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11. 发明授权

US5286739A Parenteral formulations for the inhibition of systemic hypotension associated with nitric oxide production or endothelial derived relaxing factor 失效
标题翻译：用于抑制与一氧化氮产生或内皮衍生的松弛因子相关的全身性低血压的肠胃外制剂
公开(公告)号：US5286739A
公开(公告)日：1994-02-15
申请号：US767265
申请日：1991-09-27
申请人： Robert G. Kilbourn , Owen W. Griffith , Steven S. Gross
发明人： Robert G. Kilbourn , Owen W. Griffith , Steven S. Gross
IPC分类号： A61K31/415 , A61K31/715 , A61K38/04 , A61K38/19 , A61K31/195
CPC分类号： A61K31/715 , A61K31/415 , Y10S514/921 , Y10S514/929
摘要： An anti-hypotensive formulation comprising an essentially arginine-free or low arginine (less than about 0.1%, most preferably, about 0.01%) containing mixture of amino acids is provided. The invention in particular embodiments of the anti-hypotensive formulation includes ornithine, citrulline or both. A method for prophylaxis and treatment of systemic hypotension in an animal is provided. Most particularly, a method for treating hypotension caused by nitric oxide synthesis through administering a low or essentially arginine-free parenteral formulation to an animal, so as to reduce or eliminate nitric oxide synthesis is described. A method for treating an animal in septic shock is also disclosed, comprising administering to the animal an anti-hypotensive formulation comprising a mixture of amino acids, which is essentially arginine free. Prophylaxis or treatment of systemic hypotension, particularly that hypotension incident to chemotherapeutic treatment with biologic response modifiers, such as tumor necrosis factor or interleukin-1 or -2, may be accomplished through the administration of the defined anti-hypotensive formulations until physiologically acceptable systolic blood pressure levels are achieved in the animal. Treatment of an animal for septic shock induced by endotoxin may also be accomplished by administering to the animal the arginine-free formulations described.
摘要翻译：提供包含基本上不含精氨酸或低精氨酸（小于约0.1％，最优选约0.01％）的包含氨基酸混合物的抗低血压制剂。本发明在抗低血压制剂的具体实施方案中包括鸟氨酸，瓜氨酸或两者。提供了一种预防和治疗动物体内低血压的方法。最特别地，描述了一种通过向动物施用低或基本上不含精氨酸的肠胃外制剂以治疗由一氧化氮合成引起的低血压以减少或消除一氧化氮合成的方法。还公开了一种用于治疗脓毒性休克的动物的方法，包括向动物施用包含基本上不含精氨酸的氨基酸混合物的抗低血压制剂。预防或治疗全身性低血压，特别是生物反应调节剂如肿瘤坏死因子或白细胞介素-1或-2的化学治疗引起的低血压可以通过给予定义的抗低血压制剂直至生理学上可接受的收缩血在动物体内实现压力水平。内毒素引起的脓毒性休克动物的治疗也可以通过向动物施用所述的不含精氨酸的制剂来实现。

