Patent EP0430459A1 successfully refreshed from Google Patents.
EP0430459A1
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Tetrahydronaphthalene derivatives and preparation thereof
Assignee: Tanabe Pharma Corp
•
Filing: 1990-11-06
•
Granted: —
•
Expires: 2010-11-06
Abstract
Abstract A tetrahydronaphthalene derivative of the formula: wherein R¹ is a substituted or unsubstituted phenyl group, naphthyl group, a sulfur- or nitrogen-containing heterocyclic group, a lower alkyl group or cycloalkyl group, and R² is hydroxymethyl group, carboxyl group, a lower alkoxycarbonyl group or a group of the formula: wherein R³ is hydrogen atom or a lower alkyl group, R⁴ is a lower alkoxycarbonyl-phenyl group, carboxy-phenyl group, a lower alkyl group, a lower alkoxycarbonyl-lower alkyl group or carboxy-lower alkyl group, and m and n are different and are 1 or 2, or a pharmaceutically acceptable salt thereof, which are useful as a platelet aggregation-inhibiting agent and as an agent for the treatment, amelioration and/or prophylaxis of a variety of thrombosis or embolism, coronary and cerebral vascular smooth muscle vellication, asthma, and the like, processes for the preparation thereof, and pharmaceutical composition containing said compound as an active ingredient.
Inventors
- 👤 Hideo Nakai
- 👤 Toyohura Yamashita
- 👤 Harumichi Kohno
- 👤 Yasuhiko Sasaki
- 👤 Okio Odawara
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-03 18:54
CPC Classifications
C; C07; C07C; C07C311/00; C07C311/22; C07C311/29; A; A61; A61P; A61P7/00; A61P7/02; C07C311/01; C07C311/02; C07C311/07; C07C311/14; C07C311/15; C07C311/20; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/62; C07D213/70; C07D213/71; C07D333/00; C07D333/02; C07D333/04; C07D333/26; C07D333/30; C07D333/34; C07C2602/00; C07C2602/02; C07C2602/04; C07C2602/10
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
110 words
A process for preparing a pharmaceutical composition, comprising mixing a tetrahydronaphthalene derivative of the formula: wherein R¹ is a substituted or unsubstituted phenyl group, naphthyl group, a sulfur- or nitrogen-containing heterocyclic group, a lower alkyl group or cycloalkyl group, and R² is hydroxymethyl group, carboxyl group, a lower alkoxycarbonyl group or a group of the formula: wherein R³ is hydrogen atom or a lower alkyl group, R⁴ is a lower alkoxycarbonyl-phenyl group, carboxy-phenyl group, a lower alkyl group, a lower alkoxycarbonyl-lower alkyl group or carboxy-lower alkyl group, and m and n are different and are 1 or 2, or a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable carrier therefor.
Claim 2
Dependent Claim
110 words
A process for preparing a pharmaceutical composition, comprising mixing a tetrahydronaphthalene derivative of the formula: wherein R¹ is a substituted or unsubstituted phenyl group, naphthyl group, a sulfur- or nitrogen-containing heterocyclic group, a lower alkyl group or cycloalkyl group, and R² is hydroxymethyl group, carboxyl group, a lower alkoxycarbonyl group or a group of the formula: wherein R³ is hydrogen atom or a lower alkyl group, R⁴ is a lower alkoxycarbonyl-phenyl group, carboxy-phenyl group, a lower alkyl group, a lower alkoxycarbonyl-lower alkyl group or carboxy-lower alkyl group, and m and n are different and are 1 or 2, or a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable carrier therefor.
Claim 3
Dependent Claim
49 words
A process as claimed in claim 1 in which R¹ is a phenyl group, a lower alkylphenyl group, a lower alkoxyphenyl group, a halogenophenyl group, naphthyl group, sulfur- or nitrogen-containing 5- or 6- membered heteromonocyclic groups, a lower alkyl group or cycloalkyl group of three to six carbon atoms.
Claim 4
Dependent Claim
32 words
A process as claimed in claim 2 in which R² is hydroxymethyl group, carboxyl group, or a group of the formula: wherein R³ is hydrogen atom and R⁴ is carboxy-lower alkyl group.
