WO2011068881A1 - Novel tricyclic compounds - Google Patents

Novel tricyclic compounds Download PDF

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Publication number
WO2011068881A1
WO2011068881A1 PCT/US2010/058572 US2010058572W WO2011068881A1 WO 2011068881 A1 WO2011068881 A1 WO 2011068881A1 US 2010058572 W US2010058572 W US 2010058572W WO 2011068881 A1 WO2011068881 A1 WO 2011068881A1
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WO
WIPO (PCT)
Prior art keywords
optionally substituted
cio
pyrrolo
pyrazin
compound
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.)
Ceased
Application number
PCT/US2010/058572
Other languages
English (en)
French (fr)
Inventor
Neil Wishart
Maria A. Argiriadi
David J. Calderwood
Anna M. Ericsson
Bryan A. Fiamengo
Kristine E. Frank
Michael Friedman
Dawn M. George
Eric R. Goedken
Nathan S. Josephsohn
Biqin C. Li
Michael J. Morytko
Kent D. Stewart
Jeffrey W. Voss
Grier A. Wallace
Lu Wang
Kevin R. Woller
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.)
Abbott Laboratories
Original Assignee
Abbott Laboratories
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=44070404&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2011068881(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority to AU2010326108A priority Critical patent/AU2010326108C1/en
Priority to RU2012127306A priority patent/RU2570416C9/ru
Priority to RS20170760A priority patent/RS56317B1/sr
Priority to MX2012006311A priority patent/MX346959B/es
Priority to SG2012040465A priority patent/SG181472A1/en
Priority to KR1020187025442A priority patent/KR20180101626A/ko
Priority to CR20170159A priority patent/CR20170159A/es
Priority to NZ600161A priority patent/NZ600161A/en
Priority to LTEP10835061.2T priority patent/LT2506716T/lt
Priority to EP21173353.0A priority patent/EP3950692A1/en
Priority to ES10835061.2T priority patent/ES2637588T3/es
Priority to DK10835061.2T priority patent/DK2506716T3/en
Priority to PL10835061T priority patent/PL2506716T3/pl
Priority to EP10835061.2A priority patent/EP2506716B1/en
Priority to JP2012542161A priority patent/JP5607174B2/ja
Priority to CN201080062920.6A priority patent/CN102711476B/zh
Priority to UAA201207925A priority patent/UA111466C2/uk
Priority to HRP20171175TT priority patent/HRP20171175T1/hr
Priority to PH1/2012/501076A priority patent/PH12012501076B1/en
Priority to MEP-2017-167A priority patent/ME02800B/me
Priority to KR1020127017105A priority patent/KR101785257B1/ko
Priority to BR112012013349-7A priority patent/BR112012013349B1/pt
Application filed by Abbott Laboratories filed Critical Abbott Laboratories
Priority to CA2781891A priority patent/CA2781891C/en
Priority to KR1020177027803A priority patent/KR20170118230A/ko
Priority to SI201031517T priority patent/SI2506716T1/sl
Publication of WO2011068881A1 publication Critical patent/WO2011068881A1/en
Priority to IL220054A priority patent/IL220054A/en
Priority to ZA2012/03999A priority patent/ZA201203999B/en
Anticipated expiration legal-status Critical
Priority to AU2016201825A priority patent/AU2016201825B2/en
Priority to PH12016501009A priority patent/PH12016501009A1/en
Priority to IL248466A priority patent/IL248466A/en
Priority to IL253516A priority patent/IL253516B/en
Priority to CY20171100817T priority patent/CY1119175T1/el
Priority to AU2018201663A priority patent/AU2018201663B2/en
Priority to IL261778A priority patent/IL261778A/en
Priority to AU2020201390A priority patent/AU2020201390A1/en
Priority to LU00149C priority patent/LUC00149I2/fr
Priority to NO2020006C priority patent/NO2020006I1/no
Priority to CY2020007C priority patent/CY2020007I2/el
Priority to NL301035C priority patent/NL301035I2/nl
Priority to LTPA2020505C priority patent/LTC2506716I2/lt
Ceased legal-status Critical Current

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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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    • A61P7/08—Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
    • A—HUMAN NECESSITIES
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
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    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Definitions

