Abstract:
The present invention relates to a process for the preparation of Treosulfan using sodium borohydride and iodine as reducing agent, which is less hazardous and convenient as compared to the reagents used in the prior art. The invention also relates to a novel intermediate to obtain Treosulfan in high yield and high purity.
Abstract:
Die vorliegende Erfindung beschreibt neue beta-Aminoaldehyd-Derivate der Formeln (I), (II) und (III),in welchen die Substituenten R 1 bis R 5 und A die in der Beschreibung angegebene Bedeutung haben, ein neues Verfahren zur deren Herstellung, dessen Zwischenprodukte, sowie Verwendungen dieser neuen beta-Aminoaldehyd-Derivate, z.B. zur (chemischen) Verwendung als reaktive Intermediate, zur Verwendung in der Medizin, z.B. als Peptidomimetikum, als Kopplungsagens, etc.
Abstract:
Compounds which function as melanocortin receptor ligands and having utility in the treatment of melanocortin receptor-based disorders. The compounds have the following structure (I): (R 4 ) s (R 2 ) n N~ X 1 -X 2 (CR 1a CR lb ) q 1~ N R 1 -lm 1 O R 3 (I) including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein m, n, q, s, R 1 , R 1a , R 1b , R 2 , R 3 , R 4 , X 1 X 2 and X 3 are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
Abstract:
The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, 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. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.
Abstract:
The dicarboalkoxy dioxolanes of formula (I) are stable in acidic aqueous alcoholic and non-alcoholic beverages. Therefore they are useful in food products especially in beverages to stabilize the citral character of these products by releasing citral over a prolonged period.
Abstract:
Compounds represented by general formula (I), pharmacologically acceptable salts or esters thereof, antitumor agents comprising these as the active ingredients, and intermediates therefor wherein Ar represents aryl or heteroaryl; Ar represents a group represented by (A) or (B), Ar and Ar each represents aryl or heteroaryl; Cy represents aryl, heteroaryl, or an alicyclic group optionally having one or two oxygen atoms; A represents C1-4 hydrocarbyl; m is an integer of 1 to 6; n and p each is an integer of 0 to 3; Q represents a single bond, a group represented by -CH2O-, -OCH2-, -CH2S-, or -SCH2-, or C1-6 hydrocarbyl; Q represents a single bond or a group represented by -(CH2)m- or -(CH2)n-W-(CH2)p-; Q represents a single bond, oxygen, sulfur, methylene, vinylene, or a group represented by -CO-, -NH-, -COO-, -OCO-, -CH2CH2-, -OCH2-, -SCH2-, -CH2O-, -CH2S-, -NHCO-, or -CONH-; R represents lower alkyl; R and R each represents hydrogen, hydroxy, or lower alkyl; W represents oxygen, sulfur, vinylene, or ethynylene; x is an interger of 0 to 2; and y is 0 or 1.
Abstract:
Gegenstand der vorliegenden Erfindung sind Verbindungen der allgemeinen Formel (I), in welcher R 1 ein Wasserstoffatom, eine Hydroxy- oder Methoxy-Gruppe, ein Halogenatom oder eine NO 2 -Gruppe ist; R 2 ein Wasserstoffatom, eine Hydroxy- oder Methoxygruppe, ein Acyl- oder Aroylrest ist; R 3 Wasserstoff, Trifluoracetyl (C(=O)CF 3 ) oder p -Nitrobenzoyl (C(=O)PhNO 2 ) ist und die gewellte Linie jeweils beide möglichen Konfigurationen von -OR 3 in Bezug zum Grundkörper bedeutet; Y= [C(=O)], [C(=N)-OH] oder [CH-OH], [CH-NR 5 R 6 ] in beiden möglichen stereoisomeren Anordnungen bedeutet, wobei R 5 und R 6 entweder jeweils für ein Wasserstoffatom stehen oder für ein Wasserstoffatom und eine Trifluoracetylgruppe (TFA) stehen; worin X = O, S oder NR, mit R = Wasserstoff oder einer C 1 bis C 4 Alkylgruppe bedeutet; R 4 eine unverzweigte oder verzweigte Alkyl- oder Heteroalkylkette mit einer Kettenlänge von 1 bis 19 Elementen bedeutet, wobei maximal 6 Heteroatome (O, N, S) beliebig kombinierbar durch mindestens zwei Kohlenstoffatome voneinander getrennt sind. Des Weiteren betrifft die vorliegende Erfindung unter anderem Verfahren zur Herstellung der Verbindungen gemäß Formel (I) sowie pharmazeutische Zusammensetzungen, einen pharmazeutischen Kit und deren Verwendung als Medikament zur Behandlung von proliferierenden Krankheiten oder Krankheitszuständen, vorzugsweise Krebs.
