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    .alpha.-Hydroxy thioethers
    1.
    发明授权
    .alpha.-Hydroxy thioethers 失效
    α-羟基硫醚

    公开(公告)号：US4808572A

    公开(公告)日：1989-02-28

    申请号：US936671

    申请日：1986-12-01

    申请人： Andreas Beck ,  Werner Breitenstein ,  Andreas von Sprecher ,  Robert W. Lang ,  Konrad Oertle

    发明人： Andreas Beck ,  Werner Breitenstein ,  Andreas von Sprecher ,  Robert W. Lang ,  Konrad Oertle

    IPC分类号： A61K31/16 ,  A61K31/165 ,  A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61K31/22 ,  A61K31/23 ,  A61K38/00 ,  A61K45/00 ,  A61P11/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07C67/00 ,  C07C313/00 ,  C07C321/18 ,  C07C323/00 ,  C07C323/52 ,  C07C323/58 ,  C07C323/59 ,  C07C323/60 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07C149/243

    CPC分类号： C07K5/0606 ,  A61K31/19 ,  A61K31/215 ,  C07C323/00 ,  A61K38/00

    摘要： Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: a is an integer of from 1 to 7,R.sup.o represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted at the terminal carbon atom by a free or acylated hydroxy group, by a halogen atom having an atomic number of at most 17, or by methoxy, or represents C.sub.1-3 -perfluoroalkyl,R.sup.2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene or alternatively, if R.sup.1 represents a halogenated radical and/or B represents phenylene or ethylene, a single bond or vinylene,B represents a single bond, ethynylene or phenylene,R.sup.3 represents hydroxy, C.sub.1-7 -alkoxy or an optionally substituted amino group, and--X-- represents a single bond, a methylene group of an optionally N-acylated primary aminomethylene group,and their salts are active as leucotriene antagonists since they eliminate the contractions of smooth muscles brought about by leucotrienes, and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.

    摘要翻译： 式（I）的新型不对称硫醚，其中通式具有以下含义：a为1至7的整数，R 4表示氢或C 1-7 - 烷酰基，R 1表示C 1-3 - 烷基， 可以在末端碳原子上被游离或酰化的羟基，原子数至多为17的卤素原子或甲氧基取代，或表示C1-3-全氟烷基，R2表示任选不饱和的脂肪族基，其具有 5至15个碳原子，A代表乙烯，或者，如果R1代表卤代基，和/或B代表亚苯基或亚乙基，则单键或亚乙烯基，B代表单键，亚乙炔基或亚苯基，R3代表羟基，C1-7 - 烷氧基或任选取代的氨基，-X-表示单键，任选N-酰化的伯氨基亚甲基的亚甲基，并且它们的盐作为白三烯拮抗剂是有活性的，因为它们消除平滑肌的收缩b 由白细胞三烯生成，因此适用于治疗过敏性疾病，特别是哮喘病症。

    Aromatic thioethers
    2.
    发明授权
    Aromatic thioethers 失效
    芳香硫醚

    公开(公告)号：US4785004A

    公开(公告)日：1988-11-15

    申请号：US941676

    申请日：1986-12-15

    申请人： Andreas Von Sprecher ,  Werner Breitenstein ,  Andreas Beck ,  Robert W. Lang ,  Konrad Oertle

    发明人： Andreas Von Sprecher ,  Werner Breitenstein ,  Andreas Beck ,  Robert W. Lang ,  Konrad Oertle

