公开(公告)号：US4444691A

公开(公告)日：1984-04-24

申请号：US351884

申请日：1982-02-24

Applicant: Charles V. Grudzinskas ,  Martin J. Weiss

Inventor： Charles V. Grudzinskas ,  Martin J. Weiss

IPC: C07C405/00 ,  C07C121/46 ,  C07C121/70

CPC classification number: C07C405/00 ,  C07C405/0033 ,  C07C405/0041

Abstract: This disclosure describes 11-deoxy-11-substituted members of the E.sub.2, F.sub.2, E.sub.1, F.sub.1, dihydro E.sub.1 and dihydro F.sub.1 prostaglandin series which are useful as hypotensive agents and as anti-ulcer agents.

Abstract translation: 本公开描述了可用作降压药和抗溃疡剂的E2，F2，E1，F1，二氢E1和二氢F1前列腺素系列的11-脱氧-11-取代的成员。

公开(公告)号：US4239900A

公开(公告)日：1980-12-16

申请号：US74942

申请日：1979-09-13

Applicant: Middleton B. Floyd, Jr. ,  Martin J. Weiss ,  Charles V. Grudzinskas ,  Sow-Mei L. Chen

Inventor： Middleton B. Floyd, Jr. ,  Martin J. Weiss ,  Charles V. Grudzinskas ,  Sow-Mei L. Chen

IPC: C07C29/10 ,  C07C29/42 ,  C07C405/00 ,  C07D307/42 ,  C07F7/08 ,  C07F7/18 ,  C07F7/22 ,  C07C177/00

CPC classification number: C07D307/42 ,  C07C29/10 ,  C07C29/42 ,  C07C405/00 ,  C07F7/0818 ,  C07F7/1864 ,  C07F7/1896 ,  C07F7/2212 ,  C07B2200/07 ,  C07C2101/10

Abstract: 15-Deoxy-16-hydroxy-16-ethynyl and 16-ethynylsubstituted prostanoic acids and congeners thereof, useful as bronchodilators, hypotensive agents, and as agents for the control of excessive gastric secretion.

公开(公告)号：US4230879A

公开(公告)日：1980-10-28

申请号：US46513

申请日：1979-06-07

Applicant: Allen Wissner ,  Charles V. Grudzinskas

Inventor： Allen Wissner ,  Charles V. Grudzinskas

IPC: C07C45/71 ,  C07C405/00 ,  C07F7/18 ,  C07C177/00

CPC classification number: C07F7/1852 ,  C07C405/00 ,  C07C45/71

Abstract: The invention disclosed herein relates to pharmacologically active prostaglandins of the E and F series in which C-16 is substituted with hydroxyl and formyl or dimethoxymethyl as well as the pharmaceutically acceptable, non-toxic lower alkyl esters and salts thereof, and to the intermediates and processes for producing such compounds.

Abstract translation: 本文公开的本发明涉及E和F系列的药理学活性前列腺素，其中C-16被羟基和甲酰基或二甲氧基甲基以及其药学上可接受的无毒低级烷基酯及其盐取代，并且涉及中间体和 制备这种化合物的方法。

公开(公告)号：US4219496A

公开(公告)日：1980-08-26

申请号：US885526

申请日：1978-03-10

Applicant: Charles V. Grudzinskas ,  Martin J. Weiss

Inventor： Charles V. Grudzinskas ,  Martin J. Weiss

IPC: C07C405/00 ,  C07C121/46

CPC classification number: C07C405/00 ,  C07C405/0033 ,  C07C405/0041

Abstract: This disclosure describes 11-deoxy-11-substituted members of the E.sub.2, F.sub.2, E.sub.1, F.sub.1, dihydro E.sub.1 and dihydro F.sub.1 prostaglandin series which are useful as hypotensive agents and as anti-ulcer agents.

