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    Cannabinoid receptor modulators
    1.
    发明授权
    Cannabinoid receptor modulators 失效
    大麻素受体调节剂

    公开(公告)号：US08173680B2

    公开(公告)日：2012-05-08

    申请号：US12745708

    申请日：2008-12-08

    Applicant: Jean-Marie Receveur ,  Emelie Bjurling ,  Anthony Murray ,  Thomas Hoegberg ,  Peter Aadal Nielsen ,  Jean-Michel Linget ,  Pia Karina Noerregaard ,  Dorthe Almholt

    Inventor： Jean-Marie Receveur ,  Emelie Bjurling ,  Anthony Murray ,  Thomas Hoegberg ,  Peter Aadal Nielsen ,  Jean-Michel Linget ,  Pia Karina Noerregaard ,  Dorthe Almholt

    IPC: A61K31/445 ,  A61K31/41 ,  A61K31/415 ,  C07D401/02 ,  C07D271/06 ,  C07D231/00

    CPC classification number: C07D413/06 ,  C07D231/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04

    Abstract: Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful inter alia for treatment of obesity: Formula (I). Wherein: X is a bond, or a divalent radical selected from —C(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(R11)CH2—*, —C(R10)(R11)CH2—O—*, —CH2C(R10)(R11)—*, —CH2C(R10)(R11)—O—*, and —CH2—O—C(R10)(R11)—*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; Z is a carboxyl isostere radical selected from the group specified; R3 is hydrogen, (C1-C)alkyl or (C1C3)fluoroalkyl; R4 is a radical of formula -(Alk1)p-(Q1)r (L)s-Q2 wherein p, r, s, Alk1, L, Q1 and Q2 are as specified; or R3and R4 taken together with the nitrogen to which they are attached form a cyclic amino ring of 4 to 7 ring atoms which is optionally substituted by a radical of formula -(L)s-Q2 wherein s, L and Q2 are as defined above, or by an optional substituent selected from hydroxy, methoxy, —NH2—, or mono- or di-(C1C3)alkylamino; R5, R6, R7 and R8 are each independently selected from hydrogen —F, —Cl, —Br, —CN, (C1-C3)alkyl, (C1C3)fluoroalkyl, cyclopropyl, and —OR9; R10 is hydrogen, (C1C3)alkyl, hydroxyl or NH2, and R11 is hydrogen or (C1-C3)alkyl; or R10 and R11 taken together with the carbon atom to which they are attached form a (C3-C5)cycloalkyl ring.

    Abstract translation: 式（I）化合物是大麻素受体CB1的调节剂，尤其用于治疗肥胖症：式（I）。 其中X为键或选自-C（R 10）（R 11） - *，-C（R 10）（R 11）-O- *，-C（R 10）（R 11）CH 2 - C（R10）（R11）CH2-O- *，-CH2C（R10）（R11） - *，-CH2C（R10）（R11）-O- *和-CH2-O-C（R10）（R11） - *，其中由星号表示的键连接到吡唑环上; Z是选自指定组的羧基等价基团; R3是氢，（C1-C）烷基或（C1C3）氟烷基; R4是式 - （Alk1）p-（Q1）r（L）s-Q2的基团，其中p，r，s，Alk1，L，Q1和Q2如所规定; 或R 3和R 4与它们所连接的氮一起形成4至7个环原子的环状氨基，其任选被式 - （L）s-Q 2的基团取代，其中s，L和Q2如上所定义 或选自羟基，甲氧基，-NH 2 - 或单 - 或二 - （C 1 -C 3）烷基氨基的任选取代基; R5，R6，R7和R8各自独立地选自-F，-Cl，-Br，-CN，（C1-C3）烷基，（C1C3）氟烷基，环丙基和-OR9; R 10是氢，（C 1 -C 3）烷基，羟基或NH 2，R 11是氢或（C 1 -C 3）烷基; 或R 10和R 11与它们所连接的碳原子一起形成（C 3 -C 5）环烷基环。

    Modulators of CB1 receptors
    2.
    发明授权
    Modulators of CB1 receptors 有权

    公开(公告)号：US08148404B2

    公开(公告)日：2012-04-03

    申请号：US12518446

    申请日：2007-12-17

    Applicant: Martin Cooper ,  Jean-Marie Receveur ,  Thomas Hoegberg ,  Peter Aadal Nielsen ,  Jean-Michel Linget ,  Pia Karina Noeregaard ,  Anthony Murray ,  Emelie Bjurling

    Inventor： Martin Cooper ,  Jean-Marie Receveur ,  Thomas Hoegberg ,  Peter Aadal Nielsen ,  Jean-Michel Linget ,  Pia Karina Noeregaard ,  Anthony Murray ,  Emelie Bjurling

    IPC: A61K31/445 ,  C07D401/14

    CPC classification number: C07D231/12 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D409/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14