Abstract translation:本发明涉及通式(I),其中R1是氢原子,羟基或甲氧基,卤原子或NO 2基团的化合物; R2是氢原子,羟基或甲氧基,酰基或芳酰基; R 3是氢,三氟乙酰基(C(= O)CF 3)或对硝基苯甲酰基(C(= O)PhNO2),并且在每种情况下,波浪线-OR3的两个可能的配置是指相对于底座主体; Y = [C(= O)],[C(= N)OH]或[CH-OH],[CH-NR 5 R 6]表示在两种可能的立体异构构型,其是R5和R6或者各自是氢原子或 提供一个氢原子和三氟乙酰基(TFA); 其中X = O,S或NR,其中R =氢或C1〜C4烷基; R 4是直链或支链的烷基或杂烷基是指具有1-19成员的链长,其中至多6个杂原子(O,N,S),如通过至少两个碳原子彼此分开可进行组合。 此外,本发明除其它外,根据式(I)和药物组合物,药物试剂盒和作为用于增殖性疾病或病症,优选癌症的治疗的药物中的用途制备化合物的方法。
Abstract:
Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed, compound of the formula (I): wherein n is 1 or 2; m is 0, 1, 2, 3, 4, 5, 6, 7 or 8; q is 0 or 1; t is 0 or 1; R 1 is alkyl having from 1 to 3 carbon atoms; R 2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; R 3 and R 4 together are alkyl having two or three carbon atoms; or R 3 and R 4 are the same as each other and each is methyl or ethyl; R 5 is hydrogen or alkyl having from one to six carbon atoms. A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, hydroxy, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or A is cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or A is a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula (I) by a ring carbon. Alternatively, the agent can be a pharmaceutically acceptable salt of the compound of Formula (I).
Abstract translation:公开了用于治疗各种代谢紊乱(例如胰岛素抵抗综合征,糖尿病,多囊卵巢综合征,高脂血症,脂肪肝疾病,恶病质,肥胖症,动脉粥样硬化和动脉硬化)的药剂,其中n为1 或2; m为0,1,2,3,4,5,6,7或8; q为0或1; t为0或1; R 1是具有1至3个碳原子的烷基; R 2是氢,卤素,具有1至3个碳原子的烷基或具有1至3个碳原子的烷氧基; R 3和R 4一起是具有两个或三个碳原子的烷基; 或R 3和R 4彼此相同,各自为甲基或乙基; R 5是氢或具有1至6个碳原子的烷基。 A是未取代的或被1或2个选自:卤素,羟基,具有1或2个碳原子的烷基,全氟甲基,具有1或2个碳原子的烷氧基和全氟甲氧基取代的苯基; 或A是具有3至6个环碳原子的环烷基,其中环烷基是未取代的或一个或两个环碳独立地被甲基或乙基单取代; 或A是具有1或2个选自N,S和O的环杂原子的5或6元杂芳环,杂芳环通过环碳与式(I)化合物的其余部分共价结合。 或者,试剂可以是式(I)化合物的药学上可接受的盐。