JP5254961B2 - ベータアゴニスト活性を有するフェニル置換ピラジノイルグアニジンナトリウムチャネル遮断薬 - Google Patents

ベータアゴニスト活性を有するフェニル置換ピラジノイルグアニジンナトリウムチャネル遮断薬 Download PDF

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JP5254961B2
JP5254961B2 JP2009514564A JP2009514564A JP5254961B2 JP 5254961 B2 JP5254961 B2 JP 5254961B2 JP 2009514564 A JP2009514564 A JP 2009514564A JP 2009514564 A JP2009514564 A JP 2009514564A JP 5254961 B2 JP5254961 B2 JP 5254961B2
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mmol
phenyl
compound
butyl
nmr
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JP2009539882A5 (enExample
JP2009539882A (ja
Inventor
マイケル・ロス・ジョンソン
アンドリュー・ジェイ・ハーシュ
リチャード・シー・バウチャー
ジャンツォン・ツァン
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パリオン・サイエンシィズ・インコーポレーテッド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C07D241/28—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
    • C07D241/30—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms in which said hetero-bound carbon atoms are part of a substructure —C(=X)—X—C(=X)—X— in which X is an oxygen or sulphur atom or an imino radical, e.g. imidoylguanidines
    • C07D241/32—(Amino-pyrazinoyl) guanidines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P1/10—Laxatives
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/16—Emollients or protectives, e.g. against radiation
    • 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
    • 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
    • A61P27/02—Ophthalmic 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
    • A61P27/02—Ophthalmic agents
    • A61P27/04—Artificial tears; Irrigation solutions
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Oncology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Toxicology (AREA)
  • Otolaryngology (AREA)
  • Nutrition Science (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2009514564A 2006-06-09 2007-06-11 ベータアゴニスト活性を有するフェニル置換ピラジノイルグアニジンナトリウムチャネル遮断薬 Expired - Fee Related JP5254961B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US81207706P 2006-06-09 2006-06-09
US60/812,077 2006-06-09
PCT/US2007/070861 WO2007146869A1 (en) 2006-06-09 2007-06-11 Phenyl substituted pyrazinoylguanidine sodium channel blockers possessing beta agonist activity

Publications (3)

Publication Number Publication Date
JP2009539882A JP2009539882A (ja) 2009-11-19
JP2009539882A5 JP2009539882A5 (enExample) 2010-07-29
JP5254961B2 true JP5254961B2 (ja) 2013-08-07

Family

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Family Applications (1)

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JP2009514564A Expired - Fee Related JP5254961B2 (ja) 2006-06-09 2007-06-11 ベータアゴニスト活性を有するフェニル置換ピラジノイルグアニジンナトリウムチャネル遮断薬

Country Status (12)

Country Link
US (1) US8163758B2 (enExample)
EP (1) EP2035004B1 (enExample)
JP (1) JP5254961B2 (enExample)
AU (1) AU2007257781B2 (enExample)
CA (1) CA2654244A1 (enExample)
DK (1) DK2035004T3 (enExample)
ES (1) ES2392999T3 (enExample)
NO (1) NO20085128L (enExample)
PL (1) PL2035004T3 (enExample)
PT (1) PT2035004E (enExample)
SI (1) SI2035004T1 (enExample)
WO (1) WO2007146869A1 (enExample)

