KR860008131A - 루코트리엔 길항근 - Google Patents
루코트리엔 길항근 Download PDFInfo
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- KR860008131A KR860008131A KR1019860002994A KR860002994A KR860008131A KR 860008131 A KR860008131 A KR 860008131A KR 1019860002994 A KR1019860002994 A KR 1019860002994A KR 860002994 A KR860002994 A KR 860002994A KR 860008131 A KR860008131 A KR 860008131A
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- Prior art keywords
- alkyl
- hydrogen
- compound
- phenyl
- hydroxy
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
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- C07C323/56—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
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- C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
- C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
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- C07C323/66—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton containing sulfur atoms of sulfo, esterified sulfo or halosulfonyl groups, bound to the carbon skeleton
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- C07C323/64—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton
- C07C323/67—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton containing sulfur atoms of sulfonamide groups, bound to the carbon skeleton
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- C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
- C07C45/68—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
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- C07C45/68—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
- C07C45/70—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form
- C07C45/71—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form being hydroxy groups
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Abstract
내용 없음
Description
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Claims (1)
- 다음 일반 구조식(Ⅰ)의 화합물을 제조하는 방법.여기서, R1는 C8내지 C13알킬, C7내지 C12알콕시, C7내지 C12티오알킬, C10내지 C12-1알키필, 10-운데시필옥시, 11-도데피실, 페필- C4내지 C10알킬, 페닐- C3내지 C9알콕시, 광학적으로 브로모, 클로로, 트리플루오르메틸, 메톡시, 메틸티오 또는 트리플루오로메틸티오로, 단일 치환된 페닐을 가지고 있는 페닐티오- C3내지 C9알킬, 푸릴- C4내지 C10알킬, 트리플루오로메틸 C7내지 C12알킬 또는 사이클로핵실 C4내지 C10알킬; R2는 수소, 브로모, 크로로, 메틸, 트리플루오로메틸, 하이드록시, 메톡시 또는 니트로이다; 또는 R1은 수소이고 R2는 C8내지 C13알킬, C7내지 C12알콕시, C7내지 C12티오알킬, C10내지 C121-알키닐, 10-운데시닐옥시, 11-도데시닐, 광학적으로 브로모, 크로로, 트리플루오로메틸, 메톡시, 메틸티오 또는 트리플루오로 메틸티오로 단일 치환된 페닐을 가지고 있는 페닐-C4내지 C10알킬, 페닐-C3내지 C9알콕시, 페닐티오-C3내지 C9알킬, 푸릴-C4내지 C10알킬, 트리플루오로 메틸- C7내지 C12알킬또는 사이클로핵실-C4내지 C10알킬; Y는 COR3 혹은 (CH2)0-1-C-테트라졸일; R3는 하이드록시 혹은 아미노; R4는 수소, 메틸, 메톡시, 플루오로 혹은 하이드록시; m는 0,1 혹은 2이며; R는 8CH2)nCHCOR6,CH(CO2H)CH2CO2H,CH2CH2Z 혹은n은 0,1 혹은 2; R5는 수소, 아미노 혹은 NHCOCH2CH2CH(NH2)CO2H; R6는 하이드록시, 아미노 혹은NHCH2CO2H; Z는 SO3H, SO2NH2혹은 CN; R7는 수소, C1내지 C4알킬 혹은 C3내지 C4알케닐; R8은 수소, C1내지 C4알킬, 카르복실 또는 카르복스 아미도 또는 (CH2)pCO2H 여기서 R7과 R9가 수소 또는 C1내지 C4일때는 p는 1 또는 2이다. R9는 수소, C1내지 C4알킬 또는 CH2CO2H이다. 다만 n이 0일 때R5는 수소이며, R7,R8및 R9가 모두 수소는 아니다; 또는 제약학적으로 바러직한 이외염 및 R이 청구범위 1에서 정의된 바와같은, 적절하게 보호 치환된 티올, RSH를 아래 화합물과 반응시킨후, 이어서 보호기를 제거하여 디아스테레오머릭 화합물의 혼합물 광학적으로 분해하여 제약학적으로 바람직한 염을 만드는 방법이 포함된다.