ZA200606880B - Diaminopyrimidines as P2X3 and P2X2/3 antagonists - Google Patents

Diaminopyrimidines as P2X3 and P2X2/3 antagonists Download PDF

Info

Publication number
ZA200606880B
ZA200606880B ZA200606880A ZA200606880A ZA200606880B ZA 200606880 B ZA200606880 B ZA 200606880B ZA 200606880 A ZA200606880 A ZA 200606880A ZA 200606880 A ZA200606880 A ZA 200606880A ZA 200606880 B ZA200606880 B ZA 200606880B
Authority
ZA
South Africa
Prior art keywords
alkyl
hydrogen
formula
alkoxy
halo
Prior art date
Application number
ZA200606880A
Other languages
English (en)
Inventor
Carter David Scott
Hawley Ronald Charles
Parish Daniel Warren
Jahangir Alam
Dillon Michael Patrick
Lin Clara Jeou Jen
Broka Chris Allen
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of ZA200606880B publication Critical patent/ZA200606880B/en

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
    • C07D239/48—Two nitrogen atoms
    • C07D239/49—Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
    • 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
    • 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
    • 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
    • A61P1/04—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
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P13/06—Anti-spasmodics
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • 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
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • 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
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • 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
    • 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
    • C07D239/48—Two nitrogen atoms
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/12—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 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
    • C07D405/02—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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Toxicology (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
ZA200606880A 2004-03-05 2006-08-17 Diaminopyrimidines as P2X3 and P2X2/3 antagonists ZA200606880B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US55049904P 2004-03-05 2004-03-05

Publications (1)

Publication Number Publication Date
ZA200606880B true ZA200606880B (en) 2008-04-30

Family

ID=34961010

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA200606880A ZA200606880B (en) 2004-03-05 2006-08-17 Diaminopyrimidines as P2X3 and P2X2/3 antagonists

Country Status (31)

