专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US07268125B2 β-lactamyl vasopressin V1a antagonists 有权
标题翻译： β-内酰胺加压素V1a拮抗剂
公开(公告)号：US07268125B2
公开(公告)日：2007-09-11
申请号：US11442788
申请日：2006-05-30
申请人： Robert F. Bruns, Jr. , Christophe D. G. Guillon , Ned D. Heindel , Gary A. Koppel , Marvin J. Miller
发明人： Robert F. Bruns, Jr. , Christophe D. G. Guillon , Ned D. Heindel , Gary A. Koppel , Marvin J. Miller
IPC分类号： C07D413/04 , C07D413/14 , C07D205/085 , C07D403/04 , A61K31/496
CPC分类号： C07D413/14 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D413/04 , C07D417/14
摘要： Novel 2-(azetidin-2-on-1-yl)alkanedioic acid derivatives and 2-(azetidin-2-on-1-yl)alkoxyalkanoic acid derivatives are described for use in the treatment of disease states responsive to antagonism of the vasopressin V1a receptor
摘要翻译：描述了新的2-（氮杂环丁烷-2-对-1-基）烷二酸衍生物和2-（氮杂环丁-2-酮-1-基）烷氧基烷酸衍生物用于治疗对加压素拮抗作用有反应的疾病状态 V 1a受体

2. 发明申请

US20110059935A1 Beta-LACTAMYL VASOPRESSIN V1a ANTAGONISTS 审中-公开
标题翻译： β-LACTAMYL VASOPRESSIN V1a ANTAGONISTS
公开(公告)号：US20110059935A1
公开(公告)日：2011-03-10
申请号：US12868277
申请日：2010-08-25
申请人： Robert F. Bruns, JR. , Christophe D. G. Guillon , Ned D. Heindel , Gary A. Koppel , Marvin J. Miller
发明人： Robert F. Bruns, JR. , Christophe D. G. Guillon , Ned D. Heindel , Gary A. Koppel , Marvin J. Miller
IPC分类号： A61K31/397 , A61P25/00
CPC分类号： C07D413/14 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D413/04 , C07D417/14
摘要： Novel 2-(azetidin-2-on-1-yl)alkanedioic acid derivatives and 2-(azetidin-2-on-1-yl)alkoxyalkanoic acid derivatives are described for use in the treatment of disease states responsive to antagonism of the vasopressin V1a receptor.
摘要翻译：描述了新的2-（氮杂环丁烷-2-对-1-基）烷二酸衍生物和2-（氮杂环丁-2-酮-1-基）烷氧基烷酸衍生物用于治疗对加压素拮抗作用有反应的疾病状态 V1a受体。

3. 发明授权

US07119083B2 β-Lactamyl vasopressin V1a Antagonists 有权
标题翻译： β-内酰胺基加压素V1a拮抗剂
公开(公告)号：US07119083B2
公开(公告)日：2006-10-10
申请号：US10492323
申请日：2002-10-11
申请人： Robert F. Bruns, Jr. , Christophe D. G. Guillon , Ned D. Heindel , Gary A. Koppel , Marvin J. Miller
发明人： Robert F. Bruns, Jr. , Christophe D. G. Guillon , Ned D. Heindel , Gary A. Koppel , Marvin J. Miller
IPC分类号： C07D205/085 , C07D403/04 , C07D413/04 , C07D413/14 , A61K31/496
CPC分类号： C07D413/14 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D413/04 , C07D417/14
摘要： Novel 2-(azetidin-2-on-1-yl)alkanedioic acid derivatives and 2-(azetidin-2-on-1-yl)alkoxyalkanoic acid derivatives are described for use in the treatment of disease states responsive to antagonism of the vasopressin V1a receptor.
摘要翻译：描述了新的2-（氮杂环丁烷-2-对-1-基）烷二酸衍生物和2-（氮杂环丁-2-酮-1-基）烷氧基烷酸衍生物用于治疗对加压素拮抗作用有反应的疾病状态 V 1a受体。

