JP2014501789A5 - - Google Patents

Download PDF

Info

Publication number
JP2014501789A5
JP2014501789A5 JP2013548604A JP2013548604A JP2014501789A5 JP 2014501789 A5 JP2014501789 A5 JP 2014501789A5 JP 2013548604 A JP2013548604 A JP 2013548604A JP 2013548604 A JP2013548604 A JP 2013548604A JP 2014501789 A5 JP2014501789 A5 JP 2014501789A5
Authority
JP
Japan
Prior art keywords
hydrogen
pharmaceutical composition
methyl
composition according
gluc
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.)
Granted
Application number
JP2013548604A
Other languages
English (en)
Other versions
JP2014501789A (ja
JP6132773B2 (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2012/020640 external-priority patent/WO2012096884A1/en
Publication of JP2014501789A publication Critical patent/JP2014501789A/ja
Publication of JP2014501789A5 publication Critical patent/JP2014501789A5/ja
Application granted granted Critical
Publication of JP6132773B2 publication Critical patent/JP6132773B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Description

別の実施態様において、R1は-C(O)R5であり、R2は水素であり、R3はエチルであり、かつR5は非置換のメチルである。
別の実施態様において、R1は-C(O)R5であり、R2は水素であり、R3は水素であり、かつR5は非置換のメチルである。
別の実施態様において、R1は-C(O)R5であり、R2glucであり、R3はエチルであり、かつR5は非置換のメチルである。
別の実施態様において、R1は-C(O)R5であり、R2はメチルであり、R3glucであり、かつR5は非置換のメチルである。
別の実施態様において、R1は-C(O)R5であり、R2はメチルであり、R3は水素であり、かつR5は非置換のメチルである。
一実施態様において、R1は水素であり、R2は水素であり、R3はエチルであり、かつR4はヒドロキシルである。
別の実施態様において、R1は水素であり、R2はメチルであり、R3はエチルであり、かつR4はヒドロキシルである。

Claims (10)

  1. 式(I)の化合物、又は、その医薬として許容し得る塩、溶媒和物、若しくは立体異性体を含む、医薬組成物:
    Figure 2014501789
    (式中、
    R1は、水素又は-C(O)R5であり;
    R2は、水素、メチル、又はグルクロニド(gluc)であり;
    R3は、水素、エチル、又はglucであり;
    R4は、水素又はヒドロキシルであり;
    R5は、-OR6で任意に置換された、1〜6個の炭素原子を含む直鎖状アルキルであり;かつ
    R6は、水素又はglucであり;
    R1が-C(O)R5であり、かつR5が非置換のメチルである場合:
    R2が水素であり、かつR3がエチルであるか;
    R2が水素であり、かつR3が水素であるか;
    R2がglucであり、かつR3がエチルであるか;
    R2がメチルであり、かつR3がglucであるか;又は
    R2がメチルであり、かつR3が水素であり;
    ただし、R2がメチルであり、R3がエチルであり、かつR4が水素である場合、R1は水素ではない。)。
  2. R1が-C(O)R5である、請求項1記載の医薬組成物。
  3. R5が、-OHで任意に置換されたメチルである、請求項2記載の医薬組成物。
  4. R5が、-O-glucで任意に置換されたメチルである、請求項2記載の医薬組成物。
  5. R1及びR2が両方とも水素である、請求項1記載の医薬組成物。
  6. R3がエチルである、請求項1記載の医薬組成物。
  7. R1が水素である、請求項1記載の医薬組成物。
  8. R3がエチルであり、かつR4がヒドロキシルである、請求項7記載の医薬組成物。
  9. 前記化合物が、
    Figure 2014501789
    又は、それらの医薬として許容し得る塩若しくは溶媒和物である、請求項1記載の医薬組成物。
  10. 請求項1記載の化合物、又はその医薬として許容し得る塩、溶媒和物若しくは立体異性体を含む、疾患又は障害を治療、管理又は予防するための医薬組成物であって、該疾患又は障害が、癌、血管新生と関連する障害、疼痛、黄斑変性若しくは関連症候群、皮膚病、肺障害、アスベスト関連障害、寄生虫病、免疫不全障害、CNS障害、CNS損傷、アテローム性動脈硬化症若しくは関連障害、機能不全性睡眠若しくは関連障害、異常ヘモグロビン症若しくは関連障害、又はTNFα関連障害である、前記医薬組成物。
JP2013548604A 2011-01-10 2012-01-09 Pde4及び/又はサイトカインの阻害剤としてのフェネチルスルホンイソインドリン誘導体 Active JP6132773B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161431350P 2011-01-10 2011-01-10
US61/431,350 2011-01-10
PCT/US2012/020640 WO2012096884A1 (en) 2011-01-10 2012-01-09 Phenethylsulfone isoindoline derivatives as inhibitors of pde 4 and/or cytokines

