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    Quinazoline derivatives and pharmaceutical compositions containing them
    1.
    发明授权
    Quinazoline derivatives and pharmaceutical compositions containing them 有权
    喹唑啉衍生物和含有它们的药物组合物

    公开(公告)号：US08586608B2

    公开(公告)日：2013-11-19

    申请号：US12563340

    申请日：2009-09-21

    Applicant: Frank Himmelsbach ,  Elke Langkopf ,  Stefan Blech ,  Birgit Jung ,  Anke Baum ,  Flavio Solca

    Inventor： Frank Himmelsbach ,  Elke Langkopf ,  Stefan Blech ,  Birgit Jung ,  Anke Baum ,  Flavio Solca

    IPC: A61K31/47 ,  A01N43/42

    CPC classification number: C07D405/12 ,  C07D239/94

    Abstract: A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetra-hydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetra-hydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.

    Abstract translation: 通式I的化合物，其中：R a是苄基，1-苯乙基或3-氯-4-氟苯基; Rb是二甲基氨基，N-甲基-N-乙基氨基，二乙基氨基，N-甲基-N-异丙基氨基，N-甲基-N-环丙基氨基，N-甲基-N-（2-甲氧基乙基）氨基，N-乙基-N- （2-甲氧基乙基）氨基，双（2-甲氧基乙基）氨基，吗啉代，N-甲基-N-（四氢呋喃-3-基）氨基，N-甲基-N-（四氢呋喃-2-基甲基）氨基，N - 甲基-N-（四氢呋喃-3-基甲基）氨基，N-甲基-N-（四氢吡喃-4-基）氨基或N-甲基-N-（四氢吡喃-4-基甲基）氨基; Rc为环丙基甲氧基，环丁氧基，环戊氧基，四氢呋喃-3-基氧基，四氢呋喃-2-基甲氧基，四氢呋喃-3-基甲氧基，四氢吡喃-4-基氧基或四氢吡喃-4-基甲氧基，或互变异构体，立体异构体或盐 特别是其具有有价值的药理学特性的无机或有机酸或碱的生理上可接受的盐，特别是对由酪氨酸激酶介导的信号转导的抑制作用，它们在治疗疾病尤其是肿瘤疾病和肺疾病中的用途 和气道及其制备。

    METHODS OF TREATING DISEASES USING QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    2.
    发明申请
    METHODS OF TREATING DISEASES USING QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
    使用喹唑啉衍生物和含有它们的药物组合物治疗疾病的方法

    公开(公告)号：US20110046168A1

    公开(公告)日：2011-02-24

    申请号：US12914003

    申请日：2010-10-28

    Applicant: Frank HIMMELSBACH ,  Elke LANGKOPF ,  Stefan BLECH ,  Birgit JUNG ,  Anke BAUM ,  Flavio SOLCA

    Inventor： Frank HIMMELSBACH ,  Elke LANGKOPF ,  Stefan BLECH ,  Birgit JUNG ,  Anke BAUM ,  Flavio SOLCA

    IPC: A61K31/517 ,  A61P35/00 ,  A61P1/00 ,  A61P11/00 ,  A61P17/06

    CPC classification number: C07D405/12 ,  C07D239/94

    Abstract: A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetrahydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetrahydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.

    Abstract translation: 通式I的化合物，其中：R a是苄基，1-苯乙基或3-氯-4-氟苯基; Rb是二甲基氨基，N-甲基-N-乙基氨基，二乙基氨基，N-甲基-N-异丙基氨基，N-甲基-N-环丙基氨基，N-甲基-N-（2-甲氧基乙基）氨基，N-乙基-N- （2-甲氧基乙基）氨基，双（2-甲氧基乙基）氨基，吗啉代，N-甲基-N-（四氢呋喃-3-基）氨基，N-甲基-N-（四氢呋喃-2-基甲基）氨基，N-甲基 -N-（四氢呋喃-3-基甲基）氨基，N-甲基-N-（四氢吡喃-4-基）氨基或N-甲基-N-（四氢吡喃-4-基甲基）氨基; Rc为环丙基甲氧基，环丁氧基，环戊氧基，四氢呋喃-3-基氧基，四氢呋喃-2-基甲氧基，四氢呋喃-3-基甲氧基，四氢吡喃-4-基氧基或四氢吡喃-4-基甲氧基，或互变异构体，立体异构体或盐 特别是其具有有价值的药理学特性的无机或有机酸或碱的生理上可接受的盐，特别是对由酪氨酸激酶介导的信号转导的抑制作用，它们在治疗疾病尤其是肿瘤疾病和肺疾病中的用途 和气道及其制备。

    Quinazoline derivatives and pharmaceutical compositions containing them
    3.
    发明申请
    Quinazoline derivatives and pharmaceutical compositions containing them 审中-公开

    公开(公告)号：US20060100223A1

    公开(公告)日：2006-05-11

    申请号：US11313304

    申请日：2005-12-21

    Applicant: Frank Himmelsbach ,  Elke Langkopf ,  Stefan Blech ,  Birgit Jung ,  Anke Baum ,  Flavio Solca

    Inventor： Frank Himmelsbach ,  Elke Langkopf ,  Stefan Blech ,  Birgit Jung ,  Anke Baum ,  Flavio Solca

    IPC: A61K31/517 ,  C07D405/02 ,  C07D239/84

    CPC classification number: C07D405/12 ,  C07D239/94

    Abstract: A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetrahydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetrahydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.

