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1. 发明授权

US08487093B2 β-lactamase inhibitors 有权
标题翻译： β-内酰胺酶抑制剂
公开(公告)号：US08487093B2
公开(公告)日：2013-07-16
申请号：US12812763
申请日：2009-01-15
申请人： Timothy A. Blizzard , Helen Chen , Candido Gude , Jeffrey D. Hermes , Jason Imbriglio , Seongkon Kim , Jane Y. Wu , Christopher J. Mortko , Ian Mangion , Nelo Rivera , Rebecca T. Ruck , Michael Shevlin
发明人： Timothy A. Blizzard , Helen Chen , Candido Gude , Jeffrey D. Hermes , Jason Imbriglio , Seongkon Kim , Jane Y. Wu , Christopher J. Mortko , Ian Mangion , Nelo Rivera , Rebecca T. Ruck , Michael Shevlin
IPC分类号： C07D243/00 , A61K31/551
CPC分类号： C07D471/08 , C07D211/58 , C07D211/60 , C07D211/78 , C07D487/08 , C07D519/00
摘要： Substituted bicyclic beta-lactams of Formula I: (I), are β-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds can be employed with a β-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.
摘要翻译：式I的取代的双环β-内酰胺：（I）是β-内酰胺酶抑制剂，其中a，X，R 1和R 2在本文中定义。化合物及其药学上可接受的盐可用于与β-内酰胺抗生素联合治疗细菌感染。特别地，由于β-内酰胺酶的存在，该化合物可与β-内酰胺抗生素（例如亚胺培南，哌拉西林或头孢他啶）一起用于抗β-内酰胺抗生素的微生物。

2. 发明申请

US20110294777A1 BETA-LACTAMASE INHIBITORS 有权
标题翻译： BETA-LACTAMASE抑制剂
公开(公告)号：US20110294777A1
公开(公告)日：2011-12-01
申请号：US12812763
申请日：2009-01-15
申请人： Timothy A. Blizzard , Helen Chen , Candido Gude , Jeffrey D. Hermes , Jason Imbriglio , Seongkon Kim , Jane Y. Wu , Sookhee Ha , Christopher J. Mortko , Ian Mangion , Nelo Rivera , Rebecca T. Ruck , Michael Shevlin
发明人： Timothy A. Blizzard , Helen Chen , Candido Gude , Jeffrey D. Hermes , Jason Imbriglio , Seongkon Kim , Jane Y. Wu , Sookhee Ha , Christopher J. Mortko , Ian Mangion , Nelo Rivera , Rebecca T. Ruck , Michael Shevlin
IPC分类号： A61K31/4545 , C07D487/08 , C07D519/00 , A61K31/55 , A61K31/454 , A61P31/04 , A61K31/439 , A61K31/553 , A61K31/496 , C07D401/12 , A61P31/00 , C07D471/08 , A61K31/4439
CPC分类号： C07D471/08 , C07D211/58 , C07D211/60 , C07D211/78 , C07D487/08 , C07D519/00
摘要： Substituted bicyclic beta-lactams of Formula I: (I), are β-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds can be employed with a β-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.
摘要翻译：式I的取代的双环β-内酰胺：（I）是β-内酰胺酶抑制剂，其中a，X，R 1和R 2在本文中定义。化合物及其药学上可接受的盐可用于治疗与β-内酰胺抗生素组合的细菌感染。特别地，由于β-内酰胺酶的存在，这些化合物可以与抗β-生物抗生素（例如亚胺培南，哌拉西林或头孢他啶）一起用于抗β-内酰胺抗生素的微生物。

