CA2854217C - Substituted pyrazinoylguanidine compounds and their use as epithelial sodium channel blockers, medicaments containing said compounds and processes for the preparation thereof - Google Patents
Substituted pyrazinoylguanidine compounds and their use as epithelial sodium channel blockers, medicaments containing said compounds and processes for the preparation thereof Download PDFInfo
- Publication number
- CA2854217C CA2854217C CA2854217A CA2854217A CA2854217C CA 2854217 C CA2854217 C CA 2854217C CA 2854217 A CA2854217 A CA 2854217A CA 2854217 A CA2854217 A CA 2854217A CA 2854217 C CA2854217 C CA 2854217C
- Authority
- CA
- Canada
- Prior art keywords
- alkyl
- compound
- acid
- phenyl
- amino
- 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.)
- Expired - Fee Related
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/14—Antitussive agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/10—Anthelmintics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Otolaryngology (AREA)
- Immunology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Virology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Infusion, Injection, And Reservoir Apparatuses (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11187553 | 2011-11-02 | ||
| EP11187553.0 | 2011-11-02 | ||
| PCT/EP2012/071352 WO2013064450A1 (en) | 2011-11-02 | 2012-10-29 | Heterocyclic compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2854217A1 CA2854217A1 (en) | 2013-05-10 |
| CA2854217C true CA2854217C (en) | 2019-12-31 |
Family
ID=47073464
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2854217A Expired - Fee Related CA2854217C (en) | 2011-11-02 | 2012-10-29 | Substituted pyrazinoylguanidine compounds and their use as epithelial sodium channel blockers, medicaments containing said compounds and processes for the preparation thereof |
Country Status (34)
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2006332726B2 (en) | 2005-12-28 | 2012-12-13 | Vertex Pharmaceuticals Incorporated. | Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| JP6091513B2 (ja) | 2011-11-02 | 2017-03-08 | 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 | 複素環化合物、前記化合物を含む薬物、これらの使用及びこれらの調製方法 |
| CN105518000B (zh) * | 2013-07-02 | 2018-09-14 | 加州生物医学研究所 | 用于治疗囊性纤维化的化合物 |
| 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 |
| 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 |
| BR112017008178A2 (pt) * | 2014-10-24 | 2017-12-19 | Ono Pharmaceutical Co | ativador do canal de kcnq2-5 |
| WO2016112120A1 (en) * | 2015-01-07 | 2016-07-14 | The California Institute For Biomedical Research | Compounds for treatment of cystic fibrosis |
| 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 |
| GB201808093D0 (en) | 2018-05-18 | 2018-07-04 | Enterprise Therapeutics Ltd | Compounds |
| AU2021341508A1 (en) | 2020-09-10 | 2023-05-25 | Precirix N.V. | Antibody fragment against fap |
| CN112107580A (zh) * | 2020-09-29 | 2020-12-22 | 北京鑫开元医药科技有限公司 | 一种脾酪氨酸激酶抑制剂的制剂组合物及其制备方法 |
| WO2023203135A1 (en) | 2022-04-22 | 2023-10-26 | Precirix N.V. | Improved radiolabelled antibody |
| CN119584994A (zh) | 2022-05-02 | 2025-03-07 | 普雷西里克斯公司 | 预靶向 |
| WO2024243025A1 (en) * | 2023-05-19 | 2024-11-28 | Ikena Oncology, Inc. | Naphthyl-substituted pyrido[4,3-d]pyrimidines and related compounds and their use in treating medical conditions |
Family Cites Families (17)
| 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 |
| CA2378181A1 (en) | 1999-07-19 | 2001-01-25 | Richard C. Boucher, Jr. | Conjugates of sodium channel blockers and methods of using the same |
| AU2001229501A1 (en) | 2000-01-24 | 2001-07-31 | Isis Pharmaceuticals, Inc. | Antisense modulation of inducible nitric oxide synthase expression |
| CA2575670A1 (en) | 2004-08-18 | 2006-03-02 | Michael R. Johnson | Aliphatic amide & ester pyrazinoylguanidine sodium channel blockers |
| GB0526244D0 (en) | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
| US20080124276A1 (en) * | 2006-07-24 | 2008-05-29 | Lifeline Cell Technology | Synthetic cornea from retinal stem cells |
| CN101687851B (zh) * | 2007-05-07 | 2013-02-27 | 诺瓦提斯公司 | 有机化合物 |
