AR118162A2 - Procesos e intermedios para hacer un inhibidor de jak - Google Patents

Procesos e intermedios para hacer un inhibidor de jak

Info

Publication number
AR118162A2
AR118162A2 ARP200100486A ARP200100486A AR118162A2 AR 118162 A2 AR118162 A2 AR 118162A2 AR P200100486 A ARP200100486 A AR P200100486A AR P200100486 A ARP200100486 A AR P200100486A AR 118162 A2 AR118162 A2 AR 118162A2
Authority
AR
Argentina
Prior art keywords
intermediates
processes
make
jak inhibitor
jak
Prior art date
Application number
ARP200100486A
Other languages
English (en)
Original Assignee
Incyte Holdings Corp
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=50382653&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR118162(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Incyte Holdings Corp filed Critical Incyte Holdings Corp
Publication of AR118162A2 publication Critical patent/AR118162A2/es

Links

Classifications

    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J31/00—Catalysts comprising hydrides, coordination complexes or organic compounds
    • B01J31/02—Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J31/00—Catalysts comprising hydrides, coordination complexes or organic compounds
    • B01J31/26—Catalysts comprising hydrides, coordination complexes or organic compounds containing in addition, inorganic metal compounds not provided for in groups B01J31/02 - B01J31/24
    • B01J31/28—Catalysts comprising hydrides, coordination complexes or organic compounds containing in addition, inorganic metal compounds not provided for in groups B01J31/02 - B01J31/24 of the platinum group metals, iron group metals or copper
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/04—Esters of boric acids

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Materials Engineering (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Ésta se refiere a procesos e intermedios para hacer {1-{1-[3-fluoro-2-(trifluorometil)isonicotinoil]piperidin-4-il}-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrilo, útil en el tratamiento de enfermedades relacionadas con la actividad de cinasas Janus (JAK) incluyendo trastornos inflamatorios, trastornos autoinmunes, cáncer y otras enfermedades.
ARP200100486A 2013-03-06 2020-02-21 Procesos e intermedios para hacer un inhibidor de jak AR118162A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361773659P 2013-03-06 2013-03-06

Publications (1)

Publication Number Publication Date
AR118162A2 true AR118162A2 (es) 2021-09-22

Family

ID=50382653

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP140100716A AR095018A1 (es) 2013-03-06 2014-03-05 Procesos e intermedios para hacer un inhibidor de jak
ARP200100486A AR118162A2 (es) 2013-03-06 2020-02-21 Procesos e intermedios para hacer un inhibidor de jak

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP140100716A AR095018A1 (es) 2013-03-06 2014-03-05 Procesos e intermedios para hacer un inhibidor de jak

Country Status (35)

Country Link
US (3) US8987443B2 (es)
EP (3) EP3489239B1 (es)
JP (2) JP6397831B2 (es)
KR (2) KR102236232B1 (es)
CN (1) CN105189509B (es)
AR (2) AR095018A1 (es)
AU (1) AU2014225938B2 (es)
BR (2) BR112015021458B1 (es)
CA (2) CA3091179C (es)
CL (2) CL2015002468A1 (es)
CR (2) CR20190518A (es)
CY (2) CY1121512T1 (es)
DK (1) DK2964650T3 (es)
EA (2) EA201891157A1 (es)
ES (2) ES2707355T3 (es)
HK (1) HK1218540A1 (es)
HR (2) HRP20211922T1 (es)
HU (2) HUE057262T2 (es)
IL (3) IL240891A0 (es)
LT (2) LT2964650T (es)
ME (1) ME03350B (es)
MX (2) MX2020003446A (es)
NZ (2) NZ711976A (es)
PE (2) PE20151902A1 (es)
PH (1) PH12015501958A1 (es)
PL (2) PL3489239T3 (es)
PT (2) PT3489239T (es)
RS (2) RS58547B1 (es)
SG (2) SG10201707259PA (es)
SI (2) SI2964650T1 (es)
TR (1) TR201820520T4 (es)
TW (1) TWI634121B (es)
UA (2) UA121532C2 (es)
WO (1) WO2014138168A1 (es)
ZA (1) ZA201908345B (es)

