公开(公告)号：US09750720B2

公开(公告)日：2017-09-05

申请号：US15359120

申请日：2016-11-22

申请人： Novassay S.A.

发明人： Premji Meghani ,  Franz Kricek

IPC分类号： A61K31/41 ,  A61K31/4245 ,  C07D257/04 ,  C07D271/07 ,  C07C259/14 ,  C07C205/50 ,  C07C233/10 ,  C07C255/31

CPC分类号： A61K31/41 ,  A61K31/4245 ,  C07B2200/07 ,  C07C205/50 ,  C07C233/10 ,  C07C255/31 ,  C07C259/14 ,  C07C2602/20 ,  C07D257/04 ,  C07D271/07

摘要： A compound of Formula 1 wherein R1 represents hydrogen, halo, a C1-C4 alkyl group, a C1-C4 alkylhalide group, a C1-C4 alkoxy-C2-C4 alkyl group, a C2-C4 alkenyl group, a C2-C4 alkynyl group or a C3-C7 cycloalkyl group; R2 represents or a tautomer thereof; and R3 represents hydrogen, a C1-C4 alkyl group, a C1-C4 alkoxy-C2-C4 alkyl group or a C3-C7 cycloalkyl group; or a pharmaceutically acceptable salt or solvate thereof. Processes to prepare said compounds and novel intermediates are also claimed. Such compound finds utility in treating neuropathic pain and disorders of the central nervous system.

公开(公告)号：US09266846B2

公开(公告)日：2016-02-23

申请号：US14474566

申请日：2014-09-02

申请人： Lantheus Medical Imaging, Inc.

发明人： Richard R. Cesati ,  Thomas D. Harris ,  Simon P. Robinson ,  Richard J. Looby ,  Edward H. Cheesman ,  Padmaja Yalamanchili ,  David S. Casebier

IPC分类号： C07D257/02 ,  C07D209/20 ,  A61K49/10 ,  A61K51/04 ,  C07C259/14 ,  C07C271/22 ,  C07D213/56 ,  C07D403/12 ,  C07C53/18 ,  C07C259/06

CPC分类号： C07D257/02 ,  A61K49/103 ,  A61K49/106 ,  A61K51/04 ,  C07C53/18 ,  C07C259/06 ,  C07C259/14 ,  C07C271/22 ,  C07C2601/14 ,  C07D209/20 ,  C07D213/56 ,  C07D403/12

摘要： The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.

公开(公告)号：US08852553B2

公开(公告)日：2014-10-07

申请号：US13723333

申请日：2012-12-21

申请人： Lantheus Medical Imaging, Inc.

发明人： Richard R. Cesati ,  Thomas D. Harris ,  Simon P. Robinson ,  Richard J. Looby ,  Edward H. Cheesman ,  Padmaja Yalamanchili ,  David S. Casebier

IPC分类号： A61K49/00 ,  A61K49/04 ,  A61K51/04 ,  C07C271/22 ,  C07D403/12 ,  C07C259/14 ,  C07D257/02 ,  C07D213/56 ,  C07D209/20 ,  A61K49/10

CPC分类号： C07D257/02 ,  A61K49/103 ,  A61K49/106 ,  A61K51/04 ,  C07C53/18 ,  C07C259/06 ,  C07C259/14 ,  C07C271/22 ,  C07C2601/14 ,  C07D209/20 ,  C07D213/56 ,  C07D403/12

摘要： The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.

摘要翻译： 本公开涉及化合物，诊断剂和相关方法。 在某些情况下，提供了治疗患者的方法。 更具体地，本公开提供了用于检测和/或成像和/或监测富含弹性蛋白的组织的化合物，诊断剂和试剂盒。 此外，本公开提供了检测和/或成像和/或监测冠状动脉斑块，颈动脉斑块，髂骨/股骨斑块，主动脉斑块，肾动脉斑块，任何动脉血管的斑块，动脉瘤，血管炎，其他疾病的存在的方法 的动脉壁，和/或韧带，子宫，肺或皮肤的损伤或结构变化，如总血管壁面积，内腔大小和外动脉周长的变化所示。

公开(公告)号：US08530453B2

公开(公告)日：2013-09-10

申请号：US12924214

申请日：2010-09-23

申请人： Irving Sucholeiki

发明人： Irving Sucholeiki

IPC分类号： A01N37/18 ,  A01N43/40 ,  A61K31/65 ,  A61K31/44 ,  C07D209/00

CPC分类号： A61K31/65 ,  A61K31/343 ,  A61K31/38 ,  A61K31/4035 ,  A61K31/405 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/45 ,  C07C235/82 ,  C07C237/26 ,  C07C259/14 ,  C07C317/44 ,  C07C323/52 ,  C07D207/337 ,  C07D209/18 ,  C07D209/48 ,  C07D213/79 ,  C07D233/76 ,  C07D235/22 ,  C07D235/24 ,  C07D307/85 ,  C07D309/08

摘要： The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.