Abstract translation: 本公开描述了可用作降压药和抗溃疡剂的E2，F2，E1，F1，二氢E1和二氢F1前列腺素系列的11-脱氧-11-取代的成员。

公开(公告)号：US4390711A

公开(公告)日：1983-06-28

申请号：US206492

申请日：1980-11-13

Applicant: Charles V. Grudzinskas ,  Sow-Mei L. Chen ,  Allan Wissner

Inventor： Charles V. Grudzinskas ,  Sow-Mei L. Chen ,  Allan Wissner

IPC: C07D307/935 ,  A61K31/557 ,  A61K31/5575 ,  A61P1/04 ,  A61P7/02 ,  A61P9/00 ,  A61P9/08 ,  A61P9/12 ,  A61P11/08 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D307/937 ,  C07D317/04 ,  C07D407/06 ,  C07F7/18

CPC classification number: C07D307/937 ,  C07C405/0016 ,  C07C405/0025 ,  C07D317/04 ,  C07F7/1804 ,  C07F7/1856

Abstract: This disclosure describes certain 6,9.alpha.-epoxy prostacyclines and their intermediates. These compounds are useful as bronchodilators and inflammatory mediator release inhibitors.

Abstract translation: 本公开描述了某些6,9个α-环氧前列环素及其中间体。 这些化合物可用作支气管扩张剂和炎症介质释放抑制剂。

公开(公告)号：US4250325A

公开(公告)日：1981-02-10

申请号：US969479

申请日：1978-12-14

Applicant: Middleton B. Floyd, Jr. ,  Martin J. Weiss ,  Charles V. Grudzinskas ,  Sow-Mei L. Chen

Inventor： Middleton B. Floyd, Jr. ,  Martin J. Weiss ,  Charles V. Grudzinskas ,  Sow-Mei L. Chen

IPC: A61K31/557 ,  C07C29/10 ,  C07C29/42 ,  C07C45/59 ,  C07C45/71 ,  C07C49/743 ,  C07C405/00 ,  C07D307/32 ,  C07D307/42 ,  C07F7/18 ,  C07C177/00

CPC classification number: C07D307/32 ,  A61K31/557 ,  C07C29/10 ,  C07C29/42 ,  C07C405/00 ,  C07C405/0025 ,  C07C45/59 ,  C07C45/71 ,  C07C49/743 ,  C07D307/42 ,  C07F7/1852 ,  C07F7/1896 ,  C12C11/02 ,  C07B2200/07 ,  C07B2200/09 ,  C07C2101/08 ,  C07C2101/10

Abstract: The invention described herein relates to novel 15-deoxy-16-hydroxy-16-ethynyl or 16-(1-propynyl) prostaglandins of E, F, D and A series having on the terminal methylene carbon of the alpha chain a substituent selected from the group consisting of: ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and C.sub.1 -C.sub.6 alkyl; R.sub.15 is selected from the group consisting of C.sub.1 -C.sub.4 alkyl, di-C.sub.1 -C.sub.4 -alkylamino, phenyl and phenyl substituted with one or more substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, OR, SR, F or Cl, wherein R is an alkyl group.

Abstract translation: 本文描述的本发明涉及E，F，D和A系列的新型15-脱氧-16-羟基-16-乙炔基或16-（1-丙炔基）前列腺素，其在α链的末端亚甲基上具有选自以下的取代基 由以下组成的组成：其中R 1选自氢和C 1 -C 6烷基; R 15选自C 1 -C 4烷基，二-C 1 -C 4烷基氨基，苯基和被一个或多个选自C 1 -C 4烷基，OR，SR，F或Cl的取代基取代的苯基，其中 R是烷基。

公开(公告)号：US4239899A

公开(公告)日：1980-12-16

申请号：US74941

申请日：1979-09-13

Applicant: Middleton B. Floyd, Jr. ,  Martin J. Weiss ,  Charles V. Grudzinskas ,  Sow-Mei L. Chen

Inventor： Middleton B. Floyd, Jr. ,  Martin J. Weiss ,  Charles V. Grudzinskas ,  Sow-Mei L. Chen

IPC: C07C29/10 ,  C07C29/42 ,  C07C405/00 ,  C07D307/42 ,  C07F7/18 ,  C07F7/22 ,  C07C177/00 ,  C07F7/08

CPC classification number: C07D307/42 ,  C07C29/10 ,  C07C29/42 ,  C07C405/00 ,  C07F7/1864 ,  C07F7/1896 ,  C07F7/2212 ,  C07B2200/07 ,  C07B2200/09 ,  C07C2101/08

Abstract: 15-Deoxy-16-hydroxy-16-ethynyl and 16-ethynylsubstituted prostanoic acids and congeners thereof, useful as bronchodilators, hypotensive agents, and as agents for the control of excessive gastric secretion.