Families Citing this family (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3466953B1 (en) 2005-12-13 2021-02-03 Incyte Holdings Corporation Pyrrolo[2,3-d]pyrimidine derivative as janus kinase inhibitor
SI2173752T2 (sl) 2007-06-13 2022-09-30 Incyte Holdings Corporation Soli inhibitorja za janus kinazo (r)-3-(4-(7h-pirolo(2,3-d)pirimidin-4- il)-1h-pirazol-1-il)-3-ciklopentilpropannitrila
AR076920A1 (es) 2009-05-22 2011-07-20 Incyte Corp 3-(4-(7h-pirrolo(2,3-d)pirimidin-4-il)-1h-pirazol-1-il)octano-o heptano--nitrilo como inhibidores de jak
MX2011012353A (es) 2009-05-22 2011-12-14 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2, 3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de la cinasa janus.
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
AR081315A1 (es) 2010-03-10 2012-08-08 Incyte Corp Derivados heterociclicos de piperidin y pirimidin -4-il-azetidina, una forma cristalina de la sal del acido acetonitriladipico de un derivado pirimidinico, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades relacionadas con la inhibicion de jak-1, t
CN103002875B (zh) 2010-05-21 2016-05-04 因塞特控股公司 Jak抑制剂的局部用制剂
BR112013012502A2 (pt) 2010-11-19 2019-03-06 Incyte Corporation pirrolopiridina ciclobutil substituída e derivados de pirrolopirimidina derivativos como inibidores de jak
MX344479B (es) 2011-06-20 2016-12-16 Incyte Holdings Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de cinasa janus (jak).
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
WO2013173720A1 (en) 2012-05-18 2013-11-21 Incyte Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
EP2906654B1 (en) 2012-10-09 2020-04-08 Avery Dennison Corporation Adhesives and related methods
EA031882B1 (ru) 2012-11-01 2019-03-29 Инсайт Холдингс Корпорейшн Трициклические конденсированные производные тиофена как ингибиторы jak
UA120834C2 (uk) 2012-11-15 2020-02-25 Інсайт Холдінгс Корпорейшн Лікарські форми руксолітинібу зі сповільненим вивільненням
US9278950B2 (en) 2013-01-14 2016-03-08 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
TW201932456A (zh) 2013-01-15 2019-08-16 美商英塞特控股公司 適用作pim激酶抑制劑之噻唑甲醯胺及吡啶甲醯胺化合物
RS58547B1 (sr) 2013-03-06 2019-05-31 Incyte Holdings Corp Postupci i intermedijeri za dobijanje inhibitora jak
MX2015015738A (es) 2013-05-17 2016-03-16 Incyte Corp Derivados del bipirazol como inhibidores de janus cinasa (jak).
MY195091A (en) 2013-08-07 2023-01-10 Incyte Corp Sustained Release Dosage Forms for a JAK1 Inhibitor
WO2015027124A1 (en) 2013-08-23 2015-02-26 Incyte Corporation Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors
MX2020004398A (es) 2014-04-08 2022-06-06 Incyte Corp Tratamiento de neoplasias malignas de linfocitos b mediante una combinacion de inhibidores de janus cinasa (jak) y fosfatidilinositol 3 cinasa (pi3k).
US9802957B2 (en) 2014-04-30 2017-10-31 Incyte Corporation Processes of preparing a JAK1 inhibitor and new forms thereto
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
WO2016010897A1 (en) 2014-07-14 2016-01-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors
US10106525B2 (en) 2015-01-26 2018-10-23 BioAxone BioSciences, Inc. Rho kinase inhibitor BA-1049 (R) and active metabolites thereof
US10857157B2 (en) 2015-01-26 2020-12-08 BioAxone BioSciences, Inc. Treatment of cerebral cavernous malformations and cerebral aneurysms with rho kinase inhibitors
US9540347B2 (en) 2015-05-29 2017-01-10 Incyte Corporation Pyridineamine compounds useful as Pim kinase inhibitors
AR104918A1 (es) * 2015-06-19 2017-08-23 Lilly Co Eli Procesos e intermediarios para la preparación de {1-(etilsulfonil)-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]azetidin-3-il}acetonitrilo
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
