AU2016340167B2 - Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof - Google Patents

Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof Download PDF

Info

Publication number
AU2016340167B2
AU2016340167B2 AU2016340167A AU2016340167A AU2016340167B2 AU 2016340167 B2 AU2016340167 B2 AU 2016340167B2 AU 2016340167 A AU2016340167 A AU 2016340167A AU 2016340167 A AU2016340167 A AU 2016340167A AU 2016340167 B2 AU2016340167 B2 AU 2016340167B2
Authority
AU
Australia
Prior art keywords
compound
freebase
solid state
another aspect
formula
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
Application number
AU2016340167A
Other languages
English (en)
Other versions
AU2016340167A1 (en
AU2016340167A8 (en
Inventor
Ayman D. Allian
Lakshmi Bhagavatula
Thomas B. Borchardt
Jayanthy Jayanth
Ben Klünder
Patrick J. MARROUM
Peter T. Mayer
Mohamed-Eslam F. Mohamed
Mathew M. Mulhern
Fredrik Lars Nordstrom
Ahmed A. Othman
Michael J. Rozema
Ahmad Y. Sheikh
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
AbbVie Inc
Original Assignee
AbbVie Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=57209916&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AU2016340167(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by AbbVie Inc filed Critical AbbVie Inc
Publication of AU2016340167A1 publication Critical patent/AU2016340167A1/en
Publication of AU2016340167A8 publication Critical patent/AU2016340167A8/en
Application granted granted Critical
Publication of AU2016340167B2 publication Critical patent/AU2016340167B2/en
Priority to AU2021236570A priority Critical patent/AU2021236570B2/en
Priority to AU2023251492A priority patent/AU2023251492B2/en
Priority to AU2025205010A priority patent/AU2025205010A1/en
Priority to AU2025256155A priority patent/AU2025256155A1/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • 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
    • C07D487/04—Ortho-condensed systems
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Inorganic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyrrole Compounds (AREA)
  • Catalysts (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
AU2016340167A 2015-10-16 2016-10-17 Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof Active AU2016340167B2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
AU2021236570A AU2021236570B2 (en) 2015-10-16 2021-09-24 Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
AU2023251492A AU2023251492B2 (en) 2015-10-16 2023-10-19 Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
AU2025205010A AU2025205010A1 (en) 2015-10-16 2025-07-01 Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
AU2025256155A AU2025256155A1 (en) 2015-10-16 2025-10-23 Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201562242797P 2015-10-16 2015-10-16
US62/242,797 2015-10-16
US201562267672P 2015-12-15 2015-12-15
US62/267,672 2015-12-15
US201662301537P 2016-02-29 2016-02-29
US62/301,537 2016-02-29
US201662352380P 2016-06-20 2016-06-20
US62/352,380 2016-06-20
PCT/US2016/057372 WO2017066775A1 (en) 2015-10-16 2016-10-17 PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2021236570A Division AU2021236570B2 (en) 2015-10-16 2021-09-24 Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof

Publications (3)

Publication Number Publication Date
AU2016340167A1 AU2016340167A1 (en) 2018-04-26
AU2016340167A8 AU2016340167A8 (en) 2018-05-10
AU2016340167B2 true AU2016340167B2 (en) 2021-06-24

Family

ID=57209916

Family Applications (5)

Application Number Title Priority Date Filing Date
AU2016340167A Active AU2016340167B2 (en) 2015-10-16 2016-10-17 Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
AU2021236570A Active AU2021236570B2 (en) 2015-10-16 2021-09-24 Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
AU2023251492A Active AU2023251492B2 (en) 2015-10-16 2023-10-19 Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
AU2025205010A Pending AU2025205010A1 (en) 2015-10-16 2025-07-01 Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
AU2025256155A Pending AU2025256155A1 (en) 2015-10-16 2025-10-23 Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof

Family Applications After (4)

Application Number Title Priority Date Filing Date
AU2021236570A Active AU2021236570B2 (en) 2015-10-16 2021-09-24 Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
AU2023251492A Active AU2023251492B2 (en) 2015-10-16 2023-10-19 Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
AU2025205010A Pending AU2025205010A1 (en) 2015-10-16 2025-07-01 Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
AU2025256155A Pending AU2025256155A1 (en) 2015-10-16 2025-10-23 Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof

Country Status (13)

Country Link
US (39) US20170129902A1 (OSRAM)
EP (3) EP4647129A3 (OSRAM)
JP (7) JP6770775B2 (OSRAM)
KR (2) KR20250010141A (OSRAM)
CN (7) CN116270645A (OSRAM)
AU (5) AU2016340167B2 (OSRAM)
BR (1) BR122022024925B1 (OSRAM)
CA (8) CA3002220C (OSRAM)
IL (3) IL314468A (OSRAM)
MX (2) MX387822B (OSRAM)
RU (1) RU2018117889A (OSRAM)
SG (8) SG10201913997WA (OSRAM)
WO (1) WO2017066775A1 (OSRAM)

Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2836833A1 (de) 1978-08-23 1980-04-10 Volkswagenwerk Ag Brennkraftmaschine mit in zwei reihen angeordneten zylindern
CN102711476B (zh) 2009-12-01 2014-12-03 Abbvie公司 新的三环化合物
US11512092B2 (en) 2015-10-16 2022-11-29 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11773106B2 (en) 2015-10-16 2023-10-03 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
RU2018117889A (ru) 2015-10-16 2019-11-20 Эббви Инк. СПОСОБЫ ПОЛУЧЕНИЯ (3S,4R)-3-ЭТИЛ-4-(3H-ИМИДАЗО[1,2-a]ПИРРОЛО[2,3-e]-ПИРАЗИН-8-ИЛ)-N-(2,2,2-ТРИФТОРЭТИЛ)ПИРРОЛИДИН-1-КАРБОКСАМИДА И ЕГО ТВЕРДОФАЗНЫХ ФОРМ
US10550126B2 (en) 2015-10-16 2020-02-04 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11365198B2 (en) 2015-10-16 2022-06-21 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US20240316042A1 (en) 2023-03-22 2024-09-26 Abbvie Inc. Methods of treating pediatric patients with upadacitinib
US11524964B2 (en) 2015-10-16 2022-12-13 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US12365689B2 (en) 2015-10-16 2025-07-22 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11564922B2 (en) 2017-03-09 2023-01-31 Abbvie Inc. Methods of treating crohn's disease and ulcerative colitis
US20190046527A1 (en) 2017-03-09 2019-02-14 Abbvie Inc. Methods of treating crohn's disease and ulcerative colitis
US20210163409A1 (en) * 2017-07-19 2021-06-03 Dr. Reddy's Laboratories Limited Alternate processes for the preparation of pyrrolidine derivatives
HUE067471T2 (hu) * 2018-03-30 2024-10-28 Incyte Corp Gennyes verejtékmirigy-gyulladás kezelése jak inhibitorok alkalmazásával
WO2020043033A2 (zh) * 2018-08-31 2020-03-05 苏州鹏旭医药科技有限公司 一种乌帕替尼及其中间体的合成方法
CN110872250B (zh) * 2018-08-31 2023-01-10 苏州鹏旭医药科技有限公司 两种化合物及其制备方法和在合成乌西替尼中的用途
US20220002306A1 (en) * 2018-09-29 2022-01-06 Crystal Pharmaceutical (Suzhou) Co., Ltd. Crystal form of upadacitinib and preparation method and use thereof
CN111217819B (zh) * 2018-11-27 2021-05-14 杭州科巢生物科技有限公司 乌帕替尼的合成方法
EP3891151A1 (en) 2018-12-05 2021-10-13 LEK Pharmaceuticals d.d. Crystalline phosphate salt of selective jak1 inhibitor upadacitinib
CN109369659B (zh) * 2018-12-06 2020-10-27 浙江师范大学 一种jak抑制剂的合成方法
WO2020115213A1 (en) 2018-12-07 2020-06-11 Lek Pharmaceuticals D.D. Solvate of a selective jak1 inhibitor
CN109705011B (zh) * 2019-01-18 2021-02-19 浙江师范大学 一种乌帕替尼中间体的合成方法及中间体
CN112888692A (zh) * 2019-03-01 2021-06-01 苏州科睿思制药有限公司 一种Upadacitinib的晶型及其制备方法和用途
WO2020202183A1 (en) 2019-03-29 2020-10-08 Mylan Laboratories Limited The process for the preparation of upadacitinib and its intermediates
CN111909160B (zh) * 2019-05-09 2024-05-28 苏州鹏旭医药科技有限公司 一种乌帕替尼盐类化合物及其制备方法
CN110229160A (zh) * 2019-06-11 2019-09-13 南京新酶合医药科技有限公司 (5-甲苯磺酰基-5H-吡咯并[2,3-b]吡嗪-2-基)氨基甲酸乙酯的制备方法
CN110117245B (zh) * 2019-06-21 2021-03-02 浙江师范大学 一种jak抑制剂中间体的合成方法
WO2021005484A1 (en) * 2019-07-11 2021-01-14 Mankind Pharma Ltd. Pyrrolidine compounds, its salt and use in the preparation of upadacitinib thereof
CN110615753A (zh) * 2019-09-02 2019-12-27 南京新酶合医药科技有限公司 一种(3r,4s)-1-取代-4-乙基吡咯-3-羧酸的合成方法
CN114929227A (zh) 2019-09-30 2022-08-19 艾伯维公司 用乌帕替尼治疗脊柱关节炎和银屑病
CN111072543B (zh) * 2019-11-13 2021-06-04 北京海美桐医药科技有限公司 一种(3r,4s)-4-乙基吡咯烷-3-羧酸类化合物的制备方法及其应用
WO2021123288A1 (en) 2019-12-19 2021-06-24 Crystal Pharma, S.A.U. Process and intermediates for the preparation of upadacitinib
WO2021176473A1 (en) * 2020-03-05 2021-09-10 Mylan Laboratories Limited A process for the preparation of upadacitinib and its intermediates
CN114206877B (zh) * 2020-06-05 2024-04-19 苏州科睿思制药有限公司 一种乌帕替尼的晶型及其制备方法和用途
EP4180435A1 (en) * 2020-07-08 2023-05-17 Crystal Pharmaceutical (Suzhou) Co., Ltd. Crystal form of upadacitinib, preparation method therefor, and use thereof
WO2022044037A1 (en) 2020-08-24 2022-03-03 Mylan Laboratories Limited An improved process for the preparation of upadacitinib intermediate
CN114621127A (zh) * 2020-12-08 2022-06-14 苏州鹏旭医药科技有限公司 一种取代二氢吡咯的合成方法
WO2022217257A1 (en) * 2021-04-07 2022-10-13 Abbvie Inc. Cocrystals of upadacitinib
CN115724781A (zh) * 2021-08-30 2023-03-03 凯特立斯（深圳）科技有限公司 一种合成乌帕替尼关键手性中间体的方法
CN114380837B (zh) * 2021-12-27 2023-06-30 上海邈金医药科技有限公司 一种具有Janus激酶抑制活性的化合物、包括该化合物的组合物及其应用
EP4460503A4 (en) * 2022-01-06 2025-12-03 Msn Laboratories Private Ltd R&D Center IMPROVED PROCESS FOR THE PREPARATION OF UPADACITINIB
AU2022435654A1 (en) 2022-01-20 2024-08-01 Renata Pharmaceutical (Ireland) Limited Sustained release pharmaceutical composition of upadacitinib
CN114315679B (zh) * 2022-01-21 2024-08-30 杭州新博思生物医药有限公司 一种乌帕替尼手性中间体的制备方法
EP4215196A1 (en) 2022-01-24 2023-07-26 Abivax Combination of 8-chloro-n-(4-(trifluoromethoxy)phenyl)quinolin-2-amine and its derivatives with a jak inhibitor
WO2024075131A1 (en) * 2022-10-03 2024-04-11 Natco Pharma Limited Co-crystal of upadacitinib and diacetyl-d-tartaric acid and process for the preparation thereof
CN121127242A (zh) 2023-05-23 2025-12-12 艾伯维公司 用乌帕替尼治疗白癜风的方法
US20250049789A1 (en) 2023-08-08 2025-02-13 Abbvie Inc. Methods of treating alopecia araeta
CN117534678A (zh) * 2023-11-08 2024-02-09 浙江宏元药业股份有限公司 一种乌帕替尼的新结晶形式及其制备方法
CN117285537B (zh) * 2023-11-27 2024-02-06 中节能万润股份有限公司 一种乌帕替尼的制备方法
CN117285536B (zh) * 2023-11-27 2024-02-20 中节能万润股份有限公司 一种乌帕替尼中间体的制备方法
CN117285535B (zh) * 2023-11-27 2024-02-02 中节能万润股份有限公司 一种乌帕替尼中间体及成盐中间体的制备方法
CN117447481A (zh) * 2023-12-23 2024-01-26 潍坊医学院 一种乌帕替尼-焦谷氨酸盐的无定形物及其制备方法与应用
WO2025149011A1 (zh) * 2024-01-11 2025-07-17 浙江华海药业股份有限公司 一种乌帕替尼或其水合物的合成工艺
CN118047785A (zh) * 2024-03-07 2024-05-17 和鼎（南京）医药技术有限公司 制备乌帕替尼及其中间体的方法
KR20250146517A (ko) 2024-04-01 2025-10-13 주식회사 파마코스텍 유파다시티닙(upadacitinib)의 알킬 포함 술폰산염 화합물, 및 이의 제조방법
WO2025221754A1 (en) 2024-04-17 2025-10-23 Abbvie Inc. Upadacitinib for use in the treatment of giant cell arteritis
CN118370734B (zh) * 2024-06-26 2024-10-01 山东则正医药技术有限公司 一种乌帕替尼缓释片及其制备方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011068881A1 (en) * 2009-12-01 2011-06-09 Abbott Laboratories Novel tricyclic compounds

