公开(公告)号：US06936619B2

公开(公告)日：2005-08-30

申请号：US10387106

申请日：2003-03-12

申请人： Julian Blagg ,  Michael Jonathan Fray ,  Mark Llewellyn Lewis ,  John Paul Mathias ,  Mark Henryk Stefaniak ,  Alan Stobie

发明人： Julian Blagg ,  Michael Jonathan Fray ,  Mark Llewellyn Lewis ,  John Paul Mathias ,  Mark Henryk Stefaniak ,  Alan Stobie

IPC分类号： C07D239/95 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5386 ,  A61P3/06 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P15/00 ,  A61P15/08 ,  A61P15/10 ,  A61P27/06 ,  A61P43/00 ,  C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00

CPC分类号： C07D401/04 ,  C07D471/04 ,  C07D487/04

摘要： Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, wherein R1 represents C1-4 alkyl; R2 represents halo, C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyloxy, —SO2(C1-4 alkyl), optionally substituted C1-4 alkyloxy, Het or —OHet; R3 represents a bicyclic group of the formula  wherein X and Y are selected from C and N, provided that at least one is C; Ring A together with X and Y represents a 5- or 6-membered aromatic ring containing 0, 1, 2 or 3 nitrogen atoms in the ring; n is), 1 or 2 L represents a direct link, C1-4 alkylene or C1-4 alkoxyalkylene; R4 represents H, —NR5R6, C3-6 cycloalkyl, —OR7, Het1 or Het4; R5 and R6 are independently selected from H, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-4 alkylene, —SO2(C1-4 alkyl) and optionally substituted C1-4 alkyl R7 is selected from H, C1-4 alkyl, C1-4 alkoxyalkyl, C3-6cycloalkyl, Het2 and C1-4alkyl-Het3; R8 is H or C1-4 alkyl; Het, Het1, Het2 and Het3 independently represent an optionally substituted 4 to 7 membered saturated heterocyclic group which may be mono- or bi-cyclic and which contains one or more heteroatoms selected from N, O or S; Het4 represents an optionally substituted 5 or 6 membered unsaturated heterocyclic group containing one or more heteroatoms selected from N, O or S; R9 is H or C1-4 alkyl; R10 and R11 are independently selected from H and C1-4 alkyl; are useful in the treatment of hypertension, myocardial infarction, male erectile dysfunction (MED), hyperlipidaemia, cardiac arrhythmia, glaucoma and benign prostatic hyperplasia (BPH). They also find utility in the treatment of female sexual arousal dysfunction (FSAD).

公开(公告)号：US06417203B1

公开(公告)日：2002-07-09

申请号：US09662241

申请日：2000-09-14

申请人： Julian Blagg ,  Alan Daniel Brown ,  Elisabeth Colette Louise Gautier ,  Julian Duncan Smith ,  Andrew Brian McElroy

发明人： Julian Blagg ,  Alan Daniel Brown ,  Elisabeth Colette Louise Gautier ,  Julian Duncan Smith ,  Andrew Brian McElroy

IPC分类号： A61K314439

CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14

摘要： Compounds of formula (I): are antithrombotic agents, having utility in a variety of therapeutic areas including the prevention and/or treatment of deep vein thrombosis (DVT) after surgery, major medical illness, paralysis, malignancy, prolonged immobilisation trauma, application of lower limb plaster casts, or fractures of the lower limbs or pelvis; recurrent DVT; DVT during pregnancy when there is a previous history thereof; reocclusion following thrombolytic therapy; chronic arterial obstruction; peripheral vascular disease; acute myocardial infarction; unstable angina; atrial fibrillation; thrombotic stroke; transient ischaemic attacks; disseminated intravascular coagulation; coagulation in extra-corporeal circuits; occlusion of arterio-venous shunts and blood vessel grafts (including coronary artery by-pass grafts); and restenosis and occlusion following angioplasty.

摘要翻译： 式（I）化合物是抗血栓形成剂，可用于各种治疗领域，包括手术后预防和/或治疗深静脉血栓形成（DVT），主要医学疾病，麻痹，恶性肿瘤，长期固定创伤，应用 下肢石膏或下肢或骨盆骨折; 复发DVT; 怀孕期间DVT有先前的病史; 溶栓治疗后再闭塞; 慢性动脉阻塞; 周边血管疾病; 急性心肌梗塞; 不稳定型心绞痛; 房颤; 血栓性脑卒中 短暂性脑缺血发作; 弥散性血管内凝血; 额外体内循环中的凝血; 静脉分流和血管移植物（包括冠状动脉旁路移植物）的闭塞; 以及血管成形术后的再狭窄和闭塞。

