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PE20060166A1 - Derivados de amida como inhibidores de proteinas de apoptosis (iap) - Google Patents

Derivados de amida como inhibidores de proteinas de apoptosis (iap)

Info

Publication number
PE20060166A1
PE20060166A1 PE2005000384A PE2005000384A PE20060166A1 PE 20060166 A1 PE20060166 A1 PE 20060166A1 PE 2005000384 A PE2005000384 A PE 2005000384A PE 2005000384 A PE2005000384 A PE 2005000384A PE 20060166 A1 PE20060166 A1 PE 20060166A1
Authority
PE
Peru
Prior art keywords
alkyl
iap
methyl
apoptosis proteins
inhibitors
Prior art date
Application number
PE2005000384A
Other languages
English (en)
Inventor
Mark G Palermo
Sushil Kumar Sharma
Run-Ming Wang
Yanlin Zhang
Yaping Wang
Wojciech Wrona
Mark G Charest
Feng He
Gang Liu
Fan Yang
Zhuoliang Chen
Leigh Zawel
Christopher Straub
Original Assignee
Novartis 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34962601&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20060166(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20060166A1 publication Critical patent/PE20060166A1/es

Links

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26—Androgens
    • 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
    • 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
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    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/06—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 radicals, substituted by hetero atoms, attached to ring carbon atoms
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
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    • 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
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    • 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
    • C07D405/10—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 carbon chain containing aromatic rings
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    • 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
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    • 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
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    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
  • Pyrrole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE AMIDA DE FORMULA (I), EN DONDE R1 Y R2 SON INDEPENDIENTEMENTE H O ALQUILO(C1-C4); R3 ES H, -CF3, -C2F5, ALQUILO(C1-C4), ENTRE OTROS; R4 ES ALQUILO, ALQUENILO, ALQUINILO(C1-C16), CICLOALQUILO, -(CH2)(1-6)-Z1, -(CH2)0-6-FENILO O -(CH2)0-6-HET, ENTRE OTROS; R5 ES H, ALQUILO(C1-C10), ALQUILO(C1-C10)-ARILO, -C(O)-(CH2)0-6-FENILO, ARILO, ENTRE OTROS; U ES LA ESTRUCTURA (II), EN DONDE n ES DE 0 A 5; X ES -CH O N; Ra Y Rb SON INDEPENDIENTEMENTE O, S, O N O ALQUILO(C0-C8). SON COMPUESTOS PREFERIDOS: N-[1-CICLOHEXIL-2-OXO-2-(6-FENETIL-OCTAHIDRO-PIRROLO-[2,3-c]-PIRIDIN-1-IL)-ETIL]-2-METIL-AMINO-ACETAMIDA, N-{2-[2-BENCILOXI-IMINO-METIL)-PIRROLIDIN-1-IL}-1-CICLOHEXIL-2-OXO-ETIL-2-METIL-AMINO-PROPIONAMIDA, ENTRE OTROS. ESTOS COMPUESTOS INHIBEN EL ENLACE DE LA PROTEINA Smac AL INHIBIDOR DE PROTEINAS DE APOPTOSIS (IAP), POR LO QUE SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES PROLIFERATIVAS COMO EL CANCER
PE2005000384A 2004-04-07 2005-04-06 Derivados de amida como inhibidores de proteinas de apoptosis (iap) PE20060166A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US56018604P 2004-04-07 2004-04-07

Publications (1)

Publication Number Publication Date
PE20060166A1 true PE20060166A1 (es) 2006-04-25

Family

ID=34962601

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2009001297A PE20110102A1 (es) 2004-04-07 2005-04-06 Derivados de n-(2-oxo-2-pirrolidinil-1-il)etil-2-amino-acetamida como inhibidores de proteinas de apoptosis (iap)
PE2005000384A PE20060166A1 (es) 2004-04-07 2005-04-06 Derivados de amida como inhibidores de proteinas de apoptosis (iap)

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2009001297A PE20110102A1 (es) 2004-04-07 2005-04-06 Derivados de n-(2-oxo-2-pirrolidinil-1-il)etil-2-amino-acetamida como inhibidores de proteinas de apoptosis (iap)

Country Status (31)

