公开(公告)号：US08435968B2

公开(公告)日：2013-05-07

申请号：US13063956

申请日：2009-09-18

申请人： Iain Robert Greig ,  Rose Mary Sheridan ,  Raymond Fisher ,  Matthew John Tozer ,  Juha Andrew Clase ,  Andrew Smith ,  Andrew Robert Tuffnell ,  Robert Jurgen Van 't Hof

发明人： Iain Robert Greig ,  Rose Mary Sheridan ,  Raymond Fisher ,  Matthew John Tozer ,  Juha Andrew Clase ,  Andrew Smith ,  Andrew Robert Tuffnell ,  Robert Jurgen Van 't Hof

IPC分类号： A61K31/69 ,  A61K31/18 ,  A61K31/505 ,  A61K31/5375 ,  A61K31/40 ,  C07D239/30 ,  C07D213/61 ,  C07D265/30 ,  C07D207/04

CPC分类号： A61K31/18 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/505 ,  C07C311/20 ,  C07C311/28 ,  C07C311/29 ,  C07D207/04 ,  C07D213/34 ,  C07D213/52 ,  C07D213/61 ,  C07D239/26 ,  C07D239/30 ,  C07D295/135

摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, Paget's disease and the like, etc.; and of cancer, such as a haematological malignancy, a solid tumour, etc. Formula (I).

摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及下列通式的某些芳基 - 苯基 - 亚磺酰氨基 - 环烷基化合物（在本文中统称为“APSAC化合物”）。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内在治疗例如炎症和/或关节破坏和/或骨丢失中的用途; 由免疫系统的过度和/或不适当和/或延长的激活介导的疾病; 炎性和自身免疫性疾病，例如类风湿性关节炎，牛皮癣，牛皮癣关节炎，慢性阻塞性肺病（COPD），动脉粥样硬化，炎性肠病，强直性脊柱炎等; 与骨丢失相关的疾病，例如与类风湿性关节炎中的过度破骨细胞活性相关的骨丢失，骨质疏松症，癌症相关的骨病，佩吉特氏病等; 和癌症，如血液恶性肿瘤，实体肿瘤等。式（I）。

公开(公告)号：US07893058B2

公开(公告)日：2011-02-22

申请号：US11803015

申请日：2007-05-11

申请人： Martin James Inglis Andrews ,  Paul Edwards ,  Philip Huxley ,  Wolfgang Schmidt ,  Veronique Birault ,  Mark Stuart Chambers ,  Clifford John Harris ,  Angus MacLeod ,  Kim Louise Hirst ,  Juha Andrew Clase ,  Gregory Bar

发明人： Martin James Inglis Andrews ,  Paul Edwards ,  Philip Huxley ,  Wolfgang Schmidt ,  Veronique Birault ,  Mark Stuart Chambers ,  Clifford John Harris ,  Angus MacLeod ,  Kim Louise Hirst ,  Juha Andrew Clase ,  Gregory Bar

IPC分类号： C07D487/04 ,  A61K31/4985

CPC分类号： C07D487/04

摘要： Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, arthritis, inflammation, and others.

摘要翻译： 公开了具有下列表示的式的新型咪唑并[1,2-a]吡嗪化合物：该化合物可以制备为药物组合物，并且可用于预防和治疗包括人在内的哺乳动物中的多种病症， 包括作为非限制性实例的关节炎，炎症等。

公开(公告)号：US08148369B2

公开(公告)日：2012-04-03

申请号：US12151585

申请日：2008-05-07

申请人： Martin James Inglis Andrews ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Giovanni Alessandro Tricarico ,  Grégory Louis Joseph Bar ,  Kim Louise Hirst ,  Olga Raquel Pinto Santos Oliveira Roussel ,  Juha Andrew Clase

发明人： Martin James Inglis Andrews ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Giovanni Alessandro Tricarico ,  Grégory Louis Joseph Bar ,  Kim Louise Hirst ,  Olga Raquel Pinto Santos Oliveira Roussel ,  Juha Andrew Clase

IPC分类号： A61K31/50 ,  A61K31/535 ,  C07D413/14 ,  C07D471/04

CPC分类号： C07D487/04

摘要： Novel fused pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammation, rheumatoid arthritis and others.

