BRPI0408338A - piperidinas substituìdas como novos inibidores de mdm2-p53 - Google Patents

piperidinas substituìdas como novos inibidores de mdm2-p53

Info

Publication number
BRPI0408338A
BRPI0408338A BRPI0408338-5A BRPI0408338A BRPI0408338A BR PI0408338 A BRPI0408338 A BR PI0408338A BR PI0408338 A BRPI0408338 A BR PI0408338A BR PI0408338 A BRPI0408338 A BR PI0408338A
Authority
BR
Brazil
Prior art keywords
mdm2
formula
replaced
new inhibitors
iii
Prior art date
Application number
BRPI0408338-5A
Other languages
English (en)
Inventor
Kyungjin Kim
Emily Aijun Liu
Steven Gregory Mischke
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 BRPI0408338A publication Critical patent/BRPI0408338A/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/36—Heterocyclic 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
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/52—Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/96—Sulfur atom

Abstract

"PIPERIDINAS SUBSTITUìDAS COMO NOVOS INIBIDORES DE MDM2-p53". A presente invenção proporciona compostos tendo a fórmula (II) ou a fórmula (III) e os sais farmaceuticamente aceitáveis dos mesmos; em que X, n, e R~ 1~-R~ 12~ são definidos aqui. A invenção também proporciona uma composição farmacêutica compreendendo uma quantidade terapeuticamente efetiva de um composto representado pela fórmula (II) ou (III) e um veículo ou excipiente farmaceuticamente aceitável. Os compostos são úteis para o tratamento de câncer.
BRPI0408338-5A 2003-03-13 2004-03-08 piperidinas substituìdas como novos inibidores de mdm2-p53 BRPI0408338A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US45438703P 2003-03-13 2003-03-13
PCT/EP2004/002339 WO2004080460A1 (en) 2003-03-13 2004-03-08 SUBSTITUTED PIPERIDINES AS NOVEL MDM2-p53 INHIBITORS

Publications (1)

Publication Number Publication Date
BRPI0408338A true BRPI0408338A (pt) 2006-03-21

Family

ID=32990900

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0408338-5A BRPI0408338A (pt) 2003-03-13 2004-03-08 piperidinas substituìdas como novos inibidores de mdm2-p53

Country Status (11)

Country Link
US (2) US6916833B2 (pt)
EP (1) EP1605941A1 (pt)
JP (1) JP4468897B2 (pt)
KR (1) KR100755767B1 (pt)
CN (1) CN100372837C (pt)
AU (1) AU2004218842B2 (pt)
BR (1) BRPI0408338A (pt)
CA (1) CA2516145A1 (pt)
MX (1) MXPA05009611A (pt)
RU (1) RU2333201C2 (pt)
WO (1) WO2004080460A1 (pt)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2037919A2 (en) * 2006-06-30 2009-03-25 Schering Corporation Method of using substituted piperidines that increase p53 activity
CN101595107A (zh) 2006-06-30 2009-12-02 先灵公司 能提高p53活性的有取代哌啶及其用途
KR20090090383A (ko) 2006-12-14 2009-08-25 다이이찌 산쿄 가부시키가이샤 이미다조티아졸 유도체
WO2009151069A1 (ja) 2008-06-12 2009-12-17 第一三共株式会社 ４，７－ジアザスピロ［２．５］オクタン環構造を有するイミダゾチアゾール誘導体
US8354444B2 (en) * 2008-09-18 2013-01-15 Hoffmann-La Roche Inc. Substituted pyrrolidine-2-carboxamides
EP2749554B1 (en) * 2009-04-22 2017-12-20 SMA Therapeutics, Inc. 2,5-disubstituted arylsulfonamide CCR3 antagonists
EP2488028B1 (en) 2009-10-14 2020-08-19 Merck Sharp & Dohme Corp. Substituted piperidines that increase p53 activity and the uses thereof
NZ600430A (en) 2009-11-12 2014-06-27 Univ Michigan Spiro-oxindole mdm2 antagonists
US10159669B2 (en) * 2010-03-02 2018-12-25 Ian H. Chan Individual and combination of mdivi-1 and nutlin-3 for topical or intravitreal ophthalmic use
JO2998B1 (ar) * 2010-06-04 2016-09-05 Amgen Inc مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان
FR2967072B1 (fr) 2010-11-05 2013-03-29 Univ Dundee Procede pour ameliorer la production de virus et semences vaccinales influenza
EA201390682A1 (ru) 2010-11-12 2014-01-30 Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган Спирооксиндольные антагонисты mdm2
JP2014513699A (ja) 2011-05-11 2014-06-05 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン スピロ−オキシインドールｍｄｍ２アンタゴニスト
WO2013062923A1 (en) 2011-10-28 2013-05-02 Merck Sharp & Dohme Corp. MACROCYCLES THAT INCREASE p53 ACTIVITY AND THE USES THEREOF
US9062071B2 (en) 2011-12-21 2015-06-23 Merck Sharp & Dohme Corp. Substituted piperidines as HDM2 inhibitors
CA2895504A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
US9540377B2 (en) 2013-01-30 2017-01-10 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as HDM2 inhibitors
JOP20200296A1 (ar) * 2013-06-10 2017-06-16 Amgen Inc عمليات صنع وأشكال بلورية من mdm2 مثبط
KR101851270B1 (ko) * 2015-07-10 2018-04-25 고려대학교 산학협력단 자연 살해세포의 대량증식 방법 및 배양용 조성물
US11192898B2 (en) 2016-04-06 2021-12-07 The Regents Of The University Of Michigan MDM2 protein degraders
CA3020281A1 (en) 2016-04-06 2017-10-12 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
PL3458101T3 (pl) 2016-05-20 2021-05-31 F. Hoffmann-La Roche Ag Koniugaty PROTAC-przeciwciało i sposoby ich stosowania
CN108088727B (zh) * 2016-11-21 2020-07-07 中国科学院大连化学物理研究所 一种离体体液中蛋白质的预处理方法
JP2022504541A (ja) 2018-10-08 2022-01-13 ザ リージェンツ オブ ザ ユニバーシティー オブ ミシガン 低分子ｍｄｍ２タンパク質デグレーダー
EP4121043A1 (en) 2020-03-19 2023-01-25 Kymera Therapeutics, Inc. Mdm2 degraders and uses thereof
WO2023056069A1 (en) 2021-09-30 2023-04-06 Angiex, Inc. Degrader-antibody conjugates and methods of using same

