ES2548022T3 - Diaminopirimidinas como antagonistas de P2X3 y P2X2/3 - Google Patents

Diaminopirimidinas como antagonistas de P2X3 y P2X2/3 Download PDF

Info

Publication number
ES2548022T3
ES2548022T3 ES10179618.3T ES10179618T ES2548022T3 ES 2548022 T3 ES2548022 T3 ES 2548022T3 ES 10179618 T ES10179618 T ES 10179618T ES 2548022 T3 ES2548022 T3 ES 2548022T3
Authority
ES
Spain
Prior art keywords
isopropyl
pyrimidin
benzyl
diamine
methoxy
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES10179618.3T
Other languages
English (en)
Spanish (es)
Inventor
Chris Allen Broka
David Scott Carter
Michael Patrick Dillon
Ronald Charles Hawley
Alam Jahangir
Clara Jeou Jen Lin
Daniel Warren Parish
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Application granted granted Critical
Publication of ES2548022T3 publication Critical patent/ES2548022T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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
    • 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
    • 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
    • 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)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Toxicology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
ES10179618.3T 2004-03-05 2005-02-25 Diaminopirimidinas como antagonistas de P2X3 y P2X2/3 Expired - Lifetime ES2548022T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US55049904P 2004-03-05 2004-03-05
US550499P 2004-03-05

Publications (1)

Publication Number Publication Date
ES2548022T3 true ES2548022T3 (es) 2015-10-13

Family

ID=34961010

Family Applications (2)

Application Number Title Priority Date Filing Date
ES10179618.3T Expired - Lifetime ES2548022T3 (es) 2004-03-05 2005-02-25 Diaminopirimidinas como antagonistas de P2X3 y P2X2/3
ES05715558T Expired - Lifetime ES2391636T3 (es) 2004-03-05 2005-02-25 Diaminopirimidinas como antagonistas de P2X3 y P2X2/3

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES05715558T Expired - Lifetime ES2391636T3 (es) 2004-03-05 2005-02-25 Diaminopirimidinas como antagonistas de P2X3 y P2X2/3

Country Status (31)

Country Link
US (12) US7858632B2 (enEXAMPLES)
EP (2) EP1725540B1 (enEXAMPLES)
JP (4) JP4717876B2 (enEXAMPLES)
KR (1) KR100822530B1 (enEXAMPLES)
CN (1) CN1930135B (enEXAMPLES)
AR (1) AR047992A1 (enEXAMPLES)
AU (1) AU2005229331B2 (enEXAMPLES)
BE (1) BE2024C508I2 (enEXAMPLES)
BR (2) BR122018003623B8 (enEXAMPLES)
CA (1) CA2557372C (enEXAMPLES)
CY (2) CY1113450T1 (enEXAMPLES)
DK (1) DK1725540T5 (enEXAMPLES)
ES (2) ES2548022T3 (enEXAMPLES)
FI (1) FIC20240007I1 (enEXAMPLES)
FR (1) FR24C1011I2 (enEXAMPLES)
HR (1) HRP20120901T1 (enEXAMPLES)
HU (1) HUS2400005I1 (enEXAMPLES)
IL (2) IL177438A (enEXAMPLES)
LT (1) LTC1725540I2 (enEXAMPLES)
LU (1) LUC00333I2 (enEXAMPLES)
MY (1) MY145465A (enEXAMPLES)
NL (1) NL301261I2 (enEXAMPLES)
NO (4) NO339497B1 (enEXAMPLES)
NZ (1) NZ549069A (enEXAMPLES)
PL (1) PL1725540T3 (enEXAMPLES)
PT (1) PT1725540E (enEXAMPLES)
RU (1) RU2422441C2 (enEXAMPLES)
SI (1) SI1725540T1 (enEXAMPLES)
TW (1) TWI313604B (enEXAMPLES)
WO (1) WO2005095359A1 (enEXAMPLES)
ZA (1) ZA200606880B (enEXAMPLES)

