CA3002220C - 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

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CA3002220C
CA3002220C CA3002220A CA3002220A CA3002220C CA 3002220 C CA3002220 C CA 3002220C CA 3002220 A CA3002220 A CA 3002220A CA 3002220 A CA3002220 A CA 3002220A CA 3002220 C CA3002220 C CA 3002220C
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compound
formula
freebase
solid state
another aspect
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CA3002220A
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French (fr)
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CA3002220A1 (en
Inventor
Ayman D. Allian
Jayanthy Jayanth
Mohamed-Eslam F. Mohamed
Mathew M. Mulhern
Fredrik Lars Nordstrom
Ahmad Y. Sheikh
Michael J. Rozema
Lakshmi Bhagavatula
Patrick J. MARROUM
Peter T. Mayer
Thomas B. Borchardt
Ahmed A. Othman
Ben Kluender
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AbbVie Inc
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AbbVie Inc
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Priority to CA3123260A priority Critical patent/CA3123260C/en
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    • 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

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  • 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)
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  • Pharmacology & Pharmacy (AREA)
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  • 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)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Diabetes (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)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CA3002220A 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 CA3002220C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CA3123260A CA3123260C (en) 2015-10-16 2016-10-17 CRYSTALLINE HEMIHYDRATE OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-A]PYRROLO[2,3-E]PYRAZINE-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND FORMS IN SOLID STATE

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)

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CA3123260A Division CA3123260C (en) 2015-10-16 2016-10-17 CRYSTALLINE HEMIHYDRATE OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-A]PYRROLO[2,3-E]PYRAZINE-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND FORMS IN SOLID STATE

Publications (2)

Publication Number Publication Date
CA3002220A1 CA3002220A1 (en) 2017-04-20
CA3002220C true CA3002220C (en) 2021-07-20

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Family Applications (7)

Application Number Title Priority Date Filing Date
CA3123260A Active CA3123260C (en) 2015-10-16 2016-10-17 CRYSTALLINE HEMIHYDRATE OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-A]PYRROLO[2,3-E]PYRAZINE-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND FORMS IN SOLID STATE
CA3257305A Active CA3257305C (en) 2015-10-16 2016-10-17 PROCESS FOR 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 ITS SOLID FORMS
CA3251507A Pending CA3251507A1 (en) 2015-10-16 2016-10-17 Use of a solid dosage form comprising (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 for treating rheumatoid arthritis
CA3254966A Pending CA3254966A1 (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
CA3002220A Active CA3002220C (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
CA3252702A Pending CA3252702A1 (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]PYRAZINE-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND RELATED SOLID FORMS
CA3257291A Pending CA3257291A1 (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]PYRAZINE-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND RELATED SOLID FORMS

Family Applications Before (4)

Application Number Title Priority Date Filing Date
CA3123260A Active CA3123260C (en) 2015-10-16 2016-10-17 CRYSTALLINE HEMIHYDRATE OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-A]PYRROLO[2,3-E]PYRAZINE-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND FORMS IN SOLID STATE
CA3257305A Active CA3257305C (en) 2015-10-16 2016-10-17 PROCESS FOR 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 ITS SOLID FORMS
CA3251507A Pending CA3251507A1 (en) 2015-10-16 2016-10-17 Use of a solid dosage form comprising (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 for treating rheumatoid arthritis
CA3254966A Pending CA3254966A1 (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

Family Applications After (2)

Application Number Title Priority Date Filing Date
CA3252702A Pending CA3252702A1 (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]PYRAZINE-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND RELATED SOLID FORMS
CA3257291A Pending CA3257291A1 (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]PYRAZINE-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND RELATED SOLID FORMS

Country Status (13)

Country Link
US (39) US20170129902A1 (enExample)
EP (3) EP4219503A1 (enExample)
JP (7) JP6770775B2 (enExample)
KR (2) KR20250010141A (enExample)
CN (7) CN120478294A (enExample)
AU (5) AU2016340167B2 (enExample)
BR (1) BR122022024925B1 (enExample)
CA (7) CA3123260C (enExample)
IL (3) IL314468A (enExample)
MX (2) MX387822B (enExample)
RU (1) RU2018117889A (enExample)
SG (8) SG10201913987UA (enExample)
WO (1) WO2017066775A1 (enExample)

