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1. 发明授权

US5567411A Dendritic amplifier molecules having multiple terminal active groups stemming from a benzyl core group 失效
标题翻译：树枝状放大器分子具有来自苄基核心基团的多个末端活性基团
公开(公告)号：US5567411A
公开(公告)日：1996-10-22
申请号：US316787
申请日：1994-09-29
申请人： John F. W. Keana , Vladimir Martin , William H. Ralston
发明人： John F. W. Keana , Vladimir Martin , William H. Ralston
IPC分类号： A61K49/18 , A61K49/20 , C07C291/04 , C07F11/00 , A61K49/00 , A61K51/00 , C07C69/80 , C07D207/38 , C07D209/48 , C12N9/96
CPC分类号： A61K49/20 , A61K49/1812 , C07C291/04 , Y10S436/803 , Y10S436/806 , Y10T436/24
摘要： Dendritic derivatives of 3,5-bis(aminomethyl)benzene and aminomethyl benzene core groups are disclosed. In each derivative, termed an "amplifier" because the dendritic structure on each molecule terminates with multiple termini to each of which an "active group" can be attached, the desired effect of the active group per mole is amplified compared to conventional compounds having only one active group per molecule. Amplifier molecules can include a targeting group permitting the molecules to preferentially attach to a particular anatomical or physiological situs. Active groups are any of various pharmacologically or therapeutically active moieties, including moieties useful for magnetic-resonance contrast enhancement. The dendritic structures comprise linkers and branch groups covalently bonded to each other in any of various structural combinations. The amplifiers can be prepared as a solution or mixture with a physiologically compatible carrier for administration to a warm-blooded animal subject. Also disclosed are methods for using the compounds in diagnosis and therapy, such as obtaining a magnetic resonance image of a subject.
摘要翻译：公开了3,5-双（氨基甲基）苯和氨基甲基苯核心的树枝状衍生物。在每个衍生物中，称为“放大器”，因为每个分子上的树突状结构终止于可以连接“活性基团”的每个末端的多个末端，与仅具有仅活性基团的常规化合物相比，活性基团每摩尔的期望效应被扩增每个分子一个活性基团。放大器分子可以包括允许分子优先附着到特定解剖或生理部位的靶向基团。活性基团是各种药理学或治疗活性部分中的任何一种，包括可用于磁共振对比度增强的部分。树枝状结构包括以各种结构组合中的任何一种彼此共价键合的接头和分支基团。放大器可以制备成与生理相容的载体的溶液或混合物，用于给温血动物受试者施用。还公开了在诊断和治疗中使用化合物的方法，例如获得受试者的磁共振图像。

2. 发明授权

US08883775B2 Treatment of hyperproliferative diseases with vinca alkaloid N-oxide analogs 有权
标题翻译：用长春花生物碱N-氧化物类似物治疗过度增殖性疾病
公开(公告)号：US08883775B2
公开(公告)日：2014-11-11
申请号：US13280974
申请日：2011-10-25
申请人： John G. Curd , John F. W. Keana , Alshad S. Lalani , Paul B. Westberg , Bradford Goodwin , W. David Henner
发明人： John G. Curd , John F. W. Keana , Alshad S. Lalani , Paul B. Westberg , Bradford Goodwin , W. David Henner
IPC分类号： A61K31/55 , A61K31/435 , C07D519/04
CPC分类号： C07D519/04
摘要： The present invention relates to vinca alkaloid and analog N-oxides having activity for treating hyperproliferative disorders. Further, the invention relates to pharmaceutical compositions and methods of using vinca alkaloid and analog N-oxides, alone or in combination with one or more other active agents or treatments, to treat hyperproliferative disorders.
摘要翻译：本发明涉及具有用于治疗过度增殖性疾病的活性的长春花生物碱和类似物N-氧化物。此外，本发明涉及使用长春花生物碱和类似物N-氧化物的药物组合物和方法，其单独或与一种或多种其它活性剂或治疗剂组合以治疗过度增殖性疾病。

