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PE20110102A1 - Derivados de n-(2-oxo-2-pirrolidinil-1-il)etil-2-amino-acetamida como inhibidores de proteinas de apoptosis (iap) - Google Patents

Derivados de n-(2-oxo-2-pirrolidinil-1-il)etil-2-amino-acetamida como inhibidores de proteinas de apoptosis (iap)

Info

Publication number
PE20110102A1
PE20110102A1 PE2009001297A PE2009001297A PE20110102A1 PE 20110102 A1 PE20110102 A1 PE 20110102A1 PE 2009001297 A PE2009001297 A PE 2009001297A PE 2009001297 A PE2009001297 A PE 2009001297A PE 20110102 A1 PE20110102 A1 PE 20110102A1
Authority
PE
Peru
Prior art keywords
oxo
methyl
amino
penethyl
octahydro
Prior art date
Application number
PE2009001297A
Other languages
English (en)
Inventor
Mark G Palermo
Sushil Kumar Sharma
Christopher Straub
Run-Ming Wang
Leigh Zawel
Yanlin Zhang
Zhuoliang Chen
Yaping Wang
Fan Yang
Wojciech Wrona
Gang Liu
Mark G Charest
Feng He
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=PE20110102(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 PE20110102A1 publication Critical patent/PE20110102A1/es

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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
    • C07D207/10—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
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
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    • A61P5/26—Androgens
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    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • 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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    • C07D207/04—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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    • C07D207/02—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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    • 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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    • 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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    • 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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    • C07D403/06—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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    • 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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    • 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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    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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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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  • 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 UN COMPUESTO DE FORMULA (I) DONDE R1 ES H; R2 ES ALQUILO C1-C4; R3 ES ALQUILO C1-C4; R4 ES CICLOALQUILO C3-C10; U-R5 ES DE PREFERENCIA 6-FENETIL-OCTAHIDROPIRROLO-[2,3-c]-PIRIDINA, 8-OXO-7-FENETIL-OCTAHIDRO-PIRROLO[2,3-c]AZEPIN; 2-[3-FENIL-METIL]-FENIL-PRROLIDIN, ENTRE OTROS. SON COMPUESTOS PREFERIDOS N-[1-CICLOHEXIL-2-OXO-2-(6-FENETIL-OCTAHIDRO-PIRROLO[2,3-c]-PIRIDIN-1-IL)-ETIL]-2-METIL-AMINO-ACETAMIDA; 2-METIL-AMINO-N-[2-METIL-1-(7-OXO-6-FENETIL-OCTAHIDRO-PIRROLO-[2,3-c]-PIRIDIN-1-CARBONIL)-PROPIL]-PROPIONAMIDA; 2-METIL-AMINO-N-[2-METIL-1-(7-OXO-6-FENETIL-OCTAHIDRO-PIRROLO-[2,3-c]-PIRIDIN-1-CARBONIL)-PROPIL]-PROPIONAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UN METODODE PREPARACION Y UN COMPUESTO FARMACEUTICO. DICHO COMPUESTO ES UN INHIBIDOR DEL ENLACE DE PROTEINA Smac AL INNHIBIDOR DE PROTEINAS DE APOPTOSIS (IAP) UTIL EN EL TRATAMIENTO DE ENFERMEDADES PROLIFERATIVAS INCLUYENDO EL CANCER
PE2009001297A 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) PE20110102A1 (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
PE20110102A1 true PE20110102A1 (es) 2011-02-07

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 After (1)

Application Number Title Priority Date Filing Date
PE2005000384A PE20060166A1 (es) 2004-04-07 2005-04-06 Derivados de amida como inhibidores de proteinas de apoptosis (iap)

Country Status (31)

