HK1068609A1 - Sodium channel blockers - Google Patents

Sodium channel blockers

Info

Publication number
HK1068609A1
HK1068609A1 HK04110387A HK04110387A HK1068609A1 HK 1068609 A1 HK1068609 A1 HK 1068609A1 HK 04110387 A HK04110387 A HK 04110387A HK 04110387 A HK04110387 A HK 04110387A HK 1068609 A1 HK1068609 A1 HK 1068609A1
Authority
HK
Hong Kong
Prior art keywords
sodium channel
channel blockers
sup
formula
compounds
Prior art date
Application number
HK04110387A
Other languages
English (en)
Inventor
Michael R Johnson
Original Assignee
Parion Sciences Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Parion Sciences Inc filed Critical Parion Sciences Inc
Publication of HK1068609A1 publication Critical patent/HK1068609A1/xx

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10Laxatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/12Mucolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic 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
    • C07D241/14Heterocyclic 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
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26Carbon 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
HK04110387A 2002-02-19 2004-12-31 Sodium channel blockers HK1068609A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US10/076,551 US6858614B2 (en) 2002-02-19 2002-02-19 Phenolic guanidine sodium channel blockers
PCT/US2003/004823 WO2003070184A2 (en) 2002-02-19 2003-02-19 Sodium channel blockers

Publications (1)

Publication Number Publication Date
HK1068609A1 true HK1068609A1 (en) 2005-04-29

Family

ID=27752676

Family Applications (1)

Application Number Title Priority Date Filing Date
HK04110387A HK1068609A1 (en) 2002-02-19 2004-12-31 Sodium channel blockers

Country Status (14)

Country Link
US (6) US6858614B2 (xx)
EP (1) EP1485359B1 (xx)
JP (1) JP2005526726A (xx)
KR (1) KR20040091065A (xx)
AT (1) ATE380181T1 (xx)
AU (1) AU2003215286A1 (xx)
CA (1) CA2476837A1 (xx)
CY (1) CY1107228T1 (xx)
DE (1) DE60317884T8 (xx)
DK (1) DK1485359T3 (xx)
ES (1) ES2298505T3 (xx)
HK (1) HK1068609A1 (xx)
PT (1) PT1485359E (xx)
WO (1) WO2003070184A2 (xx)