3. 发明授权

US08048872B2 Treatment of hyperproliferative diseases with vinca alkaloid N-oxide and analogs 有权
标题翻译：用长春花生物碱N-氧化物和类似物治疗过度增殖性疾病
公开(公告)号：US08048872B2
公开(公告)日：2011-11-01
申请号：US12111672
申请日：2008-04-29
申请人： John G. Curd , John F. W. Keana , Alshad S. Lalani , Paul B. Westberg , Bradford Goodwin , W. David Henner
发明人： John G. Curd , John F. W. Keana , Alshad S. Lalani , Paul B. Westberg , Bradford Goodwin , W. David Henner
IPC分类号： A61K31/33 , C07D487/22
CPC分类号： C07D519/04
摘要： The present invention relates to vinca alkaloid and analog N-oxides having activity for treating hyperproliferative disorders. Further, the invention relates to pharmaceutical compositions and methods of using vinca alkaloid and analog N-oxides, alone or in combination with one or more other active agents or treatments, to treat hyperproliferative disorders.
摘要翻译：本发明涉及具有用于治疗过度增殖性疾病的活性的长春花生物碱和类似物N-氧化物。此外，本发明涉及使用长春花生物碱和类似物N-氧化物的药物组合物和方法，其单独或与一种或多种其它活性剂或治疗剂组合以治疗过度增殖性疾病。

4. 发明授权

US07557251B2 Production of gossypol co-crystals 有权
标题翻译：生产棉酚共晶体
公开(公告)号：US07557251B2
公开(公告)日：2009-07-07
申请号：US11729638
申请日：2007-03-29
申请人： Shaomeng Wang , Jianyong Chen , John F. W. Keana , Ming Guo
发明人： Shaomeng Wang , Jianyong Chen , John F. W. Keana , Ming Guo
IPC分类号： C07C39/12 , C07C39/38 , C07C39/10 , C07C53/08
CPC分类号： C07B57/00 , A61K31/192 , A61K31/78 , C07C45/516 , C07C45/79 , C07C45/85 , C07C47/57 , C07C51/487 , C07C53/08
摘要： This invention relates to relates to methods for producing gossypol acetic acid co-crystals and (−)-gossypol acetic acid co-crystals. The invention also relates to pharmaceutical compositions comprising gossypol acetic acid co-crystals and (−)-gossypol acetic acid co-crystals and the use of gossypol acetic acid co-crystals and (−)-gossypol acetic acid co-crystals for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.
摘要翻译：本发明涉及生产棉酚乙酸共晶体和（ - ） - 棉酚乙酸共晶体的方法。本发明还涉及包含棉酚乙酸共晶和（ - ） - 棉酚乙酸共晶体的药物组合物，以及使用棉酚乙酸共晶体和（ - ） - 棉酚乙酸共晶体诱导细胞凋亡细胞和致敏细胞诱导凋亡细胞死亡。

5. 发明授权

US06534525B1 2-substituted piperidine analogs and their use as subtype-selective NMDA receptor antagonists 失效
标题翻译： 2-取代的哌啶类似物及其作为亚型选择性NMDA受体拮抗剂的用途
公开(公告)号：US06534525B1
公开(公告)日：2003-03-18
申请号：US09598162
申请日：2000-06-21
申请人： Christopher F. Bigge , John F. W. Keana , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Anthony P. Guzikowski
发明人： Christopher F. Bigge , John F. W. Keana , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Anthony P. Guzikowski
IPC分类号： A61K31445
CPC分类号： C07D401/12 , A61K31/445 , A61K31/454 , C07D211/14
摘要： Novel 2-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 2-substituted piperidine analogs as selectively active antagonist of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headaches, chronics pain, glaucoma, CMV retinitis, psychosis, urinary incontinence, opioid tolerance or withdrawal, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.
摘要翻译：新的2-取代的哌啶类似物，含有它们的药物组合物和使用2-取代的哌啶类似物作为N-甲基-D-天冬氨酸（NMDA）受体亚型的选择性活性拮抗剂的方法，用于治疗诸如中风，脑缺血，中枢神经系统创伤，低血糖症，焦虑症，抽搐，氨基糖苷类抗生素诱发的听力损失，偏头痛，脊髓痛，青光眼，CMV视网膜炎，精神病，尿失禁，阿片样物质耐受或戒断，或神经退行性疾病，如幻影，阿尔茨海默病，帕金森综合征并描述亨廷顿氏病。