    IPC分类号： C07D215/54 ,  C07D311/24 ,  C07C149/40 ,  A61K31/235

    CPC分类号： C07D311/24 ,  C07D215/54

    摘要： Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: R.sup.0 represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted by one or more halogen atoms having an atomic number of at most 17,R.sup.2 represents an aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene, a single bond or vinylene,B.sup.1 represents C.sub.1-7 -alkylene or phenylene,B.sup.2 represents a single bond, ethylene or phenylene, andM represents an aromatic radical of the partial formula ##STR2## in which the symbols have the following meanings: R.sup.3 represents hydrogen or C.sub.1-4 -alkyl,X represents NH, O, S or if R.sup.4 represents hydrogen, a single bond,one of the symbols R.sup.4 and R.sup.5 represents hydrogen and the other represents the group --CO--R.sup.6, orR.sup.4 and R.sup.5 together represent the radical --CO--C(R.sup.6).dbd.C(R.sup.7)--or--CO--C(R.sup.7).dbd.C(R.sup.6)--orR.sup.4 R.sup.5, together with X, represent the radical --N.dbd.C(R.sup.8)--C(R.sup.6).dbd.CH--,in whichR.sup.6 represents --(CH.sub.2).sub.b --COOR.sup.3 (in which b=0 to 2)R.sup.7 represents hydrogen or C.sub.1-4 -alkyl andR.sup.8 represents hydrogen, methyl, mythoxy or halogen,and their salts are active as leucotriene antagonists since they eliminate the contractions of smooth muscles brought about by leucotrienes, and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.

    摘要翻译： 式（I）的新颖的不对称硫醚，其中通式符号具有以下含义：R 0表示氢或C 1-7 - 烷酰基，R 1表示可以被一个或多个具有 原子数最多为17，R 2表示具有5至15个碳原子的脂族基团，A表示乙烯，单键或亚乙烯基，B1表示C1-7 - 亚烷基或亚苯基，B2表示单键，乙烯或亚苯基 ，M表示部分结构式（M）的芳族基团，其中符号具有以下含义：R 3表示氢或C 1-4 - 烷基，X表示NH，O，S或如果R 4表示氢，则 单键，R4和R5之一表示氢，另一个表示-CO-R6基团，或R4和R5一起代表基团-CO-C（R6）= C（R7）-OR-CO-C（ R7）= C（R6） - 或R4R5与X一起代表基团-N = C（R8）-C（R6）= CH-，其中R6表示 - （CH2）b-COOR3（其中b = 0至2）R7表示氢或C1-4烷基，R8表示氢，甲基，乙氧基或卤素，并且它们的盐作为白三烯拮抗剂是有活性的，因为它们消除了由白三烯引起的平滑肌的收缩，因此适用于 治疗过敏，特别是哮喘，病情。

    Alkanophenones useful for treating allergies
    3.
    发明授权
    Alkanophenones useful for treating allergies 失效
    用于治疗过敏的苯胺酮

    公开(公告)号：US5149717A

    公开(公告)日：1992-09-22

    申请号：US795227

    申请日：1991-11-15

    申请人： Andreas von Sprecher ,  Andreas Beck ,  Bruno Schaub ,  Robert W. Lang

    发明人： Andreas von Sprecher ,  Andreas Beck ,  Bruno Schaub ,  Robert W. Lang

    IPC分类号： C07D311/24 ,  C07D405/04

    CPC分类号： C07D405/04 ,  C07D311/24

    摘要： Substituted alkanophenones of general formula ##STR1## in which R.sub.1 is unsubstituted or fluorinated lower alkyl, R.sub.2 is hydrogen, or unsubstituted or fluorinated lower alkyl or lower alkenyl, X is lower alkylene, oxy, thio or a direct bond, alk is lower alkylene, n is 1 or 2, R.sub.3 is phenyl that is unsubstituted or is substituted by unsubstituted or fluorinated lower alkyl, by etherified or esterified hydroxy, by unsubstituted or lower alkylated amino and/or by free, esterified or amidated carboxy, or is lower alkyl that is unsubstituted, substituted by fluoro and chloro or substituted by free esterified or amidated carboxy, R.sub.4 is free, esterified or amidated carboxy or 5-tetrazolyl, and R.sub.5 is hydrogen or lower alkyl, have leucotriene-antagonistic properties and can be used as anti-allergic active ingredients in medicaments.