Family Cites Families (149)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB716327A (en) 1951-09-05 1954-10-06 Ici Ltd New heterocyclic compounds
BE640616A (OSRAM) 1962-12-19
US3492397A (en) 1967-04-07 1970-01-27 Warner Lambert Pharmaceutical Sustained release dosage in the pellet form and process thereof
US4060598A (en) 1967-06-28 1977-11-29 Boehringer Mannheim G.M.B.H. Tablets coated with aqueous resin dispersions
US3538214A (en) 1969-04-22 1970-11-03 Merck & Co Inc Controlled release medicinal tablets
US3663559A (en) 1969-12-03 1972-05-16 Union Carbide Corp Preparation of oxo-furo-pyridines from furylvinyl isocyanates
ZA737247B (en) 1972-09-29 1975-04-30 Ayerst Mckenna & Harrison Rapamycin and process of preparation
US4053474A (en) 1976-04-21 1977-10-11 E. R. Squibb & Sons, Inc. Pyrazolo[4,3-e][1,2,4]triazolo[4,3-c]pyrimidine
US4173626A (en) 1978-12-11 1979-11-06 Merck & Co., Inc. Sustained release indomethacin
US5605690A (en) 1989-09-05 1997-02-25 Immunex Corporation Methods of lowering active TNF-α levels in mammals using tumor necrosis factor receptor
US5270316A (en) 1989-10-20 1993-12-14 Kyowa Hakko Kogyo Co., Ltd. Condensed purine derivatives
CA2073500C (en) 1990-01-11 2008-03-25 Phillip Dan Cook Compositions and methods for detecting and modulating rna activity and gene expression
US6262241B1 (en) 1990-08-13 2001-07-17 Isis Pharmaceuticals, Inc. Compound for detecting and modulating RNA activity and gene expression
EP1857554A1 (en) 1991-03-18 2007-11-21 New York University Monoclonal and chimeric antibodies specific for human tumor necrosis factor
JP3147902B2 (ja) 1991-06-14 2001-03-19 ファルマシア・アンド・アップジョン・カンパニー イミダゾ〔１，５−ａ〕キノキサリン
US5212310A (en) 1991-12-19 1993-05-18 Neurogen Corporation Certain aryl fused imidazopyrimidines; a new class of GABA brain receptor ligands
US5266698A (en) 1992-04-30 1993-11-30 Neurogen Corporation Certain aryl and cycloalkyl fused imidazopyrazinediones; a new class of GABA brain receptor ligands
US5306819A (en) 1992-08-27 1994-04-26 Neurogen Corporation Certain aryl a cycloalkyl fused imidazopyrazinols; and new class of GABA brain receptor ligands
EP1005870B1 (en) 1992-11-13 2009-01-21 Biogen Idec Inc. Therapeutic application of chimeric antibodies to human B lymphocyte restricted differentiation antigen for treatment of B cell lymphoma
HUT72640A (en) 1993-02-26 1996-05-28 Schering Corp 2-benzyl-polycyclic guanine derivatives, pharmaceutical compositions containing them and process for preparing them
US5733905A (en) 1993-07-29 1998-03-31 American Cyanamid Company Tricyclic diazepine vasopressin antagonists and oxytocin antagonists
US5736540A (en) 1993-07-29 1998-04-07 American Cyanamid Company Tricyclic diazepine vasopressin antagonists and oxytocin antagonists
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
US5547975A (en) 1994-09-20 1996-08-20 Talley; John J. Benzopyranopyrazolyl derivatives for the treatment of inflammation
RU2158127C2 (ru) 1994-12-23 2000-10-27 Варнер-Ламберт Компани Способы ингибирования тирозинкиназы рецептора эпидермального фактора роста, азотсодержащие трициклические соединения, фармацевтическая композиция, предназначенная для введения ингибитора тирозинкиназы рецептора эпидермального фактора роста, например, erb-b2, erb-b3 или erb-b4, и противозачаточная композиция
US5753648A (en) 1995-01-17 1998-05-19 American Cyanamid Company Tricyclic benzazepine vasopressin antagonists
US5521173A (en) 1995-01-17 1996-05-28 American Home Products Corporation Tricyclic benzazepine vasopressin antagonists
US5763137A (en) 1995-08-04 1998-06-09 Agfa-Gevaert, N.V. Method for making a lithographic printing plate
US6090382A (en) 1996-02-09 2000-07-18 Basf Aktiengesellschaft Human antibodies that bind human TNFα
FR2742676B1 (fr) 1995-12-21 1998-02-06 Oreal Nanoemulsion transparente a base de tensioactifs silicones et utilisation en cosmetique ou en dermopharmacie
US5703244A (en) 1996-11-21 1997-12-30 Abbott Laboratories Process for preparation of chiral 3-amino-pyrrolidine and analogous bicyclic compounds
CZ297535B6 (cs) 1997-02-05 2007-01-03 Merck & Co., Inc. Způsob krystalizace inhibitoru na bázi benzoxazinonu
ATE430149T1 (de) 1998-03-04 2009-05-15 Bristol Myers Squibb Co Heterocyclen substituierte imidazopyrazine als protein- tyrosin-kinase-inhibitoren
