JP2018529721A5 - - Google Patents
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- Publication number
- JP2018529721A5 JP2018529721A5 JP2018516461A JP2018516461A JP2018529721A5 JP 2018529721 A5 JP2018529721 A5 JP 2018529721A5 JP 2018516461 A JP2018516461 A JP 2018516461A JP 2018516461 A JP2018516461 A JP 2018516461A JP 2018529721 A5 JP2018529721 A5 JP 2018529721A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- nhc
- aryl
- cycloalkyl
- optionally substituted
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 35
- 150000001875 compounds Chemical class 0.000 claims 25
- 125000000753 cycloalkyl group Chemical group 0.000 claims 16
- 125000001072 heteroaryl group Chemical group 0.000 claims 15
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 14
- 125000003118 aryl group Chemical group 0.000 claims 13
- 125000005843 halogen group Chemical group 0.000 claims 13
- 125000003710 aryl alkyl group Chemical group 0.000 claims 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims 7
- 125000001188 haloalkyl group Chemical group 0.000 claims 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 4
- 125000003107 substituted aryl group Chemical group 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 125000002837 carbocyclic group Chemical group 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- -1 —C (O) NH 2 Chemical group 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 208000028185 Angioedema Diseases 0.000 claims 2
- 102000003827 Plasma Kallikrein Human genes 0.000 claims 2
- 108090000113 Plasma Kallikrein Proteins 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 208000002780 macular degeneration Diseases 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- 102000009027 Albumins Human genes 0.000 claims 1
- 108010088751 Albumins Proteins 0.000 claims 1
- 206010001580 Albuminuria Diseases 0.000 claims 1
- 206010048962 Brain oedema Diseases 0.000 claims 1
- 206010051055 Deep vein thrombosis Diseases 0.000 claims 1
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000032843 Hemorrhage Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000001344 Macular Edema Diseases 0.000 claims 1
- 206010025415 Macular oedema Diseases 0.000 claims 1
- 206010030113 Oedema Diseases 0.000 claims 1
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 206010038934 Retinopathy proliferative Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010047249 Venous thrombosis Diseases 0.000 claims 1
- 206010000891 acute myocardial infarction Diseases 0.000 claims 1
- 230000032683 aging Effects 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 208000034158 bleeding Diseases 0.000 claims 1
- 230000000740 bleeding effect Effects 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 208000006752 brain edema Diseases 0.000 claims 1
- 230000002612 cardiopulmonary effect Effects 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 201000011190 diabetic macular edema Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000029142 excretion Effects 0.000 claims 1
- 239000003527 fibrinolytic agent Substances 0.000 claims 1
- 230000003480 fibrinolytic effect Effects 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 230000002068 genetic effect Effects 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 201000010230 macular retinal edema Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 230000007170 pathology Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 206010044008 tonsillitis Diseases 0.000 claims 1
- VSBGZUFFBZVRNX-JLGCCPRNSA-N CO[C@H](C[C@@H]1C(Nc2cc(C(CCC3CC3)(c3ccncc3)N)ccc2F)=O)CN1C(Nc([s]1)ccc1Cl)=O Chemical compound CO[C@H](C[C@@H]1C(Nc2cc(C(CCC3CC3)(c3ccncc3)N)ccc2F)=O)CN1C(Nc([s]1)ccc1Cl)=O VSBGZUFFBZVRNX-JLGCCPRNSA-N 0.000 description 1