4. 发明授权

US08343971B2 Pharmacologically-active vanilloid carbamates 有权
标题翻译：药理活性甘草酸氨基甲酸酯
公开(公告)号：US08343971B2
公开(公告)日：2013-01-01
申请号：US12882351
申请日：2010-09-15
申请人： Jeffrey D. Laskin , Diane E. Heck , Carl Jeffrey Lacey , Erik Aponte , Mou-Tuan Huang , Ned D. Heindel
发明人： Jeffrey D. Laskin , Diane E. Heck , Carl Jeffrey Lacey , Erik Aponte , Mou-Tuan Huang , Ned D. Heindel
IPC分类号： A61K31/535 , C07D295/18
CPC分类号： C07C271/24 , C07C271/12 , C07C271/16 , C07C271/22 , C07C2601/14 , C07C2602/08 , C07D277/16 , C07D295/13
摘要： This application relates to pharmacologically-active vanilloid compounds which are useful for the treatment of various anti-inflammatory states characterized by inhibition of FAAH, such as, Alzheimer's dementia, Parkinson's disease, depression, pain, rheumatoid arthritis, pathophysiology of mood disorders, multiple sclerosis, and inflammation, or antagonism of TRPV1, such as, for example, Huntington's disease, hypertension, arthritis, allergic airway inflammation, Crohn's disease, ulcerative colitis, and neuropathic pain.
摘要翻译：本申请涉及药理学活性的香草酸化合物，其可用于治疗以抑制FAAH为特征的各种抗炎状态，例如阿尔茨海默氏痴呆，帕金森病，抑郁症，疼痛，类风湿性关节炎，情绪障碍的病理生理学，多发性硬化，以及TRPV1的炎症或拮抗作用，例如亨廷顿氏病，高血压，关节炎，过敏性气道炎症，克罗恩病，溃疡性结肠炎和神经性疼痛。

5. 发明授权

US06255324B1 Amino-and mercurio-substituted 4′,5'-dihydropsoralens and therapeutical uses thereof 有权
标题翻译：氨基和巯基取代的4'，5'-二氢补骨脂素及其治疗用途
公开(公告)号：US06255324B1
公开(公告)日：2001-07-03
申请号：US09199552
申请日：1998-11-25
申请人： Ned D. Heindel , Jeffrey D. Laskin , Diane E. Heck , Robert D. Rapp , Marilyn S. Whittemore , Thomas E. McNeel , Ivan Jabin
发明人： Ned D. Heindel , Jeffrey D. Laskin , Diane E. Heck , Robert D. Rapp , Marilyn S. Whittemore , Thomas E. McNeel , Ivan Jabin
IPC分类号： A61K314709
CPC分类号： C07D493/04 , C07D311/44 , C07D311/56 , C07F3/14
摘要： 5′-substituted, 4′,5′-dihydropsoralen compounds (5) bearing tertiary amines (and salts thereof), quaternary ammonium moieties or organomercurial moieties are described. Also described are 2-substituted mercurimethyl-2-3-dihydro-benzofurans of forumla (7): Also reported are versatile direct syntheses through a hitherto unknown compounds such as 3-R-4,8-dimethyl-4′,5′-dihydro-5′-bromomethylpsoralen or a 3-R-4,8-dimethyl-4′, 5′-dihydro-5′-iodomethylpsoralen to prepare a structurally diverse array of partially reduced psoralens and benzofurans. The presence of a permanent ammonium charge in these psoralens precludes membrane passage and the mono-unsaturation precludes the cross-linking of nuclear DNA, thereby minimizing the mutagenic/carcinogenic side effects long associated with psoralen-derived therapies. The presence of a mercury functionality provides a reactive cell-binding group on these psoralens with unique cytotoxicity without light activation and an enhancement of cytotoxicity activity upon light activation. The invention also relates to These partially reduced and quaternized psoralens, amino-substituted psoralens, and mercurio psoralens display impressive pharmacology against PAM 212 keratinocytes, a model cell line employed as a test system to indicate epidermal cytotoxicity and cancer. The compounds of the invention also have antimicrobicidal activity useful in pharmacologic agents for mammals (e.g. the treatment of tuberculosis) as well as in controlling the growth of microorganisms on substrates and in aqueous systems.
摘要翻译：描述了含有叔胺（及其盐），季铵部分或有机聚合物部分的5'取代的4'，5'-二氢补骨脂素化合物（5）。还描述了2-取代的缩水甘油二甲基-2,3-二氢 - 苯并呋喃论坛（7）：还报道了通过迄今为止未知的化合物如3-R-4,8-二甲基-4'，5'-二氢-5'-溴甲基口服或3-R-4,8- 二甲基-4'，5'-二氢-5'-碘甲基肌醇，以制备结构不同的部分还原的补骨脂素和苯并呋喃的阵列。在这些补骨脂素中存在永久铵电荷排除了膜通过，并且单不饱和度排除了核DNA的交联，从而使与补骨脂素衍生疗法长期相关的诱变/致癌副作用最小化。汞功能的存在在这些补骨脂素上提供了具有独特细胞毒性的反应性细胞结合基团，而没有光活化，并且在光活化时增强细胞毒性活性。本发明还涉及这些部分还原和季铵化的补骨脂素，氨基取代的补骨脂素和补骨脂素，对PAM 212角质形成细胞，用作指示表皮细胞毒性和癌症的测试系统的模型细胞系显示令人印象深刻的药理学。本发明的化合物还具有用于哺乳动物的药理学（例如治疗结核病）以及控制底物和水系统中的微生物生长的抗除菌活性。

