KR840005111A - 복소환식 화합물 - Google Patents
복소환식 화합물 Download PDFInfo
- Publication number
- KR840005111A KR840005111A KR1019830002511A KR830002511A KR840005111A KR 840005111 A KR840005111 A KR 840005111A KR 1019830002511 A KR1019830002511 A KR 1019830002511A KR 830002511 A KR830002511 A KR 830002511A KR 840005111 A KR840005111 A KR 840005111A
- Authority
- KR
- South Korea
- Prior art keywords
- compound
- formula
- hydrogen
- group
- preparing
- Prior art date
Links
- 150000002391 heterocyclic compounds Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 24
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
- 238000004519 manufacturing process Methods 0.000 claims 6
- 238000000034 method Methods 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical group 0.000 claims 4
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 125000006239 protecting group Chemical group 0.000 claims 3
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- 238000005917 acylation reaction Methods 0.000 claims 2
- 125000003277 amino group Chemical group 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 239000012948 isocyanate Substances 0.000 claims 2
- 150000002513 isocyanates Chemical class 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- -1 amino, hydroxy Chemical group 0.000 claims 1
- 125000001589 carboacyl group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 1
- 230000007062 hydrolysis Effects 0.000 claims 1
- 238000006460 hydrolysis reaction Methods 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- HKRDYSUZYCDGCG-UHFFFAOYSA-N n-[4-(6-oxo-1h-pyrazin-3-yl)phenyl]acetamide Chemical compound C1=CC(NC(=O)C)=CC=C1C1=CNC(=O)C=N1 HKRDYSUZYCDGCG-UHFFFAOYSA-N 0.000 claims 1
- 230000001546 nitrifying effect Effects 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/18—Oxygen or sulfur atoms
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (14)
- 일반식(1)의 화합물이나 이들의 약제학상 허용 가능한 염을 제조하는 방법.여기에서, R1,R2및 R3는 독립적으로 수소이거나, C1―4알킬이고, R4는 수소, 아미노에 의해 선택적으로 치환된 C1―6알콕시 카르보닐그룹, 하이드록시, C1―4알콕시 혹은 카르복시이고(여기에서 치환체는 ―CO―O―일부분에 인접한 탄소원자상에 있지 않는다); 혹은 R4는 그룹 ―CO―(NR5)n―R6인데 여기서 n은 제로이거나 1이고, R6는 수소, 선택적으로 치환된 C1―6알킬, 선택적으로 치환된 페닐, 혹은 선택적으로 치환된 피리딜이고, R5는 수소, C1―6알킬이거나 혹은 R5와 R6가 이들이 피레리딘, 모른폴리노, 피페리진 혹은 N―(C1―6) 알킬 피페라진환에 붙어있는 질소원자와 동시에 형성되는 것이다.이 공정은 (a) 아실화반응을 일으키게하는 R4가 수소인 일반식(1)의 화합물이나 이들의 유도체를 아실화하는 것; (b) R5가 수소인 일반식(1)의 화합물을 형성키 위해, R4가 수소인 일반식(1)의 화합물을 이소시아네이트로 반응시키는 것; (c) 5―(4―아니모페닐)―2(1H)― 피라지논의 제조를 제외하고, R3가 전기 정의된 바와같고 R10이 보호그룹이거나 혹은 수소를 제의한 전기 전의된 바와같은 그룹 R4인 일반식(Ⅳ)의 화합물을 R1과 R2가 앞서 정의된 바와같고 R11이 이탈그룹인 일반식(V)의 화합물과 반응시키거나, 혹은(d) R1,R2및 R3가 앞서 정의된 바와같은 일반식(Ⅳ)의 화합물을 환원하거나; 또는(e) R2및 R3가 앞서 정의된 바와같고 R12가 니트로이거나 혹은 R10이 보호그룹이거나 수소를 제외한 그룹 R4인 그룹 R10인 일반식(Ⅶ)의 화합물을R1이 앞서 정의된 바와 같고, R12가 아미노로 환원하는 니트로일때의 일반식(Ⅷ)의 화합물과 반응시키거나; 혹은(f) n이 1인 일반식(1)의 화합물을 형성하기 위해, R1,R2및 R3가 앞서 정의된 바와같고 X가 하이드록시 혹은 클로로인 일반식(Ⅸ)의 화합물을R5′및 R6'가 각기 앞서 정의된 바와 같은 그룹 R5및 R6이거나 이들의 보호된 유도체이며 X가 하이드록시인 화합물을 가수분해하는 클로로일때의 일반식(X)의 아민과 반응시키는 것과;HNR5'R6' (X)그후 필요하다면; (i) 어떤 보호그룹을 제거하는 것, (ii) 아실화 반응을 일으키게 하는 아미노그룹(R4) 이거나 이들의 유도체를 아실화하는 것, (iii) R5가 수소인 화합물의 제조가 필요시되면 아미노그룹(R4)을 이소시아네이트와 반응시키는 것, (iv) 약제학상 허용 가능한 염을 제조하는 것을 포함한다.
