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11. 发明授权

US5278146A CRF analogs 失效
标题翻译： CRF类似物
公开(公告)号：US5278146A
公开(公告)日：1994-01-11
申请号：US905564
申请日：1992-06-29
申请人： Jean E. F. Rivier , Wylie W. Vale, Jr.
发明人： Jean E. F. Rivier , Wylie W. Vale, Jr.
IPC分类号： A61K38/00 , C07K14/575 , A61K37/40 , C07K7/38
CPC分类号： C07K14/57509 , A61K38/00
摘要： Analogs of CRF, which are based upon hCRF, oCRF, sauvagine and alpha-helical CRF, are disclosed that can be administered to achieve a substantial elevation of ACTH, .beta.-endorphin, .beta.-lipotropin, other products of the pro-opiomelanocortin gene and corticosterone levels and/or an increase in blood pressure over an extended period of time. One CRF agonist which has been found to be particularly potent is: H-Ser-Gln-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Met-Thr-Lys-Ala-Asp-Gln-Leu-Ala-Gln-Gln-Ala-His-Ser-Asn-Arg-Lys-Leu-Leu-Asp-Ile-Ala-NH.sub.2. In these agonist analogs, one or more of the first six N-terminal residues may be deleted and/or the N-terminal alpha-amino group may be acylated by an acylating agent containing up to 7 carbon atoms. A number of other substitutions may also be made throughout the chain. These analogs or pharmaceutically or veterinarily acceptable salts thereof, dispersed in a pharmaceutically or veterinarily acceptable liquid or solid carrier, can be administered to mammals, including humans. These analogs may also be used as stimulants to elevate mood and improve memory and learning, as well as diagnostically.
摘要翻译：公开了基于hCRF，oCRF，sauvagine和α-螺旋CRF的CRF的类似物，其可以被施用以实现ACTH，（β） - 内啡肽，（β） - 促性腺激素，其他产物的显着升高 - 皮质酮皮质素基因和皮质酮水平和/或长时间的血压升高。已经发现特别有效的一种CRF激动剂是：H-Ser-Gln-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-D-Phe-His-Leu-Leu-Arg-Glu -Val-Leu-Glu-Met-Thr-Lys-Ala-Asp-Gln-Leu-Ala-Gln-Gln-Ala-His-Ser-Asn-Arg-Lys-Leu-Leu-Asp-Ile-Ala-NH2 。在这些激动剂类似物中，前6个N末端残基中的一个或多个可以被缺失，和/或N-末端α-氨基可以被含有至多7个碳原子的酰化剂酰化。还可以在整个链中进行许多其它取代。分散在药学上或兽医学上可接受的液体或固体载体中的这些类似物或其药学或兽医学上可接受的盐可以施用于哺乳动物，包括人。这些类似物也可以用作兴奋剂以提高心情，改善记忆和学习以及诊断。

