CN101198608B - A2b腺苷受体拮抗剂的前药 - Google Patents

A2b腺苷受体拮抗剂的前药 Download PDF

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Publication number
CN101198608B
CN101198608B CN2006800213389A CN200680021338A CN101198608B CN 101198608 B CN101198608 B CN 101198608B CN 2006800213389 A CN2006800213389 A CN 2006800213389A CN 200680021338 A CN200680021338 A CN 200680021338A CN 101198608 B CN101198608 B CN 101198608B
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CN
China
Prior art keywords
methyl
compound
ethyl
phenyl
trifluoromethyl
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Expired - Fee Related
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CN2006800213389A
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English (en)
Chinese (zh)
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CN101198608A (zh
Inventor
德米特里·科尔通
杰夫·扎布沃茨基
拉奥·卡拉
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Gilead Palo Alto Inc
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Gilead Palo Alto Inc
CV Therapeutics Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • 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
    • 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
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Molecular Biology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biochemistry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN2006800213389A 2005-06-16 2006-06-14 A2b腺苷受体拮抗剂的前药 Expired - Fee Related CN101198608B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US69140805P 2005-06-16 2005-06-16
US60/691,408 2005-06-16
PCT/US2006/023167 WO2006138376A1 (en) 2005-06-16 2006-06-14 Prodrugs of a2b adenosine receptor antagonists

Publications (2)

Publication Number Publication Date
CN101198608A CN101198608A (zh) 2008-06-11
CN101198608B true CN101198608B (zh) 2011-04-27

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CN2006800213389A Expired - Fee Related CN101198608B (zh) 2005-06-16 2006-06-14 A2b腺苷受体拮抗剂的前药

Country Status (14)

Country Link
US (3) US7625881B2 (enExample)
EP (2) EP2301937A1 (enExample)
JP (1) JP5044823B2 (enExample)
KR (1) KR20080016645A (enExample)
CN (1) CN101198608B (enExample)
AU (1) AU2006259411B2 (enExample)
CA (1) CA2612344A1 (enExample)
IL (1) IL188103A0 (enExample)
MX (1) MX2007015909A (enExample)
NO (1) NO20080278L (enExample)
NZ (1) NZ564326A (enExample)
RU (2) RU2415858C2 (enExample)
WO (1) WO2006138376A1 (enExample)
ZA (1) ZA200710878B (enExample)