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE7708555L (sv) * 1976-08-05 1978-02-06 Delmar Chem 4-arylpiperidinderivat och forfarande for framstellning derav
US4286095A (en) * 1976-08-05 1981-08-25 Canada Packers Inc. 4-Arylpiperidine derivatives
US6274735B1 (en) * 1998-08-10 2001-08-14 Hoffmann-La Roche Inc. Process and intermediates for preparation of substituted piperidines
GB9819860D0 (en) 1998-09-12 1998-11-04 Zeneca Ltd Chemical compounds
GB9912961D0 (en) * 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors

Also Published As

Publication number Publication date
AU2004218842B2 (en) 2009-11-12
WO2004080460A1 (en) 2004-09-23
CA2516145A1 (en) 2004-09-23
US7060713B2 (en) 2006-06-13
JP4468897B2 (ja) 2010-05-26
US20050171157A1 (en) 2005-08-04
MXPA05009611A (es) 2005-10-18
KR20050106505A (ko) 2005-11-09
US6916833B2 (en) 2005-07-12
RU2333201C2 (ru) 2008-09-10
CN100372837C (zh) 2008-03-05
KR100755767B1 (ko) 2007-09-10
AU2004218842A1 (en) 2004-09-23
JP2006519767A (ja) 2006-08-31
RU2005131501A (ru) 2006-05-27
CN1758909A (zh) 2006-04-12
EP1605941A1 (en) 2005-12-21
US20040180929A1 (en) 2004-09-16

Similar Documents

Publication Publication Date Title
BRPI0408338A (pt) piperidinas substituìdas como novos inibidores de mdm2-p53
DK1265606T3 (da) Celleadhæsionsinhibitorer
BR0311806A (pt) Derivados heteroaril benzocondensado-amida de tienopiridinas úteis como agentes terapêuticos, composições farmacêuticas que os incluem e métodos para o seu uso
BRPI0507903A (pt) derivados de quinazolina e composição farmacêutica compreendendo os mesmos
BR0317435A (pt) Derivados de pirimidina para o tratamento do crescimento celular anormal
BR0317455A (pt) Derivados de pirrol-pirazol substituìdos como inibidores de quinase
BR0212378A (pt) Inibidores de 17beta-hidroxiesteróide desidrogenase tipo 3 para o tratamento de doenças dependentes de androgênio
ATE307810T1 (de) Imidazol-2-carbonsäureamid derivate als raf- kinase-inhibitoren
BR0205889A (pt) Pirazolopirimidinas como agentes tepapêuticos
BRPI0410630A (pt) antagonista de nk1
BR0206433A (pt) Composto, composição farmacêutica, processo para a prepapação de um composto, e, uso de um composto
BR0209127A (pt) compostos, composições farmacêuticas, métodos para o tratamento de dores, métodos para a modulação de uma resposta farmacológica e usos de compostos
BR0209129A (pt) Compostos, composições farmacêuticas, métodos para tratamento de dores, métodos para modulação de uma resposta farmacológica e usos de compostos
DK1767535T3 (da) Syntese af epothiloner, mellemprodukter deraf, analoge og deres anvendelse
BR0315580A (pt) Derivados de metileno uréia
BR0212968A (pt) Composição farmacêutica, composto, e, método para tratar ou prevenir condições mediadas pelo ccr2, mcp-1 ou pela interação destes
BRPI0408353A (pt) composto, composição farmacêutica, métodos para o tratamento de neoplasias suscetìveis e para o tratamento de infecções virais, e, uso de um composto
DE60324544D1 (de) Muskarin antagonisten
BRPI0410669A (pt) inibidores de caspase e usos dos mesmo
BR0309188A (pt) Compostos pirazolo como agentes antiinflamatórios e analgésicos
BR0210028A (pt) Agentes antibacterianos
ATE543803T1 (de) 3-ä2-(3-azylamino-2-oxo-2h-pyridin-1- yl)acetylaminoü-4-oxopentansäurederivate und deren verwendung als caspase-inhibitoren
BR0309305A (pt) Compostos de imidazol como agentes antiinflamatórios e analgésicos
BR9908125A (pt) Composto, composto dimérico, composição farmacêutica, uso do composto, processo compreendendo inibir células de câncer, e, processo terapêutico
BR0209128A (pt) Compostos, composições farmacêuticas, métodos para o tratamento de dores, métodos para a modulação de uma resposta farmacológica e usos de compostos

Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 8A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2159 DE 22/05/2012.