JP5957077B2 - タンキラーゼ阻害剤として使用するための４−ピペリジニル化合物 - Google Patents
タンキラーゼ阻害剤として使用するための４−ピペリジニル化合物 Download PDFInfo
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- JP5957077B2 JP5957077B2 JP2014519688A JP2014519688A JP5957077B2 JP 5957077 B2 JP5957077 B2 JP 5957077B2 JP 2014519688 A JP2014519688 A JP 2014519688A JP 2014519688 A JP2014519688 A JP 2014519688A JP 5957077 B2 JP5957077 B2 JP 5957077B2
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- JP
- Japan
- Prior art keywords
- piperidin
- oxo
- methoxy
- pyrrolidin
- ylmethyl
- 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.)
- Expired - Fee Related
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- 108010017601 Tankyrases Proteins 0.000 title description 55
- 239000003112 inhibitor Substances 0.000 title description 10
- 102000004535 Tankyrases Human genes 0.000 title description 2
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims description 192
- -1 3- (4- (4-methoxybenzoyl) piperidin-1-yl) -2-oxopyrrolidin-1-yl Chemical group 0.000 claims description 86
- 150000003839 salts Chemical class 0.000 claims description 67
- 125000000217 alkyl group Chemical group 0.000 claims description 39
- 125000001424 substituent group Chemical group 0.000 claims description 38
- 206010028980 Neoplasm Diseases 0.000 claims description 32
- 125000005843 halogen group Chemical group 0.000 claims description 31
- 125000003545 alkoxy group Chemical group 0.000 claims description 28
- 201000011510 cancer Diseases 0.000 claims description 24
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 22
- 239000008194 pharmaceutical composition Substances 0.000 claims description 21
- 125000001072 heteroaryl group Chemical group 0.000 claims description 17
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 15
- QNXSIUBBGPHDDE-UHFFFAOYSA-N indan-1-one Chemical class C1=CC=C2C(=O)CCC2=C1 QNXSIUBBGPHDDE-UHFFFAOYSA-N 0.000 claims description 15
- 125000005842 heteroatom Chemical group 0.000 claims description 14
- DNCYBUMDUBHIJZ-UHFFFAOYSA-N 1h-pyrimidin-6-one Chemical compound O=C1C=CN=CN1 DNCYBUMDUBHIJZ-UHFFFAOYSA-N 0.000 claims description 13
- 125000004429 atom Chemical group 0.000 claims description 12
- 125000001999 4-Methoxybenzoyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1OC([H])([H])[H])C(*)=O 0.000 claims description 11
- 229910052799 carbon Inorganic materials 0.000 claims description 11
- 229910052757 nitrogen Inorganic materials 0.000 claims description 10
- 229910052760 oxygen Inorganic materials 0.000 claims description 10
- 229910052717 sulfur Inorganic materials 0.000 claims description 9
- 229910052739 hydrogen Inorganic materials 0.000 claims description 7
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- 125000003386 piperidinyl group Chemical group 0.000 claims description 5
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 4
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- TVSSLHKEVCLVAI-UHFFFAOYSA-N 2-[[3-[4-(4-methoxybenzoyl)piperidin-1-yl]-2-oxopyrrolidin-1-yl]methyl]-6-methyl-1h-pyrimidin-4-one Chemical compound C1=CC(OC)=CC=C1C(=O)C1CCN(C2C(N(CC=3NC(C)=CC(=O)N=3)CC2)=O)CC1 TVSSLHKEVCLVAI-UHFFFAOYSA-N 0.000 claims description 3
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Classifications
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- C—CHEMISTRY; METALLURGY
- 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
- C07D401/04—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- C—CHEMISTRY; METALLURGY
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
