Abstract:
Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.
Abstract:
The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a N-substituted-N-sulfonylaminocyclopropane compound of formula (1) : wherein R 1 is -W-A 1 -W 1 -A 2 , W is (CH 2 ) m -X-(CH 2 )n-, wherein W 1 is -(CH 2 ) m1 -X 1 -(CH 2 ) n1 -, m, m1, n and n1 are the same or different and each is 0 to 6, X and X1 are the same or different and each is a single bond, etc., A1 is an optionally substituted C 3-14 hydrocarbon ring group, etc. and A 2 is a substituted C 3-14 hydrocarbon ring group etc.; R 2 is -(CH 2 ) r -CO-R 8 , etc., wherein r is 0 to 6 and R 8 is a C 1-6 alkoxy group, etc.; R 3 and R 4 are the same or different and each is a hydrogen atom, a C 1-6 alkyl group, etc.; and R 5 is -CO 2 R 21 , etc.; R 30 and R 31 are the same or different and each is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
Abstract translation:本发明提供具有聚集蛋白聚糖蛋白聚糖酶抑制活性和MMP-13抑制活性的化合物,可用作骨关节炎,类风湿性关节炎等的治疗剂,更具体而言,可以使用式(1)所示的N-取代-N-磺酰氨基环丙烷化合物: 其中R 1是-WA 1 -W 1 -A 2,W是(CH 2)m X-(CH 2)n - ,其中W 1是 - (CH 2)m1-X 1 - (CH 2)n - ,m ,m1,n和n1相同或不同,分别为0〜6,X和X1相同或不同,均为单键等,A1为任选取代的C3-14烃环基等。 A 2是取代的C 3-14烃环基等。 R 2为 - (CH 2)r -CO-R 8等,其中r为0至6,R 8为C 1-6烷氧基等; R 3和R 4相同或不同,各自为氢原子,C 1-6烷基等; R 5为-CO 2 R 21等; R 30和R 31相同或不同,各自为氢原子等; 或其前药或其药学上可接受的盐。
Abstract:
Compounds represented by general formula (I) (wherein R1 and R2 may be the same or different and each represents a hydrogen or halogen atom), their open-ring free acid derivatives, amides and salts are disclosed. A process for preparing the above-described compounds from known compound ML-236B is also disclosed.
Abstract:
A process for producing amide derivatives represented by general formula [XV] or enantiomers thereof, novel intermediate compounds useful for producing these compounds, etc., and a process for producing the same, wherein each symbol is as defined in the specification. Compared with the conventional processes, the above process can be very easily effected and enables an efficient production of the compounds [XV], i.e., those involving the compounds [XVI] having an HIV protease inhibitory effect in high yields. The n ovel intermediates are highly advantageous as intermediates for producing not only the above compounds [XVI] but also those which are useful as an X-ray contrast medium, etc.
Abstract:
A process for producing clean articles comprising the steps of contacting an article bearing contaminants adherent thereto with an organic solvent except for fluorohydrocarbon and rinsing the article thus treated by contact with an aliphatic fluorinated hydrocarbon represented by the general formula: CnFmH2n+2-m. This process enables the use of organic solvents that have been difficult to use, can dispense with the use of purified water, serves to reduce the cost necessary in the drying step and waste water disposal facilities, and prevents environmental pollution.
Abstract translation:一种生产清洁物品的方法,包括以下步骤:将含有污染物的物品与除氟氟烃之外的有机溶剂接触,并通过与由通式C n F m H 2n + 2-m表示的脂族氟代烃接触进行处理。 该方法能够使用难以使用的有机溶剂,可以省去使用净化水,用于降低干燥步骤和废水处理设备所需的成本,并防止环境污染。
Abstract:
The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R 1 is - (CH 2 ) m -X- (CH 2 ) n -A 1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A 1 is a substituted C 3-14 hydrocarbon ring group, etc.; R 2 and R 3 are the same or different and each is a hydrogen atom, -(CH 2 ) p -X 1 -(CH 2 ) q -A 2 , etc., wherein p and q are the same or different and each is 0 to 6, X 1 is a single bond, etc. and A 2 is an optionally substituted C 3-14 hydrocarbon ring group, etc.; R 4 is -C0 2 R 9 , etc., wherein R 9 is a hydrogen atom, etc.; and R 20 and R 21 are the same or different and each is a hydrogen atom, - (CH 2 ) m12- X 12- (CH 2 ) m12 -R 30 , etc., wherein m12 and m12 are the same or different and each is 0 to 6, X 12 is a single bond, etc. and R 30 is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
Abstract:
Compounds, pharmaceutical compositions and methods that are useful in the treatment or prevention of metabolic and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the activity of proteins involved in lipid metabolism and cell proliferation.
Abstract:
Compounds, pharmaceutical compositions and methods that are useful in the treatment or prevention of metabolic and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the activity of proteins involved in lipid metabolism and cell proliferation.
Abstract:
Compounds, pharmaceutical compositions and methods that are useful in the treatment or prevention of metabolic and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the activity of proteins involved in lipid metabolism and cell proliferation.
Abstract:
Diazabicyclo[3.3.1]nonane derivatives represented by general formula (1), wherein R represents -CONH-(CHR )m-R (wherein R represents hydrogen or alkyl; m is 0, 1 or 2; and R represents optionally substituted aryl, optionally substituted heterocycle, optionally substituted cycloalkyl, alkyl or alkyenyl) or -CO-R [wherein R represents alkyl, aralkyloxy or -NR R {wherein R and R are the same or different and each represents alkyl, or R and R together with the nitrogen atom to which they are bonded from a group (a) (wherein n is 2 or 3)}]; interm ediates thereof; and a nicotinic cholinergic agent containing the diazabicyclo[3.3.1]nonane derivatives. The compounds have a nicotinic cholinergic effect and a dopamine-releasing effect and are usable as a remeddy for dementia such as Alzheimer's disease, a drug for relieving memory disorders, a remedy for central nerve degeneration diseases, and a drug for relieving cerebral function disorders.
Abstract translation:由通式(1)表示的二氮杂双环[3.3.1]壬烷衍生物,其中R表示-CONH-(CHR 1)m R 2(其中R 1表示氢或烷基; m是0,1或2 ; R 2代表任选取代的芳基,任选取代的杂环,任选取代的环烷基,烷基或烷基)或-CO-R 3 [其中R 3表示烷基,芳烷氧基或-NR 4 R 5 >其中R 4和R 5相同或不同,并且各自代表烷基,或者R 4和R 5与它们所连接的氮原子一起(a)(其中 n为2或3)}]; 其间; 和含有二氮杂双环[3.3.1]壬烷衍生物的烟碱型胆碱能药剂。 所述化合物具有烟碱性胆碱能作用和多巴胺释放作用,并且可用作痴呆症的补救剂,例如阿尔茨海默氏病,用于缓解记忆障碍的药物,用于中枢神经变性疾病的药物,以及用于缓解脑功能障碍的药物。