JP2004513127A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2004513127A5 JP2004513127A5 JP2002539348A JP2002539348A JP2004513127A5 JP 2004513127 A5 JP2004513127 A5 JP 2004513127A5 JP 2002539348 A JP2002539348 A JP 2002539348A JP 2002539348 A JP2002539348 A JP 2002539348A JP 2004513127 A5 JP2004513127 A5 JP 2004513127A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- compound
- compound according
- substituted
- alkyleneoxy
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000002947 alkylene group Chemical group 0.000 claims 5
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000005529 alkyleneoxy group Chemical group 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- -1 isobenzylfuranyl Chemical group 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 3
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- 125000000532 dioxanyl group Chemical group 0.000 claims 2
- 125000005879 dioxolanyl group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- YCKRFDGAMUMZLT-UHFFFAOYSA-N fluorine atom Chemical compound [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 125000005842 heteroatoms Chemical group 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 125000003566 oxetanyl group Chemical group 0.000 claims 2
- 125000003072 pyrazolidinyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000005551 pyridylene group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000011780 sodium chloride Substances 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000006701 (C1-C7) alkyl group Chemical group 0.000 claims 1
- 208000006673 Asthma Diseases 0.000 claims 1
- 206010010741 Conjunctivitis Diseases 0.000 claims 1
- WCDWBPCFGJXFJZ-UHFFFAOYSA-N Etanidazole Chemical group OCCNC(=O)CN1C=CN=C1[N+]([O-])=O WCDWBPCFGJXFJZ-UHFFFAOYSA-N 0.000 claims 1
- 206010039083 Rhinitis Diseases 0.000 claims 1
- 241000009298 Trigla lyra Species 0.000 claims 1
- 206010046736 Urticarias Diseases 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 125000000033 alkoxyamino group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 230000000172 allergic Effects 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000003016 chromanyl group Chemical group O1C(CCC2=CC=CC=C12)* 0.000 claims 1
- 125000004230 chromenyl group Chemical group O1C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims 1
- 201000004624 dermatitis Diseases 0.000 claims 1
- 231100000406 dermatitis Toxicity 0.000 claims 1
- 125000005056 dihydrothiazolyl group Chemical group S1C(NC=C1)* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000003838 furazanyl group Chemical group 0.000 claims 1
- YZCKVEUIGOORGS-UHFFFAOYSA-N hydrogen atom Chemical compound [H] YZCKVEUIGOORGS-UHFFFAOYSA-N 0.000 claims 1
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 1
- 238000006460 hydrolysis reaction Methods 0.000 claims 1
- 125000002632 imidazolidinyl group Chemical group 0.000 claims 1
- 125000002636 imidazolinyl group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 1