6. 发明授权

US5356929A Reduced and quaternized psoralens as photo-activated therapeutics 失效
标题翻译：还原和季铵化补骨脂素作为光激活治疗剂
公开(公告)号：US5356929A
公开(公告)日：1994-10-18
申请号：US52660
申请日：1993-04-23
申请人： Ned D. Heindel , Jeffrey D. Laskin
发明人： Ned D. Heindel , Jeffrey D. Laskin
IPC分类号： C07D493/04 , C07D307/77
CPC分类号： C07D493/04
摘要： The invention features phototherapeutic compositions comprising Type 1, Type 2, or Type 3 psoralens and methods of using such compounds for treatment of proliferative diseases of skin, blood and bone marrow.
摘要翻译：本发明的特征在于包含1型，2型或3型补骨脂素的光治疗组合物和使用这些化合物治疗皮肤，血液和骨髓增生性疾病的方法。

7. 发明授权

US4950770A Psoralens aminomethylation 失效
标题翻译：补骨脂素氨基甲基化
公开(公告)号：US4950770A
公开(公告)日：1990-08-21
申请号：US220874
申请日：1988-07-14
申请人： Ned D. Heindel , Mridula D. Choudhuri
发明人： Ned D. Heindel , Mridula D. Choudhuri
IPC分类号： C07D493/04
CPC分类号： C07D493/04
摘要： A direct, acid-catalyzed substitution reaction incorporates an N-phthalimidomethyl group on the 4' or 5' carbon of a psoralen in yields of 60-80% via the condensation of an N-hydroxymethylamide or phthalimide (e.g. N-hydroxymethylphthalimide) and an appropriately substituted psoralen. The phthalimide moiety is cleaved from the psoralen ring by treatment with hydrazine to give 60 to 70% yields of the aminomethylpsoralens.
摘要翻译：直接的酸催化的取代反应通过N-羟甲基酰胺或邻苯二甲酰亚胺（例如N-羟甲基邻苯二甲酰亚胺）的缩合与补骨脂素的4'或5'碳结合，得到60-80％的N-邻苯二甲酰亚氨基甲基，适当取代的补骨脂素。通过用肼处理从补骨脂环中切割邻苯二甲酰亚胺部分，得到60至70％的氨基甲基肉桂酸酯产率。

8. 发明授权

US09422233B2 Vanilloid fatty hydroxamates as therapeutic anti-inflammatory pharmaceuticals 有权
标题翻译：香草酸脂肪异羟肟酸盐作为治疗性抗炎药物
公开(公告)号：US09422233B2
公开(公告)日：2016-08-23
申请号：US13422565
申请日：2012-03-16
申请人： Jeffrey D. Laskin , Ned D. Heindel , Carl Jeffrey Lacey , Abhilash N. Pillai , Marion Gordon , Diane E. Heck
发明人： Jeffrey D. Laskin , Ned D. Heindel , Carl Jeffrey Lacey , Abhilash N. Pillai , Marion Gordon , Diane E. Heck
IPC分类号： A61K31/27 , C07C271/16 , C07C259/06
CPC分类号： C07C271/16 , C07C259/06
摘要： Three unique subtypes of N-hydroxyamides and N-hydroxycarbamates containing both the vanilloid moiety (4-hydroxy-3-methoxybenzyl) and a lipophilic aliphatic moiety. Also disclosed are direct syntheses of these vanilloid fatty hydroxamates. The compounds possess inhibitory activity against the enzymes fatty acid amide hydrolase (FAAH) and matrix metallo-proteinase 9 (MMP-9). In addition, these substances bind to the calcium channel protein TRPV1 and inhibit vesicant-induced inflammation in skin and cornea. The compounds have utility in treating topical or systemic inflammatory processes in the skin and/or eye.
摘要翻译：含有香草酸部分（4-羟基-3-甲氧基苄基）和亲脂性脂肪族部分的N-羟基酰胺和N-羟基氨基甲酸酯的三种独特亚型。还公开了这些香草酸脂肪异羟肟酸酯的直接合成。该化合物对酶脂肪酸酰胺水解酶（FAAH）和基质金属蛋白酶9（MMP-9）具有抑制活性。此外，这些物质结合钙通道蛋白TRPV1并抑制皮肤和角膜中的引发炎症的炎症。该化合物可用于治疗皮肤和/或眼睛中的局部或全身炎症过程。

