HU229403B1 - Novel sulfamides and their use as endothelin receptor antagonists - Google Patents

Novel sulfamides and their use as endothelin receptor antagonists Download PDF

Info

Publication number
HU229403B1
HU229403B1 HU0301654A HUP0301654A HU229403B1 HU 229403 B1 HU229403 B1 HU 229403B1 HU 0301654 A HU0301654 A HU 0301654A HU P0301654 A HUP0301654 A HU P0301654A HU 229403 B1 HU229403 B1 HU 229403B1
Authority
HU
Hungary
Prior art keywords
formula
amide
acid
bromo
ethoxy
Prior art date
Application number
HU0301654A
Other languages
English (en)
Hungarian (hu)
Inventor
Martin Bolli
Christoph Boss
Walter Fischli
Martine Clozel
Thomas Weller
Original Assignee
Actelion Pharmaceuticals Ltd
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=8164206&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HU229403(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Actelion Pharmaceuticals Ltd filed Critical Actelion Pharmaceuticals Ltd
Publication of HUP0301654A2 publication Critical patent/HUP0301654A2/hu
Publication of HUP0301654A3 publication Critical patent/HUP0301654A3/hu
Publication of HU229403B1 publication Critical patent/HU229403B1/hu

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • A61P1/04—Drugs 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
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P35/00—Antineoplastic 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/56—One oxygen atom and one sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/60—Three or more oxygen or sulfur atoms
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
HU0301654A 2000-12-18 2001-12-04 Novel sulfamides and their use as endothelin receptor antagonists HU229403B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP0012890 2000-12-18
PCT/EP2001/014182 WO2002053557A1 (en) 2000-12-18 2001-12-04 Novel sulfamides and their use as endothelin receptor antagonists

Publications (3)

Publication Number Publication Date
HUP0301654A2 HUP0301654A2 (en) 2007-03-28
HUP0301654A3 HUP0301654A3 (en) 2007-08-28
HU229403B1 true HU229403B1 (en) 2013-12-30

Family

ID=8164206

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0301654A HU229403B1 (en) 2000-12-18 2001-12-04 Novel sulfamides and their use as endothelin receptor antagonists

Country Status (27)

Country Link
US (2) US7094781B2 (oth)
EP (2) EP1345920B1 (oth)
JP (1) JP4245130B2 (oth)
KR (1) KR100819668B1 (oth)
CN (1) CN100432070C (oth)
AR (1) AR035610A1 (oth)
AT (1) ATE323079T1 (oth)
AU (1) AU2002227984B8 (oth)
BE (1) BE2014C019I2 (oth)
BR (1) BRPI0116237B8 (oth)
CA (1) CA2431675C (oth)
CY (2) CY1105060T1 (oth)
DE (1) DE60118782T2 (oth)
DK (1) DK1345920T3 (oth)
ES (1) ES2260318T3 (oth)
FR (1) FR14C0017I2 (oth)
HU (1) HU229403B1 (oth)
IL (2) IL155805A0 (oth)
LU (1) LU92381I2 (oth)
MX (1) MXPA03004780A (oth)
MY (1) MY129150A (oth)
NL (1) NL300672I2 (oth)
NO (2) NO324952B1 (oth)
NZ (1) NZ525614A (oth)
PT (1) PT1345920E (oth)
WO (1) WO2002053557A1 (oth)
ZA (1) ZA200303695B (oth)

Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2002227984B8 (en) * 2000-12-18 2007-01-04 Actelion Pharmaceuticals Ltd. Novel sulfamides and their use as endothelin receptor antagonists
WO2003049739A1 (en) * 2001-12-07 2003-06-19 Vertex Pharmaceuticals, Inc. Pyrimidine-based compounds useful as gsk-3 inhibitors
EP1569914B1 (en) 2002-12-02 2009-02-18 Actelion Pharmaceuticals Ltd. Pyrimidine-sulfamides and their use as endothelian receptor antagonist
ES2548022T3 (es) 2004-03-05 2015-10-13 F. Hoffmann-La Roche Ag Diaminopirimidinas como antagonistas de P2X3 y P2X2/3
UA90269C2 (ru) 2004-04-02 2010-04-26 Мицубиси Танабе Фарма Корпорейшн Тетрагидрохинолиновые производные и способ их получения
TW200628467A (en) * 2004-11-11 2006-08-16 Actelion Pharmaceuticals Ltd Novel sulfamides
DK1913015T3 (en) 2005-07-29 2014-03-10 Janssen R & D Ireland Macrocyclic inhibitors of hepatitis C virus
ME01318B (me) 2005-07-29 2013-12-20 Tibotec Pharm Ltd Makrociklički inhibitori virusa hepatitisa C
ES2562056T3 (es) 2005-09-01 2016-03-02 F. Hoffmann-La Roche Ag Diaminopirimidinas como moduladores P2X3 y P2X2/3
BRPI0615613A2 (pt) 2005-09-01 2009-05-19 Hoffmann La Roche diaminopirimidinas como moduladores de p2x3 e p3x2/3
EP1924564B1 (en) * 2005-09-01 2016-11-09 F.Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
CN101262847B (zh) * 2005-09-12 2010-11-24 埃科特莱茵药品有限公司 包含嘧啶-磺酰胺的稳定性医药组合物
AR062501A1 (es) 2006-08-29 2008-11-12 Actelion Pharmaceuticals Ltd Composiciones terapeuticas
US7983024B2 (en) 2007-04-24 2011-07-19 Littelfuse, Inc. Fuse card system for automotive circuit protection
MX2010001837A (es) * 2007-08-17 2010-03-10 Actelion Pharmaceuticals Ltd Derivados de 4-pirimidinasulfamida.
US20100222347A1 (en) 2007-09-27 2010-09-02 Kowa Company, Ltd. Prophylactic and/or therapeutic agent for anemia, comprising tetrahydroquinoline compound as active ingredient
ES2446303T3 (es) * 2008-02-20 2014-03-07 Actelion Pharmaceuticals Ltd. Combinación que comprende paclitaxel para el tratamiento del cáncer de ovarios
BR122019015876B8 (pt) * 2008-07-08 2021-07-27 Incyte Holdings Corp compostos derivados de 1,2,5-oxadiazóis, composição, bem como seus usos
HUE036071T2 (hu) * 2008-08-13 2018-06-28 Actelion Pharmaceuticals Ltd Macitentánt tartalmazó terápiás készítmények
EP2415764A4 (en) 2009-03-31 2012-08-08 Kowa Co PROPHYLACTIC AND / OR THERAPEUTIC AGENT AGAINST ANEMIA WITH A TETRAHYDROCHINOLINE COMPOUND AS AN ACTIVE SUBSTANCE
ES2543280T3 (es) 2009-08-10 2015-08-17 Board Of Regents, The University Of Texas System Tratamiento de metástasis cerebrales con inhibidores de los receptores de endotelina en combinación con un agente quimioterapéutico citotóxico
BR112012003637A2 (pt) 2009-08-17 2017-04-25 Memorial Sloan Kettering Cancer Center "compostos de ligação de proteína de choque térmico, composições, e métodos para preparar e usar os mesmos"
WO2011078143A1 (ja) * 2009-12-22 2011-06-30 塩野義製薬株式会社 ピリミジン誘導体およびそれらを含有する医薬組成物
EP2670405B1 (en) * 2011-02-04 2015-09-02 Actelion Pharmaceuticals Ltd. Combinations comprising macitentan for the treatment of glioblastoma multiforme
EP2970116A1 (en) * 2013-03-15 2016-01-20 F. Hoffmann-La Roche AG ARYL SULFAMIDE AND SULFAMATE DERIVATIVES AS RORc MODULATORS
AR095727A1 (es) * 2013-03-27 2015-11-04 Actelion Pharmaceuticals Ltd Preparación de intermediarios de pirimidina
DE14721256T1 (de) 2013-04-22 2017-03-16 Sandoz Ag Pharmazeutische zusammensetzungen mit kristallinem macitentan
CN105693624B (zh) * 2013-06-14 2018-05-18 杭州普晒医药科技有限公司 马西替坦晶体及其制备方法、其药物组合物和用途
AR096865A1 (es) * 2013-07-12 2016-02-03 Actelion Pharmaceuticals Ltd Proceso para la preparación de un intermediario de pirimidina