公开(公告)号：US20100298300A1

公开(公告)日：2010-11-25

申请号：US12399979

申请日：2009-03-08

申请人： Martin James Inglis Andrews ,  Paul Edwards ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Juha Andrew Clase ,  Gregory Bar ,  Kim Louise Hirst ,  Angus MacLeod

发明人： Martin James Inglis Andrews ,  Paul Edwards ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Juha Andrew Clase ,  Gregory Bar ,  Kim Louise Hirst ,  Angus MacLeod

IPC分类号： A61K31/551 ,  A61K31/5377 ,  A61K31/519 ,  C07D487/04 ,  C07D243/08 ,  A61P29/00 ,  A61P19/02 ,  A61P9/10 ,  A61P9/00

CPC分类号： C07D487/04

摘要： Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, and others.

摘要翻译： 公开了具有下列化学式的新型[1.2.4]三唑并[1,5-a]吡嗪化合物：该化合物可以制备成药物组合物，并可用于预防和治疗各种病症 在包括人的哺乳动物中，包括作为非限制性实例的疼痛，炎症等。

公开(公告)号：US20120232075A1

公开(公告)日：2012-09-13

申请号：US13411450

申请日：2012-03-02

申请人： Martin James Inglis Andrews ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Giovanni Alessandro Tricarico ,  Grégory Louis Joseph Bar ,  Kim Louise Hirst ,  Olga Raquel Pinto Santos Oliveira Roussel ,  Juha Andrew Clase

发明人： Martin James Inglis Andrews ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Giovanni Alessandro Tricarico ,  Grégory Louis Joseph Bar ,  Kim Louise Hirst ,  Olga Raquel Pinto Santos Oliveira Roussel ,  Juha Andrew Clase

IPC分类号： A61K31/4985 ,  A61K31/5377 ,  A61P29/00 ,  A61P19/02 ,  A61P19/10 ,  A61P19/04 ,  A61P1/02 ,  A61P35/04 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P1/16 ,  A61P9/10 ,  A61P9/04 ,  A61P25/00 ,  C07D487/04

CPC分类号： C07D487/04

摘要： Novel fused pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammation, rheumatoid arthritis and others.

摘要翻译： 公开了具有下列表示的式的新型稠合吡嗪化合物：该化合物可以制备成药物组合物，并且可用于预防和治疗包括人在内的哺乳动物中的各种病症，包括以非限制性方式 例如炎症，类风湿关节炎等。

公开(公告)号：US08207167B2

公开(公告)日：2012-06-26

申请号：US13063950

申请日：2009-09-18

申请人： Iain Robert Greig ,  Rose Mary Sheridan ,  Raymond Fisher ,  Matthew John Tozer ,  Juha Andrew Clase ,  Andrew Smith ,  Andrew Robert Tuffnell ,  Robert Jurgen Van 't Hof

发明人： Iain Robert Greig ,  Rose Mary Sheridan ,  Raymond Fisher ,  Matthew John Tozer ,  Juha Andrew Clase ,  Andrew Smith ,  Andrew Robert Tuffnell ,  Robert Jurgen Van 't Hof

IPC分类号： A61K31/5375 ,  A61K31/18 ,  C07D265/30 ,  C07C311/01

CPC分类号： C07D303/36 ,  C07C311/21 ,  C07C311/39 ,  C07C2601/02 ,  C07D239/26 ,  C07D239/30 ,  C07D263/20 ,  C07D295/135

摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-phenylene compounds of the following formula (I) (collectively referred to herein as “APSAP compounds”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, Paget's disease and the like, etc.; and of cancer, such as a haematological malignancy, a solid tumor, etc.

摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及下列通式（I）的某些芳基 - 苯基 - 亚磺酰氨基 - 亚苯基化合物（本文统称为“APSAP化合物”）。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内在治疗例如炎症和/或关节破坏和/或骨丢失中的用途; 由免疫系统的过度和/或不适当和/或延长的激活介导的疾病; 炎性和自身免疫性疾病，例如类风湿性关节炎，牛皮癣，牛皮癣关节炎，慢性阻塞性肺病（COPD），动脉粥样硬化，炎性肠病，强直性脊柱炎等; 与骨丢失相关的疾病，例如与类风湿性关节炎中的过度破骨细胞活性相关的骨丢失，骨质疏松症，癌症相关的骨病，佩吉特氏病等; 和癌症，如血液恶性肿瘤，实体瘤等。

公开(公告)号：US07915256B2

公开(公告)日：2011-03-29

申请号：US12399979

申请日：2009-03-08

申请人： Martin James Inglis Andrews ,  Paul Edwards ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Juha Andrew Clase ,  Gregory Bar ,  Kim Louise Hirst ,  Angus MacLeod

发明人： Martin James Inglis Andrews ,  Paul Edwards ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Juha Andrew Clase ,  Gregory Bar ,  Kim Louise Hirst ,  Angus MacLeod

IPC分类号： C07D403/12 ,  A61K31/506

CPC分类号： C07D487/04

摘要： Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, and others.