Country Link
US (4) US20080242658A1 (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
WO2005097791A1 (en) * 2004-04-07 2005-10-20 Novartis Ag Inhibitors of iap
WO2006014361A1 (en) 2004-07-02 2006-02-09 Genentech, Inc. Inhibitors of iap
JP5230865B2 (ja) 2004-07-15 2013-07-10 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結合性化合物
EA019420B1 (ru) * 2004-12-20 2014-03-31 Дженентех, Инк. Пирролидиновые ингибиторы иап (ингибиторов апоптоза)
US20080300259A1 (en) * 2005-02-23 2008-12-04 Hauske James R Multimediator 5-Ht6 Receptor Antagonists, and Uses Related Thereto
DK1851200T3 (da) 2005-02-25 2014-04-14 Tetralogic Pharm Corp Dimere iap-inhibitorer
WO2006107964A2 (en) * 2005-04-06 2006-10-12 Novartis Ag Processes to prepare 6-phenethyl-octahydro-pyrrolo [2 , 3-c] pyridine and related compounds
CA2607940C (en) 2005-05-18 2009-12-15 Aegera Therapeutics Inc. Bir domain binding compounds
AU2006279929A1 (en) * 2005-08-09 2007-02-22 Tetralogic Pharmaceuticals Corporation Treatment of proliferative disorders
US20100256046A1 (en) * 2009-04-03 2010-10-07 Tetralogic Pharmaceuticals Corporation Treatment of proliferative disorders
WO2007048224A1 (en) 2005-10-25 2007-05-03 Aegera Therapeutics Inc. Iap bir domain binding compounds
CN101374829A (zh) * 2005-12-19 2009-02-25 健泰科生物技术公司 Iap的抑制剂
CN101340947B (zh) * 2005-12-20 2012-09-05 诺瓦提斯公司 Iap-抑制剂和紫杉烷7的组合
TWI543988B (zh) 2006-03-16 2016-08-01 科學製藥股份有限公司 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
EP2314297A1 (en) * 2006-04-05 2011-04-27 Novartis AG Combinations comprising bcr-abl/c-kit/pdgf-r tk inhibitors for treating cancer
US20090099103A1 (en) * 2006-04-05 2009-04-16 Novartis Ag. Combinations of therapeutic agents for treating cancer
US8168383B2 (en) 2006-04-14 2012-05-01 Cell Signaling Technology, Inc. Gene defects and mutant ALK kinase in human solid tumors
ES2561406T3 (es) 2006-04-14 2016-02-26 Cell Signaling Technology, Inc. Defectos de genes y quinasa ALK mutante en tumores sólidos humanos
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.
MY159563A (en) 2006-05-16 2017-01-13 Pharmascience Inc Iap bir domain binding compounds
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
US20100056495A1 (en) * 2006-07-24 2010-03-04 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
US20100113326A1 (en) * 2006-07-24 2010-05-06 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
US20100144650A1 (en) * 2006-07-24 2010-06-10 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
EP2049563B1 (en) * 2006-07-24 2014-03-12 Tetralogic Pharmaceuticals Corporation Dimeric iap antagonists
PE20110224A1 (es) * 2006-08-02 2011-04-05 Novartis Ag PROCEDIMIENTO PARA LA SINTESIS DE UN PEPTIDOMIMETICO DE Smac INHIBIDOR DE IAP, Y COMPUESTOS INTERMEDIARIOS PARA LA SINTESIS DEL MISMO
JP5190062B2 (ja) * 2006-10-12 2013-04-24 ノバルティス アーゲー Ｉａｐ阻害剤としてのピロリジン誘導体
KR20090082221A (ko) * 2006-10-19 2009-07-29 노파르티스 아게 유기 화합물
KR20090087094A (ko) * 2006-11-28 2009-08-14 노파르티스 아게 Ｉａｐ 억제제 및 ｆｌｔ3 억제제의 조합물
MX2009005551A (es) * 2006-11-28 2009-06-08 Novartis Ag Uso de inhibidores de iap para el tratamiento de leucemia mieloide aguda.
JP2010513561A (ja) * 2006-12-19 2010-04-30 ジェネンテック， インコーポレイテッド Ｉａｐのイミダゾピリジンインヒビター
WO2008109057A1 (en) * 2007-03-02 2008-09-12 Dana-Farber Cancer Institute, Inc. Organic compounds and their uses
EP2079309B1 (en) 2007-04-12 2015-11-11 Joyant Pharmaceuticals Inc SMAC MIMEE DIMERS AND TRIMERS USEFUL AS ANTICANCER AGENTS
AR066348A1 (es) 2007-04-30 2009-08-12 Genentech Inc Inhibidores de las iap
JP2010528587A (ja) * 2007-05-07 2010-08-26 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 アポトーシス阻害タンパク質のアンタゴニストに対する感受性のバイオマーカーとしてＴＮＦα遺伝子の発現を用いる方法
WO2008144925A1 (en) * 2007-05-30 2008-12-04 Aegera Therapeutics Inc. Iap bir domain binding compounds
PL2240506T3 (pl) * 2008-01-11 2013-05-31 Genentech Inc Inhibitory 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