3. 发明申请

US20070105827A1 Estrogen receptor modulators 审中-公开
标题翻译：雌激素受体调节剂
公开(公告)号：US20070105827A1
公开(公告)日：2007-05-10
申请号：US10579652
申请日：2004-11-19
申请人： Timothy Blizzard , Candido Gude , Jerry Morgan
发明人： Timothy Blizzard , Candido Gude , Jerry Morgan
IPC分类号： A61K31/56
CPC分类号： C07J1/0022 , A61K31/56 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or pre-vention of a variety of conditions related to estrogen functioning including: bone loss, bone fracturs, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.
摘要翻译：本发明涉及其化合物及其衍生物，其合成及其作为雌激素受体调节剂的用途。本发明的化合物是雌激素受体的配体，因此可用于治疗或预防与雌激素功能相关的各种病症，包括：骨丢失，骨折，骨质疏松症，转移性骨病，佩吉特氏病，牙周病疾病，软骨变性，子宫内膜异位症，子宫肌瘤疾病，潮热，LDL胆固醇水平升高，心血管疾病，认知功能障碍，脑退行性疾病，再狭窄，男子乳腺发育不良，血管平滑肌细胞增殖，肥胖，失禁，炎症，炎症肠疾病，性功能障碍，高血压，视网膜变性和癌症，特别是乳腺，子宫和前列腺。

4. 发明授权

US09062070B2 Inhibitors of the renal outer medullary potassium channel 有权
标题翻译：肾外髓质钾通道抑制剂
公开(公告)号：US09062070B2
公开(公告)日：2015-06-23
申请号：US14239649
申请日：2012-08-16
申请人： Alexander Pasternak , Timothy Blizzard , Harry Chobanian , Reynalda de Jesus , Fa-Xiang Ding , Shuzhi Dong , Candido Gude , Dooseop Kim , Haifeng Tang , Shawn Walsh , Barbara Pio , Jinlong Jiang
发明人： Alexander Pasternak , Timothy Blizzard , Harry Chobanian , Reynalda de Jesus , Fa-Xiang Ding , Shuzhi Dong , Candido Gude , Dooseop Kim , Haifeng Tang , Shawn Walsh , Barbara Pio , Jinlong Jiang
IPC分类号： C07D498/04 , A61K31/4985 , A61K31/5383 , A61K31/542 , A61K31/553 , A61K45/06 , C07D487/04 , C07D513/04
CPC分类号： C07D498/04 , A61K31/4985 , A61K31/5383 , A61K31/542 , A61K31/553 , A61K45/06 , C07D487/04 , C07D513/04
摘要： The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
摘要翻译：本发明提供式Ia化合物及其药学上可接受的盐，它们是ROMK（Kir1.1）通道的抑制剂。该化合物可以用作利尿剂和/或利尿钠剂，并且用于治疗和预防包括心血管疾病如高血压，心力衰竭以及与过量盐和水滞留有关的病症的医学病症。

5. 发明申请

US20140206618A1 Inhibitors of the Renal Outer Medullary Potassium Channel 有权
标题翻译：肾外侧髓质钾通道抑制剂
公开(公告)号：US20140206618A1
公开(公告)日：2014-07-24
申请号：US14239649
申请日：2012-08-16
申请人： Alexander Pasternak , Timothy Blizzard , Harry Chobanian , Reynalda de Jesus , Fa-Xiang Ding , Shuzhi Dong , Candido Gude , Dooseop Kim , Haifeng Tang , Shawn Walsh , Barbara Pio , Jinlong Jiang
发明人： Alexander Pasternak , Timothy Blizzard , Harry Chobanian , Reynalda de Jesus , Fa-Xiang Ding , Shuzhi Dong , Candido Gude , Dooseop Kim , Haifeng Tang , Shawn Walsh , Barbara Pio , Jinlong Jiang
IPC分类号： C07D498/04 , A61K45/06 , A61K31/4985 , C07D513/04 , A61K31/542 , C07D487/04 , A61K31/5383 , A61K31/553
CPC分类号： C07D498/04 , A61K31/4985 , A61K31/5383 , A61K31/542 , A61K31/553 , A61K45/06 , C07D487/04 , C07D513/04
摘要： The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
摘要翻译：本发明提供式Ia化合物及其药学上可接受的盐，它们是ROMK（Kir1.1）通道的抑制剂。这些化合物可以用作利尿剂和/或利尿钠剂，并且用于治疗和预防包括心血管疾病如高血压，心力衰竭以及与过量盐和保水有关的病症的医学病症。

