JP2008543764A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2008543764A5 JP2008543764A5 JP2008515911A JP2008515911A JP2008543764A5 JP 2008543764 A5 JP2008543764 A5 JP 2008543764A5 JP 2008515911 A JP2008515911 A JP 2008515911A JP 2008515911 A JP2008515911 A JP 2008515911A JP 2008543764 A5 JP2008543764 A5 JP 2008543764A5
- Authority
- JP
- Japan
- Prior art keywords
- aryl
- heteroaryl
- heterocyclyl
- alkyl
- alkoxy
- 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 description 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 38
- 125000003118 aryl group Chemical group 0.000 claims 36
- 125000000217 alkyl group Chemical group 0.000 claims 32
- 125000000623 heterocyclic group Chemical group 0.000 claims 32
- 125000003545 alkoxy group Chemical group 0.000 claims 22
- 125000000753 cycloalkyl group Chemical group 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 16
- -1 SOCR 2 R 2a Inorganic materials 0.000 claims 14
- 150000002367 halogens Chemical class 0.000 claims 14
- 125000001188 haloalkyl group Chemical group 0.000 claims 12
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 10
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 10
- 125000003342 alkenyl group Chemical group 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- 125000004414 alkyl thio group Chemical group 0.000 claims 6
- 125000004104 aryloxy group Chemical group 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 125000003282 alkyl amino group Chemical group 0.000 claims 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims 4
- 125000001769 aryl amino group Chemical group 0.000 claims 4
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 4
- 125000005110 aryl thio group Chemical group 0.000 claims 4
- 125000004438 haloalkoxy group Chemical group 0.000 claims 4
- 125000005241 heteroarylamino group Chemical group 0.000 claims 4
- 102000004277 11-beta-hydroxysteroid dehydrogenases Human genes 0.000 claims 2
- 108090000874 11-beta-hydroxysteroid dehydrogenases Proteins 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000005236 alkanoylamino group Chemical group 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 125000004659 aryl alkyl thio group Chemical group 0.000 claims 2
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 2
- 125000005418 aryl aryl group Chemical group 0.000 claims 2
- 125000004658 aryl carbonyl amino group Chemical group 0.000 claims 2
- 125000005160 aryl oxy alkyl group Chemical group 0.000 claims 2
- 125000005325 aryloxy aryl group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 2
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000005114 heteroarylalkoxy group Chemical group 0.000 claims 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 2
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 125000003396 thiol group Chemical class [H]S* 0.000 claims 2
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 description 6
- 230000015572 biosynthetic process Effects 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 238000006243 chemical reaction Methods 0.000 description 3
- LMDZBCPBFSXMTL-UHFFFAOYSA-N 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide Chemical compound CCN=C=NCCCN(C)C LMDZBCPBFSXMTL-UHFFFAOYSA-N 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 description 2
- 239000003153 chemical reaction reagent Substances 0.000 description 2
- ODIGIKRIUKFKHP-UHFFFAOYSA-N (n-propan-2-yloxycarbonylanilino) acetate Chemical compound CC(C)OC(=O)N(OC(C)=O)C1=CC=CC=C1 ODIGIKRIUKFKHP-UHFFFAOYSA-N 0.000 description 1
