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    Dihydroimidazo[2,1-b]thiazole and dihydro-5h-thiazolo[3,2-A]pyrimidines as antidepressant agents
    2.
    发明授权
    Dihydroimidazo[2,1-b]thiazole and dihydro-5h-thiazolo[3,2-A]pyrimidines as antidepressant agents 失效
    二氢咪唑并[2,1-b]噻唑和二氢-5H-噻唑并[3,2-A]嘧啶作为抗抑郁剂

    公开(公告)号：US06900216B2

    公开(公告)日：2005-05-31

    申请号：US10221459

    申请日：2001-03-10

    申请人： Kevin James Doyle ,  Frank Kerrigan ,  John Paul Watts

    发明人： Kevin James Doyle ,  Frank Kerrigan ,  John Paul Watts

    IPC分类号： A61K31/429 ,  A61K31/519 ,  A61P1/04 ,  A61P1/14 ,  A61P1/16 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P7/00 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/16 ,  A61P15/00 ,  A61P15/10 ,  A61P19/02 ,  A61P25/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/34 ,  A61P35/00 ,  A61P43/00 ,  C07D513/04

    CPC分类号： C07D513/04

    摘要： The present invention relates to certain novel substituted dihydroimidazo[2,1-b]thiazole and dihydro-5H-thiazolo[3,2-a]pyrimidine compounds including pharmaceutically acceptable salts thereof which have an affinity for 5-HT1A receptors and which inhibit neuronal reuptake of 5-hydroxytryptamine and/or noradrenaline, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of depression, anxiety, psychoses including schizophrenia, tardive dyskinesia, obesity, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders such as bulimia, anorexia, snaking and binge eating, non-insulin dependent diabetes mellitus, hyperglycaemia, hyperlipidaemia, stress, as an aid to smoking cessation and in the treatment and/or prophylaxis of seizures, neurological disorders such as epilepsy and/or in which there is neurological damage such as stroke, brain trauma, cerebral ischaemia, head injuries and haemorrhage.

    摘要翻译： 本发明涉及某些新的取代的二氢咪唑并[2,1-b]噻唑和二氢-5H-噻唑并[3,2-a]嘧啶化合物，其包括其对5-HT 1A具有亲和力的药学上可接受的盐， 并且其抑制5-羟色胺和/或去甲肾上腺素的神经元再摄取，其制备方法，含有它们的药物组合物及其用于治疗抑郁，焦虑，精神病，包括精神分裂症，迟发性运动障碍，肥胖症， 药物成瘾，药物滥用，认知障碍，阿尔茨海默病，强迫症，恐慌发作，社交恐怖症，进食障碍如贪食症，厌食症，sn食和暴饮暴食，非胰岛素依赖性糖尿病，高血糖症，高脂血症，压力等 帮助戒烟和治疗和/或预防癫痫发作，神经系统疾病如癫痫和/或其中存在神经损伤，如手指 e，脑创伤，脑缺血，头部损伤和出血。

    Tetrahydrofuro(3,2-B) pyrrol-3-one derivatives as inhibitors of cysteine proteinases
    3.
    发明授权
    Tetrahydrofuro(3,2-B) pyrrol-3-one derivatives as inhibitors of cysteine proteinases 有权
    四氢呋喃（3,2-B）吡咯-3-酮衍生物作为半胱氨酸蛋白酶的抑制剂

    公开(公告)号：US07799791B2

    公开(公告)日：2010-09-21

    申请号：US12319555

    申请日：2009-01-08

    申请人： Martin Quibell ,  John Paul Watts

    发明人： Martin Quibell ,  John Paul Watts

    IPC分类号： A61K31/427 ,  C07D491/04 ,  A61P19/10

    CPC分类号： C07D491/04

    摘要： A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; or R1 and R2 are both H; one of R3 and R4 is H, and the other is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; or R3 and R4 are joined together with the adjacent backbone carbon atom to form a spiro-C5-C6 cycloalkyl group; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl; or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; R8 is C1-8-alkyl or C3-8-cycloalkyl; R9 is a para-substituted 6-membered monocyclic aryl or heteroaryl ring which includes up to five heteroatoms. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.