  • the invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Jakl, Jak2, Jak3, Tyk2, KDR, Flt-3, CDK2, CDK4, TANK, Trk, FAK, Abl, Bcr-Abl, cMet, b-RAF, FGFR3, c-kit, PDGF-R, Syk, BTK, CSF1R, PKC kinases or Aurora kinases.
  • the protein kinases represent a large family of proteins that play a central role in the regulation of a wide variety of cellular processes and maintenance of cellular function.
  • a partial, non-limiting, list of these kinases include: non-receptor tyrosine kinases such as the Janus kinase family (Jakl, Jak2, Jak3 and Tyk2); the fusion kinases, such as BCR-Abl, focal adhesion kinase (FAK), Fes, Lck and Syk; receptor tyrosine kinases such as platelet-derived growth factor receptor kinase (PDGF-R), the receptor kinase for stem cell factor, c-kit, the hepatocyte growth factor receptor, c-Met, and the fibroblast growth factor receptor, FGFR3; and serine/threonine kinases such as b-RAF, mitogen-activated protein kinases (e.g., MKK6) and SAPKZp.
  • the invention provdes a compound according to the any of the foregoing embodiments wherein T is N, U is N, X is CR 3 and Y is N and forms a compound of Formula (la)
  • Phenyl-carbamic acid (15,3 ⁇ ,45)-3-6 1-4-(6 ⁇ 1 ⁇ [2,3-6][1,2,4] ⁇ 1 ⁇ [4,3- a]pyrazin- 1 -yl)-cyclopentyl ester;
  • the invention provides a compound according to the first through twelfth embodiments wherein T is CR 6 , U is N, X is CR 3 and Y is N and forms a compound of Formula (lb)
  • R ! ,and R 2 are independently hydrogen, deuterium, -N(R a )(R b ), halogen, -OR a , -SR a , - S(0)R a , -S(0) 2 R a , -NO 2 , -C(0)OR a , -CN, -C(0)N(R a )(R b ), -N(R a )C(0)(R b ), -C(0)R a , - C(OH)R a R b , -N(R a )S(0) 2 -R b , -S(0) 2 N(R a )(R b ), -CF 3 , -OCF 3 , optionally substituted (Ci-C 6 )alkyl, optionally substituted (C 2 -C 6 )alkenyl, optionally substituted (C 2 -C 6 )alkynyl, optionally substituted (C 3
  • R a and R b are each independently hydrogen, deuterium, CN, an optionally substituted (Ci- Cio)alkyl, an optionally substituted (C 2 -Cio)alkenyl, an optionally substituted (C 2 -Cio)alkynyl, an optionally substituted (Ci-Ci 0 )alkyl-O-(Ci-Ci 0 )alkyl, an optionally substituted (C 3 -Ci 0 )cycloalkyl, an optionally substituted (Ce-Cio)aryl, an optionally substituted (Ci-Cio)heteroaryl, an optionally substituted (Ci-Cio)heterocyclyl, an optionally substituted -(Ci-C 6 )alkylene-(C3-Cio)cycloalkyl, an optionally substituted -(Ci-C 6 )alkylene-(C3-Cio)cycloalkyl, an optional
  • a compound of Formula (I) or Formula (II) can be combined with corticosteroids, for example, budenoside and dexamethasone; sulfasalazine, 5 -aminosalicylic acid; olsalazine; and agents which interfere with synthesis or action of proinflammatory cytokines such as IL-1, for example, IL- ⁇ converting enzyme inhibitors and IL-lra; T cell signaling inhibitors, for example, tyrosine kinase inhibitors; 6-mercaptopurine; IL-11 ; mesalamine; prednisone; azathioprine; mercaptopurine; infliximab; methylprednisolone sodium succinate; diphenoxylate/atrop sulfate; loperamide hydrochloride; methotrexate; omeprazole; folate; ciprofloxacin/dextrose-water; hydrocodone bitartrate/apap; t
  • Non-limiting examples of therapeutic agents for HCV with which a compound of Formula (I) or Formula (II) can be combined include the following: Interferon-alpha-2a, Interferon-alpha-2 , Interferon-alpha conl, Interferon-alpha-nl, pegylated interferon-alpha-2a, pegylated interferon-alpha-2 , ribavirin, peginterferon alfa-2b + ribavirin, ursodeoxycholic acid, glycyrrhizic acid, thymalfasin, Maxamine, VX-497 and any compounds that are used to treat HCV through intervention with the following targets: HCV polymerase, HCV protease, HCV helicase, and HCV IRES (internal ribosome entry site).
  • bridged (C2-C10) heterocyclyl means bicyclic or polycyclic aza- bridged hydrocarbon groups and may include azanorbornyl, quinuclidinyl, isoquinuclidinyl, tropanyl, azabicyclo[3.2.1]octanyl, azabicyclo[2.2.1]heptanyl, 2-azabicyclo[3.2.1]octanyl, azabicyclo[3.2.1]octanyl, azabicyclo[3.2.2]nonanyl, azabicyclo[3.3.0]nonanyl, and azabicyclo [3.3.1]nonanyl.
  • heterocyclic rings azepinyl, azetidinyl, indolinyl, isoindolinyl, morpholinyl, piperazinyl, piperidinyl, pyrrolidinyl, quinucludinyl, thiomorpholinyl, tetrahydropyranyl, tetrahydrofuranyl, tetrahydroindolyl, thiomorpholinyl and tropanyl.
  • heteroaryl or “heteroarylene” as used herein, include aromatic ring systems, including, but not limited to, monocyclic, bicyclic and tricyclic rings, and have 5 to 12 atoms including at least one heteroatom, such as nitrogen, oxygen, or sulfur.
  • the compounds can be formulated for parenteral administration by injection, e.g. bolus injection or continuous infusion.
  • Formulations for injection may be presented in unit dosage form, e.g. in ampoules or in multi-dose containers, with an added preservative.
  • the compositions may take such forms as suspensions, solutions or emulsions in oily or aqueous vehicles, and may contain formulatory agents such as suspending, stabilizing and/or dispersing agents.
  • the compounds may also be formulated in rectal compositions such as suppositories or retention enemas, e.g., containing conventional suppository bases such as cocoa butter or other glycerides.
  • capsules 10 parts by weight of active compound and 240 parts by weight of lactose can be de-aggregated and blended. The mixture can be filled into hard gelatin capsules, each capsule containing a unit dose or part of a unit dose of active compound.
  • the active compound, the lactose and some of the starch can be de-aggregated, blended and the resulting mixture can be granulated with a solution of the polyvinylpyrrolidone in ethanol.
  • the dry granulate can be blended with the magnesium stearate and the rest of the starch.
  • the mixture is then compressed in a tabletting machine to give tablets each containing a unit dose or a part of a unit dose of active compound.

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Priority Applications (40)

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SI201031517T SI2506716T1 (sl) 2009-12-01 2010-12-01 Nove triciklične spojine
RU2012127306A RU2570416C9 (ru) 2009-12-01 2010-12-01 Имидазопирролопиразиновые производные, полезные для лечения заболеваний, вызванных аномальной активностью протеинкиназ Jak1, Jak3 или Syk
RS20170760A RS56317B1 (sr) 2009-12-01 2010-12-01 Nova triciklična jedinjenja
MX2012006311A MX346959B (es) 2009-12-01 2010-12-01 Nuevos compuestos triciclicos.
SG2012040465A SG181472A1 (en) 2009-12-01 2010-12-01 Novel tricyclic compounds
KR1020187025442A KR20180101626A (ko) 2009-12-01 2010-12-01 신규한 트리사이클릭 화합물
CR20170159A CR20170159A (es) 2009-12-01 2010-12-01 Nuevos compuestos tricíclicos
NZ600161A NZ600161A (en) 2009-12-01 2010-12-01 Novel tricyclic compounds
LTEP10835061.2T LT2506716T (lt) 2009-12-01 2010-12-01 Nauji tricikliniai junginiai
EP21173353.0A EP3950692A1 (en) 2009-12-01 2010-12-01 Novel tricyclic compounds
ES10835061.2T ES2637588T3 (es) 2009-12-01 2010-12-01 Nuevos compuestos tricíclicos
DK10835061.2T DK2506716T3 (en) 2009-12-01 2010-12-01 HIS UNKNOWN TRICYCLIC RELATIONS
PL10835061T PL2506716T3 (pl) 2009-12-01 2010-12-01 Nowe związki tricykliczne
EP10835061.2A EP2506716B1 (en) 2009-12-01 2010-12-01 Novel tricyclic compounds
JP2012542161A JP5607174B2 (ja) 2009-12-01 2010-12-01 新規な三環式化合物
CN201080062920.6A CN102711476B (zh) 2009-12-01 2010-12-01 新的三环化合物
UAA201207925A UA111466C2 (uk) 2009-12-01 2010-12-01 Трициклічні сполуки
HRP20171175TT HRP20171175T1 (hr) 2009-12-01 2010-12-01 Novi triciklički spojevi
PH1/2012/501076A PH12012501076B1 (en) 2009-12-01 2010-12-01 Novel tricyclic compounds
MEP-2017-167A ME02800B (me) 2009-12-01 2010-12-01 Nova triciklična jedinjenja
BR112012013349-7A BR112012013349B1 (pt) 2009-12-01 2010-12-01 compostos tricíclicos
AU2010326108A AU2010326108C1 (en) 2009-12-01 2010-12-01 Novel tricyclic compounds
KR1020127017105A KR101785257B1 (ko) 2009-12-01 2010-12-01 신규한 트리사이클릭 화합물
CA2781891A CA2781891C (en) 2009-12-01 2010-12-01 Novel tricyclic compounds as protein kinase inhibitors
KR1020177027803A KR20170118230A (ko) 2009-12-01 2010-12-01 신규한 트리사이클릭 화합물
IL220054A IL220054A (en) 2009-12-01 2012-05-29 Tricyclic compounds
ZA2012/03999A ZA201203999B (en) 2009-12-01 2012-05-31 Novel tricyclic compounds
AU2016201825A AU2016201825B2 (en) 2009-12-01 2016-03-23 Novel tricyclic compounds
PH12016501009A PH12016501009A1 (en) 2009-12-01 2016-05-27 Novel tricyclic compounds
IL248466A IL248466A (en) 2009-12-01 2016-10-25 Tricyclic compounds for drug preparation
IL253516A IL253516B (en) 2009-12-01 2017-07-16 tricyclic compounds
CY20171100817T CY1119175T1 (el) 2009-12-01 2017-07-31 Καινοτομες τρικυκλικες ενωσεις
AU2018201663A AU2018201663B2 (en) 2009-12-01 2018-03-07 Novel tricyclic compounds
IL261778A IL261778A (en) 2009-12-01 2018-09-13 Novel tricyclic compounds
AU2020201390A AU2020201390A1 (en) 2009-12-01 2020-02-26 Novel tricyclic compounds
LU00149C LUC00149I2 (https=) 2009-12-01 2020-03-09
NO2020006C NO2020006I1 (no) 2009-12-01 2020-03-11 upadacitinib or a pharmaceutically acceptable salt thereof
CY2020007C CY2020007I2 (el) 2009-12-01 2020-03-16 Καινοτομες τρικυκλικες ενωσεις
LTPA2020505C LTC2506716I2 (lt) 2009-12-01 2020-03-17 Nauji tricikliniai junginiai
NL301035C NL301035I2 (nl) 2009-12-01 2020-03-17 upadacitinib of een farmaceutisch aanvaardbaar zout daarvan