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6858615B2 (en) 2002-02-19 2005-02-22 Parion Sciences, Inc. Phenyl guanidine sodium channel blockers
US6858614B2 (en) * 2002-02-19 2005-02-22 Parion Sciences, Inc. Phenolic guanidine sodium channel blockers
US6903105B2 (en) * 2003-02-19 2005-06-07 Parion Sciences, Inc. Sodium channel blockers
AU2004266704B2 (en) * 2003-08-18 2012-02-23 Parion Sciences, Inc. Capped pyrazinoylguanidine sodium channel blockers
US7375107B2 (en) * 2003-08-18 2008-05-20 Parion Sciences, Inc. Alaphatic pyrazinoylguanidine sodium channel blockers
US7317013B2 (en) * 2003-08-18 2008-01-08 Parion Sciences, Inc. Cyclic pyrazinoylguanidine sodium channel blockers
US20090253714A1 (en) * 2003-08-20 2009-10-08 Johnson Michael R Methods of reducing risk of infection from pathogens
US7745442B2 (en) * 2003-08-20 2010-06-29 Parion Sciences, Inc. Methods of reducing risk of infection from pathogens
CN1882353B (zh) * 2003-11-19 2011-04-20 明治制果株式会社 催涎剂和混合该催涎剂的口腔用组合物以及食品组合物
CA2575670A1 (en) * 2004-08-18 2006-03-02 Michael R. Johnson Aliphatic amide & ester pyrazinoylguanidine sodium channel blockers
US7399766B2 (en) * 2004-08-18 2008-07-15 Parion Sciences, Inc. Soluble amide & ester pyrazinoylguanidine sodium channel blockers
AU2005277398A1 (en) 2004-08-18 2006-03-02 Michael R. Johnson Cyclic amide and ester pyrazinoylguanidine sodium channel blockers
US8569367B2 (en) * 2004-11-16 2013-10-29 Allergan, Inc. Ophthalmic compositions and methods for treating eyes
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
GB0520405D0 (en) * 2005-10-07 2005-11-16 Imp College Innovations Ltd Biological agents and method
WO2007070509A2 (en) * 2005-12-13 2007-06-21 University Of Pittsburgh-Of The Commonwealth System Of Higher Education Epithelial sodium channel inhibiting agents and uses therefor
CA2653757A1 (en) * 2006-06-09 2007-12-21 Parion Sciences, Inc. Aliphatic pyrazinoylguanidine sodium channel blockers with beta agonist activity
ES2392999T3 (es) * 2006-06-09 2012-12-17 Parion Sciences, Inc. Bloqueadores de canales de sodio pirazinoilguanidina sustituida con fenilo que tienen actividad agonista beta
CA2653773A1 (en) * 2006-06-09 2007-12-21 Parion Sciences, Inc. Cyclic substituted pyrazinoylguanidine sodium channel blockers possessing beta agonist activity
AR062741A1 (es) * 2006-09-07 2008-12-03 Hirsh Andrew J Metodo para aumentar la hidratacion de la mucosa y la evacuacion de l a mucosa mediante tratamiento con bloquadores de los canales del sodio y osmolitos
AR062742A1 (es) * 2006-09-07 2008-12-03 Johnson Michael R Hidratacion de la mucosa y depuracion de la mucosa aumentadas por tratamiento con bloquadores de canales de sodio y osmolitos
GB2447298A (en) * 2007-03-09 2008-09-10 Geraldine Carter Toothpaste containing chromium
US20080293740A1 (en) * 2007-04-03 2008-11-27 Parion Sciences, Inc. Method of treating acid-sensing ion channel mediated pain, cough suppression, and central nervous system disorders
US8288391B2 (en) * 2007-04-03 2012-10-16 Parion Sciences, Inc. Pyrazinoylguanidine compounds for use as taste modulators
AU2008310734B2 (en) 2007-10-10 2014-06-05 Parion Sciences, Inc. Delivering osmolytes by nasal cannula
AU2009246799B2 (en) * 2008-02-26 2014-02-27 Parion Sciences, Inc. Poly aromatic pyrazinoylguanidine sodium channel blockers
US20100074881A1 (en) * 2008-07-11 2010-03-25 Parion Sciences, Inc. Multiple nebulizer systems
EP2717855A4 (en) 2011-06-07 2014-11-12 Parion Sciences Inc PROCESSING METHODS
US8945605B2 (en) 2011-06-07 2015-02-03 Parion Sciences, Inc. Aerosol delivery systems, compositions and methods
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
CN103687488B (zh) 2011-06-27 2015-06-10 帕里昂科学公司 化学和代谢稳定的具有钠通道阻滞剂活性的二肽
US9907826B2 (en) 2011-12-07 2018-03-06 Allergan, Inc. Efficient lipid delivery to human tear film using a salt-sensitive emulsion system
EP2855435B1 (en) 2012-05-29 2018-04-11 Parion Sciences, Inc. Dendrimer like amino amides possessing sodium channel blocker activity for the treatment of dry eye and other mucosal diseases
MX2015007797A (es) 2012-12-17 2015-10-05 Parion Sciences Inc Compuestos de 3,5-diamino-6-cloro-n-(n-(4-fenilbutil) carbamimidoil) pirazin-2-carboxamida.
CA2895512C (en) 2012-12-17 2021-10-19 Parion Sciences, Inc. Chloro-pyrazine carboxamide derivatives useful for the treatment of diseases favoured by insufficient mucosal hydration
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
WO2015003083A1 (en) 2013-07-02 2015-01-08 The California Institute For Biomedical Research Compounds for treatment of cystic fibrosis
JP6596421B2 (ja) 2013-08-23 2019-10-23 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薬
US9102633B2 (en) 2013-12-13 2015-08-11 Parion Sciences, Inc. Arylalkyl- and aryloxyalkyl-substituted epithelial sodium channel blocking compounds
US20150376145A1 (en) 2014-06-30 2015-12-31 Parion Sciences, Inc. Stable sodium channel blockers
WO2016112120A1 (en) * 2015-01-07 2016-07-14 The California Institute For Biomedical Research Compounds for treatment of cystic fibrosis
KR20170108088A (ko) 2015-01-30 2017-09-26 패리온 사이언스 인코퍼레이티드 신규 모노티올 점액용해제
WO2016133967A2 (en) * 2015-02-18 2016-08-25 Parion Sciences, Inc. Sodium channel blockers for skin disorders
WO2016176423A1 (en) 2015-04-30 2016-11-03 Parion Sciences, Inc. Novel prodrugs of dithiol mucolytic agents
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