CN103724281A (zh) * 2013-12-03 2014-04-16 镇江圣安医药有限公司 N-[5-（4-溴苯基）-6-[2-[（5-溴-2-嘧啶基）氧基]乙氧基]-4-嘧啶基]-n′-丙基磺酰胺的新型衍生物及其应用
EP2907811A1 (en) * 2014-02-14 2015-08-19 Actelion Pharmaceuticals Ltd. Process for manufacturing pyrimidine sulfamide derivatives
CN103819411A (zh) * 2014-03-14 2014-05-28 成都克莱蒙医药科技有限公司 一种马西替坦中间体新的制备方法
EA201692155A1 (ru) 2014-05-13 2017-04-28 Мемориал Слоун-Кеттеринг Кэнсэ Сентр МОДУЛЯТОРЫ Hsp70 И СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ
WO2016009322A1 (en) * 2014-07-15 2016-01-21 Sifavitor S.R.L. Amorphous form and new crystalline forms of macitentan
CN104447572A (zh) * 2014-12-15 2015-03-25 南京艾德凯腾生物医药有限责任公司 一种马西替坦的制备方法
WO2016203489A1 (en) 2015-06-15 2016-12-22 Megafine Pharma (P) Ltd. Process for the preparation of macitentan and intermediates thereof
ZA201605808B (en) 2015-08-26 2017-08-30 Cipla Ltd Process for preparing an endothelin receptor antagonist
CN105388244B (zh) * 2015-12-10 2017-03-08 合肥久诺医药科技有限公司 一种马西替坦有关物质的高效液相色谱分析方法
CN105461639B (zh) * 2015-12-10 2018-03-09 合肥久诺医药科技有限公司 一种高纯度马西替坦的精制方法
WO2017191565A1 (en) * 2016-05-04 2017-11-09 Shilpa Medicare Limited Process for preparation of macitentan
CN107868055B (zh) * 2016-09-28 2020-02-07 普济生物科技（台州）有限公司 一种马西替坦的制备方法
CN106478522A (zh) * 2016-10-11 2017-03-08 合肥久诺医药科技有限公司 一种马西替坦杂质标准品的制备方法
CN106478520B (zh) * 2016-10-11 2018-09-11 合肥久诺医药科技有限公司 一种马西替坦杂质标准品的合成方法
MY199557A (en) 2017-02-27 2023-11-07 Idorsia Pharmaceuticals Ltd Combinations of a 4-pyrimidinesulfamide derivative with active ingredients for the treatment of endothelin related diseases
WO2018185013A1 (en) 2017-04-03 2018-10-11 Syngenta Participations Ag Microbiocidal oxadiazole derivatives
CN107141238A (zh) * 2017-06-16 2017-09-08 吴宁怡 一种马西替坦中间体的制备方法
US11319305B2 (en) * 2017-11-21 2022-05-03 Shijiazhuang Sagacity New Drug Development Co., Ltd. Pyrimidine sulfamide derivative and preparation method and medical application thereof
IL274943B2 (en) 2017-11-30 2025-04-01 Idorsia Pharmaceuticals Ltd Combination of a 4-pyrimidinsulfamide derivative with an SGLT-2 inhibitor for the treatment of endothelin-related diseases
CN108653292B (zh) * 2018-07-03 2019-05-24 中国人民解放军总医院 一种化合物在治疗或预防高原病中的用途
CN108997223B (zh) * 2018-08-09 2020-06-30 浙江先锋科技股份有限公司 5-(4-溴苯基)-4，6-二氯嘧啶的制备方法
CN109232546B (zh) 2018-09-25 2020-09-04 中国人民解放军总医院 一种嘧啶磺酰胺类衍生物的医药用途
PT3897646T (pt) 2018-12-21 2024-07-08 Actelion Pharmaceuticals Ltd Macitentano para tratamento de hipertensão arterial pulmonar
TW202042818A (zh) 2019-01-25 2020-12-01 瑞士商艾克泰聯製藥有限公司 用於治療慢性血栓性肺高血壓之醫藥組成物
TW202103703A (zh) 2019-04-05 2021-02-01 瑞士商艾克泰聯製藥有限公司 用於治療門脈肺高血壓之方法
CN113874364B (zh) 2019-05-22 2024-04-05 无锡智康弘义生物科技有限公司 一种嘧啶磺酰胺类化合物的晶型及其制备方法
WO2021005478A1 (en) 2019-07-05 2021-01-14 TECNIMEDE - Sociedade Técnico-medicinal, SA Compressed macitentan compositions, methods and uses thereof
BR112022010311A2 (pt) 2019-11-29 2022-08-16 Actelion Pharmaceuticals Ltd Métodos de tratamento de hipertensão arterial pulmonar
TW202317119A (zh) 2021-06-11 2023-05-01 瑞士商艾克泰聯製藥有限公司 用於口服投予之分散錠
EP4154873A1 (en) 2021-09-22 2023-03-29 Sanovel Ilac Sanayi Ve Ticaret A.S. The tablet comprising macitentan
WO2023227490A1 (en) 2022-05-22 2023-11-30 Idorsia Pharmaceuticals Ltd Aprocitentan for the treatment of hypertension
US20250340520A1 (en) 2022-05-25 2025-11-06 Idorsia Pharmaceuticals Ltd Crystalline forms of sodium (5-(4-bromophenyl)-6-(2-((5-bromopyrimidin-2-yl)oxy)ethoxy)pyrimidin-4-yl)(sulfamoyl)amide
WO2024099953A1 (en) 2022-11-07 2024-05-16 Actelion Pharmaceuticals Ltd Combination of macitentan and tadalafil for the treatment of pulmonary arterial hypertension
WO2025102245A1 (zh) * 2023-11-14 2025-05-22 浙江天宇药业股份有限公司 一种双重内皮素受体拮抗剂阿普昔腾坦的合成方法

