公开(公告)号：GB2113678A

公开(公告)日：1983-08-10

申请号：GB8235222

申请日：1982-12-10

Applicant: NAT RES DEV

Inventor： JONES ROBERT LESLIE ,  WILSON NORMAN HAPPER

IPC: A61K31/16 ,  A61K31/17 ,  A61K31/195 ,  A61K31/215 ,  A61K31/557 ,  A61P7/02 ,  C07C59/74 ,  A61P11/08 ,  A61P29/00 ,  C07C43/315 ,  C07C45/44 ,  C07C51/00 ,  C07C59/325 ,  C07C59/353 ,  C07C59/62 ,  C07C59/80 ,  C07C59/86 ,  C07C67/00 ,  C07C69/608 ,  C07C69/716 ,  C07C69/738 ,  C07C229/28 ,  C07C229/32 ,  C07C231/00 ,  C07C233/05 ,  C07C233/65 ,  C07C235/06 ,  C07C235/20 ,  C07C235/46 ,  C07C237/24 ,  C07C239/00 ,  C07C275/26 ,  C07C275/28 ,  C07C335/16 ,  C07C401/00 ,  C07C405/00 ,  C07D213/55 ,  C07D277/62 ,  C07D307/00 ,  C07D493/00 ,  C07D493/08 ,  C07C101/02 ,  A61K31/00 ,  C07C127/19 ,  C07C157/09

Abstract: Novel compounds have a formula (I) wherein represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1] heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R and at the 6-position by the group ANR R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R and at the 3-position by the group ANR R or at the 2-position by the group ANR R and at the 3-position by the group R , a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R and at the 5-position by the group ANR R or a 1-hydroxycyclopentane substituted at the 2-position by the group R and at the 2-position by the group ANR R, R is a 6-carboxyhex-2-enyl group or a modification thereof as defined herein; A is an unbranched or branched aliphatic hydrocarbon group with a chain length between the points of attachment to the divalent cyclic group and to the group NR R of 1 to 5 carbon atoms or such a group substituted by an aromatic group; R is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by an aromatic group or groups, and R is a group -CO.NR R , -CS.NR R , -CNH.NR R , -CO.R or -CS.R in which R is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by an aromatic group or groups, and R is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly by an aromatic.

公开(公告)号：DE3062376D1

公开(公告)日：1983-04-28

申请号：DE3062376

申请日：1980-01-04

Applicant: NAT RES DEV

Inventor： JONES ROBERT LESLIE ,  WILSON NORMAN HAPPER

IPC: A61K31/15 ,  C07C131/00

公开(公告)号：AU598789B2

公开(公告)日：1990-07-05

申请号：AU6842687

申请日：1987-01-15

Applicant: NAT RES DEV

Inventor： JONES ROBERT LESLIE ,  WILSON NORMAN HAPPER

IPC: C07C59/80 ,  C07C62/34 ,  C07C62/36 ,  C07C405/00 ,  C07D493/08 ,  C07C131/00 ,  A61K31/19 ,  A61K31/215 ,  A61K31/557 ,  C07C59/13 ,  C07C69/708 ,  C07C133/02 ,  C07C149/26 ,  C07C159/00