6. 发明授权

US06251948B1 Tri-and tetra-substituted guanidines and their use as excitatory amino acid antagonists 失效
标题翻译：三取代和四取代的胍和它们作为兴奋性氨基酸拮抗剂的用途
公开(公告)号：US06251948B1
公开(公告)日：2001-06-26
申请号：US08468028
申请日：1995-06-06
申请人： Eckard Weber , John F. W. Keana
发明人： Eckard Weber , John F. W. Keana
IPC分类号： A61K31155
CPC分类号： B41J2/471 , A61K31/155 , C07C279/18 , C07D311/18 , G03G15/1675 , G03G15/168 , G03G2215/1614 , G03G2215/1657
摘要： Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.
摘要翻译：表现出对苯环利定（PCP）受体的高结合亲和力，更优选对大脑σ受体的低亲和力的三取代和四取代胍基。这些胍衍生物通过作为NMDA受体 - 离子通道复合物的离子通道的阻断剂，作为NMDA受体的谷氨酸诱导反应的非竞争性抑制剂。因此，这些化合物发挥神经保护活性，并且可用于治疗缺氧，低血糖，脑或脊髓缺血以及脑或脊髓创伤中的神经元损失，以及用于治疗癫痫，阿尔茨海默病，肌萎缩性侧索硬化症，帕金森病，亨廷顿舞蹈病，唐氏综合征，柯萨科夫病和其他神经退行性疾病。

7. 发明授权

US06184210B2 Dipeptide apoptosis inhibitors and the use thereof 有权
标题翻译：二肽凋亡抑制剂及其用途
公开(公告)号：US06184210B2
公开(公告)日：2001-02-06
申请号：US09270736
申请日：1999-03-16
申请人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe
发明人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe
IPC分类号： A61K3805
CPC分类号： C07D233/64 , A61K38/00 , C07C237/22 , C07C271/22 , C07C323/60 , C07D277/16 , C07K5/06191 , C12N2810/40 , Y10S514/885
摘要： The present invention is directed to novel dipeptides thereof, represented by the general Formula I: where R1-R3 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
摘要翻译：本发明涉及其由通式I表示的新型二肽：其中R1-R3和AA在本文中定义。本发明涉及发现具有式I的化合物是凋亡性细胞死亡的有效抑制剂。因此，本发明的抑制剂可以在发生细胞，组织或整个器官的损失的各种临床病症中阻滞或阻断细胞死亡。

8. 发明授权

US06124323A 4-substituted piperidine analogs and their use as subtype selective NMDA receptor antagonists 失效
标题翻译： 4-取代的哌啶类似物及其作为亚型选择性NMDA受体拮抗剂的用途
公开(公告)号：US06124323A
公开(公告)日：2000-09-26
申请号：US091598
申请日：1998-09-16
申请人： Christopher F. Bigge , Po-Wai Yuen , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Zhang-Lin Zhou , John F. W. Keana , Anthony P. Guzikowski
发明人： Christopher F. Bigge , Po-Wai Yuen , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Zhang-Lin Zhou , John F. W. Keana , Anthony P. Guzikowski
IPC分类号： C07D211/14 , C07D211/18 , C07D211/22 , C07D211/28 , C07D211/30 , C07D211/38 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D417/12 , C07D487/04 , A01N43/40 , C07D211/20 , C07D211/26 , C07D211/60
CPC分类号： C07D401/04 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/28 , C07D211/30 , C07D211/38 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/64 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D417/12 , C07D487/04
摘要： Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs are selective active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, psychosis, anxiety, migraine headaches, glaucoma, CMV retinitis, aminoglycoside antibiotics-induced hearing loss, convulsions, chronic pain, opioid tolerance or withdrawal, urinary incontinence or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.
摘要翻译： PCT No.PCT / US96 / 20872 Sec。 371日期：1998年9月16日 102（e）1998年9月16日PCT PCT 1996年12月20日PCT公布。第WO97 / 23216号公报日期1997年7月3日新颖的4-取代的哌啶类似物，含有它们的药物组合物和使用4-取代的哌啶类似物的方法是N-甲基-D-天冬氨酸（NMDA）受体亚型的选择性活性拮抗剂，用于治疗诸如中风，脑缺血，中枢神经系统创伤，低血糖症，精神病，焦虑症，偏头痛，青光眼，CMV视网膜炎，氨基糖苷类抗生素诱发的听力损失，惊厥，慢性疼痛，阿片样物质耐受或戒断，尿失禁或神经退行性疾病，如幻影，描述了阿尔茨海默病，帕金森综合征和亨廷顿氏病。