Publications (3)

Publication Number Publication Date
JP2014501789A JP2014501789A (ja) 2014-01-23
JP2014501789A5 true JP2014501789A5 (ja) 2015-02-26
JP6132773B2 JP6132773B2 (ja) 2017-05-24

Family

ID=45525016

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2013548604A Active JP6132773B2 (ja) 2011-01-10 2012-01-09 Pde4及び/又はサイトカインの阻害剤としてのフェネチルスルホンイソインドリン誘導体

Country Status (8)

Country Link
US (1) US8853175B2 (ja)
EP (1) EP2663549B1 (ja)
JP (1) JP6132773B2 (ja)
CN (1) CN103402980B (ja)
AU (1) AU2012205809B2 (ja)
ES (1) ES2673114T3 (ja)
MX (1) MX347928B (ja)
WO (1) WO2012096884A1 (ja)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20170087129A1 (en) * 2014-05-16 2017-03-30 Celgene Corporation Compositions and methods for the treatment of atherosclerotic cardiovascular diseases with pde4 modulators
WO2016055482A1 (en) * 2014-10-08 2016-04-14 Ucb Biopharma Sprl Isoindoline derivatives
BR112017019850A2 (pt) 2015-03-19 2018-06-05 Cipla Ltd ?processo melhorado para a preparação de apremilast?
WO2017089347A1 (en) 2015-11-25 2017-06-01 Inserm (Institut National De La Sante Et De La Recherche Medicale) Methods and pharmaceutical compositions for the treatment of braf inhibitor resistant melanomas
CN106547040B (zh) * 2016-11-23 2019-02-12 大连理工大学 一种高强度光子晶体膜及其制备方法
ES2902052T3 (es) 2017-02-28 2022-03-24 Kangpu Biopharmaceuticals Ltd Nuevo derivado de isoindolina, y composición farmacéutica y aplicación del mismo
WO2019144970A1 (zh) 2018-01-29 2019-08-01 石家庄智康弘仁新药开发有限公司 一种1H-咪唑并[4,5-b]吡啶-2(3H)-酮类化合物的晶型及其制备方法
MX2020009288A (es) 2018-03-07 2020-09-28 Amgen Europe Gmbh Metodos y composiciones de los profarmacos isoindolina-1,3-diona e isoindol utiles para el tratamiento del cancer, colitis ulcerosa y enfermedades inflamatorias relacionadas.

