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Meta-guanidine, urea, thiourea or azacyclic amino benzoic and derivatives as integrin antagaonists

A heterocyclic, amino technology, applied in the field of treatment of diseases mediated by αvβ3

Inactive Publication Date: 2002-06-05
GD SEARLE & CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it has also been demonstrated that RGD peptides are generally nonselective for RGD-dependent integrins, for example with α v beta 3 Most RGD peptides that bind also bind α v beta 5 , α v beta 1 and alpha IIb beta 3

Method used

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  • Meta-guanidine, urea, thiourea or azacyclic amino benzoic and derivatives as integrin antagaonists

Examples

Experimental program
Comparison scheme
Effect test

Embodiment I

[0209] R 7 = Me, Example FR 7 = Me, Example J

Embodiment K

[0211] R 7 = Et, Example H R 7 =Et, Example L

Embodiment 139

[0216] R 7 = Me,R 1 = ethynyl, R = Et, Example 140 R 7 = Me,R 1 =ethynyl, Example 141i) pyridine, dimethyl N-cyanodithioimidocarbonate, 70°C. ii) R 7 NH 2 , EtOH, reflux. iii) THF, MeOH, H 2 O, NaOH. iv) CH 2 Cl 2 , DMAP, NEt 3 , EDCl. v) THF, MeOH, H 2 O, NaOH, 2) H + .

[0217] FlowchartX

[0218] Flowchart XI i) N, N'-Bis-Boc-thiourea, DMF, NEt 3 , HgCl 2 , 0, 15 minsii) MeOH, THF, H 2 O, KOH. iii) CH 2 Cl 2 , TFA, 0°, 90mins.

[0219] Schemes IX, X and XI are additional examples of the synthesis of specific compounds of the invention. All starting materials and reagents are either commercially available or described in this specification. Additional methods, reagents, and conditions may be used by those skilled in the art for the synthesis.

[0220] Flowchart XII

[0221] In the compound 1) R 1 =CO 2 H(E) can be bought

[0222] (E) obtained by process V step A) wherein, refers...

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Abstract

The present invention relates to a class of compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions thereof and methods of using such compounds and compositions as alpha v beta 3 integrin antagonists.

Description

[0001] This application claims priority to US Application No. 60 / 003277, filed August 30, 1995, under 35 USC § 119(e). [0002] scope of invention [0003] The present invention relates to the use of alpha v beta 3 Integrin antagonists and thus pharmaceutical compounds for use in pharmaceutical compositions. The present invention also relates to the inhibition or antagonism of alpha v beta 3 Integrin to treat by alpha v beta 3 Methods of mediating disease. Background of the invention [0004] Integrins are a class of cell surface glycoproteins that regulate cell adhesion and are thus useful regulators of cell-adhesive interactions that occur in various biological processes. Integrins are heterodimers composed of α and β polypeptide subunits through non-covalent bonding. So far, 11 different α subunits and 6 β subunits have been identified. Various α subunits can combine with various β subunits to form specific integrins....

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/00A61K31/155A61K31/17A61K31/195A61K31/24A61K31/335A61K31/34A61K31/341A61K31/343A61K31/357A61K31/36A61K31/38A61K31/40A61K31/403A61K31/404A61K31/4045A61K31/41A61K31/415A61K31/4164A61K31/4168A61K31/4184A61K31/4196A61K31/44A61K31/4406A61K31/445A61K31/4453A61K31/4458A61K31/47A61K31/505A61K31/513A61K31/535A61K31/5375A61K31/54A61K31/541A61K31/70A61K31/7028A61K31/7034A61K38/00A61P5/38A61P25/06A61P35/00A61P35/04A61P43/00C07C275/28C07C275/42C07C279/18C07C279/24C07C279/28C07C311/19C07C311/37C07C313/34C07C317/50C07C323/59C07C323/62C07C323/63C07C335/22C07C335/28C07D207/14C07D207/22C07D209/16C07D211/72C07D213/55C07D213/61C07D213/74C07D215/14C07D223/12C07D231/06C07D231/12C07D231/14C07D233/50C07D233/64C07D235/30C07D239/14C07D239/26C07D239/54C07D239/545C07D249/14C07D295/12C07D295/14C07D295/20C07D295/215C07D295/22C07D307/54C07D307/79C07D307/81C07D317/60C07D317/64C07D319/18C07D319/20C07D333/20C07D333/24C07D333/28C07D401/12C07D401/14C07D405/10C07D405/12C07D413/12C07D417/12C07H15/203C07K5/062
CPCC07D239/545C07D239/14C07D231/06C07H15/203C07C323/59C07D401/14C07D317/60C07C275/42C07C323/63C07D233/50C07D333/24C07D239/26C07D231/12C07D307/54C07D319/18C07C311/19C07D295/215C07C279/18C07C323/62C07D223/12C07D307/81C07C317/50C07D405/12C07D333/28C07D213/61C07D207/14C07D413/12C07D307/79C07C279/24C07D215/14C07D401/12C07C335/22C07C311/37C07C335/28C07C279/28C07D417/12C07D231/14C07D211/72C07D213/55C07D249/14A61P19/00A61P25/06A61P35/00A61P35/04A61P43/00A61P5/38C07D213/56
Inventor P·G·卢明斯基M·克拉雷P·W·科林斯B·N·德塞R·J·林马克J·G·里科T·E·罗杰斯M·A·卢瑟尔
Owner GD SEARLE & CO
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