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公开(公告)号:US4714696A
公开(公告)日:1987-12-22
申请号:US574257
申请日:1984-01-26
申请人: Maurice Manning , Wilbur H. Sawyer
发明人: Maurice Manning , Wilbur H. Sawyer
IPC分类号: A61K38/00 , A61K38/095 , A61K38/22 , A61P5/00 , A61P7/10 , C07K7/16 , C07K14/575 , A61K37/34
CPC分类号: C07K7/16 , A61K38/00 , Y10S514/807 , Y10S930/15
摘要: Compounds acting as antagonists of the antidiuretic/and or vasopressor activity of arginine vasopressin are those of the formula ##STR1## wherein n is 4 or 5; X is (D- or L-)Tyr(R), D-Phe, D-Val, D-Leu, D-Ile, D-Nva, D-Nle, D-Cha, D-Abu, D-Thr, D-Asn, D-Met or D-Gln; Y is Val, Ile, Thr, Ala, Lys, Cha, Nva, Met, Nle, Orn, Ser, Asn, Gln, Phe, Tyr, Gly, Abu or Leu; Z is (D- or L-) Arg, Orn or Lys; Q is Arg(NH.sub.2), Ser(NH.sub.2), (D- or L-)Ala(NH.sub.2), Gly, OH or NH.sub.2 and R is methyl, ethyl, propyl or butyl; provided that, when Y is Gln or Val, R may also be H.
摘要翻译: 作为精氨酸加压素的抗利尿和/或加压素活性的拮抗剂的化合物是下式的化合物,其中n为4或5; X是(D-或L-)Tyr(R),D-Phe,D-Val,D-Leu,D-Ile,D-Nva,D-Nle,D-Cha,D-Abu, D-Asn,D-Met或D-Gln; Y是Val,Ile,Thr,Ala,Lys,Cha,Nva,Met,Nle,Orn,Ser,Asn,Gln,Phe,Tyr,Gly,Abu或Leu; Z是(D-或L-)Arg,Orn或Lys; Q是Arg(NH2),Ser(NH2),(D或L)Ala(NH2),Gly,OH或NH2,R是甲基,乙基,丙基或丁基; 条件是当Y是Gln或Val时,R也可以是H.
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公开(公告)号:US4482486A
公开(公告)日:1984-11-13
申请号:US486863
申请日:1983-04-20
申请人: Frantisek Brtnik , Tomislav Barth , Pavel Hrbas , Karel Jost , Ivan Krejci , Bela Kupkova , Alena Machova , Linda Servitova , Jana Skopkova
发明人: Frantisek Brtnik , Tomislav Barth , Pavel Hrbas , Karel Jost , Ivan Krejci , Bela Kupkova , Alena Machova , Linda Servitova , Jana Skopkova
IPC分类号: A61K38/095 , A61K38/00 , C07K7/16 , C07K14/575 , C07C103/52 , A61K37/00
CPC分类号: C07K7/16 , A61K38/00 , Y10S930/15
摘要: Vasopressin analogs of the formula ##STR1## wherein R.sup.1 is H, R.sup.2 is CH.sub.2 S and R.sup.3 is D-Arg,R.sup.1 is NH.sub.2, R.sup.2 is S-S and R.sup.3 is D-Arg or L-Orn are described. The described analogs resist enzymatic cleavage while retaining their effect on the central nervous system. These compounds lack a glycinamide residue in the 9 position and have the L-arginine in the 8 position replaced with its stereoisomeric form or with an ornithine residue. The compounds evidence little or no peripheral endocrine effects of natural vasopressin.
摘要翻译: 其中R1是H,R2是CH2S,R3是D-Arg,R1是NH2,R2是S-S,R3是D-Arg或L-Orn的加压素类似物。 所描述的类似物抵抗酶裂解,同时保留其对中枢神经系统的作用。 这些化合物在9位缺少一个甘氨酰胺残基,8位中的L-精氨酸以其立体异构形式或鸟氨酸残基取代。 这些化合物证明天然加压素几乎没有或没有周围的内分泌作用。
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公开(公告)号:US4402942A
公开(公告)日:1983-09-06
申请号:US238715
申请日:1981-02-27
申请人: Per O. R. Melin
发明人: Per O. R. Melin
IPC分类号: A61K38/00 , A61K38/095 , A61P13/02 , A61P15/00 , C07K7/16 , C07K14/575 , A61K37/00 , C07C103/52
CPC分类号: C07K7/16 , A61K38/00 , Y10S514/807
摘要: New oxytocin derivatives having an inhibitory effect on uterine contractions, pharmaceutical compositions containing the oxytocin derivatives, and use of the derivatives in the production of medicines are described. The derivatives are 1-deamino-(2-O-alkyltyrosine)-oxytocin of the formula ##STR1## wherein Mpa is a 3-mercaptopropionyl residue and X is an alkyl group having 2-4 carbon atoms, preferably an ethyl group. Apart from their inhibitory effect on vasopressin and oxytocin induced uterine contractions, the new oxytocin derivatives are capable of inhibiting the spontaneous contraction pattern of the uterus.
