CN101146803A - Iap的吡咯烷抑制剂 - Google Patents
Iap的吡咯烷抑制剂 Download PDFInfo
- Publication number
- CN101146803A CN101146803A CNA2005800484668A CN200580048466A CN101146803A CN 101146803 A CN101146803 A CN 101146803A CN A2005800484668 A CNA2005800484668 A CN A2005800484668A CN 200580048466 A CN200580048466 A CN 200580048466A CN 101146803 A CN101146803 A CN 101146803A
- Authority
- CN
- China
- Prior art keywords
- mmol
- alkyl
- heterocycle
- compound
- mixture
- 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.)
- Pending
Links
- WHOXVKHKTYRKQR-GARJWBAXSA-N CNC(CF)C(N[C@@H](C1CCOCC1)C(N(CCC1)[C@@H]1c1nc(-c(c2c3cccc2)ccc3F)c[s]1)=O)=O Chemical compound CNC(CF)C(N[C@@H](C1CCOCC1)C(N(CCC1)[C@@H]1c1nc(-c(c2c3cccc2)ccc3F)c[s]1)=O)=O WHOXVKHKTYRKQR-GARJWBAXSA-N 0.000 description 1
- UYNULFXALRVPGY-KCDYQERQSA-N CN[C@@H](C=C)C(N[C@@H]([C@H](CC1)CC[C@@H]1O)C(N(CCC1)[C@@H]1c1nc(-c(cc2)c(cccc3)c3c2F)c[s]1)=O)=O Chemical compound CN[C@@H](C=C)C(N[C@@H]([C@H](CC1)CC[C@@H]1O)C(N(CCC1)[C@@H]1c1nc(-c(cc2)c(cccc3)c3c2F)c[s]1)=O)=O UYNULFXALRVPGY-KCDYQERQSA-N 0.000 description 1
- KNSDWZOXOMEPDB-XJABCFGWSA-N C[C@@H](C(N[C@@H](C1CCOCC1)C(N(CCC1)[C@@H]1c1nc(-c2c(C)nc3[n]2cccc3)c[s]1)=O)=O)NC Chemical compound C[C@@H](C(N[C@@H](C1CCOCC1)C(N(CCC1)[C@@H]1c1nc(-c2c(C)nc3[n]2cccc3)c[s]1)=O)=O)NC KNSDWZOXOMEPDB-XJABCFGWSA-N 0.000 description 1
- IPELFFOXUNVQAY-DQLWACAZSA-N C[C@@H](C(N[C@@H](C1CCOCC1)C(N(CCC1)[C@@H]1c1nc(-c2cc3nnn[n]3c3c2cccc3)c[s]1)=O)=O)NC Chemical compound C[C@@H](C(N[C@@H](C1CCOCC1)C(N(CCC1)[C@@H]1c1nc(-c2cc3nnn[n]3c3c2cccc3)c[s]1)=O)=O)NC IPELFFOXUNVQAY-DQLWACAZSA-N 0.000 description 1
- MPXIUOXUEKTOPO-JZWJADFXSA-N C[C@@H](C(N[C@@H](C1CCOCC1)C(N(CC[C@@H]1C)[C@@H]1c1nc(-c(cc2)c(cccc3)c3c2F)c[s]1)=O)=O)NC Chemical compound C[C@@H](C(N[C@@H](C1CCOCC1)C(N(CC[C@@H]1C)[C@@H]1c1nc(-c(cc2)c(cccc3)c3c2F)c[s]1)=O)=O)NC MPXIUOXUEKTOPO-JZWJADFXSA-N 0.000 description 1
- MRQNEBMOTIPVCT-BIIQLVEXSA-N C[C@@H](C(N[C@H](C(N(CCC1)[C@@H]1c1nc(-c2cc(C)nc3c2cccc3)c[s]1)O)C1CCOCC1)=O)NC Chemical compound C[C@@H](C(N[C@H](C(N(CCC1)[C@@H]1c1nc(-c2cc(C)nc3c2cccc3)c[s]1)O)C1CCOCC1)=O)NC MRQNEBMOTIPVCT-BIIQLVEXSA-N 0.000 description 1
- 0 C[C@@](C(N[C@](C(N(CCC1)[C@@]1c1nc(-c2c(cccc3)c3nc(*)c2)c[s]1)=O)C1=CCCCC1)=O)NC Chemical compound C[C@@](C(N[C@](C(N(CCC1)[C@@]1c1nc(-c2c(cccc3)c3nc(*)c2)c[s]1)=O)C1=CCCCC1)=O)NC 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—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
- 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
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—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
- C07D417/02—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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—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
- C07D417/14—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 three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pyrrole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63820204P | 2004-12-20 | 2004-12-20 | |
| US60/638,202 | 2004-12-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101146803A true CN101146803A (zh) | 2008-03-19 |
Family
ID=36129810
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2005800484668A Pending CN101146803A (zh) | 2004-12-20 | 2005-12-19 | Iap的吡咯烷抑制剂 |
Country Status (18)
| Country | Link |
|---|---|
| US (4) | US20060167066A1 (enExample) |
| EP (1) | EP1836201B2 (enExample) |
| JP (2) | JP5007235B2 (enExample) |
| KR (2) | KR20120127754A (enExample) |
| CN (1) | CN101146803A (enExample) |
| AT (1) | ATE477254T1 (enExample) |
| AU (1) | AU2005319305B2 (enExample) |