- NGNBDVOYPDDBFK-UHFFFAOYSA-N 2-[2,4-di(pentan-2-yl)phenoxy]acetyl chloride Chemical compound CCCC(C)C1=CC=C(OCC(Cl)=O)C(C(C)CCC)=C1 NGNBDVOYPDDBFK-UHFFFAOYSA-N 0.000 description 1
- FNRMMDCDHWCQTH-UHFFFAOYSA-N 2-chloropyridine;3-chloropyridine;4-chloropyridine Chemical compound ClC1=CC=NC=C1.ClC1=CC=CN=C1.ClC1=CC=CC=N1 FNRMMDCDHWCQTH-UHFFFAOYSA-N 0.000 description 1
- MTAODLNXWYIKSO-UHFFFAOYSA-N 2-fluoropyridine Chemical compound FC1=CC=CC=N1 MTAODLNXWYIKSO-UHFFFAOYSA-N 0.000 description 1
- YEDUAINPPJYDJZ-UHFFFAOYSA-N 2-hydroxybenzothiazole Chemical compound C1=CC=C2SC(O)=NC2=C1 YEDUAINPPJYDJZ-UHFFFAOYSA-N 0.000 description 1
- YOETUEMZNOLGDB-UHFFFAOYSA-N 2-methylpropyl carbonochloridate Chemical compound CC(C)COC(Cl)=O YOETUEMZNOLGDB-UHFFFAOYSA-N 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 150000001408 amides Chemical class 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 230000008878 coupling Effects 0.000 description 1
- 238000010168 coupling process Methods 0.000 description 1
- 238000005859 coupling reaction Methods 0.000 description 1
- 125000000524 functional group Chemical group 0.000 description 1
- NPZTUJOABDZTLV-UHFFFAOYSA-N hydroxybenzotriazole Substances O=C1C=CC=C2NNN=C12 NPZTUJOABDZTLV-UHFFFAOYSA-N 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000010647 peptide synthesis reaction Methods 0.000 description 1
- RLOWWWKZYUNIDI-UHFFFAOYSA-N phosphinic chloride Chemical compound ClP=O RLOWWWKZYUNIDI-UHFFFAOYSA-N 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US68899305P | 2005-06-09 | 2005-06-09 | |
| US60/688,993 | 2005-06-09 | ||
| US11/448,946 US7572807B2 (en) | 2005-06-09 | 2006-06-07 | Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors |
| US11/448,946 | 2006-06-07 | ||
| PCT/US2006/022260 WO2006135667A1 (en) | 2005-06-09 | 2006-06-08 | Imidiazo -and triazolopyridines as inhibitors of 11-beta hydroxysteroid dehydrogenase type i |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008543764A JP2008543764A (ja) | 2008-12-04 |
| JP2008543764A5 true JP2008543764A5 (https=) | 2009-02-05 |
| JP5124450B2 JP5124450B2 (ja) | 2013-01-23 |
Family
ID=37524860
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008515911A Expired - Fee Related JP5124450B2 (ja) | 2005-06-09 | 2006-06-08 | １１β−ヒドロキシステロイドデヒドロゲナーゼＩ型阻害剤としてのイミダゾおよびトリアゾロピリジン類 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US7572807B2 (https=) |
| EP (1) | EP1912986B1 (https=) |
| JP (1) | JP5124450B2 (https=) |
| KR (1) | KR20080018942A (https=) |
| AR (1) | AR057357A1 (https=) |
| AU (1) | AU2006258077B2 (https=) |
| ES (1) | ES2392656T3 (https=) |
| MX (1) | MX2007015283A (https=) |
| NO (1) | NO20076054L (https=) |
| PE (1) | PE20070002A1 (https=) |
| TW (1) | TW200716116A (https=) |
| WO (1) | WO2006135667A1 (https=) |
Families Citing this family (100)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0420722D0 (en) * | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| HUE030390T2 (en) | 2005-12-21 | 2017-05-29 | Janssen Pharmaceutica Nv | Triazolopyridazines as tyrosine kinase modulators |
| TWI417095B (zh) | 2006-03-15 | 2013-12-01 | Janssen Pharmaceuticals Inc | １，４-二取代之３-氰基-吡啶酮衍生物及其作為ｍＧｌｕＲ２-受體之正向異位性調節劑之用途 |
| EP2013169B1 (en) * | 2006-04-24 | 2012-08-22 | Merck Canada Inc. | Indole amide derivatives as ep4 receptor antagonists |
| PE20110235A1 (es) | 2006-05-04 | 2011-04-14 | Boehringer Ingelheim Int | Combinaciones farmaceuticas que comprenden linagliptina y metmorfina |
| US8198448B2 (en) | 2006-07-14 | 2012-06-12 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| PE20080403A1 (es) | 2006-07-14 | 2008-04-25 | Amgen Inc | Derivados heterociclicos fusionados y metodos de uso |
