公开(公告)号：US5786332A

公开(公告)日：1998-07-28

申请号：US400983

申请日：1995-03-06

申请人： Beverly E. Girten ,  Richard A. Houghten ,  Costas C. Loullis ,  Mark J. Suto ,  Ronald R. Tuttle

发明人： Beverly E. Girten ,  Richard A. Houghten ,  Costas C. Loullis ,  Mark J. Suto ,  Ronald R. Tuttle

IPC分类号： A61K38/00 ,  C07K5/087 ,  C07K5/117 ,  C07K7/06 ,  C07K14/68 ,  C07K14/695

CPC分类号： C07K7/06 ,  C07K14/68 ,  C07K14/695 ,  C07K5/0812 ,  C07K5/1024 ,  A61K38/00

摘要： The present invention relates to novel peptides that are potent cytokine restraining agents. In addition, the present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a cytokine restraining agent. Administration of such a cytokine restraining agent to a subject restrains, but does not necessarily suppress, cytokine activity completely. Thus, the present invention provides a method of restraining pathologically elevated cytokine activity in a subject. The invention also provides methods of treating disuse deconditioning and diseases mediated by nitric oxide and cytokines, such as diabetes and glomerulonephritis, a method of organ protection, a method of organ protection, and a method of reducing the negative side effects of cancer chemotherapy, such as nephrotoxicity.

公开(公告)号：US5278317A

公开(公告)日：1994-01-11

申请号：US906260

申请日：1992-06-29

申请人： Susan E. Hagen ,  Mark J. Suto

发明人： Susan E. Hagen ,  Mark J. Suto

IPC分类号： A61K31/435 ,  A61K31/47 ,  A61P31/04 ,  C07D207/06 ,  C07D207/08 ,  C07D207/09 ,  C07D207/14 ,  C07D215/54 ,  C07D401/04 ,  C07D403/04 ,  C07D471/04

CPC分类号： C07D207/08 ,  C07D207/09 ,  C07D401/04 ,  C07D471/04

摘要： Optically pure isomers of 7-[3-(1,1-dialkylmethyl-1-amino)-1-pyrrolidinyl]quinolones and naphthyridones as therapeutically active and safe antibacterial agents are described, as well as pharmaceutical compositions thereof, and a method of treating bacterial infections therewith. Also described is a method of manufacture of the quinolones and naphthyridones as well as the starting materials, the optically pure pyrrolidine moieties for attachment at the 7-position.

摘要翻译： 描述了作为治疗活性和安全的抗菌剂的7- [3-（1,1-二烷基甲基-1-氨基）-1-吡咯烷基]喹诺酮和萘啶酮的光学纯异构体及其药物组合物，以及治疗方法 细菌感染。 还描述了制备喹诺酮和萘啶酮的方法以及起始材料，用于连接在7-位的光学纯的吡咯烷部分。

公开(公告)号：US5157128A

公开(公告)日：1992-10-20

申请号：US730362

申请日：1991-07-15

申请人： Susan E. Hagen ,  Mark J. Suto

发明人： Susan E. Hagen ,  Mark J. Suto

IPC分类号： A61K31/435 ,  A61K31/47 ,  A61P31/04 ,  C07D207/06 ,  C07D207/08 ,  C07D207/09 ,  C07D207/14 ,  C07D215/54 ,  C07D401/04 ,  C07D403/04 ,  C07D471/04

CPC分类号： C07D207/08 ,  C07D207/09 ,  C07D401/04 ,  C07D471/04

摘要： Optically pure isomers of 7-[3-(1,1-dialkylmethyl-1-amino)-1 -pyrrolidinyl[quinolones and naphthyridones as therapeutically active and safe antibacterial agents are described, as well as pharmaceutical compositions thereof, and a method of treating bacterial infections therewith. Also described is a method of manufacture of the quinolones and naphthyridones as well as the starting materials, the optically pure pyrrolidine moieties for attachment at the 7-position.