12. 发明授权

US4350703A .beta.-Lactam antibacterial agents 失效
标题翻译： β-内酰胺抗菌剂
公开(公告)号：US4350703A
公开(公告)日：1982-09-21
申请号：US222282
申请日：1981-01-05
申请人： Kay H. Dickinson , Terence C. Smale , Robert Southgate
发明人： Kay H. Dickinson , Terence C. Smale , Robert Southgate
IPC分类号： C07D205/08 , C07D205/12 , C07D477/08 , C07F9/535 , C07F9/54 , C07F9/568 , C07F9/6561 , C07D487/04 , A61K37/40
CPC分类号： C07F9/5352 , C07D205/08 , C07D205/12 , C07D477/08 , C07F9/5442 , C07F9/5683 , C07F9/65613
摘要： Compounds are described of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group; A.sub.1 is a hydrogen atom; and A.sub.2 is a group CR.sub.2 R.sub.3 R.sub.4 wherein R.sub.2 is a hydrogen atom or a hydroxyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, a benzyl group, a phenyl group or is joined to R.sub.3 to form part of a C.sub.5-7 carboxylic ring or is a group of the formula CH(OH)R.sub.5 or CHX wherein R.sub.5 is a hydrogen atom or lower alkyl group and X is an oxygen atom or a CR.sub.6 R.sub.7 group where R.sub.6 is a hydrogen atom or a lower alkyl, phenyl, CN, CO.sub.2 R.sub.8 where R.sub.8 is a lower alkyl, phenyl or benzyl group and R.sub.7 is a hydrogen atom or a lower alkyl group or is joined to R.sub.6 to form part of a C.sub.5-7 carbocyclic ring. These compounds have been found to possess antibacterial properties. The preparation of these compounds is described.
摘要翻译：化合物描述为式（II）：其中R 1是使CO 2 R 1是酯基的基团; A1是氢原子; A2为基团CR2R3R4，其中R2为氢原子或羟基; R3是氢原子或低级烷基; R4为氢原子或低级烷基，苄基，苯基或与R3结合形成C5-7羧酸环的一部分，或为式CH（OH）R5或CHX的基团，其中R5 是氢原子或低级烷基，X是氧原子或其中R6是氢原子或低级烷基，苯基，CN，CO2R8的CR6R7基团，其中R8是低级烷基，苯基或苄基，R7是氢原子或低级烷基，或者连接到R6以形成C5-7碳环的一部分。已经发现这些化合物具有抗菌性质。描述了这些化合物的制备。

13. 发明授权

US3923772A (1-{60 -aminoisobutyric acid)-corticotropin peptides 失效
标题翻译：（1- {6-氨基异丁酸）-CORTICOTROPIN PEPTIDES
公开(公告)号：US3923772A
公开(公告)日：1975-12-02
申请号：US46989074
申请日：1974-05-14
申请人： SHIONOGI & CO
发明人： OTSUKA HIDEO , INOUYE KEN
IPC分类号： A61K38/00 , C07K14/695 , C07C103/52 , A61K37/40
CPC分类号： C07K14/695 , A61K38/00 , Y10S514/805
摘要： Highly active corticotropin peptides which have an Alpha aminoisobutyric acid residue at the amino-terminal in place of the serine in native corticotropin, derivatives thereof, intermediates therefor and compositions thereof are disclosed. Such peptides are useful as a medicament, because they show corticotropic properties remarkably improved in enhancement of potency and prolongation of action. They can be prepared by condensing the amino acids together one by one or by condensing the small peptide fragments together in a per se conventional manner.
摘要翻译：公开了在天然促肾上腺皮质激素，其衍生物，其中间体及其组合物中在氨基末端具有α-氨基异丁酸残基代替丝氨酸的高活性促肾上腺皮质激素肽。这样的肽可用作药物，因为它们显示出在提高效力和作用延长方面显着改善的皮质醇性质。它们可以通过将氨基酸一个一个地缩合在一起，或者通过将这些小肽片段以本来常规的方式一起冷凝来制备。

14. 发明授权

US4801612A Method of inhibiting inflammatory response 失效
标题翻译：抑制炎症反应的方法
公开(公告)号：US4801612A
公开(公告)日：1989-01-31
申请号：US881321
申请日：1986-07-03
申请人： Edward T. Wei , Juliann G. Kiang
发明人： Edward T. Wei , Juliann G. Kiang
IPC分类号： A61K38/22 , A61K37/40
CPC分类号： A61K38/2228
摘要： Many malignant neoplasias are treated by radiation therapy which can result in painful inflammation of the covering skin and/or mucosal membranes. Similarly, skin disorder patients receiving U.V. treatment may experience an inflammatory response.Certain neuropeptides have been discovered to have the unusual properties of preventing, or inhibiting, the edema and protein extravasation of skin and mucosal membrane injuries due to thermal or radiation assault or exposure to trauma or noxious agents. A method for inhibiting an inflammatory response in the skin or mucosal membranes of a patient is provided in which a therapeutically effective amount of a neuropeptide, such as Corticotropin Releasing Factor ("CRF") or its analogs, is administered.
摘要翻译：许多恶性肿瘤通过放射治疗来治疗，这可能导致覆盖皮肤和/或粘膜的疼痛的炎症。类似地，接受紫外线的皮肤失调患者治疗可能会发生炎症反应。已经发现某些神经肽具有预防或抑制由于热或辐射攻击或暴露于创伤或有毒药物引起的皮肤和粘膜损伤的水肿和蛋白质渗出的不寻常的特性。提供一种抑制患者皮肤或粘膜中炎性反应的方法，其中施用治疗有效量的神经肽，例如促肾上腺皮质激素释放因子（“CRF”）或其类似物。