WO2009136290A1 (en) * 2008-05-05 2009-11-12 Aegera Therapeutics, Inc. Functionalized pyrrolidines and use thereof as iap inhibitors
ES2882855T3 (es) 2008-05-16 2021-12-02 Dana Farber Cancer Inst Inc Inmunomodulación por inhibidores de IAP
EP2310402A1 (en) * 2008-06-27 2011-04-20 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
NZ590500A (en) * 2008-08-16 2012-06-29 Genentech Inc Azaindole inhibitors of iap
AU2009293403A1 (en) 2008-09-17 2010-03-25 Tetralogic Pharmaceuticals Corp. IAP inhibitors
US8841067B2 (en) 2009-01-09 2014-09-23 Dana-Farber Cancer Institute, Inc. NOL3 is a predictor of patient outcome
EA201171414A1 (ru) * 2009-05-28 2012-06-29 Тетралоджик Фармасьютикалз Корп. Ингибиторы белков семейства iap
JP5642777B2 (ja) * 2009-05-28 2014-12-17 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
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
US20110034469A1 (en) * 2009-08-04 2011-02-10 Takeda Pharmaceutical Company Limited Heterocyclic Compound
AU2010283748A1 (en) 2009-08-12 2012-02-09 Novartis Ag Solid oral formulations and crystalline forms of an inhibitor of apoptosis protein
CN102612651A (zh) * 2009-09-18 2012-07-25 诺瓦提斯公司 Iap抑制剂化合物的生物标志物
US8551955B2 (en) 2009-10-28 2013-10-08 Joyant Pharmaceuticals, Inc. Dimeric Smac mimetics
NZ602368A (en) 2010-02-12 2014-10-31 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
US20140243276A1 (en) 2011-09-30 2014-08-28 Tetralogic Pharmaceuticals Corporation Smac mimetic (birinapant) for use in the treatment of proliferative diseases (cancer)
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
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
US20130196927A1 (en) * 2012-01-27 2013-08-01 Christopher BENETATOS Smac Mimetic Therapy
US9353419B2 (en) 2012-05-04 2016-05-31 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
MX366978B (es) 2013-03-15 2019-08-01 Novartis Ag Conjugados de anticuerpo - farmaco.
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
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
US9278978B2 (en) 2013-08-23 2016-03-08 Boehringer Ingelheim International Gmbh 6-Alkynyl Pyridine
US9249151B2 (en) * 2013-08-23 2016-02-02 Boehringer Ingelheim International Gmbh Bis-amido pyridines
LT3083616T (lt) 2013-12-20 2021-09-10 Astex Therapeutics Limited Bicikinių heterociklų junginiai ir jų panaudojimas terapijoje
CA2974651A1 (en) 2014-01-24 2015-07-30 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
US10300074B2 (en) 2014-06-04 2019-05-28 Sanford Burnham Prebys Medical Discovery Institute Use of inhibitor of apoptosis protein (IAP) antagonists in HIV therapy
WO2016020791A1 (en) 2014-08-05 2016-02-11 Novartis Ag Ckit antibody drug conjugates
KR20170040249A (ko) 2014-08-12 2017-04-12 노파르티스 아게 항-cdh6 항체 약물 접합체
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
US11352351B2 (en) 2015-01-20 2022-06-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
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
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
EP3310813A1 (en) 2015-06-17 2018-04-25 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
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, 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
CN109715620B (zh) * 2016-08-29 2022-05-06 密歇根大学董事会 作为alk抑制剂的氨基嘧啶
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
KR20230127371A (ko) 2016-11-01 2023-08-31 아비나스 오퍼레이션스, 인코포레이티드 타우(Tau)-단백질 표적화 프로탁(PROTAC) 및 관련 사용 방법
IL297717A (en) 2016-12-01 2022-12-01 Arvinas Operations Inc History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists
WO2018119441A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Egfr proteolysis targeting chimeric molecules and associated methods of use
MX2019007649A (es) 2016-12-23 2019-09-10 Arvinas Operations Inc Compuestos y metodos para la degradacion dirigida de polipeptidos de fibrosarcoma acelerado rapidamente.
