JP2004534774A5 - - Google Patents
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- Publication number
- JP2004534774A5 JP2004534774A5 JP2002591503A JP2002591503A JP2004534774A5 JP 2004534774 A5 JP2004534774 A5 JP 2004534774A5 JP 2002591503 A JP2002591503 A JP 2002591503A JP 2002591503 A JP2002591503 A JP 2002591503A JP 2004534774 A5 JP2004534774 A5 JP 2004534774A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- halogen
- optionally substituted
- aryl
- heteroaryl
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 81
- 229910052736 halogen Inorganic materials 0.000 claims 44
- 150000002367 halogens Chemical class 0.000 claims 40
- 150000001875 compounds Chemical class 0.000 claims 30
- 125000003118 aryl group Chemical group 0.000 claims 27
- 125000001072 heteroaryl group Chemical group 0.000 claims 25
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 239000001257 hydrogen Substances 0.000 claims 15
- 125000005843 halogen group Chemical group 0.000 claims 14
- -1 amino, carboxy Chemical group 0.000 claims 11
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 9
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 8
- 125000003226 pyrazolyl group Chemical group 0.000 claims 8
- 125000000081 (C5-C8) cycloalkenyl group Chemical group 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 150000002431 hydrogen Chemical group 0.000 claims 5
- 125000001624 naphthyl group Chemical group 0.000 claims 5
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- 125000001544 thienyl group Chemical group 0.000 claims 5
- 125000000168 pyrrolyl group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000003943 azolyl group Chemical group 0.000 claims 3
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 2
- 125000005493 quinolyl group Chemical group 0.000 claims 2
- 239000011593 sulfur Chemical group 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 claims 1
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims 1
- NPDLYUOYAGBHFB-WDSKDSINSA-N Asn-Arg Chemical group NC(=O)C[C@H](N)C(=O)N[C@H](C(O)=O)CCCN=C(N)N NPDLYUOYAGBHFB-WDSKDSINSA-N 0.000 claims 1
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 206010028735 Nasal congestion Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 201000009961 allergic asthma Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 230000001387 anti-histamine Effects 0.000 claims 1
- 239000000739 antihistaminic agent Substances 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 125000001589 carboacyl group Chemical group 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000002993 cycloalkylene group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 239000003199 leukotriene receptor blocking agent Substances 0.000 claims 1
- 150000002617 leukotrienes Chemical class 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 229910052757 nitrogen Chemical group 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- BHMBVRSPMRCCGG-OUTUXVNYSA-N prostaglandin D2 Chemical compound CCCCC[C@H](O)\C=C\[C@@H]1[C@@H](C\C=C/CCCC(O)=O)[C@@H](O)CC1=O BHMBVRSPMRCCGG-OUTUXVNYSA-N 0.000 claims 1
- BHMBVRSPMRCCGG-UHFFFAOYSA-N prostaglandine D2 Natural products CCCCCC(O)C=CC1C(CC=CCCCC(O)=O)C(O)CC1=O BHMBVRSPMRCCGG-UHFFFAOYSA-N 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29307701P | 2001-05-23 | 2001-05-23 | |