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Cited By (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102516146A (zh) * 2011-11-24 2012-06-27 爱斯特（成都）生物制药有限公司 5位为氮的四元氮杂螺环衍生物及其制备方法和用途
WO2012127506A1 (en) 2011-03-22 2012-09-27 Advinus Therapeutics Limited Substituted fused tricyclic compounds, compositions and medicinal applications thereof
EP2420502A4 (en) * 2009-04-14 2012-12-19 Astellas Pharma Inc CONDENSED PYRROLOPYRIDINE DERIVATIVE
WO2013007765A1 (en) * 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Fused tricyclic compounds for use as inhibitors of janus kinases
WO2013024895A1 (en) 2011-08-12 2013-02-21 Nissan Chemical Industries, Ltd. Tricyclic heterocyclic compounds and jak inhibitors
WO2013043826A1 (en) 2011-09-21 2013-03-28 Abbvie Inc. Tricyclic compounds useful as protein kinase inhibitors
US8461328B2 (en) 2010-01-12 2013-06-11 Genentech, Inc. Tricyclic heterocyclic compounds, compositions and methods of use thereof
WO2014123167A1 (ja) 2013-02-08 2014-08-14 日産化学工業株式会社 ３環性ピロロピリジン化合物及びｊａｋ阻害剤
WO2014128591A1 (en) 2013-02-22 2014-08-28 Pfizer Inc. Pyrrolo [2, 3 -d]pyrimidine derivatives as inhibitors of janus- related kinases (jak)
JP2015529242A (ja) * 2012-09-21 2015-10-05 アドヴィヌス セラピューティクス リミテッドＡｄｖｉｎｕｓ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｌｉｍｉｔｅｄ 置換された縮合三環式化合物、組成物およびその医薬用途
WO2016024185A1 (en) 2014-08-12 2016-02-18 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase
US9492444B2 (en) 2013-12-17 2016-11-15 Pharmaceutical Manufacturing Research Services, Inc. Extruded extended release abuse deterrent pill
US9499535B2 (en) 2011-04-21 2016-11-22 Origenis Gmbh Kinase inhibitors
KR20170003521A (ko) 2014-05-14 2017-01-09 닛산 가가쿠 고교 가부시키 가이샤 3 고리성 화합물 및 jak 저해제
WO2017066775A1 (en) * 2015-10-16 2017-04-20 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
US9707184B2 (en) 2014-07-17 2017-07-18 Pharmaceutical Manufacturing Research Services, Inc. Immediate release abuse deterrent liquid fill dosage form
WO2017162604A1 (en) 2016-03-21 2017-09-28 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for diagnosis and treatment of solar lentigo
US10000482B2 (en) 2012-10-19 2018-06-19 Origenis Gmbh Kinase inhibitors
WO2018167283A1 (en) 2017-03-17 2018-09-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling
US10172797B2 (en) 2013-12-17 2019-01-08 Pharmaceutical Manufacturing Research Services, Inc. Extruded extended release abuse deterrent pill
US10195153B2 (en) 2013-08-12 2019-02-05 Pharmaceutical Manufacturing Research Services, Inc. Extruded immediate release abuse deterrent pill
US10294226B2 (en) 2016-12-16 2019-05-21 Janssen Pharmaceutica Nv Small molecule inhibitors of the JAK family of kinases
US10508113B2 (en) 2018-03-12 2019-12-17 Abbvie Inc. Inhibitors of tyrosine kinase 2 mediated signaling
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
WO2020043033A3 (zh) * 2018-08-31 2020-04-16 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
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
WO2020115213A1 (en) 2018-12-07 2020-06-11 Lek Pharmaceuticals D.D. Solvate of a selective jak1 inhibitor
WO2020115212A1 (en) 2018-12-05 2020-06-11 Lek Pharmaceuticals D.D. Crystalline phosphate salt of selective jak1 inhibitor upadacitinib
US10959958B2 (en) 2014-10-20 2021-03-30 Pharmaceutical Manufacturing Research Services, Inc. Extended release abuse deterrent liquid fill dosage form
US10981911B2 (en) 2016-12-16 2021-04-20 Janssen Pharmaceutica Nv Imidazopyrrolopyridine as inhibitors of the JAK family of kinases
WO2021123288A1 (en) 2019-12-19 2021-06-24 Crystal Pharma, S.A.U. Process and intermediates for the preparation of upadacitinib
KR20210090173A (ko) * 2018-11-01 2021-07-19 링크 파마슈티컬스 컴퍼니 리미티드 트리사이클릭 야누스 키나제 1 억제제 및 이의 조성물 및 방법
US11066406B2 (en) 2018-06-15 2021-07-20 Janssen Pharmaceutica Nv Small molecule inhibitors of the JAK family of kinases
EP3129373B1 (en) * 2014-04-11 2021-09-01 Taipei Medical University Histone deacetylase inhibitors
CN113603693A (zh) * 2021-07-13 2021-11-05 陕西丽彩药业有限公司 一种2-溴-5-对甲苯磺酰基-5H-吡咯并[2,3-b]吡嗪的制备方法
WO2022054005A1 (en) * 2020-09-14 2022-03-17 Galderma Holding SA Novel jak inhibitor compounds, method for synthesizing same and use 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
US11406640B2 (en) 2019-03-05 2022-08-09 Incyte Corporation JAK1 pathway inhibitors for the treatment of chronic lung allograft dysfunction
WO2022217257A1 (en) * 2021-04-07 2022-10-13 Abbvie Inc. Cocrystals of upadacitinib
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
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
US11564922B2 (en) 2017-03-09 2023-01-31 Abbvie Inc. Methods of treating crohn's disease and ulcerative colitis
US11572365B2 (en) 2020-07-08 2023-02-07 Crystal Pharmaceutical (Suzhou) Co., Ltd. Crystal form of upadacitinib, preparation method therefor, and use thereof
US11607411B2 (en) 2017-03-09 2023-03-21 Abbvie Inc. Methods of treating Crohn's disease and ulcerative colitis
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
US11718622B2 (en) 2020-03-16 2023-08-08 Exelixis Inc. Heterocyclic adenosine receptor antagonists
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
AU2020320992B2 (en) * 2019-07-26 2024-02-29 Guangzhou Yufan Nantu Biotechnologies Co., Ltd IRAK4 kinase inhibitor and preparation method therefor
WO2025000671A1 (zh) * 2023-06-30 2025-01-02 凌科药业(杭州)有限公司 一种磺酰胺类化合物及其应用
WO2025102268A1 (en) * 2023-11-15 2025-05-22 Lynk Pharmaceuticals Co. Ltd. Solid state forms, pharmaceutical compositions, preparation methods and use 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
US20250250277A1 (en) * 2015-10-16 2025-08-07 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
US12390451B2 (en) 2021-03-11 2025-08-19 Janssen Pharmaceutica Nv Small molecule inhibitor of the JAK family of kinases