公开(公告)号：DE3762415D1

公开(公告)日：1990-05-31

申请号：DE3762415

申请日：1987-01-15

Applicant: NAT RES DEV

Inventor： JONES ROBERT LESLIE ,  WILSON NORMAN HAPPER

IPC: C07C59/80 ,  C07C62/34 ,  C07C62/36 ,  C07C405/00 ,  C07D493/08 ,  C07C251/32 ,  C07C281/06 ,  C07C337/00

公开(公告)号：DE3280020D1

公开(公告)日：1989-12-21

申请号：DE3280020

申请日：1982-12-10

Applicant: NAT RES DEV

Inventor： JONES ROBERT LESLIE ,  WILSON NORMAN HAPPER

IPC: C07C59/74 ,  A61K31/16 ,  A61K31/17 ,  A61K31/195 ,  A61K31/215 ,  A61K31/557 ,  A61P7/02 ,  A61P11/08 ,  A61P29/00 ,  C07C43/315 ,  C07C45/44 ,  C07C51/00 ,  C07C59/325 ,  C07C59/353 ,  C07C59/62 ,  C07C59/80 ,  C07C59/86 ,  C07C67/00 ,  C07C69/608 ,  C07C69/716 ,  C07C69/738 ,  C07C229/28 ,  C07C229/32 ,  C07C231/00 ,  C07C233/05 ,  C07C233/65 ,  C07C235/06 ,  C07C235/20 ,  C07C235/46 ,  C07C237/24 ,  C07C239/00 ,  C07C275/26 ,  C07C275/28 ,  C07C335/16 ,  C07C401/00 ,  C07C405/00 ,  C07D213/55 ,  C07D277/62 ,  C07D307/00 ,  C07D493/00 ,  C07D493/08 ,  C07C127/15 ,  C07C157/05 ,  C07C101/28 ,  A61K31/19 ,  A61K31/34

Abstract: Novel compounds have a formula (I) wherein represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1] heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R and at the 6-position by the group ANR R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R and at the 3-position by the group ANR R or at the 2-position by the group ANR R and at the 3-position by the group R , a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R and at the 5-position by the group ANR R or a 1-hydroxycyclopentane substituted at the 2-position by the group R and at the 2-position by the group ANR R, R is a 6-carboxyhex-2-enyl group or a modification thereof as defined herein; A is an unbranched or branched aliphatic hydrocarbon group with a chain length between the points of attachment to the divalent cyclic group and to the group NR R of 1 to 5 carbon atoms or such a group substituted by an aromatic group; R is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by an aromatic group or groups, and R is a group -CO.NR R , -CS.NR R , -CNH.NR R , -CO.R or -CS.R in which R is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by an aromatic group or groups, and R is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly by an aromatic.

公开(公告)号：DE3067397D1

公开(公告)日：1984-05-10

申请号：DE3067397

申请日：1980-01-04

Applicant: NAT RES DEV

Inventor： JONES ROBERT LESLIE ,  WILSON NORMAN HAPPER

IPC: C07C59/11 ,  C07C59/205 ,  C07C59/46 ,  C07C59/80

公开(公告)号：DE3063709D1

公开(公告)日：1983-07-21

申请号：DE3063709

申请日：1980-01-04

Applicant: NAT RES DEV

Inventor： JONES ROBERT LESLIE ,  WILSON NORMAN HAPPER

IPC: A61K31/19 ,  A61K31/557 ,  A61P7/02 ,  A61P43/00 ,  C07C41/54 ,  C07C43/315 ,  C07C45/44 ,  C07C59/46 ,  C07C59/62 ,  C07C59/74 ,  C07C59/80 ,  C07C67/00 ,  C07C239/00 ,  C07C241/00 ,  C07C251/82 ,  C07C281/08 ,  C07C405/00 ,  C07C109/12 ,  C07C133/06 ,  A61K31/16 ,  A61K31/175

Abstract: Novel bicyclo [2,2,1] heptanes and hept-2-enes are substituted at the 5-position by a 6-carboxyhex-2-enyl group or a modification thereof, and at the 6-position by a grouping -C(R)=N-NHCO-(NH)a-R' in which R is hydrogen, an aliphatic hydrocarbon residue, an aromatic residue or an aliphatic hydrocarbon residue substituted by an aromatic residue, a is 0 or 1 and R' is an aliphatic hydrocarbon residue, an aromatic residue, or an aliphatic hydrocarbon residue substituted directly or through an oxygen or sulphur atom by an aromatic residue. The compounds are of value for use in pharmaceutical compositions particularly in the context of the inhibition of thromboxane activity.

