound of general formula (I): ##STR1## wherein: R.sup.1 represents hydrogen, halogen, trifluoromethyl, nitro, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, arylC.sub.1-6 alkoxy, --CO.sub.2 R.sup.4, --(CH.sub.2).sub.n CN, --(CH.sub.2).sub.n CONR.sup.5 R.sup.6, --(CH.sub.2).sub.n SO.sub.2 NR.sup.5 R.sup.6, C.sub.1-6 alkanoylamino (CH.sub.2).sub.n, or C.sub.1-6 alkylsulphonylamino (CH.sub.2).sub.n ;R.sup.4 represents hydrogen, C.sub.1-6 alkyl or arylC.sub.1-6 alkyl;R.sup.5 and R.sup.6 each independently represent hydrogen or C.sub.1-6 alkyl, or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached form a ring;n represents 0, 1 or 2; andR.sup.2 and R.sup.3 each independently represent hydrogen, C.sub.1-6 alkyl or benzyl or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino or hexahydroazepino ring;or a physiologically acceptable salt thereof, in the manufacture of a medicament for the treatment of a condition where a 5-HT.sub.1 -like agonist is indicated, for example migraine. Novel compounds of formula (I), processes for preparing them and pharmaceutical compositions containing them are also described.
Abstract translation:通式(I)的化合物:其中:R 1表示氢,卤素,三氟甲基,硝基,羟基,C 1-6烷基,C 1-6烷氧基,芳基C 1-6烷氧基,-CO 2 R 4, - (CH 2 )nCN, - (CH 2)nCONR 5 R 6, - (CH 2)n SO 2 NR 5 R 6,C 1-6烷酰基氨基(CH 2)n或C 1-6烷基磺酰基氨基(CH 2)n; R 4表示氢,C 1-6烷基或芳基C 1-6烷基; R 5和R 6各自独立地表示氢或C 1-6烷基,或者R 5和R 6与它们所连接的氮原子一起形成环; n表示0,1或2; 并且R 2和R 3各自独立地表示氢,C 1-6烷基或苄基,或与它们所连接的氮原子一起形成吡咯烷子基,哌啶子基或六氢氮杂环; 或其生理上可接受的盐在制备用于治疗其中指示5-HT1样激动剂的病症的药物中,例如偏头痛。 还描述了新的式(I)化合物,其制备方法和含有它们的药物组合物。
Abstract:
##STR1## A process for preparing compounds of formula (I), by nitrosating compounds of formula (II), compounds of formula (I) having pharmaceutical activity.
Abstract:
The present invention relates to novel glycoforms and preparations of the soluble complement receptor type 1 (sCR1), and their uses in the therapy of complement mediated diseases and disorders involving inflammation and inappropriate complement activation and in thrombotic or shock state conditions. The invention provides novel glycoforms and methods for producing, detecting, enriching and purifying such glycoforms. The invention further provides methods of specifically producing a glycoform by recombinant or chemical means. Preferred embodiments of the invention include sialylated glycoforms and glycoforms with a pI.ltoreq.5.1 determined by chromatofocusing or with a sialic acid to mannose molar ratio of >0.25. The glycoforms may be formulated alone in therapeutic compositions or in combination with thrombolytic agents.