- 0 CO[C@](C[C@@]1C(Nc(cc(C2(CCC3CC3)*3cnccc23)cc2)c2F)=O)CN1C(c1ccc(cc[n]2)c2c1)=O Chemical compound CO[C@](C[C@@]1C(Nc(cc(C2(CCC3CC3)*3cnccc23)cc2)c2F)=O)CN1C(c1ccc(cc[n]2)c2c1)=O 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021117361A JP7431778B2 (ja) | 2015-10-01 | 2021-07-15 | ヒト血漿カリクレイン阻害剤 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562235754P | 2015-10-01 | 2015-10-01 | |
| US62/235,754 | 2015-10-01 | ||
| PCT/US2016/054619 WO2017059178A1 (en) | 2015-10-01 | 2016-09-30 | Human plasma kallikrein inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021117361A Division JP7431778B2 (ja) | 2015-10-01 | 2021-07-15 | ヒト血漿カリクレイン阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018529721A JP2018529721A (ja) | 2018-10-11 |
| JP2018529721A5 true JP2018529721A5 (https=) | 2019-11-07 |
| JP6916171B2 JP6916171B2 (ja) | 2021-08-11 |
Family
ID=58424336
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018516461A Active JP6916171B2 (ja) | 2015-10-01 | 2016-09-30 | ヒト血漿カリクレイン阻害剤 |
| JP2021117361A Active JP7431778B2 (ja) | 2015-10-01 | 2021-07-15 | ヒト血漿カリクレイン阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021117361A Active JP7431778B2 (ja) | 2015-10-01 | 2021-07-15 | ヒト血漿カリクレイン阻害剤 |
Country Status (31)
| Country | Link |
|---|---|
| US (3) | US10562850B2 (https=) |
| EP (2) | EP4019022B1 (https=) |
| JP (2) | JP6916171B2 (https=) |
| KR (1) | KR102696432B1 (https=) |
| CN (2) | CN108289893B (https=) |
| AR (1) | AR106241A1 (https=) |
| AU (2) | AU2016330926B2 (https=) |
| CA (1) | CA2999164A1 (https=) |
| CO (1) | CO2018004572A2 (https=) |
| CY (1) | CY1124907T1 (https=) |
| DK (2) | DK4019022T3 (https=) |
| EA (2) | EA202191548A1 (https=) |
| ES (2) | ES2905401T3 (https=) |
| FI (1) | FI4019022T3 (https=) |
| HR (2) | HRP20220059T1 (https=) |
| HU (2) | HUE057106T2 (https=) |
| IL (3) | IL291268B2 (https=) |
| LT (2) | LT4019022T (https=) |
| MA (1) | MA43052B1 (https=) |
| MD (1) | MD3355890T2 (https=) |
| MX (2) | MX385687B (https=) |
| MY (1) | MY198346A (https=) |
| PH (2) | PH12022550143A1 (https=) |
| PL (2) | PL3355890T3 (https=) |
| PT (2) | PT3355890T (https=) |
| RS (2) | RS65443B1 (https=) |
| SG (1) | SG10202003705WA (https=) |
| SI (2) | SI4019022T1 (https=) |
| SM (2) | SMT202400111T1 (https=) |
| TW (2) | TWI734702B (https=) |
| WO (1) | WO2017059178A1 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK4019022T3 (en) * | 2015-10-01 | 2024-02-19 | Biocryst Pharm Inc | Human plasma kallikrein inhibitors |
| WO2019028362A1 (en) * | 2017-08-04 | 2019-02-07 | Dyax Corp. | INHIBITORS OF PLASMATIC KALLIKREIN AND USES THEREOF |
| US20230022157A1 (en) | 2018-08-20 | 2023-01-26 | Achillion Pharmaceuticals, Inc. | Pharmaceutical compounds for the treatment of complement factor d medical disorders |
| JP7443375B2 (ja) | 2018-09-06 | 2024-03-05 | アキリオン ファーマシューティカルズ， インコーポレーテッド | 医学的障害の治療のための大環状化合物 |
| UY38438A (es) | 2018-11-02 | 2020-05-29 | Biocryst Pharm Inc | Sales cristalinas de un inhibidor de calicreína plasmática |
| CN110938077B (zh) * | 2019-12-25 | 2021-04-27 | 武汉九州钰民医药科技有限公司 | 合成Avapritinib的方法 |
| TW202144331A (zh) * | 2020-02-13 | 2021-12-01 | 德商百靈佳殷格翰國際股份有限公司 | 作為血漿激肽釋放酶抑制劑之雜芳族甲醯胺衍生物 |
| CN115362162A (zh) | 2020-02-20 | 2022-11-18 | 艾其林医药公司 | 用于治疗补体因子d介导的障碍的杂芳基化合物 |
| CN116444485B (zh) * | 2023-03-30 | 2024-01-23 | 广西中医药大学 | 吡啶基取代不对称脲的非金属催化、免柱层析合成方法 |
Family Cites Families (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4559157A (en) | 1983-04-21 | 1985-12-17 | Creative Products Resource Associates, Ltd. | Cosmetic applicator useful for skin moisturizing |
| LU84979A1 (fr) | 1983-08-30 | 1985-04-24 | Oreal | Composition cosmetique ou pharmaceutique sous forme aqueuse ou anhydre dont la phase grasse contient un polyether oligomere et polyethers oligomeres nouveaux |