| US8217177B2 (en) | 2006-07-14 | 2012-07-10 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| EP2070927A4 (en) | 2006-09-13 | 2010-10-13 | Kyowa Hakko Kirin Co Ltd | CONDENSED HETEROCYCLIC DERIVATIVE |
| EP2086973B1 (en) * | 2006-10-11 | 2012-01-25 | Amgen Inc., | Imidazo- and triazolo-pyridine compounds and methods of use therof |
| EA201300152A1 (ru) | 2006-11-27 | 2013-07-30 | Х. Лундбекк А/С | Гетероариламидные производные |
| WO2008078091A1 (en) | 2006-12-22 | 2008-07-03 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as fgfr inhibitors |
| CN101679409B (zh) | 2006-12-22 | 2014-11-26 | Astex治疗学有限公司 | 双环杂环衍生化合物、其医药组合物和其用途 |
| TW200900065A (en) * | 2007-03-07 | 2009-01-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives |
| TW200845978A (en) | 2007-03-07 | 2008-12-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives |
| US8546394B2 (en) | 2007-04-17 | 2013-10-01 | Bristol-Myers Squibb Company | Substituted [1,2,4]triazolo[4,3-A]pyrazine 11-beta-hydroxysteroid dehydrogenase inhibitors |
| WO2009005675A1 (en) * | 2007-06-28 | 2009-01-08 | Abbott Laboratories | Novel triazolopyridazines |
| US20090069288A1 (en) * | 2007-07-16 | 2009-03-12 | Breinlinger Eric C | Novel therapeutic compounds |
| PL2203439T3 (pl) | 2007-09-14 | 2011-06-30 | Addex Pharmaceuticals Sa | 1',3'-dipodstawione-4-fenylo-3,4,5,6-tetrahydro-2H, 1'H-[1, 4']bipirydynylo-2'-ketony |
| US8722894B2 (en) | 2007-09-14 | 2014-05-13 | Janssen Pharmaceuticals, Inc. | 1,3-disubstituted-4-phenyl-1H-pyridin-2-ones |
| US8252937B2 (en) | 2007-09-14 | 2012-08-28 | Janssen Pharmaceuticals, Inc. | 1,3-disubstituted 4-(aryl-X-phenyl)-1H-pyridin-2-ones |
| US8119658B2 (en) | 2007-10-01 | 2012-02-21 | Bristol-Myers Squibb Company | Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors |
| GB0720038D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New compounds |
| GB0720041D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New Compounds |
| RU2492170C9 (ru) | 2007-11-14 | 2013-12-27 | Орто-Макнейл-Янссен Фармасьютикалз, Инк. | Имидазо[1,2-а]пиридиновые производные и их применение в качестве положительных аллостерических модуляторов рецепторов mglur2 |
| EP2072516A1 (en) * | 2007-12-21 | 2009-06-24 | Santhera Pharmaceuticals (Schweiz) AG | Substituted imidazopyridine derivates as Melancortin-4 receptor antagonists |
| WO2009102761A1 (en) * | 2008-02-12 | 2009-08-20 | Bristol-Myers Squibb Company | 1,2,3-triazoles as 11-beta hydroxysteroid dehydrogenase type i inhibitors |
| WO2009126624A1 (en) * | 2008-04-11 | 2009-10-15 | Bristol-Myers Squibb Company | Triazolo compounds useful as dgat1 inhibitors |
| US8394823B2 (en) * | 2008-04-11 | 2013-03-12 | Bristol-Myers Squibb Company | Triazolopyridine compounds useful as DGAT1 inhibitors |
| GB0810902D0 (en) | 2008-06-13 | 2008-07-23 | Astex Therapeutics Ltd | New compounds |
| JP5547194B2 (ja) | 2008-09-02 | 2014-07-09 | ジャンセン ファーマシューティカルズ， インコーポレイテッド． | 代謝型グルタミン酸受容体の調節因子としての３−アザビシクロ［３．１．０］ヘキシル誘導体 |
| RU2517181C2 (ru) | 2008-10-16 | 2014-05-27 | Орто-Макнейл-Янссен Фармасьютикалз, Инк. | Производные индола и бензоморфолина в качестве модулятора метаботропных глутаматных рецепторов |
| WO2010060589A1 (en) | 2008-11-28 | 2010-06-03 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc. | Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors |
| PA8854101A1 (es) | 2008-12-18 | 2010-07-27 | Ortho Mcneil Janssen Pharm | Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa |
| WO2010089292A1 (en) | 2009-02-06 | 2010-08-12 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc | Novel substituted bicyclic heterocyclic compounds as gamma secretase modulators |