Country Link
US (12) US7858632B2 (enExample)
EP (2) EP1725540B1 (enExample)
JP (4) JP4717876B2 (enExample)
KR (1) KR100822530B1 (enExample)
CN (1) CN1930135B (enExample)
AR (1) AR047992A1 (enExample)
AU (1) AU2005229331B2 (enExample)
BE (1) BE2024C508I2 (enExample)
BR (2) BRPI0508461B8 (enExample)
CA (1) CA2557372C (enExample)
CY (2) CY1113450T1 (enExample)
DK (1) DK1725540T5 (enExample)
ES (2) ES2548022T3 (enExample)
FI (1) FIC20240007I1 (enExample)
FR (1) FR24C1011I2 (enExample)
HR (1) HRP20120901T1 (enExample)
HU (1) HUS2400005I1 (enExample)
IL (2) IL177438A (enExample)
LT (1) LTC1725540I2 (enExample)
LU (1) LUC00333I2 (enExample)
MY (1) MY145465A (enExample)
NL (1) NL301261I2 (enExample)
NO (4) NO339497B1 (enExample)
NZ (1) NZ549069A (enExample)
PL (1) PL1725540T3 (enExample)
PT (1) PT1725540E (enExample)
RU (1) RU2422441C2 (enExample)
SI (1) SI1725540T1 (enExample)
TW (1) TWI313604B (enExample)
WO (1) WO2005095359A1 (enExample)
ZA (1) ZA200606880B (enExample)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1725540E (pt) * 2004-03-05 2012-11-29 Hoffmann La Roche Diaminopirimidinas como antagonistas de p2x3 e p2x2/3
EP1814841A4 (en) * 2004-10-29 2011-03-16 Musc Found For Res Dev CERAMIDES AND LIGANDS OF SIGNALING APOPTOSIS
AU2006286576B2 (en) * 2005-09-01 2012-06-14 F. Hoffmann-La Roche Ag Diaminopyrimidines as P2X3 and P3X2/3 modulators
ES2562056T3 (es) * 2005-09-01 2016-03-02 F. Hoffmann-La Roche Ag Diaminopirimidinas como moduladores P2X3 y P2X2/3
ES2612890T3 (es) * 2005-09-01 2017-05-19 F. Hoffmann-La Roche Ag Diaminopirimidinas como moduladores de P2X3 y P2X2/3
SI1924264T1 (sl) 2005-09-01 2013-12-31 F. Hoffmann-La Roche Ag Diaminopirimidini kot modulatorji p2x3 in p2x2/3
ATE529413T1 (de) * 2005-09-01 2011-11-15 Hoffmann La Roche Verfahren zur synthese von aryloxydiaminopyrimidinen
EP1770089A1 (en) * 2005-10-03 2007-04-04 Institut Pasteur Pyranodibenzofuran derivatives with antifungal and antibacterial activity
DK2343281T3 (en) * 2006-10-04 2014-03-24 Hoffmann La Roche Process for the Synthesis of Phenoxydiamino-Pyrimidine Derivatives
JP5084839B2 (ja) * 2006-11-09 2012-11-28 エフ．ホフマン−ラ ロシュ アーゲー チアゾール及びオキサゾール置換アリールアミド
WO2008104472A1 (en) * 2007-02-28 2008-09-04 F. Hoffmann-La Roche Ag 2, 4 -diaminopyrimidine derivatives and their use as p2x antagonists or as prodrugs thereof
WO2008104474A1 (en) * 2007-02-28 2008-09-04 F. Hoffmann-La Roche Ag Diaminopyrimidines
TW200843739A (en) 2007-03-30 2008-11-16 Shionogi & Co Novel pyrrolinone derivative and composition containing the same
CN103351390A (zh) * 2007-11-21 2013-10-16 解码遗传Ehf公司 用于治疗肺部和心血管病症的联芳基pde4 抑制剂
JP5637562B2 (ja) * 2008-09-25 2014-12-10 塩野義製薬株式会社 新規ピロリノン誘導体およびそれを含有する医薬組成物
CA2742866C (en) 2008-11-06 2017-10-24 Musc Foundation For Research Development Lysosomotropic inhibitors of acid ceramidase
BRPI0921185A2 (pt) 2008-11-24 2018-05-29 Basf Se composição curável, artigo para revestimento ou ligado, uso de um composto, e, composto
CA2748546A1 (en) * 2008-12-30 2010-07-08 Musc Foundation For Research Development Sphingo-guanidines and their use as inhibitors of sphingosine kinase
SG173647A1 (en) 2009-02-13 2011-10-28 Shionogi & Co Novel triazine derivative and pharmaceutical composition containing same