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
ME02800B (me) 2009-12-01 2018-01-20 Abbvie Inc Nova triciklična jedinjenja
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
CN120478294A (zh) 2015-10-16 2025-08-15 艾伯维公司 制备咪唑并[1,2-a]吡咯并[2,3-e]吡嗪类化合物及其固态形式的方法
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
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
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
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
US11780848B2 (en) 2015-10-16 2023-10-10 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
CN110392572A (zh) 2017-03-09 2019-10-29 艾伯维公司 治疗克罗恩病和溃疡性结肠炎的方法
US20210163409A1 (en) * 2017-07-19 2021-06-03 Dr. Reddy's Laboratories Limited Alternate processes for the preparation of pyrrolidine derivatives
EP4424328A3 (en) * 2018-03-30 2024-12-04 Incyte Corporation Treatment of hidradenitis suppurativa using jak inhibitors
EP3845521B1 (en) * 2018-08-31 2024-11-06 Suzhou Pengxu Pharmatech Co., Ltd. Synthesis methods for upadacitinib and intermediate thereof
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
WO2020063939A1 (zh) * 2018-09-29 2020-04-02 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
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
WO2020115212A1 (en) 2018-12-05 2020-06-11 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
US20210380596A1 (en) * 2019-03-01 2021-12-09 Crystal Pharmaceutical (Suzhou) Co., Ltd. Upadacitinib crystal form and preparation method therefor and use thereof
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
WO2021067465A1 (en) 2019-09-30 2021-04-08 Abbvie Inc. Treating spondyloarthritic and psoriatic conditions with upadacitinib
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
WO2021244323A1 (zh) * 2020-06-05 2021-12-09 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
AU2021303629A1 (en) * 2020-07-08 2023-03-09 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
AU2022255047A1 (en) * 2021-04-07 2023-10-19 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
WO2023131978A1 (en) * 2022-01-06 2023-07-13 Msn Laboratories Private Limited, R&D Center Improved process for the preparation of upadacitinib
EP4465971A1 (en) 2022-01-20 2024-11-27 Renata Phramaceutical (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
WO2024197127A1 (en) 2023-03-22 2024-09-26 Abbvie Inc. Methods of treating pediatric patients with upadacitinib
AU2024275269A1 (en) 2023-05-23 2025-11-06 Abbvie Inc. Methods of treating vitiligo with upadacitinib
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
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
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
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

Family Cites Families (150)