| ES2427917T3 (es) * | 2009-02-10 | 2013-11-04 | Astrazeneca Ab | Derivados de triazolo [4,3-b] piridazina y sus usos para el cáncer de próstata |
| TWI461425B (zh) | 2009-02-19 | 2014-11-21 | Janssen Pharmaceuticals Inc | 作為伽瑪分泌酶調節劑之新穎經取代的苯并唑、苯并咪唑、唑并吡啶及咪唑并吡啶衍生物類 |
| CA2756870A1 (en) * | 2009-03-31 | 2010-10-07 | Arqule, Inc. | Substituted indolo-pyridinone compounds |
| GB0906470D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| GB0906472D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| AU2010262036B2 (en) | 2009-05-07 | 2014-10-30 | Cellzome Limited | Novel substituted indazole and aza-indazole derivatives as gamma secretase modulators |
| PE20120473A1 (es) * | 2009-05-11 | 2012-05-27 | Astrazeneca Ab | [1,2,4]triazolo[4,3-b]piridazinas como ligandos del receptor de androgenos |
| MY153913A (en) | 2009-05-12 | 2015-04-15 | Janssen Pharmaceuticals Inc | 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| CN102439008B (zh) | 2009-05-12 | 2015-04-29 | 杨森制药有限公司 | 1,2,4-三唑并[4,3-a]吡啶衍生物及其用于治疗或预防神经和精神病症的用途 |
| MY153912A (en) | 2009-05-12 | 2015-04-15 | Janssen Pharmaceuticals Inc | 1, 2, 4,-triazolo[4,3-a[pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| JP2012532912A (ja) | 2009-07-15 | 2012-12-20 | ジヤンセン・フアーマシユーチカルズ・インコーポレーテツド | ガンマセクレターゼモジュレーターとしての置換されたトリアゾールおよびイミダゾール誘導体 |
| US8952034B2 (en) * | 2009-07-27 | 2015-02-10 | Gilead Sciences, Inc. | Fused heterocyclic compounds as ion channel modulators |
| JP5781510B2 (ja) | 2009-08-12 | 2015-09-24 | ノバルティス アーゲー | ヘテロ環式ヒドラゾン化合物および癌および炎症の処置のためのそれらの使用 |
| JP5775871B2 (ja) | 2009-08-20 | 2015-09-09 | ノバルティス アーゲー | ヘテロ環式オキシム化合物 |
| PH12012500778A1 (en) | 2009-10-30 | 2012-11-26 | Janssen Pharmaceutica Nv | IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS |
| BR112012017310A2 (pt) | 2010-01-15 | 2016-04-19 | Janssen Pharmaceuticals Inc | derivados de triazol substituídos como moduladores de gama secretase |
| AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
| BR112012033402A2 (pt) | 2010-07-02 | 2017-01-24 | Gilead Sciences Inc | moduladores de canais de íons conforme os compostos heterocíclicos fundidos |
| CN103261195B (zh) | 2010-11-08 | 2015-09-02 | 杨森制药公司 | 1,2,4-三唑并[4,3-a]吡啶衍生物及其作为MGLUR2受体的正变构调节剂的用途 |
| PL2649069T3 (pl) | 2010-11-08 | 2016-01-29 | Janssen Pharmaceuticals Inc | Pochodne 1,2,4-triazolo[4,3-a]pirydyny i ich zastosowanie jako dodatnich allosterycznych modulatorów receptorów mGluR2 |
| EP2661435B1 (en) | 2010-11-08 | 2015-08-19 | Janssen Pharmaceuticals, Inc. | 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS |
| US9000186B2 (en) | 2011-02-01 | 2015-04-07 | Kyowa Hakko Kirin Co., Ltd. | Ring-fused heterocyclic derivative |
| AU2012230348A1 (en) | 2011-03-24 | 2013-08-29 | Cellzome Limited | Novel substituted triazolyl piperazine and triazolyl piperidine derivatives as gamma secretase modulators |
| CA2834164A1 (en) | 2011-05-10 | 2012-11-15 | Gilead Sciences, Inc. | Fused benzoxazinones as ion channel modulators |
| BR112013033375B1 (pt) | 2011-06-27 | 2022-05-10 | Janssen Pharmaceutica N.V | Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxa-lina, seu uso, composição farmacêutica que os compreende, processo de preparação dos mesmos, solução estéril e composto intermediário |
| TW201837023A (zh) | 2011-07-01 | 2018-10-16 | 美商基利科學股份有限公司 | 作為離子通道調節劑之稠合雜環化合物 |
| NO3175985T3 (https=) | 2011-07-01 | 2018-04-28 | ||
| KR101913135B1 (ko) | 2011-07-15 | 2018-10-30 | 얀센 파마슈티칼즈, 인코포레이티드 | 감마 세크레타제 조절 인자로서의 신규의 치환 인돌 유도체 |
| EA026655B1 (ru) | 2011-09-15 | 2017-05-31 | Новартис Аг | 6-ЗАМЕЩЕННЫЕ 3-(ХИНОЛИН-6-ИЛТИО)[1,2,4]ТРИАЗОЛО[4,3-a]ПИРИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ c-MET ТИРОЗИНКИНАЗЫ |