9. 发明授权

US06177424B1 4′-Substituted-4′,5′-dihydropsoralens and therapeutical uses thereof 失效
标题翻译： 4'-取代-4'，5'-二氢补骨脂素及其治疗用途
公开(公告)号：US06177424B1
公开(公告)日：2001-01-23
申请号：US09450560
申请日：1999-11-30
申请人： Ned D. Heindel , Jeffrey D. Laskin , Marilyn S. Whittemore , Thomas E. McNeel , Christophe Guillon , Diane E. Heck , Robert D. Rapp
发明人： Ned D. Heindel , Jeffrey D. Laskin , Marilyn S. Whittemore , Thomas E. McNeel , Christophe Guillon , Diane E. Heck , Robert D. Rapp
IPC分类号： A61K3137
CPC分类号： C07D493/04
摘要： The invention relates to 4′-substituted-4′,5′-dihydropsoralen compounds of formula(V): In the formula R is hydrogen, a halogen, CN or an acyl group; T is a halogen, CN, a carboalkoxy group NR1R2, or (N+R1R2R3)X−, R1 and R2 are independently a C1-C6 alkyl, or R1 and R2 together with the nitrogen form a 5-8 member heterocyclic ring, or when T is (N+R1R2R3)X−, R1 and R2 together with the nitrogen form a 5-8 member heterocyclic ring or heterocyclic aromatic ring; R3 is hydrogen, a C1-C12 alkyl, or, when R1 and R2 together with the nitrogen form a heterocyclic aromatic ring, R3 is a double bond within the heterocyclic aromatic ring; X− is a halide. In another embodiment, the invention relates to processes for preparing 4′-substituted-4′,5′-dihydropsoralen compounds described above. The compounds of the invention have beneficial pharmaceutical properties and can be used alone or in pharmaceutical compositions used to treat a proliferative skin disorder and to treat microbial infections in a mammal by administering to the mammal an effective amount of a compound of the invention and then irradiating the mammal with ultraviolet light.
摘要翻译：本发明涉及式（Ⅴ）的4'-取代-4'，5'-二氢补骨脂素化合物：式中R是氢，卤素，CN或酰基; T是卤素，CN，烷氧羰基NR1R2或（N + R1R2R3）X-，R1和R2独立地是C1-C6烷基，或R1和R2与氮一起形成5-8元杂环，或当T是（N + R1R2R3）X - 时，R1和R2与氮一起形成5-8元杂环或杂环芳环; R3是氢，C1-C12烷基，或当R1和R2与氮一起形成杂环芳环时，R3是杂环芳环中的双键; X-是卤化物。在另一个实施方案中，本发明涉及制备上述4'-取代-4'，5'-二氢补骨脂素化合物的方法。本发明的化合物具有有益的药物性质，并且可以单独使用或用于治疗增殖性皮肤病症的药物组合物和通过向哺乳动物施用有效量的本发明化合物然后照射而治疗哺乳动物的微生物感染哺乳动物用紫外线照射。

10. 发明授权

US5082964A Selective acetylcholinesterase inhibitors and methods of making and using same 失效
标题翻译：选择性乙酰胆碱酯酶抑制剂及其制备和使用方法
公开(公告)号：US5082964A
公开(公告)日：1992-01-21
申请号：US872677
申请日：1986-06-10
申请人： Ned D. Heindel , Miguel Turizo , Hugh D. Burns , Venkataraman Balasubramanian
发明人： Ned D. Heindel , Miguel Turizo , Hugh D. Burns , Venkataraman Balasubramanian
IPC分类号： C07C69/96
CPC分类号： C07C69/96
摘要： A new group of alpha substituted cresol choline carbonate salts, that act as site-specific, irreversible inhibitors of acetylcholinesterase. A halomethylation method and a halogenation method for producing said alpha substituted cresol choline carbonate salts and analogs thereof. Methods of using the inhibitors as anticholinergic insecticides and to reduce acetylcholinesterase activity levels in organisms with excessive levels of acetylcholinesterase.
摘要翻译：一组新的α取代甲酚胆碱碳酸盐，作为位点特异性，不可逆的乙酰胆碱酯酶抑制剂。用于制备所述α取代的甲酚胆碱碳酸酯盐及其类似物的卤代甲基化方法和卤化方法。将抑制剂用作抗胆碱能杀虫剂并降低乙酰胆碱酯酶水平过高的生物体内乙酰胆碱酯酶活性水平的方法。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式