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    2-aminoquinoline derivatives having d4-agonistic activity
    2.
    发明授权
    2-aminoquinoline derivatives having d4-agonistic activity 有权
    具有d4-激动活性的2-氨基喹啉衍生物

    公开(公告)号：US06281216B1

    公开(公告)日：2001-08-28

    申请号：US09601765

    申请日：2000-10-23

    申请人： Jacobus A. J. Den Hartog ,  Gerben M. Visser ,  Bartholomeus J. Van Steen ,  Martinus T. M. Tulp ,  Eric Ronken ,  Cornelis G. Kruse

    发明人： Jacobus A. J. Den Hartog ,  Gerben M. Visser ,  Bartholomeus J. Van Steen ,  Martinus T. M. Tulp ,  Eric Ronken ,  Cornelis G. Kruse

    IPC分类号： A61K31496

    CPC分类号： C07D215/38 ,  C07D401/12 ,  C07D405/12

    摘要： The present invention relates to a group of novel 2-aminoquinoline derivatives which are potent and selective agonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 1 or 2 substituents, which can be the same or different, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C1-2)amino, or two groups R1 at adjacent carbon atoms together with the benzene ring may form the benzdioxane group or benzofuran group, X represents nitrogen or carbon, and the dotted line may represent a double bond, (R2)p represents 0, 1 or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R2)p is a methylene bridge or ethylene bridge, R3 is hydrogen or methyl, and (R)m represents 0, 1, or 2 substituents, which can be the same or different and can be located at all available positions of the quinolyl group, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C1-2)amino, on the understanding that R1 cannot represent o-OCH3 when X is nitrogen, (R2)p and R3 are hydrogen, m is 0 and n is 1

    摘要翻译： 本发明涉及一组新的2-氨基喹啉衍生物，其是多巴胺D4-受体的有效和选择性激动剂。 化合物具有通式（I），其中（R1）n表示1或2个可以相同或不同的取代基，可以是C1-3 - 烷基或烷氧基，卤素，三氟甲基，硝基，氨基和单 - 或 二烷基（C1-2）氨基或相邻碳原子上的两个基团R 1与苯环可以形成苯并二恶烷基或苯并呋喃基，X代表氮或碳，虚线可以表示双键，（R2）p 代表0,1或2个与甲基和乙基基团相同或不同的取代基，或（R2）p是亚甲基桥或乙烯桥，R3是氢或甲基，（R）m表示0， 1或2个取代基，其可以相同或不同，并且可以位于喹啉基的所有可用位置，C 1-3 - 烷基或烷氧基，卤素，三氟甲基，硝基，氨基和单 - 或二烷基 （C1-2）氨基，可以理解，当X是氮时，R1不能表示o-OCH3，（R2）p和R3是氢，m是0，而ni s 1

    Benzisoxazole derivatives having d4-antagonistic activity
    3.
    发明授权
    Benzisoxazole derivatives having d4-antagonistic activity 有权
    具有d4拮抗活性的苯并异恶唑衍生物

    公开(公告)号：US06335326B1

    公开(公告)日：2002-01-01

    申请号：US09601795

    申请日：2000-10-23

    申请人： Jacobus A. J. Den Hartog ,  Gerben M. Visser ,  Bartholomeus J. Van Steen ,  Martinus T. M. Tulp ,  Eric Ronken ,  Cornelis G. Kruse ,  Josephus H. M. Lange

    发明人： Jacobus A. J. Den Hartog ,  Gerben M. Visser ,  Bartholomeus J. Van Steen ,  Martinus T. M. Tulp ,  Eric Ronken ,  Cornelis G. Kruse ,  Josephus H. M. Lange

    IPC分类号： A01N4346

    CPC分类号： C07D413/14

    摘要： The present invention relates to a group of novel benzisoxazole derivatives which are potent and selective antagonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 0, 1, or 2 substituents, which can be the same or different, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino mono- or dialkyl (C1-2)-amino, sulfonyl-(C1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1-2)-amino, X is O, S, NH or NCH3, Y represents CH2, or (CH2)2, (R2)m represents 0, 1, or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R2)m is a methylene bridge or ethylene bridge, A is a group —CH2—(CRH)p— wherein R is hydrogen or methyl and p is 0 or 1, and B represents 2- or 3-indolyl or 2-benzimidazolyl, which groups may be substituted at carbon with 1 or 2 substituents from the group C-1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, mono- or dialkyl (C1-2)amino, sulfonyl-(C1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1-2)-amino.

