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1. 发明授权

US08834841B2 Imaging agents 有权
标题翻译：成像剂
公开(公告)号：US08834841B2
公开(公告)日：2014-09-16
申请号：US13857164
申请日：2013-04-05
申请人： Emory University
发明人： Mark M. Goodman
IPC分类号： A61K51/00 , A61M36/14 , C07B59/00 , C07D345/00 , C07D291/04 , A61K51/04 , C07C229/48 , C07F13/00
CPC分类号： C07C229/48 , A61K51/0402 , A61K51/0406 , C07B59/001 , C07C2601/04 , C07D291/04 , C07D345/00 , C07F13/005
摘要： The present invention provides novel amino acid compounds useful in detecting and evaluating brain and body tumors. These compounds have the advantageous properties of rapid uptake and prolonged retention in tumors and can be labeled with halogen isotopes such as fluorine-18, iodine-123, iodine-124, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77, bromine-82, astatine-210, astatine-211, and other astatine isotopes. These compounds can also be labeled with technetium and rhenium isotopes using known chelation complexes. The compounds disclosed herein bind tumor tissues in vivo with high specificity and selectivity when administered to a subject. Preferred compounds show a target to non-target ratio of at least 2:1, are stable in vivo and substantially localized to target within 1 hour after administration. Preferred compounds include 1-amino-2-[18F]fluorocyclobutyl-1-carboxylic acid (2-[18F]FACBC) and 1-amino-2-[18]fluoromethylcyclobutyl-1-carboxylic acid (2-[18F]FMACBC). The labeled amino acid compounds of the invention are useful as imaging agents in detecting and/or monitoring tumors in a subject by PET or SPECT.
摘要翻译：本发明提供了可用于检测和评估脑和体肿瘤的新型氨基酸化合物。这些化合物具有在肿瘤中快速吸收和延长保留的有利特性，并可用卤素同位素如氟-18，碘-123，碘-124，碘-125，碘-131，溴-75，溴-76 ，溴-77，溴-82，ast ine -21，ast ine -211和其他ast同位素。这些化合物也可以使用已知的螯合络合物用锝和铼同位素标记。当给予受试者时，本文所公开的化合物以高特异性和选择性在体内结合肿瘤组织。优选的化合物显示至少2:1的目标与非目标比例，在给药后1小时内在体内是稳定的并且基本上定位于靶标上。优选的化合物包括1-氨基-2- [18 F]氟代环丁基-1-羧酸（2- [18 F] FACBC）和1-氨基-2- [18]氟甲基环丁基-1-羧酸（2- [18 F] FMACBC）。本发明的标记氨基酸化合物可用作通过PET或SPECT检测和/或监测受试者的肿瘤的成像剂。

2. 发明申请

US20060276494A1 Novel sulfonamides as L-CPT1 inhibitors 有权
标题翻译：新型磺酰胺作为L-CPT1抑制剂
公开(公告)号：US20060276494A1
公开(公告)日：2006-12-07
申请号：US11444765
申请日：2006-06-01
申请人： Konrad Bleicher , Simona Ceccarelli , Odile Chomienne , Patrizio Mattei , Tanja Schulz-Gasch , Christoph Stahl
发明人： Konrad Bleicher , Simona Ceccarelli , Odile Chomienne , Patrizio Mattei , Tanja Schulz-Gasch , Christoph Stahl
IPC分类号： A61K31/513 , A61K31/425 , A61K31/42 , A61K31/195 , C07D413/02 , C07D409/02
CPC分类号： C07D413/04 , C07C311/21 , C07C311/29 , C07D257/04 , C07D271/07 , C07D291/04 , C07D409/04
摘要： The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型磺酰胺衍生物，其中R 2，R 3，R 4，A，X，Y 3， SUP> 1，Y 2，Y 3，Y 4和Z 1如上定义在说明书和权利要求书中，以及其生理上可接受的盐和酯。这些化合物抑制L-CPT1，可用作药物。