| EA017919B1 (ru) | 2007-12-10 | 2013-04-30 | Новартис Аг | Производные пиразин-2-карбоксамида для лечения заболеваний, которые поддаются лечению путем блокирования эпителиальных натриевых каналов |
| BRPI0912542A2 (pt) * | 2008-05-13 | 2015-10-13 | Novartis Ag | derivados de ácido 3,5-diamino-cloro-pirazina-2-carboxílico e seu uso como bloqueadores do canal de sódio epitelial para o tratamento de vias aéreas. |
| EA201001848A1 (ru) | 2008-06-10 | 2011-08-30 | Новартис Аг | Производные пиразина в качестве блокаторов эпителиальных натриевых каналов |
| US9050339B2 (en) | 2010-09-17 | 2015-06-09 | Novartis Ag | Pyrazine derivatives as ENaC blockers |
| US8372845B2 (en) | 2010-09-17 | 2013-02-12 | Novartis Ag | Pyrazine derivatives as enac blockers |
| EP2723176B1 (en) | 2011-06-27 | 2017-04-12 | Parion Sciences, Inc. | A chemically and metabolically stable dipeptide possessing potent sodium channel blocker activity |
| 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 |
| JP2015501324A (ja) | 2011-11-02 | 2015-01-15 | 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 | アシルグアニジン及びアシルチオ尿素の新規調製方法 |
| JP6091513B2 (ja) | 2011-11-02 | 2017-03-08 | 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 | 複素環化合物、前記化合物を含む薬物、これらの使用及びこれらの調製方法 |
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2012
- 2012-10-29 JP JP2014539297A patent/JP6091513B2/ja active Active
- 2012-10-29 ME MEP-2017-247A patent/ME02905B/me unknown
- 2012-10-29 BR BR112014010583A patent/BR112014010583A2/pt active Search and Examination
- 2012-10-29 ES ES12777930.4T patent/ES2645744T3/es active Active
- 2012-10-29 HU HUE12777930A patent/HUE034929T2/en unknown
- 2012-10-29 AP AP2014007670A patent/AP2014007670A0/xx unknown
- 2012-10-29 AU AU2012331274A patent/AU2012331274B2/en not_active Ceased
- 2012-10-29 CA CA2854217A patent/CA2854217C/en not_active Expired - Fee Related
- 2012-10-29 CN CN201280065806.8A patent/CN104024244B/zh active Active
- 2012-10-29 US US13/662,791 patent/US8759349B2/en active Active
- 2012-10-29 PH PH1/2014/500970A patent/PH12014500970B1/en unknown
- 2012-10-29 GE GEAP201213485A patent/GEP20186880B/en unknown
- 2012-10-29 EP EP12777930.4A patent/EP2773633B1/en active Active
- 2012-10-29 LT LTEP12777930.4T patent/LT2773633T/lt unknown
- 2012-10-29 PL PL12777930T patent/PL2773633T3/pl unknown
- 2012-10-29 CN CN201610685839.2A patent/CN106279110B/zh active Active
- 2012-10-29 WO PCT/EP2012/071352 patent/WO2013064450A1/en not_active Ceased
- 2012-10-29 RS RS20171069A patent/RS56498B1/sr unknown
- 2012-10-29 PE PE2014000641A patent/PE20141607A1/es active IP Right Grant
- 2012-10-29 UA UAA201405764A patent/UA115868C2/uk unknown
- 2012-10-29 DK DK12777930.4T patent/DK2773633T3/da active
- 2012-10-29 SI SI201231100T patent/SI2773633T1/sl unknown
- 2012-10-29 SG SG11201401907TA patent/SG11201401907TA/en unknown
- 2012-10-29 MX MX2014005166A patent/MX348522B/es active IP Right Grant
- 2012-10-29 NO NO12777930A patent/NO2773633T3/no unknown
- 2012-10-29 HR HRP20171614TT patent/HRP20171614T1/hr unknown
- 2012-10-29 KR KR1020147012186A patent/KR102006612B1/ko not_active Expired - Fee Related
- 2012-10-29 PT PT127779304T patent/PT2773633T/pt unknown
- 2012-10-29 EA EA201400521A patent/EA025158B9/ru not_active IP Right Cessation
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2014
- 2014-04-09 IL IL232035A patent/IL232035A/en not_active IP Right Cessation
- 2014-04-24 CL CL2014001047A patent/CL2014001047A1/es unknown
- 2014-04-28 US US14/263,344 patent/US20140228374A1/en not_active Abandoned
- 2014-04-28 TN TNP2014000180A patent/TN2014000180A1/en unknown
- 2014-04-30 CO CO14092699A patent/CO6940429A2/es unknown
- 2014-05-26 EC ECIEPI20141929A patent/ECSP14001929A/es unknown
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2015
- 2015-08-05 US US14/818,478 patent/US9920035B2/en active Active
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2017
- 2017-10-30 CY CY171101128T patent/CY1120974T1/el unknown
- 2017-12-13 US US15/840,309 patent/US20180194747A1/en not_active Abandoned
Also Published As
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20171030 |
|
| MKLA | Lapsed |
Effective date: 20211029 |