| US9181245B2 (en) | 2012-05-16 | 2015-11-10 | Janssen Pharmaceuticals, Inc. | Substituted pyrido[1,2-a]pyrazines and substituted pyrido[1,2-a][1,4]diazepines for the treatment of (inter alia) Alzheimer's disease |
| HK1206250A1 (en) | 2012-06-26 | 2016-01-08 | Janssen Pharmaceutica Nv | Combinations comprising pde 2 inhibitors such as 1-aryl-4-methyl-[1,2,4] triazolo [4,3-a] quinoxaline compounds and ped 10 inhibitors for use in the treatment of neurological or metabolic disorders |
| WO2014009305A1 (en) | 2012-07-09 | 2014-01-16 | Janssen Pharmaceutica Nv | Inhibitors of phosphodiesterase 10 enzyme |
| CA2894536C (en) | 2012-12-18 | 2020-07-28 | Vertex Pharmaceuticals Incorporated | Mannose derivatives for treating bacterial infections |
| CA2889249C (en) | 2012-12-20 | 2021-02-16 | Francois Paul Bischoff | Tricyclic 3,4-dihydro-2h-pyrido[1,2-a]pyrazine-1,6-dione derivatives as gamma secretase modulators |
| CA2891755C (en) | 2013-01-17 | 2021-10-26 | Janssen Pharmaceutica Nv | Substituted pyrido-piperazinone derivatives as gamma secretase modulators |
| MX2015012472A (es) | 2013-03-12 | 2016-02-10 | Vertex Pharma | Derivados de manosa para el tratamiento de infecciones bacterianas. |
| US9776997B2 (en) | 2013-06-04 | 2017-10-03 | Bayer Pharma Aktiengesellschaft | 3-aryl-substituted imidazo[1,2-A]pyridines and their use |
| JO3368B1 (ar) | 2013-06-04 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2 |
| JO3367B1 (ar) * | 2013-09-06 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2 |
| US9738642B2 (en) | 2013-09-19 | 2017-08-22 | Bristol-Myers Squibb Company | Triazolopyridine ether derivatives and their use in neurological and pyschiatric disorders |
| US9580422B2 (en) | 2013-10-22 | 2017-02-28 | Bristol-Myers Squibb Company | Isotopically labeled triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors |
| GB201321742D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| TW201609722A (zh) * | 2013-12-13 | 2016-03-16 | 美國禮來大藥廠 | 新穎三唑并吡啶化合物 |
| AU2014372638A1 (en) | 2013-12-23 | 2016-06-16 | Norgine B.V. | Compounds useful as CCR9 modulators |
| US10562897B2 (en) | 2014-01-16 | 2020-02-18 | Janssen Pharmaceutica Nv | Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators |
| HUE053734T2 (hu) | 2014-01-21 | 2021-07-28 | Janssen Pharmaceutica Nv | 2-es altípusú metabotróp glutamáterg receptor pozitív allosztérikus modulátorait tartalmazó kombinációk és alkalmazásuk |
| KR20220049612A (ko) | 2014-01-21 | 2022-04-21 | 얀센 파마슈티카 엔.브이. | 대사 조절형 글루탐산 작동성 수용체 제2아형의 양성 알로스테릭 조절제 또는 오르토스테릭 작동제를 포함하는 조합 및 그 용도 |
| EP3105219B9 (en) | 2014-02-13 | 2018-10-03 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| MX373103B (es) | 2014-02-13 | 2020-04-17 | Incyte Holdings Corp | Ciclopropilaminas como inhibidores de desmetilasa específica de lisina 1 (lsd1). |
| SI3105218T1 (sl) | 2014-02-13 | 2019-11-29 | Incyte Corp | Ciklopropilamini kot inhibitorji LSD1 |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| US9688699B2 (en) | 2014-02-19 | 2017-06-27 | Bayer Pharma Aktiengesellschaft | 3-(pyrimidine-2-yl)imidazo[1,2-a]pyridines |
| TWI687419B (zh) | 2014-07-10 | 2020-03-11 | 美商英塞特公司 | 作為ｌｓｄ１抑制劑之咪唑并吡啶及咪唑并吡嗪 |
| TW201613925A (en) | 2014-07-10 | 2016-04-16 | Incyte Corp | Imidazopyrazines as LSD1 inhibitors |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| US9580420B2 (en) * | 2014-08-06 | 2017-02-28 | Bristol-Meyers Squibb Company | Process for the preparation of 4-(8-(2-chlorophenoxy)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)bicyclo[2.2.1]heptan-1-ol and novel intermediates therefor |