    摘要翻译： 式（I）化合物或其药学上可接受的盐，水合物，复合物或前药，其中：R 1和R 2之一为H，另一个选自OR 6，SR 6，NR 6 R 7，N 3，Me，Et ，CF3，SOR8和SO2R8; 或R 1和R 2均为H; R3和R4之一是H，另一个选自叔丁基甲基，异丙基甲基，仲丁基，叔丁基，环戊基和环己基; 或者R 3和R 4与相邻的主链碳原子连接在一起形成螺C5-C6环烷基; R 6和R 7各自独立地选自H，C 1-8 - 烷基和C 3-8 - 环烷基; 或R 6和R 7与它们所连接的氮一起形成环状基团; R 8是C 1-8 - 烷基或C 3-8 - 环烷基; R9是包含至多5个杂原子的对位取代的6元单环芳基或杂芳基环。 本发明还涉及包含式（I）化合物的药物组合物，以及这些化合物在治疗选自骨质疏松症，佩吉特氏病，恰加斯病，疟疾，牙龈疾病，高钙血症，代谢性骨病，涉及 基质或软骨降解，以及骨癌症如骨转移和相关的疼痛。

    FURO[3. 2-B] PYRROL DERIVATIVES
    4.
    发明申请
    FURO[3. 2-B] PYRROL DERIVATIVES 有权
    FURO [3。 2-B]吡咯烷衍生物

    公开(公告)号：US20100216811A1

    公开(公告)日：2010-08-26

    申请号：US12773524

    申请日：2010-05-04

    申请人： Martin Quibell ,  John Paul Watts

    发明人： Martin Quibell ,  John Paul Watts

    IPC分类号： A61K31/497 ,  C12N5/02 ,  A61K31/454 ,  A61P35/00 ,  A61P19/08 ,  A61P19/10

    CPC分类号： C07D491/02

    摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R3 is tert-butylmethyl, sec-butyl or tert-butyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.

    摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐，其中：R3是叔丁基甲基，仲丁基或叔丁基; X是CH或N; 且R 4为任选取代的C 1-8烷基或任选取代的C 3-8环烷基。 本发明还涉及包含式（I）化合物的药物组合物，以及这些化合物在治疗选自骨质疏松症，佩吉特氏病，恰加斯病，疟疾，牙龈疾病，高钙血症，代谢性骨病，涉及 基质或软骨降解，以及骨癌症如骨转移和相关的疼痛。

    Tetrahydrofuro(3,2-B) pyrrol-3-one derivatives as inhibitors of cysteine proteinases
    5.
    发明申请
    Tetrahydrofuro(3,2-B) pyrrol-3-one derivatives as inhibitors of cysteine proteinases 有权
    四氢呋喃（3,2-B）吡咯-3-酮衍生物作为半胱氨酸蛋白酶的抑制剂

    公开(公告)号：US20090186831A1

    公开(公告)日：2009-07-23

    申请号：US12319555

    申请日：2009-01-08

    申请人： Martin Quibell ,  John Paul Watts

    发明人： Martin Quibell ,  John Paul Watts

    IPC分类号： A61K38/05 ,  C07D493/04 ,  C12N9/99 ,  C12Q1/37 ,  G01N33/573 ,  A61P19/02

    CPC分类号： C07D491/04

    摘要： A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; or R1 and R2 are both H; one of R3 and R4 is H, and the other is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; or R3 and R4 are joined together with the adjacent backbone carbon atom to form a spiro-C5-C6 cycloalkyl group; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl; or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; R8 is C1-8-alkyl or C3-8-cycloalkyl; R9 is a para-substituted 6-membered monocyclic aryl or heteroaryl ring which includes up to five heteroatoms. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.