CA2339273C (en) 1998-09-14 2005-10-18 Warner-Lambert Company Branched alkyl pyrrolidine-3-carboxylic acids
US6448253B1 (en) 1998-09-16 2002-09-10 King Pharmaceuticals Research And Development, Inc. Adenosine A3 receptor modulators
DE19853665B4 (de) 1998-11-20 2005-06-30 Siemens Ag Fahrzeugkommunikationssystem und Verfahren zum Austausch von Daten in einem Kraftfahrzeug
CO5271670A1 (es) 1999-10-29 2003-04-30 Pfizer Prod Inc Antagonistas del factor de liberacion de corticitropina y composiciones relacionadas
TWI271406B (en) 1999-12-13 2007-01-21 Eisai Co Ltd Tricyclic condensed heterocyclic compounds, preparation method of the same and pharmaceuticals comprising the same
JP2004505942A (ja) 2000-08-07 2004-02-26 ニューロゲン　コーポレイション Ｇａｂａａ受容体の配位子としての複素環式化合物
GB0115393D0 (en) 2001-06-23 2001-08-15 Aventis Pharma Ltd Chemical compounds
GB0124299D0 (en) 2001-10-10 2001-11-28 Astrazeneca Ab Crystal structure of enzyme and uses thereof
ATE353013T1 (de) 2002-02-19 2007-02-15 Pfizer Italia Srl Trizyklische pyrazolderivate, verfahren zu ihrer herstellung und ihre verwendung als antitumor mittel
US20030181488A1 (en) 2002-03-07 2003-09-25 Boehringer Ingelheim Pharma Gmbh & Co. Kg Administration form for the oral application of 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionic acid ethyl ester and the salts thereof
TW200400034A (en) 2002-05-20 2004-01-01 Bristol Myers Squibb Co Pyrazolo-pyrimidine aniline compounds useful as kinase inhibitors
BR0315233A (pt) 2002-10-09 2005-08-23 Scios Inc Derivados de azaindol como inibidores de p38 cinase
MXPA05007503A (es) 2003-01-17 2005-09-21 Warner Lambert Co Heterociclicos 2-aminopiridina sustituidos como inhibidores de proliferacion celular.
EP1460088A1 (en) 2003-03-21 2004-09-22 Biotest AG Humanized anti-CD4 antibody with immunosuppressive properties
AR044510A1 (es) 2003-04-14 2005-09-14 Merck & Co Inc Procedimiento e intermedios para preparar acidos carboxilicos de pirrolidina
US7176214B2 (en) 2003-05-21 2007-02-13 Bristol-Myers Squibb Company Imidazo-fused oxazolo[4,5-β]pyridine and imidazo-fused thiazolo[4,5-β]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
US7169926B1 (en) 2003-08-13 2007-01-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
CA2540868A1 (en) 2003-10-09 2005-04-21 Abbott Laboratories Pyrrolidinyl urea derivatives as angiogenesis inhibitors
US7592466B2 (en) * 2003-10-09 2009-09-22 Abbott Laboratories Ureas having antiangiogenic activity
MXPA06013250A (es) 2004-05-14 2007-02-28 Abbott Lab Inhibidores de quinasa como agentes terapeuticos.
PE20060526A1 (es) 2004-06-15 2006-07-13 Schering Corp Compuestos triciclicos como antagonistas de mglur1
US8039009B2 (en) 2004-06-17 2011-10-18 Forest Laboratories Holdings Limited Modified release formulations of memantine oral dosage forms
WO2006010567A1 (de) 2004-07-23 2006-02-02 Curacyte Discovery Gmbh INHIBITOREN DER PHOSPHODIESTERASE 4 UND TNFα-FREISETZUNG
US7626021B2 (en) 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
CA2573573A1 (en) 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
CN100381175C (zh) 2004-10-09 2008-04-16 山西中医学院 一种微乳制剂及其制备方法
CN101098872B (zh) 2004-11-22 2012-09-05 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的吡咯并吡嗪和吡唑并吡嗪
RS50996B (sr) 2004-12-21 2010-10-31 Arena Pharmaceuticals Inc. Kristalni oblici (r)-8-hloro-1-metil-2,3,4,5-tetrahidro-1h-benzazepin hlorhidrat
EP1844048B1 (en) 2005-01-14 2010-05-26 Janssen Pharmaceutica N.V. Pyrazolopyrimidines as cell cycle kinase inhibitors
CA2594425A1 (en) 2005-01-14 2006-07-20 Janssen Pharmaceutica N.V. 5-membered annelated heterocyclic pyrimidines as kinase inhibitors
US20060183758A1 (en) * 2005-02-17 2006-08-17 Cb Research And Development, Inc. Method for synthesis of AZA-annelated pyrroles, thiophenes, and furans
JP2008538119A (ja) 2005-04-01 2008-10-09 コーリー ファーマシューティカル グループ，インコーポレーテッド ピラゾロ［３，４−ｃ］キノリン類、ピラゾロ［３，４−ｃ］ナフチリジン類、これらの類似体、および方法
US7737279B2 (en) 2005-05-10 2010-06-15 Bristol-Myers Squibb Company 1,6-dihydro-1,3,5,6-tetraaza-as-indacene based tricyclic compounds and pharmaceutical compositions comprising same
US7593820B2 (en) 2005-05-12 2009-09-22 Cytopia Research Pty Ltd Crystal structure of human Janus Kinase 2 (JAK2) and uses thereof
EP1910358A2 (en) 2005-07-14 2008-04-16 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
CN102127078A (zh) 2005-07-14 2011-07-20 安斯泰来制药株式会社 Janus激酶3的杂环类抑制剂