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104592231A (zh) * 2008-06-10 2015-05-06 Abbvie公司 新的三环化合物
RU2711869C3 (ru) * 2009-12-01 2022-02-02 Эббви Инк. Имидазопирролопиразиновые производные, полезные для лечения заболеваний, вызванных аномальной активностью протеинкиназ Jak1, Jak3 или Syk
PH12012501000A1 (en) * 2009-12-01 2013-02-11 Abbvie Inc Novel tricyclic compounds
RS58514B1 (sr) 2012-06-13 2019-04-30 Incyte Holdings Corp Supstituisana triciklična jedinjenja kao inhibitori fgfr
CA3012383C (en) 2013-02-28 2021-03-02 Teewinot Technologies Limited Biosynthesis of cannabinoids
AU2014339897A1 (en) * 2013-10-24 2016-04-21 Abbvie Inc. JAK1 selective inhibitor and uses thereof
CN109593651A (zh) 2014-08-25 2019-04-09 蒂威诺特科技有限公司 用于大麻素化合物的同时生产的设备和方法
HK1254892A1 (zh) 2016-01-14 2019-08-02 韩德株式会社 拮抗a3腺苷受体的化合物、其制备方法、及其医学用途
US10364245B2 (en) 2017-06-07 2019-07-30 Chiesi Farmaceutici S.P.A. Kinase inhibitors
CN109535164B (zh) * 2017-09-21 2022-01-18 上海华汇拓医药科技有限公司 Jak激酶抑制剂及其制备方法和在医药领域的应用
AU2019262579B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Salts of an FGFR inhibitor
HRP20241288T1 (hr) 2018-05-04 2024-12-06 Incyte Corporation Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju
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
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
CN109761885B (zh) * 2019-02-21 2020-06-26 北京悦康科创医药科技股份有限公司 一种阿加曲班异构体杂质的拆分方法
US20210380596A1 (en) * 2019-03-01 2021-12-09 Crystal Pharmaceutical (Suzhou) Co., Ltd. Upadacitinib crystal form and preparation method therefor and use thereof
EP3939979A4 (en) 2019-03-14 2022-04-06 Shanghai Synergy Pharmaceutical Sciences Co., Ltd Jak kinase inhibitor, preparation method for same, and applications thereof in field of medicine
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
CN110938048B (zh) * 2019-12-02 2023-03-28 四川大学 路易酸催化的插入反应高效合成二氢呋喃衍生物
JP7832891B2 (ja) 2019-12-04 2026-03-18 インサイト・コーポレイション Ｆｇｆｒ阻害剤の誘導体
CN111007184B (zh) * 2019-12-30 2023-05-16 天津天士力圣特制药有限公司 一种4-甲基哌嗪-1-甲酰氯盐酸盐含量的检测方法
WO2021176473A1 (en) 2020-03-05 2021-09-10 Mylan Laboratories Limited A process for the preparation of upadacitinib and its intermediates
US20210371389A1 (en) * 2020-04-24 2021-12-02 Kansas Soybean Commission One-step synthesis of soybean polyols
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
WO2022044037A1 (en) 2020-08-24 2022-03-03 Mylan Laboratories Limited An improved process for the preparation of upadacitinib intermediate
BR112023004550A2 (pt) * 2020-10-08 2023-05-02 Unichem Lab Ltd Compostos tricíclicos substituídos
CN112578034B (zh) * 2020-11-04 2022-02-11 广东众生睿创生物科技有限公司 一种手性胺小分子及其盐的质量控制方法
CN114790208B (zh) * 2021-01-26 2024-06-07 珠海宇繁生物科技有限责任公司 一种irak4激酶抑制剂及其制备方法
CN113200967B (zh) * 2021-05-07 2022-05-24 中国人民解放军陆军军医大学 吲哚苯醌类化合物、其制备方法及其应用
AU2022271927B2 (en) * 2021-05-13 2025-07-10 Innovstone Therapeutics Limited Compound having anti-tumor activity and use thereof
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
US12487299B2 (en) 2022-06-20 2025-12-02 Shanghai United Imaging Healthcare Co., Ltd. Magnetic resonance imaging devices and radiation therapy systems including the magnetic resonance imaging devices
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

Citations (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6090382A (en) 1996-02-09 2000-07-18 Basf Aktiengesellschaft Human antibodies that bind human TNFα
WO2005110410A2 (en) * 2004-05-14 2005-11-24 Abbott Laboratories Kinase inhibitors as therapeutic agents
WO2006058120A1 (en) 2004-11-22 2006-06-01 Vertex Pharmaceuticals Incorporated Bicyclic inhibitors or rho kinase
WO2007007919A2 (en) 2005-07-14 2007-01-18 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
WO2007014011A2 (en) 2005-07-21 2007-02-01 Ardea Biosciences, Inc. N-(arylamino)-sulfonamide inhibitors of mek
WO2007077949A1 (en) 2005-12-28 2007-07-12 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
US20070293509A1 (en) 2006-06-19 2007-12-20 Paul Hebeisen Pyrazinecarboxamide derivatives as CB1 antagonists
WO2008004117A1 (en) 2006-07-06 2008-01-10 Pfizer Products Inc. Selective azole pde10a inhibitor compounds
WO2008063287A2 (en) * 2006-10-06 2008-05-29 Abbott Laboratories Novel imidazothiazoles and imidazoxazoles
US20080248537A1 (en) 2007-04-04 2008-10-09 Steven Paul Hanlon Biocatalytic asymmetric reduction in preparation of (s)-n-[5-(1,2-dihydroxy-ethyl)-pyrazinyl]-2,2-dimethyl-propionamide
WO2009005675A1 (en) * 2007-06-28 2009-01-08 Abbott Laboratories Novel triazolopyridazines
WO2009018238A1 (en) 2007-07-30 2009-02-05 Ardea Biosciences, Inc. Combinations of mek inhibitors and raf kinase inhibitors and uses thereof
EP2123651A1 (en) 2007-01-12 2009-11-25 Astellas Pharma Inc. Condensed pyridine compound
WO2009152133A1 (en) 2008-06-10 2009-12-17 Abbott Laboratories Novel tricyclic compounds