Family Cites Families (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US397686A (en) * 1889-02-12 Scale for surface measurements
US386401A (en) * 1888-07-17 heady
US2987091A (en) * 1957-08-08 1961-06-06 Cincinnati Mine Machinery Co Set screw construction
NL299931A (xx) 1962-10-30
DE1903999U (de) * 1964-04-02 1964-11-05 Jon Martin Jonsson Befestigungsvorrichtung fuer einen bidetzusatz an wasserklosetts.
US3472848A (en) 1966-11-17 1969-10-14 Merck & Co Inc 3-hydroxy and 3-mercapto-pyrazinoyl-guanidines,corresponding ethers and thioethers and processes for their preparation
US3625950A (en) 1968-07-03 1971-12-07 Merck & Co Inc Certain halophenoxy alkanamides, hydrazides and derivatives thereof
US3539569A (en) * 1968-08-21 1970-11-10 Merck & Co Inc Preparation of pyrazinoylguanidines from pyrazinoylureas
US3544571A (en) 1968-09-04 1970-12-01 Merck & Co Inc Process for making pyrazinoylthiourea compounds
US3668241A (en) 1968-11-25 1972-06-06 Merck & Co Inc Substituted 1-oxoinden-5-yloxy alkanoic acids
US3573306A (en) * 1969-03-05 1971-03-30 Merck & Co Inc Process for preparation of n-substituted 3,5-diamino-6-halopyrazinamides
US3684552A (en) * 1970-11-16 1972-08-15 Minnesota Mining & Mfg Heat-sensitive sheet material
US3864401A (en) 1970-12-23 1975-02-04 Merck & Co Inc Substituted 2-aminomethyl-4,6-dihalophenols
US3794734A (en) 1971-03-03 1974-02-26 Merck & Co Inc Methods of treating edema and hypertension using certain 2-aminoethylphenols
US3953476A (en) 1971-12-27 1976-04-27 Merck & Co., Inc. 3-Amino-5-sulfonylbenzoic acids
US3976686A (en) 1972-10-13 1976-08-24 Merck & Co., Inc. [1-Oxo-2,3-hydrocarbylene-5-indanyloxy(or thio)]alkanoic acids
US3984465A (en) 1972-10-13 1976-10-05 Merck & Co., Inc. 1-Oxo-2,2-disubstituted-5-indanyloxy(or thio)alkanoic acids
US4085219A (en) 1972-10-13 1978-04-18 Merck & Co., Inc. 1-Oxo-2,2-disubstituted-5-indanyloxy(or thio)alkanoic acids
US3928324A (en) * 1973-02-08 1975-12-23 Pfizer Malonyl derivatives of 6-({60 -aminoacylamido)penicillanic acids
US3987091A (en) 1973-04-12 1976-10-19 Merck & Co., Inc. 11,12-secoprostaglandins
US3894065A (en) 1973-04-27 1975-07-08 Merck & Co Inc Aryl-oxo-alkanoic acids
US4177285A (en) 1973-10-11 1979-12-04 Merck & Co., Inc. [1-Oxo-2-thienyl-2-substituted-5-indanyloxy (or thio)]alkanoic acids and derivatives thereof
US4003927A (en) 1973-10-12 1977-01-18 Merck & Co., Inc. (1-Oxo-7,8-disubstituted-1,2,3,4-tetrahydro-6-naphthyloxy)- and (3,4-disubstituted-5-oxo-6,7,8,9-tetrahydro-5H-benzocycloheptene-2-yloxy) acetic acids and derivatives
US4012524A (en) 1973-10-12 1977-03-15 Merck & Co., Inc. [1-Hydroxy-5-indanyloxy (or thio)]-alkanoic acids
US3966966A (en) 1973-10-12 1976-06-29 Merck & Co., Inc. Pharmaceutical compositions and method of treatment employing 1,3-dioxo-2,2-disubstituted indanyloxy alkanoic acids
