KR900006285A - 소염성 3-아실-2-옥신돌-1-카복사미드의 전구약제 - Google Patents
소염성 3-아실-2-옥신돌-1-카복사미드의 전구약제 Download PDFInfo
- Publication number
- KR900006285A KR900006285A KR1019890014914A KR890014914A KR900006285A KR 900006285 A KR900006285 A KR 900006285A KR 1019890014914 A KR1019890014914 A KR 1019890014914A KR 890014914 A KR890014914 A KR 890014914A KR 900006285 A KR900006285 A KR 900006285A
- Authority
- KR
- South Korea
- Prior art keywords
- compound
- carbon atoms
- alkyl
- alkanoyl
- alkoxycarbonyl
- Prior art date
Links
- 230000003110 anti-inflammatory effect Effects 0.000 title claims 2
- 229940002612 prodrug Drugs 0.000 title 1
- 239000000651 prodrug Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 34
- 125000004432 carbon atom Chemical group C* 0.000 claims 24
- -1 chlorobenzoyl Chemical group 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 125000001589 carboacyl group Chemical group 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 4
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims 3
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 3
- 125000001309 chloro group Chemical group Cl* 0.000 claims 3
- 125000001153 fluoro group Chemical group F* 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 3
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 2
- 125000005194 alkoxycarbonyloxy group Chemical group 0.000 claims 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims 2
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 1
- 125000006678 phenoxycarbonyl group Chemical group 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/32—Oxygen atoms
- C07D209/34—Oxygen atoms in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Rheumatology (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pain & Pain Management (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
내용 없음.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (33)
- 하기 일반식의 화합물상기식에서, X와 Y는 각각 수소, 플루오로 및 클로로로 구성된 군중에서 선택되고 ; R1은 2-티에닐 및 벤질로 구성된 군중에서 선택되고 ; R은 탄소원자 2 내지 10개를 같는 알카노일, 탄소원자 5 내지 7개를 갖는 사이클로알킬카보닐, 탄소원자 7 내지 10개를 갖는 페닐알카노일, 클로로벤조일, 메톡시벤조일, 테노일, 오메가-알콕시카보닐알카노일 (상기 알콕시는 탄소원자 1 내지 3개를 갖고, 상기 알카노일은 탄소원자 3 내지 5 개를 갖는다), 탄소원자 2 내지 10개를 갖는 알콕시카보닐, 페녹시카보닐, 1-(아실옥시) 알킬(상기 아실은 탄소원자 2 내지 4개를 갖고, 상기 알킬은 탄소원자 1 내지 4개를 갖는다), 1-(알콕시카보닐옥시)알킬(상기 알콕시는 탄소워자 2 내지 5개를 갖고, 상기 알킬은 탄소원자 1 내지 4개를 갖는다), 탄소원자 1 내지 3개를 갖는 알킬설포닐, 메틸페닐설포닐 및 디알킬포스포네이트(상기 알킬은 각각 탄소원자 1 내지 3개를 갖는다)로 이루어진 군중에서 선택된다.
- 제1항에 있어서, R1이 2-티에닐이고, X가 클로로이고, Y가 수소인 화합물.
- 제2항에 있어서, R이 탄소원자 2 내지 10개를 갖는 알카노일인 화합물.
- 제3항에 있어서, R이 아세틸인 화합물.
- 제3항에 있어서, R이 프로피오닐인 화합물.
- 제3항에 있어서, R이 이소부티릴인 화합물.
- 제2항에 있어서, R인 탄소원자 7 내지 10개를 갖는 페닐알카노일인 화합물.
- 제7항에 있어서, R이 페닐아세틸인 화합물.
- 제2항에 있어서, R이 오메가-알콕시카보닐알카노일(상기 알콕시는 탄소원자 1 내지 3개를 갖고 상기 알카노일은 탄소원자 3 내지 5개를 갖는다)인 화합물.
- 제9항에 있어서, R이 오메가-에톡시카보닐프로피오닐인 화합물.
- 제2항에 있어서, R이 탄소원자 2 내지 10개를 갖는 알콕시카보닐인 화합물.
- 제11항에 있어서, R이 메톡시카보닐인 화합물.
- 제11항에 있어서, R이 에톡시카보닐인 화합물.
- 제11항에 있어서, R이 n-헥스옥시카보일인 화합물.
- 제2항에 있어서, R이 1-(알콕시카보닐옥시)알킬(상기 알콕시는 탄소원자 2 내지 5개를 갖고 상기 알킬은 탄소원자 1 내지 4개를 갖는다)인 화합물.
- 제15항에 있어서, R이 1-(에톡시카보닐옥시)에틸인 화합물.
- 제2항에 있어서, R이 탄소원자 1 내지 3개를 갖는 알킬설포닐인 화합물.
- 제17항에 있어서, R이 메틸설포닐인 화합물.
- 제1항에 있어서, R1이 2-티에닐이고, X가 플루오로이고 Y가 클로로인 화합물.