12. 发明授权

US5028627A Method of using arginine derivatives to inhibit systemic hypotension associated with nitric oxide production or endothelial derived relaxing factor 失效
标题翻译：使用精氨酸衍生物抑制与一氧化氮产生或内皮衍生松弛因子相关的全身性低血压的方法
公开(公告)号：US5028627A
公开(公告)日：1991-07-02
申请号：US406909
申请日：1989-09-13
申请人： Robert G. Kilbourn , Steven Gross , Roberto Levi , Owen W. Griffith
发明人： Robert G. Kilbourn , Steven Gross , Roberto Levi , Owen W. Griffith
IPC分类号： A61K31/00 , A61K31/195 , A61K31/198 , A61K31/223 , A61K38/00 , A61K38/21 , A61K45/00 , A61P9/02 , A61P43/00
CPC分类号： A61K31/00 , A61K31/195 , A61K31/198 , A61K31/223 , Y10S514/93
摘要： A method for prophylaxis of treatment of an animal for systemic hypotension induced by internal nitrogen oxide production. The method involves administering a therapeutically effective amount of certain arginine derivatives to inhibit nitrogen oxide formation from arginine. Preferaby N.sup.G -substituted arginine or an N.sup.G,N.sup.G -disubstituted arginine (having at least one hydrogen on a terminal guanidino amino group replaced by another atomic species) is administered to an animal possibly developing or already having induced systemic hypotension. The arginine derivatives are preferably of the L configuration and include pharmaceutically acceptable addition salts. Prophylaxis or treatment or systemic hypotension in a patient which has been induced by chemotherapeutic treatment with biologic response modifiers such as tumor necrosis factor or interleukin-2 may be accomplished. Treatment of an animal for systemic hypotension induced by endotoxin, i.e., septic shock may also be accomplished by treatment with the arginine derivatives.
摘要翻译：一种用于预防由内部氮氧化物产生引起的全身性低血压的动物治疗的方法。该方法包括施用治疗有效量的某些精氨酸衍生物以抑制由精氨酸形成的氮氧化物。优选NG取代的精氨酸或NG，NG-二取代精氨酸（在由另一种原子物质取代的末端胍基氨基上具有至少一个氢）向可能发展或已经具有诱导的全身性低血压的动物施用。精氨酸衍生物优选为L构型，并且包括药学上可接受的加成盐。可以通过用生物反应调节剂如肿瘤坏死因子或白细胞介素-2进行化学治疗诱导的患者中的预防或治疗或全身性低血压。由内毒素引起的系统性低血压的治疗，即败血性休克也可以通过用精氨酸衍生物进行治疗来实现。

13. 发明授权

US5663364A Heme binding compounds and use thereof 失效
标题翻译：血红素结合化合物及其用途
公开(公告)号：US5663364A
公开(公告)日：1997-09-02
申请号：US550645
申请日：1995-10-31
申请人： Owen W. Griffith , Krishnaswamy Narayanan
发明人： Owen W. Griffith , Krishnaswamy Narayanan
IPC分类号： C07D333/20 , A61K31/18 , A61K31/195 , A61K31/198 , A61P9/00 , A61P25/00 , A61P37/06 , A61P43/00 , C07C281/16 , C07C323/25 , C07C335/04 , C07C335/08 , C07D233/64 , C07D333/22 , C07D207/335
CPC分类号： C07C335/08 , C07D333/22
摘要： Inhibitors of nitric oxide formation from arginine useful for treating hypotension, inflammation, stroke and to restore vascular contractile sensitivity to the effects of .alpha..sub.1 adrenergic agonists are physiologically active compounds including N.sup..delta. -substituted ornithine or N.sup..epsilon. -substituted lysine moieties or monoalkyl carbon-substituted N.sup..delta. -substituted ornithine or N.sup..epsilon. -substituted lysine moieties, having the formula ##STR1## wherein R is (CH.sub.2).sub.y CH.sub.3 or H, R' is CH.sub.2 or C(H)(CH.sub.2).sub.y CH.sub.3, and R" is CH.sub.2 or C(H)(CH.sub.2).sub.y CH.sub.3, with y ranging from 0 to 5, and x is 0 or 1 and wherein none or only one of R, R' and R" provides an alkyl substituent on ornithine or lysine moiety, and wherein Q is a heme binding moiety and/or a sulfur-containing binding moiety and Q' is --NH.sub.2 when there is a double bond between the omega carbon and Q and Q' is .dbd.NH when there is a single bond between the omega carbon and Q, and physiologically acceptable acid addition salts thereof.
摘要翻译：用于治疗低血压，炎症，中风和恢复对α1肾上腺素能激动剂的作用的血管收缩敏感性的精氨酸形成一氧化氮的抑制剂是生理活性化合物，包括N-3取代的鸟氨酸或Nε-取代的赖氨酸部分或单烷基碳 - 其中R是（CH 2）y CH 3或H，R'是CH 2或C（H）（CH 2）y CH 3，R“是CH 2 或C（H）（CH 2）y CH 3，y在0至5之间，x是0或1，并且其中R，R'和R“中没有一个或只有一个在鸟氨酸或赖氨酸部分上提供烷基取代基，其中当ω-碳和Q之间存在双键时，Q是血红素结合部分和/或含硫结合部分，Q'是-NH 2，并且当ω碳之间存在单键时，Q'为= NH 和Q，及其生理上可接受的酸加成盐。