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 125000003384 isochromanyl group Chemical group C1(OCCC2=CC=CC=C12)* 0.000 claims 1
- 125000004594 isoindolinyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 claims 1
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N oxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000005936 piperidyl group Chemical group 0.000 claims 1
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 claims 1
- 125000002755 pyrazolinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000001422 pyrrolinyl group Chemical group 0.000 claims 1
- 125000005493 quinolyl group Chemical group 0.000 claims 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
Claims (14)
- 式(I)の化合物
A2はアルキレン、アルキレンオキシ、アルキレンチオ、アルカノイレン又はアルキレンオキシアルキレン基を表し;
W1はフェニレン、フラニレン又はピリジニレン基であって、置換されていないか、あるいは1又は複数のハロゲン原子、アルコキシ基及び/又はアルキル基によって置換されたものを表し;
W2は1〜3個のヘテロ原子を含む3〜10員の単環式又は二環式の基であって、置換されていないか、あるいは1又は複数のハロゲン原子、アルキル基、アルコキシ基及び/又はオキソ基によって置換されているものを表し;
R1は水素又はハロゲン原子あるいはアルキル、アルコキシ又はメチルアミノ基を表し;そして
R2はカルボキシル基を表す)及び医薬として許容されるその塩。 - A1がC1-3アルキレン又はC1-5アルキレンオキシである、請求項1に記載の化合物。
- A2がC1-5アルキレン、C1-5アルカノイレン、C2-5アルキレンオキシ、C2-5アルキレンチオ又はC2-5アルキレンオキシ-C1-5アルキレン基を表す、請求項1又は2に記載の化合物。
- W1が非置換のフェニレン、フラニレン又はピリジニレン基、あるいはフッ素原子、塩素原子、臭素原子、メチル基及びメトキシ基から選択された1又は2つの置換基によって置換されたフェニレン基を表す、請求項1〜3のいずれか1項に記載の化合物。
- 置換基W2に含まれるヘテロ原子が。酸素、硫黄及び窒素から選択される、請求項1〜4のいずれか1項に記載の化合物。
- W2が、非置換の、あるいは1又は複数のハロゲン原子、C1-7アルキル基、C1-7アルコキシ基及び/又はオキソ基によって置換された、ジオキソラニル、ジオキサニル、ピラゾリジニル、イソインドリニル、ベンゾジオキソラニル、テトラヒドロピラニル、テトラヒドロフラニル、オキセタニル、フラニル、チエニル、ピロリル、ピリジニル、イミダゾリル、ジヒドロチアゾリル、ベンゾチアゾリル、ピロリジニル、ベンゾオキサゾリル、ベンゾチエニル、ピラニル、ベンゾフラニル、イソベンジルフラニル、クロメニル、ピラゾリル、オキサゾリル、イソオキサゾリル、フラザニル、イソクロマニル、クロマニル、ピロリニル、イミダゾリジニル、イミダゾリニル、ピラゾリニル、ピペリジル、ピペラジニル、インドリニル、モルホリニル、ピラジニル、ピリミジニル、ピリダジニル、インドリジニル、イソインドリル、インドリル、インダゾリル、キナゾリニル、イソキナゾリニル、キノリル、フタラジニル、ナフチリジニル、キノキサリニル、キナゾリニル又はシンノリニル基を表す、請求項5に記載の化合物。
- W2が、非置換の、あるいは1又は複数のフッ素原子、塩素原子、臭素原子、C1-4アルキル基、C1-4アルコキシ基及び/又はオキソ基によって置換された、ジオキソラニル、ジオキサニル、ピラゾリジニル、ベンゾジオキソラニル、テトラヒドロピラニル、テトラヒドロフラニル、オキセタニル、フラニル、チエニル、ピロリル、ピリジニル、ピロリジニル又はベンゾオキサゾリル基を表す、請求項6に記載の化合物。
- R1が水素、フッ素、塩素又は臭素原子あるいはメチル、メトキシ又はメチルアミノ基を表す、請求項1〜7のいずれか1項に記載の化合物。
- 請求項1〜9のいずれか1項に記載の化合物及び医薬として許容される希釈剤又は担体を含んで成る医薬組成物。
- ヒト又は動物の身体の処置方法における使用のための、請求項1〜9のいずれか1項に記載の化合物又は請求項11に記載の組成物。
- アレルギー性障害又は疾患の処置のための薬剤であって、請求項1〜9のいずれか1項に記載の化合物を含んで成る薬剤。
- 医薬が気管支喘息、鼻炎、結膜炎、皮膚炎又は蕁麻疹の処置のためのものである、請求項13に記載の薬剤。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
ES200002615A ES2172436B1 (es) | 2000-10-31 | 2000-10-31 | Derivados de indolilpiperidina como agentes antihistaminicos y antialergicos. |
PCT/EP2001/012450 WO2002036589A1 (en) | 2000-10-31 | 2001-10-26 | Indolylpiperidine derivatives as antihistaminic and antiallergic agents |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2004513127A JP2004513127A (ja) | 2004-04-30 |
JP2004513127A5 true JP2004513127A5 (ja) | 2005-04-28 |
JP4184785B2 JP4184785B2 (ja) | 2008-11-19 |
Family
ID=8495472
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2002539348A Expired - Fee Related JP4184785B2 (ja) | 2000-10-31 | 2001-10-26 | 抗ヒスタミン薬及び抗アレルギー薬としてのインドリルピペリジン誘導体 |
Country Status (16)