- 제19항에 있어서, R이 탄소원자 2 내지 10개를 갖는 알카노일인 화합물.
- 제20항에 있어서, R이 아세틸인 화합물.
- 제20항에 있어서, R이 프로피오닐인 화합물.
- 제20항에 있어서, R이 이소부티릴인 화합물.
- 제19항에 있어서, R이 탄소원자 2 내지 10개를 갖는 알콕시카보닐인 화합물.
- 제24항에 있어서, R이 메톡시카보닐인 화합물.
- 제24항에 있어서, R이 에톡시카보닐인 화합물.
- 제24항에 있어서, R이n-헥스옥시카보닐인 화합물.
- 제1항에 있어서, R1이 벤질이고, X가 수소이고, Y가 플루오로인 화합물.
- 제28항에 있어서, R이 탄소원자 2 내지 10개를 갖는 알카노일인 화합물.
- 제29항에 있어서, R이 아세틸인 화합물.
- 제28항에 있어서, R이 탄소원자 2 내지 10개를 갖는 알콕시카보닐인 화합물.
- 제31항에 있어서, R이 메톡시카보닐인 화합물.
- 제1항에 청구된 화합물로부터 선택한 화합물 소염 효과량을 포유동물에게 투여함을 포함하는 상기 포유동물의 염증을 치료하는 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US88/03658 | 1988-10-18 | ||
USPCT/US88/3658 | 1988-10-18 | ||
PCT/US1988/003658 WO1990004393A1 (en) | 1988-10-18 | 1988-10-18 | Prodrugs of antiinflammatory 3-acyl-2-oxindole-1-carboxamides |
Publications (2)
Publication Number | Publication Date |
---|---|
KR900006285A true KR900006285A (ko) | 1990-05-07 |
KR910007237B1 KR910007237B1 (ko) | 1991-09-24 |
Family
ID=22208957
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019890014914A KR910007237B1 (ko) | 1988-10-18 | 1989-10-17 | 소염성 3-아실-2-옥신돌-1-카복사미드의 전구약제 |
Country Status (33)
Country | Link |
---|---|
US (1) | US5118703A (ko) |
JP (1) | JPH07597B2 (ko) |
KR (1) | KR910007237B1 (ko) |
CN (1) | CN1022241C (ko) |
AP (1) | AP118A (ko) |
AR (1) | AR246519A1 (ko) |
AT (1) | ATE125794T1 (ko) |
AU (1) | AU606819B2 (ko) |
BG (1) | BG50834A3 (ko) |
CA (1) | CA1339558C (ko) |
CZ (1) | CZ278983B6 (ko) |
DD (1) | DD285604A5 (ko) |
DK (1) | DK514989A (ko) |
EG (1) | EG19887A (ko) |
FI (1) | FI95253C (ko) |
HU (1) | HU208421B (ko) |
IE (1) | IE66586B1 (ko) |
IL (1) | IL91960A (ko) |
IS (1) | IS1598B (ko) |
MA (1) | MA21657A1 (ko) |
MX (1) | MX18021A (ko) |
MY (1) | MY104238A (ko) |
NO (1) | NO178027C (ko) |
NZ (1) | NZ231044A (ko) |
OA (1) | OA09140A (ko) |
PH (1) | PH27554A (ko) |
PL (2) | PL162316B1 (ko) |
PT (1) | PT92000B (ko) |
RO (1) | RO109195B1 (ko) |
RU (1) | RU2036905C1 (ko) |
SK (1) | SK278175B6 (ko) |
WO (1) | WO1990004393A1 (ko) |
YU (1) | YU48070B (ko) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5059693A (en) * | 1989-10-06 | 1991-10-22 | Pfizer Inc. | Process for making 3-aroyl-2-oxindole-1-carboxamides |
US5648502A (en) * | 1992-11-23 | 1997-07-15 | Pfizer Inc. | Regioselective synthesis of 4-chloro-2-thiophenecarboxylic acid |
US5270331A (en) * | 1993-01-26 | 1993-12-14 | Pfizer, Inc. | Prodrugs of antiinflammatory 3-acyl-2-oxindole-1-carboxamides |
WO1994018194A1 (en) * | 1993-02-09 | 1994-08-18 | Pfizer Inc. | Oxindole 1-[n-(alkoxycarbonyl)]carboxamides and 1-(n-carboxamido)carboxamides as intiinflammatory agents |
US5449788A (en) * | 1994-01-28 | 1995-09-12 | Catalytica, Inc. | Process for preparing 2-oxindole-1-carboxamides |
CN1094819C (zh) * | 1997-04-30 | 2002-11-27 | 大兴株式会社 | 环状坯料之制造装置 |
EP0984012A3 (en) * | 1998-08-31 | 2001-01-10 | Pfizer Products Inc. | Nitric oxide releasing oxindole prodrugs with analgesic and anti-inflammatory properties |
EP1223809A4 (en) * | 1999-10-26 | 2004-03-03 | Univ Texas Southwestern Med Ct | METHODS OF TREATING HAIR LOSS COMPRISING THE ADMINISTRATION OF AN INDOLIN COMPOUND |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
NL96047C (ko) * | 1956-06-08 | |||
US3564009A (en) * | 1966-01-13 | 1971-02-16 | Sumitomo Chemical Co | Process for producing 1-acylindole derivatives |
BE756447A (fr) * | 1969-10-15 | 1971-03-22 | Pfizer | Oxindolecarboxamides |