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- 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
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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
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- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
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- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
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Applications Claiming Priority (3)
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| US201161507321P | 2011-07-13 | 2011-07-13 | |
| US61/507,321 | 2011-07-13 | ||
| PCT/IB2012/053613 WO2013008217A1 (en) | 2011-07-13 | 2012-07-13 | 4 - piperidinyl compounds for use as tankyrase inhibitors |
Publications (3)
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| JP2014522855A JP2014522855A (ja) | 2014-09-08 |
| JP2014522855A5 JP2014522855A5 (https=) | 2015-08-06 |
| JP5957077B2 true JP5957077B2 (ja) | 2016-07-27 |
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| EP (1) | EP2731940B1 (https=) |
| JP (1) | JP5957077B2 (https=) |
| KR (1) | KR20140051944A (https=) |
| CN (1) | CN103797006B (https=) |
| AP (1) | AP2014007400A0 (https=) |
| AU (1) | AU2012282076A1 (https=) |
| BR (1) | BR112014000792A2 (https=) |
| CA (1) | CA2841932A1 (https=) |
| CO (1) | CO6880065A2 (https=) |
| CR (1) | CR20140071A (https=) |
| DO (1) | DOP2014000012A (https=) |
| EA (1) | EA201490272A1 (https=) |
| ES (1) | ES2548513T3 (https=) |
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| PH (1) | PH12014500126A1 (https=) |
| TN (1) | TN2014000016A1 (https=) |
| WO (1) | WO2013008217A1 (https=) |
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| US9181266B2 (en) * | 2011-07-13 | 2015-11-10 | Novartis Ag | 2-piperidin-1-yl-acetamide compounds for use as tankyrase inhibitors |
| CA2865511A1 (en) | 2012-03-07 | 2013-09-12 | Institute Of Cancer Research: Royal Cancer Hospital (The) | 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use |
| JP6473133B2 (ja) * | 2013-03-15 | 2019-02-20 | アラクセス ファーマ エルエルシー | Ｋｒａｓｇ１２ｃの共有結合性阻害剤 |
| NZ717552A (en) * | 2013-08-07 | 2021-07-30 | Merck Patent Gmbh | Piperidine urea derivatives |
| US9611223B2 (en) | 2013-09-11 | 2017-04-04 | Institute Of Cancer Research: Royal Cancer Hospital (The) | 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use |
| CN105793264B (zh) * | 2014-03-10 | 2017-09-01 | 四川海思科制药有限公司 | 取代的二氢苯并呋喃‑哌啶‑甲酮衍生物、其制备及用途 |
| CA2948067A1 (en) | 2014-05-07 | 2015-11-12 | Merck Patent Gmbh | Heterocyclyl-butanamide derivatives |
| WO2016006975A2 (en) * | 2014-07-11 | 2016-01-14 | St Pharm Co., Ltd. | Novel imidazotriazinone or imidazopyrazinone derivatives, and use thereof |
| KR20160007347A (ko) | 2014-07-11 | 2016-01-20 | 에스티팜 주식회사 | 신규한 이미다조트리아지논 또는 이미다조피라지논 유도체, 및 이들의 용도 |
| WO2016006974A2 (en) * | 2014-07-11 | 2016-01-14 | St Pharm Co., Ltd. | Novel triazolopyrimidinone or triazolopyridinone derivatives, and use thereof |
| KR101739003B1 (ko) | 2014-07-11 | 2017-05-23 | 에스티팜 주식회사 | 신규한 트리아졸로피리미디논 또는 트리아졸로피리디논 유도체, 및 이들의 용도 |
| WO2017076484A1 (en) * | 2015-11-02 | 2017-05-11 | Merck Patent Gmbh | 1,4-dicarbonyl-piperidyl derivatives |
| KR101777475B1 (ko) * | 2015-12-08 | 2017-09-11 | 에스티팜 주식회사 | 신규한 디히드로피라노피리미디논 유도체 및 이들의 용도 |
| JP7114076B2 (ja) | 2015-12-22 | 2022-08-08 | シャイ・セラピューティクス・エルエルシー | がん及び炎症性疾患の処置のための化合物 |
| US10722484B2 (en) | 2016-03-09 | 2020-07-28 | K-Gen, Inc. | Methods of cancer treatment |
| JP7514005B2 (ja) | 2017-06-21 | 2024-07-10 | シャイ・セラピューティクス・エルエルシー | がん、炎症性疾患、ラソパシー、及び線維性疾患の治療のためのｒａｓスーパーファミリーと相互作用する化合物 |