Country Link
US (4) US7419975B2 (es)
EP (3) EP1735307B1 (es)
JP (3) JP4691549B2 (es)
KR (2) KR20080083220A (es)
CN (1) CN1964970B (es)
AR (1) AR048927A1 (es)
AU (1) AU2005231956B2 (es)
BR (1) BRPI0509721A (es)
CA (1) CA2560162C (es)
CY (1) CY1113511T1 (es)
DK (1) DK2253614T3 (es)
EC (1) ECSP066893A (es)
ES (2) ES2394441T3 (es)
HR (1) HRP20121023T1 (es)
IL (1) IL178104A (es)
MA (1) MA28630B1 (es)
ME (1) ME02125B (es)
MY (1) MY165401A (es)
NO (1) NO20065114L (es)
NZ (1) NZ549925A (es)
PE (2) PE20110102A1 (es)
PL (1) PL2253614T3 (es)
PT (1) PT2253614E (es)
RS (1) RS52545B (es)
RU (1) RU2425838C2 (es)
SG (1) SG152225A1 (es)
SI (1) SI2253614T1 (es)
TN (1) TNSN06323A1 (es)
TW (1) TWI417092B (es)
WO (1) WO2005097791A1 (es)
ZA (1) ZA200607696B (es)

Families Citing this family (146)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2005228950B2 (en) 2004-03-23 2012-02-02 Genentech, Inc. Azabicyclo-octane inhibitors of IAP
NZ549925A (en) * 2004-04-07 2010-08-27 Novartis Ag Inhibitors of IAP
EP1778718B1 (en) 2004-07-02 2014-10-08 Genentech, Inc. Inhibitors of iap
ES2475207T3 (es) 2004-07-15 2014-07-10 Tetralogic Pharmaceuticals Corporation Compuestos de unión a IAP
KR20120127754A (ko) * 2004-12-20 2012-11-23 제넨테크, 인크. Ｉａｐ의 피롤리딘 억제제
EP1879574A2 (en) * 2005-02-23 2008-01-23 Prexa Pharmaceuticals, Inc. Multimediator 5-ht6 receptor antagonists, and uses related thereto
JP5198880B2 (ja) 2005-02-25 2013-05-15 テトラロジック ファーマシューティカルズ コーポレーション 二量体ｉａｐ阻害剤
WO2006107964A2 (en) * 2005-04-06 2006-10-12 Novartis Ag Processes to prepare 6-phenethyl-octahydro-pyrrolo [2 , 3-c] pyridine and related compounds
US7772177B2 (en) 2005-05-18 2010-08-10 Aegera Therapeutics, Inc. BIR domain binding compounds
US20100256046A1 (en) * 2009-04-03 2010-10-07 Tetralogic Pharmaceuticals Corporation Treatment of proliferative disorders
WO2007021825A2 (en) * 2005-08-09 2007-02-22 Tetralogic Pharmaceuticals Corporation Treatment of proliferative disorders
KR20080067357A (ko) * 2005-10-25 2008-07-18 에게라 쎄라퓨틱스 인코포레이티드 Ｉａｐ ｂｉｒ 도메인 결합 화합물
CA2632807A1 (en) * 2005-12-19 2007-09-20 Genentech, Inc. Inhibitors of iap
EP1965865B1 (en) * 2005-12-20 2018-05-16 Novartis AG Combination of an iap-inhibitor and a taxane
TWI504597B (zh) 2006-03-16 2015-10-21 Pharmascience Inc 結合於細胞凋亡抑制蛋白（ｉａｐ）之桿狀病毒ｉａｐ重複序列（ｂｉｒ）區域之化合物
BRPI0709749A2 (pt) * 2006-04-05 2011-07-26 Novartis Ag combinaÇÕes de agentes terapÊuticos para tratamento de cÂncer
RU2008143554A (ru) * 2006-04-05 2010-05-10 Новартис АГ (CH) Комбинации терапевтических агентов для лечения рака
US8168383B2 (en) 2006-04-14 2012-05-01 Cell Signaling Technology, Inc. Gene defects and mutant ALK kinase in human solid tumors
SI2450437T1 (sl) 2006-04-14 2017-12-29 Cell Signaling Technology Inc. Okvarjenost genov in mutantna ALK kinaza v človeških solidnih tumorjih
MX2008014502A (es) * 2006-05-16 2008-11-27 Aegera Therapeutics Inc Compuestos de union a dominio de repeticion de proteinas inhibidoras de apoptosis baculovirales de las proteinas inhibidoras de apoptosis.
SG10201407457UA (en) 2006-05-16 2014-12-30 Pharmascience Inc Iap bir domain binding compounds
WO2008014240A2 (en) * 2006-07-24 2008-01-31 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
US20100144650A1 (en) * 2006-07-24 2010-06-10 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