摘要翻译： 本发明一般涉及药剂，尤其涉及金属蛋白酶抑制剂化合物。 更具体地说，本发明提供了一类新的双作用MMP-2和MMP-9抑制化合物，其相对于目前已知的用于治疗的MMP-2和MMP-9抑制剂表现出增加的效力，代谢稳定性和/或降低的毒性 的疼痛等疾病。 另外，本发明涉及用于治疗患者的疼痛，成瘾和/或戒断症状的方法，包括向患者施用减少疼痛的有效量的本发明化合物。

公开(公告)号：US08361438B2

公开(公告)日：2013-01-29

申请号：US12350628

申请日：2009-01-08

申请人： Richard R. Cesati ,  Thomas D. Harris ,  Simon P. Robinson ,  Richard J. Looby ,  Edward H. Cheesman ,  Padmaja Yalamanchili ,  David S. Casebier

发明人： Richard R. Cesati ,  Thomas D. Harris ,  Simon P. Robinson ,  Richard J. Looby ,  Edward H. Cheesman ,  Padmaja Yalamanchili ,  David S. Casebier

IPC分类号： A61K49/00 ,  A61K49/04

CPC分类号： C07D257/02 ,  A61K49/103 ,  A61K49/106 ,  A61K51/04 ,  C07C53/18 ,  C07C259/06 ,  C07C259/14 ,  C07C271/22 ,  C07C2601/14 ,  C07D209/20 ,  C07D213/56 ,  C07D403/12

摘要： The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.

摘要翻译： 本公开涉及化合物，诊断剂和相关方法。 在某些情况下，提供了治疗患者的方法。 更具体地，本公开提供了用于检测和/或成像和/或监测富含弹性蛋白的组织的化合物，诊断剂和试剂盒。 此外，本公开提供了检测和/或成像和/或监测冠状动脉斑块，颈动脉斑块，髂骨/股骨斑块，主动脉斑块，肾动脉斑块，任何动脉血管的斑块，动脉瘤，血管炎，其他疾病的存在的方法 的动脉壁，和/或韧带，子宫，肺或皮肤的损伤或结构变化，如总血管壁面积，内腔大小和外动脉周长的变化所示。

公开(公告)号：US20100304966A1

公开(公告)日：2010-12-02

申请号：US12739606

申请日：2008-10-09

申请人： Joachim Rheinheimer ,  Barbara Nave ,  Doris Kremzow ,  Stefan Redlich ,  Christian Pilger ,  Claudia Rosenbaum ,  Wassilios Grammenos

发明人： Joachim Rheinheimer ,  Barbara Nave ,  Doris Kremzow ,  Stefan Redlich ,  Christian Pilger ,  Claudia Rosenbaum ,  Wassilios Grammenos

IPC分类号： A01N43/56 ,  C07D231/12 ,  C07D249/08 ,  A01N43/653 ,  C07C229/40 ,  A01N37/10 ,  C07D311/16 ,  A01N43/16 ,  C07D319/20 ,  A01N43/32 ,  C07D215/06 ,  A01N43/42 ,  C07D233/64 ,  A01N43/50 ,  C07D265/30 ,  A01N43/84 ,  C07D265/36 ,  C07D261/04 ,  A01N43/80 ,  C07D213/89 ,  A01N43/40 ,  C07D231/18 ,  A01P3/00

CPC分类号： C07D213/63 ,  A01N37/52 ,  A01N39/00 ,  C07C257/12 ,  C07C259/14 ,  C07C261/04 ,  C07C311/08 ,  C07C2601/14 ,  C07D215/26 ,  C07D231/12 ,  C07D319/20

摘要： Compounds of the formula I in which the substituents have the meaning given in the description, processes for preparing these compounds, compositions comprising them and their use for controlling harmful fungi.