(a) 다음 일반식의 화합물여기서 R1과 R2는 청구범위 1에서, 정의된 바와같고, L는 클로로, 크로모 또는 하이드록시로부터 선택된 유리그룹이며, Y는 R10이 에스테르 보호그룹이고, R12가 수소, 메틸, 메톡시 또는 플루오로인 CO2R10또는 CH(R12)CO2R|10으로서 Y가 CO2H 또는 CH(R12)CO2H인 화합물을 형성한다.(b) 다음 일반식의 화합물여기서, R1,R2및 m은 청구범위 1에서 정의된 바와같고, R11은 저급알킬로서 Y가 CH(OH)(CH2)mCO2H인 화합물을 형성한다.(c) 다음 일반식의 화합물여기서 R1과 R2는 청구범위 1에서 정의된 바와 같고 Y가 (CH2)3CO2인 화합물을 형성한다.(d) 다음 일반식의 화합물여기서 R1과 R2는 청구범위 1에서 정의된 바와같고, R10은 에스테르 보호그룹으로서 Y가 CH2CO2H인 화합물을 형성한다.2) 메틸 3-[2-(8-페닐옥틸)페닐]-2,3-에톡시프로피오네이트와 메틸 3-메트캅토프로피오네이트를 반응시켜 3-(2-카르복시에틸티오)-3-[2-(8-페닐옥틸)페닐]-2-하이드록시 프로파노익산을 얻는 경우의 청구범위 1(b)의 방법.3) 디미스테레오머의 에리트로 혼합물을 분해하여 2(S)-하이드록시-3(R)-(2-카르복시에틸티오)-3-[2-(8-페닐옥틸)페닐]-프로파노익산을 얻는 경우의 청구범위 1(b)의 방법.4) 생성물을 더 소디움염으로 전환시키는 경우의 청구범위 5의 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
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US72526485A | 1985-04-19 | 1985-04-19 | |
US725,264 | 1985-04-19 | ||
US725264 | 1985-04-19 |
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KR860008131A true KR860008131A (ko) | 1986-11-12 |
KR950003335B1 KR950003335B1 (ko) | 1995-04-10 |
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KR1019860002994A KR950003335B1 (ko) | 1985-04-19 | 1986-04-18 | 류코트리엔 길항제, 이의 제조방법 및 이를 함유한 약제학적 조성물 |
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EP (2) | EP0202759B1 (ko) |
JP (3) | JPS61249958A (ko) |
KR (1) | KR950003335B1 (ko) |
CN (2) | CN1008091B (ko) |
AT (2) | ATE53991T1 (ko) |
AU (3) | AU595193B2 (ko) |
CA (2) | CA1276937C (ko) |
CY (1) | CY1733A (ko) |
DE (2) | DE3688561T2 (ko) |
DK (1) | DK176586A (ko) |
EG (1) | EG18226A (ko) |
ES (1) | ES8801175A1 (ko) |
FI (1) | FI88293C (ko) |
GR (1) | GR860993B (ko) |
HK (2) | HK106893A (ko) |
HU (2) | HU198918B (ko) |
IE (1) | IE58958B1 (ko) |
IL (1) | IL78495A (ko) |
MY (1) | MY102219A (ko) |
NO (1) | NO164414C (ko) |
PH (1) | PH23745A (ko) |
PT (1) | PT82394B (ko) |
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Families Citing this family (13)
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US5143931A (en) * | 1982-06-24 | 1992-09-01 | Smithkline Beecham Corporation | Leukotriene antagonists containing tetrazolyl groups |
US4937253A (en) * | 1985-04-19 | 1990-06-26 | Smithkline Beecham Corporation | Ester prodrugs |
DE3688561T2 (de) | 1985-04-19 | 1993-09-23 | Smithkline Beckman Corp | Zwischenprodukte fuer die herstellung von leukotrien-antagonisten. |
US5314918A (en) * | 1987-06-24 | 1994-05-24 | Smithkline Beecham Corporation | Leukotriene antagonists |
CA1334200C (en) * | 1987-06-24 | 1995-01-31 | James Simpson Frazee | Leukotriene antagonists |
US4954513A (en) * | 1988-12-23 | 1990-09-04 | Smithkline Beecham Corporation | Leukotriene antagonists |
PT94376A (pt) * | 1989-06-14 | 1991-03-20 | Smithkline Beecham Corp | Processo de preparacao de derivados de feniloxirano, intermediarios na preparacao de acidos 2-hidroxi-3-(tio substituido)-3-(fenil substituido)carboxilicos, de amidas e esteres |
US5110959A (en) * | 1989-06-14 | 1992-05-05 | Smithkline Beckman Corp. | Process for preparation of epoxy esters and intermediates prepared thereby |
DE69123428T2 (de) * | 1990-04-26 | 1997-05-15 | Senju Pharma Co | Inhibitor von lebererkrankungen |