Family Cites Families (74)

* 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
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
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
DK0559751T3 (da) 1990-11-26 1997-10-06 Robert R Recker Behandling af osteoporosis under anvendelse af væksthormonfrigivende faktor (GRF) i kombination med parathyreoideahormon (PTH)
EP1857553A1 (en) 1991-03-18 2007-11-21 New York University Monoclonal and chimeric antibodies specific for human tumor necrosis factor
KR100207360B1 (ko) 1991-06-14 1999-07-15 돈 더블유. 슈미츠 이미다조[1,5,-a]퀸옥살린
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
DK0752248T3 (da) 1992-11-13 2000-11-13 Idec Pharma Corp Terapeutisk anvendelse af kimæriske og radioaktivt mærkede antistoffer mod humant B-lymfocytbegrænset differentieringsantig
US5939419A (en) 1993-02-26 1999-08-17 Schering-Plough Corporation 2-benzyl-polycyclic guanine derivatives 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
CA2322311C (en) * 1998-03-04 2009-10-13 Bristol-Myers Squibb Company Heterocyclo-substituted imidazopyrazine protein tyrosine kinase inhibitors
US6448253B1 (en) 1998-09-16 2002-09-10 King Pharmaceuticals Research And Development, Inc. Adenosine A3 receptor modulators
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
JP4100865B2 (ja) * 1999-12-13 2008-06-11 エーザイ・アール・アンド・ディー・マネジメント株式会社 三環式縮合異項環化合物、その製造法およびその医薬
PY0119496A (es) 2000-08-07 2003-11-03 Neurogen Corp Compuestos heterociclicos como ligandos de receptores 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
US20050176796A1 (en) 2002-02-19 2005-08-11 D'alessio Roberto Tricyclic pyrazole derivatives, process for their preparation and their use as antitumor agents
TW200400034A (en) 2002-05-20 2004-01-01 Bristol Myers Squibb Co Pyrazolo-pyrimidine aniline compounds useful as kinase inhibitors
DE60333762D1 (de) * 2002-08-23 2010-09-23 Novartis Vaccines & Diagnostic Pyrrolverbindungen als glykogen synthase kinase 3 inhibitoren
MXPA05007503A (es) * 2003-01-17 2005-09-21 Warner Lambert Co Heterociclicos 2-aminopiridina sustituidos como inhibidores de proliferacion celular.
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
TW200524864A (en) * 2003-11-10 2005-08-01 Wyeth Corp Sulfonyltetrahydro-3H-benzo(E)indole-8-amine compounds as 5-hydroxytryptamine-6 ligands
PE20060526A1 (es) * 2004-06-15 2006-07-13 Schering Corp Compuestos triciclicos como antagonistas de mglur1
DE502005008916D1 (de) 2004-07-23 2010-03-11 Medicines Co Leipzig Gmbh Substituierte pyridoä3',2':4,5üthienoä3,2-düpyrimidine und pyridoä3',2':4,5üfuroä3,2-dü-pyrimidine zur verwendung als inhibitoren der pda-4 und/oder tnf-alpha freisetzung
WO2006074984A1 (en) * 2005-01-14 2006-07-20 Janssen Pharmaceutica N.V. Pyrazolopyrimidines as cell cycle kinase inhibitors
EP1846408B1 (en) * 2005-01-14 2013-03-20 Janssen Pharmaceutica NV 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
EP1863813A2 (en) * 2005-04-01 2007-12-12 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
CN101223168A (zh) * 2005-07-14 2008-07-16 安斯泰来制药株式会社 Janus激酶3的杂环类抑制剂
US7589101B2 (en) * 2005-08-16 2009-09-15 Irm Llc Compounds and compositions as protein kinase inhibitors
AU2006292119A1 (en) 2005-09-23 2007-03-29 3M Innovative Properties Company Method for 1H-imidazo[4,5-c]pyridines and analogs thereof
JP5052518B2 (ja) * 2005-10-06 2012-10-17 シェーリング コーポレイション プロテインキナーゼインヒビターとしてのピラゾロピリミジン
JP5249772B2 (ja) 2005-11-22 2013-07-31 メルク・シャープ・アンド・ドーム・コーポレーション キナーゼの阻害剤として有用な三環式化合物
ES2545907T3 (es) 2005-12-29 2015-09-16 Abbvie Inc. Inhibidores de proteína quinasa
EP2468748B1 (en) * 2006-02-15 2016-05-25 AbbVie Inc. Pyrazoloquinolones are potent parp inhibitors
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
CA2676665A1 (en) * 2007-01-30 2008-08-07 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
US7723343B2 (en) * 2007-03-30 2010-05-25 King Pharmaceuticals Research And Development, Inc. Adenosine A2A receptor antagonists
PE20091485A1 (es) * 2008-02-06 2009-10-26 Novartis Ag DERIVADOS DE PIRROLO-[2,3-d]-PIRIMIDINA COMO INHIBIDORES DE CINASAS
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
JP5368485B2 (ja) 2008-02-25 2013-12-18 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インヒビター
CA2712507A1 (en) 2008-02-25 2009-09-03 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
US20110201599A1 (en) * 2008-07-03 2011-08-18 Exelixis, Inc. CDK Modulators
CA2758359A1 (en) * 2009-04-14 2010-10-21 Astellas Pharma Inc. Fused pyrrolopyridine derivative
US8361962B2 (en) * 2009-07-27 2013-01-29 Roche Palo Alto Llc Tricyclic inhibitors of JAK
PH12012501000A1 (en) 2009-12-01 2013-02-11 Abbvie Inc Novel tricyclic compounds
RU2711869C3 (ru) 2009-12-01 2022-02-02 Эббви Инк. Имидазопирролопиразиновые производные, полезные для лечения заболеваний, вызванных аномальной активностью протеинкиназ Jak1, Jak3 или Syk
WO2011156698A2 (en) 2010-06-11 2011-12-15 Abbott Laboratories NOVEL PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS
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
AU2014339897A1 (en) 2013-10-24 2016-04-21 Abbvie Inc. JAK1 selective inhibitor and uses thereof
SG10201913990RA (en) 2015-10-16 2020-03-30 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