Claim 5
Dependent Claim
17 words
A process as claimed in any preceding claim in which m is 1 and n is 2.
Claim 6
Dependent Claim
31 words
A process as claimed in any one of claims 2 to 4 in which sulfur- or nitrogen-containing 5- or 6- membered heteromonocyclic groups of R¹ are thienyl group or pyridyl group.
Claim 7
Dependent Claim
51 words
A process as claimed in any preceding claim in which R¹ is a phenyl group, methylphenyl group, methoxyphenyl group, chlorophenyl group, thienyl group, methyl group or cyclohexyl group, and R² is carboxyl group or a group of the formula: wherein R³ is hydrogen atom and R⁴ is a carboxy-lower alkyl group.
Claim 8
Dependent Claim
36 words
A process as claimed in claim 6 in which R¹ is a chlorophenyl group, and R² is a group of the formula: wherein R³ is hydrogen atom and R⁴ is a carboxyethyl group or carboxypropyl group.
Claim 9
Dependent Claim
22 words
A process as claimed in claim 1 wherein the derivative of formula (1) is 4-([6-(4-chlorophenyl)sulfonylamino-5,6,7,8-tetrahydronaphthalene-2-yl]acetylamino)-n-butyric acid or a pharmaceutically acceptable salt thereof.
Claim 10
Dependent Claim
161 words
A process for preparing a tetrahydronaphthalene derivative of the formula: wherein R¹ is a substituted or unsubstituted phenyl group, naphthyl group, a sulfur- or nitrogen-containing heterocyclic group, a lower alkyl group or cycloalkyl group, and R² is hydroxymethyl group, carboxyl group, a lower alkoxycarbonyl group or a group of the formula: wherein R³ is hydrogen atom or a lower alkyl group, R⁴ is a lower alkoxycarbonyl-phenyl group, carboxy-phenyl group, a lower alkyl group, a lower alkoxycarbonyl-lower alkyl group or carboxy-lower alkyl group, and m and n are different and are 1 or 2, or a pharmaceutically acceptable salt thereof, which comprises: condensing an aminotetrahydronaphthalene derivative of the formula: wherein R², m and n are as defined above, or a salt thereof with a sulfonic acid compound of the formula: R¹SO₃H (III) wherein R¹ is as defined above, or a reactive derivative thereof, and when compound (I) is a free form, optionally further converting the product into a pharmaceutically acceptable salt thereof.
Claim 11
Dependent Claim
161 words
A process for preparing a tetrahydronaphthalene derivative of the formula: wherein R¹ is a substituted or unsubstituted phenyl group, naphthyl group, a sulfur- or nitrogen-containing heterocyclic group, a lower alkyl group or cycloalkyl group, and R² is hydroxymethyl group, carboxyl group, a lower alkoxycarbonyl group or a group of the formula: wherein R³ is hydrogen atom or a lower alkyl group, R⁴ is a lower alkoxycarbonyl-phenyl group, carboxy-phenyl group, a lower alkyl group, a lower alkoxycarbonyl-lower alkyl group or carboxy-lower alkyl group, and m and n are different and are 1 or 2, or a pharmaceutically acceptable salt thereof, which comprises: condensing an aminotetrahydronaphthalene derivative of the formula: wherein R², m and n are as defined above, or a salt thereof with a sulfonic acid compound of the formula: R¹SO₃H (III) wherein R¹ is as defined above, or a reactive derivative thereof, and when compound (I) is a free form, optionally further converting the product into a pharmaceutically acceptable salt thereof.
Claim 12
Dependent Claim
63 words
A process for preparing a tetrahydronaphthalene derivative of the formula: wherein R¹ is a substituted or unsubstituted phenyl group, naphthyl group, a sulfur- or nitrogen-containing heterocyclic group, a lower alkyl group or cycloalkyl group, and m and n are different and are 1 or 2, which comprises: reducing a compound of the formula (I-b): wherein R¹, m and n are as defined above.
Claim 13
Dependent Claim
63 words
A process for preparing a tetrahydronaphthalene derivative of the formula: wherein R¹ is a substituted or unsubstituted phenyl group, naphthyl group, a sulfur- or nitrogen-containing heterocyclic group, a lower alkyl group or cycloalkyl group, and m and n are different and are 1 or 2, which comprises: reducing a compound of the formula (I-b): wherein R¹, m and n are as defined above.
