JP2015502379A5 - - Google Patents
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- JP2015502379A5 JP2015502379A5 JP2014547960A JP2014547960A JP2015502379A5 JP 2015502379 A5 JP2015502379 A5 JP 2015502379A5 JP 2014547960 A JP2014547960 A JP 2014547960A JP 2014547960 A JP2014547960 A JP 2014547960A JP 2015502379 A5 JP2015502379 A5 JP 2015502379A5
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- LTXTYSOFFIGWKB-UHFFFAOYSA-N 3,5-diamino-6-chloro-n-[n'-[1-[[4-[2-(2-hydroxyethoxy)ethylcarbamoyl]phenyl]methyl]piperidin-4-yl]carbamimidoyl]pyrazine-2-carboxamide Chemical compound N=1C(Cl)=C(N)N=C(N)C=1C(=O)N=C(N)NC(CC1)CCN1CC1=CC=C(C(=O)NCCOCCO)C=C1 LTXTYSOFFIGWKB-UHFFFAOYSA-N 0.000 claims description 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 25
- 150000001875 compounds Chemical class 0.000 claims 14
- 229910052757 nitrogen Inorganic materials 0.000 claims 14
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 11
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 206010006451 bronchitis Diseases 0.000 claims 5
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 4
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 4
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 230000000172 allergic effect Effects 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000001153 fluoro group Chemical group F* 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- PKDPUENCROCRCH-UHFFFAOYSA-N 1-piperazin-1-ylethanone Chemical compound CC(=O)N1CCNCC1 PKDPUENCROCRCH-UHFFFAOYSA-N 0.000 claims 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims 2
- 208000029523 Interstitial Lung disease Diseases 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 208000010668 atopic eczema Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000005647 linker group Chemical group 0.000 claims 2
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- PVOAHINGSUIXLS-UHFFFAOYSA-N 1-Methylpiperazine Chemical compound CN1CCNCC1 PVOAHINGSUIXLS-UHFFFAOYSA-N 0.000 claims 1
- WGCYRFWNGRMRJA-UHFFFAOYSA-N 1-ethylpiperazine Chemical compound CCN1CCNCC1 WGCYRFWNGRMRJA-UHFFFAOYSA-N 0.000 claims 1
- YEQAMPOYHLICPF-UHFFFAOYSA-N 1-piperazin-1-ylpropan-1-one Chemical compound CCC(=O)N1CCNCC1 YEQAMPOYHLICPF-UHFFFAOYSA-N 0.000 claims 1
- AOEMJQMQKWGQMS-UHFFFAOYSA-N 2-[4-[[4-[[amino-[(3,5-diamino-6-chloropyrazine-2-carbonyl)amino]methylidene]amino]piperidin-1-yl]methyl]phenoxy]acetic acid Chemical compound N=1C(Cl)=C(N)N=C(N)C=1C(=O)N=C(N)NC(CC1)CCN1CC1=CC=C(OCC(O)=O)C=C1 AOEMJQMQKWGQMS-UHFFFAOYSA-N 0.000 claims 1
- ZKAIKFIKDXVJMV-UHFFFAOYSA-N 3,5-diamino-6-chloro-n-[n'-[1-[[4-[1-[2-[2-(2-hydroxyethoxy)ethoxy]ethyl]triazol-4-yl]phenyl]methyl]piperidin-4-yl]carbamimidoyl]pyrazine-2-carboxamide Chemical compound N1=C(Cl)C(N)=NC(N)=C1C(=O)NC(=N)NC1CCN(CC=2C=CC(=CC=2)C=2N=NN(CCOCCOCCO)C=2)CC1 ZKAIKFIKDXVJMV-UHFFFAOYSA-N 0.000 claims 1
- UTVMGKBIGHFOJU-UHFFFAOYSA-N 3,5-diamino-n-[n'-[1-[[4-[2-[4-[3-[bis(2-hydroxyethyl)amino]-3-oxopropyl]triazol-1-yl]ethyl]phenyl]methyl]piperidin-4-yl]carbamimidoyl]-6-chloropyrazine-2-carboxamide Chemical compound N=1C(Cl)=C(N)N=C(N)C=1C(=O)N=C(N)NC(CC1)CCN1CC(C=C1)=CC=C1CCN1C=C(CCC(=O)N(CCO)CCO)N=N1 UTVMGKBIGHFOJU-UHFFFAOYSA-N 0.000 claims 1
- VZFSBYTXYYWNHF-UHFFFAOYSA-N 3,5-diamino-n-[n'-[1-[[4-[4-[[3-aminopropanoyl(methyl)amino]methyl]triazol-1-yl]phenyl]methyl]piperidin-4-yl]carbamimidoyl]-6-chloropyrazine-2-carboxamide Chemical compound N1=NC(CN(C)C(=O)CCN)=CN1C(C=C1)=CC=C1CN1CCC(NC(N)=NC(=O)C=2C(=NC(N)=C(Cl)N=2)N)CC1 VZFSBYTXYYWNHF-UHFFFAOYSA-N 0.000 claims 1