WO2018118598A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
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
US11179413B2 (en) 2017-03-06 2021-11-23 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
US20200362058A1 (en) 2017-05-24 2020-11-19 Novartis Ag Antibody-cytokine engrafted proteins and methods of use
IL322309A (en) 2017-05-24 2025-09-01 Novartis Ag IL2 antibody grafted proteins and methods of use in cancer treatment
CN114685602A (zh) * 2017-11-13 2022-07-01 正大天晴药业集团股份有限公司 用作iap抑制剂的smac模拟物及其用途
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
US11028088B2 (en) 2018-03-10 2021-06-08 Yale University Modulators of BTK proteolysis and methods of use
JP7720698B2 (ja) 2018-04-04 2025-08-08 アルビナス・オペレーションズ・インコーポレイテッド タンパク質分解の調節因子および関連する使用方法
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
CA3103385A1 (en) 2018-07-10 2020-01-16 Novartis Ag 3-(5-hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and their use in the treatment of ikaros family zinc finger 2 (ikzf2)-dependent diseases
WO2020023851A1 (en) 2018-07-26 2020-01-30 Yale University Bifunctional substitued pyrimidines as modulators of fak proteolyse
CN112912376A (zh) 2018-08-20 2021-06-04 阿尔维纳斯运营股份有限公司 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物
MX2021002559A (es) 2018-09-07 2021-07-21 Arvinas Operations Inc Compuestos policiclicos y metodos para la degradacion dirigida de polipeptidos de fibrosarcoma rapidamente acelerado.
WO2020089811A1 (en) 2018-10-31 2020-05-07 Novartis Ag Dc-sign antibody drug conjugates
WO2020128972A1 (en) 2018-12-20 2020-06-25 Novartis Ag Dosing regimen and pharmaceutical combination comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
KR20210107731A (ko) 2018-12-21 2021-09-01 노파르티스 아게 Pmel17에 대한 항체 및 이의 접합체
ES2982474T3 (es) 2019-02-15 2024-10-16 Novartis Ag Derivados de 3-(1-oxoisoindolin-2-il)piperidin-1,6-diona sustituidos y usos de estos
ES3032659T3 (en) 2019-02-15 2025-07-23 Novartis Ag 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
PT3967702T (pt) * 2019-05-10 2024-04-09 Chia Tai Tianqing Pharmaceutical Group Co Ltd Cristalização de miméticos de smac utilizados como inibidores de iap e método para a sua preparação
US11912699B2 (en) 2019-07-17 2024-02-27 Arvinas Operations, Inc. Tau-protein targeting compounds and associated
US20220257698A1 (en) 2019-08-02 2022-08-18 Lanthiopep B.V. Angiotensin type 2 (at2) receptor agonists for use in the treatment of cancer
EP4021450B1 (en) 2019-08-26 2025-11-05 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
MX2022007759A (es) 2019-12-20 2022-07-19 Novartis Ag Combinacion del anticuerpo anti tim-3 mbg453 y anticuerpo anti tgf-beta nis793, con o sin decitabina o el anticuerpo anti pd-1 spartalizumab, para el tratamiento de mielofibrosis y sindrome mielodisplasico.
AU2021211871A1 (en) 2020-01-20 2022-09-08 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
HUP2200468A1 (hu) 2020-04-29 2023-03-28 X Chem Zrt IAP antagonisták és gyógyászati alkalmazásuk
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
MX2022015852A (es) 2020-06-23 2023-01-24 Novartis Ag Regimen de dosificacion que comprende derivados de 3-(1-oxoisoindolin-2-il)piperidina-2,6-diona.
EP4188549A1 (en) 2020-08-03 2023-06-07 Novartis AG Heteroaryl substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
EP4204418A1 (en) 2020-08-28 2023-07-05 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
EP4211128A1 (en) 2020-09-14 2023-07-19 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
CA3216880A1 (en) 2021-04-16 2022-10-20 Novartis Ag Antibody drug conjugates and methods for making thereof
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
EP4562010A1 (en) 2022-07-26 2025-06-04 Novartis AG Crystalline forms of an akr1c3 dependent kars inhibitor
