中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

260 records (took 0.022 seconds)

    Procedure for the preparation of racemic and enantiomerically pure derivatives of 1,5 diaryl-3-trifluorromethyl-Δ2-pyrazolines
    31.
    发明授权
    Procedure for the preparation of racemic and enantiomerically pure derivatives of 1,5 diaryl-3-trifluorromethyl-Δ2-pyrazolines 失效

    公开(公告)号：US06958403B2

    公开(公告)日：2005-10-25

    申请号：US11007449

    申请日：2004-12-08

    Applicant: Montserrat Alcon-Marrugat ,  Miguel Angel Pericas-Brondo ,  Maria Rosa Cuberes-Altisen ,  Jordi Frigola-Constansa

    Inventor： Montserrat Alcon-Marrugat ,  Miguel Angel Pericas-Brondo ,  Maria Rosa Cuberes-Altisen ,  Jordi Frigola-Constansa

    IPC: C07D231/06 ,  C07D231/12

    CPC classification number: C07D231/06

    Abstract: Procedure for preparation of compounds with the general formula 1, which include the racemic mixtures (±)-1, and the enantiomerically pure compounds (−)-1 and (+)-1, wherein R1 and R3, like or different, represent an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl or methoxy group; R2 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group; R4 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group, with the condition that one of the substituents R2 or R4 is a methylsulphonyl or aminosulphonyl group; which involves obtaining the racemic mixture with the general formula (±)-1 by reacting an (E)-1,1,1-trifluoro-4-aryl-3-buten-2-one with a phenylhydrazine, followed by a treatment with chlorosulphonic acid, or by reacting with chlorosulphonic acid followed by a reaction with sodium hydroxide and, finally, with thionyl chloride. The product obtained by either of these methods is made to react with ammonium carbonate or ammonia, or with sodium sulphite and methyl iodide or methyl sulphate. In addition, to obtain the enantiomerically pure compounds with the general formula 1 by resolving the racemic mixture with the general formula (±)-1, a reaction is effected with optically active ephedrine, followed by formation of the sodium salt of each enantiomer, reaction with thionyl chloride and ammonium carbonate or ammonia, or instead with thionyl chloride followed by sodium sulphite and methyl iodide or methyl sulphate to thereby obtain separately the enantiomerically pure compounds with the general formulae (−)-1 and (±)-1.

    Thienylazolylalkoxyethanamines, their preparation and their application as medicaments
    32.
    发明申请
    Thienylazolylalkoxyethanamines, their preparation and their application as medicaments 审中-公开
    噻嗪基烷氧基乙胺，它们的制备及其作为药物的应用

    公开(公告)号：US20020188017A1

    公开(公告)日：2002-12-12

    申请号：US10139674

    申请日：2002-05-06

    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.

    Inventor： Ramon Merce-Vidal ,  Blas Andaluz-Mataro ,  Jordi Frigola-Constansa

    IPC: C07D49/02

    CPC classification number: A61K31/4155 ,  C07D409/04 ,  C07D409/06

    Abstract: The thienylazolylalkoxyethanamines (I) where R1 is a hydrogen atom, a halogen atom or a lower alkyl radical; R2, R3 and R4 represent, independently, a hydrogen atom or a lower alkyl radical; and Az represents a five-member nitrogenated hetercyclic aromatic group, N-methyl-substituted, that contains from one to three nitrogen atoms. They have analgesic activity in mammals, including humans. The compounds (I) can be obtained, for example, by reaction of a derivative of hydroxy-thienylazol (IV) with a derivative of a suitable N-(ethyl)amine. The compounds (IV) are useful intermediates in the synthesis of the compounds (I). The compounds (I) have an application in human and/or veterinary medicine.