摘要翻译： 式I化合物，其中取代基具有在说明书中给出的含义，制备这些化合物的方法，包含它们的组合物及其用于控制​​有害真菌的用途。

公开(公告)号：US07709533B2

公开(公告)日：2010-05-04

申请号：US11346546

申请日：2006-02-01

申请人： Xiaodong Wang ,  Alan Bradley Fulp ,  Darrick Seconi

发明人： Xiaodong Wang ,  Alan Bradley Fulp ,  Darrick Seconi

IPC分类号： A61K31/13 ,  C07C249/02

CPC分类号： C07D213/54 ,  C07C251/40 ,  C07C251/80 ,  C07C257/06 ,  C07C257/14 ,  C07C257/22 ,  C07C259/12 ,  C07C259/14 ,  C07D213/58 ,  C07D413/06 ,  C07F9/12

摘要： The present invention provides a class of chemical compounds useful in the treatment of sickle cell disease, diseases characterized by unwanted or abnormal cell proliferation and for the treatment of ocular disorders such as glaucoma. The active compounds are tri-(aryl or heteroaryl) methane compounds or analogues thereof which further comprise an imine moiety and where the tertiary carbon atom can be replaced with a different atom such as Si, Ge, N or P. The compounds enhance resistance to degradation in a biological medium, inhibit potassium flux in a cell, reduce mammalian cell proliferation, reduce the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.

摘要翻译： 本发明提供了一类用于治疗镰状细胞病，特征在于不想要的或异常细胞增殖的疾病和用于治疗眼部疾病如青光眼的化合物。 活性化合物是三（芳基或杂芳基）甲烷化合物或其类似物，其还包含亚胺部分，其中叔碳原子可被不同的原子如Si，Ge，N或P替代。化合物增强了对 在生物培养基中降解，抑制细胞内的钾通量，减少哺乳动物细胞增殖，减少红细胞的Gardos通道，减少镰状红细胞脱水和/或延缓红细胞镰状或变形的发生。

公开(公告)号：US20070037785A1

公开(公告)日：2007-02-15

申请号：US10575883

申请日：2004-10-15

申请人： Siegfried Ansorge ,  Ute Bank ,  Karsten Nordhoff ,  Michael Taeger ,  Frank Striggow

发明人： Siegfried Ansorge ,  Ute Bank ,  Karsten Nordhoff ,  Michael Taeger ,  Frank Striggow

IPC分类号： A61K31/55 ,  A61K31/397 ,  A61K31/519 ,  A61K31/538 ,  A61K31/5377 ,  A61K31/497 ,  A61K31/506 ,  A61K31/4745 ,  A61K31/473 ,  A61K31/165

CPC分类号： C07C235/56 ,  C04B35/632 ,  C07C229/34 ,  C07C243/28 ,  C07C251/80 ,  C07C251/86 ,  C07C255/61 ,  C07C259/14 ,  C07C271/28 ,  C07C311/08 ,  C07C311/19 ,  C07C311/29 ,  C07C323/60 ,  C07C327/48 ,  C07C2601/10 ,  C07C2603/74 ,  C07D205/08 ,  C07D213/82 ,  C07D225/02 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  C07F9/6506

摘要： The present invention relates to substances capable of specifically inhibiting Gly-Pro-p-nitroanilide cleaving peptidases, for a use in the medical field. Furthermore, the invention relates to the use of at least one of such substances or of at least one pharmaceutical or cosmetic composition containing at least one such substance for a prophylaxis or a therapy of diseases, particularly for a prophylaxis and a therapy of diseases accompanied by an excessive immune response (autoimmune diseases, allergies, transplant rejections), of other chronic-inflammatory diseases, of neuronal diseases and cerebral damage, of skin diseases (inter alia acne, psoriasis), of tumor diseases and of specific virus infections (inter alia SARS).

摘要翻译： 本发明涉及能够特异性抑制Gly-Pro-对硝基苯胺裂解肽酶的物质，用于医疗领域。 此外，本发明涉及至少一种这样的物质或至少一种含有至少一种这样的物质的药物或化妆品组合物用于预防或治疗疾病，特别是用于预防和治疗伴随着 其他慢性炎性疾病，神经元疾病和脑损伤，皮肤病（尤其是痤疮，牛皮癣），肿瘤疾病和特定病毒感染（特别是其他疾病）的过度免疫应答（自身免疫疾病，过敏，移植排斥） SARS）。

公开(公告)号：US07101900B2

公开(公告)日：2006-09-05

申请号：US11061470

申请日：2005-02-22

申请人： Joachim Rheinheimer ,  Karl Eicken ,  Ingo Rose ,  Thomas Grote ,  Eberhard Ammermann ,  John-Bryan Speakman ,  Siegfried Strathmann ,  Gisela Lorenz

发明人： Joachim Rheinheimer ,  Karl Eicken ,  Ingo Rose ,  Thomas Grote ,  Eberhard Ammermann ,  John-Bryan Speakman ,  Siegfried Strathmann ,  Gisela Lorenz

