JP2014526492A5 - - Google Patents
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- JP2014526492A5 JP2014526492A5 JP2014530262A JP2014530262A JP2014526492A5 JP 2014526492 A5 JP2014526492 A5 JP 2014526492A5 JP 2014530262 A JP2014530262 A JP 2014530262A JP 2014530262 A JP2014530262 A JP 2014530262A JP 2014526492 A5 JP2014526492 A5 JP 2014526492A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- optionally substituted
- independently
- ring
- carbon atoms
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 25
- 125000004432 carbon atom Chemical group C* 0.000 claims description 22
- 125000005842 heteroatom Chemical group 0.000 claims description 22
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 18
- 229910052736 halogen Inorganic materials 0.000 claims description 16
- 150000002367 halogens Chemical class 0.000 claims description 16
- 239000003112 inhibitor Substances 0.000 claims description 16
- 229920006395 saturated elastomer Polymers 0.000 claims description 16
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 12
- 125000003118 aryl group Chemical group 0.000 claims description 8
- -1 Pyridinyl- Chemical group 0.000 claims description 7
- 125000002950 monocyclic group Chemical group 0.000 claims description 7
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 6
- 125000004122 cyclic group Chemical group 0.000 claims description 6
- 125000002619 bicyclic group Chemical group 0.000 claims description 5
- 239000003814 drug Substances 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 5
- 102100029921 Dipeptidyl peptidase 1 Human genes 0.000 claims description 4
- 101710087078 Dipeptidyl peptidase 1 Proteins 0.000 claims description 4
- 239000005557 antagonist Substances 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 229940079593 drug Drugs 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 230000001225 therapeutic effect Effects 0.000 claims description 4
- 125000000217 alkyl group Chemical group 0.000 claims description 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 3
- 238000000034 method Methods 0.000 claims description 3
- QWENRTYMTSOGBR-UHFFFAOYSA-N 1H-1,2,3-Triazole Chemical compound C=1C=NNN=1 QWENRTYMTSOGBR-UHFFFAOYSA-N 0.000 claims description 2
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
- 102100022718 Atypical chemokine receptor 2 Human genes 0.000 claims description 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 2
- 208000027004 Eosinophilic disease Diseases 0.000 claims description 2
- 208000018522 Gastrointestinal disease Diseases 0.000 claims description 2
- 229940122236 Histamine receptor antagonist Drugs 0.000 claims description 2
- 101000678892 Homo sapiens Atypical chemokine receptor 2 Proteins 0.000 claims description 2
- 101000716070 Homo sapiens C-C chemokine receptor type 9 Proteins 0.000 claims description 2
- 101000577881 Homo sapiens Macrophage metalloelastase Proteins 0.000 claims description 2
- 101000990902 Homo sapiens Matrix metalloproteinase-9 Proteins 0.000 claims description 2
- 102100027998 Macrophage metalloelastase Human genes 0.000 claims description 2
- 102100030412 Matrix metalloproteinase-9 Human genes 0.000 claims description 2
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 claims description 2
- 108050000258 Prostaglandin D receptors Proteins 0.000 claims description 2
- 102100024218 Prostaglandin D2 receptor 2 Human genes 0.000 claims description 2