Patent Citations (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6090382A (en) 1996-02-09 2000-07-18 Basf Aktiengesellschaft Human antibodies that bind human TNFα
WO2005110410A2 (en) * 2004-05-14 2005-11-24 Abbott Laboratories Kinase inhibitors as therapeutic agents
WO2006058120A1 (en) 2004-11-22 2006-06-01 Vertex Pharmaceuticals Incorporated Bicyclic inhibitors or rho kinase
WO2007007919A2 (en) 2005-07-14 2007-01-18 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
WO2007014011A2 (en) 2005-07-21 2007-02-01 Ardea Biosciences, Inc. N-(arylamino)-sulfonamide inhibitors of mek
WO2007077949A1 (en) 2005-12-28 2007-07-12 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
US20070293509A1 (en) 2006-06-19 2007-12-20 Paul Hebeisen Pyrazinecarboxamide derivatives as CB1 antagonists
WO2008004117A1 (en) 2006-07-06 2008-01-10 Pfizer Products Inc. Selective azole pde10a inhibitor compounds
WO2008063287A2 (en) * 2006-10-06 2008-05-29 Abbott Laboratories Novel imidazothiazoles and imidazoxazoles
EP2123651A1 (en) 2007-01-12 2009-11-25 Astellas Pharma Inc. Condensed pyridine compound
US20080248537A1 (en) 2007-04-04 2008-10-09 Steven Paul Hanlon Biocatalytic asymmetric reduction in preparation of (s)-n-[5-(1,2-dihydroxy-ethyl)-pyrazinyl]-2,2-dimethyl-propionamide
WO2009005675A1 (en) * 2007-06-28 2009-01-08 Abbott Laboratories Novel triazolopyridazines
WO2009018238A1 (en) 2007-07-30 2009-02-05 Ardea Biosciences, Inc. Combinations of mek inhibitors and raf kinase inhibitors and uses thereof
WO2009152133A1 (en) 2008-06-10 2009-12-17 Abbott Laboratories Novel tricyclic compounds

Non-Patent Citations (59)

* Cited by examiner, † Cited by third party
Title
"Remington's Pharmaceutical Sciences", MACK PUBLISHING CO.
ADVANCED SYNTHESIS & CATALYSIS, vol. 346, 2004, pages 1599 - 1626
BAIER, G. ET AL., J. BIOL. CHEM., vol. 268, 1993, pages 4997
BAIER-BITTERLICH, G. ET AL., MOL. CELL. BIOL., vol. 16, 1996, pages 842
BEESLEY, T. E.; SCOTT, R. P. W., CHIRAL CHROMATOGRAPHY, 1999
BERG-BROWN, N.N. ET AL., J. EXP. MED., vol. 199, 2004, pages 743
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 17, no. 12, 2007, pages 3373 - 3377
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 77, no. 12, 2007, pages 3373 - 3377
BIOORGANIC & MEDICINAL CHEMISTRY, vol. 15, 2007, pages 7581
BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS, vol. 17, no. 5, 2007, pages 1233 - 1237
CIARLETTA, A.B. ET AL., 2005 AMERICAN THORACIC SOCIETY INTERNATIONAL CONFERENCE, 2005
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 36, no. 3, 2001, pages 255 - 264
G. SUBRAMANIAN: "Chiral Separation Techniques", 2007
GENERAL PROCEDURE O OR BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS, vol. 14, no. 17, 2004, pages 4453 - 4459
GENERAL PROCEDURE XX OR ORGANIC LETTERS, vol. 10, no. 18, 2008, pages 4109 - 4112
GORDON, A. J.; FORD, R. A., THE CHEMIST'S COMPANION, 1972
GREENE, T.W.; WUTS, P.G.M.: "Protective Groups in Organic Synthesis", 1999, WILEY-INTERSCIENCE
GUSCHIN D ET AL., EMBO J., vol. 14, no. 7, 3 April 1995 (1995-04-03), pages 1421 - 9
HARWOOD, L. M.; MOODY, C. J.; PERCY, J. M: "Experimental Organic Chemistry: Standard and Microscale", 1999
INT. IMMUNITY, vol. 12, 2000, pages 1499
J. ORG. CHEM., vol. 69, 2004, pages 1629
JOURNAL OF IMMUNOLOGY, vol. 178, 2007, pages 2623
JOURNAL OF MEDICINAL CHEMISTRY, vol. 33, no. 9, 1990, pages 2326 - 2334
JOURNAL OF MEDICINAL CHEMISTRY, vol. 33, no. 9, 1990, pages 2326 - 34
JOURNAL OF MEDICINAL CHEMISTRY, vol. 46, no. 4, 2003, pages 461 - 473
JOURNAL OF MEDICINAL CHEMISTRY, vol. 48, no. 14, 2005, pages 4535 - 4546
JOURNAL OF MEDICINAL CHEMISTRY, vol. 52, no. 24, 2009, pages 7946 - 7949
JOURNAL OF ORGANIC CHEMISTRY, vol. 58, 1993, pages 4745
KIMATA, M. ET AL., BIOCHEM. BIOPHYS. RES. COMMUN., vol. 257, no. 3, 1999, pages 895
LANDGREBE, J. A.: "Theory and Practice in the Organic Laboratory", 1993
LAROCK, R.C.: "Comprehensive Organic Transformations: A Guide to Functional Group Preparations", 1999, WILEY-VCH
LAWLOR K.E. ET AL., PROC NATL ACAD SCI U.S.A., vol. 101, no. 31, 2004, pages 11398 - 403
LI, J.J.: "Name Reactions. A Collection of Detailed Reaction Mechanisms", 2003, SPRINGER
LIN, X. ET AL., MOL. CELL. BIOL., vol. 20, 2000, pages 2933
LIU, Y. ET AL., J. LEUKOC. BIOL., vol. 69, 2001, pages 831
MALEK TR ET AL., IMMUNITY, vol. 17, no. 2, 2002, pages 167 - 78
MARSLAND, B.J. ET AL., J. EXP. MED., vol. 200, 2004, pages 181
MATTILA, P. ET AL., LIFE SCI., vol. 55, 1994, pages 1253
MISCHAK, H. ET AL., FEBS LETT., vol. 326, 1993, pages 51
MONKS, C. ET AL., NATURE, vol. 385, 1997, pages 83
N. COUDRONNIERE ET AL., PROC. NAT. ACAD. SCI. U.S.A., vol. 97, 2000, pages 3394
NISHIMOTO N. ET AL., ANN RHEUM DIS., vol. 66, no. 9, 2007, pages 1162 - 7
ORG. LETT., vol. 11, 2009, pages 3566
PALLEROS, D. R., EXPERIMENTAL ORGANIC CHEMISTRY, 2000
PARGANAS E, CELL, vol. 93, no. 3, 1 May 1998 (1998-05-01), pages 385 - 95
RODIG S.J. ET AL., CELL, vol. 93, no. 3, 1 May 1998 (1998-05-01), pages 373 - 83
SHASHI NAYANA ET AL.: "CoMFA and docking studies on triazolopyridine oxazole derivatives as p38 MAP kinase inhibitors", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 43, 2008, pages 1261 - 1269, XP022694994, DOI: doi:10.1016/j.ejmech.2007.07.010 *
SKOOG, D. A.; LEARY, J. J.: "Principles of Instrumental Analysis", 1992
STICHLMAIR, J. G.; FAIR, J. R., DISTILLATION; PRINCIPLES AND PRACTICES, 1998
STILL, W. C.; KAHN; M. MITRA, A, J. ORG. CHEM., vol. 43, 1978, pages 2923
SUN, Z. ET AL., NATURE, vol. 404, 2000, pages 402
TET. LETT., vol. 24, no. 48, 1983, pages 5363
TETRAHEDRON LETTERS, 1992, pages 309 - 312
TETRAHEDRON LETTERS, vol. 40, no. 47, 1999, pages 8193 - 8195
TETRAHEDRON LETTERS, vol. 47, no. 34, 2006, pages 6113 - 6115
WILLERFORD DM ET AL., IMMUNITY, vol. 3, no. 4, 1995, pages 521 - 30
Y. KAZAKEVICH; R. LOBRUTTO, HPLC FOR PHARMACEUTICAL SCIENTISTS, 2007
YAMANOUCHI J ET AL., NAT GENET., vol. 39, no. 3, 2007, pages 329 - 37
YAN, B., ANALYSIS AND PURIFICATION METHODS IN COMBINATORIAL CHEMISTRY, 2003

