Beruflich Dokumente
Kultur Dokumente
logout
Post New Content Invite People
Inbox Contacts Groups
Media Locker atp cooperative
Shop Search Inbox Sear
Media ch
Locker Invit
atp e
cooperative Post
"atpcorporation" Website: GODSEND Products- Fulvic
Acid ("Miracle Molecule") & Natural ZEOLITES , * * * "
F R E E " in the P H I L I P P I N E S ! ! ! . with
"ORGANIC GERMANIUM" - SYNTHESIZED by ATP with
the DIVINE PROVIDENCE of our CREATOR ****
CONTACT US / JOIN US . . . . TOGETHER LET'S MAKE
A BEAUTIFUL WOLD * * * *
HomeNotesBlogPhotosVideoMusicCalendarReviewsLinks
You atpcoop
atp
cooperat
ive
Online
now
Quezon
City, NCR
U
pgrade
Account
C
ustomize
My Site
P
romote My
may wa nt to
Site
M
y Contacts
--------------------------------
----
Process for making ORGANIC
GERMANIUM (US PATENT #03).
By - ATP Global Foundtion.
Series # 030
---------------------------------
Patents/Preparation of Opioid
peptide-degrading enzyme
inhibitor with a germanium
compound
United States
4,748,187
Patent
Kakimoto , et al. May 31, 1988
Opioid peptide-
degrading enzyme
inhibitor with a
germanium
compound
Abstract
The present invention provides (1) a
new organogermanium compound of
the following general formula:
##STR1## wherein A represents a
hydrogen atom, a lower alkyl group
such as a methyl or ethyl group or a
phenyl group, B represents a hydrogen
atom or a lower alkyl group as
mentioned above and Z represents a
hydroxyl or amino group and (2) an
opioid peptide-degrading enzyme
inhibitor containing the compound (1)
as a principal ingredient.
.
Inventors: Kakimoto; Norihiro (Tokyo, JP);
Katayama; Takashi (Tokyo, JP);
Tadahiko (Saitama, JP); Ohnishi; Tsuto
(Tokyo, JP)
Assignee: Asai Germanium Research Institute
(Tokyo, JP)
Appl. No.: 930561
Filed: November 14, 1986
Foreign Application Priority Data
Jul 01, 1983[JP] 58-119856
Jul 11, 1983[JP] 58-125725
Claims
What is claimed is:
H.sub.2 N-Tyr-GlY-Gly-Phe-Met-OH
EXAMPLE 1
Compound (1)
______________________________________
elementary analysis:
Ge C H S
______________________________________
found 37.44 18.61 2.62 24.83
calculated 37.41 18.58 2.62 24.88
______________________________________
Compound (4)
______________________________________
elementary analysis:
Ge C H S
______________________________________
calculated: 32.73 27.07 4.09 21.68
found: 32.50 27.13 4.02 21.92
______________________________________
EXAMPLE 2
Compound (11)
______________________________________
elementary analysis:
Ge C H N S
______________________________________
calculated:
32.87 27.20 4.56 6.34 21.87
found: 32.59 27.37 4.43 6.25 21.56
______________________________________
TABLE (1)
___________________________________________________________
____________
Physical Properties
Elementary
calculated
Melt-
Com-
analysis found ing Yield
pound
Ge C H S point
IR(KBr, cm.sup.-1)
(Solvent)
NMR (.delta.) (%)
___________________________________________________________
____________
(2)
##STR11##
##STR12##
##STR13##
##STR14##
185 (dec)
3420, 1705, 425
CD.sub.3 OD
##STR15## 57.7
(3)
##STR16##
##STR17##
##STR18##
##STR19##
196 3410, 1705, 425
CD.sub.3 OD
##STR20## 93
(5)
##STR21##
##STR22##
##STR23##
##STR24##
205 (dec)
3450, 2960, 1700, 1460, 1380 1220,
1130, 680,
620, 425 CD.sub.3 OD
1.46(6H, s,
(CH.sub.3).sub.2), .sub.