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US6858615B2 (en) 2002-02-19 2005-02-22 Parion Sciences, Inc. Phenyl guanidine sodium channel blockers
AU2004266704B2 (en) 2003-08-18 2012-02-23 Parion Sciences, Inc. Capped pyrazinoylguanidine sodium channel blockers
US7807834B2 (en) 2005-08-03 2010-10-05 Parion Sciences, Inc. Capped pyrazinoylguanidine sodium channel blockers
KR100901664B1 (ko) 2007-08-06 2009-06-09 주식회사 오스코텍 β-아미노알콜 유도체, 이의 제조방법 및 이를유효성분으로 함유하는 ＴＮＦ-α 매개성 질환의 예방 및치료용 약학적 조성물
DE102007040615A1 (de) * 2007-08-27 2009-03-05 Bitop Ag Osmolyte zur Behandlung von allergisch oder viral bedingten Atemwegserkrankungen
WO2009049159A1 (en) 2007-10-10 2009-04-16 Parion Sciences, Inc. Delivering osmolytes by nasal cannula
DE102007052380A1 (de) * 2007-10-31 2009-05-07 Bitop Ag Osmolythaltige Zubereitungen zur Anwendung bei trockenen Schleimhäuten
WO2009139948A1 (en) * 2008-02-26 2009-11-19 Johnson Michael R Poly aromatic sodium channel blockers
WO2011143106A1 (en) 2010-05-10 2011-11-17 Gilead Sciences, Inc. Bi - functional pyrazolopyridine compounds
US8394829B2 (en) 2010-05-10 2013-03-12 Gilead Sciences, Inc. Bi-functional quinoline analogs
WO2012032546A2 (en) * 2010-09-08 2012-03-15 Cadila Healthcare Limited Process for the preparation of salmeterol and its intermediates
DE102011103347B4 (de) * 2011-05-27 2014-10-30 Meda Pharma Gmbh & Co. Kg Nasale pharmazeutische Formulierung
EP2717855A4 (en) 2011-06-07 2014-11-12 Parion Sciences Inc Methods of Treatment
US8945605B2 (en) 2011-06-07 2015-02-03 Parion Sciences, Inc. Aerosol delivery systems, compositions and methods
SI2723176T1 (sl) 2011-06-27 2017-09-29 Parion Sciences, Inc. Kemijsko in metabolno stabilni dipeptid, ki ima močno aktivnost blokiranja natrijevega kanala
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
WO2013181232A2 (en) 2012-05-29 2013-12-05 Michael Ross Johnson Dendrimer like amino amides possessing sodium channel blocker activity for the treatment of dry eye and other mucosal diseases
RU2671976C2 (ru) 2012-12-17 2018-11-08 Пэрион Сайенсиз, Инк. Соединения 3,5-диамино-6-хлор-n-(n-(4-фенилбутил)карбамимидоил)пиразин-2-карбоксамида
ES2674665T3 (es) * 2012-12-17 2018-07-03 Parion Sciences, Inc. Compuestos de 3,5-diamino-6-cloro-N-(N-(4-fenilbutilo)carbamimidoilo)-pirazina-2-carboxamida
HUE032891T2 (hu) * 2012-12-17 2017-11-28 Parion Sciences Inc Klórpirazin-karboxamid-származékok nem kielégítõ nyálkahártya-hidratáció által elõsegített megbetegedések kezelésére
SG11201601291QA (en) 2013-08-23 2016-03-30 Parion Sciences Inc Dithiol mucolytic agents
US9102633B2 (en) 2013-12-13 2015-08-11 Parion Sciences, Inc. Arylalkyl- and aryloxyalkyl-substituted epithelial sodium channel blocking compounds
GB201406225D0 (en) * 2014-04-07 2014-05-21 Hall Roderick L Treatment for respiratory disease
US20150376145A1 (en) 2014-06-30 2015-12-31 Parion Sciences, Inc. Stable sodium channel blockers
BR112017016067A2 (pt) 2015-01-30 2018-04-03 Parion Sciences Inc agentes mucolíticos de monotiol
JP2018520986A (ja) 2015-04-30 2018-08-02 パリオン・サイエンシィズ・インコーポレーテッド ジチオール粘液溶解剤の新規なプロドラッグ

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US20070021439A1 (en) * 2005-07-25 2007-01-25 Parion Sciences, Inc. Methods of reducing risk of infection from pathogens with soluble amide and ester pyrazinoylguanidine sodium channel blockers
US7807834B2 (en) 2005-08-03 2010-10-05 Parion Sciences, Inc. Capped pyrazinoylguanidine sodium channel blockers
AU2007294547A1 (en) 2006-09-07 2008-03-13 Parion Sciences, Inc. Methods of enhancing mucosal hydration and mucosal clearance by treatment with sodium channel blockers and osmolytes
WO2008124496A1 (en) 2007-04-03 2008-10-16 Parion Sciences, Inc. Method of treating acid-sensing ion channel mediated pain, cough, and central nervous system disorders
US8288391B2 (en) 2007-04-03 2012-10-16 Parion Sciences, Inc. Pyrazinoylguanidine compounds for use as taste modulators

Also Published As

Publication number Publication date
NO20085128L (no) 2009-02-18
ES2392999T3 (es) 2012-12-17
EP2035004B1 (en) 2012-08-08
PL2035004T3 (pl) 2013-01-31
AU2007257781A1 (en) 2007-12-21
PT2035004E (pt) 2012-11-21
US8163758B2 (en) 2012-04-24
EP2035004A1 (en) 2009-03-18
US20110008268A1 (en) 2011-01-13
AU2007257781B2 (en) 2012-11-22
SI2035004T1 (sl) 2012-12-31
CA2654244A1 (en) 2007-12-21
EP2035004A4 (en) 2010-06-30
DK2035004T3 (en) 2013-01-02
WO2007146869A1 (en) 2007-12-21
JP2009539882A (ja) 2009-11-19

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