US3929872A (en) 1973-10-12 1975-12-30 Merck & Co Inc Indanacetic acid compounds
US3976681A (en) 1973-10-12 1976-08-24 Merck & Co., Inc. [1,3-Dioxo-2-substituted and 2,2-disubstituted- indanyloxy (or thio] alkanoic acids
US4006180A (en) 1973-10-12 1977-02-01 Merck & Co., Inc. [1,3-Dihydroxy-2-substituted and 2,2-disubstituted-indanyloxy(or thio)]alkanoic acids
US3989749A (en) 1973-10-17 1976-11-02 Merck & Co., Inc. 11,12-Secoprostaglandins
US3991087A (en) 1973-12-13 1976-11-09 Merck & Co., Inc. 8-Halo-11,12-secoprostaglandins
US3979361A (en) 1974-02-20 1976-09-07 Merck & Co., Inc. 2-Aminomethyl-6-trihalo-methylphenols
US3914253A (en) 1974-03-04 1975-10-21 Merck & Co Inc 5-Oxo-6-substituted-cyclopent-{8 f{9 -indole-2-carboxylic acids
US3931239A (en) 1974-04-03 1976-01-06 Merck & Co., Inc. 6-Oxo-7-substituted-6H-indeno-[5,4-b]furan(and thiophene)-carboxylic acids
US3958004A (en) 1974-04-23 1976-05-18 Merck & Co., Inc. Phenoxyacetic acid derivatives as uricosuric agents
US3928624A (en) 1974-04-25 1975-12-23 Merck & Co Inc Phenol compounds in treating pain, fever and inflammation
US3956374A (en) 1974-05-03 1976-05-11 Merck & Co., Inc. Aryl-oxo-heptenoic acids
US3974212A (en) 1974-05-22 1976-08-10 Merck & Co., Inc. [1-Hydroximino-2,2-disubstituted-5-indanyloxy-(or thio)]alkanoic acids
US3991106A (en) 1974-09-13 1976-11-09 Merck & Co., Inc. 16-Ethers of 8-aza-9-dioxothia-11,12-seco-prostaglandins
US3984552A (en) 1975-02-24 1976-10-05 Merck & Co., Inc. 6-Oxo-7-substituted and 7,7-disubstituted-6H-indeno-[5,4-b]furan (and thiophene) carboxylic acids
US4092414A (en) 1975-04-25 1978-05-30 Merck & Co., Inc. 3,4-Dihydrospiro-2H-1,3-benzoxazines and their use in treating edema, abnormal electrolyte retention, and inflammation
US4296122A (en) 1975-07-09 1981-10-20 Merck & Co., Inc. 2,3-Dihydro-6,7-disubstituted-5-(acyl)benzofuran-2-carboxylic acids
US4087542A (en) 1975-07-09 1978-05-02 Merck & Co., Inc. 2,3-Dihydro-6,7-disubstituted-5-acyl benzofuran-2-carboxylic acids
US4181727A (en) 1975-07-09 1980-01-01 Merck & Co., Inc. 2,3-Dihydro-6,7-disubstituted-5-acyl benzofuran-2-carboxylic acids
US4100394A (en) * 1975-12-12 1978-07-11 Adams Industries, Inc. Electric water heater and hot water dispenser
US4085211A (en) 1975-12-15 1978-04-18 Merck & Co., Inc. Pyrazinecarboxamides and processes for preparing same
US4025292A (en) * 1975-12-15 1977-05-24 Bailey A Preston High pressure burner with integral pilot
US4025625A (en) 1976-06-15 1977-05-24 Merck & Co., Inc. Imidazothiazines
US4087526A (en) 1976-07-23 1978-05-02 Merck & Co., Inc. (3-Amino-5-substituted-6-fluoropyrazinoyl or pyrazamido)-guanidines and their derivatives bearing substituents on the guanidino nitrogens
