JP2015528798A5 - - Google Patents
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- Publication number
- JP2015528798A5 JP2015528798A5 JP2015519357A JP2015519357A JP2015528798A5 JP 2015528798 A5 JP2015528798 A5 JP 2015528798A5 JP 2015519357 A JP2015519357 A JP 2015519357A JP 2015519357 A JP2015519357 A JP 2015519357A JP 2015528798 A5 JP2015528798 A5 JP 2015528798A5
- Authority
- JP
- Japan
- Prior art keywords
- solid form
- phenyl
- ray powder
- powder diffraction
- disease
- 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
- 239000007787 solid Substances 0.000 claims 16
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical group CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 6
- 238000000634 powder X-ray diffraction Methods 0.000 claims 6
- 102000003827 Plasma Kallikrein Human genes 0.000 claims 4
- 108090000113 Plasma Kallikrein Proteins 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 230000001404 mediated effect Effects 0.000 claims 4
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims 3
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 3
- 201000011190 diabetic macular edema Diseases 0.000 claims 3
- 238000002329 infrared spectrum Methods 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- -1 4-aminomethyl-benzylcarbamoyl Chemical group 0.000 claims 2
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims 2
- 238000002347 injection Methods 0.000 claims 2
- 239000007924 injection Substances 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- DHNSEQGWKLRFOE-XJEPUKKESA-N n-[(2r)-1-[[(2s)-1-[[4-(aminomethyl)phenyl]methylamino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(4-ethoxyphenyl)-1-oxopropan-2-yl]benzamide;hydrochloride Chemical compound Cl.C1=CC(OCC)=CC=C1C[C@H](C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)NCC=1C=CC(CN)=CC=1)NC(=O)C1=CC=CC=C1 DHNSEQGWKLRFOE-XJEPUKKESA-N 0.000 claims 2
- 239000011877 solvent mixture Substances 0.000 claims 2
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
- 208000031229 Cardiomyopathies Diseases 0.000 claims 1
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 1
- 206010019860 Hereditary angioedema Diseases 0.000 claims 1
- 208000001953 Hypotension Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 206010051077 Post procedural haemorrhage Diseases 0.000 claims 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 1
- 206010040070 Septic Shock Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 1
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000002612 cardiopulmonary effect Effects 0.000 claims 1
- 230000006735 deficit Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 208000009190 disseminated intravascular coagulation Diseases 0.000 claims 1
- 230000036543 hypotension Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 150000004682 monohydrates Chemical class 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000002207 retinal effect Effects 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 230000008728 vascular permeability Effects 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261668543P | 2012-07-06 | 2012-07-06 | |
| GB201212081A GB201212081D0 (en) | 2012-07-06 | 2012-07-06 | New polymorph |
| US61/668,543 | 2012-07-06 | ||
| GB1212081.2 | 2012-07-06 | ||
| PCT/GB2013/051781 WO2014006414A1 (en) | 2012-07-06 | 2013-07-05 | Polymorphs of|n-[(r)-1 -[(s)-1-(4-aminomethyl-benzylcarbamoyl)-2-phenyl-ethylcarbamoy l]-2-(4-e|thoxy-phenyl)-ethyl]-benzamide hydrochloride |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015528798A JP2015528798A (ja) | 2015-10-01 |