| US10292970B2 (en) | 2014-12-02 | 2019-05-21 | Bayer Pharma Aktiengesellschaft | Heteroaryl-substituted imidazo[1,2-A]pyridines and their use |
| EP3277689B1 (en) | 2015-04-03 | 2019-09-04 | Incyte Corporation | Heterocyclic compounds as lsd1 inhibitors |
| LT3334709T (lt) | 2015-08-12 | 2025-03-10 | Incyte Holdings Corporation | Lsd1 inhibitoriaus druskos |
| JP6999574B2 (ja) | 2016-04-22 | 2022-01-18 | インサイト・コーポレイション | Ｌｓｄ１阻害剤の製剤 |
| WO2018184976A1 (de) | 2017-04-05 | 2018-10-11 | Bayer Pharma Aktiengesellschaft | Substituierte imidazo[1,2-a]pyridincarboxamide und ihre verwendung |
| WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
| BR112023026747A2 (pt) | 2021-06-18 | 2024-03-12 | Aligos Therapeutics Inc | Métodos e composições para direcionamento de pd-l1 |
| CA3240346A1 (en) | 2021-12-16 | 2023-06-22 | Aligos Therapeutics, Inc. | Methods and compositions for targeting pd-l1 |
Family Cites Families (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3597423A (en) | 1966-08-31 | 1971-08-03 | Boehringer Mannheim Gmbh | 5-nitrofuryl-2-s-triazolo-(4,3-a)-pyridine derivatives |
| US4358453A (en) | 1982-01-08 | 1982-11-09 | Schering Corporation | 1,2,4-Triazolo[4,3-a]pyridines |
| DE3540149A1 (de) * | 1985-11-13 | 1987-05-14 | Boehringer Mannheim Gmbh | Verwendung von 1-(benztriazol-4-yloxy)3-(2-(2-methoxyphenoxy) -ethylamino)-2-propanol als antiglaukommittel, optisch aktive r und s isomere dieser substanz, verfahren zur herstellung derselben sowie arzneimittel, die diese substanzen enthalten |
| NZ224714A (en) | 1987-06-01 | 1990-03-27 | Janssen Pharmaceutica Nv | Substituted benzotriazole derivatives and pharmaceutical compositions |
| US5236917A (en) | 1989-05-04 | 1993-08-17 | Sterling Winthrop Inc. | Saccharin derivatives useful as proteolytic enzyme inhibitors and compositions and method of use thereof |
| CA2026792A1 (en) | 1989-11-01 | 1991-05-02 | Michael N. Greco | (6,7-dihydro-5h-pyrrolo[1,2-c]imidazol-5-yl)- and (5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl) substituted 1h-benzotriazole derivatives |
| IL96432A0 (en) | 1989-11-30 | 1991-08-16 | Schering Ag | Pesticidal compositions containing pyridine derivatives and novel pyridine derivatives |
| JP3531169B2 (ja) | 1996-06-11 | 2004-05-24 | 三菱ウェルファーマ株式会社 | 縮合ヘテロ環化合物およびその医薬用途 |
| ES2194205T3 (es) | 1996-07-25 | 2003-11-16 | Merck Sharp & Dohme | Derivados de triazolo-piridazina sustituidos como ligandos para los receptores gaba. |
| GB2345443A (en) | 1999-01-08 | 2000-07-12 | Merck Sharp & Dohme | Use of triazolo-pyridazines for treating premenstrual syndrome |
| PL351987A1 (en) | 1999-04-28 | 2003-07-14 | Reddys Lab Ltd Dr | Substitution bicyclic-heterocyclic compounds, method of obtaining thereof, and use of such compounds to control adiposis and to reduce the level of cholesterol |
| JP2000319277A (ja) | 1999-05-11 | 2000-11-21 | Ono Pharmaceut Co Ltd | 縮合ピラジン化合物およびその化合物を有効成分とする薬剤 |
| EE200300437A (et) | 2001-03-09 | 2004-02-16 | Pfizer Products Inc. | Triasolopüridiinid kui põletikuvastased ained |
| JP4250756B2 (ja) | 2001-07-06 | 2009-04-08 | 株式会社大万 | 遊技機 |
| US20050113283A1 (en) | 2002-01-18 | 2005-05-26 | David Solow-Cordero | Methods of treating conditions associated with an EDG-4 receptor |
| WO2003065983A2 (en) | 2002-02-01 | 2003-08-14 | Merck & Co., Inc. | 11-beta-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia |
| AR040241A1 (es) | 2002-06-10 | 2005-03-23 | Merck & Co Inc | Inhibidores de la 11-beta-hidroxiesteroide deshidrogrenasa 1 para el tratamiento de la diabetes obesidad y dislipidemia |