| PCT/CA2002/000745 WO2002094830A2 (en) | 2001-05-23 | 2002-05-22 | DIHYDROPYRROLO[1,2-A]INDOLE AND TETRAHYDROPYRIDO[1,2-a]-INDOLE DERIVATIVES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2004534774A JP2004534774A (ja) | 2004-11-18 |
| JP2004534774A5 true JP2004534774A5 (OSRAM) | 2005-12-22 |
| JP4279561B2 JP4279561B2 (ja) | 2009-06-17 |
Family
ID=23127559
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002591503A Expired - Fee Related JP4279561B2 (ja) | 2001-05-23 | 2002-05-22 | プロスタグランジンD2受容体拮抗薬としてのジヒドロピロロ[1,2−a]インドールおよびテトラヒドロピリド[1,2−a]−インドール誘導体 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US7144913B2 (OSRAM) |
| EP (1) | EP1395590B1 (OSRAM) |
| JP (1) | JP4279561B2 (OSRAM) |
| AT (1) | ATE340796T1 (OSRAM) |
| AU (1) | AU2002302248B2 (OSRAM) |
| CA (1) | CA2447779C (OSRAM) |
| DE (1) | DE60215000T2 (OSRAM) |
| ES (1) | ES2272712T3 (OSRAM) |
| WO (1) | WO2002094830A2 (OSRAM) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60334015D1 (de) | 2002-10-30 | 2010-10-14 | Merck Frosst Canada Ltd | Pyridopyrrolizin- und pyridoindolizinderivate |
| ES2401079T3 (es) | 2002-12-20 | 2013-04-16 | Amgen Inc. | Moduladores del asma y de la inflamación alérgica |
| AR041089A1 (es) * | 2003-05-15 | 2005-05-04 | Merck & Co Inc | Procedimiento y composiciones farmaceutiicas para tratar aterosclerosis, dislipidemias y afecciones relacionadas |
| PE20050483A1 (es) | 2003-10-31 | 2005-08-25 | Arena Pharm Inc | Derivados de tetrazol de formula (i), sus composiciones farmaceuticas y procesos para producir composiciones farmaceuticas |
| AU2005229356B2 (en) | 2004-03-11 | 2011-06-09 | Idorsia Pharmaceuticals Ltd | Tetrahydropyridoindole derivatives |
| ITMI20040874A1 (it) * | 2004-04-30 | 2004-07-30 | Ist Naz Stud Cura Dei Tumori | Derivati indolici ed azaindolici con azione antitumorale |
| US20070299122A1 (en) * | 2004-11-08 | 2007-12-27 | Tobert Jonathan A | Method of Treating Pathological Blushing |
| PE20060949A1 (es) | 2004-12-23 | 2006-10-11 | Arena Pharm Inc | Derivados fusionados de pirazol como agonistas del receptor de niacina |
| ATE518834T1 (de) | 2004-12-27 | 2011-08-15 | Actelion Pharmaceuticals Ltd | 2,3,4,9-tetrahydro-1h-carbazol-derivative als crth2-rezeptorantagonisten |
| KR20070113295A (ko) * | 2005-03-17 | 2007-11-28 | 노파르티스 아게 | 티로신/트레오닌 키나제 억제제, 특히 b-raf 키나제억제제로서의n-[3-(1-아미노-5,6,7,8-테트라히드로-2,4,4b-트리아자플루오렌-9-일)-페닐]벤즈아미드 |
| JP5072594B2 (ja) | 2005-07-22 | 2012-11-14 | 塩野義製薬株式会社 | Pgd2受容体アンタゴニスト活性を有するインドール誘導体 |
| WO2007010965A1 (ja) | 2005-07-22 | 2007-01-25 | Shionogi & Co., Ltd. | Pgd2受容体アンタゴニスト活性を有するアザインドール酸誘導体 |
| EP1915372B1 (en) * | 2005-08-12 | 2013-11-20 | Merck Canada Inc. | Indole derivatives as crth2 receptor antagonists |
| JP5147401B2 (ja) | 2005-09-06 | 2013-02-20 | 塩野義製薬株式会社 | Pgd2受容体アンタゴニスト活性を有するインドールカルボン酸誘導体 |
| KR101411820B1 (ko) | 2006-08-07 | 2014-06-24 | 액테리온 파마슈티칼 리미티드 | (3-아미노-1,2,3,4-테트라하이드로-9h-카르바졸-9-일)-아세트산 유도체 |
| RU2451019C2 (ru) * | 2007-10-10 | 2012-05-20 | КЕМИТЕК, ЭлЭлСи | Гетероциклические соединения в качестве антагонистов crth2 рецептора |
| BRPI0821197A2 (pt) | 2007-12-19 | 2015-06-16 | Amgen Inc | Composto, composição farmacêutica, uso de um composto, processo, e, intermediário. |
| EP2245002A4 (en) * | 2008-02-01 | 2011-08-17 | Amira Pharmaceuticals Inc | AMINOALKYLBIPHENYL ANTAGONISTS N, N 'DISUBSTITUTED FROM D2 RECEPTORS OF PROSTAGLANDIN |