US4067980A (en) 1976-08-16 1978-01-10 Merck & Co., Inc. Spirobenzoxazinium salts, method of use and compositions thereof as antihypertensive agents
US4085117A (en) 1976-10-18 1978-04-18 Merck & Co., Inc. 6,7-Disubstituted-5-(acyl)benzofuran-2-carboxylic acids
US4100294A (en) 1976-12-06 1978-07-11 Merck & Co., Inc. 5-(Hydroxy (substituted) methyl)-2,3-dihydrobenzo furan-2-carboxylic acid and its derivatives
US4105769A (en) 1977-01-24 1978-08-08 Merck & Co., Inc. Inhibition of indoleamine-N-methyl transferase by 2-iminopyridines
US4196292A (en) 1977-06-29 1980-04-01 Merck & Co., Inc. 6-Substituted amiloride derivatives
US4140776A (en) 1977-09-16 1979-02-20 Merck & Co., Inc. N-pyrazinecarbonyl-N'-acylguanidines
US4159279A (en) 1977-11-23 1979-06-26 Merck & Co., Inc. Nuclear substituted 2-hydroxyphenylmethanesulfamic acids
US4145551A (en) 1978-01-09 1979-03-20 Merck & Co., Inc. Pyrazine-2-carbonyloxyguanidines
US4401669A (en) 1978-01-27 1983-08-30 Merck & Co., Inc. 2,3-Dihydro-substituted-5-benzoyl benzofuran-2-carboxylic acids and their use in treating hypertension
US4163781A (en) 1978-04-17 1979-08-07 Merck & Co., Inc. 3-Amino-N-[(phosphonoamino)iminomethyl]-6-halopyrazinecarboxamide compounds, compositions and methods of use
US4246406A (en) 1979-03-27 1981-01-20 Merck & Co., Inc. Heterocyclic substituted pyrazinoylguanidines
US4237144A (en) 1979-06-21 1980-12-02 Merck & Co., Inc. 2,3-Dihydro-2,6,7-trisubstituted-5-acylbenzofurans
US4291050A (en) 1979-06-21 1981-09-22 Merck & Co., Inc. 6,7-Disubstituted-2 or 2,2-substituted-5-substituted-1-indanones
US4237130A (en) 1979-06-21 1980-12-02 Merck & Co., Inc. 2,3-Dihydro-6,7-disubstituted-5-(substituted sulfonyl)benzofuran-2-carboxylic acids
US4298743A (en) 1979-09-11 1981-11-03 Merck & Co., Inc. 4-(Substituted phenyl thiazolyl)-3-hydroxy-3-pyrroline-2,5-diones
US4362724A (en) 1980-05-19 1982-12-07 Merck & Co., Inc. Method of treating edema and hypertension and pharmaceutical composition therefor in which the active ingredient comprises a novel substituted pyrazinyl-1,2,4-oxadiazole and a kaliuretic diuretic
US4277602A (en) 1980-07-02 1981-07-07 Merck & Co., Inc. 3-Amino-5-substituted-6-halo-N-(3,4-dihydro-6-substituted-1,3,5-truazin-2-yl)2-pyrazinecarboxamides
US4317822A (en) 1980-07-02 1982-03-02 Merck & Co., Inc. 3-Amino-5-substituted-6-halo-N-(3,4-dihydro-6-substituted-1,3,5-triazin-2-yl)2-pyrazinecarboxamides
US6475509B1 (en) * 1999-07-19 2002-11-05 The University Of North Carolina At Chapel Hill Covalent conjugates of sodium channel blockers and active compounds
US6858615B2 (en) * 2002-02-19 2005-02-22 Parion Sciences, Inc. Phenyl guanidine sodium channel blockers
US6858614B2 (en) * 2002-02-19 2005-02-22 Parion Sciences, Inc. Phenolic guanidine sodium channel blockers
US6903105B2 (en) * 2003-02-19 2005-06-07 Parion Sciences, Inc. Sodium channel blockers