WO2017059251A1 (en) 2015-10-02 2017-04-06 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
CN105294699B (zh) * 2015-12-04 2019-06-11 上海勋和医药科技有限公司 巴瑞替尼的制备方法
CN105541891B (zh) * 2016-02-04 2017-11-28 东南大学 巴瑞替尼的中间体及其制备方法及由该中间体制备巴瑞替尼的方法
CN107759623B (zh) * 2016-08-23 2020-08-14 苏州旺山旺水生物医药有限公司 Jak抑制剂的中间体及其制备方法
CN106496195B (zh) * 2016-10-18 2019-03-08 杭州科巢生物科技有限公司 巴瑞替尼及其中间体的合成方法
JP7117306B2 (ja) * 2016-12-21 2022-08-12 バイオアクソン バイオサイエンシーズ インコーポレイテッド Ｒｈｏキナーゼ阻害剤ＢＡ‐１０４９（Ｒ）及びその活性代謝物
US11198680B2 (en) 2016-12-21 2021-12-14 BioAxone BioSciences, Inc. Rho kinase inhibitor BA-1049 (R) and active metabolites thereof
CN106946917B (zh) * 2017-03-20 2019-06-11 杭州科巢生物科技有限公司 一种jak抑制剂巴瑞替尼及其中间体的新合成方法
WO2019014322A1 (en) 2017-07-11 2019-01-17 BioAxone BioSciences, Inc. KINASE INHIBITORS FOR THE TREATMENT OF DISEASES
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
SG11202007164UA (en) * 2018-01-30 2020-08-28 Incyte Corp Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
BR122023022189A2 (pt) 2018-02-16 2024-02-20 Incyte Corporation Usos de inibidores da via de jak1 para o tratamento de distúrbios relacionados a citocinas
EP3775284A1 (en) 2018-03-30 2021-02-17 Incyte Corporation Biomarkers for inflammatory skin disease
KR20210018203A (ko) 2018-03-30 2021-02-17 인사이트 코포레이션 Jak 억제제를 사용하는 화농성 한선염의 치료
CA3097025A1 (en) 2018-04-13 2019-10-17 Incyte Corporation Biomarkers for graft-versus-host disease
JP2021535176A (ja) * 2018-09-04 2021-12-16 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー Ｊａｋ阻害剤およびその中間体を調製するためのプロセス
AU2019374072A1 (en) 2018-10-31 2021-05-27 Incyte Corporation Combination therapy for treatment of hematological diseases
EP3897627A1 (en) 2018-12-19 2021-10-27 Incyte Corporation Jak1 pathway inhibitors for the treatment of gastrointestinal disease
CN114007621A (zh) 2019-03-05 2022-02-01 因赛特公司 用于治疗慢性肺同种异体移植物功能障碍的jak1途径抑制剂
EP3941474A2 (en) 2019-03-19 2022-01-26 Incyte Corporation Biomarkers for vitiligo
CN112225739B (zh) * 2019-07-15 2024-04-26 宜昌东阳光制药有限公司 一种氮杂环丁烷化合物的制备方法
WO2021072116A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
WO2021072098A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
WO2021076124A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Use of jak1 inhibitors for the treatment of cutaneous lupus erythematosus and lichen planus (lp)
CN110627714A (zh) * 2019-10-16 2019-12-31 安庆博曼生物技术有限公司 3-氟-2-三氟甲基异烟酸的合成方法
US11992490B2 (en) 2019-10-16 2024-05-28 Incyte Corporation Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP)
CN110683978A (zh) * 2019-10-30 2020-01-14 西安医学院 一种3-腈基亚甲基氮杂环丁烷-1-碳酸叔丁酯的制备方法
CN111320634A (zh) * 2020-04-14 2020-06-23 浙江工业大学 一种乙酰氧取代的吡咯并[2,3-d]嘧啶衍生物的制备方法
US11685731B2 (en) 2020-06-02 2023-06-27 Incyte Corporation Processes of preparing a JAK1 inhibitor
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
JP2023539126A (ja) 2020-08-18 2023-09-13 インサイト・コーポレイション Ｊａｋ阻害剤を調製するための方法及び中間体
JP2023538614A (ja) 2020-08-18 2023-09-08 インサイト・コーポレイション Ｊａｋ１阻害剤を調製するためのプロセス及び中間体
MX2023006638A (es) 2020-12-04 2023-08-22 Incyte Corp Inhibidor de la cinasa janus (jak) con un análogo de la vitamina d para el tratamiento de enfermedades de la piel.
MX2023006542A (es) 2020-12-08 2023-08-25 Incyte Corp Inhibidores de la vía cinasa jano 1 (jak1) para el tratamiento del vitiligo.
CN112625030A (zh) * 2020-12-25 2021-04-09 杭州澳赛诺生物科技有限公司 一种一锅法合成n-保护3-溴代吡唑的合成方法
MX2023008141A (es) 2021-01-11 2023-10-20 Incyte Corp Terapia combinada que comprende el inhibidor de la vía de proteínas tirosina cinasas de janus cinasas (jak) y el inhibidor de la proteína cinasa asociada a rho (rock).
JP2024526762A (ja) 2021-07-12 2024-07-19 インサイト・コーポレイション Ｊａｋ阻害剤を調製するためのプロセス及び中間体
US20240058343A1 (en) 2022-08-05 2024-02-22 Incyte Corporation Treatment of urticaria using jak inhibitors