公开(公告)号：GB2218311A

公开(公告)日：1989-11-15

申请号：GB8911736

申请日：1989-05-22

Applicant: NAT RES DEV

Inventor： JONES ROBERT LESLIE ,  WILSON NORMAN HAPPER

IPC: C07C59/80 ,  C07C405/00 ,  C07D493/08

公开(公告)号：AU578386B2

公开(公告)日：1988-10-20

申请号：AU7002987

申请日：1987-03-13

Applicant: NAT RES DEV

Inventor： JONES ROBERT LESLIE ,  WILSON NORMAN HAPPER

IPC: C07C59/74 ,  A61K31/16 ,  A61K31/17 ,  A61K31/195 ,  A61K31/215 ,  A61K31/557 ,  A61P7/02 ,  A61P11/08 ,  A61P29/00 ,  C07C43/315 ,  C07C45/44 ,  C07C51/00 ,  C07C59/325 ,  C07C59/353 ,  C07C59/62 ,  C07C59/80 ,  C07C59/86 ,  C07C67/00 ,  C07C69/608 ,  C07C69/716 ,  C07C69/738 ,  C07C229/28 ,  C07C229/32 ,  C07C231/00 ,  C07C233/05 ,  C07C233/65 ,  C07C235/06 ,  C07C235/20 ,  C07C235/46 ,  C07C237/24 ,  C07C239/00 ,  C07C275/26 ,  C07C275/28 ,  C07C335/16 ,  C07C401/00 ,  C07C405/00 ,  C07D213/55 ,  C07D277/62 ,  C07D307/00 ,  C07D493/00 ,  C07D493/08 ,  C07C101/28 ,  C07C69/73 ,  C07D495/08

Abstract: Novel compounds have a formula (I) wherein represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1] heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R and at the 6-position by the group ANR R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R and at the 3-position by the group ANR R or at the 2-position by the group ANR R and at the 3-position by the group R , a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R and at the 5-position by the group ANR R or a 1-hydroxycyclopentane substituted at the 2-position by the group R and at the 2-position by the group ANR R, R is a 6-carboxyhex-2-enyl group or a modification thereof as defined herein; A is an unbranched or branched aliphatic hydrocarbon group with a chain length between the points of attachment to the divalent cyclic group and to the group NR R of 1 to 5 carbon atoms or such a group substituted by an aromatic group; R is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by an aromatic group or groups, and R is a group -CO.NR R , -CS.NR R , -CNH.NR R , -CO.R or -CS.R in which R is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by an aromatic group or groups, and R is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly by an aromatic.

公开(公告)号：GB2187451A

公开(公告)日：1987-09-09

申请号：GB8700836

申请日：1987-01-15

Applicant: NAT RES DEV

Inventor： JONES ROBERT LESLIE ,  WILSON NORMAN HAPPER

IPC: C07C59/80 ,  C07C62/34 ,  C07C62/36 ,  C07C405/00 ,  C07D493/08 ,  C07C131/00 ,  A61K31/15 ,  C07C59/00 ,  C07C133/00

Abstract: Novel compounds have the formula (I> represents one of the divalent cyclic groups the letters a and b indicating in each case the points of attachment of the substituents R and CV(R )-NV'R, respectively; R is a group -(CH2)b -(A)a-(CH2)c-B-CH2-CO2R' in which A and B are each separately oxygen or sulphur, a is 0, b is 0 and c is an integer from 3 to 10, or a is 1, b is 0 or an integer from 1 to 7 and c is an integer from 2 to 9 with the sum of b and c being from 2 to 9, and CO2R' is a carboxy group or an amide, ester or salt derivative thereof; V and V' either each separately is hydrogen or together are the second bond of a carbon-nitrogen double bond; R is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by an aromatic group directly or through an oxygen or sulphur atom; and R is a hydrzino, hydrazono, oximino or oxamino group. The compounds are of value for use in pharmaceutical compositions particularly in the context of the inhibition of thromboxane acitivity. Intermediates of formula IIIa are also claimed: