摘要:
Disclosed are compounds of Formula (1), including all stereoisomers, N-oxides, and salts thereof, (Formula (1)) wherein G, J, Q1, R4, Y2, Q2, R5 and Y1 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.
摘要:
The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
摘要:
Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
摘要:
Phenyliodonium ylide derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are shown for use as precursors in aromatic nucleophilic substitution reactions. The iodonium ylide group is substituted by nucleophiles such as halide ions to provide the corresponding haloaryl derivatives. No-carrier-added [F-18]fluoride ion exclusively substitutes the iodonium ylide moiety in these derivatives and provides high specific activity F-18 labeled fluoro derivatives. Protected L-dopa-6-iodonium ylide derivative have been synthesized as a precursors for the preparation of no-carrier-added 6-[F-18]fluoro-L-dopa. The iodonium ylide group in this L-dopa.derivative is nucleophilically substituted by no-carrier-added [F-18]fluoride ion to provide a [F-18]fluoro intermediates which upon acid hydrolysis yielded 6-[F-18]fluoro-L-dopa.
摘要:
The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.
摘要:
The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, X1 and X2 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
摘要翻译:本发明提供了可用于治疗HIV感染或预防HIV感染或治疗AIDS或ARC的化合物。 本发明的化合物具有式I,其中R 1,R 2,R 3,R 4, X 1和X 2如本文所定义。 本发明还公开了用本文定义的化合物治疗HIV感染的方法和含有所述化合物的药物组合物。
摘要:
A method is provided for carrying out depolymerization of a polymer containing electrophilic linkages in the presence of a catalyst and a nucleophilic reagent, wherein production of undesirable byproducts resulting from polymer degradation is minimized. The reaction can be carried out at a temperature of 80° C. or less, and generally involves the use of an organic, nonmetallic catalyst, thereby ensuring that the depolymerization product(s) are substantially free of metal contaminants. In an exemplary depolymerization method, the catalyst is a carbene compound such as an N-heterocyclic carbene, or is a precursor to a carbene compound. The method provides an important alternative to current recycling techniques such as those used in the degradation of polyesters, polyamides, and the like.
摘要:
The present invention describes 1,3-dihydro-1-(phenylalkyl)-2H-imidazol-2-one compounds and their use for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases.
摘要:
The present invention concerns the compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; difluoromethyl; trifluoromethyl; C.sub.3-6 cycloalkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; bicyclo�2.2.1!-2-heptenyl; bicyclo�2.2.1!heptanyl; C.sub.1-6 alkylsulfonyl; arylsulfonyl; or substituted C.sub.1-10 alkyl; R3 is hydrogen, halo or C.sub.1-6 alkyloxy ##STR2## is a bivalent radical of formula ##STR3## Alk is C1-4alkanediyl; --A--B-- is a bivalent radical of formula: --CR.sup.6 .dbd.CR.sup.7 -- or --CHR.sup.6 --CHR.sup.7 --; L is hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; C.sub.1-6 alkyloxycarbonyl; optionally substituted C.sub.3-6 alkenyl; optionally substituted piperidinyl; C.sub.1-6 alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het.sup.1 is morpholinyl or optionally substituted pyridinyl, -furanyl, -thienyl, -hydroxypyridinyl, -imidazolyl, -thiazolyl, -oxazolyl, -isoquinolinyl, -quinolinonyl, -piperidinyl, -piperazinyl; and Het.sup.2 is morpholinyl or optionally substituted piperidinyl, -piperazinyl, -pyridinyl, -furanyl or -thienyl; having PDE IV and cytokine inhibiting activity. The invention also relates to processes for preparing the compounds of formula (I) and pharmaceutical compositions thereof.
摘要:
A compound of formula (I): ##STR1## where E is oxygen or sulphur; A is CR.sup.3 or N where R.sup.3 is hydrogen or hydrocarbyl; D completes a 5 or 6-membered non-aromatic heterocyclic ring which optionally contains additional heteroatoms selected from oxygen, nitrogen or sulphur and which is optionally substituted by an optionally substituted lower hydrocarbyl group, or an optionally substituted heteroaryl group; R.sup.1 and R.sup.2 are each independently hydrogen; optionally substituted lower hydrocarbyl, or optionally substituted heteroaryl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached, form a heterocyclic ring; Z represents halogen optionally substituted lower hydrocarbyl, optionally substituted lower hydocarbyloxy, optionally substituted lower hydrocarbylthio, hydrocarbylsulphinyl or hydrocarbylsulphonyl, cyano, nitro, CHO, NHOH, ONR.sup.7' R.sup.7", SF.sub.5 ; CO (optionally substituted lower hydrocarbyl), acylamino, COOR.sup.7, SO.sub.2 NR.sup.8 R.sup.9, CONR.sup.10 R.sup.11, OR.sup.12 or NR.sup.13 R.sup.14 where R.sup.7, R.sup.7', R.sup.7", R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are independently hydrogen or lower hydrocarbyl; R.sup.12 is hydrogen; SO.sub.2 lower hydrocarbyl or COR.sup.15 ; R.sup.13 and R.sup.14 are independently lower hydrocarbyl, lower hydrocarbyloxy or a group R.sup.12 ; R.sup.15 is OR.sup.16, NR.sup.17 R.sup.18, hydrogen or lower hydrocarbyl; R.sup.16 is lower hydrocarbyl; R.sup.17 and R.sup.18 are independently hydrogen or lower hydrocarbyl; provided that when there are two or more substituents Z, they may be the same or different; and m is 0 or an integer from 1 to 5.
摘要翻译:PCT No.PCT / GB93 / 02350 Sec。 371日期1995年10月6日 102(e)日期1995年10月6日PCT 1993年11月16日PCT公布。 公开号WO94 / 13652 日期:1994年6月23日式(I)化合物:其中E是氧或硫; A是CR 3或N,其中R 3是氢或烃基; D完成5或6元非芳族杂环,其任选地含有选自氧,氮或硫的另外的杂原子,并且其任选被任选取代的低级烃基或任选取代的杂芳基取代; R1和R2各自独立地为氢; 任选取代的低级烃基或任选取代的杂芳基,或者R 1和R 2与它们所连接的氮原子一起形成杂环; Z表示卤素任选取代的低级烃基,任选取代的低级含氧羰氧基,任选取代的低级烃基硫代,烃基亚磺酰基或烃基磺酰基,氰基,硝基,CHO,NHOH,ONR7'R7“,SF5; CO(任选取代的低级烃基),酰基氨基,COOR 7,SO 2 NR 8 R 9,CONR 10 R 11,OR 12或NR 13 R 14,其中R 7,R 7',R 7“,R 8,R 9,R 10和R 11独立地为氢或低级烃基; R12是氢; SO2低级烃基或COR15; R 13和R 14独立地为低级烃基,低级烃氧基或R 12基团; R 15是OR 16,NR 17 R 18,氢或低级烃基; R16为低级烃基; R 17和R 18独立地是氢或低级烃基; 条件是当存在两个或更多个取代基Z时,它们可以相同或不同; m为0或1〜5的整数。