JP5452223B2 (ja) * 2006-07-24 2014-03-26 テトラロジック ファーマシューティカルズ コーポレーション Ｉａｐ阻害剤
EP2409984A1 (en) 2006-07-24 2012-01-25 Tetralogic Pharmaceuticals Corporation Dimeric IAP Antagonists
US20100056495A1 (en) * 2006-07-24 2010-03-04 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
PE20110217A1 (es) * 2006-08-02 2011-04-01 Novartis Ag DERIVADOS DE 2-OXO-ETIL-AMINO-PROPIONAMIDA-PIRROLIDIN-2-IL-SUSTITUIDOS COMO INHIBIDORES DEL ENLACE DE LA PROTEINA Smac AL INHIBIDOR DE LA PROTEINA DE APOPTOSIS
US8044209B2 (en) 2006-10-12 2011-10-25 Novartis Ag Pyrrolydine derivatives as IAP inhibitors
KR20090082221A (ko) * 2006-10-19 2009-07-29 노파르티스 아게 유기 화합물
MX2009005551A (es) * 2006-11-28 2009-06-08 Novartis Ag Uso de inhibidores de iap para el tratamiento de leucemia mieloide aguda.
US8492429B2 (en) * 2006-11-28 2013-07-23 Novartis Ag Combination of IAP inhibitors and FLT3 inhibitors
US8063218B2 (en) * 2006-12-19 2011-11-22 Genentech, Inc. Imidazopyridine inhibitors of IAP
WO2008109057A1 (en) * 2007-03-02 2008-09-12 Dana-Farber Cancer Institute, Inc. Organic compounds and their uses
BRPI0810178A2 (pt) 2007-04-12 2014-09-23 Joyant Pharmaceuticals Inc Dímeros e trímeros miméticos de smac úteis como agentes anticâncer
PE20090211A1 (es) * 2007-04-30 2009-04-02 Genentech Inc Inhibidores de las iap
EP2156189A1 (en) * 2007-05-07 2010-02-24 Tetralogic Pharmaceuticals Corp. Tnf gene expression as a biomarker of sensitivity to antagonists of inhibitor of apoptosis proteins
US20100203012A1 (en) * 2007-05-30 2010-08-12 Aegera Therapeutics, Inc. Iap bir domain binding compounds
SI2240506T1 (sl) * 2008-01-11 2013-04-30 Genentech, Inc. Inhibitorji IAP
BRPI0906785A2 (pt) * 2008-01-24 2015-07-14 Tetralogic Pharm Corp Composto, composição farmacêutica, e, métodos para induzir a apoptose em uma célula, para tratar câncer e uma doença autoimune
US20110117081A1 (en) * 2008-05-05 2011-05-19 Aegera Therapeutics, Inc. Functionalized pyrrolidines and use thereof as iap inhibitors
EP2698158B1 (en) 2008-05-16 2021-06-30 Novartis AG Immunomodulation by IAP Inhibitors
US20110171171A1 (en) * 2008-06-27 2011-07-14 Aegera Therapeutics, Inc. Bridged secondary amines and use thereof as iap bir domain binding compounds
NZ590550A (en) 2008-08-02 2013-05-31 Genentech Inc Inhibitors of Apoptosis (IAP) for treating cancer
AU2009282978A1 (en) * 2008-08-16 2010-02-25 Genentech, Inc. Azaindole inhibitors of IAP
EP2328412A4 (en) * 2008-09-17 2012-03-14 Tetralogic Pharm Corp IPA INHIBITORS
US8841067B2 (en) 2009-01-09 2014-09-23 Dana-Farber Cancer Institute, Inc. NOL3 is a predictor of patient outcome
WO2010138496A1 (en) * 2009-05-28 2010-12-02 Tetralogic Pharmaceuticals Corp. Iap inhibitors
EA201171415A1 (ru) * 2009-05-28 2013-01-30 Тетралоджик Фармасьютикалз Корп. Ингибиторы белков семейства iap
CN101928326B (zh) * 2009-06-24 2015-07-08 中国人民解放军军事医学科学院毒物药物研究所 取代的氨酰基五元杂环烷类化合物及其用途
US8283372B2 (en) 2009-07-02 2012-10-09 Tetralogic Pharmaceuticals Corp. 2-(1H-indol-3-ylmethyl)-pyrrolidine dimer as a SMAC mimetic
WO2011016576A1 (en) 2009-08-04 2011-02-10 Takeda Pharmaceutical Company Limited Alanine derivatives as inhibitors of apoptosis proteins
IN2012DN00858A (es) * 2009-08-12 2015-07-10 Novartis Ag
US20120196793A1 (en) 2009-09-18 2012-08-02 Firestone Brant G Biomarkers for iap inhibitor compounds