- 239000013543 active substance Substances 0.000 claims description 2
- 208000026935 allergic disease Diseases 0.000 claims description 2
- 208000006673 asthma Diseases 0.000 claims description 2
- 239000003246 corticosteroid Substances 0.000 claims description 2
- 208000015181 infectious disease Diseases 0.000 claims description 2
- 230000002757 inflammatory effect Effects 0.000 claims description 2
- YEESKJGWJFYOOK-IJHYULJSSA-N leukotriene D4 Chemical compound CCCCC\C=C/C\C=C/C=C/C=C/[C@H]([C@@H](O)CCCC(O)=O)SC[C@H](N)C(=O)NCC(O)=O YEESKJGWJFYOOK-IJHYULJSSA-N 0.000 claims description 2
- 244000000010 microbial pathogen Species 0.000 claims description 2
- 125000002971 oxazolyl group Chemical group 0.000 claims description 2
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims description 2
- 230000001078 anti-cholinergic effect Effects 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 229940121647 egfr inhibitor Drugs 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 0 CC(C)S(N1CCC(*)CC1)(=O)=O Chemical compound CC(C)S(N1CCC(*)CC1)(=O)=O 0.000 description 5
- CCBHAIKSYFMWBC-XQRVVYSFSA-N C=N/C=C(/C1CC1)\N Chemical compound C=N/C=C(/C1CC1)\N CCBHAIKSYFMWBC-XQRVVYSFSA-N 0.000 description 1
- FPSLNIKJVXOHRC-UHFFFAOYSA-N CC(C)NC(N1CCC(C)CC1)=O Chemical compound CC(C)NC(N1CCC(C)CC1)=O FPSLNIKJVXOHRC-UHFFFAOYSA-N 0.000 description 1
- LBTABEMXXIJAST-UHFFFAOYSA-N CC(CC1)CCN1S=O Chemical compound CC(CC1)CCN1S=O LBTABEMXXIJAST-UHFFFAOYSA-N 0.000 description 1
- OWCWMQJOCMEVLE-UHFFFAOYSA-N CC1CCN(CC(F)F)CC1 Chemical compound CC1CCN(CC(F)F)CC1 OWCWMQJOCMEVLE-UHFFFAOYSA-N 0.000 description 1
- JOLSRNOUXISBRG-UHFFFAOYSA-N CCC(N1CCC(C)CC1)=O Chemical compound CCC(N1CCC(C)CC1)=O JOLSRNOUXISBRG-UHFFFAOYSA-N 0.000 description 1
- SEXYCMHETBVTFR-UHFFFAOYSA-N CCCC(N1CCC(C)CC1)=O Chemical compound CCCC(N1CCC(C)CC1)=O SEXYCMHETBVTFR-UHFFFAOYSA-N 0.000 description 1
- KTBPNPCUNDUYAN-UHFFFAOYSA-N CCNC(N1CCC(C)CC1)=O Chemical compound CCNC(N1CCC(C)CC1)=O KTBPNPCUNDUYAN-UHFFFAOYSA-N 0.000 description 1
- ZBIMOFZASGTLNO-YFHOEESVSA-N CN/C=C(/c1cccc(OC)c1)\N Chemical compound CN/C=C(/c1cccc(OC)c1)\N ZBIMOFZASGTLNO-YFHOEESVSA-N 0.000 description 1
- HZFJTLFHAAKENV-UHFFFAOYSA-N COc(cccc1)c1C1=C[NH+](C=C)[N-]1 Chemical compound COc(cccc1)c1C1=C[NH+](C=C)[N-]1 HZFJTLFHAAKENV-UHFFFAOYSA-N 0.000 description 1
- BQOHGIXUJUOZGA-UHFFFAOYSA-N Cc(cc1)ccc1[S+](NC)[OH2+] Chemical compound Cc(cc1)ccc1[S+](NC)[OH2+] BQOHGIXUJUOZGA-UHFFFAOYSA-N 0.000 description 1
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000000812 cholinergic antagonist Substances 0.000 description 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 description 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 238000011287 therapeutic dose Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11181805 | 2011-09-19 | ||
| EP11181805.0 | 2011-09-19 | ||
| PCT/EP2012/068284 WO2013041497A1 (en) | 2011-09-19 | 2012-09-18 | Substituted n- [1-cyano-2- (phenyl) ethyl] -2-azabicyclo [2.2.1] heptane-3-carboxamide inhibitors of cathepsin c |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014526492A JP2014526492A (ja) | 2014-10-06 |
| JP2014526492A5 true JP2014526492A5 (https=) | 2015-11-12 |
| JP6012736B2 JP6012736B2 (ja) | 2016-10-25 |
Family
ID=46875812