- R4가 수소이거나, 그룹 ―CO―(NR5)n―R6인 일반식(1)의 화합물 제조하는 공정과 청구범위 1에서 정의되고 R12가 그룹 R10인(a)에서 (e) 반응중의 어느 하나인 공정으로서 여기에서 R5,R6및 n은 R5와 R6가 이것들이 환계에 붙어있는 질소원자와 동시에 형성될때 그 환계는 피페리디노, 피페리진 혹은 N―(C1―6)알킬피페라진인 것을 조건으로 청구범위 1항에서 정의된 바와 같다.
- 청구범위 1항아니 청구범위 2항에 따라 R1,R2및 R3가 동시에 수소인 일반식(1)의 화합물을 제조하는 방법.
- 청구범위 1항 내지 3항중의 어느 하나에 따라 R4가 C1―6알카노일인 일반식(1)의 화합물을 제조하는 방법
- 청구범위 1 내지 4항중의 어느 하나에 따라 R4가 아세틸린 일반식(1)의 화합물을 제조하는 방법.
- 청구범위 1항에 따른 R4은 C1―6알콕시카르보닐인 일반식(1)의 화합물을 제조하는 방법.
- R4가 C1―6알킬 아미노 카르보닐인 청구범위 1항 내지 3항중의 어느 하나에 따른 방법.
- 청구범위 1항 내지 5항중의 어느하나에 따라 5―(4―아세트―아미도페닐)―2 ―(1H)―피라지논을 제조하는 방법.
- 청구범위 1항에서 정의된 바와같은 일반식의 화합물과 약제학적으로 허용 가능한 담체를 화합하는 것으로 구성된 약제학적으로 허용가능한 조성물을 제조하는 방법.
- 조성물이 살균형태인 청구범위 9항에 따른 방법.
- 청구범위 1에서 정의된 바와 같은 일반식(1)의 화합물과 약제학상 허용가능한 담체로 구성되는 약제학적 조성물.
- R1,R2및 R3가 청구범위 1항에서 정의된 바와 같고, R1,R2및 R3가 청구범위 1항에서 정의된 바와같은 일반식(XI)의 화합물을 질산화하는 것을 포함하는 일반식(VI)의 화합물을 제조하는 방법.
- R1,R2및 R3가 칭구범위 1항에서 정의된 바와같은 일반식(VI)의 화합물.
- R1,R2및 R3가 동시에 수소인 일반식(VI)의 화합물.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB8216437 | 1982-06-05 | ||
| GB8216437 | 1982-06-05 | ||
| GB838300476A GB8300476D0 (en) | 1983-01-08 | 1983-01-08 | Heterocyclic compounds |
| GB8300476 | 1983-01-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR840005111A true KR840005111A (ko) | 1984-11-03 |
Family
ID=26283037
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019830002511A KR840005111A (ko) | 1982-06-05 | 1983-06-04 | 복소환식 화합물 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US4514568A (ko) |
| EP (1) | EP0096517A3 (ko) |
| KR (1) | KR840005111A (ko) |
| AU (1) | AU1527583A (ko) |
| DD (1) | DD209818A5 (ko) |
| DK (1) | DK247783A (ko) |
| ES (2) | ES8500244A1 (ko) |
| FI (1) | FI831998L (ko) |
| GR (1) | GR79299B (ko) |
| JO (1) | JO1255B1 (ko) |
| NO (1) | NO832016L (ko) |
| PL (1) | PL242354A1 (ko) |
| PT (1) | PT76791B (ko) |
| RO (1) | RO86851B (ko) |
| ZW (1) | ZW12783A1 (ko) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4657906A (en) * | 1982-06-05 | 1987-04-14 | Smith Kline & French Laboratories Ltd. | Heterocyclic compounds having inotropic activity |
| GB8332313D0 (en) * | 1983-12-02 | 1984-01-11 | Smith Kline French Lab | Chemical compounds |
| US4595766A (en) * | 1984-10-26 | 1986-06-17 | Ciba-Geigy Corporation | Process for the preparation of an indoline carboxylic acid |
| US4697016A (en) * | 1984-10-26 | 1987-09-29 | Ciba-Geigy Corporation | Intermediates for the preparation of a carboxylic acid |
| JPS62198671A (ja) * | 1986-02-25 | 1987-09-02 | Toyo Jozo Co Ltd | １−置換アルキル１，２−ジヒドロ−２−ピラジノン誘導体 |
| US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
| MX354786B (es) | 2007-06-04 | 2018-03-21 | Synergy Pharmaceuticals Inc | Agonistas de guanilato ciclasa utiles para el tratamiento de trastornos gastrointestinales, inflamacion, cancer y otros trastornos. |
| US8969514B2 (en) | 2007-06-04 | 2015-03-03 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases |
| CA2726917C (en) | 2008-06-04 | 2018-06-26 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
| WO2010009319A2 (en) | 2008-07-16 | 2010-01-21 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders |
| CA2770454A1 (en) * | 2009-08-19 | 2011-02-24 | Ambit Biosciences Corporation | Biaryl compounds and methods of use thereof |