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1725540B1 (en) * 2004-03-05 2012-09-12 F.Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 antagonists
CA2585645C (en) * 2004-10-29 2014-10-21 Musc Foundation For Research Development Ceramides and apoptosis-signaling ligand
EP1926716B1 (en) 2005-09-01 2011-10-19 F. Hoffmann-La Roche AG Process for synthesis of aryloxy diaminopyrimidines
KR101025381B1 (ko) * 2005-09-01 2011-03-28 에프. 호프만-라 로슈 아게 Ｐ2ｘ3 및 ｐ2ｘ2/3 조정자로서의 다이아미노피리미딘
JP4850911B2 (ja) * 2005-09-01 2012-01-11 エフ．ホフマン−ラ ロシュ アーゲー Ｐ２ｘ３およびｐ２ｘ２／３モジュレーターとしてのジアミノピリミジン
CN101300235B (zh) * 2005-09-01 2011-12-07 弗·哈夫曼-拉罗切有限公司 作为p2x3和p2x2/3调节剂的二氨基嘧啶类化合物
DK1924264T5 (en) * 2005-09-01 2014-03-24 Hoffmann La Roche Diaminopyrimidines as P2X3- and P2X2 / 3 modulators
EP1770089A1 (en) * 2005-10-03 2007-04-04 Institut Pasteur Pyranodibenzofuran derivatives with antifungal and antibacterial activity
KR101176701B1 (ko) 2006-10-04 2012-08-23 에프. 호프만-라 로슈 아게 펜옥시 다이아미노피리미딘 유도체의 합성 방법
MX2009004900A (es) * 2006-11-09 2009-05-19 Hoffmann La Roche Arilamidas sustituidas por tiazol u oxazol.
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
CA2682473A1 (en) 2007-03-30 2008-10-09 Shionogi & Co., Ltd. Novel pyrrolinone derivative and pharmaceutical composition comprising 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
US8575197B2 (en) 2008-09-25 2013-11-05 Shionogi & Co., Ltd. Pyrolinone derivative and pharmaceutical composition comprising the same
EP2348839B1 (en) 2008-11-06 2017-04-05 MUSC Foundation For Research Development Lysosomotropic inhibitors of acid ceramidase
JP5250116B2 (ja) 2008-11-24 2013-07-31 ビーエーエスエフ ソシエタス・ヨーロピア 熱潜在性塩基を含む硬化性組成物
AU2009332952A1 (en) * 2008-12-30 2011-07-21 Musc Foundation For Research Development Sphingo-guanidines and their use as inhibitors of sphingosine kinase
CA2752269C (en) 2009-02-13 2016-08-30 Hiroyuki Kai Novel triazine derivative and pharmaceutical composition comprising the same
CN102753177A (zh) * 2009-08-17 2012-10-24 纪念斯隆-凯特琳癌症中心 热休克蛋白结合化合物、组合物以及其制备和使用方法
CN103140221A (zh) * 2010-08-10 2013-06-05 盐野义制药株式会社 新型杂环衍生物和含有其的药物组合物
CA2807947C (en) 2010-08-10 2018-06-19 Shionogi & Co., Ltd. Triazine derivative and pharmaceutical compound that contains same and exhibits analgesic activity
WO2013118855A1 (ja) * 2012-02-09 2013-08-15 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
KR102196885B1 (ko) * 2013-08-23 2020-12-30 애퍼런트 파마슈티컬스 인크. 급성, 아급성 또는 만성 기침의 치료를 위한 디아미노피리미딘 p2x3 및 p2x2/3 수용체 조절제
JP6607870B2 (ja) 2014-05-13 2019-11-20 メモリアル スローン ケタリング キャンサー センター Ｈｓｐ７０モジュレーターならびにその作製および使用方法
WO2016004358A1 (en) 2014-07-03 2016-01-07 Afferent Pharmaceuticals, Inc. Methods and compositions for treating diseases and conditions
JP6573618B2 (ja) 2014-09-09 2019-09-11 アステラス製薬株式会社 尿失禁予防用及び／又は治療用新規医薬組成物
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
MA43821A (fr) * 2016-03-14 2018-11-28 Afferent Pharmaceuticals Inc Pyrimidines et variantes de celles-ci, et leurs utilisations
KR102377805B1 (ko) * 2016-03-25 2022-03-22 애퍼런트 파마슈티컬스 인크. 피리미딘 및 그의 변이체, 및 그의 용도
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
KR102557242B1 (ko) 2016-12-20 2023-07-18 애퍼런트 파마슈티컬스 인크. Ｐ2ｘ3 길항제의 결정질 염 및 다형체