摘要翻译： 公开了具有下列化学式的新型[1.2.4]三唑并[1,5-a]吡嗪化合物：该化合物可以制备成药物组合物，并可用于预防和治疗各种病症 在包括人的哺乳动物中，包括作为非限制性实例的疼痛，炎症等。

公开(公告)号：US07501411B2

公开(公告)日：2009-03-10

申请号：US11809294

申请日：2007-05-30

申请人： Martin James Inglis Andrews ,  Paul Edwards ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Juha Andrew Clase ,  Gregory Bar ,  Kim Louise Hirst ,  Angus MacLeod

发明人： Martin James Inglis Andrews ,  Paul Edwards ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Juha Andrew Clase ,  Gregory Bar ,  Kim Louise Hirst ,  Angus MacLeod

IPC分类号： C07D487/04 ,  A61K31/4985

CPC分类号： C07D487/04

摘要： Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, and others.

摘要翻译： 公开了具有下列化学式的新型[1.2.4]三唑并[1,5-a]吡嗪化合物：该化合物可以制备成药物组合物，并可用于预防和治疗各种病症 在包括人的哺乳动物中，包括作为非限制性实例的疼痛，炎症等。

公开(公告)号：US20130245018A1

公开(公告)日：2013-09-19

申请号：US13886799

申请日：2013-05-03

申请人： Iain Robert Greig ,  Rose Mary Sheridan ,  Raymond Fisher ,  Matthew John Tozer ,  Juha Andrew Clase ,  Andrew Smith ,  Andrew Robert Tuffnell ,  Robert Jurgen Van 't Hof

发明人： Iain Robert Greig ,  Rose Mary Sheridan ,  Raymond Fisher ,  Matthew John Tozer ,  Juha Andrew Clase ,  Andrew Smith ,  Andrew Robert Tuffnell ,  Robert Jurgen Van 't Hof

IPC分类号： C07C311/20 ,  C07D239/26 ,  C07D213/61 ,  C07D239/30 ,  C07D207/04 ,  C07D295/135

CPC分类号： A61K31/18 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/505 ,  C07C311/20 ,  C07C311/28 ,  C07C311/29 ,  C07D207/04 ,  C07D213/34 ,  C07D213/52 ,  C07D213/61 ,  C07D239/26 ,  C07D239/30 ,  C07D295/135

摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, Paget's disease and the like, etc.; and of cancer, such as a haematological malignancy, a solid tumour, etc.

摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及下列通式的某些芳基 - 苯基 - 亚磺酰氨基 - 环烷基化合物（在本文中统称为“APSAC化合物”）。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内在治疗例如炎症和/或关节破坏和/或骨丢失中的用途; 由免疫系统的过度和/或不适当和/或延长的激活介导的疾病; 炎性和自身免疫性疾病，例如类风湿性关节炎，牛皮癣，牛皮癣关节炎，慢性阻塞性肺病（COPD），动脉粥样硬化，炎性肠病，强直性脊柱炎等; 与骨丢失相关的疾病，例如与类风湿性关节炎中的过度破骨细胞活性相关的骨丢失，骨质疏松症，癌症相关的骨病，佩吉特氏病等; 和癌症，如血液恶性肿瘤，实体瘤等。

公开(公告)号：US08178530B2

公开(公告)日：2012-05-15

申请号：US12970632

申请日：2010-12-16

申请人： Martin James Inglis Andrews ,  Paul Edwards ,  Reginald Christophe Xavier Brys ,  Philip Huxley ,  Wolfgang Schmidt ,  Veronique Birault ,  Mark Stuart Chambers ,  Clifford John Harris ,  Angus MacLeod ,  Kim Louise Hirst ,  Juha Andrew Clase ,  Gregory Bar

发明人： Martin James Inglis Andrews ,  Paul Edwards ,  Reginald Christophe Xavier Brys ,  Philip Huxley ,  Wolfgang Schmidt ,  Veronique Birault ,  Mark Stuart Chambers ,  Clifford John Harris ,  Angus MacLeod ,  Kim Louise Hirst ,  Juha Andrew Clase ,  Gregory Bar

IPC分类号： C07D487/04 ,  A61K31/4985

CPC分类号： C07D487/04

摘要： Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, arthritis, inflammation, and others.