CA2878319C - Polymorphs of n-[(r)-1-[(s)-1-(4-aminomethyl-benzylcarbamoyl)-2-phenyl-ethylcarbamoyl]-2-(4-ethoxy-phenyl)-ethyl]-benzamide hydrochloride - Google Patents
Polymorphs of n-[(r)-1-[(s)-1-(4-aminomethyl-benzylcarbamoyl)-2-phenyl-ethylcarbamoyl]-2-(4-ethoxy-phenyl)-ethyl]-benzamide hydrochloride Download PDFInfo
- Publication number
- CA2878319C CA2878319C CA2878319A CA2878319A CA2878319C CA 2878319 C CA2878319 C CA 2878319C CA 2878319 A CA2878319 A CA 2878319A CA 2878319 A CA2878319 A CA 2878319A CA 2878319 C CA2878319 C CA 2878319C
- Authority
- CA
- Canada
- Prior art keywords
- phenyl
- solid form
- ethyl
- plasma kallikrein
- ethoxy
- 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.)
- Active
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/10—Antioedematous agents; Diuretics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/22—Separation; Purification; Stabilisation; Use of additives
- C07C231/24—Separation; Purification
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
- C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Vascular Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261668543P | 2012-07-06 | 2012-07-06 | |
| US61/668,543 | 2012-07-06 | ||
| GB1212081.2 | 2012-07-06 | ||
| GB201212081A GB201212081D0 (en) | 2012-07-06 | 2012-07-06 | New polymorph |
| 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 (2)
| Publication Number | Publication Date |
|---|---|
| CA2878319A1 CA2878319A1 (en) | 2014-01-09 |
| CA2878319C true CA2878319C (en) | 2021-02-09 |
Family
ID=46766283
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2878319A Active CA2878319C (en) | 2012-07-06 | 2013-07-05 | Polymorphs of n-[(r)-1-[(s)-1-(4-aminomethyl-benzylcarbamoyl)-2-phenyl-ethylcarbamoyl]-2-(4-ethoxy-phenyl)-ethyl]-benzamide hydrochloride |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9512065B2 (https=) |
| EP (1) | EP2870137B8 (https=) |
| JP (1) | JP6367187B2 (https=) |
| CA (1) | CA2878319C (https=) |
| ES (1) | ES2679370T3 (https=) |
| GB (1) | GB201212081D0 (https=) |
| HU (1) | HUE039775T2 (https=) |
| PL (1) | PL2870137T3 (https=) |
| TR (1) | TR201809681T4 (https=) |
| WO (1) | WO2014006414A1 (https=) |
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 |
| GB201421085D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
| GB201421083D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | Enzyme inhibitors |
| AU2017231765A1 (en) | 2016-03-10 | 2018-08-23 | Oxurion NV | Posterior ocular fibrosis inhibition by antagonizing placental growth factor |
| IL263235B (en) | 2016-05-31 | 2022-07-01 | Kalvista Pharmaceuticals Ltd | History of pyrazoles as plasma kallikrein inhibitors |
| 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 |
| LT3555097T (lt) | 2016-12-16 | 2022-08-25 | Janssen Pharmaceutica Nv | Imidazo[4,5-d]pirolo[2,3-b]piridino junginiai kaip janus kinazės inhibitoriai |
| JOP20190144A1 (ar) | 2016-12-16 | 2019-06-16 | Janssen Pharmaceutica Nv | إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز |
| KR20190113858A (ko) | 2017-01-30 | 2019-10-08 | 얀센 바이오테크 인코포레이티드 | 활성 건선성 관절염의 치료를 위한 항-tnf 항체, 조성물, 및 방법 |
| MA47442A (fr) | 2017-02-07 | 2019-12-18 | Janssen Biotech Inc | Anticorps anti-tnf, compositions et méthodes pour le traitement de la spondylarthrite ankylosante active |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| HUE057912T2 (hu) | 2017-11-29 | 2022-06-28 | Kalvista Pharmaceuticals Ltd | Plazma kallikrein inhibitort tartalmazó dózisformák |