JP5016601B2 (ja) 2005-08-16 2012-09-05 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤としての化合物および組成物
US8106066B2 (en) * 2005-09-23 2012-01-31 Memory Pharmaceuticals Corporation Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines, and preparation and uses thereof
KR20080048550A (ko) * 2005-09-23 2008-06-02 메모리 파마슈티칼스 코포레이션 인다졸, 벤조티아졸, 벤조이소티아졸, 벤즈이속사졸,피라졸로피리딘, 이소티아졸로피리딘, 및 이들의 제법 및용도
EP1937683A4 (en) 2005-09-23 2010-08-25 Coley Pharm Group Inc PROCESS FOR 1H-IMIDAZO [4,5-C] PYRIDINES AND ANALOGUE THEREOF
WO2007061764A2 (en) 2005-11-22 2007-05-31 Merck & Co., Inc. Tricyclic compounds useful as inhibitors of kinases
TW201307354A (zh) 2005-12-29 2013-02-16 Abbott Lab 蛋白質激酶抑制劑
CN101460461B (zh) * 2006-04-03 2012-10-03 弗·哈夫曼-拉罗切有限公司 对映体富集的环β-芳基或杂芳基羧酸的制备方法
ATE522518T1 (de) 2006-05-31 2011-09-15 Takeda San Diego Inc Indazol- und isoindolderivate als glucokinaseaktivierende stoffe
WO2008019996A2 (en) 2006-08-14 2008-02-21 Boehringer Ingelheim International Gmbh Formulations of flibanserin and method for manufacturing the same
US8063225B2 (en) 2006-08-14 2011-11-22 Chembridge Corporation Tricyclic compound derivatives useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders
CN101553224A (zh) 2006-10-06 2009-10-07 艾博特公司 新型咪唑并噻唑和咪唑并唑
AU2007337886C1 (en) 2006-12-22 2014-10-16 Astex Therapeutics Limited Bicyclic heterocyclic compounds as FGFR inhibitors
EP2123651A4 (en) 2007-01-12 2011-05-04 Astellas Pharma Inc CONDENSED PYRIDINE COMPOUND
CN101230059B (zh) * 2007-01-23 2011-08-17 上海恒瑞医药有限公司 双环氮杂烷类衍生物、其制备方法及其在医药上的用途
US20110281821A9 (en) 2007-01-30 2011-11-17 Biogen Idec Ma Inc. Modulators of Mitotic Kinases
WO2008112695A2 (en) 2007-03-12 2008-09-18 Irm Llc Pyrazolo [3,4-d] pyrimidines and 1, 2, 5, 6-tetraaza- as- indacenes as protein kinase inhibitors for cancer treatment
US7834024B2 (en) 2007-03-26 2010-11-16 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
US7691869B2 (en) 2007-03-30 2010-04-06 King Pharmaceuticals Research And Development, Inc. Pyrrolotriazolopyrimidine derivatives, pharmaceutical compositions containing them and methods of treating conditions and diseases mediated by the adenosine A2A receptor activity
US20110160185A9 (en) 2007-04-02 2011-06-30 Jorge Salas Solana Pyrrolopyrimidine derivatives as jak3 inhibitors
AU2007352872B2 (en) 2007-05-07 2013-03-14 Evonik Operations Gmbh Solid dosage forms comprising an enteric coating with accelerated drug release
SI2152712T1 (sl) 2007-05-11 2012-03-30 Pfizer Amino heterociklične spojine
US8188083B2 (en) 2007-06-28 2012-05-29 Abbott Laboratories Triazolopyridazines
US20090022789A1 (en) 2007-07-18 2009-01-22 Supernus Pharmaceuticals, Inc. Enhanced formulations of lamotrigine
GB0720041D0 (en) 2007-10-12 2007-11-21 Astex Therapeutics Ltd New Compounds
US20090169618A1 (en) 2007-12-26 2009-07-02 Limor Ari-Pardo Zolpidem pharmaceutical compositions
RU2503676C2 (ru) * 2008-02-25 2014-01-10 Ф.Хоффманн-Ля Рош Аг Пирролопиразиновые ингибиторы киназы
ATE517107T1 (de) 2008-02-25 2011-08-15 Hoffmann La Roche Pyrrolopyrazinkinaseinhibitoren
EP2250172B1 (en) * 2008-02-25 2011-08-31 F. Hoffmann-La Roche AG Pyrrolopyrazine kinase inhibitors
WO2009108827A1 (en) 2008-02-29 2009-09-03 Wyeth Fused tricyclic pyrazolo[1, 5-a]pyrimidines, methods for preparation and uses thereof
EP2271317B1 (de) 2008-03-28 2017-04-19 Boehringer Ingelheim International GmbH Verfahren zur herstellung von säurepellets
RS54560B1 (sr) 2008-06-10 2016-06-30 Abbvie Inc. Triciklična jedinjenja
GB0810902D0 (en) 2008-06-13 2008-07-23 Astex Therapeutics Ltd New compounds
WO2010003133A2 (en) 2008-07-03 2010-01-07 Exelixis Inc. Cdk modulators
CN101638423B (zh) * 2008-07-29 2012-09-05 常州高新技术产业开发区三维工业技术研究所有限公司 根皮苷衍生物及其制备方法和用途
KR101276530B1 (ko) 2009-02-24 2013-06-18 머크 캐나다 인크. Ｃｒｔｈ２ 수용체 길항제로서의 인돌 유도체
WO2010117796A2 (en) 2009-03-30 2010-10-14 Codexis, Inc. Processes for the preparation of alpha-chloroketones from carboxylic acids
EP2420502A4 (en) 2009-04-14 2012-12-19 Astellas Pharma Inc CONDENSED PYRROLOPYRIDINE DERIVATIVE
GB0906472D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
GB0906470D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
US8367689B2 (en) 2009-05-06 2013-02-05 Portola Pharmaceuticals, Inc. Inhibitors of JAK
CN101904814A (zh) 2009-06-04 2010-12-08 上海恒瑞医药有限公司 制备载药乳剂的方法