14. 发明授权

US5523084A Enhancing the anti-tumor effect of melphalan by prior administration of L-amino acid oxidase with or without intermediate administration of anti-L-amino acid oxidase antibody 失效
标题翻译：通过事先给予L-氨基酸氧化酶，在或不加中间施用抗L-氨基酸氧化酶抗体的情况下，增强美法仑的抗肿瘤作用
公开(公告)号：US5523084A
公开(公告)日：1996-06-04
申请号：US301769
申请日：1994-09-07
申请人： Darell D. Bigner , Henry S. Friedman , Owen W. Griffith
发明人： Darell D. Bigner , Henry S. Friedman , Owen W. Griffith
IPC分类号： A61K38/44 , A61K37/48 , A61K31/195 , A61K37/50 , A61K39/395
CPC分类号： A61K38/44
摘要： L-amino acid oxidase is utilized to reduce plasma level of large neutral amino acids to allow the opportunity of increased melphalan transport into tumors and melphalan is administered when the plasma level of L-amino acid oxidase is sufficiently low so the gain from increased transport outweighs the loss from L-amino acid oxidase-mediated metabolism of melphalan. Preferably anti L-amino acid oxidase antibody is administered intermediate the L-amino acid oxidase and melphalan administrations to deplete L-amino acid oxidase activity once the L-amino acid oxidase has caused the melphalan transport improving plasma level reduction of large neutral amino acids thereby to reduce or eliminate degrading of melphalan by L-amino acid oxidase.
摘要翻译： L-氨基酸氧化酶被用于降低大中性氨基酸的血浆水平，以便当L-氨基酸氧化酶的血浆水平足够低时，给予美法仑输送到肿瘤中并且美法仑的机会被施用，因此增加运输的增益超过来自L-氨基酸氧化酶介导的美法仑代谢的损失。优选地，抗L-氨基酸氧化酶抗体在L-氨基酸氧化酶和美法仑给药之间施用，以在L-氨基酸氧化酶引起美法仑输送改善大中性氨基酸的血浆水平降低后消耗L-氨基酸氧化酶活性，从而通过L-氨基酸氧化酶降低或消除美法仑降解。

15. 发明授权

US5273875A N.sup.6 -(hydrazinoiminomethyl)lysine and method of inhibiting nitric oxide formation in body 失效
标题翻译： N6-（肼基亚氨基甲基）赖氨酸和抑制体内一氧化氮形成的方法
公开(公告)号：US5273875A
公开(公告)日：1993-12-28
申请号：US865060
申请日：1992-04-08
申请人： Owen W. Griffith
发明人： Owen W. Griffith
IPC分类号： C07C281/16 , C12N5/00 , A01N1/02
CPC分类号： C07C281/16
摘要： Physiologically active N.sup.6 -(hydrazinoiminomethyl)lysine or pharmaceutically acceptable acid addition salt thereof is administered in a nitric oxide synthesis inhibiting amount to a subject in need of such inhibition (e.g., a subject with low blood pressure, e.g., due to sepsis or to therapeutic administration of cytokines, or needing immunosuppressive effect) or is added to a medium containing isolated organs, intact cells, cell homogenates or tissue homogenates in an amount sufficient to inhibit nitric oxide formation to elucide or control the biosynthesis, metabolism or physiological role of nitric oxide. CompThis invention was made at least in part with Government support under National Institutes of Health grant number DK 37116. The Government has certain rights in the invention.
摘要翻译：生理活性N6-（肼基亚氨基甲基）赖氨酸或其药学上可接受的酸加成盐以一氧化氮合成抑制量施用于需要这种抑制的受试者（例如，低血压受试者，例如由于败血症或治疗性或需要免疫抑制作用），或加入含有足以抑制一氧化氮形成以分离或控制一氧化氮的生物合成，代谢或生理作用的量的分离器官，完整细胞，细胞匀浆或组织匀浆的培养基。与已知的一氧化氮合成抑制剂相比，N6-（肼基亚氨基甲基）赖氨酸及其酸加成盐对一氧化氮合酶的诱导型异构体显示出比对一氧化氮合酶的组成型异构体更大的相对活性。 N6-（肼基亚氨基甲基）赖氨酸及其药学上可接受的酸加成盐的含量远低于NG-氨基精氨酸及其药学上可接受的酸加成盐。