| US8168678B2 (en) | 2008-02-01 | 2012-05-01 | Panmira Pharmaceuticals, Inc. | N,N-disubstituted aminoalkylbiphenyl antagonists of prostaglandin D2 receptors |
| EP2257536A4 (en) * | 2008-02-14 | 2011-03-23 | Amira Pharmaceuticals Inc | CYCLIC DIARYL ETHERS AS ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS |
| WO2009108720A2 (en) | 2008-02-25 | 2009-09-03 | Amira Pharmaceuticals, Inc. | Antagonists of prostaglandin d2 receptors |
| EP2268611A2 (en) * | 2008-04-02 | 2011-01-05 | Amira Pharmaceuticals, Inc. | Aminoalkylphenyl antagonists of prostaglandin d2 receptors |
| US20110112134A1 (en) * | 2008-05-16 | 2011-05-12 | Amira Pharmaceuticals, Inc. | Tricyclic Antagonists of Prostaglandin D2 Receptors |
| JP2011526281A (ja) * | 2008-06-24 | 2011-10-06 | アミラ ファーマシューティカルズ,インク. | プロスタグランジンd2受容体のシクロアルカン[b]インドールアンタゴニスト |
| MX2010014172A (es) * | 2008-07-03 | 2011-02-22 | Amira Pharmaceuticals Inc | Antagonistas de receptores de prostaglandina d2. |
| US8507473B2 (en) | 2008-09-11 | 2013-08-13 | Arena Pharmaceuticals, Inc. | 3H-imidazo[4,5-b]pyridin-5-ol derivatives useful in the treatment of GPR81 receptor disorders |
| GB2463788B (en) * | 2008-09-29 | 2010-12-15 | Amira Pharmaceuticals Inc | Heteroaryl antagonists of prostaglandin D2 receptors |
| US8524748B2 (en) | 2008-10-08 | 2013-09-03 | Panmira Pharmaceuticals, Llc | Heteroalkyl biphenyl antagonists of prostaglandin D2 receptors |
| GB2465062B (en) * | 2008-11-06 | 2011-04-13 | Amira Pharmaceuticals Inc | Cycloalkane(B)azaindole antagonists of prostaglandin D2 receptors |
| WO2010057118A2 (en) * | 2008-11-17 | 2010-05-20 | Amira Pharmaceuticals, Inc. | Heterocyclic antagonists of prostaglandin d2 receptors |
| US20100173313A1 (en) * | 2009-01-08 | 2010-07-08 | Amira Pharmaceuticals, Inc. | Biomarkers of inflammation |
| CA2768492A1 (en) | 2009-07-31 | 2011-02-03 | Panmira Pharmaceuticals, Llc | Ophthalmic pharmaceutical compositions of dp2 receptor antagonists |
| CN102596902A (zh) * | 2009-08-05 | 2012-07-18 | 潘米拉制药公司 | Dp2拮抗剂及其用途 |
| WO2011035417A1 (en) * | 2009-09-25 | 2011-03-31 | Aegera Therapeutics Inc. | Hsp-90 binding compounds, compositions thereof, and their use fn the treatment of autoimmune and inflammatory diseases |
| CA2782085A1 (en) | 2010-01-06 | 2011-07-14 | Panmira Pharmaceuticals, Llc | Dp2 antagonist and uses thereof |
| PL2558447T3 (pl) | 2010-03-22 | 2015-03-31 | Idorsia Pharmaceuticals Ltd | Pochodne 3-(heteroaryloamino)-1,2,3,4-tetrahydro-9h-karbazolu i ich zastosowanie jako modulatorów receptora prostaglandyny D2 |
| US8575158B2 (en) | 2010-07-05 | 2013-11-05 | Actelion Pharmaceuticals Ltd. | 1-phenyl-substituted heterocyclyl derivatives and their use as prostaglandin D2 receptor modulators |
| EP2606032B1 (en) * | 2010-08-20 | 2015-01-07 | University Of Washington Through Its Center For Commercialization | Composition and methods for treating glioblastomas |
| WO2012116942A1 (de) * | 2011-03-02 | 2012-09-07 | Bayer Cropscience Ag | Verfahren zur herstellung von aryl- und heteroarylessigsäure-derivaten |
| WO2012126084A1 (en) * | 2011-03-24 | 2012-09-27 | Pharmascience Inc. | Hsp-90 binding compounds, compositions thereof, and their use iν the treatment and prevention of fungal infections |
| US9096595B2 (en) | 2011-04-14 | 2015-08-04 | Actelion Pharmaceuticals Ltd | 7-(heteroaryl-amino)-6,7,8,9-tetrahydropyrido[1,2-a]indol acetic acid derivatives and their use as prostaglandin D2 receptor modulators |
