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    Pseudo-sequence method for comparing 7tm receptors with respect to the physico-chemical properties of their binding sites
    1.
    发明申请
    Pseudo-sequence method for comparing 7tm receptors with respect to the physico-chemical properties of their binding sites 审中-公开
    比较7tm受体相对于其结合位点的物理化学性质的伪序列方法

    公开(公告)号：US20070156342A1

    公开(公告)日：2007-07-05

    申请号：US10547944

    申请日：2004-03-05

    申请人： Thomas Frimurer ,  Trond Ulven ,  Thomas Hogberg ,  Christian Elling

    发明人： Thomas Frimurer ,  Trond Ulven ,  Thomas Hogberg ,  Christian Elling

    IPC分类号： G06F19/00 ,  G06G7/48

    CPC分类号： G16B20/00 ,  G16B15/00

    摘要： A pseudo-sequence method for comparing 7TM receptors with respect to the physicochemical properties of their binding sites, the method comprising the steps of: (i) optionally, aligning part of or all of the amino acid sequence of the first 7TM receptor with part of or all or the amino acid sequence of the one or more further 7TM receptors, (ii) selecting, in a sequential or non-sequential order, at the most 12 amino acid residues per helix and/or extracellular loops, which are involved in one or more binding sites of each 7TM receptor. (iii) forming a pseudo-sequence comprising at the most 50 amino acid residues from the selected sequential or non-sequential amino acid residues, (iv) for each 7TM receptor assigning one or more physicochemical descriptors to the amino acid residues of the selected amino acid pseudo-sequence involved in one or more binding sites, (v) optionally, for each 7TM receptor mathematically manipulating the physicochemical descriptors of step (iv) to obtain a simplified measure of the physicochemical properties of the binding site. (vi) for each 7TM receptor generating a similarity score as defined herein by comparing the physicochemical descriptor or, if relevant, the simplified measure for the first 7TM receptor with the physicochemical descriptors or, if relevant, the simplified measures for the one or further 7TM receptors, (vii) optionally, ranking the 7TM receptors with respect to the physicochemical properties of their binding sites according to the similarity scores obtained in step vi)

    摘要翻译： 一种用于比较7TM受体相对于其结合位点的物理化学性质的伪序列方法，所述方法包括以下步骤：（i）任选地使第一7TM受体的部分或全部氨基酸序列与 或全部或一个或多个其它7TM受体的氨基酸序列，（ii）以顺序或非顺序的顺序选择每个螺旋和/或细胞外环最多12个氨基酸残基，其参与一个 或更多的每个7TM受体的结合位点。 （iii）形成包含来自所选序列或非连续氨基酸残基的至多50个氨基酸残基的伪序列，（iv）对于每个7TM受体，将一个或多个物理化学描述符分配给所选氨基酸的氨基酸残基 参与一个或多个结合位点的酸性伪序列，（v）任选地，对于每个7TM受体，在数学上操纵步骤（iv）的物理化学描述符以获得结合位点的物理化学性质的简化测量。 （vi）对于每个7TM受体，通过将物理化学描述符或如果相关的第一7TM受体的简化测量与物理化学描述符相比较，或者如果相关的话，通过将一个或另外7个TM的简化测量 受体，（vii）任选地，根据步骤vi）中获得的相似性得分，相对于其结合位点的物理化学性质对7TM受体进行排序，

    Quinoline compounds for use in mch receptor related disorders
    2.
    发明申请
    Quinoline compounds for use in mch receptor related disorders 审中-公开
    用于mch受体相关疾病的喹啉化合物

    公开(公告)号：US20060111357A1

    公开(公告)日：2006-05-25

    申请号：US10538455

    申请日：2003-12-11

    申请人： Thomas Frimurer ,  Trond Ulven ,  Thomas Hogberg ,  Pia Norregaard ,  Paul Little ,  Jean-Marie Receveur

    发明人： Thomas Frimurer ,  Trond Ulven ,  Thomas Hogberg ,  Pia Norregaard ,  Paul Little ,  Jean-Marie Receveur