| JP2015528798A5 true JP2015528798A5 (enExample) | 2016-08-12 |
| JP6367187B2 JP6367187B2 (ja) | 2018-08-01 |
Family
ID=46766283
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015519357A Expired - Fee Related JP6367187B2 (ja) | 2012-07-06 | 2013-07-05 | N−[(r)−1−[(s)−1−(4−アミノメチル−ベンジルカルバモイル)−2−フェニルエチルカルバモイル]−2−(4−エトキシ−フェニル)−エチル]−ベンズアミド塩酸塩の多形体 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9512065B2 (enExample) |
| EP (1) | EP2870137B8 (enExample) |
| JP (1) | JP6367187B2 (enExample) |
| CA (1) | CA2878319C (enExample) |
| ES (1) | ES2679370T3 (enExample) |
| GB (1) | GB201212081D0 (enExample) |
| HU (1) | HUE039775T2 (enExample) |
| PL (1) | PL2870137T3 (enExample) |
| TR (1) | TR201809681T4 (enExample) |
| WO (1) | WO2014006414A1 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2510407A (en) | 2013-02-04 | 2014-08-06 | Kalvista Pharmaceuticals Ltd | Aqueous suspensions of kallikrein inhibitors for parenteral administration |
| TWI636047B (zh) | 2013-08-14 | 2018-09-21 | 英商卡爾維斯塔製藥有限公司 | 雜環衍生物 |
| GB201421083D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | Enzyme inhibitors |
| GB201421085D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
| WO2017153567A1 (en) | 2016-03-10 | 2017-09-14 | Thrombogenics Nv | Posterior ocular fibrosis inhibition by antagonizing placental growth factor |
| HRP20201131T1 (hr) | 2016-05-31 | 2020-10-30 | Kalvista Pharmaceuticals Limited | Derivati pirazola kao inhibitori kalikreina plazme |
| GB201609603D0 (en) * | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide |
| GB201609607D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts |
| ES2922379T3 (es) | 2016-12-16 | 2022-09-14 | Janssen Pharmaceutica Nv | Compuestos de imidazo[4,5,D]pirrolo[2,3,B]piridina como inhibidores de Janus quinasas |
| JOP20190144A1 (ar) | 2016-12-16 | 2019-06-16 | Janssen Pharmaceutica Nv | إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز |
| IL268007B2 (en) | 2017-01-30 | 2025-05-01 | Janssen Biotech Inc | Anti-tnf antibodies, compositions, and methods for the treatment of active psoriatic arthritis |
| AU2017398101B2 (en) | 2017-02-07 | 2025-02-06 | Janssen Biotech, Inc. | Anti-TNF antibodies, compositions, and methods for the treatment of active Ankylosing Spondylitis |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| DK3716952T3 (da) | 2017-11-29 | 2022-03-14 | Kalvista Pharmaceuticals Ltd | Doseringsformer omfattende en plasmakallikrein-inhibitor |
| TW202016110A (zh) | 2018-06-15 | 2020-05-01 | 比利時商健生藥品公司 | Jak激酶家族之小分子抑制劑 |
| UY38438A (es) | 2018-11-02 | 2020-05-29 | Biocryst Pharm Inc | Sales cristalinas de un inhibidor de calicreína plasmática |
| CA3138241A1 (en) | 2019-05-23 | 2020-11-26 | Janssen Biotech, Inc. | Method of treating inflammatory bowel disease with a combination therapy of antibodies to il-23 and tnf alpha |
| WO2021028645A1 (en) | 2019-08-09 | 2021-02-18 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
| GB201918994D0 (en) * | 2019-12-20 | 2020-02-05 | Kalvista Pharmaceuticals Ltd | Treatments of diabetic macular edema and impaired visual acuity |
| GB2591730A (en) | 2019-12-09 | 2021-08-11 | Kalvista Pharmaceuticals Ltd | New polymorphs |
| EP4596046A3 (en) | 2020-05-21 | 2025-10-22 | Janssen Biotech, Inc. | Method of treating inflammatory bowel disease with a combination therapy of antibodies to il-23 and tnf alpha |
| AU2022233254A1 (en) | 2021-03-11 | 2023-10-26 | Janssen Pharmaceutica Nv | Lorpucitinib for use in the treatment of jak mediated disorders |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5187157A (en) | 1987-06-05 | 1993-02-16 | Du Pont Merck Pharmaceutical Company | Peptide boronic acid inhibitors of trypsin-like proteases |