| LU86084A1 (fr) | 1985-09-20 | 1987-04-02 | Faco Sa | Apparei de massage electrique |
| US5102417A (en) | 1985-11-07 | 1992-04-07 | Expandable Grafts Partnership | Expandable intraluminal graft, and method and apparatus for implanting an expandable intraluminal graft |
| US4800882A (en) | 1987-03-13 | 1989-01-31 | Cook Incorporated | Endovascular stent and delivery system |
| US4820508A (en) | 1987-06-23 | 1989-04-11 | Neutrogena Corporation | Skin protective composition |
| US4886062A (en) | 1987-10-19 | 1989-12-12 | Medtronic, Inc. | Intravascular radially expandable stent and method of implant |
| US4992478A (en) | 1988-04-04 | 1991-02-12 | Warner-Lambert Company | Antiinflammatory skin moisturizing composition and method of preparing same |
| US4938949A (en) | 1988-09-12 | 1990-07-03 | University Of New York | Treatment of damaged bone marrow and dosage units therefor |
| WO1990013332A1 (en) | 1989-05-11 | 1990-11-15 | Cedars-Sinai Medical Center | Stent with sustained drug delivery |
| DE69110787T2 (de) | 1990-02-28 | 1996-04-04 | Medtronic, Inc., Minneapolis, Minn. | Intraluminale prothese mit wirkstoffeluierung. |
| US5429634A (en) | 1993-09-09 | 1995-07-04 | Pdt Systems | Biogenic implant for drug delivery and method |
| US5419760A (en) | 1993-01-08 | 1995-05-30 | Pdt Systems, Inc. | Medicament dispensing stent for prevention of restenosis of a blood vessel |
| CA2170030A1 (en) * | 1993-09-14 | 1995-03-23 | Robert A. Lazarus | Pharmaceutical compositions containing ecotin and homologs thereof |
| US6774278B1 (en) | 1995-06-07 | 2004-08-10 | Cook Incorporated | Coated implantable medical device |
| DE69718194T2 (de) * | 1996-08-16 | 2003-10-16 | Bristol-Myers Squibb Pharma Co., Wilmington | Amidinophenyl-pyrrolidine, -pyrroline und -isoxazolidine und ihre derivate |
| EP1217000A1 (en) | 2000-12-23 | 2002-06-26 | Aventis Pharma Deutschland GmbH | Inhibitors of factor Xa and factor VIIa |
| CN104744461A (zh) | 2001-09-21 | 2015-07-01 | 百时美施贵宝公司 | 含有内酰胺的化合物及其衍生物作为Xa因子的抑制剂 |
| US7030141B2 (en) * | 2001-11-29 | 2006-04-18 | Christopher Franklin Bigge | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade |
| US6770729B2 (en) | 2002-09-30 | 2004-08-03 | Medtronic Minimed, Inc. | Polymer compositions containing bioactive agents and methods for their use |
| DE10301300B4 (de) * | 2003-01-15 | 2009-07-16 | Curacyte Chemistry Gmbh | Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein |
| US7122557B2 (en) | 2003-03-18 | 2006-10-17 | Bristol-Myers Squibb Company | Sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds as factor Xa inhibitors |
| DE10315377A1 (de) * | 2003-04-03 | 2004-10-14 | Merck Patent Gmbh | Carbonylverbindungen |
| PL377633A1 (pl) * | 2003-04-03 | 2006-02-06 | Merck Patent Gmbh | Związki karbonylowe |
| US7199149B2 (en) | 2003-10-01 | 2007-04-03 | Bristol Myers Squibb Company | Monocyclic and bicyclic lactams as factor Xa inhibitors |
| DE102004014945A1 (de) * | 2004-03-26 | 2005-10-13 | Merck Patent Gmbh | Prolinylderivate |
| TW201311689A (zh) | 2011-08-05 | 2013-03-16 | 必治妥美雅史谷比公司 | 作為因子ｘｉａ抑制劑之新穎巨環化合物 |
| US20140378474A1 (en) | 2012-01-27 | 2014-12-25 | Novartis Ag | 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
| EP2807156A1 (en) | 2012-01-27 | 2014-12-03 | Novartis AG | Aminopyridine derivatives as plasma kallikrein inhibitors |
| ES2617863T3 (es) | 2012-06-04 | 2017-06-20 | Actelion Pharmaceuticals Ltd. | Derivados de bencimidazol-prolina |
| GB201300304D0 (en) | 2013-01-08 | 2013-02-20 | Kalvista Pharmaceuticals Ltd | Benzylamine derivatives |
| CA2939326A1 (en) | 2014-01-14 | 2015-07-23 | Sumitomo Dainippon Pharma Co., Ltd. | Condensed 5-oxazolidinone derivative |
| KR102736869B1 (ko) * | 2014-03-07 | 2024-12-02 | 바이오크리스트파마슈티컬즈,인코포레이티드 | 인간 혈장 칼리크레인 저해제 |