15. 发明授权

US4794104A Pharmaceutical compositions containing ACTH fragments for the therapy of shock conditions and of respiratory and cardiocirculatory insufficiencies 失效
标题翻译：含有ACTH片段的药物组合物用于治疗休克条件和呼吸和心脏循环障碍
公开(公告)号：US4794104A
公开(公告)日：1988-12-27
申请号：US000183
申请日：1987-01-02
申请人： Alfio Bertolini
发明人： Alfio Bertolini
IPC分类号： A61K38/22 , A61K38/00 , A61K38/34 , A61K38/35 , A61P9/00 , A61P11/00 , C07K14/695 , A61K37/40
CPC分类号： A61K38/35 , A61K38/34 , C07K14/695
摘要： The parenteral administration of 80-160 .mu.g per kg body weight of substituted or unsubstituted fragments of ACTH (1-39) having formula ACTH (X-Y) wherein X is an integer from 1 to 5 and Y is an integer from 10 to 39 (provided that, when X is 1, Y is not 24) restores the normal blood pressure and respiratory frequence in a patient in serious shock conditions, particularly in hypovolemic shock.
摘要翻译：胃肠外给药80-160μg/ kg体重的具有式ACTH（XY）的ACTH（1-39）的取代或未取代的片段，其中X是1至5的整数，Y是10至39的整数（条件是，当X为1时，Y不为24）在严重的休克条件下，特别是在低血容量休克中恢复患者的正常血压和呼吸频率。

16. 发明授权

US4177267A Enhancing tissue penetration of physiologically active steroidal agents with DMSC 失效
标题翻译：用DMSC增强生理活性甾体药物的组织穿透
公开(公告)号：US4177267A
公开(公告)日：1979-12-04
申请号：US304283
申请日：1972-11-06
申请人： Robert J. Herschler
发明人： Robert J. Herschler
IPC分类号： A61K8/46 , A61K8/63 , A61K31/43 , A61K38/28 , A61K47/20 , A61Q19/00 , A61K31/10 , A61K37/40
CPC分类号： A61K31/43 , A61K38/28 , A61K47/20 , A61K8/46 , A61K8/63 , A61K9/0014 , A61Q19/00 , A61Q5/00 , Y10S514/936
摘要： A method of enhancing tissue penetration of physiologically active steroidal agents by conjointly applying them to the tissue with dimethyl sulfoxide. Penetration of the skin and the mucous membranes of the body cavities by these agents may be enhanced by conjoint application of such agents and dimethyl sulfoxide directly to such membranes. Preferably, for penetration of these agents through the skin compositions of DMSO at concentrations of 50% and above are employed and for penetration through mucous membranes, compositions including DMSO at concentrations of 10% and above are employed. Steroidal agents may be advantageously administered by injection with DMSO in concentrations preferably up to 20% by weight to enhance penetration of internal tissue membrane barriers to achieve better distribution of these agents.
摘要翻译：通过使用二甲基亚砜将它们组合施用于组织来增强生理活性甾体试剂的组织穿透的方法。可以通过将这些试剂和二甲基亚砜直接施加到这些膜上来增强这些试剂对皮肤和体腔粘膜的渗透。优选地，为了使这些试剂渗透通过50％以上浓度的DMSO的皮肤组合物，并且通过粘膜渗透，使用包含浓度为10％以上的DMSO的组合物。甾族药物可以有利地通过注射DMSO以浓度优选至多20重量％的浓度来施用，以增强内部组织膜屏障的穿透以实现这些药剂的更好分布。