    摘要翻译： 本发明涉及一组新的苯并异恶唑衍生物，其是多巴胺D4受体的有效和选择性拮抗剂。 化合物具有通式（I），其中（R1）n表示0,1或2个可以相同或不同的取代基，可以是C1-3 - 烷基或烷氧基，卤素，三氟甲基，硝基， 或二烷基（C1-2） - 氨基，磺酰基 - （C1-3）烷基或 - 烷氧基，磺酰基三氟甲基，磺酰基氨基和磺酰基单 - 或二烷基（C1-2） - 氨基，X是O，S，NH或 NCH 3，Y表示CH 2或（CH 2）2，（R 2）m表示0,1或2个与甲基和乙基基团相同或不同的取代基，或（R2）m是亚甲基桥或 乙基桥，A是-CH 2 - （CRH）p - 基团，其中R是氢或甲基，p是0或1，B表示2-或3-吲哚基或2-苯并咪唑基，该基团可以在碳上被取代， 1或2个C 1-3 - 烷基或烷氧基，卤素，三氟甲基，硝基，氨基，一或二烷基（C 1-2）氨基，磺酰基 - （C 1-3）烷基或 - 烷氧基，磺酰基三氟甲基 ，磺酰基氨基和磺酰基单或二烷基（C 1-2） - 氨基。

    (THIO)MORPHOLINE DERIVATIVES AS S1P MODULATORS
    4.
    发明申请
    (THIO)MORPHOLINE DERIVATIVES AS S1P MODULATORS 有权

    公开(公告)号：US20120220552A1

    公开(公告)日：2012-08-30

    申请号：US13393497

    申请日：2010-08-27

    申请人： Wouter I. Iwema Bakker ,  Hein K.A.C. Coolen ,  Axel Stoit ,  Harmen Mons ,  Eric Ronken ,  Elizabeth Van Der Kam ,  Jurjen Frankena

    发明人： Wouter I. Iwema Bakker ,  Hein K.A.C. Coolen ,  Axel Stoit ,  Harmen Mons ,  Eric Ronken ,  Elizabeth Van Der Kam ,  Jurjen Frankena

    IPC分类号： A61K31/5375 ,  C07D413/10 ,  A61K31/5377 ,  C07F9/6533 ,  A61P25/24 ,  C07D279/12 ,  A61K31/54 ,  A61P25/00 ,  A61P25/28 ,  C07D265/30 ,  A61K31/675

    CPC分类号： C07D295/15 ,  C07D265/30 ,  C07D265/32 ,  C07D279/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07F9/6533

    摘要： The present disclosure relates to (thio)morpholine derivatives of the formula (I) wherein R1 is selected from cyano, (2-4C)alkynyl, (1-4C)alkyl, (3-6C)cycloalkyl, (4-6C)cycloalkenyl, (6-8C)bicycloalkyl, (8-10C)bicyclic group, each optionally substituted with (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (2-4C)alkynyl, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino, —SO2-(1-4C)alkyl, —CO-(1-4C)alkyl, —CO—O-(1-4C)alkyl, —NH—CO-(1-4C)alkyl and (3-6C)cycloalkyl, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl, monocyclic heterocycle optionally substituted with halogen, (1-4C)alkyl or with phenyl optionally substituted with (1-4C)alkyl, and bicyclic heterocycle optionally substituted with (1-4C)alkyl; A is selected from —CO—O—, —O—CO—, —NH—CO—, —CO—NH, —C═C—, —CCH3—O— and the linking group —Y—(CH2)n—X— wherein Y is attached to R1 and selected from a bond, —O—, —S—, —SO—, —SO2—, —CH2—O—, —CO—, —O—CO—, —CO—O—, —CO—NH—, —NH—CO—, —C═C— and —C≡C—; n is an integer from 1 to 10; and X is attached to the phenylene/pyridyl group and selected from a bond, —O—, —S—, —SO—, —SO2—, —NH, —CO—, —C═C— and —C≡C—; ring structure B optionally contains one nitrogen atom; R2 is H, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, or halogen; and R3 is (1-4C)alkylene-R5 wherein the alkylene group may be substituted with (CH2)2 to form a cyclopropyl moiety or one or two halogen atoms, or R3 is (3-6C)cycloalkylene-R5 or —CO—CH2—R5, wherein R5 is —OH, —PO3H2, —OPO3H2, —COOH, —COO(1-4C)alkyl or tetrazol-5-yl; R4 is H or (1-4C)alkyl; R6 is one or more substituents independently selected from H, (1-4C)alkyl or oxo; W is —O—, —S—, —SO— or —SO2—; or a pharmaceutically acceptable salt, a solvate or hydrate thereof; with the proviso that the derivative of formula (I) is not 2-(4-ethylphenyl)-4-morpholinoethanol or 4-[4-(2-hydroxyethyl)-2-morpholinyl]benzeneacetonitrile or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the disclosure have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of S1P receptor mediated diseases and conditions.