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US5525735A Expired / Lapsed US ⏱️ 0.0 years remaining

Methods for synthesizing diverse collections of pyrrolidine compounds

Assignee: Affymax Technologies NV
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Filing: 1994-12-12
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Granted: 1996-06-11
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Expires: 2014-12-12
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Abstract

Abstract Disclosed are methods for synthesizing very large collections of diverse pyrrolidine compounds and derivatives thereof on solid supports and synthetic compound libraries comprising pyrrolidine groups and derivatives thereof prepared by such methods.

Inventors

  • 👤 Mark A. Gallop
  • 👤 Martin A. Murphy

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-02 15:58
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/04; C07D207/10; C07D207/16; B; B01; B01J; B01J2219/00; B01J2219/00274; B01J2219/00583; B01J2219/00592; B01J2219/00718; B01J2219/0072

Claims Analysis

Total Claims: 10
Claim 1
Independent Claim 86 words
A synthetic compound library comprising a plurality of different compounds each compound covalently linked to a solid support wherein each of said compounds comprise at least one pyrrolidinyl group which group is prepared by the method which comprises (a) selecting a solid support comprising at least one compound attached thereto which compound comprises a moiety selected from the group consisting of a complementary group having at least one site of carbon-carbon unsaturation and an azomethine ylide precursor; and (b) converting said moiety to a pyrrolidinyl group.
Claim 2
Dependent Claim 86 words
A synthetic compound library comprising a plurality of different compounds each compound covalently linked to a solid support wherein each of said compounds comprise at least one pyrrolidinyl group which group is prepared by the method which comprises (a) selecting a solid support comprising at least one compound attached thereto which compound comprises a moiety selected from the group consisting of a complementary group having at least one site of carbon-carbon unsaturation and an azomethine ylide precursor; and (b) converting said moiety to a pyrrolidinyl group.
Claim 3
Dependent Claim 25 words
The synthetic compound library according to claim 1 wherein each compound of said plurality of different compounds is covalently linked to the same solid support.
Claim 4
Dependent Claim 25 words
The synthetic compound library according to claim 1 wherein each compound of said plurality of different compounds is covalently linked to a different solid support.
Claim 5
Dependent Claim 31 words
The synthetic compound library according to claim 1 wherein each compound in said library comprises a peptide compound wherein the pyrrolidinyl group is located at any point in the peptide sequence.
Claim 6
Dependent Claim 21 words
The synthetic compound library according to claim 1 wherein each compound in said library comprises a plurality of different pyrrolidinyl compounds.
Claim 7
Dependent Claim 20 words
The synthetic compound library according to claim 1, further comprising the step of: (c) cleaving the compound from the support.
Claim 8
Dependent Claim 22 words
The synthetic compound library according to claim 1, further comprising the step of: (c) treating said pyrrolidinyl group with an acylating reagent.
Claim 9
Dependent Claim 52 words
The synthetic compound library according to claim 7, wherein the acylating reagent comprises a compound having the formula: HSCH.sub.2 CHR.sup.3 C(O)X wherein R 3 is selected from the group consisting of alkyl, alkoxy, carboxyl, carboxyl ester, R 5 --C(O)-- where R 5 is alkyl or aryl and X is bromine or chlorine.
Claim 10
Dependent Claim 19 words
The synthetic compound library according to claim 8, wherein each compound in said library comprises a different mercaptoacyl proline.

References Cited (Backward Citations)

US5143854A Cited
WO1991005058A1 Cited
WO1991017271A1 Cited
WO1991019818A1 Cited
WO1992002536A1 Cited
WO1993006121A1 Cited
WO1993008278A1 Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1999-06-11 1999-12-11 2000-06-11 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 2003-06-11 2003-12-11 2004-06-11 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2007-06-11 2007-12-11 2008-06-11 $7700.00 Window Closed / Lapsed

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