3. 发明申请

US20060223837A1 Biaryl derived amide modulators of vanilloid VR1 receptor 审中-公开
标题翻译：香草素VR1受体的二芳基衍生的酰胺调节剂
公开(公告)号：US20060223837A1
公开(公告)日：2006-10-05
申请号：US11387894
申请日：2006-03-23
申请人： Ellen Codd , Scott Dax , Christopher Flores , Michelle Jetter , Mark Youngman
发明人： Ellen Codd , Scott Dax , Christopher Flores , Michelle Jetter , Mark Youngman
IPC分类号： A61K31/506 , A61K31/4709 , A61K31/444 , C07D401/02
CPC分类号： C07D291/04 , C07C233/29 , C07C233/55 , C07C237/42 , C07D213/53 , C07D213/75 , C07D233/64 , C07D233/68 , C07D235/06 , C07D271/06 , C07D333/24 , C07D401/04 , C07D401/12
摘要： The invention is directed to novel vanilloid receptor type 1 (VR1) ligands. More specifically, the invention relates to novel biaryl-derived amides that are potent antagonists or agonists of VR1. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
摘要翻译：本发明涉及新型香草素受体1型（VR1）配体。更具体地，本发明涉及作为VR1的有效拮抗剂或激动剂的新型联芳基衍生的酰胺。还描述了使用本发明的化合物治疗轻度至重度疼痛和各种疾病的药物和兽医组合物和方法。

4. 发明申请

US20030203945A1 Heterocyclic derivatives useful as pharmaceutical agents 审中-公开
标题翻译：用作药剂的杂环衍生物
公开(公告)号：US20030203945A1
公开(公告)日：2003-10-30
申请号：US10429349
申请日：2003-05-05
发明人： David Clive Blakemore , Justin Stephen Bryans , Sophie Caroline Williams
IPC分类号： A61K031/433 , A61K031/41 , A61K031/4245
CPC分类号： C07D291/04 , A61K31/41 , A61K31/4245 , A61K31/433 , A61K45/06 , A61K47/545 , A61K47/555 , C07D257/04 , C07D271/07 , C07D285/08
摘要： This invention relates to novel heterocyclic derivatives of the formula (VII), (VIII) or (IX) 1 in which P, Q, R1-R6, m and n are as defined in the specification, and to pharmaceutically acceptable salts thereof. The compounds and pharmaceutical compositions containing them are useful in the treatment of a range of disorders including epilepsy, faintness attacks, hypokinesia, cranial disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases and gastrointestinal disorders, especially irritable bowel syndrome.
摘要翻译：本发明涉及式（VII），（VIII）或（IX）的新型杂环衍生物，其中P，Q，R 1 -R 6，m和n如说明书中所定义，其可接受的盐。含有它们的化合物和药物组合物可用于治疗一系列疾病，包括癫痫，微弱发作，运动功能减退，颅内障碍，抑郁症，焦虑症，恐慌症，疼痛，神经病理学疾病，炎性疾病和胃肠道疾病，特别是肠易激综合征。

5. 发明申请

US20020077342A1 Heterocyclic derivatives useful as pharmaceutical agents 审中-公开
标题翻译：用作药剂的杂环衍生物
公开(公告)号：US20020077342A1
公开(公告)日：2002-06-20
申请号：US10015122
申请日：2001-10-26
发明人： David Clive Blakemore , Justin Stephen Bryans , Sophie Caroline Williams
IPC分类号： A61K031/433 , A61K031/4245 , A61K031/41
CPC分类号： C07D291/04 , A61K31/41 , A61K31/4245 , A61K31/433 , A61K45/06 , A61K47/545 , A61K47/555 , C07D257/04 , C07D271/07 , C07D285/08
摘要： This invention relates to novel heterocyclic derivatives of the formula (VII), (VIII) or (IX) 1 in which P, Q, R1-R6, m and n are as defined in the specification, and to pharmaceutically acceptable salts thereof. The compounds and pharmaceutical compositions containing them are useful in the treatment of a range of disorders including epilepsy, faintness attacks, hypokinesia, cranial disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases and gastrointestinal disorders, especially irritable bowel syndrome.
摘要翻译：本发明涉及式（VII），（VIII）或（IX）的新型杂环衍生物，其中P，Q，R 1 -R 6，m和n如说明书中所定义，及其药学上可接受的盐。含有它们的化合物和药物组合物可用于治疗一系列疾病，包括癫痫，微弱发作，运动功能减退，颅内障碍，抑郁症，焦虑症，恐慌症，疼痛，神经病理学疾病，炎性疾病和胃肠道疾病，特别是肠易激综合征。