IPC分类号： A61K31/15 ,  A61K31/381 ,  C07D213/44 ,  C07D333/20 ,  C07D251/158

CPC分类号： C07C259/14 ,  A01N37/52 ,  C07C2601/02

摘要： Novel benzamidoxime derivatives, processes and intermediates for their preparation and their use as fungicides are described.In the context of the present invention, benzamidoxime derivatives are compounds of the formula I where: A is an aryl or hetaryl radical; Y is a straight-chain or branched C1–C4-alkylene group, where one carbon can be replaced by oxygen, nitrogen or sulfur or by a cyclopropyl group; Rn1 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1–C6-alkyl, C1–C6-alkoxy, C1–C4-haloalkyl, C1–C4-haloalkoxy, C1–C4-alkylthio, C1–C4-alkoxyalkoxy; R2 is unsubstituted or substituted phenyl-C1–C6-alkyl, thienyl-C1–C4-alkyl, or pyrazolyl-C1–C4-alkyl, Rp3 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1–C6-alkyl, C1–C6-alkoxy, C1–C4-haloalkyl, C1–C4-haloalkoxy, C1–C4-alkylthio, C1–C4-alkoxyalkoxy, C1–C6-alkylcarbonyl; n is 0–5; p is, depending on the number of free valencies, 0–4.

摘要翻译： 描述了新的苯甲酰胺肟衍生物，其制备方法和中间体及其作为杀真菌剂的用途。 在本发明的上下文中，苯甲酰胺肟衍生物是式I的化合物，其中：A是芳基或杂芳基; Y是直链或支链C 1 -C 4 - 亚烷基，其中一个碳可被氧，氮或硫取代或被环丙基取代; R 1是与以下组成的组中的一至五个相同或不同的基团：氢，卤素，C 1 -C 6 C 1 -C 6烷基，C 1 -C 6 - 烷氧基，C 1 -C 4 - 卤代烷基 ，C 1 -C 4 - 卤代烷氧基，C 1 -C 4 - 烷硫基，C 1 -C 4 - 烷氧基烷氧基; R 2是未取代或取代的苯基-C 1 -C 6 - 烷基，噻吩基-C 1 -C 或 - 吡唑基-C 1 -C 4 - C 1-4 - 烷基，R 3 - （CH 3）3 - / SUP>是与由以下组成的组中的一至五个相同或不同的基团：氢，卤素，C 1 -C 6 - 烷基，C 1 - C 1 -C 6 - 烷氧基，C 1 -C 4 - 卤代烷基，C 1 -C 3 > 4个 - 卤代烷氧基，C 1 -C 4 - 烷硫基，C 1 -C 4 - - 烷氧基烷氧基，C 1 -C 6 - 烷基羰基; n为0-5; p取决于自由价格的数量，0-4。

公开(公告)号：US20060178346A1

公开(公告)日：2006-08-10

申请号：US11346546

申请日：2006-02-01

申请人： Xiaodong Wang ,  Alan Fulp ,  Darrick Seconi

发明人： Xiaodong Wang ,  Alan Fulp ,  Darrick Seconi

IPC分类号： A61K31/675 ,  A61K31/506 ,  A61K31/501 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/444 ,  A61K31/4178 ,  A61K31/427 ,  A61K31/422

CPC分类号： C07D213/54 ,  C07C251/40 ,  C07C251/80 ,  C07C257/06 ,  C07C257/14 ,  C07C257/22 ,  C07C259/12 ,  C07C259/14 ,  C07D213/58 ,  C07D413/06 ,  C07F9/12

摘要： The present invention provides a class of chemical compounds useful in the treatment of sickle cell disease, diseases characterized by unwanted or abnormal cell proliferation and for the treatment of ocular disorders such as glaucoma. The active compounds are tri-(aryl or heteroaryl) methane compounds or analogues thereof which further comprise an imine moiety and where the tertiary carbon atom can be replaced with a different atom such as Si, Ge, N or P. The compounds enhance resistance to degradation in a biological medium, inhibit potassium flux in a cell, reduce mammalian cell proliferation, reduce the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.

摘要翻译： 本发明提供了一类用于治疗镰状细胞病，特征在于不想要的或异常细胞增殖的疾病和用于治疗眼部疾病如青光眼的化合物。 活性化合物是三（芳基或杂芳基）甲烷化合物或其类似物，其还包含亚胺部分，其中叔碳原子可被不同的原子如Si，Ge，N或P替代。化合物增强了对 在生物培养基中降解，抑制细胞内的钾通量，减少哺乳动物细胞增殖，减少红细胞的Gardos通道，减少镰状红细胞脱水和/或延缓红细胞镰状或变形的发生。