| US7005523B2 (en) * | 2002-08-30 | 2006-02-28 | Pfizer Inc. | Cycloalkyl-[4-(trifluorophenyl)-oxazol-5yl]-triazolo-pyridines |
| MXPA05002123A (es) | 2002-08-30 | 2005-06-06 | Pfizer Prod Inc | Nuevos procedimientos e intermedios para preparar triazolo-piridinas. |
| JO2397B1 (en) | 2002-12-20 | 2007-06-17 | ميرك شارب اند دوم كوربوريشن | Terazol derivatives as beta-hydroxy steroid dihydrogenase-1 inhibitors |
| WO2004056744A1 (en) | 2002-12-23 | 2004-07-08 | Janssen Pharmaceutica N.V. | Adamantyl acetamides as hydroxysteroid dehydrogenase inhibitors |
| TW200503994A (en) | 2003-01-24 | 2005-02-01 | Novartis Ag | Organic compounds |
| CA2515190A1 (en) | 2003-02-14 | 2004-08-26 | Pfizer Products Inc. | Triazolo-pyridines as anti-inflammatory compounds |
| DE602004025220D1 (de) | 2003-04-11 | 2010-03-11 | High Point Pharmaceuticals Llc | Pharmazeutische verwendungen von kondensierten 1,2,4-triazolen |
| CA2524376A1 (en) | 2003-05-05 | 2004-12-16 | Neurogen Corporation | Substituted imidazolopyrazine and triazolopyrazyne derivatives: gabaa receptor ligands |
| US8026264B2 (en) | 2003-05-29 | 2011-09-27 | Merck Sharp And Dohme Corp. | Triazole derivatives as inhibitors of 11-β hydroxysteroid dehydrogenase-1 |
| CA2529558A1 (en) * | 2003-07-01 | 2005-01-13 | Astellas Pharma Inc. | Agent inducing increase in bone mass |
| US20050049276A1 (en) * | 2003-07-23 | 2005-03-03 | Warner-Lambert Company, Llc | Imidazopyridines and triazolopyridines |
| US7538120B2 (en) | 2003-09-03 | 2009-05-26 | Array Biopharma Inc. | Method of treating inflammatory diseases |
| US7144907B2 (en) * | 2003-09-03 | 2006-12-05 | Array Biopharma Inc. | Heterocyclic inhibitors of MEK and methods of use thereof |
| GB0325745D0 (en) | 2003-11-05 | 2003-12-10 | Astrazeneca Ab | Chemical compounds |
| GB0326029D0 (en) | 2003-11-07 | 2003-12-10 | Astrazeneca Ab | Chemical compounds |
| US7875642B2 (en) | 2004-01-26 | 2011-01-25 | Merck Sharp & Dohme Corp. | Crystalline forms of an inhibitor of 11-β-hydroxysteroid dehydrogenase type 1 |
| US7306631B2 (en) | 2004-03-30 | 2007-12-11 | The Procter & Gamble Company | Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof |
| JP2008508337A (ja) | 2004-08-02 | 2008-03-21 | シュバルツ ファルマ アクチェンゲゼルシャフト | インドリジンカルボキサミド並びにそのアザ及びジアザ誘導体 |
| PL1778686T3 (pl) | 2004-08-12 | 2009-04-30 | Pfizer | Pochodne triazolopirydynylosulfanylowe jako inhibitory kinazy MAP P38 |
| EP1786811A2 (en) | 2004-08-18 | 2007-05-23 | Pharmacia & Upjohn Company LLC | Triazolopyridine compounds |
| BRPI0514391A (pt) | 2004-08-18 | 2008-06-10 | Pharmacia & Upjohn Co Llc | compostos de triazolopiridina para o tratamento de inflamação |
| US7605168B2 (en) | 2004-09-03 | 2009-10-20 | Plexxikon, Inc. | PDE4B inhibitors |
| JP4882748B2 (ja) | 2004-09-16 | 2012-02-22 | アステラス製薬株式会社 | トリアゾール誘導体またはその塩 |
| WO2006036816A2 (en) | 2004-09-24 | 2006-04-06 | Smithkline Beecham Corporation | Chemical compounds |
| US20080261970A1 (en) | 2004-09-27 | 2008-10-23 | Elixir Pharmaceuticals, Inc. | Sufonamides and Uses Thereof |
| WO2006034804A1 (en) | 2004-09-29 | 2006-04-06 | F.Hoffmann-La Roche Ag | Indozolone derivatives as 11b-hsd1 inhibitors |
| WO2006038116A2 (en) | 2004-10-07 | 2006-04-13 | Warner-Lambert Company Llc | Triazolopyridine derivatives as antibacterial agents |
| WO2006038738A1 (ja) | 2004-10-08 | 2006-04-13 | Takeda Pharmaceutical Company Limited | 受容体機能調節剤 |
| US8097727B2 (en) | 2004-10-13 | 2012-01-17 | Merck Patent Gmbh | N,N′-diphenylurea derivatives which are suitable as kinase inhibitors |
| WO2006042599A1 (de) | 2004-10-13 | 2006-04-27 | Merck Patent Gmbh | Phenylharnstoffderivate als hemmstoffe von tyrosinkinasen zur behandlung von tumorerkrankungen |