FR2947276B1 (fr) 2009-06-24 2012-10-26 Seppic Sa Composition cosmetique a base de resines echangeuses d'ions chargees avec des lipoaminoacides
US8361962B2 (en) 2009-07-27 2013-01-29 Roche Palo Alto Llc Tricyclic inhibitors of JAK
AU2010277207B2 (en) 2009-07-31 2014-06-26 Sun Pharmaceutical Industries Limited Multi-layered, multiple unit pharmaceutical compositions
RU2012127368A (ru) 2009-12-01 2014-01-10 Эбботт Лэборетриз Новые трициклические соединения
MX354212B (es) 2010-03-10 2018-02-19 Incyte Corp Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
CA2788526A1 (en) 2010-05-14 2011-11-17 Alembic Limited Extended release formulations of desvenlafaxine base
AR081848A1 (es) 2010-06-09 2012-10-24 Presidio Pharmaceuticals Inc Inhibidores de la proteina ns5a del vhc
US8637529B2 (en) 2010-06-11 2014-01-28 AbbYie Inc. Pyrazolo[3,4-d]pyrimidine compounds
US9266855B2 (en) 2010-09-27 2016-02-23 AbbVie Deutschland GmbH & Co. KG Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors
US9011912B2 (en) 2010-10-07 2015-04-21 Abon Pharmaceuticals, Llc Extended-release oral dosage forms for poorly soluble amine drugs
US20120231083A1 (en) 2010-11-18 2012-09-13 The Board Of Trustees Of The University Of Illinois Sustained release cannabinoid medicaments
US20120330012A1 (en) 2011-04-29 2012-12-27 Abbott Laboratories Novel Tricyclic Compounds
WO2013043826A1 (en) 2011-09-21 2013-03-28 Abbvie Inc. Tricyclic compounds useful as protein kinase inhibitors
FR2991171B1 (fr) 2012-06-01 2014-05-23 Galderma Res & Dev Procede de preparation d'une composition dermatologique comprenant des oleosomes
WO2014004863A2 (en) 2012-06-27 2014-01-03 Alzheimer's Institute Of America, Inc. Compounds, compositions, and therapeutic uses thereof
KR20150028299A (ko) 2012-07-20 2015-03-13 조에티스 엘엘씨 야누스 키나제 (ｊａｋ) 억제제 투여요법
HUE054212T2 (hu) 2013-02-21 2021-08-30 Pfizer Szelektív CDK4/6 inhibitor szilárd formái
SI3290421T1 (sl) 2013-02-22 2019-03-29 Pfizer Inc. Kombinacija derivatov pirolo (2,3-D)pirimidina z enim ali več dodatnimi sredstvi za zaviranje z janusom povezane kinaze (JAK)
WO2014150289A1 (en) 2013-03-15 2014-09-25 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
JP6041823B2 (ja) 2013-03-16 2016-12-14 ファイザー・インク トファシチニブの経口持続放出剤形
WO2014174073A1 (en) 2013-04-26 2014-10-30 Sandoz Ag Sustained release formulations of tofacitinib
CA2926361A1 (en) * 2013-10-24 2015-04-30 Abbvie Inc. Jak1 selective inhibitor and uses thereof
CN106794126A (zh) 2014-08-27 2017-05-31 艾伯维公司 局部配制品
CA2987867C (en) 2015-06-09 2023-06-27 Capsugel Belgium Nv Formulations to achieve rapid dissolution of drug from spray-dried dispersions in capsules
US20180230127A1 (en) 2015-08-13 2018-08-16 Pfizer Inc. Bicyclic-Fused Heteroaryl Or Aryl Compounds
RS61719B1 (sr) 2015-08-27 2021-05-31 Pfizer Biciklična fuzionisana hetaroaril ili aril jedinjenja kao modulatori irak4
US11512092B2 (en) 2015-10-16 2022-11-29 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US10550126B2 (en) 2015-10-16 2020-02-04 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11524964B2 (en) 2015-10-16 2022-12-13 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
RU2018117889A (ru) 2015-10-16 2019-11-20 Эббви Инк. СПОСОБЫ ПОЛУЧЕНИЯ (3S,4R)-3-ЭТИЛ-4-(3H-ИМИДАЗО[1,2-a]ПИРРОЛО[2,3-e]-ПИРАЗИН-8-ИЛ)-N-(2,2,2-ТРИФТОРЭТИЛ)ПИРРОЛИДИН-1-КАРБОКСАМИДА И ЕГО ТВЕРДОФАЗНЫХ ФОРМ
US11773106B2 (en) 2015-10-16 2023-10-03 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11365198B2 (en) 2015-10-16 2022-06-21 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
DK3383363T3 (da) 2015-11-30 2021-01-18 Anacor Pharmaceuticals Inc Topiske farmaceutiske formuleringer til behandling af inflammatorisk-relaterede tilstande
WO2017126488A1 (ja) 2016-01-18 2017-07-27 持田製薬株式会社 乾癬治療用組成物および治療方法
JP7096592B2 (ja) 2016-02-16 2022-07-06 ワシントン・ユニバーシティ Ｊａｋ阻害剤およびこれらの利用
US12274794B2 (en) 2016-07-06 2025-04-15 Orient Pharma Co., Ltd. Oral dosage form with drug composition, barrier layer and drug layer
US11564922B2 (en) 2017-03-09 2023-01-31 Abbvie Inc. Methods of treating crohn's disease and ulcerative colitis
US20190046527A1 (en) 2017-03-09 2019-02-14 Abbvie Inc. Methods of treating crohn's disease and ulcerative colitis
EP4463161A2 (en) 2022-01-13 2024-11-20 Abbvie Inc. Method of administering upadacitinib to avoid adverse drug interactions and effects