| CA (1) | CA2588921C (enExample) |
| DE (1) | DE602005022936D1 (enExample) |
| DK (1) | DK1836201T4 (enExample) |
| EA (1) | EA019420B1 (enExample) |
| ES (1) | ES2349110T5 (enExample) |
| IL (1) | IL183514A (enExample) |
| MX (1) | MX2007007195A (enExample) |
| NO (1) | NO339157B1 (enExample) |
| NZ (1) | NZ589670A (enExample) |
| WO (1) | WO2006069063A1 (enExample) |
| ZA (1) | ZA200704910B (enExample) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102757426A (zh) * | 2011-04-28 | 2012-10-31 | 中国医学科学院医药生物技术研究所 | 一种苯并异恶唑基取代的噻唑类化合物、制备方法及用途 |
| WO2019091492A1 (zh) * | 2017-11-13 | 2019-05-16 | 南京明德新药研发股份有限公司 | 用作iap抑制剂的smac模拟物及其用途 |
| WO2020228642A1 (zh) * | 2019-05-10 | 2020-11-19 | 正大天晴药业集团股份有限公司 | 一种用作iap抑制剂的smac模拟物的结晶及其制备方法 |
| CN113354530A (zh) * | 2020-03-07 | 2021-09-07 | 东莞市东阳光动物保健药品有限公司 | 一种制备4-乙酰基-1-萘甲酸的方法 |
Families Citing this family (123)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1401850A1 (en) | 2001-06-20 | 2004-03-31 | Nuevolution A/S | Nucleoside derivatives for library preparation |
| IL163822A0 (en) | 2002-03-15 | 2005-12-18 | Nuevolution As | An improved method for synthesising templated molecules |
| AU2003247266A1 (en) | 2002-08-01 | 2004-02-23 | Nuevolution A/S | Multi-step synthesis of templated molecules |
| DK2348125T3 (en) | 2002-10-30 | 2017-10-02 | Nuevolution As | Process for the synthesis of a bifunctional complex |
| DE60330406D1 (de) | 2002-12-19 | 2010-01-14 | Nuevolution As | Durch quasizufallsstrukturen und funktionen geführte synthesemethode |
| EP1597395A2 (en) | 2003-02-21 | 2005-11-23 | Nuevolution A/S | Method for producing second-generation library |
| DK1670939T3 (da) | 2003-09-18 | 2010-03-01 | Nuevolution As | Fremgangsmåde til opnåelse af strukturel information om et kodet molekyle og fremgangsmåde til udvælgelse af forbindelser |
| ME02125B (me) | 2004-04-07 | 2013-04-30 | Novartis Ag | Inhibitori protein apoptoze (iap) |
| ES2475207T3 (es) | 2004-07-15 | 2014-07-10 | Tetralogic Pharmaceuticals Corporation | Compuestos de unión a IAP |
| ATE477254T1 (de) | 2004-12-20 | 2010-08-15 | Genentech Inc | Pyrrolidine als inhibitoren von iap |
| EA012810B1 (ru) | 2005-02-25 | 2009-12-30 | Тетралоджик Фармасеутикалс | Димерные ингибиторы ингибиторов белков апоптоза (iap) |
| CA2607940C (en) | 2005-05-18 | 2009-12-15 | Aegera Therapeutics Inc. | Bir domain binding compounds |
| WO2007003961A2 (en) * | 2005-06-30 | 2007-01-11 | Prosidion Limited | Gpcr agonists |
| US20100256046A1 (en) * | 2009-04-03 | 2010-10-07 | Tetralogic Pharmaceuticals Corporation | Treatment of proliferative disorders |
| DE102005046907A1 (de) | 2005-09-30 | 2007-04-12 | Voith Patent Gmbh | Verfahren und Vorrichtung zur Herstellung einer Tissuebahn |
| KR20080067357A (ko) | 2005-10-25 | 2008-07-18 | 에게라 쎄라퓨틱스 인코포레이티드 | Iap bir 도메인 결합 화합물 |
| SI3018206T1 (sl) | 2005-12-01 | 2022-02-28 | Nuevolution A/S | Postopki encimskega kodiranja za učinkovito sintezo velikih knjižnic |
| RU2451025C2 (ru) * | 2005-12-19 | 2012-05-20 | Дженентек, Инк. | Ингибиторы iap |
| 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 |
| MY159563A (en) | 2006-05-16 | 2017-01-13 | Pharmascience Inc | Iap bir domain binding compounds |
| AU2007276760B2 (en) | 2006-07-24 | 2012-01-19 | Tetralogic Pharmaceuticals Corporation | Dimeric IAP antagonists |
| US20100113326A1 (en) * | 2006-07-24 | 2010-05-06 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| WO2008014229A2 (en) * | 2006-07-24 | 2008-01-31 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| WO2008014252A2 (en) * | 2006-07-24 | 2008-01-31 | Tetralogic Pharmaceuticals Corporation | Iap inhibitors |