Family Cites Families (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3536809A (en) 1969-02-17 1970-10-27 Alza Corp Medication method
US3598123A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US3916899A (en) 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
US4008719A (en) 1976-02-02 1977-02-22 Alza Corporation Osmotic system having laminar arrangement for programming delivery of active agent
IE58110B1 (en) 1984-10-30 1993-07-14 Elan Corp Plc Controlled release powder and process for its preparation
US5073543A (en) 1988-07-21 1991-12-17 G. D. Searle & Co. Controlled release formulations of trophic factors in ganglioside-lipsome vehicle
IT1229203B (it) 1989-03-22 1991-07-25 Bioresearch Spa Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative.
US5120548A (en) 1989-11-07 1992-06-09 Merck & Co., Inc. Swelling modulated polymeric drug delivery device
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
US5733566A (en) 1990-05-15 1998-03-31 Alkermes Controlled Therapeutics Inc. Ii Controlled release of antiparasitic agents in animals
US5580578A (en) 1992-01-27 1996-12-03 Euro-Celtique, S.A. Controlled release formulations coated with aqueous dispersions of acrylic polymers
US5591767A (en) 1993-01-25 1997-01-07 Pharmetrix Corporation Liquid reservoir transdermal patch for the administration of ketorolac
WO1995003009A1 (en) 1993-07-22 1995-02-02 Oculex Pharmaceuticals, Inc. Method of treatment of macular degeneration
WO1995003807A1 (en) 1993-07-27 1995-02-09 The University Of Sydney Treatment of age-related macular degeneration
IT1270594B (it) 1994-07-07 1997-05-07 Recordati Chem Pharm Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida
IT1274549B (it) 1995-05-23 1997-07-17 Indena Spa Uso di flavanolignani per la preparazione di medicamenti ad attivita' antiproliferativa nei tumori dell'utero,dell'ovaio e del seno
US5800819A (en) 1996-01-25 1998-09-01 National Institute For Pharmaceutical Research And Development Federal Ministry Of Science And Technology Piper guineense, pterocarpus osun, eugenia caryophyllata, and sorghum bicolor extracts for treating sickle cell disease
HU228769B1 (en) 1996-07-24 2013-05-28 Celgene Corp Substituted 2(2,6-dioxopiperidin-3-yl)phthalimides and -1-oxoisoindolines and their use for production of pharmaceutical compositions for mammals to reduce the level of tnf-alpha
ES2529190T3 (es) 1996-07-24 2015-02-17 Celgene Corporation 2-(2,6-dioxopiperidin-3-il)-ftalimidas sustituidas por amino para reducir los niveles de TNF-alfa
US5635517B1 (en) 1996-07-24 1999-06-29 Celgene Corp Method of reducing TNFalpha levels with amino substituted 2-(2,6-dioxopiperidin-3-YL)-1-oxo-and 1,3-dioxoisoindolines
US6281230B1 (en) 1996-07-24 2001-08-28 Celgene Corporation Isoindolines, method of use, and pharmaceutical compositions
US6015803A (en) 1998-05-04 2000-01-18 Wirostko; Emil Antibiotic treatment of age-related macular degeneration
US6225348B1 (en) 1998-08-20 2001-05-01 Alfred W. Paulsen Method of treating macular degeneration with a prostaglandin derivative
US6001368A (en) 1998-09-03 1999-12-14 Protein Technologies International, Inc. Method for inhibiting or reducing the risk of macular degeneration
US6020358A (en) * 1998-10-30 2000-02-01 Celgene Corporation Substituted phenethylsulfones and method of reducing TNFα levels
AU2006200033B8 (en) 1998-10-30 2008-09-11 Celgene Corporation Substituted phenethylsulfones and methods of reducing TNF-alpha levels
US6667316B1 (en) 1999-11-12 2003-12-23 Celgene Corporation Pharmaceutically active isoindoline derivatives
US7182953B2 (en) 1999-12-15 2007-02-27 Celgene Corporation Methods and compositions for the prevention and treatment of atherosclerosis restenosis and related disorders
US8030343B2 (en) * 2000-06-08 2011-10-04 Celgene Corporation Pharmaceutically active isoindoline derivatives
WO2003041326A2 (en) 2001-11-09 2003-05-15 Matsushita Electric Industrial Co., Ltd. Moving picture coding method and apparatus
US6962940B2 (en) * 2002-03-20 2005-11-08 Celgene Corporation (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione: methods of using and compositions thereof
AU2003222034A1 (en) * 2002-03-20 2003-10-08 Celgene Corporation (-)-2-(1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl)-4-acetylaminoisoindoline-1,3-dione: methods of using and compositions thereof
US7323479B2 (en) 2002-05-17 2008-01-29 Celgene Corporation Methods for treatment and management of brain cancer using 1-oxo-2-(2,6-dioxopiperidin-3-yl)-4-methylisoindoline
US7393862B2 (en) 2002-05-17 2008-07-01 Celgene Corporation Method using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione for treatment of certain leukemias
US7968569B2 (en) 2002-05-17 2011-06-28 Celgene Corporation Methods for treatment of multiple myeloma using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione
US7189740B2 (en) 2002-10-15 2007-03-13 Celgene Corporation Methods of using 3-(4-amino-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione for the treatment and management of myelodysplastic syndromes
US20040087558A1 (en) * 2002-10-24 2004-05-06 Zeldis Jerome B. Methods of using and compositions comprising selective cytokine inhibitory drugs for treatment, modification and management of pain
US20050203142A1 (en) 2002-10-24 2005-09-15 Zeldis Jerome B. Methods of using and compositions comprising immunomodulatory compounds for treatment, modification and management of pain
US7776907B2 (en) * 2002-10-31 2010-08-17 Celgene Corporation Methods for the treatment and management of macular degeneration using cyclopropyl-N-{2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-3-oxoisoindoline-4-yl}carboxamide
US20040091455A1 (en) 2002-10-31 2004-05-13 Zeldis Jerome B. Methods of using and compositions comprising immunomodulatory compounds for treatment and management of macular degeneration
JP2006509743A (ja) * 2002-10-31 2006-03-23 セルジーン・コーポレーション 黄斑変性の治療および管理のための選択的サイトカイン阻害薬の使用方法およびそれを含む組成物
US7563810B2 (en) 2002-11-06 2009-07-21 Celgene Corporation Methods of using 3-(4-amino-1-oxo-1,3-dihydroisoindol-2-yl)-piperidine-2,6-dione for the treatment and management of myeloproliferative diseases
JP5269281B2 (ja) 2002-12-30 2013-08-21 セルジーン コーポレイション フルオロアルコキシ置換1,3−ジヒドロイソインドリル化合物およびそれらの医薬としての使用
US20050100529A1 (en) 2003-11-06 2005-05-12 Zeldis Jerome B. Methods of using and compositions comprising immunomodulatory compounds for the treatment and management of asbestos-related diseases and disorders
EP1694328A4 (en) 2003-12-02 2010-02-17 Celgene Corp METHOD AND COMPOSITIONS FOR THE TREATMENT AND SUPPLY OF HEMOGLOBINOPATHY AND ANEMIA
US20050143344A1 (en) 2003-12-30 2005-06-30 Zeldis Jerome B. Methods and compositions using immunomodulatory compounds for the treatment and management of central nervous system disorders or diseases
ZA200607799B (en) 2004-03-22 2008-06-25 Celgene Corp Methods of using and compositions comprising immuno-modulatory compounds for the treatment and management of skin diseases or disorders
US20050222209A1 (en) 2004-04-01 2005-10-06 Zeldis Jerome B Methods and compositions for the treatment, prevention or management of dysfunctional sleep and dysfunctional sleep associated with disease
US20080213213A1 (en) * 2004-04-14 2008-09-04 Zeldis Jerome B Method For the Treatment of Myelodysplastic Syndromes Using (+)-2-[1-(3-Ethoxy-4-Methoxyphenyl)-2-Methylsulfonylethyl]-4-Acetylaminoisoindoline-1,3-Dione
WO2005105088A2 (en) 2004-04-23 2005-11-10 Celgene Corporation Methods of using and compositions comprising immunomodulatory compounds for the treatment and management of pulmonary hypertension
MXPA06012279A (es) * 2004-04-23 2007-01-31 Celgene Corp Metodos de uso y composiciones que comprenden moduladores de pde4 para el tratamiento y manejo de la hipertension pulmonar.
US7244759B2 (en) * 2004-07-28 2007-07-17 Celgene Corporation Isoindoline compounds and methods of making and using the same
CN101098694A (zh) 2004-11-12 2008-01-02 细胞基因公司 使用免疫调节化合物治疗和控制寄生性疾病的方法和组合物
US20060122228A1 (en) 2004-11-23 2006-06-08 Zeldis Jerome B Methods and compositions using immunomodulatory compounds for treatment and management of central nervous system injury
EP1924250B1 (en) 2004-12-01 2017-01-04 Celgene Corporation Methods and compositions comprising immunomodulatory compounds for use for the treatment of immunodeficiency disorders
BRPI0519030A2 (pt) * 2004-12-13 2008-12-23 Celgene Corp mÉtodos de tratamento, prevenÇço, ou controle de inflamaÇço das vias aÉreas e de uma doenÇa ou distérbio das vias aÉreas ou pulmonar, e, composiÇço farmacÊutica
ATE499112T1 (de) 2005-09-01 2011-03-15 Celgene Corp Immunologische verwendungen von immunmodulatorischen verbindungen für einen impfstoff und therapie gegen infektionskrankheiten
ZA200805795B (en) * 2005-12-29 2009-10-28 Celgene Corp Methods for treating cutaneous lupus using aminoisoindoline compounds
US20070155791A1 (en) 2005-12-29 2007-07-05 Zeldis Jerome B Methods for treating cutaneous lupus using aminoisoindoline compounds
JP5852565B2 (ja) * 2009-06-18 2016-02-03 コンサート ファーマシューティカルズ インコーポレイテッド PDE4およびTNF−α阻害剤としての重水素化イソインドリン−1,3−ジオン誘導体

Similar Documents

Publication Publication Date Title
JP2014501789A5 (ja)
JP2015508092A5 (ja)
JP2016503793A5 (ja)
JP2010504973A5 (ja)
JP2014508811A5 (ja)
JP2015537020A5 (ja)
JP2013515073A5 (ja)
JP2016505614A5 (ja)
JP2013537203A5 (ja)
JP2015520140A5 (ja)
JP2010502627A5 (ja)
JP2017514910A5 (ja)
JP2018518537A5 (ja)
JP2015509534A5 (ja)
JP2007508361A5 (ja)
JP2014513051A5 (ja)
JP2013500986A5 (ja)
JP2016503799A5 (ja)
JP2016534063A5 (ja)
JP2019513745A5 (ja)
JP2013544860A5 (ja)
JP2020502047A5 (ja)
JP2017531688A5 (ja)
JP2013542261A5 (ja)
JP2017522277A5 (ja)