16. 发明授权

US06359004B1 Manipulating nitrosative stress to upregulate nitrosative stress defenses 失效
标题翻译：控制亚硝化压力以上调亚硝酸胁迫防御
公开(公告)号：US06359004B1
公开(公告)日：2002-03-19
申请号：US09690989
申请日：2000-10-18
申请人： Jonathan S. Stamler , Owen W. Griffith
发明人： Jonathan S. Stamler , Owen W. Griffith
IPC分类号： A61K31195
CPC分类号： A61K31/00 , A61K31/195 , A61K31/255 , C07C381/10 , Y02A50/473
摘要： Mammals are treated for infections or for conditions associated with pathologically proliferating mammalian cell growth (for example, certain cancers, restenosis, benign prostatic hypertrophy) by administration of a manipulator of nitrosative stress to selectively kill or reduce the growth of the microbes or helminths causing the infection or of host cells infected with the microbes or of the pathologically proliferating mammalian cells. Novel agents include &agr;-alkyl-S-alkyl-homocysteine sulfoximines wherein the &agr;-alkyl contains 2 to 8 carbon atoms, and the S-alkyl- contains 1 to 10 carbon atoms. In another invention herein, mammals in need of increased nitrosative stress defenses are treated, e.g., humans at risk for a stroke because of having had a transient ischemic attack, are treated. Treatments to increase nitrosative stress defenses include, for example, repeated administrations of low doses of manipulators of nitrosative stress so that the subject treated has increased tolerance to nitrosative stress. In still another invention, mammals are treated for protozoal infections by systemic administration of L-buthionine-S-sulfoximine and agent that increases nitrosative stress.
摘要翻译：哺乳动物通过施用亚硝化应激的机械手来治疗感染或与病理性增殖的哺乳动物细胞生长（例如某些癌症，再狭窄，良性前列腺肥大）相关的病症，以选择性地杀死或减少微生物或蠕虫的生长，从而导致感染或用微生物或病理增殖的哺乳动物细胞感染的宿主细胞。新型药剂包括α-烷基-S-烷基 - 高半胱氨酸亚砜，其中α-烷基含有2-8个碳原子，并且S-烷基含有1-10个碳原子。在本文的另一发明中，需要治疗需要增加的亚硝酸应激防御的哺乳动物被治疗，例如由于具有短暂性脑缺血发作而处于卒中风险的人。增加亚硝化应激防御的治疗包括例如重复施用低剂量的亚硝化应激的操纵者，使得所治疗的受试者具有增加的对亚硝化应激的耐受性。在另一个发明中，哺乳动物通过全身施用L-丁硫氨酸-S-亚磺酰亚胺和增加亚硝化压力的试剂来治疗原生动物感染。