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US8461328B2 (en) 2010-01-12 2013-06-11 Genentech, Inc. Tricyclic heterocyclic compounds, compositions and methods of use thereof
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CN105001226B (zh) * 2011-08-12 2017-09-08 日产化学工业株式会社 三环杂环化合物和jak抑制剂
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US9216999B2 (en) 2011-08-12 2015-12-22 Nissan Chemical Industries, Ltd. Substituted pyrrolo[2,3-h][1,6]naphthyridines and compositions thereof as JAK inhibitors
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WO2013024895A1 (en) 2011-08-12 2013-02-21 Nissan Chemical Industries, Ltd. Tricyclic heterocyclic compounds and jak inhibitors
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US10000482B2 (en) 2012-10-19 2018-06-19 Origenis Gmbh Kinase inhibitors
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US9475813B2 (en) 2013-02-08 2016-10-25 Nissan Chemical Industries, Ltd. Tricyclic pyrrolopyridine compound, and JAK inhibitor
WO2014123167A1 (ja) 2013-02-08 2014-08-14 日産化学工業株式会社 ３環性ピロロピリジン化合物及びｊａｋ阻害剤
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WO2014128591A1 (en) 2013-02-22 2014-08-28 Pfizer Inc. Pyrrolo [2, 3 -d]pyrimidine derivatives as inhibitors of janus- related kinases (jak)
US9549929B2 (en) 2013-02-22 2017-01-24 Pfizer Inc. Pyrrolo[2,3-D]pyrimidine derivatives
US9035074B2 (en) 2013-02-22 2015-05-19 Pfizer Inc. Pyrrolo[2,3-D]pyrimidine derivatives
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US10195153B2 (en) 2013-08-12 2019-02-05 Pharmaceutical Manufacturing Research Services, Inc. Extruded immediate release abuse deterrent pill
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US9890165B2 (en) 2014-05-14 2018-02-13 Nissan Chemical Industries, Ltd. Tricyclic compound and JAK inhibitor
KR20170003521A (ko) 2014-05-14 2017-01-09 닛산 가가쿠 고교 가부시키 가이샤 3 고리성 화합물 및 jak 저해제
US10385052B2 (en) 2014-05-14 2019-08-20 Nissan Chemical Corporation Tricyclic compound and JAK inhibitor
US9707184B2 (en) 2014-07-17 2017-07-18 Pharmaceutical Manufacturing Research Services, Inc. Immediate release abuse deterrent liquid fill dosage form
WO2016024185A1 (en) 2014-08-12 2016-02-18 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase
US10959958B2 (en) 2014-10-20 2021-03-30 Pharmaceutical Manufacturing Research Services, Inc. Extended release abuse deterrent liquid fill dosage form
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
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
US10202394B2 (en) 2015-10-16 2019-02-12 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
US10202393B2 (en) 2015-10-16 2019-02-12 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-α]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11993605B2 (en) 2015-10-16 2024-05-28 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
US10344036B2 (en) 2015-10-16 2019-07-09 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
US11795175B2 (en) 2015-10-16 2023-10-24 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
US11993606B2 (en) 2015-10-16 2024-05-28 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
US10017517B2 (en) 2015-10-16 2018-07-10 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-α]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluorethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11787815B1 (en) 2015-10-16 2023-10-17 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
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US10519164B2 (en) 2015-10-16 2019-12-31 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
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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
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US11767326B2 (en) 2015-10-16 2023-09-26 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
AU2023251492B2 (en) * 2015-10-16 2025-04-03 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
US11186584B2 (en) 2015-10-16 2021-11-30 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
US11198697B1 (en) 2015-10-16 2021-12-14 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
US11718627B2 (en) 2015-10-16 2023-08-08 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
US12077545B2 (en) 2015-10-16 2024-09-03 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
US12134621B2 (en) 2015-10-16 2024-11-05 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
US12116373B2 (en) 2015-10-16 2024-10-15 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
US12110298B2 (en) 2015-10-16 2024-10-08 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
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
US11535625B2 (en) 2015-10-16 2022-12-27 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11535626B2 (en) 2015-10-16 2022-12-27 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
US11535624B2 (en) 2015-10-16 2022-12-27 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-α]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
EP4219503A1 (en) 2015-10-16 2023-08-02 AbbVie Inc. Crytalline 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
US12110297B2 (en) 2015-10-16 2024-10-08 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
US12091415B2 (en) 2015-10-16 2024-09-17 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
US11661425B2 (en) 2015-10-16 2023-05-30 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
US11680069B2 (en) 2015-10-16 2023-06-20 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
US12103933B2 (en) 2015-10-16 2024-10-01 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
WO2017162604A1 (en) 2016-03-21 2017-09-28 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for diagnosis and treatment of solar lentigo