US3923996A (en) * | 1972-07-31 | 1975-12-02 | Sandoz Ag | 3-Substituted-oxindoles in compositions and methods of treating obesity |
IE53102B1 (en) * | 1981-05-12 | 1988-06-22 | Ici Plc | Pharmaceutical spiro-succinimide derivatives |
DE3268971D1 (en) * | 1981-10-06 | 1986-03-20 | Ici Plc | Biochemical process |
US4556672A (en) * | 1984-03-19 | 1985-12-03 | Pfizer Inc. | 3-Substituted 2-oxindole-1-carboxamides as analgesic and anti-inflammatory agents |
US4752609A (en) * | 1985-06-20 | 1988-06-21 | Pfizer Inc. | Analgesic and antiinflammatory 1,3-diacyl-2-oxindole compounds |
US5036099A (en) * | 1987-02-02 | 1991-07-30 | Pfizer Inc. | Anhydrous, crystalline sodium salt of 5-chloro-3-(2-thenoyl)-2-oxindole-1-carboxamide |
ES2075055T3 (es) * | 1988-10-18 | 1995-10-01 | Pfizer | Profarmacos de 3-acil-2-oxindol-1-carboxamidas antiinflamatorias. |
US5047554A (en) * | 1989-04-18 | 1991-09-10 | Pfizer Inc. | 3-substituted-2-oxindole derivatives |
US5059693A (en) * | 1989-10-06 | 1991-10-22 | Pfizer Inc. | Process for making 3-aroyl-2-oxindole-1-carboxamides |
-
1988
- 1988-10-18 US US07/675,883 patent/US5118703A/en not_active Expired - Lifetime
- 1988-10-18 WO PCT/US1988/003658 patent/WO1990004393A1/en active IP Right Grant
- 1988-10-18 RO RO147347A patent/RO109195B1/ro unknown
- 1988-10-18 MX MX1802188A patent/MX18021A/es unknown
- 1988-10-18 HU HU886740A patent/HU208421B/hu not_active IP Right Cessation
- 1988-10-18 SK SK5906-89A patent/SK278175B6/sk unknown
-
1989
- 1989-09-20 IS IS3509A patent/IS1598B/is unknown
- 1989-09-28 CA CA000614317A patent/CA1339558C/en not_active Expired - Fee Related
- 1989-10-04 PH PH39329A patent/PH27554A/en unknown
- 1989-10-09 AT AT89310319T patent/ATE125794T1/de active
- 1989-10-12 IL IL9196089A patent/IL91960A/xx not_active IP Right Cessation
- 1989-10-16 BG BG90022A patent/BG50834A3/xx unknown
- 1989-10-16 PT PT92000A patent/PT92000B/pt not_active IP Right Cessation
- 1989-10-16 YU YU200589A patent/YU48070B/sh unknown
- 1989-10-16 AP APAP/P/1989/000141A patent/AP118A/en active
- 1989-10-16 MY MYPI89001415A patent/MY104238A/en unknown
- 1989-10-17 OA OA59665A patent/OA09140A/xx unknown
- 1989-10-17 AU AU42956/89A patent/AU606819B2/en not_active Ceased
- 1989-10-17 NZ NZ231044A patent/NZ231044A/en unknown
- 1989-10-17 AR AR89315179A patent/AR246519A1/es active
- 1989-10-17 PL PL89281871A patent/PL162316B1/pl unknown
- 1989-10-17 JP JP1270174A patent/JPH07597B2/ja not_active Expired - Lifetime
- 1989-10-17 CN CN89107943A patent/CN1022241C/zh not_active Expired - Fee Related
- 1989-10-17 DD DD89333653A patent/DD285604A5/de not_active IP Right Cessation
- 1989-10-17 DK DK514989A patent/DK514989A/da not_active Application Discontinuation
- 1989-10-17 MA MA21909A patent/MA21657A1/fr unknown
- 1989-10-17 KR KR1019890014914A patent/KR910007237B1/ko not_active IP Right Cessation
- 1989-10-17 PL PL89296831A patent/PL163112B1/pl unknown
- 1989-10-17 IE IE333289A patent/IE66586B1/en not_active IP Right Cessation
- 1989-10-18 EG EG49689A patent/EG19887A/xx active
- 1989-10-18 CZ CS895906A patent/CZ278983B6/cs not_active IP Right Cessation
-
1991
- 1991-04-17 FI FI911855A patent/FI95253C/fi not_active IP Right Cessation
- 1991-04-17 RU SU914895525A patent/RU2036905C1/ru active
- 1991-04-17 NO NO911512A patent/NO178027C/no unknown
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