    摘要翻译： 其中R 1为未取代或氟化的低级烷基，R 2为氢或未取代或氟化的低级烷基或低级烯基，X为低级亚烷基，氧基，硫基或直接键的通式为（Ⅰ）的取代的烷基苯醌， 低级亚烷基，n是1或2，R3是未取代的或被未取代或氟化的低级烷基取代的苯基，被醚化或酯化的羟基，被未取代或低级烷基化的氨基和/或被游离的，酯化的或酰胺化的羧基取代，或者是 未取代的低级烷基，被氟和氯取代或被游离的酯化或酰胺化的羧基取代，R4是游离的，酯化的或酰胺化的羧基或5-四唑基，R 5是氢或低级烷基，具有白三烯拮抗性质，并且可以使用 作为药物中的抗过敏活性成分。

    Aliphatic thioethers
    5.
    发明授权
    Aliphatic thioethers 失效
    脂族硫醚

    公开(公告)号：US4649215A

    公开(公告)日：1987-03-10

    申请号：US748656

    申请日：1985-06-25

    申请人： Andreas von Sprecher ,  Ivan Ernest ,  Alan J. Main ,  Andreas Beck

    发明人： Andreas von Sprecher ,  Ivan Ernest ,  Alan J. Main ,  Andreas Beck

    IPC分类号： A61K38/00 ,  C07D309/12 ,  C07K5/06 ,  C07C149/20 ,  C07C147/02

    CPC分类号： C07K5/06191 ,  C07C323/00 ,  C07D309/12 ,  C07K5/0606 ,  A61K38/00

    摘要： Novel asymmetric thioethers of the formula ##STR1## in which R.sup.1 represents a C.sub.1-3 -alkyl radical or a C.sub.1-3 -hydroxyalkyl radical of which the hydroxy group may be in esterified form,R.sup.2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms,R.sup.3 represents hydroxy, alkoxy or an optionally substituted amino group, and-X- represents a single bond, a methylene group or an optionally N-acylated primary aminomethylene groupwherein the O-atom of the hydroxy group is in the transconfiguration relative to the S-atom, are effective as leucotriene-antagonists since they eliminate the contractions of smooth muscles caused by leucotrienes and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.

    摘要翻译： 式（I）的新型不对称硫醚，其中R 1表示C 1-3 - 烷基或羟基可以被酯化形成的C 1-3 - 羟基烷基，R 2表示具有 5至15个碳原子，R 3表示羟基，烷氧基或任选取代的氨基，-X-表示单键，亚甲基或任选N-酰化的伯氨基亚甲基，其中羟基的O-原子是 在相对于S原子的反式构型中，作为白三烯拮抗剂是有效的，因为它们消除了由白三烯引起的平滑肌的收缩，因此适用于治疗变态反应，特别是哮喘病症。

    Alkanophenones useful for treating allergies
    6.
    发明授权
    Alkanophenones useful for treating allergies 失效
    用于治疗过敏的苯胺酮

    公开(公告)号：US5145868A

    公开(公告)日：1992-09-08

    申请号：US794608

    申请日：1991-11-15

    申请人： Andreas von Sprecher ,  Andreas Beck

    发明人： Andreas von Sprecher ,  Andreas Beck

    IPC分类号： C07D333/16 ,  A61K8/00 ,  A61K8/49 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61P7/02 ,  A61P11/00 ,  A61P17/00 ,  A61P37/08 ,  A61Q17/04 ,  C07D311/24 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14

    CPC分类号： C07D405/04 ,  C07D311/24 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14

    摘要： Substituted alkanophenones of the general formula ##STR1## in which R.sub.1 is unsubstituted or fluorinated lower alkyl, R.sub.2 is hydrogen, or unsubstituted or fluorinated lower alkyl or lower alkenyl, X is lower alkylene, oxy, thio or a direct bond, alk is lower alkylene, n is 1 or 2, R.sub.3 is a 5-membered heteroaryl radical that contains 1N, O or S atom as hetero atom and is unsubstituted or is substituted by unsubstituted or fluorinated lower alkyl, by etherified or esterified hydroxy, by unsubstituted or lower alkylated amino and/or by free, esterfied or amidated carboxy, R.sub.4 is free, esterified or amidated carboxy or 5-tetrazolyl, and R.sub.5 is hydrogen or lower alkyl, have leucotriene-antagonistic properties can e used as antiallergic active ingredients in medicaments.