    Abstract translation: 其中R 1是氢原子，卤素原子或低级烷基的噻吩基唑烷基乙胺（I） R2，R3和R4独立地表示氢原子或低级烷基; 并且Az表示含有一至三个氮原子的五元氮杂环芳族基团N-甲基取代基。 它们在哺乳动物，包括人类中具有止痛活性。 化合物（I）可以通过例如羟基噻吩唑（IV）的衍生物与合适的N-（乙基）胺衍生物的反应来获得。 化合物（IV）是化合物（I）的合成中的有用的中间体。 化合物（I）在人和/或兽医学中有应用。

    Process for obtaining enantiomers of cis-olirtine
    33.
    发明授权
    Process for obtaining enantiomers of cis-olirtine 失效
    获得顺式 - 奥利汀对映异构体的方法

    公开(公告)号：US6118009A

    公开(公告)日：2000-09-12

    申请号：US485023

    申请日：2000-02-01

    Applicant: Antoni Torrens-Jover ,  Jordi Frigola-Constansa

    Inventor： Antoni Torrens-Jover ,  Jordi Frigola-Constansa

    IPC: C07D231/12

    CPC classification number: C07D231/12

    Abstract: The procedure comprises (a) the enantioselective reduction of a pro-chiral ketone (III) by using a reducing and agent and chiral catalyst, both boron derivatives, in an anhydrous solvent or mixture of anhydrous solvents to form an enantiomer of an alcohol (II), and (b), the alkylation of (II), in phase transfer conditions, with optionally prior isolation and purification thereof, with 2-chloro-N,N-dimethylethylamine, to form an enantiomer of (I). Cyzolirtine exhibits analgesic properties.

    Abstract translation: PCT No.PCT / ES98 / 00223 Sec。 371日期2000年2月1日 102（e）日期2000年2月1日PCT提交1998年7月31日PCT公布。 公开号WO99 /​​ 07684 日期1999年2月18日该方法包括（a）通过使用还原剂和试剂和手性催化剂（硼衍生物）在无水溶剂或无水溶剂混合物中形成对映异构体（a）对映异构选择性还原前手性酮 的醇（II）和（b）中，（II）在相转移条件下的烷基化，任选地先前用2-氯-N，N-二甲基乙胺分离和纯化，形成（I ）。 Cyzolirtine具有镇痛作用。

    Inhibition of the withdrawal syndrome
    36.
    发明授权
    Inhibition of the withdrawal syndrome 失效
    戒断综合征的抑制

    公开(公告)号：US5162323A

    公开(公告)日：1992-11-10

    申请号：US615257

    申请日：1990-11-19

    Applicant: Jordi Frigola-Constansa ,  Juan Pares-Corominas

    Inventor： Jordi Frigola-Constansa ,  Juan Pares-Corominas

    IPC: C07D403/14 ,  A61K31/496 ,  A61K31/505 ,  A61K31/506 ,  A61P3/02 ,  A61P25/20 ,  A61P25/30 ,  A61P25/32 ,  A61P43/00 ,  C07D403/12 ,  C07D521/00

    CPC classification number: C07D231/12 ,  A61K31/505 ,  C07D233/56 ,  C07D249/08 ,  C07D403/12

    Abstract: The present invention relates to the use of the derivatives of general formula I ##STR1## in which: n can have the values 1 to 6, andR represents a hydrogen atom, a halogen, a C.sub.1 to C.sub.4 lower alkyl radical, a nitro radical, a hydroxyl radical, an oxo radical, a C.sub.1 to C.sub.4 lower alkoxy radical, a cyano radical, a C.sub.1 to C.sub.4 lower alkyl carboxylate radical, an aryl or substituted aryl radical, or an amino or substituted amino radical of formula ##STR2## in which R.sub.1 and R.sub.2, which may be identical or different, represent a hydrogen atom, an alkyl radical, an aryl radical, an alkylcarboxy radical, an arylcarboxy radical, an alkylsulphonyl radical or an arylsulphonyl radical, the alkyl fragments of these radicals containing from 1 to 4 carbon atomsfor the manufacture of medicinal products intended for the treatment of disorders associated with the withdrawal syndrome induced by the discontinuation of benzodiazepines such as diazepam, cocaine, alcohol and/or nicotine.