| ATE479687T1 (de) | 2004-10-15 | 2010-09-15 | Takeda Pharmaceutical | Kinaseinhibitoren |
| DE602005014375D1 (de) | 2004-10-19 | 2009-06-18 | Neurocrine Biosciences Inc | Crf-rezeptor-antagonisten und zugehörige verfahren |
| GB0519957D0 (en) | 2005-09-30 | 2005-11-09 | Sb Pharmco Inc | Chemical compound |
| US7151176B2 (en) | 2004-10-21 | 2006-12-19 | Bristol-Myers Squibb Company | Pyrrolotriazine compounds |
| CA2588350A1 (en) | 2004-10-25 | 2006-05-04 | University Of Medicine And Dentistry Of New Jersey | Anti-mitotic anti-proliferative compounds |
| US7713979B2 (en) | 2004-10-29 | 2010-05-11 | Eli Lilly And Company | Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
| EP1666467A1 (en) | 2004-11-08 | 2006-06-07 | Evotec AG | 11Beta-HSD1 Inhibitors |
| EP1655283A1 (en) | 2004-11-08 | 2006-05-10 | Evotec OAI AG | 11beta-HSD1 Inhibitors |
| JP2008521858A (ja) | 2004-12-01 | 2008-06-26 | ラボラトワール セローノ ソシエテ アノニム | 過増殖性疾患を処置するための［１，２，４］トリアゾロ［４，３−ａ］ピリジン誘導体 |
| WO2006080533A1 (ja) | 2005-01-31 | 2006-08-03 | Mochida Pharmaceutical Co., Ltd. | ３－アミノ－１,２,４－トリアゾール誘導体 |
| WO2007007688A1 (ja) | 2005-07-08 | 2007-01-18 | Mochida Pharmaceutical Co., Ltd. | ３,５－ジアミノ－１,２,４－トリアゾール誘導体 |
-
2006
- 2006-06-07 US US11/448,946 patent/US7572807B2/en active Active
- 2006-06-08 PE PE2006000635A patent/PE20070002A1/es not_active Application Discontinuation
- 2006-06-08 WO PCT/US2006/022260 patent/WO2006135667A1/en not_active Ceased
- 2006-06-08 AU AU2006258077A patent/AU2006258077B2/en not_active Ceased
- 2006-06-08 TW TW095120382A patent/TW200716116A/zh unknown
- 2006-06-08 MX MX2007015283A patent/MX2007015283A/es active IP Right Grant
- 2006-06-08 KR KR1020087000470A patent/KR20080018942A/ko not_active Ceased
- 2006-06-08 EP EP06772525A patent/EP1912986B1/en active Active
- 2006-06-08 ES ES06772525T patent/ES2392656T3/es active Active
- 2006-06-08 JP JP2008515911A patent/JP5124450B2/ja not_active Expired - Fee Related
- 2006-06-08 AR ARP060102405A patent/AR057357A1/es unknown
-
2007
- 2007-11-26 NO NO20076054A patent/NO20076054L/no not_active Application Discontinuation
-
2009
- 2009-07-27 US US12/509,541 patent/US8158648B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2008543764A5 (https=) | ||
| ES2673160T5 (es) | Moduladores selectivos del receptor de la esfingosina 1 fosfato y métodos de síntesis quiral | |
| TWI762743B (zh) | 磺醯胺化合物及其用途 | |
| CN1250550C (zh) | 脒衍生物的制备方法 | |
| KR20220066923A (ko) | Shp2 포스파테이스 억제제 및 이의 제조 및 사용 방법 | |
| CN104411700B (zh) | 4-[5-(吡啶-4-基)-1h-1,2,4-三唑-3-基]吡啶-2-腈的多晶型及其制造方法 | |
| US8981105B2 (en) | Process of preparing a thrombin specific inhibitor | |
| JP6469214B2 (ja) | Ｎ−アシル−（３−置換）−（８−置換）−５，６−ジヒドロ−［１，２，４］トリアゾロ［４，３−ａ］ピラジンの新規キラル合成 | |
| SK283589B6 (sk) | Tieno[2,3-d]pyrimidíndióny, spôsoby ich prípravy, farmaceutické kompozície s ich obsahom a ich použitie | |
| CN103562200A (zh) | 用于治疗关节炎的新咪唑衍生物 | |
| WO2009131090A1 (ja) | アミノ酸化合物 | |
| WO2014117676A1 (zh) | 一种具有dhodh抑制活性的含n、s杂环化合物及其制备和用途 | |
| JPWO2018124000A1 (ja) | ピリミジン誘導体 | |
| CN101448819A (zh) | (5s)-5-[4-(5-氯-吡啶-2-基氧基)-哌啶-1-磺酰基甲基]-5-甲基-咪唑烷-2,4-二酮的新晶体变化形式及其中间体 | |
| JP4137174B2 (ja) | チロシンキナーゼ阻害作用を有するキナゾリン誘導体 | |
| CN1458933A (zh) | 噻吩并嘧啶化合物及其盐以及其制备方法 | |
| JP2008524210A5 (https=) | ||
| TW201400464A (zh) | 新穎嘧啶化合物及含有此之醫藥 | |
| WO2005035512A1 (ja) | チアジアゾリン誘導体 | |
| JP2018501268A (ja) | チゾキサニドホスフェート及びアルカンスルホネート並びにその医薬用途 | |
| CN100344615C (zh) | 制备N－(吡咯并[2,3－d]嘧啶－5－基)酰基谷氨酸衍生物的方法及中间体 | |
| JP2008524211A5 (https=) | ||
| JP2013530948A5 (https=) | ||
| CN119855821A (zh) | 噻唑并[5,4-b]吡啶MALT-1抑制剂 | |
| TWI327140B (en) | Pyrimidine derivatives |