    IPC分类号： A61K31/519 ,  A61K31/517 ,  A61K31/498 ,  A61K31/4745 ,  A61K31/525 ,  A61K31/4709

    CPC分类号： C07D401/04 ,  A61K31/435 ,  A61K31/4375 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/519

    摘要： The present invention relates to the use of quinoline compounds for the preparation of a pharmaceutical and/or a cosmetic composition for the treatment, prophylaxis and/or diagnosis of a condition caused by or involving a melanin-concentrating hormone. The invention also relates to novel quinoline compounds per se. The quinoline compounds have been found to interact with a melanin-concentrating hormone receptor, a MCH receptor. The compounds have modulating activity on the MCH receptor such as e.g. antagonistic, agonistic or allosteric activity and are useful for medicinal or cosmetic purposes such as, e.g. in the treatment or prevention of feeding disorders like obesity, metabolic syndrome, Type II diabetes, bulimia, etc. or in the treatment or prevention of depression.

    摘要翻译： 本发明涉及喹啉化合物在制备药物和/或化妆品组合物中的用途，用于治疗，预防和/或诊断由黑色素浓缩激素引起或涉及的病症。 本发明还涉及新的喹啉化合物本身。 已发现喹啉化合物与黑色素浓缩激素受体MCH受体相互作用。 这些化合物对MCH受体具有调节活性，例如。 拮抗，激动或变构活性，并且可用于药物或化妆品目的，例如。 治疗或预防肥胖症，代谢综合征，II型糖尿病，食欲过盛等进食障碍，或治疗或预防抑郁症。

    CRTH2 Receptor Ligands For Medicinal Uses
    4.
    发明申请
    CRTH2 Receptor Ligands For Medicinal Uses 失效
    CRTH2受体配体用于药用

    公开(公告)号：US20090099189A1

    公开(公告)日：2009-04-16

    申请号：US11597873

    申请日：2005-05-30

    申请人： Trond Ulven ,  Thomas Frimurer ,  Oystein Rist ,  Evi Kostenis ,  Thomas Hogberg ,  Jean-Marie Receveur ,  Marie Grimstrup

    发明人： Trond Ulven ,  Thomas Frimurer ,  Oystein Rist ,  Evi Kostenis ,  Thomas Hogberg ,  Jean-Marie Receveur ,  Marie Grimstrup

    IPC分类号： A61K31/53 ,  C07D263/32 ,  A61K31/421 ,  C07D403/02 ,  C07D231/12 ,  A61K31/415

    CPC分类号： A61K31/415 ,  A61K31/454 ,  C07D231/12 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D277/34

    摘要： Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis, wherein A represents a carboxyl group —COON, or a carboxyl bioisostere; A1, is hydrogen or methyl; ring Ar1 is an optionally substituted phenyl ring 5- or 6-membered monocyclic heteroaryl ring, in which AA1CHO— and L2 are linked to adjacent ring atoms; rings Are2, Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; t is 0 or 1; L2 and L3 are linker radicals as defined in the description.

    摘要翻译： 式（I）化合物可用于治疗对CRTH2受体活性调节作用的疾病，例如哮喘，鼻炎，过敏性气道综合征和过敏性鼻炎支原体，其中A表示羧基-COON或羧基生物电子等排体; A1，是氢或甲基; 环Ar1是任选取代的苯环5-或6-元单环杂芳基环，其中AA1CHO-和L2与相邻的环原子连接; 环A 2，Ar 3各自独立地表示苯基或5-或6-元单环杂芳基环，或由5-或6-元碳环或杂环组成的双环系统，其被苯并稠合或稠合至5-或 6元单环杂芳基环，所述环或环系统任选被取代; t为0或1; L2和L3是如说明书中定义的连接基团。

    CRTH2 Receptor Ligands For Therapeutic Use
    5.
    发明申请
    CRTH2 Receptor Ligands For Therapeutic Use 审中-公开
    CRTH2受体配体用于治疗用途

    公开(公告)号：US20090105218A1

    公开(公告)日：2009-04-23

    申请号：US11597938

    申请日：2005-05-30

    申请人： Trond Ulven ,  Thomas Frimurer ,  Oystein Rist ,  Evi Kostenis ,  Thomas Hogberg