17. 发明授权

US06180824B2 Manipulating nitrosative stress to kill pathologic microbes, pathologic helminths and pathologically, proliferating cells or to upregulate nitrosative stress defenses 有权
标题翻译：控制亚硝化压力以杀死病理微生物，病理性蠕虫和病理性增殖细胞或上调亚硝化应激防御
公开(公告)号：US06180824B2
公开(公告)日：2001-01-30
申请号：US09361167
申请日：1999-07-27
申请人： Jonathan S. Stamler , Owen W. Griffith
发明人： Jonathan S. Stamler , Owen W. Griffith
IPC分类号： C07C6108
CPC分类号： A61K31/00 , A61K31/195 , A61K31/255 , C07C381/10 , Y02A50/473
摘要： Mammals are treated for infection or for conditions associated with pathologically proliferating mammalian cell growth (for example, certain cancers, restenosis, benign prostatic hypertrophy) by administration of a manipulator of nitrosative stress to selectively kill or reduce the growth of the microbes or helminths causing the infection or of host cells infected with the microbes or of the pathologically proliferating mammalian cells. Novel agents include &agr;-alkyl-S-alkyl-homocysteine sulfoximines wherein the &agr;-alkyl contains 2 to 8 carbon atoms, and the S-alkyl- contains 1 to 10 carbon atoms. In another invention herein, mammals in need of increased nitrosative stress defenses are treated, e.g., humans at risk for a stroke because of having had a transient ischemic attack, are treated. Treatments to increase nitrosative stress defenses include, for example, repeated administrations of low doses of manipulators of nitrosative stress so that the subject treated has increased tolerance to nitrosative stress. In still another invention, mammals are treated for protozoal infections by systemic administration of L-buthionine-S-sulfoximine and agent that increases nitrosative stress.
摘要翻译：哺乳动物通过施用亚硝化胁迫的操纵者来治疗感染或与病理增殖的哺乳动物细胞生长（例如某些癌症，再狭窄，良性前列腺肥大）相关的病症，以选择性地杀死或减少微生物或蠕虫的生长，从而导致感染或用微生物或病理增殖的哺乳动物细胞感染的宿主细胞。新型药剂包括α-烷基-S-烷基 - 高半胱氨酸亚砜，其中α-烷基含有2-8个碳原子，并且S-烷基含有1-10个碳原子。在本文的另一发明中，需要治疗需要增加的亚硝酸应激防御的哺乳动物被治疗，例如由于具有短暂性脑缺血发作而处于卒中风险的人。增加亚硝化应激防御的治疗包括例如重复施用低剂量的亚硝化应激的操纵者，使得所治疗的受试者具有增加的对亚硝化应激的耐受性。在另一个发明中，哺乳动物通过全身施用L-丁硫氨酸-S-亚磺酰亚胺和增加亚硝化压力的试剂来治疗原生动物感染。

18. 发明授权

US6057367A Manipulating nitrosative stress to kill pathologic microbes, pathologic helminths and pathologically proliferating cells or to upregulate nitrosative stress defenses 失效
标题翻译：控制亚硝化压力以杀死病理微生物，病理蠕虫和病理增殖细胞或上调亚硝酸胁迫防御
公开(公告)号：US6057367A
公开(公告)日：2000-05-02
申请号：US852490
申请日：1997-05-07
申请人： Jonathan S. Stamler , Owen W. Griffith
发明人： Jonathan S. Stamler , Owen W. Griffith
IPC分类号： A61K31/00 , A61K31/195 , A61K31/255 , C07C381/10
CPC分类号： A61K31/00 , A61K31/195 , A61K31/255 , C07C381/10
摘要： Mammals are treated for infections or for conditions associated with pathologically proliferating mammalian cell growth (for example, certain cancers, restenosis, benign prostatic hypertrophy) by administration of a manipulator of nitrosative stress to selectively kill or reduce the growth of the microbes or helminths causing the infection or of host cells infected with the microbes or of the pathologically proliferating mammalian cells. Novel agents include .alpha.-alkyl-S-alkyl-homocysteine sulfoximines wherein the .alpha.-alkyl contains 2 to 8 carbon atoms, and the S-alkyl-contains 1 to 10 carbon atoms. In another invention herein, mammals in need of increased nitrosative stress defenses are treated, e.g., humans at risk for a stroke because of having had a transient ischemic attack, are treated. Treatments to increase nitrosative stress defenses include, for example, repeated administrations of low doses of manipulators of nitrosative stress so that the subject treated has increased tolerance to nitrosative stress. In still another invention, mammals are treated for protozoal infections by systemic administration of L-buthionine-S-sulfoximine and agent that increases nitrosative stress.
摘要翻译：哺乳动物通过施用亚硝化胁迫的机械手来治疗感染或与病理性增殖的哺乳动物细胞生长（例如某些癌症，再狭窄，良性前列腺肥大）相关的病症，以选择性地杀死或减少微生物或蠕虫的生长，从而导致感染或用微生物或病理增殖的哺乳动物细胞感染的宿主细胞。新型试剂包括α-烷基-S-烷基 - 高半胱氨酸亚砜，其中α-烷基含有2-8个碳原子，并且S-烷基含有1-10个碳原子。在本文的另一发明中，需要治疗需要增加的亚硝酸应激防御的哺乳动物被治疗，例如由于具有短暂性脑缺血发作而处于卒中风险的人。增加亚硝化应激防御的治疗包括例如重复施用低剂量的亚硝化应激的操纵者，使得所治疗的受试者具有增加的对亚硝化应激的耐受性。在另一个发明中，哺乳动物通过全身施用L-丁硫氨酸-S-亚磺酰亚胺和增加亚硝化压力的试剂来治疗原生动物感染。