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011068881A1 (en) * 2009-12-01 2011-06-09 Abbott Laboratories Novel tricyclic compounds

Also Published As

Publication number Publication date
US20250163071A1 (en) 2025-05-22
US20230312595A1 (en) 2023-10-05
SG10201913997WA (en) 2020-03-30
CA3002220A1 (en) 2017-04-20
US11718627B2 (en) 2023-08-08
US10344036B2 (en) 2019-07-09
US20240317770A1 (en) 2024-09-26
US20170342083A1 (en) 2017-11-30
US20230219968A1 (en) 2023-07-13
US20200291040A1 (en) 2020-09-17
US20240010656A1 (en) 2024-01-11
US20200361949A1 (en) 2020-11-19
US10981924B2 (en) 2021-04-20
US20230303582A1 (en) 2023-09-28
CA3123260C (en) 2025-03-11
AU2021236570A1 (en) 2021-10-28
US20240166657A1 (en) 2024-05-23
US20200181158A1 (en) 2020-06-11
CA3257305C (en) 2025-11-18
US20180141955A1 (en) 2018-05-24
SG10201913987UA (en) 2020-03-30
US9879018B2 (en) 2018-01-30
IL258654A (en) 2018-06-28
US11780847B1 (en) 2023-10-10
US9879019B2 (en) 2018-01-30
CA3123260A1 (en) 2017-04-20
MX2018004605A (es) 2018-11-29
BR112018007677A2 (pt) 2018-11-06
KR102753815B1 (ko) 2025-01-14
US20210363149A1 (en) 2021-11-25
SG10201913990RA (en) 2020-03-30
AU2025256155A1 (en) 2025-11-13
CA3254966A1 (en) 2025-04-12
US20220298165A1 (en) 2022-09-22
US20230322794A1 (en) 2023-10-12
US20180222914A1 (en) 2018-08-09
KR20180081523A (ko) 2018-07-16
US10202393B2 (en) 2019-02-12
CN116284011A (zh) 2023-06-23
US11773105B2 (en) 2023-10-03
KR20250010141A (ko) 2025-01-20
US11198697B1 (en) 2021-12-14
US20190023714A1 (en) 2019-01-24
CA3251507A1 (en) 2025-05-21
US10981923B2 (en) 2021-04-20
US9963459B1 (en) 2018-05-08
US11680069B2 (en) 2023-06-20
RU2018117889A3 (OSRAM) 2020-08-12
AU2016340167A1 (en) 2018-04-26
US20230312593A1 (en) 2023-10-05
CA3252663A1 (en) 2025-04-23
SG10201913989QA (en) 2020-03-30
CN108368121B (zh) 2023-01-13
JP2021020902A (ja) 2021-02-18
US11186584B2 (en) 2021-11-30
CA3257305A1 (en) 2025-06-12
JP2019501865A (ja) 2019-01-24
JP2024073591A (ja) 2024-05-29
US20210309667A1 (en) 2021-10-07
JP2022107001A (ja) 2022-07-20
CA3002220C (en) 2021-07-20
US20170129902A1 (en) 2017-05-11
CN120483986A (zh) 2025-08-15
CN108368121A (zh) 2018-08-03
EP4647129A3 (en) 2025-12-31
US11661425B2 (en) 2023-05-30
IL283531A (en) 2021-07-29
EP4219503A1 (en) 2023-08-02
RU2018117889A (ru) 2019-11-20
US20180162865A1 (en) 2018-06-14
US10519164B2 (en) 2019-12-31
US20240376115A1 (en) 2024-11-14
US20230374027A1 (en) 2023-11-23
IL314468A (en) 2024-09-01
AU2023251492B2 (en) 2025-04-03
JP7358317B2 (ja) 2023-10-10
US12116373B2 (en) 2024-10-15
SG10201913993QA (en) 2020-03-30
SG10201913999PA (en) 2020-03-30
US20190315761A1 (en) 2019-10-17
US12110297B2 (en) 2024-10-08
US20240034740A1 (en) 2024-02-01
US20170362247A1 (en) 2017-12-21
US12110298B2 (en) 2024-10-08
US20230058001A1 (en) 2023-02-23
US11787815B1 (en) 2023-10-17
AU2023251492A1 (en) 2023-11-09
SG10201913986YA (en) 2020-03-30
EP3362455A1 (en) 2018-08-22
US20230183257A1 (en) 2023-06-15
US20180186805A1 (en) 2018-07-05
JP2025166113A (ja) 2025-11-05
CN120289468A (zh) 2025-07-11
CA3257291A1 (en) 2025-04-07
US12077545B2 (en) 2024-09-03
US12103933B2 (en) 2024-10-01
SG11201802990RA (en) 2018-05-30
WO2017066775A1 (en) 2017-04-20
US20230348481A1 (en) 2023-11-02
US12134621B2 (en) 2024-11-05
AU2025205010A1 (en) 2025-07-24
US11795175B2 (en) 2023-10-24
CN116270646A (zh) 2023-06-23
US20230331735A1 (en) 2023-10-19
CN116270645A (zh) 2023-06-23
MX2021013812A (es) 2021-12-14
JP2025166112A (ja) 2025-11-05
US11535624B2 (en) 2022-12-27
BR122022024925B1 (pt) 2023-11-28
MX387822B (es) 2025-03-19
US12091415B2 (en) 2024-09-17
CA3252702A1 (en) 2025-07-08
US10730883B2 (en) 2020-08-04
AU2016340167A8 (en) 2018-05-10
AU2021236570B2 (en) 2023-11-02
CN120478294A (zh) 2025-08-15
US20230203049A1 (en) 2023-06-29
US20180222913A1 (en) 2018-08-09
US20230057084A1 (en) 2023-02-23
US20240174682A1 (en) 2024-05-30
US20200317682A1 (en) 2020-10-08
EP4647129A2 (en) 2025-11-12
HK1263380A1 (zh) 2020-05-29
JP2023113917A (ja) 2023-08-16
US9951080B2 (en) 2018-04-24
US10202394B2 (en) 2019-02-12
US10017517B2 (en) 2018-07-10
US20180057502A1 (en) 2018-03-01
US20190322677A1 (en) 2019-10-24
JP6770775B2 (ja) 2020-10-21
US10597400B2 (en) 2020-03-24