| GB201421083D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | Enzyme inhibitors |
| RU2017131562A (ru) | 2015-02-27 | 2019-03-27 | Версеон Корпорейшн | Замещенные пиразольные соединения как ингибиторы сериновых протеаз |
| DK4019022T3 (en) | 2015-10-01 | 2024-02-19 | Biocryst Pharm Inc | Human plasma kallikrein inhibitors |
-
2016
- 2016-09-30 DK DK21205884.6T patent/DK4019022T3/da active
- 2016-09-30 CA CA2999164A patent/CA2999164A1/en active Pending
- 2016-09-30 HU HUE16852664A patent/HUE057106T2/hu unknown
- 2016-09-30 SI SI201631818T patent/SI4019022T1/sl unknown
- 2016-09-30 US US15/764,071 patent/US10562850B2/en active Active
- 2016-09-30 CN CN201680069679.7A patent/CN108289893B/zh active Active
- 2016-09-30 ES ES16852664T patent/ES2905401T3/es active Active
- 2016-09-30 DK DK16852664.8T patent/DK3355890T3/da active
- 2016-09-30 TW TW105131766A patent/TWI734702B/zh active
- 2016-09-30 FI FIEP21205884.6T patent/FI4019022T3/fi active
- 2016-09-30 PL PL16852664T patent/PL3355890T3/pl unknown
- 2016-09-30 EP EP21205884.6A patent/EP4019022B1/en active Active
- 2016-09-30 AR ARP160103021A patent/AR106241A1/es active IP Right Grant
- 2016-09-30 EA EA202191548A patent/EA202191548A1/ru unknown
- 2016-09-30 MX MX2018003930A patent/MX385687B/es unknown
- 2016-09-30 JP JP2018516461A patent/JP6916171B2/ja active Active
- 2016-09-30 HR HRP20220059TT patent/HRP20220059T1/hr unknown
- 2016-09-30 CN CN202210213842.XA patent/CN114591212B/zh active Active
- 2016-09-30 SM SM20240111T patent/SMT202400111T1/it unknown
- 2016-09-30 ES ES21205884T patent/ES2985200T3/es active Active
- 2016-09-30 PH PH1/2022/550143A patent/PH12022550143A1/en unknown
- 2016-09-30 MY MYPI2018000405A patent/MY198346A/en unknown
- 2016-09-30 MD MDE20180777T patent/MD3355890T2/ro unknown
- 2016-09-30 PT PT168526648T patent/PT3355890T/pt unknown
- 2016-09-30 HU HUE21205884A patent/HUE066999T2/hu unknown
- 2016-09-30 KR KR1020187012013A patent/KR102696432B1/ko active Active
- 2016-09-30 WO PCT/US2016/054619 patent/WO2017059178A1/en not_active Ceased
- 2016-09-30 SI SI201631448T patent/SI3355890T1/sl unknown
- 2016-09-30 TW TW110123218A patent/TWI796714B/zh active
- 2016-09-30 HR HRP20240557TT patent/HRP20240557T8/hr unknown
- 2016-09-30 EP EP16852664.8A patent/EP3355890B1/en active Active
- 2016-09-30 SG SG10202003705WA patent/SG10202003705WA/en unknown
- 2016-09-30 EA EA201890862A patent/EA038492B1/ru unknown
- 2016-09-30 AU AU2016330926A patent/AU2016330926B2/en active Active
- 2016-09-30 RS RS20240467A patent/RS65443B1/sr unknown
- 2016-09-30 PT PT212058846T patent/PT4019022T/pt unknown
- 2016-09-30 RS RS20220035A patent/RS62807B1/sr unknown
- 2016-09-30 SM SM20220075T patent/SMT202200075T1/it unknown
- 2016-09-30 LT LTEP21205884.6T patent/LT4019022T/lt unknown
- 2016-09-30 PL PL21205884.6T patent/PL4019022T3/pl unknown
- 2016-09-30 MA MA43052A patent/MA43052B1/fr unknown
- 2016-09-30 IL IL291268A patent/IL291268B2/en unknown
- 2016-09-30 LT LTEPPCT/US2016/054619T patent/LT3355890T/lt unknown
-
2018
- 2018-03-14 IL IL258104A patent/IL258104B/en active IP Right Grant
- 2018-03-27 PH PH12018500678A patent/PH12018500678A1/en unknown
- 2018-03-28 MX MX2021010297A patent/MX2021010297A/es unknown
- 2018-04-27 CO CONC2018/0004572A patent/CO2018004572A2/es unknown
-
2019
- 2019-12-18 US US16/718,537 patent/US11066360B2/en active Active
-
2021
- 2021-02-24 IL IL281066A patent/IL281066B/en unknown
- 2021-03-26 AU AU2021201924A patent/AU2021201924B2/en active Active
- 2021-07-13 US US17/374,335 patent/US11807605B2/en active Active
- 2021-07-15 JP JP2021117361A patent/JP7431778B2/ja active Active
-
2022
- 2022-01-13 CY CY20221100030T patent/CY1124907T1/el unknown
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