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1. 发明申请

US20110190260A1 NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES 有权
标题翻译：用于治疗衰老和炎症疾病的新型化合物
公开(公告)号：US20110190260A1
公开(公告)日：2011-08-04
申请号：US13055936
申请日：2009-07-24
申请人： Christel Jeanne Marie Menet , Nolwenn Jouannigot , Javier Blanc , Luc Juliaan Corina Van Rompaey , Stephen Robert Fletcher , Alastair James Hodges , Koen Kurt Smits
发明人： Christel Jeanne Marie Menet , Nolwenn Jouannigot , Javier Blanc , Luc Juliaan Corina Van Rompaey , Stephen Robert Fletcher , Alastair James Hodges , Koen Kurt Smits
IPC分类号： A61K31/541 , C07D471/04 , A61K31/437 , A61P19/08 , A61P19/10 , A61P37/00 , A61K31/497 , A61K31/5377 , A61P29/00 , A61K31/536 , A61P19/02 , A61P1/00 , A61P17/06 , A61P11/00 , A61P11/06
CPC分类号： A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/4995 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/551 , C07D471/04
摘要： [1,2,4]Triazolo[1,5-a]pyridine compounds are disclosed that have a formula represented by the formula (I). 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, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6, transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.
摘要翻译： [1,2,4]三唑并[1,5-a]吡啶化合物，其具有由式（I）表示的式。化合物可以制备成药物组合物，并且可以用于预防和治疗包括人在内的哺乳动物中的各种病症，包括作为非限制性实例，涉及软骨降解，骨和/或关节降解的疾病，用于例如骨关节炎; 和/或涉及炎症或免疫反应的疾病，例如克罗恩病，类风湿性关节炎，银屑病，过敏性气道疾病（例如哮喘，鼻炎），幼年特发性关节炎，结肠炎，炎性肠病，内毒素驱动的疾病状态（例如旁路并发症涉及慢性心脏衰竭的手术或慢性内毒素状态），涉及软骨周转损伤的疾病（例如涉及软骨细胞的合成代谢刺激的疾病），先天性软骨畸形，与IL6分泌过高有关的疾病，移植排斥反应（例如器官移植排斥）和增殖性疾病

2. 发明授权

US09415037B2 Compounds useful for the treatment of degenerative and inflammatory diseases 有权
标题翻译：可用于治疗退行性和炎性疾病的化合物
公开(公告)号：US09415037B2
公开(公告)日：2016-08-16
申请号：US14507396
申请日：2014-10-06
申请人： Christel Jeanne Marie Menet , Luc Juliaan Corina Van Rompaey , Stephen Robert Fletcher , Javier Blanc , Nolwenn Jouannigot , Alastair James Hodges , Koen Kurt Smits
发明人： Christel Jeanne Marie Menet , Luc Juliaan Corina Van Rompaey , Stephen Robert Fletcher , Javier Blanc , Nolwenn Jouannigot , Alastair James Hodges , Koen Kurt Smits
IPC分类号： A61K31/437 , C07D471/04 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551
CPC分类号： A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/4995 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/551 , C07D471/04
摘要： [1,2,4]triazolo[1,5-a]pyridine 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, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g. diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6 and transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.
摘要翻译： [1,2,4]三唑并[1,5-a]吡啶化合物，其具有下列化学式：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哺乳动物包括人的病症，包括非限制性实例，涉及软骨退化，骨和/或关节降解的疾病，例如骨关节炎; 和/或涉及炎症或免疫反应的疾病，例如克罗恩病，类风湿性关节炎，银屑病，过敏性气道疾病（例如哮喘，鼻炎），幼年特发性关节炎，结肠炎，炎性肠病，内毒素驱动的疾病状态（例如旁路并发症手术或慢性内毒素状态，例如慢性心力衰竭），涉及软骨周转损伤的疾病（例如涉及软骨细胞的合成代谢刺激的疾病），先天性软骨畸形，与IL6分泌过高有关的疾病和移植排斥反应（例如器官移植排斥），以及增殖性疾病

3. 发明授权

US08853240B2 Compounds useful for the treatment of degenerative and inflammatory diseases 有权
标题翻译：可用于治疗退行性和炎性疾病的化合物
公开(公告)号：US08853240B2
公开(公告)日：2014-10-07
申请号：US13055936
申请日：2009-07-24
申请人： Christel Jeanne Marie Menet , Nolwenn Jouannigot , Javier Blanc , Luc Juliaan Corina Van Rompaey , Stephen Robert Fletcher , Alastair James Hodges , Koen Kurt Smits
发明人： Christel Jeanne Marie Menet , Nolwenn Jouannigot , Javier Blanc , Luc Juliaan Corina Van Rompaey , Stephen Robert Fletcher , Alastair James Hodges , Koen Kurt Smits
IPC分类号： A61K31/437 , C07D471/04
CPC分类号： A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/4995 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/551 , C07D471/04
摘要： [1,2,4]triazolo[1,5-a]pyridine 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, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g. diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6 and transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.
摘要翻译： [1,2,4]三唑并[1,5-a]吡啶化合物，其具有下列化学式：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哺乳动物包括人的病症，包括非限制性实例，涉及软骨退化，骨和/或关节降解的疾病，例如骨关节炎; 和/或涉及炎症或免疫反应的疾病，例如克罗恩病，类风湿性关节炎，银屑病，过敏性气道疾病（例如哮喘，鼻炎），幼年特发性关节炎，结肠炎，炎性肠病，内毒素驱动的疾病状态（例如旁路并发症手术或慢性内毒素状态，例如慢性心脏衰竭），涉及软骨周转损伤的疾病（例如涉及软骨细胞的合成代谢刺激的疾病），先天性软骨畸形，与IL6分泌过高相关的疾病和移植排斥反应（例如器官移植排斥）和增殖性疾病