    发明人： Trond Ulven ,  Thomas Frimurer ,  Oystein Rist ,  Evi Kostenis ,  Thomas Hogberg

    IPC分类号： A61K31/196 ,  A61K31/44 ,  A61K31/381 ,  A61K31/341 ,  A61K31/5375 ,  A61K31/445 ,  A61K31/55 ,  A61P17/00 ,  A61P25/00 ,  A61P1/00 ,  A61P11/00

    CPC分类号： A61K31/245 ,  A61K31/196 ,  A61K31/341 ,  A61K31/40 ,  A61K31/4453 ,  A61K31/5375 ,  A61K31/55 ,  A61K31/63 ,  A61K31/635

    摘要： Compounds of formula (I) are useful in the treatment of disease responsive to modulation of CRTH2 receptor activity, wherein: A represents a carboxyl group —COOH, or a carboxyl bioisostere; L1 is a bond, —CH2—, —OCH2—, —CH2CH2— or —CH═CH—; L2 is CONH—, —NHCO—, SO2NR1—, —NR1SO2 wherein R1 is hydrogen or C1-C3 alkyl, or a divalent radical of formula (X) or (Y), wherein ring Q is a non aromatic heterocyclic ring containing 5 to 7 ring atoms, including the nitrogen shown; L3 is a divalent linker radical of formula -(Alk1)m-(Z)n-(Alk2)p as defined in the description; ring Ar1 is an optionally substituted divalent phenyl radical or divalent 5- or 6-membered monocyclic heteroaryl radical, in which L1 and the H[B]sL3L2Ar2CONH-radical are linked to adjacent ring carbon atoms; ring Ar2 is an optionally substituted 1,3-phenylene radical, or an optionally substituted divalent 5- or 6-membered monocyclic heteroaryl radical, in which AL1Ar1NHCO-radical and the H[B]sL3L2-radical are linked to ring carbon atoms which are not in ortho relationship; ring B is as defined for Ar2, or an optionally substituted cycloalkyl, N-pyrrolidinyl, N-piperidinyl or N-azepinyl ring; and s is 0 or 1.

    摘要翻译： 式（I）化合物可用于治疗对CRTH2受体活性调节作用的疾病，其中：A表示羧基-COOH或羧基生物电子等排体; L 1是键，-CH 2 - ， - OCH 2 - ， - CH 2 CH 2 - 或-CH-CH-; L2是CONH，-NHCO-，SO2NR1，-NR1SO2，其中R1是氢或C1-C3烷基，或式（X）或（Y）的二价基团，其中环Q是非芳族杂环， 7个环原子，包括所示的氮; L3是描述中定义的式 - （Alk1）m-（Z）n-（Alk2）p的二价连接基团; 环Ar1是任选取代的二价苯基或二价5-或6-元单环杂芳基，其中L1和H [B] sL3L2Ar2CONH-基团与相邻的环碳原子连接; 环Ar2是任选取代的1,3-亚苯基或任选取代的二价5-或6-元单环杂芳基，其中AL1Ar1NHCO-基和H [B] sL3L2-自由基与环碳原子连接， 不在邻近关系; 环B如Ar 2所定义，或任选取代的环烷基，N-吡咯烷基，N-哌啶基或N-氮杂环基; s为0或1。

    Substituted Thiazoleacetic Acid as Crth2 Ligands
    6.
    发明申请
    Substituted Thiazoleacetic Acid as Crth2 Ligands 审中-公开
    取代噻唑乙酸作为Crth2配体

    公开(公告)号：US20080119456A1

    公开(公告)日：2008-05-22

    申请号：US11597839

    申请日：2005-05-30

    申请人： Trond Ulven ,  Thomas Frimurer ,  Oystein Rist ,  Evi Kostenis ,  Thomas Hogberg ,  Jean-Marie Receveur ,  Marie Grimstrup

    发明人： Trond Ulven ,  Thomas Frimurer ,  Oystein Rist ,  Evi Kostenis ,  Thomas Hogberg ,  Jean-Marie Receveur ,  Marie Grimstrup

