JP5788397B2 - ケモカイン受容体活性の調節薬としてのピペリジニル誘導体のプロドラッグ - Google Patents

ケモカイン受容体活性の調節薬としてのピペリジニル誘導体のプロドラッグ Download PDF

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JP5788397B2
JP5788397B2 JP2012533303A JP2012533303A JP5788397B2 JP 5788397 B2 JP5788397 B2 JP 5788397B2 JP 2012533303 A JP2012533303 A JP 2012533303A JP 2012533303 A JP2012533303 A JP 2012533303A JP 5788397 B2 JP5788397 B2 JP 5788397B2
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compound
disease
compounds
acid
mmol
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JP2013507377A5 (enExample
JP2013507377A (ja
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ジョン・ハインズ
パーシー・エイチ・カーター
リンドン・エイ・エム・コーネリアス
ティ・ジー・ムラリ・ダー
ジョン・ブイ・ダンシア
サティーシュ・ナイル
ジョゼフ・ビー・サンテッラ
ジャヤクマール・エス・ウォリアー
ウ・ホン
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Bristol Myers Squibb Co
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
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    • A61P11/00Drugs for disorders of the respiratory system
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
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    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
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    • A61P9/00Drugs for disorders of the cardiovascular system
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/52Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4
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    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/59Hydrogenated pyridine rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
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  • Medicinal Chemistry (AREA)
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  • Vascular Medicine (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
JP2012533303A 2009-10-07 2010-10-07 ケモカイン受容体活性の調節薬としてのピペリジニル誘導体のプロドラッグ Expired - Fee Related JP5788397B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US24927009P 2009-10-07 2009-10-07
US61/249,270 2009-10-07
PCT/US2010/051731 WO2011044309A1 (en) 2009-10-07 2010-10-07 Prodrugs of a piperidinyl derivative as modulators of chemokine receptor activity

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JP2013507377A JP2013507377A (ja) 2013-03-04
JP2013507377A5 JP2013507377A5 (enExample) 2013-11-21
JP5788397B2 true JP5788397B2 (ja) 2015-09-30

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JP2012533303A Expired - Fee Related JP5788397B2 (ja) 2009-10-07 2010-10-07 ケモカイン受容体活性の調節薬としてのピペリジニル誘導体のプロドラッグ

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US (2) US8410139B2 (enExample)
EP (1) EP2486013B1 (enExample)
JP (1) JP5788397B2 (enExample)
KR (1) KR20120083900A (enExample)
CN (1) CN102648179B (enExample)
AR (1) AR078543A1 (enExample)
AU (1) AU2010303441A1 (enExample)
BR (1) BR112012007755A2 (enExample)
CA (1) CA2777032A1 (enExample)
CL (1) CL2012000882A1 (enExample)
CO (1) CO6440510A2 (enExample)
EA (1) EA022150B1 (enExample)
IL (1) IL219122A (enExample)
MX (1) MX2012003656A (enExample)
NZ (1) NZ599261A (enExample)
PE (1) PE20121109A1 (enExample)
TW (1) TW201118070A (enExample)
WO (1) WO2011044309A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT3129016T (pt) 2014-04-08 2018-10-01 Neurovive Pharmaceutical Ab Compostos novos
AR106018A1 (es) * 2015-08-26 2017-12-06 Achillion Pharmaceuticals Inc Compuestos de arilo, heteroarilo y heterocíclicos para el tratamiento de trastornos médicos
WO2017035409A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Aryl, heteroaryl, and heterocyclic compounds for treatment of immune and inflammatory disorders
EP3589287B1 (en) 2017-03-01 2022-09-14 Achillion Pharmaceuticals, Inc. Macrocyclic compounds for treatment of medical disorders
CN110776481B (zh) * 2018-07-24 2023-06-16 四川大学华西医院 一类双阳离子化合物及其制备方法和用途
CN108727248B (zh) 2018-07-25 2021-05-25 四川大学华西医院 一类双季铵化合物及其制备方法和用途
EP3898617A4 (en) 2018-12-17 2022-08-17 Achillion Pharmaceuticals, Inc. TARGETED DOSAGE FOR THE TREATMENT OF COMPLEMENT INDUCED DISORDERS

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU770042B2 (en) * 1998-12-18 2004-02-12 Bristol-Myers Squibb Pharma Company N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
JP2006520783A (ja) * 2003-03-18 2006-09-14 メルク エンド カムパニー インコーポレーテッド ケモカイン受容体活性のアミノシクロブチルアミド調節物質
US7601844B2 (en) * 2006-01-27 2009-10-13 Bristol-Myers Squibb Company Piperidinyl derivatives as modulators of chemokine receptor activity
AU2007275931B2 (en) * 2006-07-19 2011-06-16 Astrazeneca Ab Novel tricyclic spiropiperidine compounds, their synthesis and their uses as modulators of chemokine receptor activity
WO2009015164A2 (en) 2007-07-24 2009-01-29 Bristol-Myers Squibb Company Piperidinyl derivatives as modulators of chemokine receptor activity
EP2173714B9 (en) 2007-07-24 2013-04-10 Bristol-Myers Squibb Company Piperidine derivatives as modulators of chemokine receptor activity
TWI433838B (zh) * 2008-06-25 2014-04-11 必治妥美雅史谷比公司 作為趨化因子受體活性調節劑之六氫吡啶衍生物

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MX2012003656A (es) 2012-04-30
EA022150B1 (ru) 2015-11-30
EP2486013B1 (en) 2015-07-08
CL2012000882A1 (es) 2012-09-07
CN102648179B (zh) 2015-06-17
NZ599261A (en) 2013-10-25
EA201270468A1 (ru) 2012-11-30
AU2010303441A1 (en) 2012-05-03
CA2777032A1 (en) 2011-04-14
WO2011044309A1 (en) 2011-04-14
US20130178444A1 (en) 2013-07-11
CN102648179A (zh) 2012-08-22
US20110082113A1 (en) 2011-04-07
TW201118070A (en) 2011-06-01
PE20121109A1 (es) 2012-08-20
US8410139B2 (en) 2013-04-02
AR078543A1 (es) 2011-11-16
BR112012007755A2 (pt) 2015-09-15
KR20120083900A (ko) 2012-07-26
JP2013507377A (ja) 2013-03-04
CO6440510A2 (es) 2012-05-15
EP2486013A1 (en) 2012-08-15
IL219122A (en) 2015-04-30
IL219122A0 (en) 2012-06-28

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