公开(公告)号：US4588738A

公开(公告)日：1986-05-13

申请号：US616145

申请日：1984-06-01

Applicant: Paolo Cozzi ,  Antonio Pillan ,  Pier P. Lovisolo

Inventor： Paolo Cozzi ,  Antonio Pillan ,  Pier P. Lovisolo

IPC: C07D233/58 ,  C07D233/60 ,  C07D521/00 ,  A61K31/415

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  Y10S514/822

Abstract: Platelet aggregation inhibiting compositions and methods of use containing compounds of the formula ##STR1## where Z completes a bond or is a ##STR2## group; one of R.sub.1 and R.sub.2 is hydroxy and the other is hydrogen or alkyl, or R.sub.1 and R.sub.2, taken together, form an oxo group; and the remaining substituents are as defined in the specification.

Abstract translation: 血小板聚集抑制组合物和使用方法，其含有下式的化合物：其中Z完成结合或者是“IMAGE”组; R 1和R 2之一是羟基，另一个是氢或烷基，或者R 1和R 2一起形成氧代基; 并且其余的取代基如说明书中所定义。

公开(公告)号：US4568686A

公开(公告)日：1986-02-04

申请号：US233306

申请日：1981-02-11

Applicant: Arto J. Karjalainen ,  Kauko O. A. Kurkela

Inventor： Arto J. Karjalainen ,  Kauko O. A. Kurkela

IPC: C07D233/56 ,  A61K31/415 ,  A61K31/4164 ,  A61P7/02 ,  A61P7/10 ,  A61P9/12 ,  A61P25/02 ,  A61P31/00 ,  A61P31/04 ,  C07D233/54 ,  C07D233/58 ,  C07D233/64 ,  C07D263/32 ,  C07D263/34

CPC classification number: C07D233/56 ,  C07D233/64 ,  C07D263/32 ,  Y10S514/822

Abstract: The invention provides compounds of the formula: ##STR1## wherein each of R.sub.1, R.sub.2 and R.sub.3, which can be the same or different, is hydrogen, chloro, bromo, fluoro, methyl, ethyl, methoxy, amino, hydroxy or nitro; R.sub.4 is hydrogen or alkyl of 1 to 7 carbons atoms; X is ##STR2## (R.sub.5 is hydrogen or hydroxy) and n is 1-4; and their non-toxic pharmaceutically acceptable acid additions salts. These compounds exhibit valuable pharmacological activity and are useful in the treatment of mammals, especially as anti-hypertensive agents. Furthermore, some of the compounds have proved to possess diuretic, .beta.-blocking activity and/or antithrombotic activity. The compounds may be made by a variety of methods and may be incorporated in pharmaceutical compositions also comprising a compatible pharmaceutically acceptable carrier.

公开(公告)号：US4537894A

公开(公告)日：1985-08-27

申请号：US494133

申请日：1983-05-16

Applicant: Jean Blanchard ,  Edouard Panak

Inventor： Jean Blanchard ,  Edouard Panak

IPC: A61K31/415 ,  A61K31/435 ,  A61K31/44 ,  A61P7/02

CPC classification number: A61K31/44 ,  Y10S514/822

Abstract: This invention relates to a therapeutic composition comprising, as active ingredient, a combination of a pyridine derivative having an anti-blood-platelet-aggregation activity and of sulfinpyrazone.Said composition has outstanding anti-blood-platelet-aggregating and antithrombotic properties, both components of the active ingredient functioning according to a synergistic effect.