US11059823B2 (en) 2016-12-16 2021-07-13 Janssen Pharmaceutica Nv Small molecule inhibitors of the JAK family of kinases
US12202831B2 (en) 2016-12-16 2025-01-21 Janssen Pharmaceutica Nv Small molecule inhibitors of the JAK family of kinases
KR102352462B1 (ko) 2016-12-16 2022-01-17 얀센 파마슈티카 엔.브이. Jak 패밀리의 키나제의 소분자 억제제
US10981911B2 (en) 2016-12-16 2021-04-20 Janssen Pharmaceutica Nv Imidazopyrrolopyridine as inhibitors of the JAK family of kinases
US10487083B2 (en) 2016-12-16 2019-11-26 Janssen Pharmaceutica Nv Small molecule inhibitors of the JAK family of kinases
US10364246B2 (en) 2016-12-16 2019-07-30 Janssen Pharmaceutica Nv Small molecule inhibitors of the JAK family of kinases
KR20190086779A (ko) * 2016-12-16 2019-07-23 얀센 파마슈티카 엔.브이. Jak 패밀리의 키나제의 소분자 억제제
US11827638B2 (en) 2016-12-16 2023-11-28 Janssen Pharmaceutica Nv Imidazopyrrolopyridine as inhibitors of the JAK family of kinases
US10294226B2 (en) 2016-12-16 2019-05-21 Janssen Pharmaceutica Nv Small molecule inhibitors of the JAK family of kinases
US11564922B2 (en) 2017-03-09 2023-01-31 Abbvie Inc. Methods of treating crohn's disease and ulcerative colitis
US11607411B2 (en) 2017-03-09 2023-03-21 Abbvie Inc. Methods of treating Crohn's disease and ulcerative colitis
WO2018167283A1 (en) 2017-03-17 2018-09-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling
US10508113B2 (en) 2018-03-12 2019-12-17 Abbvie Inc. Inhibitors of tyrosine kinase 2 mediated signaling
US11066406B2 (en) 2018-06-15 2021-07-20 Janssen Pharmaceutica Nv Small molecule inhibitors of the JAK family of kinases
US11787807B2 (en) 2018-06-15 2023-10-17 Janssen Pharmaceutica Nv Small molecule inhibitors of the JAK family of kinases
US11926633B2 (en) 2018-08-31 2024-03-12 Suzhou Pengxu Pharmatech Co., Ltd Synthesis methods for upadacitinib and intermediate thereof
WO2020043033A3 (zh) * 2018-08-31 2020-04-16 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
KR102841141B1 (ko) * 2018-11-01 2025-07-31 링크 파마슈티컬스 컴퍼니 리미티드 트리사이클릭 야누스 키나제 1 억제제 및 이의 조성물 및 방법
EP3856742A4 (en) * 2018-11-01 2022-06-22 Lynk Pharmaceuticals Co. Ltd. TRICYCLIC JANUS KINASE-1 INHIBITORS AND COMPOSITIONS AND METHODS THEREOF
US11851431B2 (en) 2018-11-01 2023-12-26 Lynk Pharmaceuticals Co. Ltd. Tricyclic Janus kinase 1 inhibitors, and compositions and methods thereof
CN113396150B (zh) * 2018-11-01 2024-03-12 凌科药业(杭州)有限公司 三环janus激酶1抑制剂及其组合物和方法
AU2019372677B2 (en) * 2018-11-01 2024-05-30 Lynk Pharmaceuticals Co. Ltd. Tricyclic Janus kinase 1 inhibitors, and compositions and methods thereof
US12024516B2 (en) 2018-11-01 2024-07-02 Lynk Pharmaceuticals Co. Ltd. Tricyclic janus kinase 1 inhibitors, and compositions and methods thereof
EP4520395A3 (en) * 2018-11-01 2025-05-21 Lynk Pharmaceuticals Co. Ltd. Tricyclic janus kinase 1 inhibitors, and compositions and methods thereof
KR20210090173A (ko) * 2018-11-01 2021-07-19 링크 파마슈티컬스 컴퍼니 리미티드 트리사이클릭 야누스 키나제 1 억제제 및 이의 조성물 및 방법
US11858933B2 (en) 2018-11-01 2024-01-02 Lynk Pharmaceuticals Co. Ltd. Tricyclic Janus kinase 1 inhibitors, and compositions and methods thereof
CN113396150A (zh) * 2018-11-01 2021-09-14 凌科药业(杭州)有限公司 三环janus激酶1抑制剂及其组合物和方法
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
WO2020115212A1 (en) 2018-12-05 2020-06-11 Lek Pharmaceuticals D.D. Crystalline phosphate salt of selective jak1 inhibitor upadacitinib
WO2020115213A1 (en) 2018-12-07 2020-06-11 Lek Pharmaceuticals D.D. Solvate of a selective jak1 inhibitor
US11406640B2 (en) 2019-03-05 2022-08-09 Incyte Corporation JAK1 pathway inhibitors for the treatment of chronic lung allograft dysfunction
US11896595B2 (en) 2019-03-05 2024-02-13 Incyte Corporation JAK1 pathway inhibitors for the treatment of chronic lung allograft dysfunction
US12582650B2 (en) 2019-07-26 2026-03-24 Guangzhou Yufan Nantu Biotechnologies Co., Ltd IRAK4 kinase inhibitor and preparation method therefor
AU2020320992B2 (en) * 2019-07-26 2024-02-29 Guangzhou Yufan Nantu Biotechnologies Co., Ltd IRAK4 kinase inhibitor and preparation method therefor
US12552746B2 (en) 2019-12-19 2026-02-17 Curia Spain, S.A.U. Process and intermediates for the preparation of upadacitinib
WO2021123288A1 (en) 2019-12-19 2021-06-24 Crystal Pharma, S.A.U. Process and intermediates for the preparation of upadacitinib
US12264161B2 (en) 2020-03-16 2025-04-01 Exelixis, Inc. Heterocyclic adenosine receptor antagonists
US11718622B2 (en) 2020-03-16 2023-08-08 Exelixis Inc. Heterocyclic adenosine receptor antagonists
US11572365B2 (en) 2020-07-08 2023-02-07 Crystal Pharmaceutical (Suzhou) Co., Ltd. Crystal form of upadacitinib, preparation method therefor, and use thereof
WO2022054005A1 (en) * 2020-09-14 2022-03-17 Galderma Holding SA Novel jak inhibitor compounds, method for synthesizing same and use thereof
US12583868B2 (en) 2020-09-14 2026-03-24 Galderma Holding SA JAK inhibitors and methods for synthesizing and using thereof
US12390451B2 (en) 2021-03-11 2025-08-19 Janssen Pharmaceutica Nv Small molecule inhibitor of the JAK family of kinases
EP4319743A4 (en) * 2021-04-07 2025-03-12 Abbvie Inc. UPADACITINIB CO-CRYSTALS
WO2022217257A1 (en) * 2021-04-07 2022-10-13 Abbvie Inc. Cocrystals of upadacitinib
CN113603693A (zh) * 2021-07-13 2021-11-05 陕西丽彩药业有限公司 一种2-溴-5-对甲苯磺酰基-5H-吡咯并[2,3-b]吡嗪的制备方法
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
WO2023139233A1 (en) 2022-01-24 2023-07-27 Abivax Combination of 8-chloro-n-(4-(trifluoromethoxy)phenyl)quinolin-2-amine and its derivatives with a jak inhibitor
WO2025000671A1 (zh) * 2023-06-30 2025-01-02 凌科药业(杭州)有限公司 一种磺酰胺类化合物及其应用
WO2025102268A1 (en) * 2023-11-15 2025-05-22 Lynk Pharmaceuticals Co. Ltd. Solid state forms, pharmaceutical compositions, preparation methods and use thereof

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