TH115253B - Benzothiazine derivatives, the preparation of this derivative and the use of this derivative as a medicine. - Google Patents
Benzothiazine derivatives, the preparation of this derivative and the use of this derivative as a medicine.Info
- Publication number
- TH115253B TH115253B TH1101001886A TH1101001886A TH115253B TH 115253 B TH115253 B TH 115253B TH 1101001886 A TH1101001886 A TH 1101001886A TH 1101001886 A TH1101001886 A TH 1101001886A TH 115253 B TH115253 B TH 115253B
- Authority
- TH
- Thailand
- Prior art keywords
- derivative
- medicine
- preparation
- hydrogen
- benzothiazine derivatives
- Prior art date
Links
- UJVBZCCNLAAMOV-UHFFFAOYSA-N 2H-1,2-benzothiazine Chemical class C1=CC=C2C=CNSC2=C1 UJVBZCCNLAAMOV-UHFFFAOYSA-N 0.000 title abstract 2
- 239000003814 drug Substances 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 3
- 239000001257 hydrogen Substances 0.000 claims abstract 3
- 150000001875 compounds Chemical class 0.000 claims abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 2
- 239000000126 substance Substances 0.000 claims abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 101710019698 Olfr5 Proteins 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- RTZKZFJDLAIYFH-UHFFFAOYSA-N diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 abstract 2
- VQGHOUODWALEFC-UHFFFAOYSA-N 2-Phenylpyridine Chemical compound C1=CC=CC=C1C1=CC=CC=N1 VQGHOUODWALEFC-UHFFFAOYSA-N 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 235000010290 biphenyl Nutrition 0.000 abstract 1
- 239000004305 biphenyl Substances 0.000 abstract 1
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 abstract 1
- 150000002148 esters Chemical group 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
Abstract
ความมุ่งหมายของการประดิษฐ์ปัจจุบันคือสารอนุพันธ์เบนโซไธอะซีน (derivatives of benzothiazine) ซึ่งมีประสิทธิภาพในการยับยั้ง 11 (สูตร)-HSD1 ไม่เพียงแต่ที่ระดับเอนไซม์เท่านั้น หากยังรวมถึงที่ระดับเซลล์ด้วย สารประกอบของการประดิษฐ์ปัจจุบันมีสูตรทั่วไป (I) (สูตรเคมี) I โดยที่ที่สำคัญคือ: R1 คือไฮโดรเจนหรือ OR1 คือเอสเทอร์หรืออีเธอร์ R2 คือแนฟธิลหรือ 1, 2, 3, 4-เตตระไฮโดร-แนฟธาลีนหรือไบฟีนิลหรือฟีนิลไพริดีนหรือ ฟีนิลที่ถูกแทนที่ R3 คือเมธิลหรือเอธิล R4 และ R'4 คือไฮโดรเจน: The aim of the present invention is a derivatives of benzothiazine, which is effective at inhibiting 11 (formula) -HSD1 not only at the enzyme level. If also at the cell level Current invention compounds have the general formula (I) (chemical formula) I, where the key is: R1 is hydrogen or OR1 is ester or ether, R2 is naphthyl or 1, 2, 3, 4. - Tetrahydro-Naphthalene or Biphenyl or Phenylpyridine or Phenyls that are replaced, R3 are methyl or ethyl, R4 and R'4 are hydrogen:
Claims (1)
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TH115253B true TH115253B (en) | 2012-07-31 |
| TH115253A TH115253A (en) | 2012-07-31 |
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