    Abstract translation: 本发明涉及通式I（I）的衍生物的用途，其中：n可以具有1至6的数值，R代表氢原子，卤素，C1至C4低级烷基， 硝基，羟基，氧基，C 1至C 4低级烷氧基，氰基，C 1至C 4低级烷基羧酸酯基，芳基或取代的芳基或氨基或取代的氨基， IMAGE>其中可以相同或不同的R 1和R 2表示氢原子，烷基，芳基，烷基羧基，芳基羧基，烷基磺酰基或芳基磺酰基，这些基团的烷基 含有1至4个碳原子用于制造旨在治疗由停止苯二氮卓类例如地西泮，可卡因，醇和/或尼古丁引起的戒断综合征相关疾病的药用产品。

    Substituted 1-diphenylmethyl azetidines
    37.
    发明授权
    Substituted 1-diphenylmethyl azetidines 失效
    取代的1-二甲基甲基丙烯酸酯

    公开(公告)号：US5073646A

    公开(公告)日：1991-12-17

    申请号：US541056

    申请日：1990-06-20

    Applicant: Augusto C. Pinol ,  Jordi F. Constansa ,  Juan P. Corominas

    Inventor： Augusto C. Pinol ,  Jordi F. Constansa ,  Juan P. Corominas

    IPC: C07D205/04

    CPC classification number: C07D205/04

    Abstract: New azetidines, characterized in that they correspond to the general formula (I) ##STR1## in which R.sub.3 represents an amino radical, an alkylamino radical, a dialkylamino radical, a cycloalkylamino radical, an acylamino radical, an alkylacylamino radical, an aminomethyl radical, an alkylaminomethyl radical, an acylaminomethyl radical or an alkylacylaminomethyl radical, in which radicals each acyl fragment may be substituted with one or more halogen, especially fluorine, atoms; and R.sub.1, R.sub.2, R.sub.4, R.sub.5 and R.sub.6 represent a hydrogen atom or a lower alkyl radical, with the proviso that at least one of them represents a lower alkyl radical, and also their salts.

    Abstract translation: 新的氮杂环丁烷，其特征在于它们对应于通式（I）其中R 3表示氨基，烷基氨基，二烷基氨基，环烷基氨基，酰基氨基，烷基酰氨基， 氨基甲基，烷基氨基甲基，酰氨基甲基或烷基酰基氨基甲基，其中每个酰基片段可被一个或多个卤素，特别是氟原子取代; 并且R 1，R 2，R 4，R 5和R 6表示氢原子或低级烷基，条件是它们中的至少一个表示低级烷基，以及它们的盐。

    2,5-Dihydroxy benzene sulfonic acid mono esters
    38.
    发明授权
    2,5-Dihydroxy benzene sulfonic acid mono esters 失效
    2,5-二羟基苯磺酸单酯

    公开(公告)号：US4115648A

    公开(公告)日：1978-09-19

    申请号：US626024

    申请日：1975-10-28

    Applicant: Antonio Esteve-Subirana

    Inventor： Antonio Esteve-Subirana

    IPC: C07C309/42 ,  C07D295/00 ,  C07D295/22 ,  C07C143/68

    CPC classification number: C07C309/00

    Abstract: Mono- and diesters of 2,5-dihydroxy benzene sulfonic acid are represented by one of the following formulae: ##STR1## wherein R and R' can be identical or different and represent an alkanyl, arylalkanoyl, aryloxyalkanoyl, aryl, alkanesulfonyl, arenesulfonyl, alkylarenesulfonyl or arylalkanesulfonyl radical, B represents the cation of an alkali metal, alkaline-earth metal of ammonia or an unsubstituted or substituted, open chain or cyclic amine, and are remarkable for their hypocholesterolemic, hypotriglycidemic and hypolipidemic activity.

    Abstract translation: 2,5-二羟基苯磺酸的单酯和二酯由下式表示：其中R和R'可以相同或不同，代表烷基，芳基烷酰基 芳基，烷磺酰基，芳烃磺酰基，烷基磺酰基或芳烷基磺酰基，B代表碱金属，氨的碱土金属或未取代的或取代的开链或环状胺的阳离子，并且对于它们的低胆固醇血症，降血糖流行和 降血脂活性。

Patent Agency Ranking