CA3076680A1 (en) 2017-11-01 2019-05-09 Beijing Tide Pharmaceutical Co., Ltd. P2x3 and/or p2x2/3 receptor antagonist, pharmaceutical composition comprising same, and use thereof
JP7502997B6 (ja) * 2018-04-23 2024-07-12 メルク・シャープ・アンド・ドーム・エルエルシー フェノキシジアミノピリミジン化合物の新規な合成方法
CN112262121A (zh) * 2018-06-15 2021-01-22 法尔玛赞公司 用于制备他喷他多的新方法
CN114007619B (zh) * 2019-04-30 2024-08-06 北京泰德制药股份有限公司 二氨基嘧啶类化合物治疗咳嗽的方法
BR112021021721A2 (pt) * 2019-04-30 2021-12-28 Beijing Tide Pharmaceutical Co Ltd Forma sólida de composto de diaminopirimidina ou hidrato do mesmo, método de preparação para a mesma e aplicação da mesma
MX2021014115A (es) * 2019-05-31 2021-12-10 Chiesi Farm Spa Derivados de aminoquinazolina como inhibidores del purinoreceptor 3 de p2x (p2x3).
WO2020244607A1 (zh) * 2019-06-06 2020-12-10 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
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
CA3187092A1 (en) 2020-08-13 2022-02-17 Wenming Li Benzimidazole derivatives, preparation method therefor and medical use thereof
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
US3991050A (en) 1969-03-06 1976-11-09 Burroughs Wellcome Co. Preparation of β-Amino-α-benzylacrylonitriles
US4052553A (en) 1969-03-06 1977-10-04 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
US3878252A (en) * 1970-09-24 1975-04-15 Burroughs Wellcome Co Ring substituted beta-hydroxy-phenyethylmethyl sulphone or sulphoxide
US3850927A (en) 1969-03-06 1974-11-26 Burroughs Wellcome Co 5-benzyl pyrimidines intermediates therefore,and method
US3849470A (en) 1969-03-06 1974-11-19 Burroughs Wellcome Co 5-benzyl pyrimidines intermediates therefore,and method
US3855265A (en) 1969-03-06 1974-12-17 Burroughs Wellcome Co 5-benzyl pyrimidines intermediates therefore, and method
US3852276A (en) 1969-03-06 1974-12-03 Burroughs Wellcome Co 5-benzyl pyrimidines intermediate therefore, and method
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
US4143227A (en) 1973-02-26 1979-03-06 Hoffmann-La Roche Inc. Process for substituted 5-benzyl-2,4-diamino-pyrimidines
US4255574A (en) 1973-02-26 1981-03-10 Hoffmann-La Roche Inc. Process for preparing 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 (enEXAMPLES) 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
CA2162630C (en) * 1994-11-25 2007-05-01 Volker Breu Sulfonamides
WO1996016963A1 (de) 1994-11-25 1996-06-06 F. Hoffmann-La Roche Ag Sulfonamide und deren verwendung als heilmittel
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
IL143935A (en) 1999-09-03 2005-08-31 Actelion Pharmaceuticals Ltd Bis-sulfonamides
AU775360B2 (en) 1999-09-24 2004-07-29 Janssen Pharmaceutica N.V. Antiviral compositions
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
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
MY140724A (en) 2000-07-21 2010-01-15 Actelion Pharmaceuticals Ltd Novel arylethene-sulfonamides
DE60140263D1 (de) 2000-09-25 2009-12-03 Actelion Pharmaceuticals Ltd Arylalkanen-sulfonamiden mit endothelin-antagonistischer aktivität
IL155805A0 (en) 2000-12-18 2003-12-23 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
DE60206164T2 (de) * 2001-05-18 2006-06-22 Abbott Laboratories, Abbott Park Trisubstituierte-n-((1s)-1,2,3,4-tetrahydro-1-naphthalenyl) benzamide welche p2x3 und p2x2/3 enthaltende rezeptoren inhibieren