    摘要翻译： 其中R 1为未取代或氟化的低级烷基，R 2为氢，或未取代或氟化的低级烷基或低级烯基，X为低级亚烷基，氧基，硫基或直接键合的取代的烷基苯甲酮 键，alk是低级亚烷基，n是1或2，R3是含有1N，O或S原子作为杂原子的5元杂芳基，未被取代或被未取代或氟化的低级烷基取代，通过醚化或酯化的羟基 通过未取代或低级烷基化的氨基和/或游离的酯化或酰胺化的羧基，R 4是游离的，酯化的或酰胺化的羧基或5-四唑基，R 5是氢或低级烷基，具有白三烯拮抗性能可以用作抗过敏活性 药物成分。

    Novel fluorinated resorcinol ethers
    8.
    发明授权
    Novel fluorinated resorcinol ethers 失效
    新型氟化间苯二酚醚

    公开(公告)号：US4670604A

    公开(公告)日：1987-06-02

    申请号：US801012

    申请日：1985-11-22

    申请人： Andreas Beck ,  Alfred Sallmann ,  Robert W. Lang ,  Paul Wenk

    发明人： Andreas Beck ,  Alfred Sallmann ,  Robert W. Lang ,  Paul Wenk

    IPC分类号： C07C39/24 ,  C07C43/225 ,  C07C43/23 ,  C07C45/46 ,  C07C45/71 ,  C07C49/825 ,  C07C49/84 ,  C07C205/37 ,  C07D257/04

    CPC分类号： C07D257/04 ,  C07C205/37 ,  C07C39/24 ,  C07C39/245 ,  C07C43/225 ,  C07C43/23 ,  C07C45/46 ,  C07C45/71 ,  C07C49/825 ,  C07C49/84

    摘要： 4-Acylresorcinol ethers of the formula ##STR1## in which R.sub.1 is lower alkyl, R.sub.2 is fluorinated lower alkyl, R.sub.3 is hydrogen, lower alkoxy, trifluoromethyl or halogen, alk is an alkylene or hydroxyalkylene radical which is uninterrupted or interrupted by oxygen, one of the radicals R.sub.4, R.sub.5 and R.sub.7 is a group of the formula --NH--C(.dbd.O)--R.sub.8, a radical R.sub.4 or R.sub.5 which differs from this is a radical R.sub.9 and a radical R.sub.7 which differs from this is a radical R.sub.10, R.sub.6 is hydrogen, lower alkyl, trifluoromethyl, halogen, carboxyl which is free, esterified or amidated, cyano or lower alkanoyl, R.sub.8 is carboxyl which is free, esterified or amidated or 5-tetrazolyl, R.sub.9 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl and R.sub.10 is hydrogen, lower alkyl, lower alkoxy, halogen, trifluoromethyl, cyano or carboxyl which is free, esterified or amidated, and their salts have antiallergic and antiinflammatory properties. They are prepared, for example, by reacting compounds of the formulae ##STR2## in which one of the radicals X.sub.5 and X.sub.6 is hydroxyl which is free or in salt form and the other is an alkoxy radical substituted by reactive esterified hydroxyl or epoxy. The invention also relates to intermediates of the formula ##STR3## in which R.sub.2 is fluorinated lower alkyl, R.sub.3 is hydrogen, lower alkoxy, trifluoromethyl or halogen and R.sub.11 is hydrogen or a group of the formula R.sub.1 --O(.dbd.O)--, in which R.sub.1 is lower alkyl, and their salts.