公开(公告)号：US09169234B2

公开(公告)日：2015-10-27

申请号：US13501932

申请日：2010-10-14

申请人： Julian Blagg

发明人： Julian Blagg

IPC分类号： C07D209/14 ,  A61K31/4045 ,  C07D401/12 ,  C07D413/12 ,  C07D209/12 ,  C07D209/16 ,  C07D209/18

CPC分类号： C07D209/14 ,  C07C235/06 ,  C07C311/37 ,  C07C317/32 ,  C07D209/12 ,  C07D209/16 ,  C07D209/18 ,  C07D213/73 ,  C07D401/12 ,  C07D413/12

摘要： Disclosed herein are small molecule heterocyclic inhibitors of sepiapterin reductase (SPR), and prodrugs and pharmaceutically acceptable salts thereof. The Also featured are pharmaceutical compositions of the compounds and uses of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, and neuropathic pain).

摘要翻译： 本文公开了间苯二酚还原酶（SPR）的小分子杂环抑制剂及其前药和药学上可接受的盐。 还特征在于化合物的药物组合物和这些化合物用于治疗或预防疼痛（例如炎性疼痛，伤害性疼痛，功能性疼痛和神经性疼痛）的用途。

公开(公告)号：US20130345181A1

公开(公告)日：2013-12-26

申请号：US14004515

申请日：2012-03-14

申请人： Vassilios Bavetsias ,  Butrus Atrash ,  Sébastien Gaston André Naud ,  Peter William Sheldrake ,  Julian Blagg

发明人： Vassilios Bavetsias ,  Butrus Atrash ,  Sébastien Gaston André Naud ,  Peter William Sheldrake ,  Julian Blagg

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as “PPA derivatives”), particularly 1H-pyrrolo[3,2-c]pyridine-6-amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them. Formula (I)

摘要翻译： 本发明涉及某些吡咯并吡啶氨基衍生物（以下称为“PPA衍生物”），特别是1H-吡咯并[3,2-c]吡啶-6-氨基衍生物用于抑制单轴1的主轴检查点功能 Mps1 - 也称为TTK）激酶直接或间接通过与Mps激酶本身的相互作用。 特别地，本发明涉及用作治疗和/或预防增殖性疾病如癌症的治疗剂的PPA衍生物。 本发明还涉及制备PPA衍生物的方法和包含它们的药物组合物。 式（I）

公开(公告)号：US20120322800A1

公开(公告)日：2012-12-20

申请号：US13501932

申请日：2010-10-14

申请人： Julian Blagg

发明人： Julian Blagg

IPC分类号： A61K31/4045 ,  C07D413/12 ,  A61P29/00 ,  C07D401/12 ,  A61K31/4439 ,  A61K31/422 ,  C07D209/14 ,  A61K31/5377

CPC分类号： C07D209/14 ,  C07C235/06 ,  C07C311/37 ,  C07C317/32 ,  C07D209/12 ,  C07D209/16 ,  C07D209/18 ,  C07D213/73 ,  C07D401/12 ,  C07D413/12

摘要： Disclosed herein are small molecule heterocyclic inhibitors of sepiapterin reductase (SPR), and prodrugs and pharmaceutically acceptable salts thereof. The Also featured are pharmaceutical compositions of the compounds and uses of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, and neuropathic pain).

摘要翻译： 本文公开了间苯二酚还原酶（SPR）的小分子杂环抑制剂及其前药和药学上可接受的盐。 还特征在于化合物的药物组合物和这些化合物用于治疗或预防疼痛（例如炎性疼痛，伤害性疼痛，功能性疼痛和神经性疼痛）的用途。

公开(公告)号：US07928099B2

公开(公告)日：2011-04-19

申请号：US12532715

申请日：2008-03-14

申请人： Mark Andrews ,  Julian Blagg ,  Paul Brennan ,  Paul Fish ,  R. Ian Storer ,  Gavin Whitlock

发明人： Mark Andrews ,  Julian Blagg ,  Paul Brennan ,  Paul Fish ,  R. Ian Storer ,  Gavin Whitlock

IPC分类号： A61P15/00 ,  A61P25/00 ,  A61K31/55 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof wherein the variables R1, R2, R3a, R3b, R3b, R3d, and R100 are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a 5-HT2c receptor-mediated disorders with a compound of formula (I) or a pharmaceutical composition comprising a compound of formula (I).

摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐，其中变量R1，R2，R3a，R3b，R3b，R3d和R100如本文所定义。 本发明还涉及包含式（I）化合物的药物组合物和用式（I）化合物治疗5-HT 2C受体介导的病症的方法或包含式（I）化合物的药物组合物的方法。

公开(公告)号：US20100113422A1

公开(公告)日：2010-05-06

申请号：US12532715

申请日：2008-03-14

申请人： Mark Andrews ,  Julian Blagg ,  Paul Brennan ,  Paul Fish ,  R. Ian Storer ,  Gavin Whitlock

发明人： Mark Andrews ,  Julian Blagg ,  Paul Brennan ,  Paul Fish ,  R. Ian Storer ,  Gavin Whitlock

IPC分类号： A61K31/55 ,  C07D487/04 ,  A61P15/00 ,  A61P25/00

CPC分类号： C07D487/04

摘要： The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof wherein the variables R1, R2, R3a, R3b, R3b, R3d, and R100 are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a 5-HT2c receptor-mediated disorders with a compound of formula (I) or a pharmaceutical composition comprising a compound of formula (I).

摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐，其中变量R1，R2，R3a，R3b，R3b，R3d和R100如本文所定义。 本发明还涉及包含式（I）化合物的药物组合物和用式（I）化合物治疗5-HT 2C受体介导的病症的方法或包含式（I）化合物的药物组合物的方法。

公开(公告)号：US09371319B2

公开(公告)日：2016-06-21

申请号：US14004515

申请日：2012-03-14

申请人： Vassilios Bavetsias ,  Butrus Atrash ,  Sebastien Gaston Andre Naud ,  Peter William Sheldrake ,  Julian Blagg

发明人： Vassilios Bavetsias ,  Butrus Atrash ,  Sebastien Gaston Andre Naud ,  Peter William Sheldrake ,  Julian Blagg

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as “PPA derivatives”), particularly 1H-pyrrolo[3,2-c]pyridine-6-amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them. Formula (I)

摘要翻译： 本发明涉及某些吡咯并吡啶氨基衍生物（以下称为“PPA衍生物”），特别是1H-吡咯并[3,2-c]吡啶-6-氨基衍生物用于抑制单轴1的主轴检查点功能 Mps1 - 也称为TTK）激酶直接或间接通过与Mps激酶本身的相互作用。 特别地，本发明涉及用作治疗和/或预防增殖性疾病如癌症的治疗剂的PPA衍生物。 本发明还涉及制备PPA衍生物的方法和包含它们的药物组合物。 式（I）

公开(公告)号：US08778925B2

公开(公告)日：2014-07-15

申请号：US13122555

申请日：2009-10-06

申请人： Edward McDonald ,  Julian Blagg ,  Mark Pichowicz ,  Simon Ross Crumpler

发明人： Edward McDonald ,  Julian Blagg ,  Mark Pichowicz ,  Simon Ross Crumpler

IPC分类号： A01N43/00 ,  A61K31/00 ,  A61K31/55 ,  A01N43/42 ,  A61K31/44 ,  A01N43/38 ,  A61K31/40 ,  C07D225/04 ,  C07D223/14 ,  C07D487/00 ,  C07D491/00 ,  C07D513/00 ,  C07D215/00 ,  C07D217/00 ,  C07D219/00 ,  C07D221/00 ,  C07D209/96 ,  C07D495/00

CPC分类号： C07D471/10 ,  C07D213/74 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.

摘要翻译： 本发明涉及基于吡啶和嘧啶的化合物，包含这些化合物的药物组合物及其作为用于治疗和/或预防癌症的治疗剂的潜在用途。

公开(公告)号：US06949577B2

公开(公告)日：2005-09-27

申请号：US10390305

申请日：2003-03-17

申请人： Charlotte Moira Norfor Allerton ,  Julian Blagg ,  Mark Edward Bunnage ,  John Steele

发明人： Charlotte Moira Norfor Allerton ,  Julian Blagg ,  Mark Edward Bunnage ,  John Steele

IPC分类号： A61K31/00 ,  C07D233/54 ,  C07D233/64 ,  C07D401/06 ,  C07D403/12 ,  A61K31/4164

CPC分类号： C07D233/64 ,  A61K31/00 ,  C07D401/06 ,  C07D403/12

摘要： The present invention provides compounds of formula (I) as well as the use of such compounds in pharmaceutical compositions and methods of treatment. The compounds described herein represent a class of TAFIa inhibitors suitable for use in treating conditions such as thrombosis, atherosclerosis, adhesions, dermal scarring, cancer, fibrotic conditions, inflammatory diseases and those conditions which benefit from maintaining or enhancing bradykinin levels in the body.

摘要翻译： 本发明提供式（I）化合物以及这些化合物在药物组合物和治疗方法中的用途。 本文所述的化合物代表适合用于治疗诸如血栓形成，动脉粥样硬化，粘连，皮肤瘢痕形成，癌症，纤维化病症，炎性疾病以及从保持或增强体内缓激肽水平等方面受益的病症的一类TAFIa抑制剂。