EP0405506A1
Expired / Lapsed
EP
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Tetrapeptide type-B CCK receptor ligands
Assignee: Abbott Laboratories
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Filing: 1990-06-27
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Granted: —
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Expires: 2010-06-27
Abstract
Abstract A tetrapeptide type-B CCK receptor ligand of the formula A-B-C-D or a pharmaceutically acceptable salt thereof, which is useful for treating central nervous system disorders, substance abuse, gastrointestinal disorders, endocrine disorders, eating-related disorders and treatment of shock, respiratory and cardiocirculatory insufficiencies.
Inventors
- 👤 John Y.-L. Chung
- 👤 Michael D. Tufano
- 👤 Paul D. May
- 👤 Kazumi Shiosaki
- 👤 Alex M. Nadzan
- 👤 David S. Garvey
- 👤 Youe-Kong Shue
- 👤 Mark S. Brodie
- 👤 Mark W. Holladay
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-06 15:25
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/10; C07K5/1002; C07K5/1016; A; A61; A61P; A61P1/00; A61P11/00; A61P25/00; A61P25/28; A61P25/30; A61P39/00; A61P39/02; A61P9/00; C07K5/02; C07K5/0207; C07K5/08; C07K5/0802; C07K5/0804; C07K5/0808; C07K5/1024; A61K; A61K38/00
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
92 words
A compound of the formula: A-B-C-D wherein A is functionalized acetyl or R9-C(O)- wherein R₉ is heterotricyclic or carbotricyclic; B is a functionalized 2-aminopropionyl residue; or A-B taken together is functionalized piperazinedionyl or functionalized 5-amino-3-aza-4-keto-hexanoyl; C is wherein R₂₀ is hydrogen or loweralkyl and R₂₁ is carboxy or tetrazolyl; or B-C taken together is a bridged Ala-Asp residue or a bridged Ala-(tetrazolyl)Ala residue; and D is functionalized ethylamino, functionalized tetrahydroisoquinolyl, functionalized piperazinon-1-yl, dehydro-Phe amide or an analog of dehydro-Phe; or C-D taken together is functionalized succinimidyl; or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
92 words
A compound of the formula: A-B-C-D wherein A is functionalized acetyl or R9-C(O)- wherein R₉ is heterotricyclic or carbotricyclic; B is a functionalized 2-aminopropionyl residue; or A-B taken together is functionalized piperazinedionyl or functionalized 5-amino-3-aza-4-keto-hexanoyl; C is wherein R₂₀ is hydrogen or loweralkyl and R₂₁ is carboxy or tetrazolyl; or B-C taken together is a bridged Ala-Asp residue or a bridged Ala-(tetrazolyl)Ala residue; and D is functionalized ethylamino, functionalized tetrahydroisoquinolyl, functionalized piperazinon-1-yl, dehydro-Phe amide or an analog of dehydro-Phe; or C-D taken together is functionalized succinimidyl; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
29 words
The compound of Claim 1 wherein A is BOC-Trp or Ctp; B is Met, Leu, Nle, Tpp or 1,4-thiazane-3-carbonyl and D is Phe-NH₂, Tiq-NH₂, (dehydro)Phe-NH₂, (NMe)Phe-NH₂, α-Nal-NH₂ or β-Nal-NH₂.
Claim 4
Dependent Claim
18 words
A compound selected from the group consisting of: Ctp-Leu-Asp-Phe-NH₂; BOC-Trp-Leu-Asp-Tiq-NH₂; Ctp-Leu-Asp-N-Me-Phe-NH₂; Ctp-Leu-Asp-(dehydro)Phe-NH₂; Boc-Trp-Tpp-Asp-Phe-NH₂; Ctp-Tpp-Asp-(NMe)Phe-NH₂; Ctp-Tpp-Asp-α-Nal-NH₂; Ctp-Tpp-Asp-β-Nal-NH₂; and Ctp-1,4-thiazane-3-carbonyl-Asp-Phe-NH₂.
Claim 5
Dependent Claim
18 words
A compound selected from the group consisting of: Ctp-Leu-Asp-Phe-NH₂; BOC-Trp-Leu-Asp-Tiq-NH₂; Ctp-Leu-Asp-N-Me-Phe-NH₂; Ctp-Leu-Asp-(dehydro)Phe-NH₂; Boc-Trp-Tpp-Asp-Phe-NH₂; Ctp-Tpp-Asp-(NMe)Phe-NH₂; Ctp-Tpp-Asp-α-Nal-NH₂; Ctp-Tpp-Asp-β-Nal-NH₂; and Ctp-1,4-thiazane-3-carbonyl-Asp-Phe-NH₂.
Claim 6
Dependent Claim
1 words
Ctp-Tpp-Asp-Phe-NH₂.
Claim 7
Dependent Claim
1 words
Ctp-Tpp-Asp-Phe-NH₂.
Claim 8
Dependent Claim
31 words
Use of a therapeutically effective amount of a compound of claim 1, for mimicking the effects of CCK on CCK type-B receptors in a mammalian host in need of such treatment.
Claim 9
Dependent Claim
35 words
Use of a therapeutically effective amount of a compound of claim 1, for treating central nervous system dysfunctions, enhancing learning and memory or appetite related disorders in a mammalian host in need of such treatment.
Claim 10
Dependent Claim
25 words
Use of a therapeutically effective amount of a compound of claim 1 for treating substance abuse in a mammalian host in need of such treatment.
Claim 11
Dependent Claim
15 words
The use of Claim 7 wherein the substance abuse is alcohol addiction or nicotine addiction.
Claim 12
Dependent Claim
21 words
A CCK type-B receptor agonist composition comprising a pharmaceutical carrier and a therapeutically effective amount of a compound of Claim 1.
Claim 13
Dependent Claim
88 words
10 . A process for the preparation of a compound of Claim 1 comprising: a) stepwise coupling of the appropriately protected amino acids or amino acid analogs represented by A, A-B, B, C, C-D and D as defined herein, followed by removal of the protecting groups; or b) coupling of the appropriately protected fragments of dipeptide length or greater, said fragments comprising the amino acids or amino acid analogs represented by A, A-B, B, C, C-D and D as defined herein, followed by removal of the protecting groups.
References Cited (Backward Citations)
No citation records indexed.
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