WO2011059763A2 (en) 2009-10-28 2011-05-19 Joyant Pharmaceuticals, Inc. Dimeric smac mimetics
AU2011214057B2 (en) 2010-02-12 2016-11-17 Pharmascience Inc. IAP BIR domain binding compounds
UY33227A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de la cdk4/6
AU2011242988B2 (en) * 2010-04-19 2013-02-07 Sri International Compositions and method for the treatment of multiple myeloma
WO2012052758A1 (en) 2010-10-22 2012-04-26 Astrazeneca Ab Response biomarkers for iap antagonists in human cancers
GB201106817D0 (en) 2011-04-21 2011-06-01 Astex Therapeutics Ltd New compound
AU2012315986A1 (en) 2011-09-30 2014-04-17 Srinivas Chunduru Smac mimetic (birinapant) for use in the treatment of proliferative diseases (cancer)
GB201121133D0 (en) 2011-12-08 2012-01-18 Dow Corning Hydrolysable silanes
GB201121128D0 (en) 2011-12-08 2012-01-18 Dow Corning Treatment of filler with silane
GB201121122D0 (en) 2011-12-08 2012-01-18 Dow Corning Hydrolysable silanes and elastomer compositions containing them
GB201121124D0 (en) 2011-12-08 2012-01-18 Dow Corning Hydrolysable silanes
GB201121132D0 (en) * 2011-12-08 2012-01-18 Dow Corning Modifying polymeric materials by amines
US20130196927A1 (en) * 2012-01-27 2013-08-01 Christopher BENETATOS Smac Mimetic Therapy
CA2871995A1 (en) 2012-05-04 2013-11-07 Novartis Ag Biomarkers for iap inhibitor therapy
KR20140011773A (ko) * 2012-07-19 2014-01-29 한미약품 주식회사 이중 저해 활성을 갖는 헤테로고리 유도체
US9498532B2 (en) 2013-03-13 2016-11-22 Novartis Ag Antibody drug conjugates
US9498543B2 (en) 2013-03-15 2016-11-22 Novartis Ag Antibody drug conjugates
US20140303090A1 (en) * 2013-04-08 2014-10-09 Tetralogic Pharmaceuticals Corporation Smac Mimetic Therapy
ES2982449T3 (es) 2013-06-25 2024-10-16 Walter & Eliza Hall Inst Medical Res Miméticos Smac para su uso en el tratamiento de una infección persistente por VIH
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
US9249151B2 (en) * 2013-08-23 2016-02-02 Boehringer Ingelheim International Gmbh Bis-amido pyridines
US9278978B2 (en) 2013-08-23 2016-03-08 Boehringer Ingelheim International Gmbh 6-Alkynyl Pyridine
SI3083616T1 (sl) 2013-12-20 2021-12-31 Astex Therapeutics Limited Biciklične heterociklične spojine in njihova uporaba pri zdravljenju
US10441654B2 (en) 2014-01-24 2019-10-15 Children's Hospital Of Eastern Ontario Research Institute Inc. SMC combination therapy for the treatment of cancer
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
EP3151920B1 (en) 2014-06-04 2025-08-06 Sanford-Burnham Medical Research Institute Use of inhibitor of apoptosis protein (iap) antagonists in hiv therapy
US10786578B2 (en) 2014-08-05 2020-09-29 Novartis Ag CKIT antibody drug conjugates
AU2015302959B2 (en) 2014-08-12 2018-09-20 Novartis Ag Anti-CDH6 antibody drug conjugates
WO2016079527A1 (en) 2014-11-19 2016-05-26 Tetralogic Birinapant Uk Ltd Combination therapy
WO2016097773A1 (en) 2014-12-19 2016-06-23 Children's Cancer Institute Therapeutic iap antagonists for treating proliferative disorders
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
HK1247204A1 (zh) 2015-01-20 2018-09-21 Arvinas Operations, Inc. 用於雄激素受体的靶向降解的化合物和方法
CN104592214A (zh) * 2015-02-13 2015-05-06 佛山市赛维斯医药科技有限公司 含葡萄糖酰胺吡啶和烷氧吡嗪结构的化合物及用途