Country | Link |
---|---|
US (1) | US7189741B2 (ja) |
EP (1) | EP1330453B1 (ja) |
JP (1) | JP4184785B2 (ja) |
AR (1) | AR031168A1 (ja) |
AT (1) | ATE321761T1 (ja) |
AU (1) | AU2002223655A1 (ja) |
CA (1) | CA2427589A1 (ja) |
DE (1) | DE60118434T2 (ja) |
DK (1) | DK1330453T3 (ja) |
ES (2) | ES2172436B1 (ja) |
MY (1) | MY155914A (ja) |
PE (1) | PE20020543A1 (ja) |
PT (1) | PT1330453E (ja) |
SI (1) | SI1330453T1 (ja) |
UY (1) | UY27001A1 (ja) |
WO (1) | WO2002036589A1 (ja) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2201899B1 (es) * | 2002-04-01 | 2005-06-01 | Almirall Prodesfarma, S.A. | Derivados de la azaindolilpiperidina como agentes antihistaminicos y antialergicos. |
ES2201907B1 (es) * | 2002-05-29 | 2005-06-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de indolilpiperidina como potentes agentes antihistaminicos y antialergicos. |
NZ537200A (en) | 2002-06-24 | 2007-09-28 | Schering Corp | Indole piperidine derivatives useful as histamine H3 antagonists |
WO2004047769A2 (en) * | 2002-11-26 | 2004-06-10 | Isis Pharmaceuticals, Inc. | Benzimidazoles and analogs thereof as antibacterials |
WO2007050381A2 (en) * | 2005-10-24 | 2007-05-03 | Janssen Pharmaceutica, N.V. | 3-piperidin-4-yl-indole orl-1 receptor modulators |
US8153660B2 (en) * | 2006-10-27 | 2012-04-10 | Boehringer Ingelheim International Gmbh | Piperidyl-propane-thiol CCR3 modulators |
DK2137162T3 (en) * | 2007-03-15 | 2018-11-26 | Novartis Ag | Organic compounds and their applications |
US20100041663A1 (en) | 2008-07-18 | 2010-02-18 | Novartis Ag | Organic Compounds as Smo Inhibitors |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DK471479A (da) | 1978-12-13 | 1980-06-14 | Pfizer | Fremgangsmaade til fremstilling af imidazolderivater og salte deraf |
US4742057A (en) * | 1985-12-05 | 1988-05-03 | Fujisawa Pharmaceutical Co., Ltd. | Antiallergic thiazole compounds |
US4843068A (en) | 1985-12-27 | 1989-06-27 | Nihon Nohyaku Co., Ltd. | Pyrazole oxime derivatives and compositions |
DK733788A (da) | 1988-01-14 | 1989-07-15 | Fujisawa Pharmaceutical Co | Indolylpiperidinderivater og fremgangsmaade til fremstilling deraf |
PT626968E (pt) * | 1992-02-13 | 2002-03-28 | Merrell Pharma Inc | Derivados de piperidinilo tiaciclicos |
JP3338913B2 (ja) * | 1993-06-29 | 2002-10-28 | 大鵬薬品工業株式会社 | テトラゾール誘導体 |
IT1271417B (it) | 1993-10-15 | 1997-05-28 | Erregierre Ind Chim | Composti ad attivita' antiistaminica procedimento per la loro preperazione e composizioni farmaceutiche che li contengono. |
DE19500689A1 (de) | 1995-01-12 | 1996-07-18 | Merck Patent Gmbh | Indolpiperidin-Derivate |
DE19707628A1 (de) | 1997-02-26 | 1998-08-27 | Merck Patent Gmbh | Oxazolidinone |
AR013669A1 (es) | 1997-10-07 | 2001-01-10 | Smithkline Beecham Corp | Compuestos y metodos |
ES2165274B1 (es) | 1999-06-04 | 2003-04-01 | Almirall Prodesfarma Sa | Nuevos derivados de indolilpiperidina como agentes antihistaminicos y antialergicos. |
AR028685A1 (es) | 2000-06-14 | 2003-05-21 | Lundbeck & Co As H | Derivados de indol |