| US20220096454A1 (en) | 2018-12-03 | 2022-03-31 | Merck Patent Gmbh | Carboxylic acid derivatives |
| JP7407461B2 (ja) | 2018-12-19 | 2024-01-04 | シャイ・セラピューティクス・エルエルシー | がん、炎症性疾患、ｒａｓ病、及び線維性疾患の処置のためのｒａｓスーパーファミリーと相互作用する化合物 |
| EP4013749B1 (en) | 2019-08-15 | 2026-03-11 | Black Diamond Therapeutics, Inc. | Alkynyl quinazoline compounds |
| US20240041859A1 (en) * | 2020-12-03 | 2024-02-08 | Washington University | Methods of treating and preventing kidney disease |
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| DE10056312A1 (de) | 2000-11-14 | 2002-05-16 | Bayer Ag | Substituierte Amidoalkyluracile und ihre Verwendung |
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| DE10201240A1 (de) | 2002-01-15 | 2003-07-24 | Bayer Ag | Substituierte Alkyluracile und ihre Verwendung |
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| ATE455110T1 (de) * | 2006-04-25 | 2010-01-15 | Lilly Co Eli | 11-beta-hydroxysteroid-dehydrogenase-1-hemmer |
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| US9181266B2 (en) * | 2011-07-13 | 2015-11-10 | Novartis Ag | 2-piperidin-1-yl-acetamide compounds for use as tankyrase inhibitors |
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- 2012-07-13 EP EP12742957.9A patent/EP2731940B1/en not_active Not-in-force
- 2012-07-13 KR KR20147003628A patent/KR20140051944A/ko not_active Withdrawn
- 2012-07-13 JP JP2014519688A patent/JP5957077B2/ja not_active Expired - Fee Related
- 2012-07-13 AU AU2012282076A patent/AU2012282076A1/en not_active Abandoned
- 2012-07-13 CN CN201280043558.7A patent/CN103797006B/zh not_active Expired - Fee Related
- 2012-07-13 ES ES12742957.9T patent/ES2548513T3/es active Active
- 2012-07-13 EA EA201490272A patent/EA201490272A1/ru unknown
- 2012-07-13 WO PCT/IB2012/053613 patent/WO2013008217A1/en not_active Ceased
- 2012-07-13 BR BR112014000792A patent/BR112014000792A2/pt not_active IP Right Cessation
- 2012-07-13 CA CA 2841932 patent/CA2841932A1/en not_active Abandoned
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- 2012-07-13 US US15/786,125 patent/USRE46942E1/en active Active
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- 2012-07-13 US US14/154,173 patent/US9163003B2/en not_active Ceased
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2014
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- 2014-02-10 MA MA36745A patent/MA35342B1/fr unknown
- 2014-02-12 CR CR20140071A patent/CR20140071A/es unknown
- 2014-02-13 CO CO14031176A patent/CO6880065A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| DOP2014000012A (es) | 2014-07-31 |
| JP2014522855A (ja) | 2014-09-08 |
| ES2548513T3 (es) | 2015-10-19 |
| MA35342B1 (fr) | 2014-08-01 |
| CO6880065A2 (es) | 2014-02-28 |
| IL230430A0 (en) | 2014-03-31 |
| NZ620426A (en) | 2015-08-28 |
| ZA201400374B (en) | 2014-10-29 |
| EP2731940B1 (en) | 2015-08-19 |
| WO2013008217A1 (en) | 2013-01-17 |
| AP2014007400A0 (en) | 2014-01-31 |
| TN2014000016A1 (en) | 2015-07-01 |
| EP2731940A1 (en) | 2014-05-21 |
| CR20140071A (es) | 2014-10-16 |
| AU2012282076A1 (en) | 2014-02-27 |
| CN103797006B (zh) | 2016-01-27 |
| CN103797006A (zh) | 2014-05-14 |
| BR112014000792A2 (pt) | 2017-10-31 |
| KR20140051944A (ko) | 2014-05-02 |
| US20150126513A1 (en) | 2015-05-07 |
| US9163003B2 (en) | 2015-10-20 |
| CA2841932A1 (en) | 2013-01-17 |
| USRE46942E1 (en) | 2018-07-10 |
| MX2014000536A (es) | 2014-12-05 |
| EA201490272A1 (ru) | 2014-05-30 |
| PH12014500126A1 (en) | 2014-02-24 |
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