    IPC分类号： A61K31/53 ,  A61K31/506 ,  A61K31/55 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

    CPC分类号： C07D277/30 ,  C07D417/04 ,  C07D417/06

    摘要： Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis; wherein X1 is —S—, —O—, —N═N—. —NR7—, —CR7═CR8—, —CR7═N—, wherein R7 and R8 are independently hydrogen or C1-C3 alkyl; A is a carboxyl group —COOH, or a carboxyl bioisostere; rings Ar2 and Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; ring B is as defined for Ar2 and Ar3, or an optionally substituted N-pyrrolidinyl, N-piperidinyl or N-azepinyl ring; s is 0 or 1; L1, L2 and L4 are linker radicals as defined in the description; Q1 and Q2 represent substituents as defined in the description.

    摘要翻译： 式（I）化合物可用于治疗对CRTH2受体活性调节作用的疾病，例如哮喘，鼻炎，过敏性气道综合征和过敏性鼻炎支原体炎; 其中X 1是-S - ， - O - ， - N-N-。 -NR 7 - ，-CR 7 -CR 8 - ，-CR 7-N-，其中R R 7和R 8独立地是氢或C 1 -C 3烷基; A是羧基-COOH或羧基生物电子等排体; 环Ar 2和Ar 3各自独立地表示苯基或5或6元单环杂芳基环，或由5-或6-元环组成的双环系统 苯并稠合或稠合到5-或6-元单环杂芳基环的碳环或杂环，所述环或环系统任选被取代; 环B如Ar 2和Ar 3所定义，或任选取代的N-吡咯烷基，N-哌啶基或N-氮杂环丁基环; s为0或1; L1，L2和L4是描述中定义的连接基团; Q 1和Q 2表示如说明书中定义的取代基。

    Efficient stereoconservative synthesis of 1-substituted (S)- and (R)-2-aminomethylpyrrolidines and intermediates thereto
    9.
    发明授权
    Efficient stereoconservative synthesis of 1-substituted (S)- and (R)-2-aminomethylpyrrolidines and intermediates thereto 失效
    1-取代（S） - 和（R）-2-氨基甲基吡咯烷的有效立体保守合成及其中间体

    公开(公告)号：US5300660A

    公开(公告)日：1994-04-05

    申请号：US974683

    申请日：1992-11-12

    申请人： Hans-Jurgen Federsel ,  Thomas Hogberg ,  Sten I. Ramsby ,  Hans E. P. Strom

    发明人： Hans-Jurgen Federsel ,  Thomas Hogberg ,  Sten I. Ramsby ,  Hans E. P. Strom

    IPC分类号： C07D207/08 ,  C07D207/09 ,  C07D207/16

    CPC分类号： C07D207/08 ,  C07D207/09 ,  C07D207/16

    摘要： Stereoconservative method for preparation of an (R)- or (S)-isomer of the compound of the formula I with at least 95% optical purity ##STR1## wherein R.sup.1 is a hydrogen atom, a saturated or unsaturated lower alkyl group, a cycloalkyl group, or a group (CH.sub.2).sub.m Ph wherein m is 0-3 and Ph is a substituted or unsubstituted phenyl group including1) O,N-dialkylation, directly or stepwise of (R)- or (S)-proline2) aminolysis3) reduction to formation of the (R)- or (S)-isomer of the compound of the formula I, and new intermediates II and III in optical active form obtained by the reaction steps above and wherein R.sup.2 is defined as R.sup.1 above. ##STR2##

    摘要翻译： 用于制备具有至少95％光学纯度（*化学结构*）（I）的式I化合物的（R） - 或（S） - 异构体的立体保真剂方法，其中R 1是氢原子，饱和或不饱和的 低级烷基，环烷基或基团（CH 2）m Ph，其中m为0-3，Ph为取代或未取代的苯基，包括1）O，N-二烷基化，直接或分步的（R） - 或（ S） - 脯氨酸2）氨解3）还原形成式I化合物的（R） - 或（S） - 异构体，以及通过上述反应步骤获得的光学活性形式的新中间体II和III，其中 R2定义为R1。 （*化学结构*）（II）（*化学结构*）（III）