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US20080318983A1 (en) * 2001-11-09 2008-12-25 Rao Kalla A2b adenosine receptor antagonists
US7317017B2 (en) * 2002-11-08 2008-01-08 Cv Therapeutics, Inc. A2B adenosine receptor antagonists
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EP2311462A1 (en) 2004-10-15 2011-04-20 Cv Therapeutics, Inc. Method of preventing and treating airway remodeling and pulmonary inflammation using A2B adenosine receptor antagonists
WO2006091898A2 (en) * 2005-02-25 2006-08-31 Adenosine Therapeutics, Llc Pyrazolyl substituted xanthines
US7598379B2 (en) * 2005-02-25 2009-10-06 Pgx Health, Llc Methods for the synthesis of unsymmetrical cycloalkyl substituted xanthines
WO2006091897A2 (en) * 2005-02-25 2006-08-31 Adenosine Therapeutics, Llc Derivatives of 8-substituted xanthines
CA2612344A1 (en) 2005-06-16 2006-12-28 Cv Therapeutics, Inc. Prodrugs of a2b adenosine receptor antagonists
CA2646333C (en) * 2006-03-17 2014-06-17 Cv Therapeutics, Inc. Method of preventing and treating hepatic disease using a2b adenosine receptor antagonists
US7884100B2 (en) * 2006-06-16 2011-02-08 Pgxhealth, Llc Substituted 8-[6-amino-3-pyridyl]xanthines
US7767685B2 (en) * 2006-06-29 2010-08-03 King Pharmaceuticals Research And Development, Inc. Adenosine A2B receptor antagonists
WO2009088518A1 (en) * 2008-01-11 2009-07-16 Cv Therapeutics, Inc. A2b adenosine receptor antagonists for the treatment of cancer
WO2009157938A1 (en) * 2008-06-26 2009-12-30 Cv Therapeutics, Inc. A2b adenosine receptor antagonists for treating cancer
EP2521545B1 (en) * 2010-01-07 2019-11-27 Alkermes Pharma Ireland Limited Prodrugs of heteroaromatic compounds
KR20130088834A (ko) * 2010-06-30 2013-08-08 길리애드 사이언시즈, 인코포레이티드 폐 고혈압의 치료를 위한 ａ２ｂ 아데노신 수용체 길항제의 용도
EP2616470B1 (en) 2010-09-13 2016-10-12 Advinus Therapeutics Limited Purine compounds as prodrugs of a2b adenosine receptor antagonists, their process and medicinal applications
AR085942A1 (es) 2011-04-07 2013-11-06 Gilead Sciences Inc Uso de receptor de aadenosina para tratar la insuficiencia cardiaca y la arritmia en pacientes posinfarto de miocardio
US9359376B2 (en) * 2011-04-08 2016-06-07 Sphaera Pharma Pte. Ltd Substituted methylformyl reagents and method of using same to modify physicochemical and/or pharmacokinetic properties of compounds
AR091279A1 (es) 2012-06-08 2015-01-21 Gilead Sciences Inc Inhibidores macrociclicos de virus flaviviridae
SI2859009T1 (sl) 2012-06-08 2017-12-29 Gilead Sciences, Inc. Makrociklični inhibitorji flaviviridae virusov
IN2014MN02652A (enExample) 2012-06-08 2015-08-21 Gilead Sciences Inc
ES2580702B1 (es) 2015-02-25 2017-06-08 Palobiofarma, S.L. Derivados de 2-aminopiridina como antagonistas del receptor A2b de adenosina y ligandos del receptor MT3 de melatonina
KR102671166B1 (ko) * 2015-12-14 2024-05-31 막스-플랑크-게젤샤프트 츄어 푀르더룽 데어 비쎈샤프텐 에.파우. 3,5-디페닐-디아졸 화합물의 수용성 유도체
JP7849948B2 (ja) * 2018-03-05 2026-04-22 テオン セラピューティクス，インク． アデノシン受容体アンタゴニストおよびその使用
JP7156154B2 (ja) * 2019-04-18 2022-10-19 株式会社島津製作所 培地処理システム及び培地処理方法
TW202327612A (zh) * 2021-09-10 2023-07-16 美商天恩治療有限公司 使用腺苷受體拮抗劑之改良療法

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CN1585769A (zh) * 2001-11-09 2005-02-23 Cv医药有限公司 A2b腺苷受体拮抗剂

Also Published As

Publication number Publication date
EP1891070A1 (en) 2008-02-27
RU2010150615A (ru) 2012-06-20
US20110160162A1 (en) 2011-06-30
EP2301937A1 (en) 2011-03-30
US20100056538A1 (en) 2010-03-04
MX2007015909A (es) 2008-03-06
RU2007146669A (ru) 2009-06-20
US7625881B2 (en) 2009-12-01
AU2006259411A1 (en) 2006-12-28
WO2006138376A1 (en) 2006-12-28
NZ564326A (en) 2010-01-29
ZA200710878B (en) 2009-05-27
NO20080278L (no) 2008-02-28
AU2006259411B2 (en) 2012-03-22
US20060293283A1 (en) 2006-12-28
KR20080016645A (ko) 2008-02-21
CA2612344A1 (en) 2006-12-28
JP5044823B2 (ja) 2012-10-10
US8143249B2 (en) 2012-03-27
RU2415858C2 (ru) 2011-04-10
JP2008543860A (ja) 2008-12-04
IL188103A0 (en) 2008-03-20
CN101198608A (zh) 2008-06-11

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