摘要:
The present invention relates to 2,6-diaminopurine-.beta.-D-ribofuranuronamide derivatives of the following formula (I). These compounds and their salts and solvates are useful as anti-inflammatory agents, particularly in the treatment of patients with inflammatory conditions who are susceptible to leukocyte-induced tissue damage. ##STR1##
摘要:
The present invention relates to compounds of formula (IV): ##STR1## wherein R.sup.a and R.sup.b each represent a hydrogen atom or together form an alkylidene group.
摘要:
The cooling system of the present invention directs a cooling mist onto the condenser coils of a conventional refrigerant charged central air conditioning unit. The mist comprises a mixture of tap water and condensate. The condensate is collected from the runoff of evaporation coils. A sensing unit is provided at the condenser coil return conduit for sensing a rise in refrigerant temperature and thereby causing the cooling mist to be directed onto the condenser coils.
摘要:
This invention relates to novel adenosine derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine. Thus the invention provides compounds of formula (I) which are agonists at the adenosine A1 receptor. ##STR1## wherein R.sup.1 represents phenyl optionally substituted by one or more substituents selected from halogen, C.sub.1-3 alkyl, trifluoromethyl, nitro, cyano, --CO.sub.2 R.sup.a.sub.1 --CONR.sup.a R.sup.b, --COR.sup.a, --SOR.sup.c, --SO.sub.2 R.sup.c, --SO.sub.3 H, --SO.sub.2 NR.sup.a R.sup.b, --OR.sup.a, --NHSO.sub.2 R.sup.c, --NHCOR.sup.a and --NR.sup.a R.sup.b,R.sup.2 represents a C.sub.1-6 alkyl or C.sub.3-6 alkenyl group; R.sup.3 represents C.sub.1-3 alkyl;R.sup.a and R.sup.b may each independently represent hydrogen or C.sub.1-3 alkyl or, when --NR.sup.a R.sup.b is directly attached to said phenyl, R.sup.a and R.sup.b together with the nitrogen atom may form a -5 or -6 or membered heterocyclic ring optionally containing a second heteroatom selected from oxygen or nitrogen, which second nitrogen heteroatom may optionally be further substituted by hydrogen or C.sub.1-3 alkyl;R.sup.c represents C.sub.1-3 alkyl;and salts and solvates thereof, in particular physiologically acceptable salts and solvates thereof.
摘要翻译:PCT No.PCT / EP97 / 02403 Sec。 371日期:1998年11月6日 102(e)日期1998年11月6日PCT提交1997年5月13日PCT公布。 WO97 / 43300 PCT出版物 日期1997年11月20日本发明涉及新型腺苷衍生物,其制备方法,含有它们的药物组合物及其在医药中的用途。 因此,本发明提供了作为腺苷A1受体的激动剂的式(I)化合物。 其中R 1表示任选被一个或多个选自卤素,C 1-3烷基,三氟甲基,硝基,氰基,-CO 2 R 1a -CONR a R b,-COR a,-SOR c,-SO 2 Rc,-SO 3 H,-SO 2 NR a R b,-OR a,-NHSO 2 R c ,-NHCOR a和-NR a R b,R 2表示C 1-6烷基或C 3-6烯基; R 3表示C 1-3烷基; R a和R b可各自独立地表示氢或C 1-3烷基,或当-NR a R b直接与所述苯基连接时,R a和R b与氮原子一起可以形成任选地含有选自第二杂原子的-5或-6元杂环 来自氧或氮,该第二氮杂原子可以任选地被氢或C 1-3烷基进一步取代; Rc表示C1-3烷基; 及其盐和溶剂合物,特别是其生理上可接受的盐和溶剂化物。
摘要:
A series of 2-(Purin-9-yl)-tetrahydrofuran-3,4-diol derivatives with broad anti-inflammatory properties which inhibit leukocyte recruitment and activation and which are agonists of the adenosine 2a receptor are described.