17. 发明授权

US4167562A Method and composition for treating arteriosclerosis 失效
标题翻译：用于治疗动脉硬化的方法和组合物
公开(公告)号：US4167562A
公开(公告)日：1979-09-11
申请号：US937533
申请日：1978-08-28
申请人： H. Ray Evers
发明人： H. Ray Evers
IPC分类号： A61K35/55 , A61K33/14 , A61K37/40 , A61K31/725 , A61K31/68
CPC分类号： A61K35/55 , Y10S514/805
摘要： New compositions and their method of use for treating cardiovascular diseases primarily due to arteriosclerosis and atherosclerosis. These new compositions are prepared from a base Ringers injection to which is added a B-complex, hydrochloric acid, sodium ascorbate, pyridoxine hydrochloride, magnesium sulfate, adrenal cortex, magnesium chloride, thiamine, heparin sodium, calcium gluconate and calcium d-saccharate. Additional embodiments of the solution composition are also disclosed containing niacin, vitamin B.sub.12, ether, algae and amino acids. The compositions are useful in removing plaques from the interior walls of the arteries and veins, thereby improving blood supply to body tissues.
摘要翻译：新的组合物及其用于治疗心血管疾病的方法主要由于动脉硬化和动脉粥样硬化。这些新组合物由基础Ringers注射液制备，向其中加入B络合物，盐酸，抗坏血酸钠，盐酸吡哆醇，硫酸镁，肾上腺皮质，氯化镁，硫胺素，肝素钠，葡萄糖酸钙和d-糖酸钙。还公开了溶液组合物的另外的实施方案，其包含烟酸，维生素B12，醚，藻类和氨基酸。组合物可用于从动脉和静脉的内壁去除斑块，从而改善对身体组织的血液供应。

18. 发明申请

WO1992021372A1 CRF ANALOGS 审中-公开
标题翻译： CRF模拟
公开(公告)号：WO1992021372A1
公开(公告)日：1992-12-10
申请号：PCT/US1992004525
申请日：1992-05-29
申请人： THE SALK INSTITUTE FOR BIOLOGICAL STUDIES
发明人： THE SALK INSTITUTE FOR BIOLOGICAL STUDIES , KORNREICH, Wayne, D. , HERNANDEZ, Jean-François , RIVIER, Jean, Edouard, Frederic , VALE, Wylie, Walker, Jr.
IPC分类号： A61K37/40
CPC分类号： C07K14/57509 , A61K38/00 , Y10S930/26
摘要： Analogs of CRF, which are based upon hCRF, oCRF and alpha-helical CRF, are disclosed that can be administered to achieve a substantial elevation of ACTH, beta -endorphin, beta -lipotropin, other products of the pro-opiomelanocortin gene and corticosterone levels. Analogs include those having the formula (see SEQ ID NO:9): Y-Ser-Xaa2-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu -Val-Leu-Xaa20-Xaa21-Xaa22-Xaa23-Xaa24-Xaa25-Gln-Leu-Ala-Gln-Gln-Ala-X aa32-Ser-Asn-Arg-Lys-Leu-Xaa38-Xaa39-Ile-Xaa41-NH2, wherein Y is an acyl group having 7 or fewer carbon atoms or hydrogen; Xaa2 is Glu or Gln; Xaa20 is Ala or Glu; Xaa21 is Met or Nle; Xaa22 is Ala or Thr; Xaa23 is Arg or Lys; Xaa24 is D-Ala or Ala; Xaa25 is Glu or Asp; Xaa32 is D-His or His; Xaa38 is Met, Nle or Leu; Xaa39 is Ala, Glu or Asp; Xaa41 is Ile or Ala; provided however that at least one of Xaa20 and Xaa39 is Ala and that the N-terminus may be shortened by a sequence of up to about 5 residues. One example is [Ala ]-oCRF. These analogs or their pharmaceutically acceptable salts, dispersed in an acceptable liquid or solid carrier, can be administered to humans.
摘要翻译：公开了基于hCRF，oCRF和α-螺旋CRF的CRF的类似物，其可以被施用以实现ACTH，β-内啡肽，β-促肌动蛋白，原乳糖皮质素基因的其他产物和皮质酮水平的显着升高。类似物包括具有式（见SEQ ID NO：9）的那些：Y-Ser-Xaa2-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu -Val-Leu-Xaa20-Xaa21-Xaa22-Xaa23-Xaa24-Xaa25-Gln-Leu-Ala-Gln-Gln-Ala-Xaa32-Ser-Asn-Arg-Lys-Leu-Xaa38-Xaa39-Ile-Xaa41- NH 2，其中Y是具有7个或更少碳原子或氢的酰基; Xaa2是Glu或Gln; Xaa20是Ala或Glu; Xaa21是Met或Nle; Xaa22是Ala或Thr; Xaa23是Arg或Lys; Xaa24是D-Ala或Ala; Xaa25是Glu或Asp; Xaa32是D-His或他的; Xaa38是Met，Nle或Leu; Xaa39是Ala，Glu或Asp; Xaa41是Ile或Ala; 但是，Xaa20和Xaa39中的至少一个是Ala，并且N末端可以被至多约5个残基的序列缩短。一个例子是[Ala 20] - oCRF。分散在可接受的液体或固体载体中的这些类似物或其药学上可接受的盐可以施用于人。