19. 发明授权

US5453441A Substituted arginines and substituted homoarginines and use thereof 失效
标题翻译：取代的精氨酸和取代的高精氨酸及其用途
公开(公告)号：US5453441A
公开(公告)日：1995-09-26
申请号：US328956
申请日：1994-10-24
申请人： Owen W. Griffith
发明人： Owen W. Griffith
IPC分类号： A61K31/195 , A61K31/198 , A61P9/02 , A61P43/00 , C07C279/14 , C07C279/36 , C07C281/16
CPC分类号： A61K31/195 , C07C279/14 , C07C279/36 , C07C281/16
摘要： Guanidino substituted arginines or homoarginines based on monoalkyl carbon-substituted ornithines or lysines, having the formula ##STR1## wherein R is (CH.sub.2).sub.y CH.sub.3 or H, R' is CH.sub.2 or C(H)(CH.sub.2).sub.y CH.sub.3, and R" is CH.sub.2 or C(H)(CH.sub.2).sub.y CH.sub.3, with y ranging from 0 to 5, and x is 0 or 1 and Q is an alkyl group containing from 1 to 6 carbon atoms or NH.sub.2 or NO.sub.2, and only one of R, R' and R" providing an alkyl substituent on the ornithine or lysine moiety. Preferred compounds are .alpha.-methyl-N.sup..omega. -methyl-DL-arginine, RS-.beta.-methyl-N.sup..omega. -methyl-DL-arginine, RS-.gamma.-methyl-N.sup..omega. -methyl-DL-arginine, .alpha.-methyl-N.sup..omega. -amino-DL-arginine, RS-.beta.-methyl-N.sup..omega. -amino-DL-arginine, RS-.gamma.-methyl-N.sup..omega. -amino-DL-arginine, .alpha.-methyl-N.sup..omega. -nitro-DL-arginine, RS-.beta.-methyl-N.sup..omega. -nitro-DL-arginine, and RS-.gamma.-methyl-N.sup..omega. -nitro-DL-arginine. A composition includes said compound together with a pharmaceutically acceptable carrier. Methods of use are directed to delivering said compound to inducible nitric oxide synthase to inhibit the ability of the enzyme to catalyze the conversion of arginine to nitric oxide, to administering said compound to inhibit pathological overproduction of nitric oxide from arginine and to administering said compound to a subject having systemic hypotension due to the pathological overproduction of nitric oxide and an .alpha..sub.1 adrenergic agonist to increase blood pressure in the subject to a clinically acceptable level.
摘要翻译：胍基取代的基于单烷基碳取代的鸟氨酸或赖氨酸的精氨酸或高精氨酸，其具有式，其中R是（CH 2）y CH 3或H，R'是CH 2或C（H）（CH 2）y CH 3，R“ CH2或C（H）（CH2）yCH3，y范围为0至5，x为0或1，Q为含有1至6个碳原子的烷基或NH2或NO2，只有一个R，R '和R“在鸟氨酸或赖氨酸部分提供烷基取代基。优选的化合物是α-甲基-Nω-甲基-DL-精氨酸，RS-β-甲基-Nω-甲基-DL-精氨酸，RS-γ-甲基-Nω-甲基-DL-精氨酸，α-甲基-N'- N-ω-氨基-DL-精氨酸，RS-β-甲基-Nω-氨基-DL-精氨酸，RS-γ-甲基-Nω-氨基-DL-精氨酸，α-甲基-Nω-硝基-L- 精氨酸，RS-β-甲基-Nω-硝基-DL-精氨酸和RS-γ-甲基-Nω-硝基-DL-精氨酸。组合物包括所述化合物和药学上可接受的载体。使用的方法是将所述化合物递送到诱导型一氧化氮合酶，以抑制酶催化精氨酸转化为一氧化氮的能力，以使所述化合物抑制来自精氨酸的一氧化氮的病理过度产生，并将所述化合物施用于由于一氧化氮的病理性过量产生的系统性低血压的受试者和α1肾上腺素能激动剂，以将受试者的血压升高到临床可接受的水平。

