TH96112B - Benzyloxazole and oxazolopyridine are useful as inhibitors of Janus kinase. - Google Patents
Benzyloxazole and oxazolopyridine are useful as inhibitors of Janus kinase.Info
- Publication number
- TH96112B TH96112B TH701004556A TH0701004556A TH96112B TH 96112 B TH96112 B TH 96112B TH 701004556 A TH701004556 A TH 701004556A TH 0701004556 A TH0701004556 A TH 0701004556A TH 96112 B TH96112 B TH 96112B
- Authority
- TH
- Thailand
- Prior art keywords
- compounds
- formula
- replaced
- benzyloxazole
- oxazolopyridine
- Prior art date
Links
- CUYUPLKTWHWPQY-UHFFFAOYSA-N 2-benzyl-1,3-oxazole Chemical compound C=1C=CC=CC=1CC1=NC=CO1 CUYUPLKTWHWPQY-UHFFFAOYSA-N 0.000 title 1
- 102000015617 Janus Kinases Human genes 0.000 title 1
- 108010024121 Janus Kinases Proteins 0.000 title 1
- BFPLMTPHDFFMTG-UHFFFAOYSA-N [1,3]oxazolo[5,4-b]pyridine Chemical compound C1=CN=C2OC=NC2=C1 BFPLMTPHDFFMTG-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 6
- 239000000126 substance Substances 0.000 claims abstract 2
- LFVPBERIVUNMGV-UHFFFAOYSA-N fasudil hydrochloride Chemical group Cl.C=1C=CC2=CN=CC=C2C=1S(=O)(=O)N1CCCNCC1 LFVPBERIVUNMGV-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- -1 cyano, hydroxyl Chemical group 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 201000010099 disease Diseases 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 238000000034 method Methods 0.000 abstract 3
- 241001465754 Metazoa Species 0.000 abstract 2
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 2
- 230000001225 therapeutic effect Effects 0.000 abstract 2
- 238000002560 therapeutic procedure Methods 0.000 abstract 2
- BCMCBBGGLRIHSE-UHFFFAOYSA-N 1,3-benzoxazole Chemical compound C1=CC=C2OC=NC2=C1 BCMCBBGGLRIHSE-UHFFFAOYSA-N 0.000 abstract 1
- BFJMHTOBRRZELQ-UHFFFAOYSA-N 3-iodo-2h-pyrazolo[3,4-c]pyridine Chemical compound N1=CC=C2C(I)=NNC2=C1 BFJMHTOBRRZELQ-UHFFFAOYSA-N 0.000 abstract 1
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 abstract 1
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 abstract 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 abstract 1
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 230000000771 oncological effect Effects 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 230000035755 proliferation Effects 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 abstract 1
Abstract
การประดิษฐ์เกี่ยวข้องกับสารประกอบ 2,7-ไดซับสทิทิวเต็ดเบนโซออกซาโซล และ 2,4-ไดซับสทิทิวเต็ด ออกซาโซโล [5,4-c]ไพริดีนตามสูตร I ซึ่งให้ไว้ด้านล่าง, เช่นเดียวกับเกลือของ พวกมัน, กระบวนการสำหรับการจัดเตรียมพวกมัน, การใช้พวกมันในกระบวนการสำหรับการบำบัด ร่างกายมนุษย์หรือสัตว์, สารประกอบเหล่านี้สำหรับใช้ในการบำบัด (ซึ่งรวมถึงการป้องกันโรค) ร่างกายสัตว์, โดยเฉพาะมนุษย์ (โดยเฉพาะที่เกี่ยวข้องกับโรคเชิงการเพิ่มจำนวน), การใช้พวกมัน- โดยลำพังหรือโดยร่วมกับหนึ่งอย่างหรือมากกว่าของสารประกอบออกฤทธิ์ทางเภสัชกรรมอื่นๆ- สำหรับการบำบัดโดยเฉพาะโรคที่เป็นสื่อโดยโปรตีน ไทโรซีน ไคเนส (เช่น โรคเนื้องอก) หรือ สำหรับการผลิตสารจัดเตรียมทางเภสัชกรรมสำหรับใช้ในการบำบัดโรคดังกล่าว, วิธีการสำหรับ การบำบัดโรคดังกล่าวและสารจัดเตรียมทางเภสัชกรรมสำหรับการบำบัดโรคที่ถูกกล่าวถึง สารประกอบคือตามสูตร I, (สูตรเคมี) (I) โดยที่สัญลักษณ์คือดังซึ่งถูกนิยามไว้ในรายละเอียด สารประกอบจะยับยั้ง, ตัวอย่างเช่น, JAK2 และ JAK3 Invention involves compounds 2,7-dysubstitutate benzooxazole and 2,4-dysubstitutated oxasolo [5,4-c] pyridine according to formula I, given side Bottom, as well as their salts, the process for their preparation, the use of them in the process for the treatment Human body or animal, these compounds for use in the therapy (This includes disease prevention) the animal body, especially humans. (Especially in relation to proliferation diseases), use of them - alone or in combination with one or more of the other active pharmaceutical compounds - for the treatment of specific diseases mediated by tyrosine proteins. Kinase (eg, oncological diseases) or for the manufacture of pharmaceutical preparations for therapeutic use, a method for Such therapies and therapeutic pharmaceutical preparations are discussed. The compound is according to the formula I, (chemical formula) (I), where the symbol is, as is defined in detail. Compounds are inhibited, for example, JAK2 and JAK3.
Claims (1)
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TH96112A TH96112A (en) | 2009-06-18 |
| TH96112B true TH96112B (en) | 2009-06-18 |
Family
ID=
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