Claim 14
Dependent Claim
147 words
A process for preparing a tetrahydronaphthalene derivative of the formula: wherein R¹ is a substituted or unsubstituted phenyl group, naphthyl group, a sulfur- or nitrogen-containing heterocyclic group, a lower alkyl group or cycloalkyl group, R³ is hydrogen atom or a lower alkyl group, R⁴ is a lower alkoxycarbonyl-phenyl group, carboxy-phenyl group, a lower alkyl group, a lower alkoxycarbonyl-lower alkyl group or carboxy-lower alkyl group, and m and n are different and are 1 or 2, or a pharmaceutically acceptable salt thereof, which comprises: condensing a compound of the formula (I-b): wherein R¹, m and n are as defined above, or a reactive derivative at carboxyl group thereof with an amine comopound of the formula: R³-NH-R⁴ (IV) wherein R³ and R⁴ are as defined above or a salt thereof, and when compound (I-c) is a free form, optionally further converting the product into a pharmaceutically acceptable salt thereof.
Claim 15
Dependent Claim
147 words
A process for preparing a tetrahydronaphthalene derivative of the formula: wherein R¹ is a substituted or unsubstituted phenyl group, naphthyl group, a sulfur- or nitrogen-containing heterocyclic group, a lower alkyl group or cycloalkyl group, R³ is hydrogen atom or a lower alkyl group, R⁴ is a lower alkoxycarbonyl-phenyl group, carboxy-phenyl group, a lower alkyl group, a lower alkoxycarbonyl-lower alkyl group or carboxy-lower alkyl group, and m and n are different and are 1 or 2, or a pharmaceutically acceptable salt thereof, which comprises: condensing a compound of the formula (I-b): wherein R¹, m and n are as defined above, or a reactive derivative at carboxyl group thereof with an amine comopound of the formula: R³-NH-R⁴ (IV) wherein R³ and R⁴ are as defined above or a salt thereof, and when compound (I-c) is a free form, optionally further converting the product into a pharmaceutically acceptable salt thereof.
Claim 16
Dependent Claim
120 words
A process for preparing a tetrahydronaphthalene derivative of the formula: wherein R¹ is a substituted or unsubstituted phenyl group, naphthyl group, a sulfur- or nitrogen-containing heterocyclic group, a lower alkyl group or cycloalkyl group, R³ is hydrogen atom or a lower alkyl group, R⁵ is carboxy-phenyl group or a carboxy-lower alkyl group, and m and n are different and are 1 or 2, or a pharmaceutically acceptable salt thereof, which comprises: hydrolyzing a compound of the formula (I-e): wherein R⁶ is a lower alkoxycarbonyl-phenyl group or a lower alkoxycarbonyl-lower alkyl group. and R¹, R³, m and n are as defined above, and when compound (I-d) is a free form, optionally further converting the product into a pharmaceutically acceptable salt thereof.
Claim 17
Dependent Claim
120 words
A process for preparing a tetrahydronaphthalene derivative of the formula: wherein R¹ is a substituted or unsubstituted phenyl group, naphthyl group, a sulfur- or nitrogen-containing heterocyclic group, a lower alkyl group or cycloalkyl group, R³ is hydrogen atom or a lower alkyl group, R⁵ is carboxy-phenyl group or a carboxy-lower alkyl group, and m and n are different and are 1 or 2, or a pharmaceutically acceptable salt thereof, which comprises: hydrolyzing a compound of the formula (I-e): wherein R⁶ is a lower alkoxycarbonyl-phenyl group or a lower alkoxycarbonyl-lower alkyl group. and R¹, R³, m and n are as defined above, and when compound (I-d) is a free form, optionally further converting the product into a pharmaceutically acceptable salt thereof.
Claim 18
Dependent Claim
39 words
A process as claimed in any one of claims 9 to 12 wherein R¹ and R² are as defined in any one of claims 2 to 7, or the starting materials are chosen so as to produce 4([6-(4-chlorophenyl)sulfonylamino-5,6,7,8-tetrahydronaphthalene-2-yl]acetylamino)-n-butyric acid.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
Maintenance schedule is calculated for granted US utility patents.