EP0334636A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Pyrrolopyrimidine derivatives, their production and use
Assignee: Takeda Pharmaceutical Co Ltd
•
Filing: 1989-03-22
•
Granted: —
•
Expires: 2009-03-22
Abstract
Abstract A compound of the formula wherein the ring Ⓐ is a pyrrole or pyrroline ring, X is an amino group or a hydroxyl group, Y is a hydrogen atom, an amino group or a hydroxyl group, R is a hydrogen atom, a fluorine atom, an alkyl group, an alkenyl group or an alkynyl groups, -COOR¹ and -COOR² are independently carboxyl group which may be esterified and n is an integer of 2 to 4, and R may be different in each of the n repeating units, and salts thereof have excellent antitumor effects, and can be used as antitumor agents in mammals.
Inventors
- 👤 Hiroshi Akimoto
- 👤 Takenori Hitaka
- 👤 Tetsuo Miwa
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-23 19:43
CPC Classifications
C; C07; C07D; C07D487/00; C07D487/02; C07D487/04; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505
Claims Analysis
Total Claims: 22
Claim 1
Independent Claim
89 words
A compound of the formula wherein the ring Ⓐ is a pyrrole or pyrroline ring, X is an amino group or a hydroxyl group, Y is a hydrogen atom, an amino group or a hydroxyl group, R is a hydrogen atom, a fluorine atom, an alkyl group, an alkenyl group or an alkynyl group, -COOR¹ and -COOR² are independently carboxyl groups which may be esterified and n is an integer of 2 to 4, and R may be different in each of the n repeating units, and salts thereof,
Claim 2
Dependent Claim
89 words
A compound of the formula wherein the ring Ⓐ is a pyrrole or pyrroline ring, X is an amino group or a hydroxyl group, Y is a hydrogen atom, an amino group or a hydroxyl group, R is a hydrogen atom, a fluorine atom, an alkyl group, an alkenyl group or an alkynyl group, -COOR¹ and -COOR² are independently carboxyl groups which may be esterified and n is an integer of 2 to 4, and R may be different in each of the n repeating units, and salts thereof,
Claim 3
Dependent Claim
15 words
The compounds as claimed in claim 1, wherein the ring Ⓐ is a pyrrole ring.
Claim 4
Dependent Claim
15 words
The compound as claimed in claim 1, wherein the ring Ⓐ is a pyrroline ring.
Claim 5
Dependent Claim
13 words
The compound as claimed in claim 1, wherein X is an amino group.
Claim 6
Dependent Claim
13 words
The compound as claimed in claim 1, wherein X is a hydroxyl group.
Claim 7
Dependent Claim
13 words
The compound as claimed in claim 1, wherein Y is a hydrogen atom.
Claim 8
Dependent Claim
13 words
The compound as claimed in claim 1, wherein Y is an amino group.
Claim 9
Dependent Claim
13 words
The compound as claimed in claim 1, wherein Y is a hydroxyl group.
Claim 10
Dependent Claim
13 words
The compound as claimed in claim 1, wherein R is a hydrogen atom.
Claim 11
Dependent Claim
26 words
The compound as claimed in claim 1, wherein R is a fluorine atom, a C₁₋₃ alkyl group, a C₂₋₅ alkenyl group or a C₂₋₅ alkynyl group.
Claim 12
Dependent Claim
15 words
The compound as claimed in claim 1, wherein -COOR¹ and -COOR² are independently carboxyl groups.
Claim 13
Dependent Claim
16 words
The compound as claimed in claim 1, wherein -COOR¹ and -COOR² are independently esterified carboxyl groups.
Claim 14
Dependent Claim
11 words
The compound as claimed in claim 1, wherein n is 3.
Claim 15
Dependent Claim
13 words
The compound as claimed in claim 1, wherein n is 2 or 4.