Similar Documents

Publication Publication Date Title
AU2023251492B2 (en) Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
HK40099372A (en) Crystalline l-maleate of (3s,4r)-3-ethyl-4-(3h-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide

Legal Events

Date Code Title Description
TH Corrigenda

Free format text: IN VOL 32 , NO 16 , PAGE(S) 2230 UNDER THE HEADING PCT APPLICATIONS THAT HAVE ENTERED THE NATIONAL PHASE - NAME INDEX UNDER THE NAME ABBVIE INC., APPLICATION NO. 2016340167, UNDER INID (72) CORRECT THE CO-INVENTOR TO NORDSTROEM, LARS F.

DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE INVENTOR TO READ ALLIAN, AYMEN D.; JAYANTH, JAYANTHY; MOHAMED, MOHAMED-ESLAM F.; MULHERN, MATHEW M.; NORDSTROM, LARS F.; OTHMAN, AHMED A.; ROZEMA, MICHAEL J.; BHAGAVATULA, LAKSHMI; MARROUM, PATRICK J.; MAYER, PETER T.; SHEIKH, AHMAD Y. AND BORCHARDT, THOMAS B.

DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE INVENTOR TO READ ALLIAN, AYMEN D.; JAYANTH, JAYANTHY; MOHAMED, MOHAMED-ESLAM F.; MULHERN, MATHEW M.; NORDSTROM, FREDRIK LARS; OTHMAN, AHMED A.; ROZEMA, MICHAEL J.; BHAGAVATULA, LAKSHMI; MARROUM, PATRICK J.; MAYER, PETER T.; SHEIKH, AHMAD Y. AND BORCHARDT, THOMAS B.

DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE INVENTOR TO READ ALLIAN, AYMAN D.; JAYANTH, JAYANTHY; MOHAMED, MOHAMED-ESLAM F.; MULHERN, MATHEW M.; NORDSTROM, FREDRIK LARS; OTHMAN, AHMED A.; ROZEMA, MICHAEL J.; BHAGAVATULA, LAKSHMI; MARROUM, PATRICK J.; MAYER, PETER T.; SHEIKH, AHMAD Y. AND BORCHARDT, THOMAS B.

DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE INVENTOR TO READ ALLIAN, AYMAN D.; JAYANTH, JAYANTHY; MOHAMED, MOHAMED-ESLAM F.; MULHERN, MATHEW M.; NORDSTROM, FREDRIK LARS; OTHMAN, AHMED A.; ROZEMA, MICHAEL J.; BHAGAVATULA, LAKSHMI; MARROUM, PATRICK J.; MAYER, PETER T.; SHEIKH, AHMAD Y.; BORCHARDT, THOMAS B. AND KLUENDER, BEN

FGA Letters patent sealed or granted (standard patent)