6. 发明申请

US20080015173A1 Estrogen Receptor Modulators 审中-公开
标题翻译：雌激素受体调节剂
公开(公告)号：US20080015173A1
公开(公告)日：2008-01-17
申请号：US11628828
申请日：2005-06-07
申请人： Timothy Blizzard , Candido Gude
发明人： Timothy Blizzard , Candido Gude
IPC分类号： A61K31/56 , A61P19/00 , A61P25/00 , A61P35/00 , C07J1/00 , C07J7/00 , C07J9/00
CPC分类号： C07J1/00
摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.
摘要翻译：本发明涉及其化合物及其衍生物，其合成及其作为雌激素受体调节剂的用途。本发明的化合物是雌激素受体的配体，因此可用于治疗或预防与雌激素功能相关的各种病症，包括：骨丢失，骨折，骨质疏松症，转移性骨病，佩吉特氏病，牙周病，软骨变性，子宫内膜异位症，子宫肌瘤病，热潮红，LDL胆固醇水平升高，心血管疾病，认知功能障碍，脑退行性疾病，再狭窄，男子乳腺发育不良，血管平滑肌细胞增殖，肥胖，失禁，炎症，炎症性肠病，性功能障碍，高血压，视网膜变性和癌症，特别是乳腺，子宫和前列腺。

7. 发明申请

US20070203102A1 Estrogen Receptor Modulators 审中-公开
标题翻译：雌激素受体调节剂
公开(公告)号：US20070203102A1
公开(公告)日：2007-08-30
申请号：US11629930
申请日：2005-06-24
申请人： Timothy Blizzard , Candido Gude
发明人： Timothy Blizzard , Candido Gude
IPC分类号： A61K31/56 , C07J1/00
CPC分类号： C07J1/00
摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.
摘要翻译：本发明涉及其化合物及其衍生物，其合成及其作为雌激素受体调节剂的用途。本发明的化合物是雌激素受体的配体，因此可用于治疗或预防与雌激素功能相关的各种病症，包括：骨丢失，骨折，骨质疏松症，转移性骨病，佩吉特氏病，牙周病，软骨变性，子宫内膜异位症，子宫肌瘤病，热潮红，LDL胆固醇水平升高，心血管疾病，认知功能障碍，脑退行性疾病，再狭窄，男子乳腺发育不良，血管平滑肌细胞增殖，肥胖，失禁，炎症，炎症性肠病，性功能障碍，高血压，视网膜变性和癌症，特别是乳腺，子宫和前列腺。

8. 发明申请

US20070099880A1 Estrogen receptor modulators 审中-公开
标题翻译：雌激素受体调节剂
公开(公告)号：US20070099880A1
公开(公告)日：2007-05-03
申请号：US10579651
申请日：2004-11-19
申请人： Timothy Blizzard , Candido Gude , Jerry Morgan
发明人： Timothy Blizzard , Candido Gude , Jerry Morgan
IPC分类号： C07J1/00 , A61K31/56
CPC分类号： C07J41/0094 , C07J1/00 , C07J1/0022
摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.
摘要翻译：本发明涉及其化合物及其衍生物，其合成及其作为雌激素受体调节剂的用途。本发明的化合物是雌激素受体的配体，因此可用于治疗或预防与雌激素功能相关的各种病症，包括：骨丢失，骨折，骨质疏松症，转移性骨病，佩吉特氏病，牙周病，软骨变性，子宫内膜异位症，子宫肌瘤病，热潮红，LDL胆固醇水平升高，心血管疾病，认知功能障碍，脑退行性疾病，再狭窄，男子乳腺发育不良，血管平滑肌细胞增殖，肥胖，失禁，炎症，炎性肠病，性功能障碍，高血压，视网膜变性和癌症，特别是乳腺，子宫和前列腺。

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