Claim 16
Dependent Claim
88 words
A compound of the formula wherein the ring Ⓐ is a pyrrole or pyrroline ring, X is an amino group or a hydroxyl group, Y is a hydrogen atom, an amino group or a hydroxyl group, R is a hydrogen atom, a fluorine atom, an alkyl group, an alkenyl group or an alkynyl group, -COOR³ is a carboxyl group which may be esterified and n is an integer of 2 to 4, and R may be different in each of the n repeating units, or a salt thereof.
Claim 17
Dependent Claim
88 words
A compound of the formula wherein the ring Ⓐ is a pyrrole or pyrroline ring, X is an amino group or a hydroxyl group, Y is a hydrogen atom, an amino group or a hydroxyl group, R is a hydrogen atom, a fluorine atom, an alkyl group, an alkenyl group or an alkynyl group, -COOR³ is a carboxyl group which may be esterified and n is an integer of 2 to 4, and R may be different in each of the n repeating units, or a salt thereof.
Claim 18
Independent Claim
143 words
A method for producing a compound of the formula wherein the ring Ⓐ is a pyrrole or pyrroline ring, X is an amino agroup or a hydroxyl group, Y is a hydrogen atom, an amino group or a hydroxyl group, R is hydrogen atom, a fluorine atom, an alkyl group, an alkenyl group or an alkynyl group, -COOR³ is a carboxyl group which may be esterified and n is an integer of 2 to 4, and R may be different in each of the n repeating units, and salts thereof, which comprises reacting a compound of the formula wherein the ring Ⓐ, X, Y, R and n are the same defined above or a refractive derivative at the carboxyl group or a salt thereof, with a compound of the formula wherein -COOR¹ and -COOR² are the same as defined above, or salts thereof.
Claim 19
Independent Claim
143 words
A method for producing a compound of the formula wherein the ring Ⓐ is a pyrrole or pyrroline ring, X is an amino agroup or a hydroxyl group, Y is a hydrogen atom, an amino group or a hydroxyl group, R is hydrogen atom, a fluorine atom, an alkyl group, an alkenyl group or an alkynyl group, -COOR³ is a carboxyl group which may be esterified and n is an integer of 2 to 4, and R may be different in each of the n repeating units, and salts thereof, which comprises reacting a compound of the formula wherein the ring Ⓐ, X, Y, R and n are the same defined above or a refractive derivative at the carboxyl group or a salt thereof, with a compound of the formula wherein -COOR¹ and -COOR² are the same as defined above, or salts thereof.
Claim 20
Dependent Claim
104 words
Anti-tumor composition containing an effective tumor-inhibiting amount of a compound of the formula wherein the ring Ⓐ is a pyrrole or pyrroline ring, X is an amino group or hydroxyl group, Y is a hydrogen atom, an amino group or a hydroxyl group, R is a hydrogen atom, a fluorine atom, an alkyl group, an alkenyl group or an alkynyl group, -COOR¹ and -COOR² are independently carboxyl groups which may be esterified and n is an integer of 2 to 4, and R may be different in each of the n repeating units, or its pharmaceutically acceptable salt, and a diluent or carrier therefor.
Claim 21
Dependent Claim
104 words
Anti-tumor composition containing an effective tumor-inhibiting amount of a compound of the formula wherein the ring Ⓐ is a pyrrole or pyrroline ring, X is an amino group or hydroxyl group, Y is a hydrogen atom, an amino group or a hydroxyl group, R is a hydrogen atom, a fluorine atom, an alkyl group, an alkenyl group or an alkynyl group, -COOR¹ and -COOR² are independently carboxyl groups which may be esterified and n is an integer of 2 to 4, and R may be different in each of the n repeating units, or its pharmaceutically acceptable salt, and a diluent or carrier therefor.
Claim 22
Dependent Claim
28 words
The use of a compound (I) as defined in claim 1, or a pharmaceutically acceptable salt thereof in the preparation of a medicine for anti-tumor or cancer therapy.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
Maintenance schedule is calculated for granted US utility patents.