    Abstract: Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A1 is hydrogen, —COOH, or tetrazolyl; p and q are independently 0 or 1; A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; R4 and R5 are independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkoxy(C1-C4 alkyl)-, cycloalkyl, or fully or partially fluorinated C1-C4 alkyl; R1 (i) a bond; (ii) a divalent radical of formula —(CH2)aB1(CH2)b wherein a and b are independently O, 1, 2 or 3 provided that a+b is 1, 2 or 3, and B1 is —CO—, -0-, —S—, —SO—, —SO2—, —CH2—, —CHCH3—, —CHOH— or —NR7—; or (iii) a divalent radical selected from —C(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(R11)CH2—*, —C(R10)(R11)CH2—O—*, —CH2C(R10)(R11)—*, —CH2C(R10)(R11)—O—*, —CH2—O—C(R10)(R11)—* and —C(R10)(R11)—O—CH2—*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; Z is as defined in the specification; R10 is hydrogen and R11 is (C1-C3)alkyl or —OH; or R10 and R11 are both (C1-C3)alkyl; or R10 and R11 taken together with the carbon atom to which they are attached form a (C3-C5)cycloalkyl ring.

    Y4 selective receptor agonists for therapeutic interventions
    4.
    发明授权
    Y4 selective receptor agonists for therapeutic interventions 失效
    Y4选择性受体激动剂治疗干预

    公开(公告)号：US08022035B2

    公开(公告)日：2011-09-20

    申请号：US12067392

    申请日：2005-09-21

    Applicant: Thue Schwartz ,  Paul Brian Little ,  Lars-Ole Gerlach ,  Christian Elling

    Inventor： Thue Schwartz ,  Paul Brian Little ,  Lars-Ole Gerlach ,  Christian Elling

    IPC: A61K38/22 ,  C07K14/575

    CPC classification number: C07K14/5759 ,  A61K38/00

    Abstract: Y4 receptor agonist peptide selected from the group consisting of: [Ala30]PP2-36, [Thr30]PP2-36, [Asn30]PP2-36, [Gln30]PP2-36, [Glu10]PP2-36, [Glu10,Leu17,Thr30]PP2-36, [Nle17,Nle30]PP2-36, [Glu10,Nle17,Nle30]PP2-36, their PP1-36 equivalents, and analogues and derivatives thereof as described in the specification, are selective agonists of the Y4 receptor relative to the Y1 and Y2 receptors, and are useful in the treatment, for example, of obesity and overweight, and conditions in which these are considered contributory factors, and in the treatment of diarrhoea and intestinal hypersecretion.

    Abstract translation: Y3受体激动剂肽，其选自：[Ala30] PP2-36，[Thr30] PP2-36，[Asn30] PP2-36，[Gln30] PP2-36，[Glu10] PP2-36，[Glu10，Leu17 ，Thr30] PP2-36，[Nle17，Nle30] PP2-36，[Glu10，Nle17，Nle30] PP2-36，它们的PP1-36当量及其如本说明书所述的其类似物和衍生物是Y4的选择性激动剂 受体相对于Y1和Y2受体，并且可用于例如肥胖和超重的治疗，以及其被认为是促成因素的病症，以及用于治疗腹泻和肠分泌过多的症状。

    MEDICINAL USE OF RECEPTOR LIGANDS
    5.
    发明申请
    MEDICINAL USE OF RECEPTOR LIGANDS 审中-公开
    受体配体的药物使用

    公开(公告)号：US20090062317A1

    公开(公告)日：2009-03-05

    申请号：US11658307

    申请日：2005-07-05

    Applicant: Jean-Marie Receveur ,  Emelie Bjurling ,  Ann Christensen ,  Thomas Hoegberg

    Inventor： Jean-Marie Receveur ,  Emelie Bjurling ,  Ann Christensen ,  Thomas Hoegberg

    IPC: A61K31/517 ,  C07D401/12 ,  A61K31/454 ,  A61K31/4709

    CPC classification number: C07D401/12 ,  C07D239/72 ,  C07D405/14

    Abstract: Compounds of formula (I) are ligands of the melanin concentrating hormone-1 receptor (MCH-1R), useful in the treatment of diseases responsive to modulation of melanin concentrating hormone (MCH) activity, for example feeding disorders and diseases for which obesity is a risk factor (I): wherein ring B is selected from specific substituted phenyl or benz-fused 5 membered N-containing heterocycles defined in the specification; R, is attached to a ring carbon of ring B, and represents hydrogen, F, Cl, or —OCH3; X is ═CH— or ═N—; L, is —CH2— or —CH2CH2—; L2 is a bond, —CH2— or —CO—; R2 is H or C, —C3 alkyl, or —N(R2) L, —is selected from specific cyclic amino linker radicals as defined in the specification; ring A is selected from specific N-containing heterocyclic rings as defined in the specification.

    Abstract translation: 式（I）化合物是黑色素浓缩激素-1受体（MCH-1R）的配体，其可用于治疗对黑色素浓缩激素（MCH）活性的调节作用的疾病，例如喂食障碍和肥胖症 风险因子（I）：其中环B选自说明书中定义的特定取代的苯基或苯并稠合的5元N型杂环; R 2连接到环B的环碳上，代表氢，F，Cl或-OCH 3; X是-CH-或-N-; L，是-CH 2 - 或-CH 2 CH 2 - ; L 2是键，-CH 2 - 或-CO-; R2是H或C 1 -C 3烷基或-N（R 2）L - 选自如说明书中所定义的特定的环状氨基接头基团; 环A选自说明书中定义的特定的含N的杂环。

    CRTH2 receptor ligands for medicinal uses
    6.
    发明授权
    CRTH2 receptor ligands for medicinal uses 失效
    用于药用的CRTH2受体配体

    公开(公告)号：US08022063B2

    公开(公告)日：2011-09-20

    申请号：US11597873

    申请日：2005-05-30

    Applicant: Trond Ulven ,  Thomas Frimurer ,  Øystein Rist ,  Evi Kostenis ,  Thomas Högberg ,  Jean-Marie Receveur ,  Marie Grimstrup

    Inventor： Trond Ulven ,  Thomas Frimurer ,  Øystein Rist ,  Evi Kostenis ,  Thomas Högberg ,  Jean-Marie Receveur ,  Marie Grimstrup

    IPC: A01N43/00 ,  C07D231/00

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

    Abstract: 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.

    Abstract translation: 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 Medicinal Uses
    7.
    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

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

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

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

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

    Abstract: 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.

    Abstract translation: 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。

    Pseudo-sequence method for comparing 7tm receptors with respect to the physico-chemical properties of their binding sites
    8.
    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

    Applicant: Thomas Frimurer ,  Trond Ulven ,  Thomas Hogberg ,  Christian Elling

    Inventor： Thomas Frimurer ,  Trond Ulven ,  Thomas Hogberg ,  Christian Elling

    IPC: G06F19/00 ,  G06G7/48

    CPC classification number: G16B20/00 ,  G16B15/00

    Abstract: 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)

    Abstract translation: 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，

    Beta-arrestin based screening assays
    9.
    发明申请
    Beta-arrestin based screening assays 审中-公开
    基于β-arrestin的筛选试验

    公开(公告)号：US20060246507A1

    公开(公告)日：2006-11-02

    申请号：US10543349

    申请日：2004-01-20

    Applicant: Anders Heding

    Inventor： Anders Heding

    IPC: G01N33/53 ,  C12Q1/37

    CPC classification number: G01N33/74 ,  G01N2333/726

    Abstract: Use of mutated β-arrestin for an improved enzyme complementation assay or translocation assay, the improved enzyme complementation assay comprising: i) adding a substrate to a cell comprising a GPCR-EA fusion protein and a β-arrestin-EB fusion protein, wherein the β-arrestin is mutated, ii) adding a ligand to obtain, if possible, a GPCR-EA/β-arrestin-EB complex, and iii) measuring a signal arising from association of EA and EB to create an enzymatically active protein catalyzing conversion of the substrate which leads to a detectable signal, wherein the improvement leads to an increased signal compared with the signal obtained by use of the same process employing a β-arrestin-EB fusion protein, wherein the β-arrestin is wild type β-arrestin, and the improved β-arrestin translocation assay comprising i) providing a cell expressing a GPCR and comprising a β-arrestin associated with an optically detectable molecule, ODM, wherein the β-arrestin is mutated, ii) adding a ligand to obtain, if possible, a GPCR/β-arrestin complex, and iii) detecting a translocation of the optically detectable molecule, wherein the improvement leads to a increased and prolonged translocation of the β-arrestin associated with an optically detectable molecule as compared with the signal obtained by use of the same assay employing a β-arrestin associated with an optically detectable molecule, wherein the β-arrestin is wild type β-arrestin.

    Abstract translation: 使用突变的β-抑制蛋白进行改进的酶互补测定或易位测定，所述改进的酶互补测定法包括：i）向包含GPCR-EA融合蛋白和β-抑制蛋白-EB融合蛋白的细胞中加入底物，其中 β-阻滞蛋白被突变，ii）加入配体以获得GPCR-EA /β-抑制蛋白-EB复合物，并且iii）测量由EA和EB结合产生的信号以产生催化活性蛋白质催化转化 的底物，其导致可检测的信号，其中与通过使用使用β-抑制蛋白-EB融合蛋白的相同方法获得的信号相比，改善导致增加的信号，其中β-抑制蛋白是野生型β-抑制蛋白 和改进的β-抑制因子易位测定法，其包括i）提供表达GPCR并包含与光学可检测分子ODM相关的β-抑制蛋白的细胞，其中β-抑制蛋白被突变，ii） 如果可能，加入配体以获得GPCR /β-抑制蛋白复合物，和iii）检测光学可检测分子的易位，其中改善导致与光学可检测分子相关的β-抑制蛋白的增加和延长的易位 与通过使用与光学可检测分子相关的β-抑制蛋白的相同测定法获得的信号相比，其中β-抑制蛋白是野生型β-抑制蛋白。

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