*

292014927

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*1909 1914 1916 veratrineephedrineatropinepapaverine1922 1921

1926 Frederick Banting (insulin) John J. Abel (JPET ) 1928 1933 *

*

*1936 1941 (penicillin)

1925

1934

1935

1940

carpain

carpain

carpain

carpain

1932

1953

cestylpentacol

cresol

1936

1936

brown-rotenon

brown-rotenon

1933

arecholine

1935

digitalis-like

1935

()

1938

emetine

*

1943

1947

1946

1947

C35H52O6

1944

1953

1945

chinin

1951

1952

safrol

safrol

1951

ascaridole

1951

C24H40O8.2H2O

1951

1957

hinokitiol

hinokitiol

1943

sinomenin

* emetine

*

*

*

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* (improving circulation) (antithrombotic)

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* + 199312

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(-)*

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12DNA3456cGMP78910

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I Phase II IIIADME()

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*(2007-2010)(Lead optimization)(Candidate drug)General PharmacologyAcute/subacute Toxicology Early Pharmacokinetics Chemical synthesis (scale up) Phase I, II, IIITranslation medicine

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DCB-CA-1BMEC-101BMEC-1217BPDC-339PDC-748DCB-SLE-1DCB-AD-1SB221DCB-WH-1

*

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Chart3

Chart3

0.45

0.3

0.05

0.12

0.08

14%

4%

12%

29%

41%

Sheet1

IVD

45.00%30.00%5.00%12.00%8.00%

Sheet2

Sheet3

**

(VCRO)()93949596CT-01-----93.12.06CT-021---193.11.17CT-032---2-CT-05 34--794.10.18CT-08 -31-495.03.16CT-09-1--195.06.02CT-10 -34-795.10.23CT-12 -11782696.10.11CT-21--1-197.12.26CT-22SLE-4-4

* (1)

CT-01 12 110 45-55 -Kupperman index CT-02 534(1)377,:=38:39;442,:=20:22 (VAS; visual analog scale) score CT-03 56,:=46:10(ASAS; assessment of ankylosing spondylitis) response criteria

* (2)

CT-04 ,2860,:=30:30; :=30:30 (SAA; average symptom scores) CT-05 ,4,3:2(A,B)75:=36:39A:B:C=25:24:26 (Lanzas score)CT-06 , Phase II 50, := 42 :8: vWF antigen, IL-1 , HDL-C , NO

* (3)

CT-07 ,12 24;:=6:18 1. 2.VAS 3. CT-08,12, Phase II 57, :=41:16:=27:30 CT-09 , Phase II 87, :=43:44; :=47:40ADA-Cog (Alzheimers Disease Assessment Scale - Cognitive Subscale)CT-10 ,680,:=10:70; :=40:40WOMAC

*

*PG2 () (2010/04)(TFDA) INDNDA(2005/3) Monascus Purpureus WentHMG-CoA reductase ()

*FDA, Guidance for Industry Botanical Drug Products(CDER)(BRT)

19972004IND >50022006/10 Veregen (MediGene) Human papilloma virus (HPV)2012/12 Fulizaq(Salix Pharmaceutics) HIV/AIDS

1. CMC() ()2. 3. 4. 5. - 1.

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*

************************