TW202432544A (zh) 2022-09-07 2024-08-16 美商亞文納營運公司 快速加速纖維肉瘤降解化合物及相關使用方法
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
LU88769I2 (fr) 1982-07-23 1996-11-05 Zeneca Ltd Bicalutamide et ses sels et esters pharmaceutiquement acceptables (Casodex (R))
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
GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd 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
DE69536015D1 (de) 1995-03-30 2009-12-10 Pfizer Prod Inc Chinazolinone Derivate
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
DK0836605T3 (da) 1995-07-06 2002-05-13 Novartis Ag Pyrrolopyrimidiner og fremgangsmåder til deres fremstilling
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
SK284073B6 (sk) 1996-04-12 2004-09-08 Warner-Lambert Company Polycyklické zlúčeniny, ich použitie a farmaceutické kompozície na ich báze
WO1997049688A1 (en) 1996-06-24 1997-12-31 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
NZ334821A (en) 1996-08-30 2000-12-22 Novartis Ag Method for producing epothilones
DE69724269T2 (de) 1996-09-06 2004-06-09 Obducat Ab Verfahren für das anisotrope ätzen von strukturen in leitende materialien
CA2265630A1 (en) 1996-09-13 1998-03-19 Gerald Mcmahon 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
CN100344627C (zh) 1996-11-18 2007-10-24 生物技术研究有限公司(Gbf) 埃坡霉素c、其制备方法以及作为细胞抑制剂和植物保护剂的应用
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
ATE307123T1 (de) 1998-02-25 2005-11-15 Sloan Kettering Inst Cancer Synthese von epothilonen, ihren zwischenprodukten und analogen verbindungen
US6472172B1 (en) * 1998-07-31 2002-10-29 Schering Aktiengesellschaft DNA encoding a novel human inhibitor-of-apoptosis protein
EP1107964B8 (en) 1998-08-11 2010-04-07 Novartis AG Isoquinoline derivatives with angiogenesis inhibiting activity
EP1135470A2 (en) 1998-11-20 2001-09-26 Kosan Biosciences, Inc. Recombinant methods and materials for producing epothilone and epothilone derivatives
MXPA02000823A (es) 2000-05-23 2002-07-30 Vertex Pharma Inhibidores de caspasa y uso de los mismos.
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)
US20020160975A1 (en) * 2001-02-08 2002-10-31 Thomas Jefferson University Conserved XIAP-interaction motif in caspase-9 and Smac/DIABLO for mediating apoptosis
AR035885A1 (es) 2001-05-14 2004-07-21 Novartis Ag Derivados de 4-amino-5-fenil-7-ciclobutilpirrolo (2,3-d)pirimidina, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos derivados para la preparacion de una composicion farmaceutica
GB0119249D0 (en) 2001-08-07 2001-10-03 Novartis Ag Organic compounds
WO2003040172A2 (en) * 2001-11-09 2003-05-15 Aegera Therapeutics, Inc. Methods and reagents for peptide-bir interaction screens
US20060128632A1 (en) * 2002-07-02 2006-06-15 Sharma Sushil K Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap)
DE60324964D1 (de) * 2002-07-15 2009-01-08 Univ Princeton Iap-bindende verbindungen
US20040171554A1 (en) * 2003-02-07 2004-09-02 Genentech, Inc. Compositions and methods for enhancing apoptosis
WO2005049853A2 (en) * 2003-11-13 2005-06-02 Genentech, Inc. Compositions and methods for screening pro-apoptotic compounds
CA2553871A1 (en) 2004-01-16 2005-08-04 The Regents Of The University Of Michigan Smac peptidomimetics and the uses thereof
AU2005218555B2 (en) * 2004-03-01 2008-01-03 Board Of Regents, The University Of Texas System Dimeric small molecule potentiators of apoptosis
WO2005097791A1 (en) 2004-04-07 2005-10-20 Novartis Ag Inhibitors of iap
WO2006014361A1 (en) 2004-07-02 2006-02-09 Genentech, Inc. Inhibitors of iap
EA019420B1 (ru) 2004-12-20 2014-03-31 Дженентех, Инк. Пирролидиновые ингибиторы иап (ингибиторов апоптоза)
PE20110224A1 (es) 2006-08-02 2011-04-05 Novartis Ag PROCEDIMIENTO PARA LA SINTESIS DE UN PEPTIDOMIMETICO DE Smac INHIBIDOR DE IAP, Y COMPUESTOS INTERMEDIARIOS PARA LA SINTESIS DEL MISMO

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