6. 发明授权

US06344473B1 Imidazoles useful as nitric oxide synthase inhibitors 失效
标题翻译：咪唑可用作一氧化氮合酶抑制剂
公开(公告)号：US06344473B1
公开(公告)日：2002-02-05
申请号：US09633601
申请日：2000-08-07
申请人： Donald W. Hansen, Jr. , Arija A. Bergmanis , Timothy J. Hagen , E. Ann Hallinan , Steven W. Kramer , Suzanne Metz , Karen B. Peterson , Barnett S. Pitzele , Foe S. Tjoeng , Mihaly V. Toth , Mahima Trivedi , R. Keith Webber , Sofya Tsymbalov , Rolando E. Gapud
发明人： Donald W. Hansen, Jr. , Arija A. Bergmanis , Timothy J. Hagen , E. Ann Hallinan , Steven W. Kramer , Suzanne Metz , Karen B. Peterson , Barnett S. Pitzele , Foe S. Tjoeng , Mihaly V. Toth , Mahima Trivedi , R. Keith Webber , Sofya Tsymbalov , Rolando E. Gapud
IPC分类号： A61K314172
CPC分类号： C07D291/04 , C07D233/96 , C07D271/07 , C07D273/04 , C07D285/08
摘要： 1,3-diazolino and 1,3-diazolidino heterocycle derivatives useful as nitric oxide synthase inhibitors.
摘要翻译：可用作一氧化氮合酶抑制剂的1,3-二唑啉和1,3-二唑烷基杂环衍生物。

7. 发明授权

US6136829A Oxathiadiazole derivatives usful as iNOS inhibitors 失效
标题翻译： Oxathiadiazole衍生物可用作iNOS抑制剂
公开(公告)号：US6136829A
公开(公告)日：2000-10-24
申请号：US356735
申请日：1999-07-19
申请人： Donald W. Hansen, Jr. , Ariia A. Bergmanis , Timothy J. Hagen , E. Ann Hallinan , Steven W. Kramer , Suzanne Metz , Karen B. Peterson , Barnett S. Pitzele , Foe S. Tjoeng , Mihaly V. Toth , Mahima Trivedi , R. Keith Webber , Sofya Tsymbalov , Rolando E. Gapud
发明人： Donald W. Hansen, Jr. , Ariia A. Bergmanis , Timothy J. Hagen , E. Ann Hallinan , Steven W. Kramer , Suzanne Metz , Karen B. Peterson , Barnett S. Pitzele , Foe S. Tjoeng , Mihaly V. Toth , Mahima Trivedi , R. Keith Webber , Sofya Tsymbalov , Rolando E. Gapud
IPC分类号： A61K31/41 , A61K31/4166 , A61K31/4245 , A61K31/433 , A61K31/535 , A61K31/5377 , A61P9/02 , A61P43/00 , C07D233/96 , C07D271/06 , C07D271/07 , C07D273/04 , C07D285/08 , C07D291/04
CPC分类号： C07D291/04 , C07D233/96 , C07D271/07 , C07D273/04 , C07D285/08
摘要： 1,3-diazolino and 1,3-diazolidino heterocycle derivatives useful as nitric oxide synthase inhibitors.
摘要翻译：可用作一氧化氮合酶抑制剂的1,3-二唑啉和1,3-二唑烷基杂环衍生物。