Also Published As

Publication number Publication date
EP1485359A4 (en) 2006-03-22
EP1485359A2 (en) 2004-12-15
CA2476837A1 (en) 2003-08-28
US20040198744A1 (en) 2004-10-07
US20040204424A1 (en) 2004-10-14
PT1485359E (pt) 2008-03-17
US6858614B2 (en) 2005-02-22
JP2005526726A (ja) 2005-09-08
US7368450B2 (en) 2008-05-06
DE60317884D1 (de) 2008-01-17
ATE380181T1 (de) 2007-12-15
US7192959B2 (en) 2007-03-20
US20040198746A1 (en) 2004-10-07
DE60317884T2 (de) 2009-01-02
US7247636B2 (en) 2007-07-24
KR20040091065A (ko) 2004-10-27
DK1485359T3 (da) 2008-04-14
EP1485359B1 (en) 2007-12-05
WO2003070184A3 (en) 2004-06-17
US7192958B2 (en) 2007-03-20
DE60317884T8 (de) 2009-06-04
US7241766B2 (en) 2007-07-10
ES2298505T3 (es) 2008-05-16
AU2003215286A1 (en) 2003-09-09
WO2003070184A2 (en) 2003-08-28
US20030195160A1 (en) 2003-10-16
US20040198747A1 (en) 2004-10-07
CY1107228T1 (el) 2012-11-21
US20040198745A1 (en) 2004-10-07

Similar Documents

Publication Publication Date Title
HK1068609A1 (en) Sodium channel blockers
MXPA03009604A (es) Compuestos de espiropirazol.
MXPA04001323A (es) Dihidro-3-halo-1h-pirazol-5-carboxilatos sustituidos, su preparacion y uso.
HK1069395A1 (en) Phthalazinone derivatives 2,3
PT1075259E (pt) Novos analogos gordos para o tratamento de diabetes
IL159418A0 (en) Novel compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
YU82304A (sh) Kristalni 3,4,4-trisupstituisani-piperidinil-n-alkilkarboksilati, intermedijeri i postupak za dobijanje
JO2654B1 (en) Multiple aryl caroxa amides are useful as lipid - lowering agents
YU82303A (sh) Analozi nociceptina
GB0127903D0 (en) Improvements relating to organic compounds
AU2002317829A1 (en) Photostable organic sunscreen compounds with antioxidant properties and compositions obtained therefrom
RS50229B (sr) Analozi vitamina d3
HU9904634D0 (en) New thiaazolidine-derivatives
BR0115996A (pt) Sulfamidotienopirimidinas
TR200302288T2 (tr) Terapi için yeni bileşikler ve metotlar.
NO20022977D0 (no) Substituerte homopiperidinylbenzimidazolanaloger som fundiske relaksanter
MXPA03002493A (es) Proceso eficiente para preparacion de un inhibidor del factor xa.
ZA951013B (en) Novel indane-2-mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase
MY136065A (en) Prodrugs to nmda receptor ligands
DK0779895T3 (da) Forbedret fremgangsmåde til fremstilling af sidekædederivater af cyclohexapeptidyl-lipopeptider
MY133207A (en) Substituted benzolactam compaunds
MXPA05003881A (es) Preparacion de compuestos triazospiro.
DE602004004093D1 (de) Alkylierte iminodibenzyle als antioxidationsmittel
MX9702486A (es) La fabricacion de levobupivacaina y sus analogos de l-lisina.
EA199800931A1 (ru) Способ получения ингибиторов фосфодиэстеразы iv

Legal Events

Date Code Title Description
PC Patent ceased (i.e. patent has lapsed due to the failure to pay the renewal fee)

Effective date: 20110219