4. 发明授权

US09505754B2 Compound useful for the treatment of degenerative and inflammatory diseases 有权
标题翻译：可用于治疗退行性和炎性疾病的化合物
公开(公告)号：US09505754B2
公开(公告)日：2016-11-29
申请号：US14451127
申请日：2014-08-04
申请人： Christel Jeanne Marie Menet , Javier Blanc
发明人： Christel Jeanne Marie Menet , Javier Blanc
IPC分类号： C07D471/04 , A61K31/437 , A61K45/06
CPC分类号： C07D471/04 , A61K31/437 , A61K45/06
摘要： A compound is disclosed that has a formula represented by the following: This compound may be prepared as a pharmaceutical composition, 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, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.
摘要翻译：该化合物可以制备为药物组合物，并且可以用于预防和治疗包括人在内的哺乳动物中的各种病症，包括作为非限制性实例，炎性病症，自身免疫性疾病，增殖性疾病，移植排斥反应，涉及软骨周转损害，先天性软骨畸形和/或与IL6分泌过多相关的疾病的疾病。

5. 发明申请

US20100331359A1 NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES 有权
标题翻译：用于治疗衰老和炎症疾病的新型化合物
公开(公告)号：US20100331359A1
公开(公告)日：2010-12-30
申请号：US12823682
申请日：2010-06-25
申请人： Christel Jeanne Marie MENET , Javier Blanc
发明人： Christel Jeanne Marie MENET , Javier Blanc
IPC分类号： A61K31/437 , C07D471/04 , A61P19/02 , A61P29/00 , A61P37/06 , A61P35/00
CPC分类号： C07D471/04 , A61K31/437 , A61K45/06
摘要： A compound is disclosed that has a formula represented by the following: This compound may be prepared as a pharmaceutical composition, 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, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.
摘要翻译：公开了具有下列化学式的化合物：该化合物可以制备为药物组合物，并且可以用于预防和治疗哺乳动物包括人的各种病症，包括作为非限制性实例，炎性病症，自身免疫性疾病，增殖性疾病，移植排斥反应，涉及软骨周转损伤的疾病，先天性软骨畸形和/或与IL6分泌过多相关的疾病。

6. 发明授权

US10179771B2 Compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders 有权
公开(公告)号：US10179771B2
公开(公告)日：2019-01-15
申请号：US15262097
申请日：2016-09-12
申请人： Christel Jeanne Marie Menet , Oscar Mammoliti , Javier Blanc , Mislav Orsulic , Maja Roscic
发明人： Christel Jeanne Marie Menet , Oscar Mammoliti , Javier Blanc , Mislav Orsulic , Maja Roscic
IPC分类号： C07D235/08 , C07D401/14 , C07D401/12 , C07D405/12 , A61K31/4184 , A61K31/4439 , A61K31/5377 , A61K45/06 , C07D413/14
摘要： The present invention discloses compounds according to Formula I: wherein Cy, R1, L1, R3, R4, R5, La, and Ra are as defined herein. Novel benzimidazoles according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, 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, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.

7. 发明授权

US08242274B2 Triazolopyridine kinase inhibitors useful for the treatment of degenerative and inflammatory diseases 有权
标题翻译：用于治疗退行性和炎性疾病的三唑并吡啶激酶抑制剂
公开(公告)号：US08242274B2
公开(公告)日：2012-08-14
申请号：US12508950
申请日：2009-07-24
申请人： Christel Jeanne Marie Menet , Javier Blanc
发明人： Christel Jeanne Marie Menet , Javier Blanc
IPC分类号： A61K31/437 , C07D471/04
CPC分类号： A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/4995 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/551 , C07D471/04
摘要： A novel [1,2,4]triazolo[1,5-a]pyridine compound is disclosed that has a formula represented by the following: This compound may be prepared as a pharmaceutical composition, 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, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g. diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6 and transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.
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]吡啶化合物：该化合物可以制备成药物组合物，并可用于预防和治疗哺乳动物包括人的各种条件，包括非限制性实例，涉及软骨退化，骨和/或关节降解的疾病，例如骨关节炎; 和/或涉及炎症或免疫反应的疾病，例如克罗恩病，类风湿性关节炎，银屑病，过敏性气道疾病（例如哮喘，鼻炎），幼年特发性关节炎，结肠炎，炎性肠病，内毒素驱动的疾病状态（例如旁路并发症手术或慢性内毒素状态，例如慢性心脏衰竭），涉及软骨周转损伤的疾病（例如涉及软骨细胞的合成代谢刺激的疾病），先天性软骨畸形，与IL6分泌过高相关的疾病和移植排斥反应（例如器官移植排斥）和增殖性疾病