Family Cites Families (285)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2985589A (en) 1957-05-22 1961-05-23 Universal Oil Prod Co Continuous sorption process employing fixed bed of sorbent and moving inlets and outlets
US3832460A (en) 1971-03-19 1974-08-27 C Kosti Anesthetic-vasoconstrictor-antihistamine composition for the treatment of hypertrophied oral tissue
US4140755A (en) 1976-02-13 1979-02-20 Hoffmann-La Roche Inc. Sustained release tablet formulations
DE3036390A1 (de) 1980-09-26 1982-05-13 Troponwerke GmbH & Co KG, 5000 Köln Neue pyrrolo-pyrimidine, verfahren zu ihrer herstellung und ihre verwendung bei der herstellung von biologischen wirkstoffen
DE3220113A1 (de) 1982-05-28 1983-12-01 Basf Ag, 6700 Ludwigshafen Difluormethoxiphenylthiophosphorsaeureester
US4402832A (en) 1982-08-12 1983-09-06 Uop Inc. High efficiency continuous separation process
US4548990A (en) 1983-08-15 1985-10-22 Ciba-Geigy Corporation Crosslinked, porous polymers for controlled drug delivery
US4498991A (en) 1984-06-18 1985-02-12 Uop Inc. Serial flow continuous separation process
NL8403224A (nl) 1984-10-24 1986-05-16 Oce Andeno Bv Dioxafosforinanen, de bereiding ervan en de toepassing voor het splitsen van optisch actieve verbindingen.
CA1306260C (en) 1985-10-18 1992-08-11 Shionogi & Co., Ltd. Condensed imidazopyridine derivatives
US4921947A (en) 1986-03-31 1990-05-01 Eli Lilly And Company Process for preparing macrolide derivatives
JPH0710876Y2 (ja) 1989-08-31 1995-03-15 石垣機工株式会社 スクリュープレスにおける脱水筒の洗浄装置
DE69027440T2 (de) 1989-10-11 1997-02-06 Teijin Ltd Bizyklische pyrimidinderivate, verfahren zu deren herstellung und diese enthaltende pharmazeutische zusammensetzung
IT1258781B (it) 1992-01-16 1996-02-29 Zambon Spa Composizione farmaceutica oftalmica contenente n-acetilcisteina e polivinilalcol
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
FR2695126B1 (fr) 1992-08-27 1994-11-10 Sanofi Elf Dérivés d'acide thiényl ou pyrrolyl carboxyliques, leur préparation et médicaments les contenant.
AU671491B2 (en) 1992-12-18 1996-08-29 F. Hoffmann-La Roche Ag N-oxycarbonyl substituted 5'-deoxy-5-fluorcytidines
JPH0710876A (ja) 1993-06-24 1995-01-13 Teijin Ltd ４位に環状アミノ基を有するピロロ［２，３―ｄ］ピリミジン
EP0727217A3 (en) 1995-02-10 1997-01-15 Suntory Ltd Pharmaceutical and cosmetic compositions containing God-type ellagitannin as an active ingredient
IL117580A0 (en) 1995-03-29 1996-07-23 Merck & Co Inc Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them
US5856326A (en) 1995-03-29 1999-01-05 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
PL324486A1 (en) 1995-07-05 1998-05-25 Du Pont Fungicidal pyrimidinones
CZ1598A3 (cs) 1995-07-06 1998-04-15 Novartis Ag Pyrrolopyrimidiny a způsoby jejich přípravy
US5630943A (en) 1995-11-30 1997-05-20 Merck Patent Gesellschaft Mit Beschrankter Haftung Discontinuous countercurrent chromatographic process and apparatus
GB9604361D0 (en) 1996-02-29 1996-05-01 Pharmacia Spa 4-Substituted pyrrolopyrimidine compounds as tyrosine kinase inhibitors
AU727939B2 (en) 1996-04-03 2001-01-04 Merck & Co., Inc. A method of treating cancer
JP2000513711A (ja) 1996-04-18 2000-10-17 メルク エンド カンパニー インコーポレーテッド 癌の治療法
US5795909A (en) 1996-05-22 1998-08-18 Neuromedica, Inc. DHA-pharmaceutical agent conjugates of taxanes
JP2000508335A (ja) 1996-05-30 2000-07-04 メルク エンド カンパニー インコーポレーテッド 癌の治療方法
US6624138B1 (en) 2001-09-27 2003-09-23 Gp Medical Drug-loaded biological material chemically treated with genipin
CA2286239A1 (en) 1997-04-07 1998-10-15 Merck & Co., Inc. A method of treating cancer
US6063284A (en) 1997-05-15 2000-05-16 Em Industries, Inc. Single column closed-loop recycling with periodic intra-profile injection
US6060038A (en) 1997-05-15 2000-05-09 Merck & Co., Inc. Radiolabeled farnesyl-protein transferase inhibitors