| BR112014015081A8 (pt) | 2011-12-21 | 2017-06-13 | Actelion Pharmaceuticals Ltd | derivados heterocíclicos e seu uso como moduladores do receptor d2 de prostaglandina |
| JP6127135B2 (ja) | 2012-07-05 | 2017-05-10 | アクテリオン ファーマシューティカルズ リミテッドActelion Pharmaceuticals Ltd | 1−フェニル置換ヘテロシクリル誘導体及びプロスタグランジンd2受容体調節剤としてのそれらの使用 |
| EP3382391A1 (en) | 2012-10-24 | 2018-10-03 | NYU Winthrop Hospital | Non-invasive biomarker to identify subjects at risk of preterm delivery |
| WO2015096651A1 (en) | 2013-12-23 | 2015-07-02 | Merck Sharp & Dohme Corp. | Pyrimidone carboxamide compounds as pde2 inhibitors |
| HUE039614T2 (hu) | 2014-03-17 | 2019-01-28 | Idorsia Pharmaceuticals Ltd | Azaindol-ecetsav-származékok és prosztaglandin D2 receptor modulátorokként történõ alkalmazásuk |
| KR20160133536A (ko) | 2014-03-18 | 2016-11-22 | 액테리온 파마슈티칼 리미티드 | 아자인돌 아세트산 유도체 및 프로스타글란딘 d2 수용체 조절제로서의 이의 용도 |
| WO2016128565A1 (en) | 2015-02-13 | 2016-08-18 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Ptgdr-1 and/or ptgdr-2 antagonists for preventing and/or treating systemic lupus erythematosus |
| WO2016145614A1 (en) | 2015-03-17 | 2016-09-22 | Merck Sharp & Dohme Corp. | Triazolyl pyrimidinone compounds as pde2 inhibitors |
| EP3285581B1 (en) | 2015-03-26 | 2021-08-11 | Merck Sharp & Dohme Corp. | Pyrazolyl pyrimidinone compounds as pde2 inhibitors |
| EP3313852B1 (en) | 2015-06-25 | 2021-01-20 | Merck Sharp & Dohme Corp. | Substituted pyrazolo/imidazolo bicyclic compounds as pde2 inhibitors |
| WO2017000277A1 (en) | 2015-07-01 | 2017-01-05 | Merck Sharp & Dohme Corp. | Substituted triazolo bicycliccompounds as pde2 inhibitors |
| MX379014B (es) | 2015-09-15 | 2025-03-10 | Idorsia Pharmaceuticals Ltd | Formas cristalinas. |
| WO2018014867A1 (zh) * | 2016-07-21 | 2018-01-25 | 正大天晴药业集团股份有限公司 | 作为crth2抑制剂的三并环类化合物 |
| KR20200109293A (ko) | 2017-09-13 | 2020-09-22 | 프로제너티, 인크. | 자간전증 바이오마커 및 관련된 시스템 및 방법 |
| EP4070113A4 (en) | 2019-12-04 | 2023-12-20 | Biora Therapeutics, Inc. | ASSESSMENT OF PREECAMPSIA USING FREE AND DISSOCIATE PLACENTAL GROWTH FACTOR ASSAYS |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA1241660A (en) * | 1984-06-25 | 1988-09-06 | Yvan Guindon | Indole-2-alkanoic acids |
| EA200000873A1 (ru) * | 1998-02-25 | 2001-04-23 | Дженетикс Инститьют, Инк. | Ингибиторы фосфолипазы a |
| AR041089A1 (es) * | 2003-05-15 | 2005-05-04 | Merck & Co Inc | Procedimiento y composiciones farmaceutiicas para tratar aterosclerosis, dislipidemias y afecciones relacionadas |
-
2002
- 2002-05-22 WO PCT/CA2002/000745 patent/WO2002094830A2/en not_active Ceased
- 2002-05-22 DE DE60215000T patent/DE60215000T2/de not_active Expired - Lifetime
- 2002-05-22 AU AU2002302248A patent/AU2002302248B2/en not_active Ceased
- 2002-05-22 EP EP02729708A patent/EP1395590B1/en not_active Expired - Lifetime
- 2002-05-22 JP JP2002591503A patent/JP4279561B2/ja not_active Expired - Fee Related
- 2002-05-22 AT AT02729708T patent/ATE340796T1/de not_active IP Right Cessation
- 2002-05-22 CA CA2447779A patent/CA2447779C/en not_active Expired - Fee Related
- 2002-05-22 US US10/474,929 patent/US7144913B2/en not_active Expired - Fee Related
- 2002-05-22 ES ES02729708T patent/ES2272712T3/es not_active Expired - Lifetime
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