* 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 (enExample) 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
DE69033614T2 (de) 1989-10-20 2001-04-19 Kyowa Hakko Kogyo K.K., Tokio/Tokyo Kondensierte Purinderivate
KR927003044A (ko) 1990-01-11 1992-12-17 크리스토퍼 케이. 미라벨리 Rna 활성과 유전자 발현을 검출하고 조절하는 조성물 및 그 방법
US6262241B1 (en) 1990-08-13 2001-07-17 Isis Pharmaceuticals, Inc. Compound for detecting and modulating RNA activity and gene expression
DE69233701T2 (de) 1991-03-18 2008-04-10 New York University Monoklonale und chimäre Antikörper spezifisch für menschlichen Tumornekrosefaktor
CA2110942A1 (en) 1991-06-14 1992-12-23 Pharmacia & Upjohn Company Llc Imidazo¬1,5-a|quinoxalines
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
DE69329503T2 (de) 1992-11-13 2001-05-03 Idec Pharma Corp Therapeutische Verwendung von chimerischen und markierten Antikörpern, die gegen ein Differenzierung-Antigen gerichtet sind, dessen Expression auf menschliche B Lymphozyt beschränkt ist, für die Behandlung von B-Zell-Lymphoma
AU681875B2 (en) 1993-02-26 1997-09-11 Schering Corporation 2-benzyl-polycyclic guanine derivatives and process for preparing them
US5736540A (en) 1993-07-29 1998-04-07 American Cyanamid Company Tricyclic diazepine vasopressin antagonists and oxytocin antagonists
US5733905A (en) 1993-07-29 1998-03-31 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
CN1191242C (zh) 1997-02-05 2005-03-02 麦克公司 不同结晶型的(－)－6－氯－4－环丙乙炔基－4－三氟甲基－1,4－二氢－2h－3,1－苯并噁嗪－2－酮
WO1999045009A1 (en) 1998-03-04 1999-09-10 Bristol-Myers Squibb Company Heterocyclo-substituted imidazopyrazine protein tyrosine kinase inhibitors
BR9913701A (pt) 1998-09-14 2001-06-05 Warner Lambert Co ácidos alquil pirrolidina-3-carboxìlicos ramificados
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
IL139197A0 (en) 1999-10-29 2001-11-25 Pfizer Prod Inc Use of corticotropin releasing factor antagonists and related compositions
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
MXPA03001186A (es) 2000-08-07 2004-04-20 Neurogen Corp Compuestos heterociclicos como ligandos del receptor acido gamma aminobutirico (gabaa).
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
WO2003070236A2 (en) 2002-02-19 2003-08-28 Pharmacia Italia S.P.A. Tricyclic pyrazole derivatives, process for their preparation and their use as antitumor agents
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
CA2501947A1 (en) 2002-10-09 2004-04-22 Scios Inc. Azaindole derivatives as inhibitors of p38 kinase
WO2004065378A1 (en) 2003-01-17 2004-08-05 Warner-Lambert Company Llc 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation
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
DE602004018811D1 (de) 2003-10-09 2009-02-12 Abbott Lab Pyrrolidinylharnstoffderivate als angiogeneseinhibitoren
US7592466B2 (en) 2003-10-09 2009-09-22 Abbott Laboratories Ureas having antiangiogenic activity
US20060074102A1 (en) 2004-05-14 2006-04-06 Kevin Cusack Kinase inhibitors as therapeutic agents
AR049300A1 (es) 2004-06-15 2006-07-12 Schering Corp Compuestos triciclicos antagonistas de mglur1 como agentes terapeuticos
CN1968684A (zh) 2004-06-17 2007-05-23 森林实验室公司 美金刚的调释制剂
EP1773840B1 (de) 2004-07-23 2010-01-20 The Medicines Company (Leipzig) GmbH Substituierte pyrido[3',2':4,5]thieno[3,2-d]pyrimidine und pyrido[3',2':4,5]furo[3,2-d]-pyrimidine zur verwendung als inhibitoren der pda-4 und/oder tnf-alpha freisetzung
US7626021B2 (en) 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
EP2239262A3 (en) 2004-07-27 2011-10-19 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
CA2587926A1 (en) 2004-11-22 2006-06-01 Vertex Pharmaceuticals Incorporated Bicyclic inhibitors or rho kinase
US8168624B2 (en) 2004-12-21 2012-05-01 Arena Pharmaceuticals, Inc. Crystalline forms of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride
EP1844048B1 (en) 2005-01-14 2010-05-26 Janssen Pharmaceutica N.V. Pyrazolopyrimidines as cell cycle kinase inhibitors
WO2006074985A1 (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
CA2603063A1 (en) 2005-04-01 2006-10-12 Coley Pharmaceutical Group, Inc. Pyrazolo[3,4-c]quinolines, pyrazolo[3,4-c]naphthyridines, analogs thereof, and methods
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
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
EP1910358A2 (en) 2005-07-14 2008-04-16 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
MX2008002165A (es) 2005-08-16 2008-04-29 Irm Llc Compuestos y composiciones como inhibidores de la proteina cinasa.
US8106066B2 (en) * 2005-09-23 2012-01-31 Memory Pharmaceuticals Corporation Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines, and preparation and uses thereof
BRPI0616338A2 (pt) 2005-09-23 2011-06-14 Coley Pharm Group Inc mÉtodo para 1h-imidazo[4,5-c] piridinas e anÁlogos da mesma
JP2009509964A (ja) * 2005-09-23 2009-03-12 メモリー・ファーマシューティカルズ・コーポレイション インダゾール類、ベンゾチアゾール類、ベンゾイソオキサゾール類、ピラゾロピリジン類、イソチアゾロピリジン類、およびそれらの製造と用途
US8518964B2 (en) 2005-11-22 2013-08-27 Merck Sharp & Dohme Corp. Tricyclic compounds useful as inhibitors of kinases
CN101389630A (zh) 2005-12-29 2009-03-18 艾博特公司 蛋白激酶抑制剂
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