8. 发明申请

US20100029709A1 NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES 有权
标题翻译：用于治疗衰老和炎症疾病的新型化合物
公开(公告)号：US20100029709A1
公开(公告)日：2010-02-04
申请号：US12508950
申请日：2009-07-24
申请人： Christel Jeanne Marie Menet , Javier Blanc
发明人： Christel Jeanne Marie Menet , Javier Blanc
IPC分类号： A61K31/437 , C07D401/14 , A61P19/00 , A61P19/02 , A61P19/04 , A61P19/08 , A61P1/00 , A61P17/06 , A61P11/06 , A61P9/00 , A61P9/04 , A61P37/06 , A61P19/10
CPC分类号： A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/4995 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/551 , C07D471/04
摘要： A novel [1,2,4]triazolo[1,5-a]pyridine compound is disclosed that has a formula represented by the following: This compound may be prepared as a pharmaceutical composition, 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, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g. diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6 and transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.
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]吡啶化合物：该化合物可以制备成药物组合物，并可用于预防和治疗哺乳动物包括人的各种条件，包括非限制性实例，涉及软骨退化，骨和/或关节降解的疾病，例如骨关节炎; 和/或涉及炎症或免疫反应的疾病，例如克罗恩病，类风湿性关节炎，银屑病，过敏性气道疾病（例如哮喘，鼻炎），幼年特发性关节炎，结肠炎，炎性肠病，内毒素驱动的疾病状态（例如旁路并发症手术或慢性内毒素状态，例如慢性心脏衰竭），涉及软骨周转损伤的疾病（例如涉及软骨细胞的合成代谢刺激的疾病），先天性软骨畸形，与IL6分泌过高相关的疾病和移植排斥反应（例如器官移植排斥）和增殖性疾病

9. 发明授权

US08796457B2 Compound useful for the treatment of degenerative and inflammatory diseases 有权
标题翻译：可用于治疗退行性和炎性疾病的化合物
公开(公告)号：US08796457B2
公开(公告)日：2014-08-05
申请号：US12823682
申请日：2010-06-25
申请人： Christel Jeanne Marie Menet , Javier Blanc
发明人： Christel Jeanne Marie Menet , Javier Blanc
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K31/437 , A61K45/06
摘要： A compound is disclosed that has a formula represented by the following: This compound may be prepared as a pharmaceutical composition, 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, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.
摘要翻译：公开了具有下列化学式的化合物：该化合物可以制备为药物组合物，并且可以用于预防和治疗哺乳动物包括人的各种病症，包括作为非限制性实例，炎性病症，自身免疫性疾病，增殖性疾病，移植排斥反应，涉及软骨周转损伤的疾病，先天性软骨畸形和/或与IL6分泌过多相关的疾病。

10. 发明申请

US20100069607A1 METHOD OF COVALENTLY LINKING A CARBOHYDRATE OR POLYALKYLENE OXIDE TO A PEPTIDE, PRECURSORS FOR USE IN THE METHOD AND RESULTANT PRODUCTS 审中-公开
标题翻译：将碳水化合物或聚氧乙烯氧化物共价连接到肽上的方法和用于方法和成果产品的前体
公开(公告)号：US20100069607A1
公开(公告)日：2010-03-18
申请号：US12306885
申请日：2007-06-29
申请人： Derek MacMillan , Javier Blanc
发明人： Derek MacMillan , Javier Blanc
IPC分类号： C07K17/10 , C07K14/00 , C08B37/00 , C08H1/00
CPC分类号： C07H19/056 , C07K1/1077 , C07K9/001
摘要： A glycopeptide of the formula S-L-X—P, wherein: S is selected from an optionally protected monosaccharide, an optionally protected polysaccharide, a polyalkylene oxide chain and a group of the formula II, wherein R1 and R3 are independently selected from H or Ac, R4 is Ac, and R2 is a group of formula IV, wherein R7 and R8 are each independently selected from an optionally protected monosaccharide and an optionally protected polysaccharide, A, B, C and D are each independently 1 or 2, and m is 1 to 5; -L- is a moiety of the formula III wherein R5 and R6 are independently selected from H and Me and n is 1 to 3; and P is a peptide chain containing at least one amino acid having on its side chain the atom X, wherein X is an oxygen, a sulphur atom or a —CH2— moiety.
摘要翻译：式SLX-P的糖肽，其中：S选自任选保护的单糖，任选保护的多糖，聚环氧烷链和式II的基团，其中R 1和R 3独立地选自H或Ac，R 4 是Ac，R 2是式IV的基团，其中R 7和R 8各自独立地选自任选受保护的单糖和任选保护的多糖，A，B，C和D各自独立地为1或2，并且m为1至 5; -L-是式III的部分，其中R 5和R 6独立地选自H和Me，n是1至3; 并且P是含有至少一个氨基酸的肽链，其侧链具有原子X，其中X是氧，硫原子或-CH 2 - 部分。

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