摘要翻译: 描述了对子宫收缩具有抑制作用的新催产素衍生物,含有催产素衍生物的药物组合物及其衍生物在制备药物中的应用。 所述衍生物是式“IMAGE”的1-脱氨基 - (2-O-烷基酪氨酸) - 催产素,其中Mpa是3-巯基丙酰基残基,X是具有2-4个碳原子的烷基,优选乙基。 除了它们对加压素和催产素诱导的子宫收缩的抑制作用外,新的催产素衍生物能够抑制子宫的自发收缩模式。
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公开(公告)号:US4140679A
公开(公告)日:1979-02-20
申请号:US731414
申请日:1976-10-12
申请人: Arthur Malley
发明人: Arthur Malley
IPC分类号: A61K31/70 , A61K38/095 , A61K39/35 , A61K39/36 , A61P37/00 , A61P37/08 , C07D311/30 , C07H17/07 , C08G69/36
CPC分类号: A61K39/36 , C07D311/30 , C07H17/07 , A61K2039/6093 , A61K2039/627 , A61K38/00 , Y10S424/805 , Y10S530/806 , Y10S530/868
摘要: A multivalent complex suitable for blocking allergic reactions comprising (1) at least one Timothy antigen D fragment having the antigenic determinant structure: ##STR1## wherein: G represents glucose, andT represents threonine or a peptide linked to said structure through a threonine molecule;Covalently bonded through at least one glucose moiety to a peptide or protein, (2) a conjugate having the structure: ##STR2## OR (3) A CONJUGATE COMPRISING AT LEAST ONE CONJUGATE OF THE STRUCTURE: ##STR3## COVALENTLY BONDED TO A PROTEIN OR PEPTIDE BY A PEPTIDE LINKAGE THROUGH THE GLUTATHIONE MOIETY.A method of forming complex (1) by activating a glucose moiety of the Timothy antigen D fragment and reacting the thus activated intermediate with a peptide or protein.A method of treating allergies comprising injecting one of the above complexes into an individual to inhibit antigen-induced histamine release.An injectable composition for blocking allergic reactions containing the above complex.
摘要翻译: 适用于阻断过敏反应的多价复合物,其包含(1)至少一种具有抗原决定簇结构的Timothy抗原D片段:其中:
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公开(公告)号:US20240180998A1
公开(公告)日:2024-06-06
申请号:US18553048
申请日:2022-04-06
发明人: Mai Bay STIE , Heidi ÖBLOM , Jette JACOBSEN , Jukka RANTANEN , Hanne Mørck NIELSEN , Natalja GENINA , Cristiana Filipa BARREIRO DA CUNHA
IPC分类号: A61K38/095 , A61J7/00 , A61K9/00 , A61K31/4174 , A61K31/525 , A61K31/721 , A61K47/34 , A61K47/36 , A61K47/38
CPC分类号: A61K38/095 , A61J7/0053 , A61K9/006 , A61K31/4174 , A61K31/525 , A61K31/721 , A61K47/34 , A61K47/36 , A61K47/38
摘要: A dosage form for application on mucosae for release of at least one active pharmaceutical ingredient, wherein the dosage form includes an adhesive layer, made of fibers, capable of adhering to the mucosae of the human or animal body, a water-repelling backing layer, and at least one intermediate layer positioned between the adhesive layer and the water-repelling backing layer. The active pharmaceutical ingredient(s) are incorporated in the intermediate layer(s) and/or in the adhesive layer.
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公开(公告)号:US11986529B2
公开(公告)日:2024-05-21
申请号:US17879441
申请日:2022-08-02
申请人: Amryt Endo, Inc.
发明人: Roni Mamluk , Moshe Tzabari , Karen Marom , Paul Salama , Irina Weinstein
IPC分类号: A61K47/44 , A61K9/00 , A61K9/10 , A61K9/48 , A61K31/70 , A61K31/7036 , A61K31/713 , A61K31/721 , A61K38/08 , A61K38/09 , A61K38/095 , A61K38/12 , A61K38/14 , A61K38/21 , A61K38/22 , A61K38/26 , A61K38/27 , A61K38/28 , A61K38/29 , A61K47/12 , A61K47/14 , A61K47/24 , A61K47/26 , A61K47/32 , A61K9/16 , A61K51/08 , A61K51/10
CPC分类号: A61K47/44 , A61K9/0031 , A61K9/0053 , A61K9/10 , A61K9/4858 , A61K9/4866 , A61K9/4891 , A61K31/70 , A61K31/7036 , A61K31/713 , A61K31/721 , A61K38/08 , A61K38/09 , A61K38/095 , A61K38/12 , A61K38/14 , A61K38/212 , A61K38/22 , A61K38/26 , A61K38/27 , A61K38/28 , A61K38/29 , A61K47/12 , A61K47/14 , A61K47/24 , A61K47/26 , A61K47/32 , A61K9/1623 , A61K51/083 , A61K51/1021 , A61K51/1024 , A61K51/1045
摘要: The pharmaceutical compositions described herein include a suspension which comprises an admixture in solid form of a therapeutically effective amount of a therapeutic agent and at least one salt of a medium chain fatty acid and a hydrophobic medium, e.g. castor oil or glyceryl tricaprylate or a mixture thereof. The pharmaceutical compositions described herein contain medium chain fatty acid salts and are substantially free of alcohols. The pharmaceutical compositions may be encapsulated in a capsule. Methods of treating or preventing diseases by administering such compositions to affected subjects are also disclosed.