-
2000
- 2000-10-31 ES ES200002615A patent/ES2172436B1/es not_active Expired - Fee Related
-
2001
- 2001-10-26 WO PCT/EP2001/012450 patent/WO2002036589A1/en active IP Right Grant
- 2001-10-26 DE DE60118434T patent/DE60118434T2/de not_active Expired - Lifetime
- 2001-10-26 EP EP01992709A patent/EP1330453B1/en not_active Expired - Lifetime
- 2001-10-26 JP JP2002539348A patent/JP4184785B2/ja not_active Expired - Fee Related
- 2001-10-26 US US10/415,693 patent/US7189741B2/en not_active Expired - Fee Related
- 2001-10-26 AU AU2002223655A patent/AU2002223655A1/en not_active Abandoned
- 2001-10-26 DK DK01992709T patent/DK1330453T3/da active
- 2001-10-26 AT AT01992709T patent/ATE321761T1/de not_active IP Right Cessation
- 2001-10-26 SI SI200130521T patent/SI1330453T1/sl unknown
- 2001-10-26 PT PT01992709T patent/PT1330453E/pt unknown
- 2001-10-26 CA CA002427589A patent/CA2427589A1/en not_active Abandoned
- 2001-10-26 ES ES01992709T patent/ES2259052T3/es not_active Expired - Lifetime
- 2001-10-30 PE PE2001001079A patent/PE20020543A1/es not_active Application Discontinuation
- 2001-10-30 AR ARP010105068A patent/AR031168A1/es not_active Application Discontinuation
- 2001-10-30 MY MYPI20015021A patent/MY155914A/en unknown
- 2001-10-31 UY UY27001A patent/UY27001A1/es unknown
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP5183647B2 (ja) | 4−ピリジルアルキルチオ基を置換基として有する新規化合物 | |
RU2399620C2 (ru) | Производные хинуклидина и их применение в качестве антагонистов мускариновых рецепторов м3 | |
JP2007537255A5 (ja) | ||
JP2007536231A5 (ja) | ||
JP2004521087A5 (ja) | ||
NO20051036L (no) | 3,4-disubstituerte syklobuten-1,2-dioner som CXC-kjemokinreseptorligander | |
RU2005135016A (ru) | Производные хинолина в качестве ингибиторов фосфодиэстеразы | |
CA2516370A1 (en) | A process of preparing imatinib and imatinib prepared thereby | |
KR20070007361A (ko) | 1-아미노-프탈라진 유도체, 이의 제조 방법 및 치료적 용도 | |
PT1500657E (pt) | Pirazoles substituídos como inibidores de cinase p38 | |
JPH08504435A (ja) | タキキニン受容体拮抗剤としての4−アミノメチル/チオメチル/スルホニルメチル−4−フェニルピペリジン | |
JP2006502112A5 (ja) | ||
JP2011500696A5 (ja) | ||
JP2002356472A5 (ja) | ||
JP2004513127A5 (ja) | ||
WO1999052525A1 (es) | Tienilazolilalcoxietanaminas, su preparacion y su aplicacion como medicamentos | |
JP2004525184A5 (ja) | ||
KR20090061029A (ko) | 퀴놀론 카르복실산, 그의 유도체, 그의 제조 방법 및 항박테리아제로서의 그의 용도 | |
ES2198567T3 (es) | Derivados de 4-((tien-5-il)metil)imidazol con actividad agonista de adrenorreceptor alfa2. | |
TW200306834A (en) | Aminopyrimidine compound and pharmaceutical use thereof | |
CA2144423A1 (en) | Heteroaryl compounds used as pharmaceuticals | |
BRPI0713107A2 (pt) | sais de siccinato de 6-metoxi-8-[4-(1-(5-flúor)-quinolin-8-ila-piperidin-4-ila)- piperazin-1-ila]-quinolina, e formas cristalinas destes | |
JP2003529597A5 (ja) | ||
RU2005111983A (ru) | Производные 4-(фенил-пиперазинил-метил)бензамида и их применение для лечения боли или желудочно-кишечных расстройств | |
CN105820104B (zh) | 一种具有抗炎作用的吲哚-2-酰胺类化合物及其在制备抗炎药物中的应用 |