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 (enExample) | 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 (enExample) |
| EP (1) | EP2794595B1 (enExample) |
| JP (1) | JP6110872B2 (enExample) |
| WO (1) | WO2013092674A1 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1993360T (pt) | 2005-12-28 | 2017-05-25 | Vertex Pharma | Formas sólidas de n-[2,4-bis(1,1-dimetiletil)-5-hidroxifenil]-1,4-di-hidro-4-oxoquinolina-3-carboxamida |
| MX2015000830A (es) | 2012-07-18 | 2015-10-26 | Sunshine Lake Pharma Co Ltd | Derivados heterociclicos nitrogenosos y su aplicacion en farmacos. |
| EP2991981B1 (en) * | 2013-04-30 | 2017-03-01 | Boehringer Ingelheim International GmbH | Diaminopyrazine compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof |
| WO2015003958A1 (en) * | 2013-07-08 | 2015-01-15 | Boehringer Ingelheim International Gmbh | Amiloride-type compounds as inhibitors in epithelial sodium channels for the treatment of diseases of the lungs and airways |
| WO2015018754A1 (en) * | 2013-08-08 | 2015-02-12 | Boehringer Ingelheim International Gmbh | Novel pyrazine amide compounds |
| 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 |
| JP2017525677A (ja) * | 2014-07-07 | 2017-09-07 | ジェネンテック， インコーポレイテッド | 治療用化合物及びその使用方法 |
| CN107250113B (zh) | 2014-10-07 | 2019-03-29 | 弗特克斯药品有限公司 | 囊性纤维化跨膜传导调节蛋白的调节剂的共晶 |
| 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 |
| CA3166630A1 (en) | 2020-01-03 | 2021-07-08 | Berg Llc | Polycyclic amides as ube2k modulators for treating cancer |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL6812003A (enExample) | 1967-09-07 | 1969-03-11 | ||
| US3953476A (en) | 1971-12-27 | 1976-04-27 | Merck & Co., Inc. | 3-Amino-5-sulfonylbenzoic acids |
| AU2001229501A1 (en) | 2000-01-24 | 2001-07-31 | Isis Pharmaceuticals, Inc. | Antisense modulation of inducible nitric oxide synthase expression |
| AU2004264441A1 (en) * | 2003-08-18 | 2005-02-24 | Parion Sciences, Inc. | Cyclic pyrazinoylguanidine sodium channel blockers |
| GB0526244D0 (en) * | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
| AU2008248598B2 (en) * | 2007-05-07 | 2011-11-17 | Novartis Ag | Organic compounds |
| US8664228B2 (en) | 2008-05-13 | 2014-03-04 | Novartis Ag | 3,5-diamino-6-chloro-pyrazine-2-carboxylic acid derivatives and their use as epithelial sodium channel blockers for the treatment of airway diseases |
| BR112013032771B1 (pt) | 2011-06-27 | 2021-01-12 | Parion Sciences, Inc. | dipeptídio quimicamente e metabolicamente estável possuindo potente atividade bloqueadora de canais de sódio |
| 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 |
-
2012
- 2012-12-18 US US13/717,848 patent/US8859559B2/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
- 2012-12-19 EP EP12805685.0A patent/EP2794595B1/en active Active
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