| US20100056495A1 (en) * | 2006-07-24 | 2010-03-04 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| PE20110218A1 (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 |
| KR20090094461A (ko) * | 2006-12-19 | 2009-09-07 | 제넨테크, 인크. | Iap의 이미다조피리딘 억제제 |
| BRPI0810178A2 (pt) | 2007-04-12 | 2014-09-23 | Joyant Pharmaceuticals Inc | Dímeros e trímeros miméticos de smac úteis como agentes anticâncer |
| BRPI0809867A2 (pt) * | 2007-04-30 | 2014-09-30 | Genentech Inc | Composto, método de indução da apoptose em uma célula, método de sensibilização de uma célula para um sinal apoptótico, método para inibir a ligação de uma proteína iap a uma proteína caspase e métodos |
| US20110008802A1 (en) * | 2007-05-07 | 2011-01-13 | Tetralogic Pharmaceuticals Corp. | TNFalpha GENE EXPRESSION AS A BIOMARKER OF SENSITIVITY TO ANTAGONISTS OF INHIBITOR OF APOPTOSIS PROTEINS |
| JP5176452B2 (ja) * | 2007-09-27 | 2013-04-03 | 住友化学株式会社 | 光学活性なテトラヒドロピラニルグリシン化合物の製造方法 |
| EP2240506B1 (en) * | 2008-01-11 | 2012-12-26 | Genentech, Inc. | Inhibitors of iap |
| EP2250160B1 (en) | 2008-01-25 | 2015-11-11 | Millennium Pharmaceuticals, Inc. | Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors |
| TW201011006A (en) * | 2008-06-16 | 2010-03-16 | Nuevolution As | IAP binding compounds |
| CA2730448A1 (en) | 2008-08-02 | 2010-02-11 | Genentech, Inc. | Inhibitors of iap |
| NZ590500A (en) * | 2008-08-16 | 2012-06-29 | Genentech Inc | Azaindole inhibitors of iap |
| US9090601B2 (en) | 2009-01-30 | 2015-07-28 | Millennium Pharmaceuticals, Inc. | Thiazole derivatives |
| WO2010090716A1 (en) | 2009-01-30 | 2010-08-12 | Millennium Pharmaceuticals, Inc. | Heteroaryls and their use as pi3k inhibitors |
| RU2404166C1 (ru) * | 2009-04-14 | 2010-11-20 | Учреждение Российской Академии Наук Институт Нефтехимии И Катализа Ран | Способ получения 1-ацетилизохинолина |
| US8283372B2 (en) | 2009-07-02 | 2012-10-09 | Tetralogic Pharmaceuticals Corp. | 2-(1H-indol-3-ylmethyl)-pyrrolidine dimer as a SMAC mimetic |
| TW201109335A (en) | 2009-08-04 | 2011-03-16 | Takeda Pharmaceutical | Heterocyclic compounds |
| WO2011018474A1 (en) | 2009-08-12 | 2011-02-17 | Novartis Ag | Solid oral formulations and crystalline forms of an inhibitor of apoptosis protein |
| WO2011035083A1 (en) | 2009-09-18 | 2011-03-24 | Novartis Ag | Biomarkers for iap inhibitor compounds |
| EP2784076A1 (en) | 2009-10-28 | 2014-10-01 | Joyant Pharmaceuticals, Inc. | Dimeric SMAC mimetics |
| AR079528A1 (es) * | 2009-12-18 | 2012-02-01 | Idenix Pharmaceuticals Inc | Inhibidores de arileno o heteroarileno 5,5-fusionado del virus de la hepatitis c |
| KR20120140658A (ko) | 2010-02-12 | 2012-12-31 | 파마사이언스 인크. | Iap bir 도메인 결합 화합물 |
| EP2558577B1 (en) | 2010-04-16 | 2018-12-12 | Nuevolution A/S | Bi-functional complexes and methods for making and using such complexes |
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| WO2019091492A1 (zh) * | 2017-11-13 | 2019-05-16 | 南京明德新药研发股份有限公司 | 用作iap抑制剂的smac模拟物及其用途 |
| CN111247161A (zh) * | 2017-11-13 | 2020-06-05 | 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 |
| US11358950B2 (en) | 2017-11-13 | 2022-06-14 | Chia Tai Tiangqing Pharmaceutical Group Co., Ltd. | SMAC mimetics used as IAP inhibitors and use thereof |
| WO2020228642A1 (zh) * | 2019-05-10 | 2020-11-19 | 正大天晴药业集团股份有限公司 | 一种用作iap抑制剂的smac模拟物的结晶及其制备方法 |
| CN113354530A (zh) * | 2020-03-07 | 2021-09-07 | 东莞市东阳光动物保健药品有限公司 | 一种制备4-乙酰基-1-萘甲酸的方法 |
| CN113354530B (zh) * | 2020-03-07 | 2025-11-18 | 东莞市东阳光动物保健药品有限公司 | 一种制备4-乙酰基-1-萘甲酸的方法 |
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