CA2295620A1 (en) 1997-08-11 1999-02-18 Boehringer Ingelheim Pharmaceuticals, Inc. 5,6-heteroaryl-dipyrido¬2,3-b:3',2'-f|azepines and their use in the prevention or treatment of hiv infection
US6075056A (en) 1997-10-03 2000-06-13 Penederm, Inc. Antifungal/steroid topical compositions
US6025366A (en) 1998-04-02 2000-02-15 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
TR200100189T2 (tr) 1998-06-04 2001-05-21 Abbott Laboratories Hücre yapışması engelleyici iltihaplanmaya karşı bileşikler
US6232320B1 (en) 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
KR100415791B1 (ko) 1998-06-19 2004-01-24 화이자 프로덕츠 인코포레이티드 피롤로[2,3-디]피리미딘 화합물
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
CA2339961C (en) 1998-08-11 2009-01-20 Novartis Ag Isoquinoline derivatives with angiogenesis inhibiting activity
JP2000119271A (ja) 1998-08-12 2000-04-25 Hokuriku Seiyaku Co Ltd １ｈ―イミダゾピリジン誘導体
PT1109534E (pt) 1998-09-10 2003-06-30 Nycomed Danmark As Composicoes farmaceuticas de farmacos de libertacao rapida
US6413419B1 (en) 1998-10-29 2002-07-02 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic
FR2785196B1 (fr) 1998-10-29 2000-12-15 Inst Francais Du Petrole Procede et dispositif de separation avec des zones chromatographiques a longueur variable
US6375839B1 (en) 1998-10-29 2002-04-23 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic zones
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
WO2000051614A1 (en) 1999-03-03 2000-09-08 Merck & Co., Inc. Inhibitors of prenyl-protein transferases
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
US6217895B1 (en) 1999-03-22 2001-04-17 Control Delivery Systems Method for treating and/or preventing retinal diseases with sustained release corticosteroids
US6239113B1 (en) 1999-03-31 2001-05-29 Insite Vision, Incorporated Topical treatment or prevention of ocular infections
WO2000063168A1 (en) 1999-04-16 2000-10-26 Coelacanth Chemical Corporation Synthesis of azetidine derivatives
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
CA2387535A1 (en) 1999-10-13 2001-04-19 Banyu Pharmaceutical Co., Ltd. Substituted imidazolidinone derivatives
SI1235830T1 (en) 1999-12-10 2004-06-30 Pfizer Products Inc. PYRROLO(2,3-d)PYRIMIDINE COMPOUNDS AS PROTEIN KINASES INHIBITORS
EE05180B1 (et) 1999-12-24 2009-06-15 Aventis Pharma Limited Asaindooli sisaldav farmatseutiline kompositsioon raviotstarbeliseks kasutamiseks, asaindoolid ning nende kasutamine ravimite valmistamiseks, mis on ette n„htud proteiinikinaasi kataltilise toime p„rssimiseks
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US7235551B2 (en) 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
PT1142566E (pt) 2000-04-07 2004-02-27 Medidom Lab Formulacao oftalmica topica na forma de uma solucao aquosa e uso de uma ciclosporina em associacao com acido hialuronico ou um de seus sais e com polisorbato 80
AU4878601A (en) 2000-04-20 2001-11-07 Mitsubishi Corporation Aromatic amide compounds
IL152275A0 (en) 2000-04-25 2003-05-29 Icos Corp Inhibitors of human phosphatidyl-inositol 3-kinase delta
US20030022819A1 (en) 2000-06-16 2003-01-30 Ling Leona E. Angiogenesis-modulating compositions and uses
US7498304B2 (en) 2000-06-16 2009-03-03 Curis, Inc. Angiogenesis-modulating compositions and uses
US6335342B1 (en) 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
ES2344831T3 (es) 2000-06-23 2010-09-08 Mitsubishi Tanabe Pharma Corporation Potenciadores de un efecto antitumoral.
JP4068958B2 (ja) 2000-06-26 2008-03-26 ファイザー・プロダクツ・インク 免疫抑制剤としてのピロロ（２，３−ｄ）ピリミジン化合物
CA2413330A1 (en) 2000-06-28 2002-01-03 Smithkline Beecham P.L.C. Wet milling process
AU2001278790A1 (en) 2000-08-22 2002-03-04 Hokuriku Seiyaku Co. Ltd 1h-imidazopyridine derivatives