WO2003042190A1 (en) * 2001-11-12 2003-05-22 Pfizer Products Inc. N-alkyl-adamantyl derivatives as p2x7-receptor antagonists
EP1725540B1 (en) * 2004-03-05 2012-09-12 F.Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 antagonists
KR101025381B1 (ko) * 2005-09-01 2011-03-28 에프. 호프만-라 로슈 아게 Ｐ2ｘ3 및 ｐ2ｘ2/3 조정자로서의 다이아미노피리미딘
DK1924264T5 (en) * 2005-09-01 2014-03-24 Hoffmann La Roche Diaminopyrimidines as P2X3- and P2X2 / 3 modulators
CN101300235B (zh) * 2005-09-01 2011-12-07 弗·哈夫曼-拉罗切有限公司 作为p2x3和p2x2/3调节剂的二氨基嘧啶类化合物
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
DK1725540T3 (da) 2012-10-01
NO343755B1 (no) 2019-05-27
CY2024006I2 (el) 2024-09-20
LUC00333I2 (enEXAMPLES) 2024-10-04
CA2557372C (en) 2013-01-08
AU2005229331A1 (en) 2005-10-13
PT1725540E (pt) 2012-11-29
KR100822530B1 (ko) 2008-04-16
AU2005229331B2 (en) 2011-10-13
LTC1725540I2 (enEXAMPLES) 2024-07-10
JP2014193906A (ja) 2014-10-09
US20190016688A1 (en) 2019-01-17
NL301261I2 (nl) 2024-03-25
JP4717876B2 (ja) 2011-07-06
CY1113450T1 (el) 2016-06-22
US20170096404A1 (en) 2017-04-06
JP2011252004A (ja) 2011-12-15
US20240158356A1 (en) 2024-05-16
IL217453A0 (en) 2012-02-29
NZ549069A (en) 2010-09-30
NO339497B1 (no) 2016-12-19
US20050209260A1 (en) 2005-09-22
TWI313604B (en) 2009-08-21
US7858632B2 (en) 2010-12-28
NO20161635A1 (no) 2016-10-12
AR047992A1 (es) 2006-03-15
FR24C1011I1 (fr) 2024-05-24
BR122018003623B8 (pt) 2021-07-27
US20230100975A1 (en) 2023-03-30
JP5576314B2 (ja) 2014-08-20
EP2343282A1 (en) 2011-07-13
SI1725540T1 (sl) 2012-12-31
BE2024C508I2 (enEXAMPLES) 2024-08-08
CN1930135B (zh) 2011-12-28
US20210009531A1 (en) 2021-01-14
US20190270713A1 (en) 2019-09-05
US20250066309A1 (en) 2025-02-27
US8846705B2 (en) 2014-09-30
MY145465A (en) 2012-02-15
RU2006135203A (ru) 2008-04-10
US20200115347A1 (en) 2020-04-16
HUS2400005I1 (hu) 2024-04-28
BRPI0508461A (pt) 2007-07-31
HK1101074A1 (en) 2007-10-05
BRPI0508461B1 (pt) 2018-05-15
ES2391636T3 (es) 2012-11-28
RU2422441C2 (ru) 2011-06-27
JP5465700B2 (ja) 2014-04-09
FR24C1011I2 (fr) 2024-12-13
BR122018003623B1 (pt) 2018-10-09
IL177438A (en) 2012-10-31
LTPA2024508I1 (enEXAMPLES) 2024-04-10
ZA200606880B (en) 2008-04-30
JP5886898B2 (ja) 2016-03-16
JP2011126899A (ja) 2011-06-30
NO20150504L (no) 2006-11-28
IL177438A0 (en) 2006-12-10
BRPI0508461B8 (pt) 2021-05-25
EP1725540A1 (en) 2006-11-29
NO2024010I1 (no) 2024-03-06
IL217453A (en) 2014-12-31
US20180141919A1 (en) 2018-05-24
HRP20120901T1 (hr) 2012-12-31
WO2005095359A1 (en) 2005-10-13
NO20064065L (no) 2006-11-28
PL1725540T3 (pl) 2013-02-28
CA2557372A1 (en) 2005-10-13
EP2343282B1 (en) 2015-07-22
CN1930135A (zh) 2007-03-14
US20140357629A1 (en) 2014-12-04
JP2007526268A (ja) 2007-09-13
FIC20240007I1 (fi) 2024-03-13
DK1725540T5 (da) 2012-10-22
TW200539885A (en) 2005-12-16
US20110077242A1 (en) 2011-03-31
US9556127B2 (en) 2017-01-31
KR20060117366A (ko) 2006-11-16
CY2024006I1 (el) 2024-09-20
EP1725540B1 (en) 2012-09-12

Similar Documents

Publication Publication Date Title
ES2548022T3 (es) Diaminopirimidinas como antagonistas de P2X3 y P2X2/3
US20250025462A1 (en) Methods of using diaminopyrimidine p2x3 and p2x2/3 receptor modulators for treatment of respiratory and gastrointestinal diseases
AU2012200211B2 (en) Diaminopyrimidines as P2X3 and P2X2/3 antagonists
MXPA06009857A (en) Diaminopyrimidines as p2x3 and p2x2/3 antagonists