| 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 |
| AR116951A1 (es) | 2018-11-02 | 2021-06-30 | Biocryst Pharm Inc | Sales cristalinas de un inhibidor de calicreína plasmática |
| WO2020234834A1 (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 |
| KR20230023663A (ko) | 2020-05-21 | 2023-02-17 | 얀센 바이오테크 인코포레이티드 | Il-23 및 tnf 알파에 대한 항체의 병용 요법으로 염증성 장질환을 치료하는 방법 |
| BR112023018286A2 (pt) | 2021-03-11 | 2023-10-31 | Janssen Pharmaceutica Nv | Lorpucitinib para uso no tratamento de distúrbios mediados por jak |
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 |
| ZA951617B (en) * | 1994-03-04 | 1997-02-27 | Lilly Co Eli | Antithrombotic agents. |
| US5914319A (en) * | 1995-02-27 | 1999-06-22 | Eli Lilly And Company | Antithrombotic agents |
| JP4179878B2 (ja) * | 2001-02-02 | 2008-11-12 | 中外製薬株式会社 | ペプチド誘導体 |
| 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 |
| NZ592039A (en) | 2003-08-27 | 2013-03-28 | Ophthotech Corp | Combination therapy for the treatment of ocular neovascular disorders |
| WO2005095328A1 (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 |
| JP2008521804A (ja) * | 2004-11-30 | 2008-06-26 | マリンクロッド・インコーポレイテッド | ベンズフェタミンの結晶化方法 |
| EP1981854B1 (en) * | 2005-12-14 | 2011-06-01 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors |
| JP5322935B2 (ja) | 2006-07-31 | 2013-10-23 | アクティベサイト ファーマシューティカルズ インコーポレイティッド | 血漿カリクレインの阻害薬 |
| DE102006050672A1 (de) * | 2006-10-24 | 2008-04-30 | Curacyte Discovery Gmbh | Hemmstoffe des Plasmins und des Plasmakallikreins |
| EP2512466A4 (en) | 2009-12-18 | 2013-07-03 | Activesite Pharmaceuticals Inc | PRODRUGS OF INHIBITORS OF PLASMATIC KALLICREIN |
| ES2569983T3 (es) | 2010-01-28 | 2016-05-13 | The Medicines Company (Leipzig) Gmbh | Inhibidores de serinproteasa de tipo tripsina y su preparación y uso |
| 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 WO PCT/GB2013/051781 patent/WO2014006414A1/en not_active Ceased
- 2013-07-05 TR TR2018/09681T patent/TR201809681T4/tr unknown
- 2013-07-05 EP EP13737357.7A patent/EP2870137B8/en active Active
- 2013-07-05 CA CA2878319A patent/CA2878319C/en active Active
- 2013-07-05 JP JP2015519357A patent/JP6367187B2/ja not_active Expired - Fee Related
- 2013-07-05 ES ES13737357.7T patent/ES2679370T3/es active Active
- 2013-07-05 US US14/413,086 patent/US9512065B2/en not_active Expired - Fee Related
- 2013-07-05 PL PL13737357T patent/PL2870137T3/pl unknown
- 2013-07-05 HU HUE13737357A patent/HUE039775T2/hu unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2878319A1 (en) | 2014-01-09 |
| EP2870137B1 (en) | 2018-05-16 |
| JP6367187B2 (ja) | 2018-08-01 |
| WO2014006414A1 (en) | 2014-01-09 |
| TR201809681T4 (tr) | 2018-07-23 |
| ES2679370T3 (es) | 2018-08-24 |
| GB201212081D0 (en) | 2012-08-22 |
| PL2870137T3 (pl) | 2018-12-31 |
| US9512065B2 (en) | 2016-12-06 |
| EP2870137A1 (en) | 2015-05-13 |
| HUE039775T2 (hu) | 2019-02-28 |
| JP2015528798A (ja) | 2015-10-01 |
| US20150191421A1 (en) | 2015-07-09 |
| EP2870137B8 (en) | 2018-07-18 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20180626 |
|
| H11 | Ip right ceased following rejected request for revival |
Free format text: ST27 STATUS EVENT CODE: T-6-6-H10-H11-H101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: TIME LIMIT FOR REVERSAL EXPIRED Effective date: 20250106 |