WO1991016889A1 (en) * | 1990-05-01 | 1991-11-14 | Smithkline Beecham Corporation | Five-membered ring alkanoic acid leukotriene antagonists |
EP0527175A4 (en) * | 1990-05-01 | 1993-05-05 | Smithkline Beecham Corporation | 3-naphthyl-3-carboxyalkylthio or oxy substituted alkanoic acid leukotriene antagonists |
CN1059521A (zh) * | 1990-08-01 | 1992-03-18 | 史密丝克莱恩比彻姆公司 | 制备2-羟基-3-硫醚-3苯基丙酸的方法和中间体 |
DE102005051788B3 (de) | 2005-10-28 | 2007-05-16 | Novelis Deutschland Gmbh | Verfahren und Vorrichtung zur Herstellung eines Wickelrohres |
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GB1577550A (en) * | 1976-10-18 | 1980-10-22 | Sagami Chem Res | -thio-alkanoic acid derivatives |
FR2468362A1 (fr) * | 1978-07-12 | 1981-05-08 | Oreal | Compositions cosmetiques a base de dithioethers pour le traitement de l'etat gras des cheveux et de la peau, nouveaux composes et leur procede d'obtention |
NZ194844A (en) * | 1979-09-05 | 1983-07-29 | Glaxo Group Ltd | Phenoxyalkoxyphenyl derivatives and pharmaceutical compositions |
US4513005A (en) * | 1981-06-18 | 1985-04-23 | Lilly Industries Limited | SRS-A antagonists |
DE3360677D1 (en) * | 1982-11-11 | 1985-10-03 | Beecham Group Plc | Arachidonic acid analogues, processes for their preparation and their use in medicine |
GB8320943D0 (en) * | 1983-08-03 | 1983-09-07 | Lilly Industries Ltd | Organic compounds |
CA1243035A (en) * | 1984-01-19 | 1988-10-11 | John G. Gleason | Leukotriene antagonists |
EP0161172A1 (fr) * | 1984-04-19 | 1985-11-13 | Synthelabo | Dérivés d'acide n-(phenylmethylthio-3 oxo-1 propyl)-aminoacétique, leur préparation et leur application en thérapeutique |
DE3688561T2 (de) | 1985-04-19 | 1993-09-23 | Smithkline Beckman Corp | Zwischenprodukte fuer die herstellung von leukotrien-antagonisten. |
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1986
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- 1986-04-17 EG EG217/86A patent/EG18226A/xx active
- 1986-04-17 DK DK176586A patent/DK176586A/da not_active Application Discontinuation
- 1986-04-18 IE IE102586A patent/IE58958B1/en not_active IP Right Cessation
- 1986-04-18 NO NO861534A patent/NO164414C/no unknown
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- 1986-04-18 CN CN86102482A patent/CN1008091B/zh not_active Expired
- 1986-04-18 ES ES554135A patent/ES8801175A1/es not_active Expired
- 1986-04-18 JP JP61091151A patent/JPS61249958A/ja active Granted
- 1986-04-18 KR KR1019860002994A patent/KR950003335B1/ko not_active IP Right Cessation
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1987
- 1987-09-30 MY MYPI87002366A patent/MY102219A/en unknown
- 1987-10-01 AU AU79291/87A patent/AU604060B2/en not_active Ceased
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1989
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1990
- 1990-06-26 AU AU57897/90A patent/AU5789790A/en not_active Abandoned
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1992
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1993
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1994
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