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2801584A1 (de) * 1978-01-14 1979-07-19 Bayer Ag Halogensubstituierte pyrimidin (2)yl-thiono-thiol-phosphor(phosphon)- saeureester, verfahren zu ihrer herstellung und ihre verwendung als insektizide und akarizide
US5132373A (en) * 1990-08-13 1992-07-21 General Electric Company Ortho ester-capped polyphenylene ethers and copolymers prepared therefrom
RU2086544C1 (ru) 1991-06-13 1997-08-10 Хоффманн-Ля Рош АГ Бензолсульфонамидные производные пиримидина или их соли, фармацевтическая композиция для лечения заболеваний, связанных с активностью эндотелина
US5324796A (en) * 1992-12-02 1994-06-28 General Electric Company Polyarylene sulfide and epoxy-functionalized siloxane blends
TW394761B (en) 1993-06-28 2000-06-21 Hoffmann La Roche Novel Sulfonylamino Pyrimidines
US5523204A (en) 1993-12-10 1996-06-04 Becton Dickinson And Company Detection of nucleic acids in cells by strand displacement amplification
WO1996016963A1 (de) * 1994-11-25 1996-06-06 F. Hoffmann-La Roche Ag Sulfonamide und deren verwendung als heilmittel
TW313568B (oth) * 1994-12-20 1997-08-21 Hoffmann La Roche
US5739333A (en) * 1995-05-16 1998-04-14 Tanabe Seiyaku Co., Ltd. Sulfonamide derivative and process for preparing the same
CN1102580C (zh) 1995-12-20 2003-03-05 山之内制药株式会社 芳基乙烯基磺酰胺衍生物及其医药组合物
TWI284642B (en) * 1999-01-18 2007-08-01 Hoffmann La Roche Novel heterocyclic sulfonamides
ATE380180T1 (de) * 1999-09-03 2007-12-15 Actelion Pharmaceuticals Ltd Bis-sulfonamiden
CA2389479A1 (en) 1999-12-22 2001-06-28 Christoph Boss Butyne diol derivatives
WO2001081335A1 (en) 2000-04-20 2001-11-01 Actelion Pharmaceuticals Ltd Pyrimidine-sulfonamides having endothelin-antagonist activity
AU2001265871A1 (en) * 2000-04-25 2001-11-07 Actelion Pharmaceuticals Ltd Substituted sulfonylaminopyrimidines
AU2002227984B8 (en) * 2000-12-18 2007-01-04 Actelion Pharmaceuticals Ltd. Novel sulfamides and their use as endothelin receptor antagonists