- ZRGHNTUZIZUJJN-UHFFFAOYSA-N 3-[[4-[[amino-[(3,5-diamino-6-chloropyrazine-2-carbonyl)amino]methylidene]amino]piperidin-1-yl]methyl]benzoic acid Chemical compound N=1C(Cl)=C(N)N=C(N)C=1C(=O)N=C(N)NC(CC1)CCN1CC1=CC=CC(C(O)=O)=C1 ZRGHNTUZIZUJJN-UHFFFAOYSA-N 0.000 claims 1
- DHIXBEJBJZXTRK-UHFFFAOYSA-N 4-[[4-[[amino-[(3,5-diamino-6-chloropyrazine-2-carbonyl)amino]methylidene]amino]piperidin-1-yl]methyl]benzoic acid Chemical compound N=1C(Cl)=C(N)N=C(N)C=1C(=O)N=C(N)NC(CC1)CCN1CC1=CC=C(C(O)=O)C=C1 DHIXBEJBJZXTRK-UHFFFAOYSA-N 0.000 claims 1
- 206010052613 Allergic bronchitis Diseases 0.000 claims 1
- 206010001889 Alveolitis Diseases 0.000 claims 1
- 208000035143 Bacterial infection Diseases 0.000 claims 1
- 206010006458 Bronchitis chronic Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010009137 Chronic sinusitis Diseases 0.000 claims 1
- 206010011224 Cough Diseases 0.000 claims 1
- -1 EGFR inhibitor Substances 0.000 claims 1
- 206010014561 Emphysema Diseases 0.000 claims 1
- 239000005977 Ethylene Substances 0.000 claims 1
- 241000233866 Fungi Species 0.000 claims 1
- 229940122696 MAP kinase inhibitor Drugs 0.000 claims 1
- 208000000592 Nasal Polyps Diseases 0.000 claims 1
- 102100029438 Nitric oxide synthase, inducible Human genes 0.000 claims 1
- 101710089543 Nitric oxide synthase, inducible Proteins 0.000 claims 1
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 claims 1
- 206010037423 Pulmonary oedema 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
- 208000036142 Viral infection Diseases 0.000 claims 1
- CQIAVTYESMSECF-UHFFFAOYSA-N [4-[[4-[[amino-[(3,5-diamino-6-chloropyrazine-2-carbonyl)amino]methylidene]amino]piperidin-1-yl]methyl]phenyl]-ethoxyphosphinic acid Chemical compound C1=CC(P(O)(=O)OCC)=CC=C1CN1CCC(NC(N)=NC(=O)C=2C(=NC(N)=C(Cl)N=2)N)CC1 CQIAVTYESMSECF-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 239000000808 adrenergic beta-agonist Substances 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 208000006682 alpha 1-Antitrypsin Deficiency Diseases 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 230000001387 anti-histamine Effects 0.000 claims 1
- 229940065524 anticholinergics inhalants for obstructive airway diseases Drugs 0.000 claims 1
- 239000000739 antihistaminic agent Substances 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 230000001580 bacterial effect Effects 0.000 claims 1
- 208000022362 bacterial infectious disease Diseases 0.000 claims 1
- 230000003454 betamimetic effect Effects 0.000 claims 1
- 201000009267 bronchiectasis Diseases 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 208000029771 childhood onset asthma Diseases 0.000 claims 1
- 239000000812 cholinergic antagonist Substances 0.000 claims 1
- 208000007451 chronic bronchitis Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000027157 chronic rhinosinusitis Diseases 0.000 claims 1
- 229940000425 combination drug Drugs 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- 229960001334 corticosteroids Drugs 0.000 claims 1
- 201000003146 cystitis Diseases 0.000 claims 1
- 239000003136 dopamine receptor stimulating agent Substances 0.000 claims 1
- 229940121647 egfr inhibitor Drugs 0.000 claims 1
- 239000002713 epithelial sodium channel blocking agent Substances 0.000 claims 1