JP4377583B2 (ja) 2000-12-05 2009-12-02 バーテックス ファーマシューティカルズ インコーポレイテッド Ｃ−ｊｕｎｎ末端キナーゼ（ｊｎｋ）および他のタンパク質キナーゼのインヒビター
GB0100622D0 (en) 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds V111
JP2004520347A (ja) 2001-01-15 2004-07-08 グラクソ　グループ　リミテッド Ｌｄｌ−受容体発現のインデューサーとしてのアリールピペリジンおよびピペラジン誘導体
JP2004528295A (ja) 2001-01-30 2004-09-16 サイトピア ピーティワイ リミテッド キナーゼ阻害方法
AU2002308748A1 (en) 2001-05-16 2002-11-25 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
GB0115393D0 (en) 2001-06-23 2001-08-15 Aventis Pharma Ltd Chemical compounds
EP1414443B1 (en) 2001-08-01 2006-11-15 Merck & Co., Inc. BENZIMIDAZO 4,5-f|ISOQUINOLINONE DERIVATIVES
EP1436291B1 (en) 2001-09-19 2009-01-14 Aventis Pharma S.A. Indolizines as kinase protein inhibitors
US6429231B1 (en) 2001-09-24 2002-08-06 Bradley Pharmaceuticals, Inc. Compositions containing antimicrobials and urea for the treatment of dermatological disorders and methods for their use
ATE335490T1 (de) 2001-10-30 2006-09-15 Novartis Pharma Gmbh Staurosporin-derivate als hemmer der flt3- rezeptor-tyrosinkinase-wirkung
JP2003155285A (ja) 2001-11-19 2003-05-27 Toray Ind Inc 環状含窒素誘導体
KR20040058340A (ko) 2001-11-30 2004-07-03 데이진 가부시키가이샤 5-(3-시아노페닐)-3-포르밀벤조산 화합물의 제조 방법
GT200200234A (es) 2001-12-06 2003-06-27 Compuestos cristalinos novedosos
US6995144B2 (en) 2002-03-14 2006-02-07 Eisai Co., Ltd. Nitrogen containing heterocyclic compounds and medicines containing the same
TW200403058A (en) 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
EP1506189A1 (en) 2002-04-26 2005-02-16 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
JP2005530745A (ja) 2002-05-02 2005-10-13 メルク　エンド　カムパニー　インコーポレーテッド チロシンキナーゼ阻害剤
KR20100120243A (ko) 2002-05-07 2010-11-12 피시비다 유에스 인코포레이티드 약물 전달 장치를 형성하는 공정
CN100558715C (zh) 2002-05-23 2009-11-11 西托匹亚有限公司 蛋白激酶抑制剂
PE20040522A1 (es) 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
CA2490340A1 (en) 2002-06-26 2004-01-08 Idemitsu Kosan Co., Ltd. Hydrogenated copolymer, production process for the same and hot melt adhesive composition using the same
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
GB0215844D0 (en) 2002-07-09 2002-08-14 Novartis Ag Organic compounds
WO2004007472A1 (ja) 2002-07-10 2004-01-22 Ono Pharmaceutical Co., Ltd. Ｃｃｒ４アンタゴニストおよびその医薬用途
CN1684738A (zh) 2002-09-20 2005-10-19 爱尔康公司 细胞因子合成抑制剂用于治疗干眼病的用途
US20040204404A1 (en) 2002-09-30 2004-10-14 Robert Zelle Human N-type calcium channel blockers
CA2506773A1 (en) 2002-11-04 2004-05-21 Vertex Pharmaceuticals Incorporated Heteroaryl-pyramidine derivatives as jak inhibitors
TWI335913B (en) 2002-11-15 2011-01-11 Vertex Pharma Diaminotriazoles useful as inhibitors of protein kinases
US20040099204A1 (en) 2002-11-25 2004-05-27 Nestor John J. Sheet, page, line, position marker
WO2004047843A1 (en) 2002-11-26 2004-06-10 Pfizer Products Inc. Method of treatment of transplant rejection
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
TWI335819B (en) 2002-12-24 2011-01-11 Alcon Inc Use of oculosurface selective glucocorticoid in the treatment of dry eye
US7135493B2 (en) 2003-01-13 2006-11-14 Astellas Pharma Inc. HDAC inhibitor
US7167750B2 (en) 2003-02-03 2007-01-23 Enteromedics, Inc. Obesity treatment with electrically induced vagal down regulation
WO2004072063A1 (en) 2003-02-07 2004-08-26 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrolls useful as inhibitors of protein kinases
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
CA2522595A1 (en) 2003-04-03 2004-10-28 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
SE0301373D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
FR2857454B1 (fr) 2003-07-08 2006-08-11 Aventis Pasteur Dosage des acides techoiques des bacteries gram+
US20050043346A1 (en) 2003-08-08 2005-02-24 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