    摘要翻译： 式（I）化合物或其药学上可接受的盐，水合物，复合物或前药，其中：R 1和R 2之一为H，另一个选自OR 6，SR 6，NR 6 R 7，N 3，Me，Et ，CF3，SOR8和SO2R8; 或R 1和R 2均为H; R3和R4之一是H，另一个选自叔丁基甲基，异丙基甲基，仲丁基，叔丁基，环戊基和环己基; 或者R 3和R 4与相邻的主链碳原子连接在一起形成螺C5-C6环烷基; R 6和R 7各自独立地选自H，C 1-8 - 烷基和C 3-8 - 环烷基; 或R 6和R 7与它们所连接的氮一起形成环状基团; R 8是C 1-8 - 烷基或C 3-8 - 环烷基; R9是包含至多5个杂原子的对位取代的6元单环芳基或杂芳基环。 本发明还涉及包含式（I）化合物的药物组合物，以及这些化合物在治疗选自骨质疏松症，佩吉特氏病，恰加斯病，疟疾，牙龈疾病，高钙血症，代谢性骨病，涉及 基质或软骨降解，以及骨癌症如骨转移和相关的疼痛。

    Tetrahydrofuro[3,2-b] pyrrol-3-one intermediates
    6.
    发明授权
    Tetrahydrofuro[3,2-b] pyrrol-3-one intermediates 有权
    四氢呋喃并[3,2-b]吡咯-3-酮中间体

    公开(公告)号：US08039641B2

    公开(公告)日：2011-10-18

    申请号：US12319562

    申请日：2009-01-08

    申请人： Martin Quibell ,  James Nally ,  Lee Patient ,  Yikang Wang ,  Claudio Dagostin ,  John Paul Watts

    发明人： Martin Quibell ,  James Nally ,  Lee Patient ,  Yikang Wang ,  Claudio Dagostin ,  John Paul Watts

    IPC分类号： C07D491/02

    CPC分类号： C07D493/04 ,  C07D307/28 ,  C07D491/04

    摘要： The present invention relates to a process for preparing a compound of formula (Ia), (Ib), (Ic) or (Id), or a pharmaceutically acceptable salt, hydrate, solvate, complex or prodrug thereof, said process comprising the steps of: (A) (i) treating a compound of formula (IVa), where R48 is alkyl or tosyl, with an oxidizing agent to form a compound of formula (Va); and (ii) converting said compound of formula (Va) to a compound of formula (Ia) or (Ic); or (B) (i) treating a compound of formula (IVb), where R48 is alkyl or tosyl, with an oxidizing agent to form a compound of formula (Vb); and (ii) converting said compound of formula (Vb) to a compound of formula (Ib) or (Id).

    摘要翻译： 本发明涉及制备式（Ia），（Ib），（Ic）或（Id）化合物或其药学上可接受的盐，水合物，溶剂化物，复合物或前药的方法，所述方法包括以下步骤： （A）（i）（i）用氧化剂处理其中R48为烷基或甲苯磺酰基的式（Ⅳa）化合物以形成式（Ⅴa）化合物; 和（ii）将所述式（Va）化合物转化为式（Ia）或（Ic）化合物; 或（B）（i）用氧化剂处理其中R48为烷基或甲苯磺酰基的式（Ⅳb）化合物以形成式（Ⅴb）化合物; 和（ii）将式（Vb）化合物转化为式（Ib）或（Id）化合物。

    Tetrahydrofuro[3,2-B] pyrrol-3-ones as cathepsin K inhibitors
    7.
    发明授权
    Tetrahydrofuro[3,2-B] pyrrol-3-ones as cathepsin K inhibitors 有权
    四氢呋喃并[3,2-B]吡咯-3-酮作为组织蛋白酶K抑制剂

    公开(公告)号：US07803803B2

    公开(公告)日：2010-09-28

    申请号：US12319564

    申请日：2009-01-08

    申请人： Martin Quibell ,  John Paul Watts

    发明人： Martin Quibell ,  John Paul Watts

    IPC分类号： A61K31/496 ,  A61K31/454 ,  C07D491/08 ,  C12Q1/37

    CPC分类号： C07D491/04

    摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: X is CH or N; one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; R3 is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl, or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; and R8 is C1-8-alkyl or C3-8-cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.

    摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐，其中：X是CH或N; R1和R2之一是H，另一个选自OR6，SR6，NR6R7，N3，Me，Et，CF3，SOR8和SO2R8; R 3选自叔丁基甲基，异丙基甲基，仲丁基，叔丁基，环戊基和环己基; R 4是任选取代的C 1-8烷基或任选取代的C 3-8环烷基; R 6和R 7各自独立地选自H，C 1-8 - 烷基和C 3-8 - 环烷基，或者R 6和R 7与它们所连接的氮一起形成环状基团; 并且R 8为C 1-8 - 烷基或C 3-8 - 环烷基。 本发明还涉及包含式（I）化合物的药物组合物，以及这些化合物在治疗选自骨质疏松症，佩吉特氏病，恰加斯病，疟疾，牙龈疾病，高钙血症，代谢性骨病，涉及 基质或软骨降解，以及骨癌症如骨转移和相关的疼痛。

    Furo[3,2-B]pyrrol-3-one derivatives and their use as cysteinyl proteinase inhibitors
    8.
    发明申请
    Furo[3,2-B]pyrrol-3-one derivatives and their use as cysteinyl proteinase inhibitors 失效
    呋喃并[3,2-B]吡咯-3-酮衍生物及其作为半胱氨酰蛋白酶抑制剂的用途

    公开(公告)号：US20090203714A1

    公开(公告)日：2009-08-13

    申请号：US12319556

    申请日：2009-01-08

    申请人： Martin Quibell ,  John Paul Watts

    发明人： Martin Quibell ,  John Paul Watts

    IPC分类号： A61K31/496 ,  C07D403/12 ,  C12N9/99 ,  A61P19/10 ,  A61P19/02 ,  A61P35/00 ,  C07D401/12 ,  A61K31/454 ,  G01N33/566 ,  A61P35/04 ,  A61P19/08

    CPC分类号： C07D491/04

    摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: X is CH or N; and R4 is optionally substituted C3-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.

    摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐，其中：X是CH或N; 并且R 4是任选取代的C 3-8烷基或任选取代的C 3-8环烷基。 本发明还涉及包含式（I）化合物的药物组合物，以及这些化合物在治疗选自骨质疏松症，佩吉特氏病，恰加斯病，疟疾，牙龈疾病，高钙血症，代谢性骨病，涉及 基质或软骨降解，以及骨癌症如骨转移和相关的疼痛。

    Tetrahdrofuro[3,2-B] pyrrol-3- one as cathepsin k inhibitors
    9.
    发明申请
    Tetrahdrofuro[3,2-B] pyrrol-3- one as cathepsin k inhibitors 有权
    作为组织蛋白酶k抑制剂的四氢呋喃并[3,2-B]吡咯-3-酮

    公开(公告)号：US20090197817A1

    公开(公告)日：2009-08-06

    申请号：US12319564

    申请日：2009-01-08

    申请人： Martin Quibell ,  John Paul Watts

    发明人： Martin Quibell ,  John Paul Watts

    IPC分类号： A61K38/05 ,  C07D487/04 ,  A61P31/04 ,  C12N9/99 ,  C12Q1/37 ,  G01N33/573

    CPC分类号： C07D491/04

    摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: X is CH or N; one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; R3 is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl, or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; and R8 is C1-8-alkyl or C3-8-cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.

    摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐，其中：X是CH或N; R1和R2之一是H，另一个选自OR6，SR6，NR6R7，N3，Me，Et，CF3，SOR8和SO2R8; R 3选自叔丁基甲基，异丙基甲基，仲丁基，叔丁基，环戊基和环己基; R 4是任选取代的C 1-8烷基或任选取代的C 3-8环烷基; R 6和R 7各自独立地选自H，C 1-8 - 烷基和C 3-8 - 环烷基，或者R 6和R 7与它们所连接的氮一起形成环状基团; 并且R 8为C 1-8 - 烷基或C 3-8 - 环烷基。 本发明还涉及包含式（I）化合物的药物组合物，以及这些化合物在治疗选自骨质疏松症，佩吉特氏病，恰加斯病，疟疾，牙龈疾病，高钙血症，代谢性骨病，涉及 基质或软骨降解，以及骨癌症如骨转移和相关的疼痛。