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公开(公告)号:US20240156895A1
公开(公告)日:2024-05-16
申请号:US17976613
申请日:2022-10-28
IPC分类号: A61K38/095 , A61K47/02 , A61K47/12 , A61K47/26 , A61P13/12
CPC分类号: A61K38/095 , A61K47/02 , A61K47/12 , A61K47/26 , A61P13/12
摘要: The principles and embodiments of the present disclosure relate to a composition for improving kidney function in an adult patient with hepatorenal syndrome with rapid reduction in kidney function. The composition includes terlipressin acetate having a formula of C52H74N16O15S2·(C2H4O2)n, where n is 2.8.
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98.
公开(公告)号:US20240122987A1
公开(公告)日:2024-04-18
申请号:US18379740
申请日:2023-10-13
发明人: Andrew P. CAP , James A. BYNUM , Xiaowu WU
IPC分类号: A61K35/19 , A61K9/00 , A61K31/137 , A61K31/437 , A61K31/4418 , A61K31/472 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K35/14 , A61K35/16 , A61K35/18 , A61K38/04 , A61K38/095 , A61K38/36 , A61K38/38 , A61K47/26 , A61P7/04
CPC分类号: A61K35/19 , A61K9/0019 , A61K31/137 , A61K31/437 , A61K31/4418 , A61K31/472 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K35/14 , A61K35/16 , A61K35/18 , A61K38/043 , A61K38/095 , A61K38/363 , A61K38/38 , A61K47/26 , A61P7/04
摘要: A majority of military casualties occur during the pre-hospital period. The cause of death is largely associated with massive traumatic bleeding that leads to organ damage due to sustained hypoxia. Currently, therapeutics are lacking at the point of injury to mitigate hypoxic damage and maintain the survivability of severe hemorrhage prior to reaching medical facilities. This invention addresses that by introducing a method of co-administering prolyl hydroxylase domain inhibitor (PHDi, MK-8617), anti-fibrinolytic agent (tranexamic acid), and bradykinin receptor antagonist (icatibant) as anti-hemorrhage agents in combination with resuscitation fluid treatment with colloid solution of 25% human albumin that has an advantage of relatively small volume requirement to maintain blood volume. In addition, a kit comprising anti-hemorrhage agents that can be easily carried to the battlefield is also provided here. The therapeutic application of those agents on or near the point of injury can stabilize hypoxia inducible factor-1 alpha and enhance blood clot formation, which improves the patient's cellular adaptation to hypoxia and reduce hemorrhage, and thus can decrease organ failure and increase the patient's survivability.
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公开(公告)号:US20240091302A1
公开(公告)日:2024-03-21
申请号:US18511467
申请日:2023-11-16
IPC分类号: A61K38/095 , A61K9/08 , A61K47/22 , A61K47/26 , A61K47/38
CPC分类号: A61K38/095 , A61K9/08 , A61K47/22 , A61K47/26 , A61K47/38
摘要: The present disclosure includes a method of making an improved carbetocin drug product. The disclosed method for making an improved carbetocin drug product comprises agitating a carbetocin preparation containing an aqueous solution of carbetocin and one or more excipients for a period of to initiate the formation of aggregate-forming solids and filtering off the aggregates that form before further processing the remaining carbetocin into a final drug product. The present disclosure also relates to an improved carbetocin drug product, wherein the drug product is substantially free of aggregate-forming solids. The disclosed carbetocin drug product can be used for the treatment of a neurodevelopmental disorder, such as Präder-Willi syndrome. Additionally, the disclosed carbetocin drug product shows content uniformity of carbetocin over long periods of time before and after one or more free/thaw cycles, provides enhanced convenience and patient compliance, and/or are highly concentrated.
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100.
公开(公告)号:US20240000705A1
公开(公告)日:2024-01-04
申请号:US18026529
申请日:2021-09-17
发明人: Leon Paul GROTHER
IPC分类号: A61K9/00 , A61K47/42 , A61K47/34 , A61K47/26 , A61K38/095 , A61K31/40 , A61K9/19 , A61K47/12
CPC分类号: A61K9/0056 , A61K47/42 , A61K47/34 , A61K47/26 , A61K38/095 , A61K31/40 , A61K9/19 , A61K47/12
摘要: The present disclosure is directed to use of surfactant with fish gelatin based, freeze dried orally disintegrating tablets. Specifically, Applicants discovered that a small amount of surfactant in combination with high molecular weight fish gelatin in a pharmaceutical formulation can ensure good solution/suspension flow into preformed molds during dosing in order that the finished dosage form has an acceptable shape.
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