NZ623069A (en) 2009-08-17 2015-11-27 Sloan Kettering Inst Cancer Heat shock protein binding compounds, compositions, and methods for making and using same
WO2012020742A1 (ja) * 2010-08-10 2012-02-16 塩野義製薬株式会社 新規複素環誘導体およびそれらを含有する医薬組成物
US9718790B2 (en) 2010-08-10 2017-08-01 Shionogi & Co., Ltd. Triazine derivative and pharmaceutical composition having an analgesic activity comprising the same
JP6124351B2 (ja) * 2012-02-09 2017-05-10 塩野義製薬株式会社 複素環および炭素環誘導体
TWI637949B (zh) 2013-06-14 2018-10-11 塩野義製藥股份有限公司 胺基三衍生物及含有其等之醫藥組合物
PE20160431A1 (es) 2013-08-23 2016-06-02 Afferent Pharmaceuticals Inc Moduladores del receptor p2x3 y p2x2/3 de diaminopiridina para el tratamiento de la tos aguda, sub-aguda o cronica
EA201692155A1 (ru) 2014-05-13 2017-04-28 Мемориал Слоун-Кеттеринг Кэнсэ Сентр МОДУЛЯТОРЫ Hsp70 И СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ
US10195198B2 (en) 2014-07-03 2019-02-05 Afferent Pharmaceuticals, Inc. Methods and compositions for treating diseases and conditions
US9987279B2 (en) 2014-09-09 2018-06-05 Astellas Pharma Inc. Pharmaceutical composition for prevention and/or treatment of urinary incontinence
RU2585727C1 (ru) * 2014-12-12 2016-06-10 Наталья Борисовна Гусева Способ лечения детей с гиперактивным мочевым пузырем
CA2998742C (en) 2015-09-29 2023-08-29 Anthony P. FORD Diaminopyrimidine p2x3 and p2x2/3 receptor modulators for use in the treatment of cough
US10822311B2 (en) 2016-03-14 2020-11-03 Afferent Pharmaceuticals, Inc. Pyrimidines and variants thereof, and uses therefor
AU2017237929B2 (en) * 2016-03-25 2021-04-15 Afferent Pharmaceuticals Inc. Pyrimidines and variants thereof, and uses therefor
CN106083653A (zh) * 2016-06-06 2016-11-09 江苏天和制药有限公司 奥美普林中间体肉桂腈的合成方法
MX381790B (es) * 2016-12-20 2025-03-13 Afferent Pharmaceuticals Inc Sales cristalinas y polimorfos de un antagonista de p2x3.
CN117186068A (zh) 2017-11-01 2023-12-08 北京泰德制药股份有限公司 P2x3和/或p2x2/3受体拮抗剂、包含其的药物组合物及其用途
WO2019209607A1 (en) 2018-04-23 2019-10-31 Merck Sharp & Dohme Corp. Novel process for synthesis of a phenoxy diaminopyrimidine compound
US20210253513A1 (en) * 2018-06-15 2021-08-19 Pharmathen S.A. A novel process for the preparation of tapentadol
EP3964505B1 (en) * 2019-04-30 2025-10-15 Beijing Tide Pharmaceutical Co., Ltd. Solid form of diaminopyrimidine compound or hydrate thereof, preparation method therefor, and application thereof
EP3960179B1 (en) * 2019-04-30 2026-03-18 Beijing Tide Pharmaceutical Co., Ltd. Method for treating cough by using diaminopyrimidine compound
MA56022A (fr) 2019-05-31 2022-04-06 Chiesi Farm Spa Dérivés d'amino quinazoline servant d'inhibiteurs de p2x3
KR102923602B1 (ko) 2019-05-31 2026-02-06 키에시 파르마슈티시 엣스. 피. 에이. P2x3 억제제로서 피리도피리미딘 유도체
US12595261B2 (en) 2019-06-06 2026-04-07 Beijing Tide Pharmaceutical Co., Ltd. P2X3 and/or P2X2/3 receptor antagonist, pharmaceutical composition containing same, and use thereof
CN110551147B (zh) * 2019-09-29 2021-11-26 蚌埠产品质量监督检验研究院 一种3-环丙基苯硼酸的合成方法
TWI849314B (zh) * 2020-06-01 2024-07-21 日商住友化學股份有限公司 化合物、樹脂、抗蝕劑組成物及抗蝕劑圖案的製造方法
WO2022033567A1 (zh) 2020-08-13 2022-02-17 上海拓界生物医药科技有限公司 苯并咪唑类衍生物、其制备方法及医药用途
WO2022060945A1 (en) 2020-09-17 2022-03-24 Teva Pharmaceuticals International Gmbh Solid state forms of gefapixant and process for preparation thereof