9. 发明授权

US5597922A Glycine receptor antagonist pharmacophore 失效
标题翻译：甘氨酸受体拮抗剂药效团
公开(公告)号：US5597922A
公开(公告)日：1997-01-28
申请号：US281995
申请日：1994-07-29
申请人： Sui X. Cai , John F. W. Keana , Eckard Weber
发明人： Sui X. Cai , John F. W. Keana , Eckard Weber
IPC分类号： A61K31/404 , A61K31/4184 , A61K31/47 , A61K31/4704 , A61K31/498 , A61K31/5025 , A61K31/517 , A61K31/536 , A61K31/538 , A61K31/55 , A61K31/551 , A61K31/553 , C07B59/00 , C07D209/34 , C07D209/38 , C07D215/22 , C07D215/227 , C07D215/38 , C07D223/16 , C07D235/26 , C07D235/28 , C07D241/38 , C07D241/44 , C07D241/52 , C07D243/24 , C07D245/06 , C07D265/26 , C07D265/36 , C07F5/02 , A61K31/495 , A61K31/535
CPC分类号： C07D215/227 , A61K31/404 , A61K31/4184 , A61K31/47 , A61K31/4704 , A61K31/498 , A61K31/5025 , A61K31/517 , A61K31/536 , A61K31/538 , A61K31/55 , A61K31/551 , A61K31/553 , C07B59/002 , C07D209/34 , C07D209/38 , C07D215/22 , C07D215/38 , C07D223/16 , C07D235/26 , C07D235/28 , C07D241/38 , C07D241/44 , C07D241/52 , C07D243/24 , C07D245/06 , C07D265/26 , C07D265/36 , C07F5/02 , C07F5/025
摘要： Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions and inducing anesthesia are disclosed by administering to an animal in need of such treatment a compound which has high binding to the glycine receptor.
摘要翻译：治疗或预防与中风，缺血，CNS创伤，低血糖和手术相关的神经元损失以及治疗神经变性疾病包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病和唐氏综合征的治疗或预防方法，治疗或预防多动症的不良后果通过向需要这种治疗的动物施用与甘氨酸受体具有高结合性的化合物来公开兴奋性氨基酸以及治疗焦虑症，慢性疼痛，抽搐和诱导麻醉。

10. 发明授权

US5552443A Substituted amidines having high binding to the sigma receptor and the use thereof 失效
标题翻译：具有与σ受体结合高的取代脒基及其用途
公开(公告)号：US5552443A
公开(公告)日：1996-09-03
申请号：US183507
申请日：1994-01-18
申请人： John F. W. Keana , Eckard Weber
发明人： John F. W. Keana , Eckard Weber
IPC分类号： A61K51/04 , C07C257/14 , C07C257/16 , C07C257/18 , A61K31/155
CPC分类号： C07C257/14 , A61K51/0406 , A61K2121/00 , C07B2200/05 , C07C2101/14 , C07C2102/42 , C07C2103/74
摘要： N,N'-disubstituted-amidines, e.g., of the formula ##STR1## wherein R, R' and R" are substituted or unsubstituted hydrocarbon and/or heterocyclic groups.Methods are provided for the treatment or prophylaxis of anxiety in an animal for treating psychosis, and for treating hypertension by administering an effective amount of an N,N'-disubstituted amidine which, preferably, has a high affinity for the sigma receptor.
摘要翻译： N，N'-二取代的脒，例如下式：其中R，R'和R“是取代或未取代的烃和/或杂环基团。提供了用于治疗或预防动物用于治疗精神病的焦虑症和通过施用有效量的N，N'-二取代的脒治疗高血压的方法，其优选地对σ受体具有高亲和力。

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