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014530262A Active JP6012736B2 (ja) | 2011-09-19 | 2012-09-18 | カテプシンｃ阻害剤である置換ｎ−［１−シアノ−２−（フェニル）エチル］−２−アザビシクロ［２．２．１］ヘプタン−３−カルボキサミド |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US8999975B2 (https=) |
| EP (1) | EP2758398B1 (https=) |
| JP (1) | JP6012736B2 (https=) |
| KR (1) | KR20140078626A (https=) |
| CN (1) | CN103814028B (https=) |
| AR (1) | AR087913A1 (https=) |
| AU (1) | AU2012311656B2 (https=) |
| BR (1) | BR112014006297A2 (https=) |
| CA (1) | CA2848929A1 (https=) |
| CL (1) | CL2014000299A1 (https=) |
| EA (1) | EA024817B1 (https=) |
| IL (1) | IL230820A (https=) |
| MX (1) | MX335941B (https=) |
| NZ (1) | NZ620208A (https=) |
| PH (1) | PH12014500529A1 (https=) |
| WO (1) | WO2013041497A1 (https=) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20160029630A1 (en) | 2012-11-27 | 2016-02-04 | Basf Se | Substituted 2-[phenoxy-phenyl]-1-[1,2,4]triazol-1-yl-ethanol compounds and their use as fungicides |
| US20150313229A1 (en) | 2012-11-27 | 2015-11-05 | Basf Se | Substituted [1,2,4] Triazole Compounds |
| WO2014082871A1 (en) | 2012-11-27 | 2014-06-05 | Basf Se | Substituted 2-[phenoxy-phenyl]-1-[1,2,4]triazol-1-yl-ethanol compounds and their use as fungicides |
| JP6441831B2 (ja) | 2013-03-14 | 2018-12-19 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | カテプシンｃの置換２−アザ−ビシクロ［２．２．２］オクタン−３−カルボン酸（ベンジル−シアノ−メチル）−アミド阻害剤 |
| US8871783B2 (en) | 2013-03-14 | 2014-10-28 | Boehringer Ingelheim International Gmbh | Substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (cyano-methyl)-amides inhibitors of cathepsin C |
| JP6437929B2 (ja) * | 2013-03-14 | 2018-12-12 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | カテプシンｃの置換二環式１−カルボン酸（ベンジル−シアノ−メチル）−アミド阻害剤 |
| PE20151727A1 (es) * | 2013-03-14 | 2015-12-17 | Boehringer Ingelheim Int | Acido 2-aza-biciclo[2.2.1]heptano-3-carboxilico (bencil-ciano-metil)-amidas sustituidas inhibidores de catepsina c |
| CN109867630A (zh) * | 2013-06-11 | 2019-06-11 | 赛尔基因第二国际有限公司 | 新型glp-1受体调节剂 |
| WO2015032943A1 (en) * | 2013-09-09 | 2015-03-12 | Prozymex A/S | Peptidyl nitril compounds as dipeptidyl peptidase i inhibitors |
| WO2015032942A1 (en) * | 2013-09-09 | 2015-03-12 | Prozymex A/S | N-substituted 3,3'-(biphenyl-4,4'-diyl)bis-2-aminopropanenitriles as dppi inhibitors |
| NO2699580T3 (https=) | 2014-01-24 | 2018-02-24 | ||
| AR100743A1 (es) | 2014-06-06 | 2016-10-26 | Basf Se | Compuestos de [1,2,4]triazol sustituido |
| JP6529575B2 (ja) * | 2014-08-01 | 2019-06-12 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 置換オキセタンおよびそれらのカテプシンｃの阻害薬としての使用 |
| KR102510588B1 (ko) * | 2014-09-12 | 2023-03-17 | 베링거 인겔하임 인터내셔날 게엠베하 | 카텝신 c의 스피로사이클릭 억제제 |
| WO2016139355A1 (en) | 2015-03-05 | 2016-09-09 | Prozymex A/S | N-substituted 3,3'-(biphenyl-4,4'-diyl)bis-2-aminopropanenitriles as dppi inhibitors |
| DK3265452T3 (en) | 2015-03-05 | 2020-06-08 | Neuprozyme Therapeutics ApS | Peptidyl nitril compounds as dipeptidyl peptidase i inhibitors |
| WO2019140380A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| KR20250002710A (ko) | 2018-03-01 | 2025-01-07 | 아스트라제네카 에이비이 | (2s)-n-｛(1s)-1-시아노-2-[4-(3-메틸-2-옥소-2,3-디하이드로-1,3-벤족사졸-5-일)페닐]에틸｝-1,4-옥사제판-2-카복스아미드를포함하는 약학 조성물 |
| WO2020010227A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| AU2019306532A1 (en) | 2018-07-17 | 2021-03-04 | Insmed Incorporated | Certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides for treating Lupus Nephritis |
| WO2020251972A1 (en) * | 2019-06-10 | 2020-12-17 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