2.60(2H, s, CH.sub.2)
80.3.--
(6)
##STR25##
##STR26##
##STR27##
##STR28##
265 (dec)
3450, 3040, 2850, 1710, 1600 1410,
1230, 700,
425 CD.sub.3 OD
3.00(2H, d, C H.sub.2 CO
.sub.-- 3.55(1H, t, GeCH)
.sub.-- 7.25(5H, m, C.sub
H.sub.5) .sub.--
94.1
(7)
##STR29##
##STR30##
##STR31##
##STR32##
215 (dec)
3450, 3030, 2980, 1705, 1455 1210,
820, 700,
680, 420 CD.sub.3 OD
1.43(3H, d, CH.sub.3),
.sub.-- 3.27(2 .sub.--H, m
CHCH), .sub.-- 7.17(5H,
C.sub.6 H.sub.5) .sub.--
86.0
___________________________________________________________
____________
TABLE (2)
___________________________________________________________
____________
Elementary
calculated Melt-
Com-
analysis found ing IR(KBr, Yield
pound
Ge C H N S point
cm.sup.-1)
(solvent)
NMR (.delta.) (%)
___________________________________________________________
____________
(8)
##STR33##
##STR34##
##STR35##
##STR36##
##STR37##
225.about. 226 (dec)
3340, 1665, 1620, 1200 1400,
DMFd.sub.7
1.98(2H, t, GeCH.sub.2)
.sub.-- 2.56(2H, t, COC
.sub.--H.sub.2)
60.2
(9)
##STR38##
##STR39##
##STR40##
##STR41##
##STR42##
248 (dec)
3300, 3200, 1600, 1400 430
CD.sub.3 OD
1.33(3H, d, GeCHCH.sub
.sub.-- 2.17.about.2.77 (3
m, GeC .sub.--HC .sub.--
H.sub.
2) 84.1
(10)
##STR43##
##STR44##
##STR45##
##STR46##
##STR47##
225 (dec)
3300, 3200, 1660, 1460 1400,
CD.sub.3 OD
1.23(3H, d, CH.sub.3) .su
.67.about.2.25 (3H, m, G
.sub.--HCH.sub.2) .sub.--
83.2
(12)
##STR48##
##STR49##
##STR50##
##STR51##
##STR52##
230 (dec)
3400, 3200, 2960, 1660, 1460 11
CD.sub.3 OD
1.22(6H, s,
CH.sub.3CCH.sub.3) .sub
2.60(2H, s, CH.sub.2CO)
.sub.-- 76.5
(13)
##STR53##
##STR54##
##STR55##
##STR56##
##STR57##
210 (dec)
3450, 3350, 3200, 1660, 1600 14
765,
700, 420
CD.sub.3 OD
2.90(2H, m, CH.sub.2) .s
.55(1H, m, CH) .sub.--
7.19(5H, s, -.sub.6 H.sub
.sub.-- 81.8
(14)
##STR58##
##STR59##
##STR60##
##STR61##
##STR62##
215 (dec)
3450, 3350, 3200, 1660, 1455 14
700,
420 CD.sub.3 OD
1.42(3H, m, CH.sub.3) .s
.23(2H, m, CHCH) .sub.--
7.15(5H, S, C.sub.6 H.su
.sub.-- 82.3
___________________________________________________________
____________
EXAMPLE 3
Pharmacological effects of the compound of the prese
invention
TABLE (3)
___________________________________________________________
____________
Enzyme
Origin
Bovine longitudinal muscle
Name
Dipeptidyl- Dipeptidyl-
carboxy- Carboxy-
amino-
Amino-
Principal
peptidase
peptidase
peptidase
peptidase
ingredient
Substrate
(1 .mu.g/1 ml)
Hip--His--Leu
Hip--L-PheAla
Enkephalin
Enkephalin
___________________________________________________________
____________
Compound (1)
76.4% - - -
Compound (2)
85.0% 6.2% - -
Compound (3)
80.0% - - -
Compound (4)
60% - - 58%
Compound (5)
78.8% - + 88.0%
Compound (6)
74.2% 89.8% + 97.0%
Compound (7)
76.8% - + -
Compound (8)
78.3% - - -
Compound (9)
68.4% - - -
Compound (10)
73.4% - - -
Compound (11)
+ - + -
Compound (12)
+ - + -
Compound (13)
+ - + -
Compound (14)
+ - + -
___________________________________________________________
____________
TABLE (4)
______________________________________
Enzyme
Origin
Monkey brain
Name
Dipeptidylaminopeptidase
Aminopeptidase
Substrate
Compound Enkephalin
______________________________________
(1) 98.2% 87.8%
(2) 97.9% 87.6%
(3) 97.7% 85.6%
(8) - -
(9) - -
(10) - -
(4) 62% -
______________________________________
TABLE (6)
______________________________________
Compound IC50 (.mu.g/m)
______________________________________
(3) 450
(6) 440
Arphamenine A 810
Arphamenine B 650
______________________________________
*****
reply
5851:U2FsdGVkX
Add a comment to this blog entry, for
everyone
Send atpcoop a personal message
navydiverjlm
ayene88
Viewing History
This Blog Entry has been viewed 2 times by 2 people, most recently on Jun 23, '09
See Detailed Viewing History
View This Page as Another User
© 2009 Multiply, Inc. About · Blog · Terms · Privacy · Corporate · Advertise · Contact · Help