8. 发明授权

US5981556A 1,3-diazolino and 1,3-diazolidino heterocycles as useful nitric oxide synthase inhibitors 失效
标题翻译： 1,3-二唑啉和1,3-二唑烷基杂环作为有用的一氧化氮合酶抑制剂
公开(公告)号：US5981556A
公开(公告)日：1999-11-09
申请号：US898110
申请日：1997-07-22
申请人： Donald W. Hansen, Jr. , Arija A. Bergmanis , Timothy J. Hagen , E. Ann Hallinan , Steven W. Kramer , Suzanne Metz , Karen B. Peterson , Barnett S. Pitzele , Foe S. Tjoeng , Mihaly V. Toth , Mahima Trivedi , R. Keith Webber , Sofya Tsymbalov , Rolando E. Gapud
发明人： Donald W. Hansen, Jr. , Arija A. Bergmanis , Timothy J. Hagen , E. Ann Hallinan , Steven W. Kramer , Suzanne Metz , Karen B. Peterson , Barnett S. Pitzele , Foe S. Tjoeng , Mihaly V. Toth , Mahima Trivedi , R. Keith Webber , Sofya Tsymbalov , Rolando E. Gapud
IPC分类号： A61K31/41 , A61K31/4166 , A61K31/4245 , A61K31/433 , A61K31/535 , A61K31/5377 , A61P9/02 , A61P43/00 , C07D233/96 , C07D271/06 , C07D271/07 , C07D273/04 , C07D285/08 , C07D291/04 , C07D285/125 , C07D417/06
CPC分类号： C07D291/04 , C07D233/96 , C07D271/07 , C07D273/04 , C07D285/08
摘要： 1,3-diazolino and 1,3-diazolidino heterocycle derivatives useful as nitric oxide synthase inhibitors.
摘要翻译：可用作一氧化氮合酶抑制剂的1,3-二唑啉和1,3-二唑烷基杂环衍生物。

9. 发明授权

US5958958A 1,2,4-oxa diazolino and 1,24-oxa diazolidion heterocycles as useful nitric oxide synthase inhibitors 失效
标题翻译： 1,2,4-氧杂二氮杂双环和1,24-氧杂二氮杂环杂环作为有用的一氧化氮合酶抑制剂
公开(公告)号：US5958958A
公开(公告)日：1999-09-28
申请号：US231478
申请日：1999-01-14
申请人： Donald W. Hansen, Jr. , Arija A. Bergmanis , Timothy J. Hagen , E. Ann Hallinan , Steven W. Kramer , Suzanne Metz , Karen B. Peterson , Barnett S. Pitzele , Foe S. Tjoeng , Mihaly V. Toth , Mahima Trivedi , R. Keith Webber , Sofya Tsymbalov , Rolando E. Gapud
发明人： Donald W. Hansen, Jr. , Arija A. Bergmanis , Timothy J. Hagen , E. Ann Hallinan , Steven W. Kramer , Suzanne Metz , Karen B. Peterson , Barnett S. Pitzele , Foe S. Tjoeng , Mihaly V. Toth , Mahima Trivedi , R. Keith Webber , Sofya Tsymbalov , Rolando E. Gapud
IPC分类号： A61K31/41 , A61K31/4166 , A61K31/4245 , A61K31/433 , A61K31/535 , A61K31/5377 , A61P9/02 , A61P43/00 , C07D233/96 , C07D271/06 , C07D271/07 , C07D273/04 , C07D285/08 , C07D291/04 , C07D271/113
CPC分类号： C07D291/04 , C07D233/96 , C07D271/07 , C07D273/04 , C07D285/08
摘要： 1,2,4-oxa-diazolino and 1,2,4-oxa-diazolidino heterocycle derivatives useful as nitric oxide synthase inhibitors.
摘要翻译：可用作一氧化氮合酶抑制剂的1,2,4-恶二唑啉和1,2,4-氧杂二氮杂环丁烷杂环衍生物。

10. 发明授权

US5271812A Electrocatalytic oxidation method for the production of cyclic sulfates and sulfamidates 失效
标题翻译：用于生产环状硫酸盐和氨磺酸盐的电催化氧化法
公开(公告)号：US5271812A
公开(公告)日：1993-12-21
申请号：US717432
申请日：1991-06-19
申请人： Yun Gao , Charles M Zepp
发明人： Yun Gao , Charles M Zepp
IPC分类号： C07D291/04 , C07D327/10 , C25B3/00
CPC分类号： C07D291/04 , C07D327/10 , C25B3/00
摘要： The invention relates to a process for the production of cyclic sulfates and cyclic sulfamidates from the corresponding cyclic sulfite and cyclic sulfamidite substrate, respectively. The method involves the electrolysis of a solvent mixture containing active metal species, non-metal oxidant species and substrate.
摘要翻译：本发明涉及分别从相应的环状亚硫酸盐和环状亚磺酰胺基质制备环状硫酸盐和环状磺酰胺酸盐的方法。该方法涉及电解含有活性金属物质，非金属氧化剂物质和底物的溶剂混合物。

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