Abstract translation: 本发明涉及治疗组合物，其包含作为活性成分的具有抗血小板聚集活性的吡啶衍生物与磺吡酮酮的组合。 所述组合物具有突出的抗血小板聚集和抗血栓形成特性，活性成分的两种成分均起协同作用。

公开(公告)号：US4510135A

公开(公告)日：1985-04-09

申请号：US370155

申请日：1982-04-21

Applicant: Lin-nar L. Teng

Inventor： Lin-nar L. Teng

IPC: C08B37/00 ,  A61K31/73 ,  A61K31/725 ,  C08B37/10

CPC classification number: A61K31/715 ,  A61K47/4803 ,  A61K47/48038 ,  A61K47/48053 ,  C08B37/0075 ,  Y10S514/822

Abstract: An orally administrable heparin comprising: a complex of heparin with (1) a protonated tertiary organic ammonium ion having the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each independently represent a branched or unbranched alkyl group of 1 to 12 carbon atoms, which may be unsubstituted or substituted with hydroxy or alkoxy groups, or R.sup.1 and R.sup.3 together with the N atom can form a pyrrolidine, imidazole or morpholine ring; or (2) an ester-containing quaternary ammonium ion having the formula: ##STR2## wherein R.sup.4, R.sup.5 and R.sup.6 each independently represent a branched or unbranched alkyl group of 1 to 12 carbon atoms, which may be unsubstituted or substituted with hydroxy or alkoxy groups, or R.sup.4 and R.sup.6 together with the N atom can form a pyrrolidine, imidazole or morpholine ring;R.sup.7 represents an alkyl group of 4 to 16 carbon atoms; andR.sup.8 represents a hydrogen atom or a methyl group.

Abstract translation: 一种可口服给药的肝素，其包含：肝素与（1）具有下式的质子化叔有机铵离子的络合物：其中R 1，R 2和R 3各自独立地表示1至12个碳原子的支链或非支链烷基，其中 可以是未取代的或被羟基或烷氧基取代，或者R 1和R 3与N原子一起可以形成吡咯烷，咪唑或吗啉环; 或（2）具有下式的含酯季铵离子：其中R 4，R 5和R 6各自独立地表示1至12个碳原子的支链或非支链烷基，其可以是未取代的或被羟基或烷氧基取代 或R 4和R 6与N原子一起可形成吡咯烷，咪唑或吗啉环; R7表示4〜16个碳原子的烷基; R8表示氢原子或甲基。

公开(公告)号：US4485258A

公开(公告)日：1984-11-27

申请号：US403119

申请日：1982-07-29

Applicant: Ryoji Kikumoto ,  Harukazu Fukami ,  Hiroto Hara ,  Kunihiro Ninomiya ,  Mamoru Sugano

Inventor： Ryoji Kikumoto ,  Harukazu Fukami ,  Hiroto Hara ,  Kunihiro Ninomiya ,  Mamoru Sugano

IPC: A61K31/13 ,  A61K31/135 ,  A61K31/19 ,  A61K31/195 ,  A61K31/445 ,  A61P7/02 ,  A61P43/00 ,  C07C67/00 ,  C07C213/00 ,  C07C217/32 ,  C07C217/84 ,  C07C219/04 ,  C07D211/62 ,  C07D295/08 ,  C07D295/092 ,  C07C59/68

CPC classification number: C07D295/088 ,  C07D211/62 ,  Y10S514/822

Abstract: (3-Aminopropoxy)bibenzyl derivatives are prepared and found useful as pharmaceutical agents, particularly as inhibitors of platelet aggregation.

Abstract translation: （3-氨基丙氧基）联苄衍生物被制备并发现可用作药剂，特别是作为血小板聚集的抑制剂。

公开(公告)号：US4464377A

公开(公告)日：1984-08-07

申请号：US292241

申请日：1981-08-12

Applicant: Jean Blanchard ,  Edouard Panak

Inventor： Jean Blanchard ,  Edouard Panak

IPC: A61K31/435 ,  A61K31/44

CPC classification number: A61K31/44 ,  A61K31/435 ,  Y10S514/822

Abstract: This invention relates to therapeutic compositions comprising, as active ingredients, a combination of a pyridine derivative having an anti-blood-platelet-aggregation activity with a derivative having beta-blocking properties, which exhibit synergistic anti-thrombotic activity.