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2658897A (en) 1951-06-27 1953-11-10 Burroughs Wellcome Co 2, 4-diamino-5-benzyl pyrimidines
US2657206A (en) * 1951-07-30 1953-10-27 Burroughs Wellcome Co 2, 4-diamino-5-aryloxy-pyrimidines
US2953567A (en) * 1956-11-23 1960-09-20 Burroughs Wellcome Co 5-phenylmercaptopyrimidines and method
US2909522A (en) 1957-02-21 1959-10-20 Burroughs Wellcome Co Trialkoxybenzylpyrimidines and method
US3849470A (en) 1969-03-06 1974-11-19 Burroughs Wellcome Co 5-benzyl pyrimidines intermediates therefore,and method
GB1261455A (en) * 1969-03-06 1972-01-26 Burroughs Wellcome Co Improvements in or relating to substituted acrylonitriles
US3855265A (en) 1969-03-06 1974-12-17 Burroughs Wellcome Co 5-benzyl pyrimidines intermediates therefore, and method
US3878252A (en) * 1970-09-24 1975-04-15 Burroughs Wellcome Co Ring substituted beta-hydroxy-phenyethylmethyl sulphone or sulphoxide
US3852276A (en) 1969-03-06 1974-12-03 Burroughs Wellcome Co 5-benzyl pyrimidines intermediate therefore, and method
US3850927A (en) 1969-03-06 1974-11-26 Burroughs Wellcome Co 5-benzyl pyrimidines intermediates therefore,and method
US4052553A (en) 1969-03-06 1977-10-04 Burroughs Wellcome Co. 5-benzyl pyrimidines intermediates therefore, and method
US3991050A (en) 1969-03-06 1976-11-09 Burroughs Wellcome Co. Preparation of β-Amino-α-benzylacrylonitriles
BR6915082D0 (pt) * 1969-05-16 1973-03-08 Wellcome Found Processo de preparacao de benzil-pirimidinas
CH513181A (de) 1969-06-12 1971-09-30 Hoffmann La Roche Verfahren zur Herstellung von N-Oxyden von Benzylpyrimidinen
US4255574A (en) 1973-02-26 1981-03-10 Hoffmann-La Roche Inc. Process for preparing 2,4-diamino-pyrimidines
US4143227A (en) 1973-02-26 1979-03-06 Hoffmann-La Roche Inc. Process for substituted 5-benzyl-2,4-diamino-pyrimidines
US3931181A (en) 1973-07-27 1976-01-06 Hoffmann-La Roche Inc. 2,4-Diamino-5-benzylpyrimidines
US4515948A (en) 1973-09-12 1985-05-07 Hoffmann-La Roche Inc. 2,4-Diamino-5-(4-amino and 4-dimethylamino-3,5-dimethoxy benzyl)pyrimidines
CH591457A5 (enExample) 1973-11-08 1977-09-15 Hoffmann La Roche
US3940393A (en) 1974-06-21 1976-02-24 American Home Products Corporation Synthesis of 2,6-diaminopyrimidines
US4039543A (en) 1974-12-24 1977-08-02 Hoffmann-La Roche Inc. Benzylpyrimidines
US4033962A (en) 1975-06-26 1977-07-05 Hoffman-La Roche Inc. 2,4-Diamino-pyrimidine derivatives and processes
GB1582245A (en) 1976-06-09 1981-01-07 Wellcome Found Benzyl cyanoacetal derivatives and their conversion to pyrimidine derivatives
US4115650A (en) 1976-11-17 1978-09-19 Hoffmann-La Roche Inc. Process for preparing 2,4-diamino-5-(substituted benzyl)-pyrimidines
US4075209A (en) 1977-02-07 1978-02-21 Hoffmann-La Roche, Inc. Process for preparing substituted 2,4-diaminopyrimidines and isoxazole intermediate
FR2397407A2 (fr) 1977-07-11 1979-02-09 Dick Pierre Derives de 2,4-diamino pyrimidines et leur mise en solution en association avec des sulfamides
US4258045A (en) 1979-11-30 1981-03-24 Merck & Co., Inc. Inhibitor of dihydrofolate reductase
DE3045720A1 (de) 1980-12-04 1982-07-08 Basf Ag, 6700 Ludwigshafen N-pyrimidinyl-carbaminsaeureester, verfahren zu ihrer herstellung und diese enthaltende arzneimittel
FR2502152A1 (fr) 1981-03-20 1982-09-24 Panmedica Laboratoires Nouveaux derives solubles n2 substitues de la diamino-2,4-benzyl-5-pyrimidines, leur procede de preparation et medicaments les contenant
IT1138146B (it) 1981-08-11 1986-09-17 Proter Spa Processo per la produzione della 2,4-diammino-(3,5-dimetossi-4-metos sietossi-benzil)-pirimidina
GB2116962A (en) * 1982-03-18 1983-10-05 Ciba Geigy Ag Nitriles; pyrimidines
US4590271A (en) 1982-05-01 1986-05-20 Burroughs Wellcome Co. 2,4-diamino-5-(substituted)pyrimidines, useful as antimicrobials
US4587341A (en) 1982-05-07 1986-05-06 Burroughs Wellcome Co. 2,4-diamino-5-(1,2,3,4-tetrahydro-(substituted or unsubstituted)-6-quinolylmethyl)pyrimidines, useful as antimicrobials
US4515574A (en) * 1983-02-16 1985-05-07 The Zeller Corporation Universal joint seal with multiple lips