US20180147202A1 (en) 2015-06-05 2018-05-31 Arvinas, Inc. TANK-BINDING KINASE-1 PROTACs AND ASSOCIATED METHODS OF USE
US20190194315A1 (en) 2015-06-17 2019-06-27 Novartis Ag Antibody drug conjugates
RU2018105094A (ru) * 2015-07-13 2019-08-14 Арвинас, Инк. Модуляторы протеолиза на основе аланина и связанные с ними способы применения
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
MA44334A (fr) 2015-10-29 2018-09-05 Novartis Ag Conjugués d'anticorps comprenant un agoniste du récepteur de type toll
CN105566447B (zh) * 2016-01-20 2019-09-20 广东工业大学 一种凋亡抑制蛋白的类肽拮抗剂及其合成方法与应用
CN105585583B (zh) * 2016-01-20 2018-04-13 广东工业大学 一种非肽类凋亡抑制蛋白拮抗剂及其合成方法与应用
CN106188098B (zh) * 2016-07-06 2017-11-03 广东工业大学 一种杂化抗癌药物及其制备方法与应用
JP7094566B2 (ja) * 2016-08-29 2022-07-04 ザ・リージェンツ・オブ・ザ・ユニバーシティ・オブ・ミシガン Ａｌｋ阻害剤としてのアミノピリミジン類
JP6899993B2 (ja) * 2016-10-04 2021-07-07 国立医薬品食品衛生研究所長 複素環化合物
US11458123B2 (en) 2016-11-01 2022-10-04 Arvinas Operations, Inc. Tau-protein targeting PROTACs and associated methods of use
EP3548483A4 (en) 2016-12-01 2020-06-10 Arvinas Operations, Inc. Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
KR20250117470A (ko) 2016-12-23 2025-08-04 아비나스 오퍼레이션스, 인코포레이티드 급속 진행성 섬유육종 폴리펩티드의 표적화 분해를 위한 화합물 및 방법
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
WO2018118598A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
US10994015B2 (en) 2016-12-23 2021-05-04 Arvinas Operations, Inc. EGFR proteolysis targeting chimeric molecules and associated methods of use
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
IL300417A (en) 2017-01-26 2023-04-01 Arvinas Operations Inc Bifunctional benzothiophene compounds, preparations containing them and their use in therapy
JOP20190187A1 (ar) 2017-02-03 2019-08-01 Novartis Ag مترافقات عقار جسم مضاد لـ ccr7
EP3592868B1 (en) 2017-03-06 2022-11-23 Novartis AG Methods of treatment of cancer with reduced ubb expression
WO2018185618A1 (en) 2017-04-03 2018-10-11 Novartis Ag Anti-cdh6 antibody drug conjugates and anti-gitr antibody combinations and methods of treatment
AR111651A1 (es) 2017-04-28 2019-08-07 Novartis Ag Conjugados de anticuerpos que comprenden agonistas del receptor de tipo toll y terapias de combinación
WO2018215937A1 (en) 2017-05-24 2018-11-29 Novartis Ag Interleukin-7 antibody cytokine engrafted proteins and methods of use in the treatment of cancer
MX2019014023A (es) 2017-05-24 2020-02-17 Novartis Ag Proteinas de anticuerpo injertadas con citocina y metodos de uso en el tratamiento del cancer.
US20200362058A1 (en) 2017-05-24 2020-11-19 Novartis Ag Antibody-cytokine engrafted proteins and methods of use
US11358950B2 (en) * 2017-11-13 2022-06-14 Chia Tai Tiangqing Pharmaceutical Group Co., Ltd. SMAC mimetics used as IAP inhibitors and use thereof
US11065231B2 (en) 2017-11-17 2021-07-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
EP3765026A4 (en) 2018-03-10 2021-12-22 Yale University BTK PROTEOLYSIS MODULATORS AND METHODS FOR USE
CA3095494C (en) 2018-04-04 2023-11-07 Arvinas Operations, Inc. Modulators of proteolysis and associated methods of use
EP4306111A3 (en) 2018-07-10 2024-04-17 Novartis AG 3-(5-hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
AR116109A1 (es) 2018-07-10 2021-03-31 Novartis Ag Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos
WO2020023851A1 (en) 2018-07-26 2020-01-30 Yale University Bifunctional substitued pyrimidines as modulators of fak proteolyse
US11707452B2 (en) 2018-08-20 2023-07-25 Arvinas Operations, Inc. Modulators of alpha-synuclein proteolysis and associated methods of use
KR102642203B1 (ko) 2018-09-07 2024-03-04 아비나스 오퍼레이션스, 인코포레이티드 급속 진행형 섬유육종 폴리펩티드의 표적화 분해를 위한 다중 고리 화합물 및 방법
WO2020089811A1 (en) 2018-10-31 2020-05-07 Novartis Ag Dc-sign antibody drug conjugates
MX2021007392A (es) 2018-12-20 2021-08-24 Novartis Ag Regimen de dosificacion y combinacion farmaceutica que comprende derivados de 3-(1-oxoisoindolin-2-il)piperidina-2,6-diona.
PH12021551479A1 (en) 2018-12-21 2022-07-18 Novartis Ag Antibodies to pmel17 and conjugates thereof
KR20210129671A (ko) 2019-02-15 2021-10-28 노파르티스 아게 3-(1-옥소-5-(피페리딘-4-일)이소인돌린-2-일)피페리딘-2,6-디온 유도체 및 이의 용도
EP3924055B1 (en) 2019-02-15 2024-04-03 Novartis AG Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
CA3138411A1 (en) * 2019-05-10 2020-11-19 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Crystallization of smac mimic used as iap inhibitor and preparation method thereof
EP3999182A1 (en) 2019-07-17 2022-05-25 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
EP4007592A1 (en) 2019-08-02 2022-06-08 LanthioPep B.V. Angiotensin type 2 (at2) receptor agonists for use in the treatment of cancer
CA3152401A1 (en) 2019-08-26 2021-03-04 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
US20230057071A1 (en) 2019-12-20 2023-02-23 Novartis Ag Combination of anti tim-3 antibody mbg453 and anti tgf-beta antibody nis793, with or without decitabine or the anti pd-1 antibody spartalizumab, for treating myelofibrosis and myelodysplastic syndrome
MX2022008874A (es) 2020-01-20 2022-08-11 Astrazeneca Ab Inhibidores de la tirosina cinasa del receptor del factor de creciminto epidermico para el tratamiento del cancer.
WO2021220178A1 (en) 2020-04-29 2021-11-04 Cominnex Zrt. Iap antagonists and their therapeutic applications
US20230181756A1 (en) 2020-04-30 2023-06-15 Novartis Ag Ccr7 antibody drug conjugates for treating cancer
US20230332104A1 (en) 2020-06-11 2023-10-19 Novartis Ag Zbtb32 inhibitors and uses thereof
AU2021297099A1 (en) 2020-06-23 2023-01-05 Novartis Ag Dosing regimen comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
WO2022029573A1 (en) 2020-08-03 2022-02-10 Novartis Ag Heteroaryl substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
JP2023539663A (ja) 2020-08-28 2023-09-15 アルビナス・オペレーションズ・インコーポレイテッド 急速進行性線維肉腫タンパク質分解化合物及び関連する使用方法
AU2021342287A1 (en) 2020-09-14 2023-04-13 Arvinas Operations, Inc. Crystalline forms of a compound for the targeted degradation of estrogen receptor
TW202304979A (zh) 2021-04-07 2023-02-01 瑞士商諾華公司 抗ＴＧＦβ抗體及其他治療劑用於治療增殖性疾病之用途
KR20240054417A (ko) 2021-04-16 2024-04-25 노파르티스 아게 항체 약물 접합체 및 이의 제조 방법
AR125874A1 (es) 2021-05-18 2023-08-23 Novartis Ag Terapias de combinación
WO2023214325A1 (en) 2022-05-05 2023-11-09 Novartis Ag Pyrazolopyrimidine derivatives and uses thereof as tet2 inhibitors
AU2023314354A1 (en) 2022-07-26 2024-11-21 Novartis Ag Crystalline forms of an akr1c3 dependent kars inhibitor
US11957759B1 (en) 2022-09-07 2024-04-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use
TW202444727A (zh) 2023-01-26 2024-11-16 美商艾維納斯手術有限公司 基於cereblon之kras降解protac及其相關用途