Also Published As

Publication number Publication date
HUP0301654A3 (en) 2007-08-28
ATE323079T1 (de) 2006-04-15
CY1105060T1 (el) 2010-03-03
NO20032699L (no) 2003-06-13
DK1345920T3 (da) 2006-08-14
NO20032699D0 (no) 2003-06-13
BE2014C019I2 (oth) 2021-01-29
JP2004517855A (ja) 2004-06-17
MXPA03004780A (es) 2004-05-21
EP1693372A1 (en) 2006-08-23
BRPI0116237B8 (pt) 2021-05-25
LU92381I2 (fr) 2014-04-28
CY2014017I1 (el) 2015-12-09
IL155805A0 (en) 2003-12-23
IL155805A (en) 2009-02-11
WO2002053557A1 (en) 2002-07-11
PT1345920E (pt) 2006-08-31
JP4245130B2 (ja) 2009-03-25
CA2431675C (en) 2011-11-08
US7094781B2 (en) 2006-08-22
BRPI0116237B1 (pt) 2016-08-09
CY2014017I2 (el) 2015-12-09
KR100819668B1 (ko) 2008-04-04
AU2002227984B2 (en) 2006-12-07
US20040077670A1 (en) 2004-04-22
ZA200303695B (en) 2004-08-13
BR0116237A (pt) 2003-09-30
AU2002227984A1 (en) 2002-07-16
AU2002227984B8 (en) 2007-01-04
AR035610A1 (es) 2004-06-16
FR14C0017I2 (fr) 2014-11-14
NO324952B1 (no) 2008-01-14
EP1345920B1 (en) 2006-04-12
ES2260318T3 (es) 2006-11-01
NL300672I2 (oth) 2016-10-11
DE60118782T2 (de) 2007-01-25
EP1345920A1 (en) 2003-09-24
DE60118782D1 (de) 2006-05-24
CN1524079A (zh) 2004-08-25
CA2431675A1 (en) 2002-07-11
NZ525614A (en) 2005-03-24
CN100432070C (zh) 2008-11-12
NO2014014I2 (no) 2015-08-31
MY129150A (en) 2007-03-30
KR20030066713A (ko) 2003-08-09
US20060178365A1 (en) 2006-08-10
FR14C0017I1 (oth) 2021-08-27
US7285549B2 (en) 2007-10-23
HUP0301654A2 (en) 2007-03-28

Similar Documents

Publication Publication Date Title
HU229403B1 (en) Novel sulfamides and their use as endothelin receptor antagonists
IL101650A (en) Use of sulphonamides for the manufacture of pharmaceutical compositions certain such novel compounds and their preparation
US6596719B1 (en) 6 alkoxy-4-pyrimidinyl bis-sulfonamides
KR101063042B1 (ko) 피리미딘-설파마이드 및 엔도텔린 수용체 길항제로서이들의 용도
KR100835770B1 (ko) 엔도텔린 길항 활성을 갖는 아릴알칸-설폰아마이드
AU2002212171A1 (en) Arylalkane-sulfonamides having endothelin-antagonist activity
KR101285463B1 (ko) 신규한 설파마이드
HUP0204168A2 (hu) Butin-diol-származékok, ilyeneket tartalmazó gyógyszerkészítmény és előállítása
EP1322624B1 (en) Arylalkane-sulfonamides having endothelin-antagonist activity
EP1465875B1 (en) Novel alkansulfonamides as endothelin antagonists

Legal Events

Date Code Title Description
FH91 Appointment of a representative

Free format text: FORMER REPRESENTATIVE(S): DR. JALSOVSZKY GYOERGYNE UEGYVED, HU

Representative=s name: DANUBIA SZABADALMI ES JOGI IRODA KFT., HU

FH92 Termination of representative

Representative=s name: DR. JALSOVSZKY GYOERGYNE UEGYVED, HU

AA1S Information on application for a supplementary protection certificate

Free format text: PRODUCT NAME: MACITENTAN; REG. NO/DATE: EU/1/13/893 20131220

Spc suppl protection certif: S1400010

Filing date: 20140305

Expiry date: 20211204

FG4S Grant of supplementary protection certificate

Free format text: PRODUCT NAME: MACITENTAN; REGISTRATION NO/DATE: EU/1/13/893 20131220

Spc suppl protection certif: S1400010

Filing date: 20140305

Expiry date: 20211204

Extension date: 20261204