摘要翻译： 描述了作为治疗活性和安全的抗菌剂的7- [3-（1,1-二烷基甲基-1-氨基）-1-吡咯烷基[喹诺酮和萘啶酮]的光学纯异构体及其药物组合物，以及治疗 细菌感染。 还描述了制备喹诺酮和萘啶酮的方法以及起始材料，用于连接在7-位的光学纯的吡咯烷部分。

公开(公告)号：US5036096A

公开(公告)日：1991-07-30

申请号：US532529

申请日：1990-06-04

申请人： Mark J. Suto

发明人： Mark J. Suto

IPC分类号： C07D233/91 ,  C07D403/06 ,  C07D413/06

CPC分类号： C07D403/06 ,  C07D233/91 ,  C07D413/06

摘要： The present invention is novel aziridino derivatives of nitroimidazoles and pharmaceutical compositions of selected derivatives useful as radiosensitizing or chemosensitizing agents in the treatment of hypoxic tumor cells. Also, the present invention is a novel process for preparing both known and novel aziridino derivatives of nitroimidazoles having novel intermediates.

摘要翻译： 本发明是硝基咪唑的新型氮丙啶衍生物和用作放射增敏剂或化学敏感剂的选定衍生物的药物组合物，用于治疗缺氧性肿瘤细胞。 此外，本发明是制备具有新型中间体的已知和新型硝基咪唑的氮丙啶衍生物的新方法。

公开(公告)号：US4918219A

公开(公告)日：1990-04-17

申请号：US250892

申请日：1989-09-29

申请人： Jagadish C. Sircar ,  Charles F. Schwender ,  Mark J. Suto

发明人： Jagadish C. Sircar ,  Charles F. Schwender ,  Mark J. Suto

IPC分类号： C07C43/174 ,  C07C43/178 ,  C07C43/225 ,  C07C43/23 ,  C07C69/157 ,  C07D473/00

CPC分类号： C07D473/00 ,  C07C43/1745 ,  C07C43/1782 ,  C07C43/1785 ,  C07C43/1788 ,  C07C43/225 ,  C07C43/23

摘要： Novel purine derivatives are described as agents for treating autoimmune diseases as well as a method of manufacture and pharmaceutical compositions as well as novel intermediates in the manufacture thereof.

摘要翻译： 新嘌呤衍生物被描述为用于治疗自身免疫性疾病的药物，以及制造方法和药物组合物以及其制造中的新型中间体。

公开(公告)号：US4677219A

公开(公告)日：1987-06-30

申请号：US886463

申请日：1986-07-17

申请人： Ellen M. Berman ,  Mark J. Suto

发明人： Ellen M. Berman ,  Mark J. Suto

IPC分类号： C07D239/95 ,  A61K20060101 ,  C07C255/00 ,  C07C255/49 ,  C07C255/51 ,  C07C255/58 ,  C07D20060101 ,  C07D239/00 ,  C07D239/84 ,  C07D239/94 ,  C07C121/54 ,  C07C121/52

CPC分类号： C07C255/00

摘要： An improved process for the preparation of 6-substituted-5-alkyl-2,4-quinazolinediamines, useful in the production of trimetrexate and similar antifolate agents, together with several novel intermediates are disclosed.

摘要翻译： 公开了用于制备三甲氧胺和类似抗叶酸剂的6-取代-5-烷基-2,4-喹唑啉二胺的改进方法，以及几种新型中间体。

公开(公告)号：US08058274B2

公开(公告)日：2011-11-15

申请号：US12193639

申请日：2008-08-18

申请人： Thomas Eugene Christos ,  George S. Amato ,  Robert N. Atkinson ,  Maria Graciela Barolli ,  Lilli Ann Wolf-Gouveia ,  Mark J. Suto

发明人： Thomas Eugene Christos ,  George S. Amato ,  Robert N. Atkinson ,  Maria Graciela Barolli ,  Lilli Ann Wolf-Gouveia ,  Mark J. Suto

IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  C07D487/00

CPC分类号： C07D471/04 ,  C07D487/04

摘要： Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.