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1524747A (en) 1976-05-11 1978-09-13 Ici Ltd Polypeptide
DE2714880A1 (de) * 1977-04-02 1978-10-26 Hoechst Ag Cephemderivate und verfahren zu ihrer herstellung
ATE28864T1 (de) 1982-07-23 1987-08-15 Ici Plc Amide-derivate.
JPS59141547A (ja) 1983-02-01 1984-08-14 Eisai Co Ltd 鎮痛作用を有する新規ペプタイドおよび製法
GB8327256D0 (en) 1983-10-12 1983-11-16 Ici Plc Steroid derivatives
FR2575753B1 (fr) * 1985-01-07 1987-02-20 Adir Nouveaux derives peptidiques a structure polycyclique azotee, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US5093330A (en) 1987-06-15 1992-03-03 Ciba-Geigy Corporation Staurosporine derivatives substituted at methylamino nitrogen
US5010099A (en) 1989-08-11 1991-04-23 Harbor Branch Oceanographic Institution, Inc. Discodermolide compounds, compositions containing same and method of preparation and use
DK167813B1 (da) * 1989-12-07 1993-12-20 Carlbiotech Ltd As Pentapeptidderivat, farmaceutisk acceptable salte heraf, fremgangsmaade til fremstilling deraf og farmaceutisk praeparat indeholdende et saadant derivat
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
TW225528B (es) 1992-04-03 1994-06-21 Ciba Geigy Ag
US5559209A (en) * 1993-02-18 1996-09-24 The General Hospital Corporation Regulator regions of G proteins
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
ES2161290T3 (es) 1995-03-30 2001-12-01 Pfizer Derivados de quinazolina.
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5843901A (en) 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
US6140332A (en) 1995-07-06 2000-10-31 Novartis Ag Pyrrolopyrimidines and processes for the preparation thereof
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
CN100503580C (zh) 1996-04-12 2009-06-24 沃尼尔·朗伯公司 酪氨酸激酶的不可逆抑制剂
ATE308527T1 (de) 1996-06-24 2005-11-15 Pfizer Phenylamino-substituierte triicyclische derivate zur behandlung hyperproliferativer krankheiten
EP0923583A1 (de) 1996-08-30 1999-06-23 Novartis AG Verfahren zur herstellung von epothilonen und zwischenprodukte innerhalb des verfahrens
JP2002513445A (ja) 1996-09-06 2002-05-08 オブデュキャット、アクチボラグ 導電材料内の構造の異方性エッチング方法
WO1998010767A2 (en) 1996-09-13 1998-03-19 Sugen, Inc. Use of quinazoline derivatives for the manufacture of a medicament in the treatment of hyperproliferative skin disorders
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
DE59711647D1 (de) 1996-11-18 2004-06-24 Biotechnolog Forschung Gmbh Epothilon d, dessen herstellung und dessen verwendung als cytostatisches mittel bzw. als pflanzenschutzmittel
US6441186B1 (en) 1996-12-13 2002-08-27 The Scripps Research Institute Epothilone analogs
CO4940418A1 (es) 1997-07-18 2000-07-24 Novartis Ag Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso
GB9721069D0 (en) 1997-10-03 1997-12-03 Pharmacia & Upjohn Spa Polymeric derivatives of camptothecin
US6194181B1 (en) 1998-02-19 2001-02-27 Novartis Ag Fermentative preparation process for and crystal forms of cytostatics
JP2002504540A (ja) 1998-02-25 2002-02-12 スローン−ケッタリング インスティトゥート フォア キャンサー リサーチ エポチロンの合成、その中間体およびそのアナログ
US6472172B1 (en) * 1998-07-31 2002-10-29 Schering Aktiengesellschaft DNA encoding a novel human inhibitor-of-apoptosis protein
ES2342240T3 (es) 1998-08-11 2010-07-02 Novartis Ag Derivados de isoquinolina con actividad que inhibe la angiogenia.
AU768220B2 (en) 1998-11-20 2003-12-04 Kosan Biosciences, Inc. Recombinant methods and materials for producing epothilone and epothilone derivatives
PE20020058A1 (es) * 2000-05-23 2002-01-31 Vertex Pharma Derivados de piperidina tetrahidroquinolina, tetrahidroisoquinolina como inhibidores de caspasas
US6608026B1 (en) * 2000-08-23 2003-08-19 Board Of Regents, The University Of Texas System Apoptotic compounds
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
US7718600B2 (en) * 2000-09-29 2010-05-18 The Trustees Of Princeton University IAP binding compounds
US20020160975A1 (en) * 2001-02-08 2002-10-31 Thomas Jefferson University Conserved XIAP-interaction motif in caspase-9 and Smac/DIABLO for mediating apoptosis
TWI238824B (en) 2001-05-14 2005-09-01 Novartis Ag 4-amino-5-phenyl-7-cyclobutyl-pyrrolo[2,3-d]pyrimidine derivatives
GB0119249D0 (en) 2001-08-07 2001-10-03 Novartis Ag Organic compounds
US20030157522A1 (en) * 2001-11-09 2003-08-21 Alain Boudreault Methods and reagents for peptide-BIR interaction screens
AU2003249920A1 (en) * 2002-07-02 2004-01-23 Novartis Ag Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap)
US20040171554A1 (en) * 2003-02-07 2004-09-02 Genentech, Inc. Compositions and methods for enhancing apoptosis
AU2004291936A1 (en) * 2003-11-13 2005-06-02 Burnham Institute Compositions and methods for screening pro-apoptotic compounds
JP2007523061A (ja) 2004-01-16 2007-08-16 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン Ｓｍａｃペプチドミメティクスおよびその使用法
CA2582734C (en) * 2004-03-01 2011-05-03 Board Of Regents, The University Of Texas System Dimeric small molecule potentiators of apoptosis
NZ549925A (en) * 2004-04-07 2010-08-27 Novartis Ag Inhibitors of IAP
EP1778718B1 (en) 2004-07-02 2014-10-08 Genentech, Inc. Inhibitors of iap
KR20120127754A (ko) 2004-12-20 2012-11-23 제넨테크, 인크. Ｉａｐ의 피롤리딘 억제제
PE20110217A1 (es) 2006-08-02 2011-04-01 Novartis Ag DERIVADOS DE 2-OXO-ETIL-AMINO-PROPIONAMIDA-PIRROLIDIN-2-IL-SUSTITUIDOS COMO INHIBIDORES DEL ENLACE DE LA PROTEINA Smac AL INHIBIDOR DE LA PROTEINA DE APOPTOSIS