- 201000001155 extrinsic allergic alveolitis Diseases 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 244000000013 helminth Species 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 208000022098 hypersensitivity pneumonitis Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- YEESKJGWJFYOOK-IJHYULJSSA-N leukotriene D4 Chemical compound CCCCC\C=C/C\C=C/C=C/C=C/[C@H]([C@@H](O)CCCC(O)=O)SC[C@H](N)C(=O)NCC(O)=O YEESKJGWJFYOOK-IJHYULJSSA-N 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- IDLZYLWEDDWBTG-UHFFFAOYSA-N methyl 2-[4-[[4-[[amino-[(3,5-diamino-6-chloropyrazine-2-carbonyl)amino]methylidene]amino]piperidin-1-yl]methyl]phenoxy]acetate Chemical compound C1=CC(OCC(=O)OC)=CC=C1CN1CCC(NC(N)=NC(=O)C=2C(=NC(N)=C(Cl)N=2)N)CC1 IDLZYLWEDDWBTG-UHFFFAOYSA-N 0.000 claims 1
- FURKYKDPPBKNDH-UHFFFAOYSA-N methyl 3-[[4-[[amino-[(3,5-diamino-6-chloropyrazine-2-carbonyl)amino]methylidene]amino]piperidin-1-yl]methyl]-5-[2-(2-hydroxyethoxy)ethylcarbamoyl]benzoate Chemical compound OCCOCCNC(=O)C1=CC(C(=O)OC)=CC(CN2CCC(CC2)NC(N)=NC(=O)C=2C(=NC(N)=C(Cl)N=2)N)=C1 FURKYKDPPBKNDH-UHFFFAOYSA-N 0.000 claims 1
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims 1
- SOTQQEVCQNNUJB-UHFFFAOYSA-N n-[n'-[1-[[4-(2-acetamidoethylsulfamoyl)phenyl]methyl]piperidin-4-yl]carbamimidoyl]-3,5-diamino-6-chloropyrazine-2-carboxamide Chemical compound C1=CC(S(=O)(=O)NCCNC(=O)C)=CC=C1CN1CCC(NC(N)=NC(=O)C=2C(=NC(N)=C(Cl)N=2)N)CC1 SOTQQEVCQNNUJB-UHFFFAOYSA-N 0.000 claims 1
- 208000037916 non-allergic rhinitis Diseases 0.000 claims 1
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 1
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims 1
- 208000005333 pulmonary edema Diseases 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 239000003848 thrombocyte activating factor antagonist Substances 0.000 claims 1
- 231100000331 toxic Toxicity 0.000 claims 1
- 230000002588 toxic effect Effects 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
- 0 CC=C[C@@](C(N=C1C(N=C(N*)NC2CCN(Cc(cc3)ccc3OCC(O)=O)CC2)=O)Cl)N=C1N* Chemical compound CC=C[C@@](C(N=C1C(N=C(N*)NC2CCN(Cc(cc3)ccc3OCC(O)=O)CC2)=O)Cl)N=C1N* 0.000 description 11
- LZSBFNWNZWDNTP-DUXPYHPUSA-N C/C=C/c(nc(c(C(/N=C(\N)/NC1CCN(Cc2cccc(C(O)=O)c2)CC1)=O)n1)N)c1Cl Chemical compound C/C=C/c(nc(c(C(/N=C(\N)/NC1CCN(Cc2cccc(C(O)=O)c2)CC1)=O)n1)N)c1Cl LZSBFNWNZWDNTP-DUXPYHPUSA-N 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11194687 | 2011-12-20 | ||
| EP11194687.7 | 2011-12-20 | ||
| PCT/EP2012/076101 WO2013092674A1 (en) | 2011-12-20 | 2012-12-19 | Heterocyclic compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015502379A JP2015502379A (ja) | 2015-01-22 |
| JP2015502379A5 true JP2015502379A5 (https=) | 2016-02-12 |
| JP6110872B2 JP6110872B2 (ja) | 2017-04-05 |
Family
ID=47428633
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014547960A Active JP6110872B2 (ja) | 2011-12-20 | 2012-12-19 | ヘテロ環式化合物、前記化合物を含む薬物、その使用及びその調製方法 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US8859559B2 (https=) |
| EP (1) | EP2794595B1 (https=) |
| JP (1) | JP6110872B2 (https=) |
| WO (1) | WO2013092674A1 (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007079139A2 (en) | 2005-12-28 | 2007-07-12 | Vertex Pharmaceuticals, Inc. | Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| BR112014030284B1 (pt) | 2012-07-18 | 2021-11-30 | Sunshine Lake Pharma Co., Ltd | Composto, composição farmacêutica, e, uso de um composto ou de uma composição farmacêutica |
