CY1111578T1 - Σουλφαμιδες ως antαγωνιστες του υποδοχεα ενδοθηλινης για τη θεραπεια καρδιαγγειακων νοσων - Google Patents

Σουλφαμιδες ως antαγωνιστες του υποδοχεα ενδοθηλινης για τη θεραπεια καρδιαγγειακων νοσων

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Publication number
CY1111578T1
CY1111578T1 CY20111100575T CY111100575T CY1111578T1 CY 1111578 T1 CY1111578 T1 CY 1111578T1 CY 20111100575 T CY20111100575 T CY 20111100575T CY 111100575 T CY111100575 T CY 111100575T CY 1111578 T1 CY1111578 T1 CY 1111578T1
Authority
CY
Cyprus
Prior art keywords
antagonists
sulfamides
cardiovascular disease
enantiomers
disease therapy
Prior art date
Application number
CY20111100575T
Other languages
English (en)
Inventor
Christoph Boss
Walter Fischli
Thomas Weller
Martine Clozel
Martin Bolli
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
Application filed by Actelion Pharmaceuticals Ltd. filed Critical Actelion Pharmaceuticals Ltd.
Publication of CY1111578T1 publication Critical patent/CY1111578T1/el

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    • 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
    • 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
    • A61P1/04—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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
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    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P35/00—Antineoplastic agents
    • 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
    • A61P37/02—Immunomodulators
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Emergency Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Gynecology & Obstetrics (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Η εφεύρεση σχετίζεται με νέα αμίδια σουλφαμικού οξέος και με τη χρήση τους ως δραστικά συστατικά στην παρασκευή φαρμακευτικών συνθέσεων. Η εφεύρεση αφορά επίσης σε σχετικές απόψεις που περιλαμβάνουν φαρμακευτικές συνθέσεις οι οποίες περιέχουν μια ή περισσότερες από αυτές τις ενώσεις και ιδίως τη χρήση τους ως ανταγωνιστές υποδοχέα ενδοθηλίνης. Στον γενικό χημικό τύπο (I), το R1 αντιπροσωπεύει τα -CH(OH)-CH3, -CH2-CH2OH, -CH2COOH, -CH2-CH2-CH2OH, -CH2-CH2-COOH ˙ το R2 αντιπροσωπεύει τα 4-βρωμοφαινυλ, 4-χλωροφαινυλ, 4-μεθυλφαινυλ, 2-μεθοξυφαινοξυ, 3-μεθοξυφαινοξυ, 2-χλωρο-5-μεθοξυ-φαινοξυ ˙ το R3 αντιπροσωπεύει το βρώμιο ή το χλώριο ˙ και οπτικά καθαρά εναντιομερή, μείγματα εναντιομερών όπως είναι τα ρακεμικά, και φαρμακευτικά αποδεκτά άλατα αυτών.
CY20111100575T 2004-11-11 2011-06-16 Σουλφαμιδες ως antαγωνιστες του υποδοχεα ενδοθηλινης για τη θεραπεια καρδιαγγειακων νοσων CY1111578T1 (el)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP2004012774 2004-11-11
EP05802290A EP1833821B1 (en) 2004-11-11 2005-11-11 Sulfamides as endothelin receptor antagonists for the treatment of cardiovascular diseases

Publications (1)

Publication Number Publication Date
CY1111578T1 true CY1111578T1 (el) 2015-10-07

Family

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Family Applications (1)

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CY20111100575T CY1111578T1 (el) 2004-11-11 2011-06-16 Σουλφαμιδες ως antαγωνιστες του υποδοχεα ενδοθηλινης για τη θεραπεια καρδιαγγειακων νοσων

Country Status (21)

Country Link
US (1) US7868012B2 (el)
EP (1) EP1833821B1 (el)
JP (1) JP5020089B2 (el)
KR (1) KR101285463B1 (el)
CN (1) CN101056872A (el)
AR (1) AR051764A1 (el)
AT (1) ATE503752T1 (el)
AU (1) AU2005303435A1 (el)
BR (1) BRPI0517565A (el)
CA (1) CA2586106C (el)
CY (1) CY1111578T1 (el)
DE (1) DE602005027251D1 (el)
DK (1) DK1833821T3 (el)
ES (1) ES2362103T3 (el)
MX (1) MX2007005566A (el)
PL (1) PL1833821T3 (el)
PT (1) PT1833821E (el)
RU (1) RU2007121842A (el)
SI (1) SI1833821T1 (el)
TW (1) TW200628467A (el)
WO (1) WO2006051502A2 (el)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100035865A1 (en) * 2007-04-03 2010-02-11 Pfizer Inc Sulfonamides and Pharmaceutical Compositions Thereof
TWI446911B (zh) * 2008-08-13 2014-08-01 Actelion Pharmaceuticals Ltd 含美西特田（ｍａｃｉｔｅｎｔａｎ）之治療組合物
AR095727A1 (es) * 2013-03-27 2015-11-04 Actelion Pharmaceuticals Ltd Preparación de intermediarios de pirimidina
US9899745B2 (en) 2013-09-13 2018-02-20 Raytheon Company Low profile high efficiency multi-band reflector antennas
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
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
HRP20230318T1 (hr) 2017-11-21 2023-05-12 Wuxi Biocity Biopharmaceutics Co., Ltd. Derivat pirimidin sulfamida, postupak pripreme i njegova medicinska primjena
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

Family Cites Families (9)

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Publication number Priority date Publication date Assignee Title
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
TW394761B (en) 1993-06-28 2000-06-21 Hoffmann La Roche Novel Sulfonylamino Pyrimidines
IL111959A (en) 1993-12-17 2000-07-16 Tanabe Seiyaku Co N-(polysubstituted pyrimidin-4-yl) benzenesulfonamide derivatives their preparation and pharmaceutical compositions containing them
TW313568B (el) 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
JPH10226649A (ja) * 1996-12-12 1998-08-25 Tanabe Seiyaku Co Ltd 医薬組成物
NZ525614A (en) 2000-12-18 2005-03-24 Actelion Pharmaceuticals Ltd Novel sulfamides and their use as endothelin receptor antagonists
RU2329255C2 (ru) 2002-12-02 2008-07-20 Актелион Фармасьютиклз Лтд Пиримидинсульфамиды и их использование в качестве антагонистов эндотелиальных рецепторов

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Publication number Publication date
US20080004298A1 (en) 2008-01-03
DE602005027251D1 (de) 2011-05-12
CA2586106A1 (en) 2006-05-18
CN101056872A (zh) 2007-10-17
WO2006051502A2 (en) 2006-05-18
ATE503752T1 (de) 2011-04-15
MX2007005566A (es) 2007-05-21
KR101285463B1 (ko) 2013-07-12
WO2006051502A3 (en) 2006-09-08
JP2008519826A (ja) 2008-06-12
PL1833821T3 (pl) 2011-09-30
KR20070085787A (ko) 2007-08-27
TW200628467A (en) 2006-08-16
US7868012B2 (en) 2011-01-11
AU2005303435A1 (en) 2006-05-18
SI1833821T1 (sl) 2011-07-29
EP1833821A2 (en) 2007-09-19
JP5020089B2 (ja) 2012-09-05
BRPI0517565A (pt) 2008-10-14
AR051764A1 (es) 2007-02-07
DK1833821T3 (da) 2011-06-06
ES2362103T3 (es) 2011-06-28
RU2007121842A (ru) 2008-12-20
PT1833821E (pt) 2011-06-06
EP1833821B1 (en) 2011-03-30
CA2586106C (en) 2014-01-21

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