JP5010917B2 (ja) 2003-08-29 2012-08-29 エグゼリクシス， インコーポレイテッド ｃ−Ｋｉｔ調節因子および使用方法
WO2005026129A1 (en) 2003-09-15 2005-03-24 Gpc Biotech Ag Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
PE20050952A1 (es) 2003-09-24 2005-12-19 Novartis Ag Derivados de isoquinolina como inhibidores de b-raf
ATE490771T1 (de) 2003-10-24 2010-12-15 Santen Pharmaceutical Co Ltd Therapeutisches mittel für keratokonjunktive erkrankungen
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
JP2007512316A (ja) 2003-11-25 2007-05-17 ファイザー・プロダクツ・インク アテローム性動脈硬化症の治療方法
KR20060096153A (ko) 2003-12-17 2006-09-07 화이자 프로덕츠 인코포레이티드 이식 거부 치료용 피롤로[2,3-ｄ]피리미딘 화합물
DK1696920T3 (en) 2003-12-19 2015-01-19 Plexxikon Inc RELATIONS AND PROCEDURES FOR THE DEVELOPMENT OF LAW MODULATORS
EP1694659B8 (en) 2003-12-19 2008-10-08 Schering Corporation Thiadiazoles as cxc- and cc- chemokine receptor ligands
JP4928949B2 (ja) 2003-12-23 2012-05-09 アステックス、セラピューティックス、リミテッド タンパク質キナーゼモジュレーターとしてのピラゾール誘導体
US20050239806A1 (en) 2004-01-13 2005-10-27 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
WO2005089502A2 (en) 2004-03-18 2005-09-29 The Brigham And Women's Hospital, Inc. Methods for the treatment of synucleinopathies
ATE508129T1 (de) 2004-03-30 2011-05-15 Vertex Pharma Als inhibitoren von jak und anderen proteinkinasen geeignete azaindole
AU2005249380C1 (en) 2004-04-23 2012-09-20 Exelixis, Inc. Kinase modulators and methods of use
US20060106020A1 (en) 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
US7558717B2 (en) 2004-04-28 2009-07-07 Vertex Pharmaceuticals Incorporated Crystal structure of human JAK3 kinase domain complex and binding pockets thereof
AU2005237254B2 (en) 2004-05-03 2010-02-04 Novartis Ag Combinations comprising a S1P receptor agonist and a JAK3 kinase inhibitor
JP2007537296A (ja) 2004-05-14 2007-12-20 アボット・ラボラトリーズ 治療薬としてのキナーゼ阻害薬
PE20060426A1 (es) 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
AR049511A1 (es) 2004-06-10 2006-08-09 Irm Llc Compuestos y composiciones como inhibidores de quinasa de proteina
US8039674B2 (en) 2004-06-23 2011-10-18 Ono Pharmaceutical Co., Ltd. Compound having S1P receptor binding potency and use thereof
EP1765819B1 (en) 2004-06-30 2014-03-12 Vertex Pharmaceuticals Inc. Azaindoles useful as inhibitors of protein kinases
US7138423B2 (en) 2004-07-20 2006-11-21 Bristol-Myers Squibb Company Arylpyrrolidine derivatives as NK-1 /SSRI antagonists
FR2873691B1 (fr) 2004-07-29 2006-10-06 Sanofi Synthelabo Derives d'amino-piperidine, leur preparation et leur application en therapeutique
WO2006013114A1 (en) 2004-08-06 2006-02-09 Develogen Aktiengesellschaft Use of a timp-2 secreted protein product for preventing and treating pancreatic diseases and/or obesity and/or metabolic syndrome
CN101006186A (zh) 2004-08-23 2007-07-25 财团法人牧岩生命工学研究所 用于检测sars冠状病毒的引物和探针，包括该引物和/或探针的试剂盒及其检测方法
US20070054916A1 (en) 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
NZ554353A (en) 2004-10-13 2010-01-29 Hoffmann La Roche Disubstituted pyrazolobenzodiazepines useful as inhibitors for CDK2 and angiogenesis, and for the treatment of breast, colon, lung and prostate cancer
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
UY29177A1 (es) 2004-10-25 2006-05-31 Astex Therapeutics Ltd Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos
PT1812440E (pt) 2004-11-04 2011-01-25 Vertex Pharma Pirazolo[1,5-a]pirimidinas úteis enquanto inibidores de proteínas cinases
AU2005309019A1 (en) 2004-11-24 2006-06-01 Novartis Ag Combinations of JAK inhibitors and at least one of Bcr-Abl, Flt-3, FAK or RAF kinase inhibitors
US7517870B2 (en) 2004-12-03 2009-04-14 Fondazione Telethon Use of compounds that interfere with the hedgehog signaling pathway for the manufacture of a medicament for preventing, inhibiting, and/or reversing ocular diseases related with ocular neovascularization
