摘要:
The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic pH to facilitate ease of injection, and sparingly soluble at physiological pH thereby precipitating at the site of administration. The precipitate will slowly dissolve and the active drug is released from dissolved depot formulation following esterase mediated cleavage of the ester link between the immobility promoting unit and the active pharmaceutical agent.
摘要:
The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.
摘要:
This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X− signifies an anion].
摘要翻译:本发明涉及具有选择性毒蕈碱M3受体拮抗作用,副作用小,适用于吸入治疗的化合物,并且可用作通式(I)的呼吸系统疾病的治疗剂; [其中A表示由式(a0)或(b0)表示的组; Ar表示任选取代的芳基或杂芳基; B 1和B 2表示脂族烃; R 1表示氟取代的环烷基; R 2,R 3和R 4表示低级烷基,单键或与B 1键合的亚烷基,或R 2和R 3一起表示亚烷基; R 5和R 7表示氢,低级烷基或与B 2键合的单键或亚烷基; R 6表示氢,低级烷基或以-N(R 8)R 9表示的基团; 而X - 表示阴离子]。
摘要:
This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X− signifies an anion].
摘要翻译:本发明涉及具有选择性毒蕈碱性M3受体拮抗作用,副作用小,适用于吸入治疗的化合物,并且可用作通式(I)的呼吸系统疾病的治疗剂; [其中A表示一组表达 通式(a0)或(b0); Ar表示任选取代的芳基或杂芳基; B 1和B 2表示脂族烃; R 1表示氟取代的环烷基; R 2,R 3和R 4表示低级烷基,单键或与B 1键合的亚烷基,或R 2和R 3一起表示亚烷基; R 5和R 7表示氢,低级烷基或与B 2键合的单键或亚烷基; R 6表示氢,低级烷基或以-N(R 8)R 9表示的基团; 而X - 表示阴离子]。
摘要:
The invention relates to methods for the treatment of central nervous system disorders, neurological disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof.
摘要:
The invention relates to methods for the treatment of central nervous system disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof. Unexpectedly, certain of the sigma receptor ligands of the present invention have selectivity for the sigma receptor over the DA, PCP and 5-HT.sub.1A receptors.
摘要:
This invention relates to novel compositions of matter which are esters with enhanced water solubility, for use in aqueous enzymatic resolution reactions of racemic mixtures of these esters for producing the separate chiral isomers of the racemic mixture. The invention also relates to novel methods for preparing these esters. The importance of the production of the separate chiral isomers of the racemic mixtures resides in the isolation of the isomers which frequently have different biological activities. Of particular significance regarding the water soluble esters of this invention is that they are derivatized with groups which enhance their aqueous solubility and their reactivity with enzymatic resolving methods which are mediated in an aqueous environment. In addition, the importance of these compounds resides in their being useful in novel methods for facilitating the enzymatic resolution reactions of racemic mixtures of esters, which are derivatized with groups which enhance the esters' aqueous solubility, in 1) a homogeneous aqueous reaction system where an extractive phase is not present, 2) a multiphase dispersion extractive reaction where an extractive phase is present, and 3) an extractive membrane reactor where the enzyme is placed alternatively either (a) in the aqueous phase, (b) in association with the membrane, or (c) in the aqueous phase and in association with the membrane, wherein the aqueous ester phase is contacted with one side of the membrane, and where an organic extractive phase is contacted with the other side of the membrane, wherein the extractive phase serves to remove the resolving reaction product.
摘要:
The invention relates to new polyfluorinated compounds which are usable as anti-wear additives for lubricants.These compounds are of general formula: ##STR1## in which R.sub.F is a perfluoroalkyl radical, R.sub.1 and R.sub.3 each denote a hydrogen atom or an alkyl, cycloalkyl or aryl radical, R.sub.2 and R.sub.4 each denote a hydrogen atom or an acyl residue, m equals 0 or 1 and X denotes a hydrogen atom or a 2-hydroxy-1-phenylethyl group. They are prepared by hydrogenation of amino alcohols of formula:R.sub.F --CF.dbd.CH--CH.sub.2 --NH--CH.sub.2 CH(R.sub.1)--OHfollowed, where appropriate, by a reaction with an epoxide and/or an esterification.
摘要:
A diaryl butyric acid derivative having the general formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, or an acyl group having 2 to 4 carbon atoms; R.sup.2 represents an alkyl group having 1 to 3 carbon atoms; andX represents a variety of substituents.This diaryl butyric acid derivative or the pharmaceutically acceptable salt thereof can be prepared by reacting a benzoxepin derivative having the general formula: ##STR2## wherein R.sup.2 is the same as defined above with an amine or alcohol derivative having the general formula;X--Hwherein X is the same as defined above in the presence of an acid catalyst at room temperature or at an elevated temperature and, optionally, further reading the reaction product with an alkylation agent having 1 to 3 carbon atoms or an acylation agent having 2 to 4 carbon atoms.This diaryl butyric acid derivative or the pharmaceutically acceptable salt thereof is effective for ameliorating or treating various symptoms based on cerebral organic disorders and pathergasia.
摘要翻译:具有以下通式的二芳基丁酸衍生物:其中R 1表示氢原子,具有1至3个碳原子的烷基或具有2至4个碳原子的酰基; R 2表示碳原子数1〜3的烷基。 X表示各种取代基。 该二芳基丁酸衍生物或其药学上可接受的盐可以通过使具有以下通式的苯并恶庚英衍生物:其中R2与上述定义相同,具有通式的胺或醇衍生物: XH其中X在酸催化剂存在下,在室温或升高的温度下与上述定义相同,并且任选地进一步用具有1至3个碳原子的烷基化试剂或具有2至 4个碳原子。 该二芳基丁酸衍生物或其药学上可接受的盐对于改善或治疗基于脑部有机疾病和麻醉的各种症状是有效的。
摘要:
This invention relates to the new 1,3-bis-(dimethylamino)-2-propyl-4-chlorophenoxyacetate of the Formula (I) ##STR1## acid addition salts thereof, a process for the preparation of the same and pharmaceutical compositions comprising the said compounds.The novel compound of the present invention corresponds to the Formula (I). This compound stimulates the function of the brain cells and thereby mental activity.The compound of the Formula (I) can be prepared by esterifying (4-chlorophenoxy)-acetic acid or a functional reactive derivative thereof with 1,3-bis-(dimethylamino)-2-propanol or a halogeno derivative thereof in a manner known per se.