| BR112022012410A2 (pt) | 2019-12-23 | 2022-08-30 | Kymera Therapeutics Inc | Degradadores smarca e usos dos mesmos |
| CN116157687A (zh) * | 2020-07-20 | 2023-05-23 | 英斯梅德股份有限公司 | 用于提取嗜中性粒细胞丝氨酸蛋白酶以及治疗二肽基肽酶1介导的病症的方法 |
| CN114106005B (zh) * | 2020-08-26 | 2025-08-01 | 西藏海思科制药有限公司 | 一种作为二肽基肽酶1抑制剂的腈衍生物及其用途 |
| CN115996923B (zh) | 2020-08-26 | 2025-07-18 | 海思科医药集团股份有限公司 | 一种作为二肽基肽酶1抑制剂的腈衍生物及其用途 |
| AU2021391452A1 (en) * | 2020-12-04 | 2023-06-29 | Reistone Biopharma Company Limited | Small molecule inhibitor of cathepsin c and medicinal use thereof |
| EP4259144A4 (en) | 2020-12-09 | 2025-08-20 | Kymera Therapeutics Inc | SMARCA DEGRADING AGENTS AND THEIR USES |
| US12479854B2 (en) | 2021-07-29 | 2025-11-25 | Enanta Pharmaceuticals, Inc. | Spiropyrrolidine derived antiviral agents |
| JP2025518345A (ja) * | 2022-06-07 | 2025-06-12 | 瑞石生物医薬有限公司 | ベンゾ［ｃ］クロマン化合物の薬学的に許容される塩、ならびに薬学的に許容される塩の多形及び使用 |
| CN119156384B (zh) | 2022-06-07 | 2025-12-09 | 瑞石生物医药有限公司 | 苯并[c]色满化合物的多晶型及其制备方法和用途 |
| WO2024094208A1 (zh) * | 2022-11-04 | 2024-05-10 | 南京明德新药研发有限公司 | 含氰基取代的杂环类衍生物及其制备方法 |
| EP4646265A1 (en) | 2023-01-06 | 2025-11-12 | Insmed Incorporated | Novel, reversible dpp1 inhibitors and uses thereof |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6960597B2 (en) | 2000-06-30 | 2005-11-01 | Orth-Mcneil Pharmaceutical, Inc. | Aza-bridged-bicyclic amino acid derivatives as α4 integrin antagonists |
| EP1372655B1 (en) * | 2001-03-02 | 2008-10-01 | Merck Frosst Canada Ltd. | Cathepsin cysteine protease inhibitors |
| JP2006527704A (ja) * | 2003-06-18 | 2006-12-07 | プロザイメックス・アクティーゼルスカブ | プロテアーゼ阻害剤 |
| TW200528440A (en) | 2003-10-31 | 2005-09-01 | Fujisawa Pharmaceutical Co | 2-cyanopyrrolidinecarboxamide compound |
| US20060223846A1 (en) * | 2005-03-08 | 2006-10-05 | Dyatkin Alexey B | Aza-bridged-bicyclic amino acid derivatives as alpha4 integrin antagonists |
| WO2009074829A1 (en) * | 2007-12-12 | 2009-06-18 | Astrazeneca Ab | Peptidyl nitriles and use thereof as dipeptidyl peptidase i inhibitors |
| WO2010142985A1 (en) | 2009-06-10 | 2010-12-16 | Astrazeneca Ab | Substituted n-[1-cyano-2-(phenyl)ethyl]piperidin-2-ylcarboxmide compounds 761 |
-
2012
- 2012-09-14 US US13/615,781 patent/US8999975B2/en active Active
- 2012-09-18 CN CN201280045607.0A patent/CN103814028B/zh not_active Expired - Fee Related
- 2012-09-18 MX MX2014003080A patent/MX335941B/es unknown
- 2012-09-18 EA EA201400358A patent/EA024817B1/ru not_active IP Right Cessation
- 2012-09-18 JP JP2014530262A patent/JP6012736B2/ja active Active
- 2012-09-18 KR KR1020147007194A patent/KR20140078626A/ko not_active Withdrawn
- 2012-09-18 WO PCT/EP2012/068284 patent/WO2013041497A1/en not_active Ceased
- 2012-09-18 AU AU2012311656A patent/AU2012311656B2/en not_active Ceased
- 2012-09-18 EP EP12759724.3A patent/EP2758398B1/en active Active
- 2012-09-18 PH PH1/2014/500529A patent/PH12014500529A1/en unknown
- 2012-09-18 CA CA2848929A patent/CA2848929A1/en not_active Abandoned
- 2012-09-18 BR BR112014006297A patent/BR112014006297A2/pt active Search and Examination
- 2012-09-18 NZ NZ620208A patent/NZ620208A/en not_active IP Right Cessation
- 2012-09-18 AR ARP120103441A patent/AR087913A1/es unknown
-
2014
- 2014-02-05 IL IL230820A patent/IL230820A/en not_active IP Right Cessation
- 2014-02-06 CL CL2014000299A patent/CL2014000299A1/es unknown
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