| WO2014177469A1 (en) | 2013-04-30 | 2014-11-06 | Boehringer Ingelheim International Gmbh,M | Diaminopyrazine compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof |
| JP6449870B2 (ja) | 2013-07-08 | 2019-01-09 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 肺および気道の疾患を処置するための上皮性ナトリウムチャネルの阻害剤としてのアミロライド型化合物 |
| JP6449880B2 (ja) * | 2013-08-08 | 2019-01-09 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 新規ピラジンアミド化合物 |
| AR099612A1 (es) | 2014-03-04 | 2016-08-03 | Actelion Pharmaceuticals Ltd | Derivados antibacterianos de 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona |
| CN106715418A (zh) * | 2014-07-07 | 2017-05-24 | 基因泰克公司 | 治疗化合物及其使用方法 |
| KR20170063954A (ko) | 2014-10-07 | 2017-06-08 | 버텍스 파마슈티칼스 인코포레이티드 | 낭성 섬유증 막횡단 전도도 조절자의 조정제의 공-결정 |
| GB201610854D0 (en) | 2016-06-21 | 2016-08-03 | Entpr Therapeutics Ltd | Compounds |
| GB201619694D0 (en) | 2016-11-22 | 2017-01-04 | Entpr Therapeutics Ltd | Compounds |
| GB201717051D0 (en) | 2017-10-17 | 2017-11-29 | Enterprise Therapeutics Ltd | Compounds |
| BR112020010898A2 (pt) * | 2017-12-20 | 2020-11-17 | Huntsman Petrochemical Llc | composto de alcoxilato de polieteramina, método para a preparação de um composto de alcoxilato de polieteramina, composição, produto embalado, composições concentrada e curável, formulação química de desempenho ou formulação de cuidados pessoais, e, concentrados emulsificável agroquímico, de suspensão agroquímica, líquido solúvel agroquímico e de aditivo de combustível. |
| GB201808093D0 (en) | 2018-05-18 | 2018-07-04 | Enterprise Therapeutics Ltd | Compounds |
| GB201918416D0 (en) | 2019-12-13 | 2020-01-29 | Z Factor Ltd | Compounds and their use for the treatment of Alpha1-Antitrypsin deficiency |
| CN115210229A (zh) | 2020-01-03 | 2022-10-18 | 博格有限责任公司 | 多环酰胺作为治疗癌症的ube2k调节剂 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL6812003A (https=) | 1967-09-07 | 1969-03-11 | ||
| US3953476A (en) | 1971-12-27 | 1976-04-27 | Merck & Co., Inc. | 3-Amino-5-sulfonylbenzoic acids |
| JP2003520042A (ja) | 2000-01-24 | 2003-07-02 | アイシス・ファーマシューティカルス・インコーポレーテッド | 誘導性一酸化窒素シンターゼ発現のアンチセンスモジュレーション |
| JP2007502829A (ja) * | 2003-08-18 | 2007-02-15 | パリオン・サイエンシィズ・インコーポレーテッド | 環状ピラジノイルグアニジンナトリウムチャネルブロッカー |
| GB0526244D0 (en) * | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
| CN101687851B (zh) * | 2007-05-07 | 2013-02-27 | 诺瓦提斯公司 | 有机化合物 |
| AU2009248179A1 (en) | 2008-05-13 | 2009-11-19 | Novartis Ag | 3,5-Diamino-6-chloro-pyrazine-2-carboxylic acid derivatives and their use as epithelial sodium channel blockers for the treatment of arway diseases |
| AR086745A1 (es) | 2011-06-27 | 2014-01-22 | Parion Sciences Inc | 3,5-diamino-6-cloro-n-(n-(4-(4-(2-(hexil(2,3,4,5,6-pentahidroxihexil)amino)etoxi)fenil)butil)carbamimidoil)pirazina-2-carboxamida |
| HUE032851T2 (en) | 2011-06-27 | 2017-11-28 | Parion Sciences Inc | A chemically and metabolically stable dipeptide having strong sodium channel blocking activity |
-
2012
- 2012-12-18 US US13/717,848 patent/US8859559B2/en active Active
- 2012-12-19 EP EP12805685.0A patent/EP2794595B1/en active Active
- 2012-12-19 WO PCT/EP2012/076101 patent/WO2013092674A1/en not_active Ceased
- 2012-12-19 JP JP2014547960A patent/JP6110872B2/ja active Active
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