19. 发明授权

US5306710A Method for treating endotoxin shock with CRF 失效
标题翻译：用CRF治疗内毒素休克的方法
公开(公告)号：US5306710A
公开(公告)日：1994-04-26
申请号：US876487
申请日：1992-04-30
申请人： Edward T. Wei
发明人： Edward T. Wei
IPC分类号： A01D1/02 , A01N1/02 , A61K38/22 , A61P3/00 , C07K14/575 , A61K37/40
CPC分类号： A61K38/2228 , A01N1/021 , A01N1/0226
摘要： Administration of a Corticotropin-Releasing Factor (or a salt or analog thereof) decreases the leakage of blood components into brain tissue produced by various adverse medical conditions and reduces bleeding when muscle tissues are cut and handled, such as in plastic and reconstructive surgery. A method of treating a patient for injury to or disease of the brain, central nervous system, or musculature in which edema is a factor comprises administering to the patient a Corticotropin-Releasing Factor (or a salt or analog) in an amount effective to decrease vascular permeability in the injured or diseased brain, nervous system tissue or musculature, and thereby to reduce edema. Administration in accordance with the method can be about two hours before surgery, or can be up to three days after injury.
摘要翻译：促肾上腺皮质激素释放因子（或其盐或类似物）的施用减少了由各种不利的医学条件产生的血液成分渗透到脑组织中，并且在肌肉组织被切割和处理时减少出血，例如在塑性和重建手术中。治疗患者对水肿是水肿的脑，中枢神经系统或肌肉组织的损伤或疾病的方法包括向患者施用有效降低的量的促肾上腺皮质激素释放因子（或盐或类似物）损伤或患病的脑，神经系统组织或肌肉组织中的血管通透性，从而减少水肿。按照方法管理可以在手术前约两个小时，否则可能在伤后三天内。

20. 发明授权

US4308166A Process for the extemporaneous preparation of liposomes 失效
标题翻译：即时制备脂质体的方法
公开(公告)号：US4308166A
公开(公告)日：1981-12-29
申请号：US89386
申请日：1979-10-30
申请人： Enzo Marchetti , Umberto Bucciarelli
发明人： Enzo Marchetti , Umberto Bucciarelli
IPC分类号： A61K9/127 , B01J13/02 , A61K9/50 , A61K9/64 , A61K37/40
CPC分类号： A61K9/1277 , Y10T428/2984
摘要： The extemperaneous preparation of liposomes incorporating englobed therapeutically active substances is effected by introducing an aspirated phopholipid emulsion into a container containing the active substance as a dry powder or lyophilate.
摘要翻译：通过将吸入的磷脂乳剂引入含有作为干粉或冻干物质的活性物质的容器中来实现包含脑内治疗活性物质的脂质体的经皮制备。

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