Abstract translation: 本发明涉及治疗组合物，其包含作为活性成分的具有抗血小板聚集活性的吡啶衍生物与具有β-阻断性质的衍生物的组合，其具有协同的抗血栓形成活性。

公开(公告)号：US4455290A

公开(公告)日：1984-06-19

申请号：US250173

申请日：1981-04-02

Applicant: Stephanie A. Olexa ,  Andrei Z. Budzynski

Inventor： Stephanie A. Olexa ,  Andrei Z. Budzynski

IPC: A61K38/00 ,  C07K14/75 ,  A61K49/00 ,  A61K43/00

CPC classification number: C07K14/75 ,  A61K38/00 ,  Y10S514/802 ,  Y10S514/822

Abstract: A purified peptide isolated from fibrinogen Fragment D.sub.1 and having the amino acid sequence Thr-Arg-Trp-Tyr-Ser-Met-Lys-Lys-Thr-Thr-Met-Lys-Ile-Ile-Pro-Phe-Asn-Arg-Leu-Thr-Ile-Gly-Glu-Gly-Gln-Gln-His-His-Leu-Gly-Gly-Ala-Lys-Gln-Ala-Gly-Asp-Val. The peptide is isloated by degrading Fragment D.sub.1 of fibrinogen with plasmin followed by separation of the resulting peptides on the basis of molecular weight and affinity for bound fibrin monomer. The purified peptide is useful as an anticoagulant and, when suitably labeled with a gamma-emitting radioisotope, as a thrombus imaging agent.

Abstract translation: 从纤维蛋白原片段D1分离并具有氨基酸序列Thr-Arg-Trp-Tyr-Ser-Met-Lys-Lys-Thr-Thr-Met-Lys-Ile-Ile-Pro-Phe-Asn-Arg的纯化肽 -Leu-Thr-Ile-Gly-Glu-Gly-Gln-Gln-His-His-Leu-Gly-Gly-Ala-Lys-Gln-Ala-Gly-Asp-Val。 通过用纤溶酶降解纤维蛋白原的片段D1来分离肽，然后基于分子量和对结合的纤维蛋白单体的亲和力分离所得肽。 纯化的肽可用作抗凝血剂，并且当用γ-发射放射性同位素适当标记时作为血栓显像剂。

公开(公告)号：US4451458A

公开(公告)日：1984-05-29

申请号：US379272

申请日：1982-05-17

Applicant: Hans Buhlmann ,  Dieter Welzel

Inventor： Hans Buhlmann ,  Dieter Welzel

IPC: A61K31/48 ,  A61K31/725

CPC classification number: A61K31/715 ,  A61K31/48 ,  Y10S514/822

Abstract: The invention provides novel pharmaceutical compositions useful in the treatment of thrombosis in mammals, comprising a mixture of dihydroergotamine or a related ergot alkaloid and heparin.

Abstract translation: 本发明提供了可用于治疗哺乳动物血栓形成的新型药物组合物，其包含二氢麦角胺或相关麦角生物碱和肝素的混合物。

公开(公告)号：US4402946A

公开(公告)日：1983-09-06

申请号：US337175

申请日：1982-01-05

Applicant: Ralph B. Thompson

Inventor： Ralph B. Thompson

IPC: A61K31/13 ,  A61K31/14 ,  A61K31/70 ,  A61K31/095 ,  A61K31/115 ,  A61K31/715

CPC classification number: A61K31/14 ,  A61K31/13 ,  Y10S514/822

Abstract: Certain salts of carbonyl sulfur dioxide adducts are found to demonstrate anticoagulant and/or venous antithrombotic activity.

Abstract translation: 发现某些羰基二氧化硫加合物的盐显示抗凝血和/或静脉抗血栓活性。

公开(公告)号：US4400397A

公开(公告)日：1983-08-23

申请号：US337121

申请日：1982-01-05

Applicant: Jose A. Arias Alvarez ,  Ralph B. Thompson

Inventor： Jose A. Arias Alvarez ,  Ralph B. Thompson

IPC: A61K31/13 ,  A61K31/14 ,  A61K31/095

CPC classification number: A61K31/13 ,  A61K31/14 ,  Y10S514/822

Abstract: Certain quaternary ammonium sulfites and bisulfites display anticoagulant and antithrombotic activity.

Abstract translation: 某些季铵亚硫酸盐和亚硫酸氢盐显示抗凝血和抗血栓形成活性。