    摘要翻译： 其中R 1是低级烷基，R 2是氟化的低级烷基，R 3是氢，低级烷氧基，三氟甲基或卤素的式（I）的4-间酰基间苯二酚醚，alk是不间断或中断的亚烷基或羟基亚烷基 氧，基团R4，R5和R7之一是式-NH-C（= O）-R8的基团，与此不同的基团R 4或R 5是基团R 9和与此不同的基团R 7， 基团R 10，R 6为氢，低级烷基，三氟甲基，卤素，羧基，其游离，酯化或酰胺化，氰基或低级烷酰基，R8为羧基，其为游离的，酯化的或酰胺化的或5-四唑基，R 9为氢，低级烷基 ，低级烷氧基，卤素或三氟甲基，R 10是氢，低级烷基，低级烷氧基，卤素，三氟甲基，氰基或羧基，它们是游离的，酯化的或酰胺化的，并且它们的盐具有抗过敏和抗炎性质。 它们例如通过使式（IMAGE）的化合物与基团X5和X6中的一个是游离的或盐形式的羟基反应而制备，另一种是被反应性酯化的羟基或环氧基取代的烷氧基。 本发明还涉及其中R 2是氟化的低级烷基，R 3是氢，低级烷氧基，三氟甲基或卤素，R 11是氢或式R 1 -O（= O）的基团的式（ⅩⅩⅢ）中间体， - ，其中R1是低级烷基，及其盐。

    Oxaloamino substituted fluorinated resorcinol ethers and anti-allergic and anti-inflammatory use thereof
    9.
    发明授权
    Oxaloamino substituted fluorinated resorcinol ethers and anti-allergic and anti-inflammatory use thereof 失效
    草酰胺取代的氟代间苯二酚醚及其抗过敏和抗炎用途

    公开(公告)号：US4820726A

    公开(公告)日：1989-04-11

    申请号：US3156

    申请日：1987-01-14

    申请人： Andreas Beck ,  Alfred Sallmann ,  Robert W. Lang ,  Paul Wenk

    发明人： Andreas Beck ,  Alfred Sallmann ,  Robert W. Lang ,  Paul Wenk

    IPC分类号： C07C39/24 ,  C07C43/225 ,  C07C43/23 ,  C07C45/46 ,  C07C45/71 ,  C07C49/825 ,  C07C49/84 ,  C07C205/37 ,  C07D257/04 ,  C07C103/14 ,  A61K31/165

    CPC分类号： C07D257/04 ,  C07C205/37 ,  C07C39/24 ,  C07C39/245 ,  C07C43/225 ,  C07C43/23 ,  C07C45/46 ,  C07C45/71 ,  C07C49/825 ,  C07C49/84

    摘要： 4-Acylresorcinol esthers of the formula ##STR1## in which R.sub.1 is lower alkyl, R.sub.2 is fluorinated lower alkyl, R.sub.3 is hydrogen, lower alkoxy, trifluoromethyl or halogen, alk is an alkylene or hydroxyalkylene radical which is uninterrupted or interrupted by oxygen, one of the radicals R.sub.4, R.sub.5 and R.sub.7 is a group of the formula --NH--C(.dbd.O)--R.sub.8, a radical R.sub.4 or R.sub.5 which differs from this is a radical R.sub.9 and a radical R.sub.7 which differs from this is a radical R.sub.10, R.sub.6 is hydrogen, lower alkyl, trifluoromethyl, halogen, carboxyl which is free, esterified or amidated, cyano or lower alkanoyl, R.sub.8 is carboxyl which is free, esterified or amidated or 5-tetrazolyl, R.sub.9 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl and R.sub.10 is hydrogen, lower alkyl, lower alkoxy, halogen, trifluoromethyl, cyano or carboxyl which is free, esterified or amidated, and their salts have antiallergic and antiinflammatory properties. They are prepared, for example, by reacting compounds of the formulae ##STR2## in which one of the radicals X.sub.5 and X.sub.6 is hydroxyl which is free or in salt form and the other is an alkoxy radical substituted by reactive esterified hydroxy or epoxy. The invention also relates to intermediates of the formula ##STR3## in which R.sub.2 is fluorinated lower alkyl, R.sub.3 is hydrogen, lower alkoxy, trifluoromethyl or halogen and R.sub.11 is hydrogen or a group of the formula R.sub.1 --C(--O)--, in which R.sub.1 is lower alkyl, and their salts.