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ZA200607696B (en) 2008-03-26
RS52545B (sr) 2013-04-30
PT2253614E (pt) 2013-01-09
HRP20121023T1 (hr) 2013-01-31
PL2253614T3 (pl) 2013-03-29
AU2005231956A1 (en) 2005-10-20
SG152225A1 (en) 2009-05-29
EP2253614A1 (en) 2010-11-24
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US20110281875A1 (en) 2011-11-17
IL178104A (en) 2015-08-31
ES2396195T3 (es) 2013-02-19
TNSN06323A1 (en) 2008-02-22
US20120207769A1 (en) 2012-08-16
US8207183B2 (en) 2012-06-26
RU2006139010A (ru) 2008-05-20
KR20080083220A (ko) 2008-09-16
CY1113511T1 (el) 2016-06-22
ES2394441T3 (es) 2013-01-31
EP2253614B1 (en) 2012-09-19
JP2013049733A (ja) 2013-03-14
EP1735307A1 (en) 2006-12-27
CN1964970B (zh) 2011-08-03
PE20110102A1 (es) 2011-02-07
RU2425838C2 (ru) 2011-08-10
IL178104A0 (en) 2006-12-31
DK2253614T3 (da) 2013-01-07
EP1735307B1 (en) 2012-08-29
TWI417092B (zh) 2013-12-01
US20050234042A1 (en) 2005-10-20
MY165401A (en) 2018-03-21
US7419975B2 (en) 2008-09-02
CN1964970A (zh) 2007-05-16
ECSP066893A (es) 2006-11-24
TW200602029A (en) 2006-01-16
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WO2005097791A1 (en) 2005-10-20
BRPI0509721A (pt) 2007-09-25

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