摘要:
To avoid danger of fuel leakage into bilges of a vessel's hull, the fuel feed pipe from the fuel supply to the vessel's engine carburetor is enclosed within a cylindrical casing sealed at one end to a fitting on the carburetor. At its other end the casing is sealed to an aperture in the hull, the feed pipe extending externally of the hull between the aperture and a container enclosing the fuel supply. Alternatively the casing is sealed at its other end directly to the container. The carburetor may have an annular fuel feed chamber with adjustable fuel orifices connected to the feed pipe through a scroll valve linked to the carburetor throttle valve.
摘要:
There are disclosed according to the invention, compounds of formula (I) wherein R1, R2 and R3 are defined in the specification. Additionally, processes of preparing the compounds of formula (I), formulations containing same, and the administration of said compounds or formulations thereof in the treatment of inflammatory diseases are also disclosed.
摘要:
Triazine derivatives of formula (I) ##STR1## or salts thereof, whereinR.sup.1 represents a halogen atom or a group selected from hydroxy; C.sub.1-8 alkyl C.sub.1-6 alkoxy; C.sub.1-3 alkoxy C.sub.1-3 alkoxy; phenoxy or phenyl C.sub.1-3 alkoxy, wherein the phenyl group is optionally substituted by a halogen atom or a group selected from C.sub.1-3 alkyl, C.sub.1-3 alkoxy, or hydroxy; fluoro C.sub.1-3 alkyl; cyano; --CO.sub.2 R.sup.3, wherein R.sup.3 represents a hydrogen atom or a C.sub.1-4 alkyl group; --CONR.sup.4 R.sup.5, wherein R.sup.4 and R.sup.5 each independently represents a hydrogen atom or a C.sub.1-4 alkyl group, or, together with the nitrogen atom to which they are attached, form a saturated 5- to 7- membered ring, which ring optionally contains one or more atoms selected from an oxygen or a sulphur atom, or a group selected from --NH-- or --N(CH.sub.3)--; andR.sup.2 represents a hydrogen or halogen atom, or a group selected from hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkoxy;are inhibitors of the enzyme 5-lipoxygenase.Processes for preparing the triazine derivatives of formula (I) and compositions containing them are also described.
摘要:
Compounds of formula (I) ##STR1## wherein R.sup.1 is selected from the group consisting of hydrogen, halogen, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, phenylC.sub.1-3 alkoxy (in which the phenyl group is optionally substituted by a substituent selected from halogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy and hydroxy), nitro, trifluoromethyl, cyano, --CO.sub.2 R.sup.3 (wherein R.sup.3 is selected from hydrogen and C.sub.1-4 alkyl) and --CONR.sup.4 R.sup.5 (wherein R.sup.4 and R.sup.5 are each independently selected from hydrogen and C.sub.1-4 alkyl, or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form a saturated 5- to 7- membered ring, which ring optionally contains one or more groups or atoms selected from oxygen, sulphur, --NH-- and --N(CH.sub.3)--); and R.sup.2 is selected from the group consisting of hydrogen, halogen, hydroxy, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; and salts thereof are inhibitors of the enzyme 5-lipoxygenase.Processes for preparing the compounds of formula (I) and compositions containing them are also described.
摘要:
The invention thus provides compounds of Formula (I) ##STR1## wherein R.sup.1 and R.sup.2 which may be the same or different represent H, C.sub.1-6 alkyl or substituted alkyl or C.sub.3-7 cycloalkyl; or aryl;R.sup.3, and R.sup.4 which may be the same or different represent H, halogen, C.sub.1-6 alkyl; or substituted aryl;R.sup.5 is H or C.sub.1-6 alkyl;n is an integer 0, 1 or 2and m is an integer 1, 2, 3, or 4;the dotted line indicates the presence or absence of an additional bond; and pharmaceutically acceptable solvates (e.g. hydrates) thereof.