摘要翻译： 提供了通过电压依赖钾通道调节钾离子通量可用于治疗疾病的化合物，组合物和方法。 更具体地说，本发明提供了可用于治疗中枢性或周围神经系统疾病（例如偏头痛，共济失调，帕金森病，双相情感障碍，三叉神经痛，痉挛状态，情绪障碍，脑肿瘤，精神病症）的杂环，组合物和方法 ，癫痫，癫痫，癫痫，癫痫发作，视网膜变性，听力和视力丧失，阿尔茨海默病，年龄相关记忆丧失，学习缺陷，焦虑，神经元变性和运动神经元疾病，维持膀胱控制或治疗尿失禁）和神经保护剂 （例如，为了预防中风等）通过调节与指示的病症的发作或复发相关的钾通道。

公开(公告)号：US5939421A

公开(公告)日：1999-08-17

申请号：US886198

申请日：1997-07-01

申请人： Moorthy S. S. Palanki ,  Mark J. Suto

发明人： Moorthy S. S. Palanki ,  Mark J. Suto

IPC分类号： C07D241/44 ,  C07D265/22 ,  C07D409/04 ,  C07D413/04 ,  A01N43/54 ,  C07D239/72 ,  C07D471/00

CPC分类号： C07D265/22 ,  C07D241/44 ,  C07D409/04 ,  C07D413/04

摘要： Compounds having utility as anti-inflammatory agents in general and, more specifically, for the prevention and/or treatment of immunoinflammatory and autoimmune diseases are disclosed. The compounds are quinazoline-containing compounds. Methods are also disclosed for preventing and/or treating inflammatory conditions by administering to an animal in need thereof an effective amount of a compound of this invention, preferably in the form of a pharmaceutical composition.

摘要翻译： 一般具有用作抗炎剂的化合物，更具体地，用于预防和/或治疗免疫炎症和自身免疫疾病的化合物被公开。 该化合物是含喹唑啉的化合物。 还公开了通过向有需要的动物施用有效量的本发明化合物，优选以药物组合物的形式，来预防和/或治疗炎性病症的方法。

公开(公告)号：US5364861A

公开(公告)日：1994-11-15

申请号：US132019

申请日：1993-10-05

申请人： Susan E. Hagen ,  Mark J. Suto

发明人： Susan E. Hagen ,  Mark J. Suto

IPC分类号： C07D207/08 ,  C07D207/09 ,  C07D401/04 ,  C07D471/04 ,  A61K31/435 ,  A61K31/47 ,  C07D215/56

CPC分类号： C07D207/08 ,  C07D207/09 ,  C07D401/04 ,  C07D471/04

摘要： Optically pure isomers of 7-[3-(1,1-dialkylmethyl-1-amino)-1-pyrrolidinyl]quinolones and naphthyridones as therapeutically active and safe antibacterial agents are described, as well as pharmaceutical compositions thereof, and a method of treating bacterial infections therewith. Also described is a method of manufacture of the quinolones and naphthyridones as well as the starting materials, the optically pure pyrrolidine moieties for attachment at the 7-position.

摘要翻译： 描述了作为治疗活性和安全的抗菌剂的7- [3-（1,1-二烷基甲基-1-氨基）-1-吡咯烷基]喹诺酮和萘啶酮的光学纯异构体及其药物组合物，以及治疗方法 细菌感染。 还描述了制备喹诺酮和萘啶酮的方法以及起始材料，用于连接在7-位的光学纯的吡咯烷部分。

公开(公告)号：US5256662A

公开(公告)日：1993-10-26

申请号：US943958

申请日：1992-09-11

申请人： John M. Domagala ,  Mark J. Suto ,  William R. Turner

发明人： John M. Domagala ,  Mark J. Suto ,  William R. Turner

IPC分类号： C07D215/56 ,  C07D401/04 ,  C07D487/08 ,  A61K31/495 ,  A61K31/47 ,  C07D401/10

CPC分类号： C07D401/04 ,  C07D215/56 ,  C07D487/08

摘要： Novel 8-alkenyl, alkynyl, allenyl and cycloalkyl-quinolinecarboxylic acids are described as antibacterial agents as well as methods of manufacture including novel intermediates used in said manufacture.

摘要翻译： 新的8-烯基，炔基，烯丙基和环烷基 - 喹啉羧酸被描述为抗菌剂，以及包括在所述制造中使用的新型中间体的制造方法。