    Process for preparing a ginger fraction and the use thereof for inhibiting human CYP enzymes
    5.
    发明申请
    Process for preparing a ginger fraction and the use thereof for inhibiting human CYP enzymes 审中-公开
    制备姜馏分的方法及其用于抑制人CYP酶的用途

    公开(公告)号：US20060051437A1

    公开(公告)日：2006-03-09

    申请号：US11209322

    申请日：2005-08-23

    Applicant: Thomas Ebner ,  Eva Ludwig-Schwellinger ,  Stefan Blech

    Inventor： Thomas Ebner ,  Eva Ludwig-Schwellinger ,  Stefan Blech

    IPC: A61K36/9068

    CPC classification number: A61K36/9068

    Abstract: The present invention relates to a process for preparing a ginger fraction, the fraction prepared by this process and the use thereof on its own or combined with drugs for inhibiting human cytochrome P450 (CYP) enzymes (particularly cytochrome P450 3A4, CYP3A4) for positively influencing the oral bioavailability and pharmacokinetics of active substances.

    Abstract translation: 本发明涉及一种制备姜馏分，通过该方法制备的级分及其用途本身或与抑制人细胞色素P450（CYP）酶（特别是细胞色素P450 3A4，CYP3A4）的药物组合的方法，用于积极影响 活性物质的口服生物利用度和药代动力学。

    Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them
    10.
    发明授权
    Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them 有权
    双环杂环，含有它们的药物组合物，它们的用途和制备它们的方法

    公开(公告)号：US06653305B2

    公开(公告)日：2003-11-25

    申请号：US09929931

    申请日：2001-08-15

    Applicant: Frank Himmelsbach ,  Elke Langkopf ,  Birgit Jung ,  Stefan Blech ,  Flavio Solca

    Inventor： Frank Himmelsbach ,  Elke Langkopf ,  Birgit Jung ,  Stefan Blech ,  Flavio Solca

    IPC: A61K31535

    CPC classification number: C07D405/12 ,  A61K31/505 ,  C07D239/94 ,  C07D413/12 ,  C07D413/14

    Abstract: A compound of formula (I) wherein: Ra is a benzyl or 1-phenylethyl group or a phenyl group substituted by the groups R1 and R2, wherein: R1 is a hydrogen, fluorine, chlorine, or bromine atom, or a methyl, trifluoromethyl, cyano, or ethynyl group, and R2 is a hydrogen or fluorine atom; Rb is an R3O—CO—CH2—N—CH2—CH2—OH group optionally substituted at the methylene groups by 1 or 2 methyl or ethyl groups, wherein R3 is a hydrogen atom or a C1-4-alkyl group, a 2-oxomorpholin-4-yl group optionally substituted by 1 or 2 methyl or ethyl groups, or a N-[(1,3-dioxolan-2-yl)methyl]methylamino group; Rc is a hydrogen atom, or a methoxy, ethoxy, 2-methoxyethoxy, 2-ethoxyethoxy, cyclobutyloxy, cyclopentyloxy, cyclohexyloxy, cyclopropylmethoxy, cyclobutylmethoxy, cyclopentylmethoxy, cyclohexylmethoxy, tetrahydrofuran-3-yloxy, tetrahydropyran-3-yloxy, tetrahydropyran-4-yloxy, tetrahydrofuranylmethoxy, or tetrahydropyranylmethoxy group; and n is 1, 2, or 3, the tautomers, stereoisomers, and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.

    Abstract translation: 式（I）的化合物，其中：R a是苄基或1-苯基乙基或被基团R 1和R 2取代的苯基，其中：R 1是氢，氟，氯或溴原子，或甲基，三氟甲基 ，氰基或乙炔基，R 2是氢或氟原子; R b是任选在亚甲基被1或2个甲基或乙基取代的R3O-CO-CH2-N-CH2-CH2-OH基团，其中R3是 氢原子或C1-4烷基，任选被1或2个甲基或乙基取代的2-氧代吗啉-4-基，或N - [（1,3-二氧戊环-2-基）甲基] 甲基氨基; R c是氢原子，或甲氧基，乙氧基，2-甲氧基乙氧基，2-乙氧基乙氧基，环丁氧基，环戊氧基，环己氧基，环丙基甲氧基，环丁基甲氧基，环戊基甲氧基，环己基甲氧基，四氢呋喃-3-基氧基，四氢吡喃-3-基氧基，四氢吡喃 -4-基氧基，四氢呋喃基甲氧基或四氢吡喃基甲氧基; andn为1,2或3，互变异构体，立体异构体及其盐，特别是其与具有有价值药理学性质的无机或有机酸或碱的生理上可接受的盐，它们在治疗疾病尤其是肿瘤疾病和疾病中的用途 的肺和气道，以及其制备。

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