DE3603577A1 (de) 1986-02-06 1987-08-13 Joachim K Prof Dr Seydel Neue substituierte 2,4-diamino-5-benzylpyrimidine, deren herstellung und deren verwendung als arzneimittel mit antibakterieller wirksamkeit
FR2595697B1 (fr) * 1986-03-13 1988-07-08 Rousselot Cie Derives de benzyl-pyrimidine, leur procede de preparation ainsi que les compositions en contenant
HU199683B (en) 1987-07-22 1990-03-28 Egyt Gyogyszervegyeszeti Gyar Process for producing pharmaceutical compositions analgesic, antiphlogistic, antipyretic, antianginic and/or antioxidative activity
US4996198A (en) 1988-07-11 1991-02-26 Hoffmann-La Roche Inc. Anticoccidial composition
US5240640A (en) 1990-06-04 1993-08-31 Coulter Corporation In situ use of gelatin or an aminodextran in the preparation of uniform ferrite particles
US5258373A (en) 1991-07-17 1993-11-02 Hoffmann-La Roche Inc. Anticoccidial compositions
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
WO1996016963A1 (de) 1994-11-25 1996-06-06 F. Hoffmann-La Roche Ag Sulfonamide und deren verwendung als heilmittel
CA2162630C (en) * 1994-11-25 2007-05-01 Volker Breu Sulfonamides
US5739333A (en) 1995-05-16 1998-04-14 Tanabe Seiyaku Co., Ltd. Sulfonamide derivative and process for preparing the same
US6440965B1 (en) 1997-10-15 2002-08-27 Krenitsky Pharmaceuticals, Inc. Substituted pyrimidine derivatives, their preparation and their use in the treatment of neurodegenerative or neurological disorders of the central nervous system
US6136971A (en) 1998-07-17 2000-10-24 Roche Colorado Corporation Preparation of sulfonamides
US6583148B1 (en) 1999-04-08 2003-06-24 Krenitsky Pharmaceuticals, Inc. Neurotrophic substituted pyrimidines
US6211185B1 (en) 1999-05-05 2001-04-03 Veterinary Pharmacy Corporation Concentrate comprising a sulfonamide in solution, a 2,4-diaminopyrimidine in stable suspension within said solution, and a suspending agent
CN100424079C (zh) 1999-09-03 2008-10-08 埃科特莱茵药品有限公司 双磺胺
TR200200763T2 (tr) 1999-09-24 2003-09-22 Janssen Pharmaceutica N.V. Antiviral bileşimler
SE9904652D0 (sv) * 1999-12-17 1999-12-17 Astra Pharma Prod Novel Compounds
US6515198B2 (en) * 2000-02-15 2003-02-04 Syntex (U.S.A.) Llc Use of purinergic receptor modulators and related reagents
AU2001263850A1 (en) 2000-04-20 2001-11-07 Actelion Pharmaceuticals Ltd Pyrimidine-sulfonamides having endothelin-antagonist activity
WO2001081338A1 (en) 2000-04-25 2001-11-01 Actelion Pharmaceuticals Ltd Substituted sulfonylaminopyrimidines
MY140724A (en) 2000-07-21 2010-01-15 Actelion Pharmaceuticals Ltd Novel arylethene-sulfonamides
US7091201B2 (en) 2000-09-25 2006-08-15 Actelion Pharmaceuticals Ltd. Arylalkane-sulfonamides having endothelin-antagonist activity
EP1693372A1 (en) 2000-12-18 2006-08-23 Actelion Pharmaceuticals Ltd. Novel Sulfamides and their use as endothelin receptor antagonists
US6423720B1 (en) 2001-02-01 2002-07-23 Duquesne University Of The Holy Ghost Pyrimidine compounds and methods for making and using the same
WO2002083650A1 (en) 2001-04-11 2002-10-24 Actelion Pharmaceuticals Ltd Novel sulfonylamino-pyrimidines
EP1392643B1 (en) * 2001-05-18 2005-09-14 Abbott Laboratories Trisubstituted-n- (1s)-1,2,3,4-tetrahydro-1-naphthalenyl] benzamides which inhibit p2x3 and p2x2/3 containing receptors
WO2003042190A1 (en) * 2001-11-12 2003-05-22 Pfizer Products Inc. N-alkyl-adamantyl derivatives as p2x7-receptor antagonists
PT1725540E (pt) * 2004-03-05 2012-11-29 Hoffmann La Roche Diaminopirimidinas como antagonistas de p2x3 e p2x2/3
ES2562056T3 (es) * 2005-09-01 2016-03-02 F. Hoffmann-La Roche Ag Diaminopirimidinas como moduladores P2X3 y P2X2/3
AU2006286576B2 (en) * 2005-09-01 2012-06-14 F. Hoffmann-La Roche Ag Diaminopyrimidines as P2X3 and P3X2/3 modulators
SI1924264T1 (sl) * 2005-09-01 2013-12-31 F. Hoffmann-La Roche Ag Diaminopirimidini kot modulatorji p2x3 in p2x2/3
WO2008104472A1 (en) * 2007-02-28 2008-09-04 F. Hoffmann-La Roche Ag 2, 4 -diaminopyrimidine derivatives and their use as p2x antagonists or as prodrugs thereof