公开(公告)号：US4227011A

公开(公告)日：1980-10-07

申请号：US046516

申请日：1979-06-07

Applicant: Sow-Mei L. Chen ,  Charles V. Grudzinskas

Inventor： Sow-Mei L. Chen ,  Charles V. Grudzinskas

IPC: C07C29/42 ,  C07C45/00 ,  C07C45/45 ,  C07C45/63 ,  C07C45/71 ,  C07C405/00 ,  C07F7/18 ,  C07F7/22 ,  C07C177/00

CPC classification number: C07F7/2212 ,  C07C29/42 ,  C07C405/00 ,  C07C405/0025 ,  C07C45/00 ,  C07C45/45 ,  C07C45/63 ,  C07C45/71 ,  C07F7/1852

Abstract: The invention disclosed herein relates to pharmacologically active prostaglandins of the E and F series in which C-16 is substituted with hydroxyl and chloromethyl or bromomethyl as well as the pharmacologically acceptable, nontoxic lower alkyl esters and salts thereof, and to the intermediates and processes for producing such compounds.

Abstract translation: 本文公开的本发明涉及E和F系列的药理学活性前列腺素，其中C-16被羟基和氯甲基或溴甲基取代，以及其药理学上可接受的无毒低级烷基酯及其盐，以及其中间体和方法 生产这样的化合物。

公开(公告)号：US4202989A

公开(公告)日：1980-05-13

申请号：US821022

申请日：1977-08-01

Applicant: Middleton B. Floyd, Jr. ,  Martin J. Weiss ,  Charles V. Grudzinskas ,  Sow-Mei L. Chen

Inventor： Middleton B. Floyd, Jr. ,  Martin J. Weiss ,  Charles V. Grudzinskas ,  Sow-Mei L. Chen

IPC: C07C405/00 ,  C07F7/18 ,  C07F7/22 ,  C07C177/00

CPC classification number: C07C405/0033 ,  C07C405/00 ,  C07F7/1804 ,  C07F7/2212

Abstract: This disclosure describes novel 15-deoxy-16-hydroxy-16-substituted prostanoic acids and congeners thereof having utility as bronchodilators as hypotensive agents, and as agents for the control of excessive gastric secretion.

Abstract translation: 本公开描述了新型的15-脱氧-16-羟基-16-取代的前列腺酸及其同系物，其具有作为减压剂的支气管扩张剂的用途，以及用于控制过度胃分泌的药剂。

公开(公告)号：US4191699A

公开(公告)日：1980-03-04

申请号：US857714

申请日：1977-12-05

Applicant: Middleton B. Floyd, Jr. ,  Martin J. Weiss ,  Charles V. Grudzinskas ,  Sow-Mei L. Chen

Inventor： Middleton B. Floyd, Jr. ,  Martin J. Weiss ,  Charles V. Grudzinskas ,  Sow-Mei L. Chen

IPC: C07C29/10 ,  C07C29/42 ,  C07C45/29 ,  C07C49/227 ,  C07C49/743 ,  C07C49/753 ,  C07C405/00 ,  C07D307/42 ,  C07F7/18 ,  C07F7/22 ,  C07C177/00

CPC classification number: C07D307/42 ,  C07C29/10 ,  C07C29/42 ,  C07C405/00 ,  C07C405/0025 ,  C07C405/0033 ,  C07C45/29 ,  C07C49/227 ,  C07C49/743 ,  C07C49/753 ,  C07F7/1804 ,  C07F7/2212

Abstract: 15-Deoxy-16-hydroxy-16-ethynyl and 16-ethynylsubstituted prostanoic acids and congeners thereof, useful as bronchodilators, hypotensive agents, and as agents for the control of excessive gastric secretion.

Abstract translation: 15-脱氧-16-羟基-16-乙炔基和16-乙炔基取代的前列腺烷酸及其同系物，其可用作支气管扩张药，降血糖药和用作控制胃分泌过多的药剂。