| IT1223401B (it) * | 1987-12-02 | 1990-09-19 | Montedison Spa | Poliesteri aromatici liquido cristallini termotropici |
| GB9019558D0 (en) | 1990-09-07 | 1990-10-24 | Szelke Michael | Enzyme inhibitors |
| SE9301911D0 (sv) | 1993-06-03 | 1993-06-03 | Ab Astra | New peptide derivatives |
| US5589467A (en) | 1993-09-17 | 1996-12-31 | Novo Nordisk A/S | 2,5',N6-trisubstituted adenosine derivatives |
| IL112795A (en) * | 1994-03-04 | 2001-01-28 | Astrazeneca Ab | Peptide derivatives as antithrombic agents their preparation and pharmaceutical compositions containing them |
| US5914319A (en) * | 1995-02-27 | 1999-06-22 | Eli Lilly And Company | Antithrombotic agents |
| US7001887B2 (en) * | 2001-02-02 | 2006-02-21 | Chugai Seiyaku Kabushiki Kaisha | Peptide derivatives |
| GB0205527D0 (en) | 2002-03-08 | 2002-04-24 | Ferring Bv | Inhibitors |
| DE10301300B4 (de) | 2003-01-15 | 2009-07-16 | Curacyte Chemistry Gmbh | Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein |
| PL1660057T3 (pl) | 2003-08-27 | 2012-10-31 | Ophthotech Corp | Terapia łączona do leczenia zaburzeń związanych z neowaskularyzacją gałki ocznej |
| AU2005227733A1 (en) * | 2004-04-02 | 2005-10-13 | Glaxo Group Limited | Chemical process and new crystalline form |
| US7453002B2 (en) * | 2004-06-15 | 2008-11-18 | Bristol-Myers Squibb Company | Five-membered heterocycles useful as serine protease inhibitors |
| DE602005014138D1 (de) * | 2004-11-30 | 2009-06-04 | Mallinckrodt Inc | Verfahren zur kristallisierung von benzphetamin |
| CA2633252A1 (en) * | 2005-12-14 | 2007-06-21 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors |
| US7625944B2 (en) | 2006-07-31 | 2009-12-01 | Activesite Pharmaceuticals, Inc. | Inhibitors of plasma kallikrein |
| DE102006050672A1 (de) | 2006-10-24 | 2008-04-30 | Curacyte Discovery Gmbh | Hemmstoffe des Plasmins und des Plasmakallikreins |
| CN102762203A (zh) | 2009-12-18 | 2012-10-31 | 艾克提弗赛特制药股份有限公司 | 血浆激肽释放酶抑制剂的前药 |
| NZ601521A (en) | 2010-01-28 | 2014-09-26 | Medicines Co Leipzig Gmbh | Trypsin-like serine protease inhibitors, and their preparation and use |
| JP2013121919A (ja) | 2010-03-25 | 2013-06-20 | Astellas Pharma Inc | 血漿カリクレイン阻害剤 |
| EP2590945B1 (en) | 2010-07-07 | 2014-04-30 | The Medicines Company (Leipzig) GmbH | Serine protease inhibitors |
| US9290485B2 (en) | 2010-08-04 | 2016-03-22 | Novartis Ag | N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides |
| WO2012142308A1 (en) | 2011-04-13 | 2012-10-18 | Activesite Pharmaceuticals, Inc. | Prodrugs of inhibitors of plasma kallikrein |
| GB2494851A (en) * | 2011-07-07 | 2013-03-27 | Kalvista Pharmaceuticals Ltd | Plasma kallikrein inhibitors |
-
2012
- 2012-07-06 GB GB201212081A patent/GB201212081D0/en not_active Ceased
-
2013
- 2013-07-05 PL PL13737357T patent/PL2870137T3/pl unknown
- 2013-07-05 TR TR2018/09681T patent/TR201809681T4/tr unknown
- 2013-07-05 CA CA2878319A patent/CA2878319C/en active Active
- 2013-07-05 ES ES13737357.7T patent/ES2679370T3/es active Active
- 2013-07-05 EP EP13737357.7A patent/EP2870137B8/en active Active
- 2013-07-05 HU HUE13737357A patent/HUE039775T2/hu unknown
- 2013-07-05 WO PCT/GB2013/051781 patent/WO2014006414A1/en not_active Ceased
- 2013-07-05 JP JP2015519357A patent/JP6367187B2/ja not_active Expired - Fee Related
- 2013-07-05 US US14/413,086 patent/US9512065B2/en not_active Expired - Fee Related
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