20. 发明授权

US5436271A N.sup.6 -(hydrazinoiminomethyl)lysine and method of inhibiting nitric oxide formation in body 失效
标题翻译： N6-（肼基亚氨基甲基）赖氨酸和抑制体内一氧化氮形成的方法
公开(公告)号：US5436271A
公开(公告)日：1995-07-25
申请号：US56761
申请日：1993-05-04
申请人： Owen W. Griffith
发明人： Owen W. Griffith
IPC分类号： C07C281/16 , A61K31/195
CPC分类号： C07C281/16
摘要： Physiologically active N.sup.6 -(hydrazinoiminomethyl)lysine or pharmaceutically acceptable acid addition salt thereof is administered in a nitric oxide synthesis inhibiting amount to a subject in need of such inhibition (e.g., a subject with low blood pressure, e.g., due to sepsis or to therapeutic administration of cytokines, or needing immunosuppressive effect) or is added to a medium containing isolated organs, intact cells, cell homogenates or tissue homogenates in an amount sufficient to inhibit nitric oxide formation to elucide or control the biosynthesis, metabolism or physiological role of nitric oxide. Compared to known nitric oxide synthesis inhibitors, N.sup.6 -(hydrazinoiminomethyl)lysine and its acid addition salts show a greater relative activity toward inducible isoform of nitric oxide synthase than toward constitutive isoform of nitric oxide synthase. N.sup.6 -(hydrazinoiminomethyl)lysine and its pharmaceutically acceptable acid addition salts are substantially less toxic than are N.sup.G -aminoarginine and its pharmaceutically acceptable acid addition salts.
摘要翻译：生理活性N6-（肼基亚氨基甲基）赖氨酸或其药学上可接受的酸加成盐以一氧化氮合成抑制量施用于需要这种抑制的受试者（例如，低血压受试者，例如由于败血症或治疗性或需要免疫抑制作用），或加入含有足以抑制一氧化氮形成以分离或控制一氧化氮的生物合成，代谢或生理作用的量的分离器官，完整细胞，细胞匀浆或组织匀浆的培养基。与已知的一氧化氮合成抑制剂相比，N6-（肼基亚氨基甲基）赖氨酸及其酸加成盐对一氧化氮合酶的诱导型异构体显示出比对一氧化氮合酶的组成型异构体更大的相对活性。 N6-（肼基亚氨基甲基）赖氨酸及其药学上可接受的酸加成盐的含量远低于NG-氨基精氨酸及其药学上可接受的酸加成盐。

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