    摘要翻译： 其中R 1是低级烷基，R 2是氟化的低级烷基，R 3是氢，低级烷氧基，三氟甲基或卤素的式（Ⅰ）的4-酰基间苯二酚衍生物，alk是不间断或中断的亚烷基或羟基亚烷基 氧，基团R4，R5和R7之一是式-NH-C（= O）-R8的基团，与此不同的基团R 4或R 5是基团R 9和与此不同的基团R 7， 基团R 10，R 6为氢，低级烷基，三氟甲基，卤素，羧基，其游离，酯化或酰胺化，氰基或低级烷酰基，R8为羧基，其为游离的，酯化的或酰胺化的或5-四唑基，R 9为氢，低级烷基 ，低级烷氧基，卤素或三氟甲基，R 10是氢，低级烷基，低级烷氧基，卤素，三氟甲基，氰基或羧基，它们是游离的，酯化的或酰胺化的，并且它们的盐具有抗过敏和抗炎性质。 它们例如通过使其中一个基团X5和X6是游离的或盐形式的羟基的另一种是由活性酯化的羟基或环氧基取代的烷氧基使式（Ⅰ）的化合物反应而制备。 本发明还涉及其中R 2是氟化的低级烷基，R 3是氢，低级烷氧基，三氟甲基或卤素，R 11是氢或式R 1 -C（-O）的基团的式（ⅩⅩⅢ）中间体， - ，其中R1是低级烷基，及其盐。

    DOOR HANDLE ASSEMBLY FOR A MOTOR VEHICLE
    10.
    发明申请
    DOOR HANDLE ASSEMBLY FOR A MOTOR VEHICLE 有权
    车门组件用于电动车

    公开(公告)号：US20140361556A1

    公开(公告)日：2014-12-11

    申请号：US14295405

    申请日：2014-06-04

    申请人： Andreas Beck ,  Ralf Lennhoff ,  Mario Christensen

    发明人： Andreas Beck ,  Ralf Lennhoff ,  Mario Christensen

    IPC分类号： E05B7/00

    CPC分类号： E05B77/06 ,  E05B77/02 ,  E05B85/10 ,  Y10S292/22 ,  Y10T292/57

    摘要： A door handle assembly for a motor vehicle includes an operating handle moveably supported on a handle mounting, a mechanical coupling device and a locking device. An acceleration force can move the locking device from a normal operating position, in which an actuation of the operating handle is possible, in a first blocking direction, in which an actuation of the closing assembly via the operating handle and/or the coupling device, is blocked. The locking device also blocks the door handle assembly when long lasting or strongly pronounced oscillations occur as a result of a crash. In that event, the locking device can move from the normal operating position in a second blocking direction, in which an actuation of the closing assembly via the operating handle and/or the coupling device is blocked, wherein the second blocking direction is oriented opposite the first blocking direction.

    摘要翻译： 用于机动车辆的门把手组件包括可移动地支撑在手柄安装件上的操作手柄，机械联接装置和锁定装置。 加速力可以将锁定装置从第一阻挡方向的操作手柄的致动操作的正常操作位置移动，其中通过操作手柄和/或联接装置致动闭合组件， 被封锁。 当由于碰撞而发生长时间或强烈显着的振荡时，锁定装置还阻挡门把手组件。 在这种情况下，锁定装置可以在第二阻挡方向上从正常操作位置移动，其中经由操作手柄和/或联接装置的闭合组件的致动被阻挡，其中第二阻挡方向与 第一阻挡方向。