TH131133B - N - ((1R, 2S, 5R) -5- (turn-butylamino) -2 - ((S) -3- (7-turn-butyl-pyrazo) Lo [1,5-A] [1,3,5] triacin-4-ilamino) -2-oxopyrrolidin-1-il) cyclohexyl) Acetaminophen, modulator with chemo-receptor activity, crystalline form and process. - Google Patents
N - ((1R, 2S, 5R) -5- (turn-butylamino) -2 - ((S) -3- (7-turn-butyl-pyrazo) Lo [1,5-A] [1,3,5] triacin-4-ilamino) -2-oxopyrrolidin-1-il) cyclohexyl) Acetaminophen, modulator with chemo-receptor activity, crystalline form and process.Info
- Publication number
- TH131133B TH131133B TH1201001641A TH1201001641A TH131133B TH 131133 B TH131133 B TH 131133B TH 1201001641 A TH1201001641 A TH 1201001641A TH 1201001641 A TH1201001641 A TH 1201001641A TH 131133 B TH131133 B TH 131133B
- Authority
- TH
- Thailand
- Prior art keywords
- turn
- triacin
- butylamino
- cyclohexyl
- butyl
- Prior art date
Links
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 title abstract 3
- 230000000694 effects Effects 0.000 title abstract 2
- 229940022659 Acetaminophen Drugs 0.000 title 1
- 108091008012 chemoreceptors Proteins 0.000 title 1
- 230000000051 modifying Effects 0.000 title 1
- RZVAJINKPMORJF-UHFFFAOYSA-N p-acetaminophenol Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 title 1
- 229960005489 paracetamol Drugs 0.000 title 1
- 239000000126 substance Substances 0.000 claims abstract 5
- 150000001875 compounds Chemical class 0.000 claims abstract 4
- 150000003839 salts Chemical class 0.000 claims abstract 2
- 239000011780 sodium chloride Substances 0.000 claims abstract 2
- DLFVBJFMPXGRIB-UHFFFAOYSA-N acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 abstract 2
- 230000002503 metabolic Effects 0.000 abstract 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 abstract 2
- 102000004497 CCR2 Receptors Human genes 0.000 abstract 1
- 108010017312 CCR2 Receptors Proteins 0.000 abstract 1
- 102000004274 CCR5 Receptors Human genes 0.000 abstract 1
- 108010017088 CCR5 Receptors Proteins 0.000 abstract 1
- 208000008787 Cardiovascular Disease Diseases 0.000 abstract 1
- 230000000172 allergic Effects 0.000 abstract 1
- 230000003042 antagnostic Effects 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 201000008937 atopic dermatitis Diseases 0.000 abstract 1
- 230000001363 autoimmune Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 239000000470 constituent Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000002757 inflammatory Effects 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrugs Drugs 0.000 abstract 1
- 125000006318 tert-butyl amino group Chemical group [H]N(*)C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 abstract 1
Abstract
การประดิษฐ์นี้ให้แอนทากอนิสท์ชนิดใหม่ N-((1R,2S,5R)-5-(เทิร์ท-บิวทิลอะมิโน)-2-((S)- 3-(7-เทิร์ท-บิวทิลไพแรโซโล[1,5-a][1,3,5]ไทรแอซิน-4-อิลอะมิโน)-2-โซพิร์โรลิดิน-1-อิล) ไซโคลเฮกซิล)แอเซแทมีด: (สูตรเคมี) หรือเกลือ, ซอลเวท หรือโพรดรักซึ่งเป็นที่ยอมรับทางเภสัชกรรมของสารนั้น, ที่มีฤทธิ์ต่อตัวรับ CCR- 2 และ CCR-5 ทั้งคู่ที่ไม่ได้คาดหวังไว้ ที่เปิดเผยไว้อีกด้วย คือ รูปผลึก, สารที่เกิดจากเมแทบอลิซึม, องค์ประกอบทางเภสัชกรรมซึ่งมีสารเหล่านั้น และวิธีใช้สารเหล่านั้นเป็นสารรักษาโรคที่เกี่ยวกับการ อักเสบ, ภูมิแพ้, โรคภูมิต้านต้นเอง, เมแทบอลิค, มะเร็ง และ/หรือ โรคหัวใจร่วมหลอดเลือด การ เปิดเผยการประดิษฐ์นี้ยังให้กรรมวิธีเตรียมสารประกอบที่มีสูตร (I) ตามที่ให้ไว้ในนี้, ซึ่งรวมถึง N-((1R,2S,5R)-5-(เทิร์ท-บิวทิลอะมิโน)-2-((S)-3-(7-เทิร์ท-บิวทิลไพแรโซโล[1,5-a][1,3,5] ไทรแอซิน-4-อิลอะมิโน)-2-ออกโซพิร์โรลิดิน-1-อิล)ไซโคลเฮกซิล)แอเซแทมีด ได้ให้สารประกอบ ซึ่งเป็นอินเทอร์มิเดียทที่เป็นประโยชน์ของกรรมวิธีนี้ ไว้ในนี้อีกด้วย: This invention gave the antagonist a new type. N - ((1R, 2S, 5R) -5- (tert-butylamino) -2 - ((S) - 3- (7-tert-butyl pyrazo Lo [1,5-a] [1,3,5] triacin-4-ilamino) -2-sopirrolidin-1-il) cyclohexyl) Azetamid: (chemical formula) or salt, salvate or prodrug, which has an unexpected effect on both CCR- 2 and CCR-5 receptors. Also disclosed are crystals, metabolic substances, pharmaceutical constituents which contain those substances. And how they are used as therapeutic agents for inflammatory, allergic, autoimmune, metabolic, cancer and / or cardiovascular diseases. Formula (I) as given here, which includes N - ((1R, 2S, 5R) -5- (turn-butylamino) -2 - ((S) -3-. (7-tert-butyl pyrazolo [1,5-a] [1,3,5] triacin-4-il-amino) -2-oxopirro Lidin-1-il) cyclohexyl) acetamide Has given the compound Which is a useful interface of this method. Also included here:
Claims (5)
Publications (2)
Publication Number | Publication Date |
---|---|
TH131133B true TH131133B (en) | 2014-01-24 |
TH131133A TH131133A (en) | 2014-01-24 |
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