Also Published As

Publication number Publication date
EP2343282A1 (en) 2011-07-13
MY145465A (en) 2012-02-15
LTPA2024508I1 (enExample) 2024-04-10
JP2014193906A (ja) 2014-10-09
NL301261I2 (nl) 2024-03-25
BE2024C508I2 (enExample) 2024-08-08
US20190016688A1 (en) 2019-01-17
NO2024010I1 (no) 2024-03-06
AU2005229331B2 (en) 2011-10-13
LTC1725540I2 (enExample) 2024-07-10
NZ549069A (en) 2010-09-30
CY2024006I1 (el) 2024-09-20
CA2557372C (en) 2013-01-08
US9556127B2 (en) 2017-01-31
US20210009531A1 (en) 2021-01-14
NO20161635A1 (no) 2016-10-12
US20140357629A1 (en) 2014-12-04
JP2011126899A (ja) 2011-06-30
IL177438A0 (en) 2006-12-10
LUC00333I2 (enExample) 2024-10-04
JP5465700B2 (ja) 2014-04-09
HUS2400005I1 (hu) 2024-04-28
NO343755B1 (no) 2019-05-27
ES2548022T3 (es) 2015-10-13
US20230100975A1 (en) 2023-03-30
JP5576314B2 (ja) 2014-08-20
BRPI0508461A (pt) 2007-07-31
AU2005229331A1 (en) 2005-10-13
AR047992A1 (es) 2006-03-15
EP2343282B1 (en) 2015-07-22
TW200539885A (en) 2005-12-16
BR122018003623B1 (pt) 2018-10-09
JP4717876B2 (ja) 2011-07-06
NO20064065L (no) 2006-11-28
CY1113450T1 (el) 2016-06-22
US20250066309A1 (en) 2025-02-27
US20170096404A1 (en) 2017-04-06
NO20150504L (no) 2006-11-28
US20240158356A1 (en) 2024-05-16
JP2011252004A (ja) 2011-12-15
BRPI0508461B8 (pt) 2021-05-25
FR24C1011I1 (fr) 2024-05-24
JP2007526268A (ja) 2007-09-13
US20110077242A1 (en) 2011-03-31
WO2005095359A1 (en) 2005-10-13
KR100822530B1 (ko) 2008-04-16
EP1725540A1 (en) 2006-11-29
BRPI0508461B1 (pt) 2018-05-15
CN1930135A (zh) 2007-03-14
HRP20120901T1 (hr) 2012-12-31
CY2024006I2 (el) 2024-09-20
IL217453A (en) 2014-12-31
JP5886898B2 (ja) 2016-03-16
RU2422441C2 (ru) 2011-06-27
EP1725540B1 (en) 2012-09-12
US8846705B2 (en) 2014-09-30
HK1101074A1 (en) 2007-10-05
TWI313604B (en) 2009-08-21
CN1930135B (zh) 2011-12-28
IL217453A0 (en) 2012-02-29
SI1725540T1 (sl) 2012-12-31
FR24C1011I2 (fr) 2024-12-13
CA2557372A1 (en) 2005-10-13
US20050209260A1 (en) 2005-09-22
RU2006135203A (ru) 2008-04-10
US20200115347A1 (en) 2020-04-16
DK1725540T5 (da) 2012-10-22
PT1725540E (pt) 2012-11-29
PL1725540T3 (pl) 2013-02-28
IL177438A (en) 2012-10-31
KR20060117366A (ko) 2006-11-16
BR122018003623B8 (pt) 2021-07-27
FIC20240007I1 (fi) 2024-03-13
NO339497B1 (no) 2016-12-19
ES2391636T3 (es) 2012-11-28
DK1725540T3 (da) 2012-10-01
US20190270713A1 (en) 2019-09-05
US20180141919A1 (en) 2018-05-24
US7858632B2 (en) 2010-12-28

Similar Documents

Publication Publication Date Title
CA2557372C (en) Diaminopyrimidines as p2x3 and p2x2/3 antagonists
AU2006286601B2 (en) Diaminopyrimidines as P2X3 and P2X2/3 modulators
AU2012200211B2 (en) Diaminopyrimidines as P2X3 and P2X2/3 antagonists