EP2049518B1 (en) 2006-05-31 2011-08-31 Takeda San Diego, Inc. Indazole and isoindole derivatives as glucokinase activating agents.
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
AU2007286288A1 (en) 2006-08-14 2008-02-21 Boehringer Ingelheim International Gmbh Formulations of flibanserin and method for manufacturing the same
CA2665214A1 (en) 2006-10-06 2008-05-29 Abbott Laboratories Novel imidazothiazoles and imidazoxazoles
MX2009006706A (es) 2006-12-22 2009-07-02 Astex Therapeutics Ltd Compuestos heterociclicos biciclicos como inhibidores del receptor del factor de crecimiento de fibroblastos.
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
JP2010516812A (ja) 2007-01-30 2010-05-20 バイオジェン・アイデック・エムエイ・インコーポレイテッド 有糸分裂キナーゼの調節剤
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
US7723343B2 (en) 2007-03-30 2010-05-25 King Pharmaceuticals Research And Development, Inc. Adenosine A2A receptor antagonists
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
GEP20125405B (en) 2007-05-11 2012-02-27 Pfizer Amino-heterocyclic compounds
EP2170337A4 (en) 2007-06-28 2013-12-18 Abbvie Inc NEW TRIAZOLOPYRIDAZINE
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
CN101945877B (zh) 2008-02-25 2013-07-03 霍夫曼-拉罗奇有限公司 吡咯并吡嗪激酶抑制剂
JP5529049B2 (ja) 2008-02-25 2014-06-25 エフ．ホフマン−ラ ロシュ アーゲー ピロロピラジンキナーゼ阻害剤
MX2010008198A (es) 2008-02-25 2010-08-23 Hoffmann La Roche Inhibidores de cinasa de pirrolopirazina.
WO2009108827A1 (en) 2008-02-29 2009-09-03 Wyeth Fused tricyclic pyrazolo[1, 5-a]pyrimidines, methods for preparation and uses thereof
WO2009118321A1 (de) 2008-03-28 2009-10-01 Boehringer Ingelheim International Gmbh Verfahren zur herstellung von säurepellets
ME02340B (me) 2008-06-10 2017-02-20 Abbvie Inc Triciklična jedinjenja
GB0810902D0 (en) 2008-06-13 2008-07-23 Astex Therapeutics Ltd New compounds
EP2320895A2 (en) 2008-07-03 2011-05-18 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
ES2450594T3 (es) 2009-02-24 2014-03-25 Merck Sharp & Dohme Corp. Derivados de indol como antagonistas del receptor CRTH2
WO2010117796A2 (en) 2009-03-30 2010-10-14 Codexis, Inc. Processes for the preparation of alpha-chloroketones from carboxylic acids
RU2011146059A (ru) 2009-04-14 2013-05-20 Астеллас Фарма Инк. Конденсированное пирролопиридиновое производное
GB0906470D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
GB0906472D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
AR076550A1 (es) 2009-05-06 2011-06-22 Portola Pharm Inc Inhibidores de la janus tirosina kinasa (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
EP2459180A1 (en) 2009-07-31 2012-06-06 Ranbaxy Laboratories Limited Multi-layered, multiple unit pharmaceutical compositions
CA2781010A1 (en) 2009-12-01 2011-06-09 Abbott Laboratories Novel tricyclic compounds
ME02800B (me) 2009-12-01 2018-01-20 Abbvie Inc Nova triciklična jedinjenja
DK3354652T3 (da) 2010-03-10 2020-05-18 Incyte Holdings Corp Piperidin-4-yl azetidinderivativer som jak1-inhibitorer
WO2011141791A2 (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
WO2011156698A2 (en) 2010-06-11 2011-12-15 Abbott Laboratories NOVEL PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS
CN103119035B (zh) 2010-09-27 2015-09-30 雅培股份有限两合公司 杂环化合物和它们作为糖原合成酶激酶-3抑制剂的用途
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
WO2012149280A2 (en) 2011-04-29 2012-11-01 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
CN104470525A (zh) 2012-07-20 2015-03-25 硕腾有限责任公司 Janus激酶(jak)抑制剂的给药方案
EP2958916B1 (en) 2013-02-21 2018-09-12 Pfizer Inc Solid forms of a selective cdk4/6 inhibitor
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)
EA201591427A1 (ru) 2013-03-15 2016-01-29 Глобал Блад Терапьютикс, Инк. Соединения и их применения для модуляции гемоглобина
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
US20170266289A1 (en) 2014-08-27 2017-09-21 Abbvie Inc. Topical formulation
US12133911B2 (en) 2015-06-09 2024-11-05 Capsugel Belgium Nv Formulations to achieve rapid dissolution of drug from spray-dried dispersions in capsules
JP2018527337A (ja) 2015-08-13 2018-09-20 ファイザー・インク 二環式縮合ヘテロアリールまたはアリール化合物
JP6804524B2 (ja) 2015-08-27 2020-12-23 ファイザー・インク Ｉｒａｋ４モジュレーターとしての二環式縮合ヘテロアリールまたはアリール化合物
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
US11780848B2 (en) 2015-10-16 2023-10-10 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
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
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
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
CN120478294A (zh) 2015-10-16 2025-08-15 艾伯维公司 制备咪唑并[1,2-a]吡咯并[2,3-e]吡嗪类化合物及其固态形式的方法
SI3383363T1 (sl) 2015-11-30 2021-03-31 Anacor Pharmaceuticals, Inc. Topične farmacevtske formulacije za zdravljenje vnetnih bolezenskih stanj
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
WO2017143014A1 (en) 2016-02-16 2017-08-24 Brian Kim Jak inhibitors and uses thereof
EP3481381B1 (en) 2016-07-06 2025-01-08 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
CN110392572A (zh) 2017-03-09 2019-10-29 艾伯维公司 治疗克罗恩病和溃疡性结肠炎的方法
CA3246767A1 (en) 2022-01-13 2023-07-20 Abbvie Inc. METHOD OF ADMINISTRATION OF UPADACITINIB TO AVOID DRUG INTERACTIONS AND ADVERSE EFFECTS

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