| US9616097B2 (en) | 2010-09-15 | 2017-04-11 | Synergy Pharmaceuticals, Inc. | Formulations of guanylate cyclase C agonists and methods of use |
| US9580471B2 (en) | 2011-03-01 | 2017-02-28 | Synergy Pharmaceuticals, Inc. | Process of preparing guanylate cyclase C agonists |
| KR20150023722A (ko) * | 2012-06-12 | 2015-03-05 | 애브비 인코포레이티드 | 피리디논 및 피리다지논 유도체 |
| US9545446B2 (en) | 2013-02-25 | 2017-01-17 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase and their uses |
| WO2014151200A2 (en) | 2013-03-15 | 2014-09-25 | Synergy Pharmaceuticals Inc. | Compositions useful for the treatment of gastrointestinal disorders |
| EP2970384A1 (en) | 2013-03-15 | 2016-01-20 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase and their uses |
| JP6606491B2 (ja) | 2013-06-05 | 2019-11-13 | シナジー ファーマシューティカルズ インコーポレイテッド | グアニル酸シクラーゼｃの超高純度アゴニスト、その作成および使用方法 |
| JP6694385B2 (ja) | 2013-08-09 | 2020-05-13 | アーデリクス，インコーポレーテッド | リン酸塩輸送阻害のための化合物及び方法 |
| WO2020237096A1 (en) | 2019-05-21 | 2020-11-26 | Ardelyx, Inc. | Combination for lowering serum phosphate in a patient |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3745161A (en) * | 1970-04-20 | 1973-07-10 | Merck & Co Inc | Phenyl-hydroxy-pyrazine carboxylic acids and derivatives |
-
1983
- 1983-05-27 EP EP83303059A patent/EP0096517A3/en not_active Withdrawn
- 1983-06-01 PT PT76791A patent/PT76791B/pt unknown
- 1983-06-01 DK DK247783A patent/DK247783A/da not_active Application Discontinuation
- 1983-06-01 JO JO19831255A patent/JO1255B1/en active
- 1983-06-01 AU AU15275/83A patent/AU1527583A/en not_active Abandoned
- 1983-06-01 GR GR71530A patent/GR79299B/el unknown
- 1983-06-02 US US06/500,484 patent/US4514568A/en not_active Expired - Fee Related
- 1983-06-02 US US06/500,486 patent/US4556711A/en not_active Expired - Lifetime
- 1983-06-03 DD DD25173683A patent/DD209818A5/de unknown
- 1983-06-03 ES ES522962A patent/ES8500244A1/es not_active Expired
- 1983-06-03 NO NO832016A patent/NO832016L/no unknown
- 1983-06-03 FI FI831998A patent/FI831998L/fi not_active Application Discontinuation
- 1983-06-03 ZW ZW127/83A patent/ZW12783A1/xx unknown
- 1983-06-03 RO RO111170A patent/RO86851B/ro unknown
- 1983-06-03 PL PL24235483A patent/PL242354A1/xx unknown
- 1983-06-04 KR KR1019830002511A patent/KR840005111A/ko not_active Application Discontinuation
-
1984
- 1984-02-24 ES ES530024A patent/ES8707507A1/es not_active Expired
Also Published As
| Publication number | Publication date |
|---|---|
| GR79299B (ko) | 1984-10-22 |
| ES522962A0 (es) | 1984-10-01 |
| AU1527583A (en) | 1983-12-08 |
| PT76791B (en) | 1986-01-24 |
| EP0096517A3 (en) | 1985-04-03 |
| FI831998A0 (fi) | 1983-06-03 |
| JO1255B1 (en) | 1985-04-20 |
| ES530024A0 (es) | 1985-12-01 |
| RO86851B (ro) | 1985-05-31 |
| ZW12783A1 (en) | 1983-08-24 |
| PL242354A1 (en) | 1984-12-17 |
| DK247783D0 (da) | 1983-06-01 |
| US4556711A (en) | 1985-12-03 |
| RO86851A (ro) | 1985-05-20 |
| US4514568A (en) | 1985-04-30 |
| DD209818A5 (de) | 1984-05-23 |
| FI831998L (fi) | 1983-12-06 |
| DK247783A (da) | 1983-12-06 |
| ES8500244A1 (es) | 1984-10-01 |
| ES8707507A1 (es) | 1985-12-01 |
| NO832016L (no) | 1983-12-06 |
| EP0096517A2 (en) | 1983-12-21 |
| PT76791A (en) | 1983-07-01 |
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