WO2006065916A1 (en) 2004-12-14 2006-06-22 Alcon, Inc. Method of treating dry eye disorders using 13(s)-hode and its analogs
TW200635899A (en) 2004-12-22 2006-10-16 Astrazeneca Ab Chemical compounds
AR054416A1 (es) 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
CA2595574A1 (en) 2005-01-20 2006-07-27 Pfizer Limited. Chemical compounds
EP1844050B1 (en) 2005-02-03 2009-01-14 Vertex Pharmaceuticals, Inc. Pyrrolopyrimidines useful as inhibitors of protein kinase
US7683171B2 (en) 2005-02-04 2010-03-23 Bristol-Myers Squibb Company 1H-imidazo[4,5-d]thieno[3,2-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
CN101500574A (zh) 2005-03-15 2009-08-05 Irm责任有限公司 用作蛋白激酶抑制剂的化合物和组合物
EP1874772A1 (en) 2005-04-05 2008-01-09 Pharmacopeia, Inc. Purine and imidazopyridine derivatives for immunosuppression
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
JP2008545660A (ja) 2005-05-20 2008-12-18 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼ阻害剤として有用なピロロピリジン化合物
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
KR101312225B1 (ko) 2005-06-08 2013-09-26 리겔 파마슈티칼스, 인크. Ｊａｋ 경로의 억제를 위한 조성물 및 방법
WO2006136823A1 (en) 2005-06-21 2006-12-28 Astex Therapeutics Limited Heterocyclic containing amines as kinase b inhibitors
CA2613015C (en) 2005-06-22 2012-04-03 Plexxikon, Inc. Pyrrolo [2, 3-b] pyridine derivatives as protein kinase inhibitors
CN102127078A (zh) 2005-07-14 2011-07-20 安斯泰来制药株式会社 Janus激酶3的杂环类抑制剂
FR2889662B1 (fr) 2005-08-11 2011-01-14 Galderma Res & Dev Emulsion de type huile-dans-eau pour application topique en dermatologie
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
EP2270014A1 (en) 2005-09-22 2011-01-05 Incyte Corporation Azepine inhibitors of janus kinases
SG151327A1 (en) 2005-09-30 2009-04-30 Vertex Pharmaceuticals Incopor Deazapurines useful as inhibitors of janus kinases
WO2007044894A2 (en) 2005-10-11 2007-04-19 Chembridge Research Laboratories, Inc. Cell-free protein expression systems and methods of use thereof
CA2623202C (en) 2005-10-14 2014-09-16 Sumitomo Chemical Company, Limited Hydrazide compound and pesticidal use of the same
DK1945631T3 (da) 2005-10-28 2012-10-22 Astrazeneca Ab 4- (3-aminopyrazole) pyrimidinderivater til anvendelse som tyrosinkinaseinhibitorer til behandling af cancer
BR122021011788B1 (pt) 2005-11-01 2022-01-25 Impact Biomedicines, Inc Inibidores de biaril meta pirimidina de cinases, composição farmacêutica e processo para preparar uma composição farmacêutica
WO2007062459A1 (en) 2005-11-29 2007-06-07 Cytopia Research Pty Ltd Selective kinase inhibitors based on pyridine scaffold
EP3466953B1 (en) 2005-12-13 2021-02-03 Incyte Holdings Corporation Pyrrolo[2,3-d]pyrimidine derivative as janus kinase inhibitor
US20130137681A1 (en) 2005-12-13 2013-05-30 Incyte Corporation HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS
WO2007076423A2 (en) 2005-12-22 2007-07-05 Smithkline Beecham Corporation INHIBITORS OF Akt ACTIVITY
CN101389324A (zh) 2005-12-23 2009-03-18 史密丝克莱恩比彻姆公司 Aurora激酶的氮杂吲哚抑制剂
WO2007084557A2 (en) 2006-01-17 2007-07-26 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of janus kinases
WO2007084667A2 (en) 2006-01-19 2007-07-26 Osi Pharmaceutical, Inc. Fused heterobicyclic kinase inhibitors
EP1981887A2 (en) 2006-02-01 2008-10-22 SmithKline Beecham Corporation Pyrrolo[2,3,b]pyridine derivatives useful as raf kinase inhibitors
US7745477B2 (en) 2006-02-07 2010-06-29 Hoffman-La Roche Inc. Heteroaryl and benzyl amide compounds
BRPI0708731A2 (pt) 2006-03-10 2011-06-07 Ono Pharmaceutical Co derivado heterocìclico nitrogenado, e agente farmacêutico compreendendo o derivado como ingrediente ativo
MX356221B (es) 2006-04-03 2018-05-18 Astellas Pharma Inc Heterocompuesto.
AU2007235487A1 (en) 2006-04-05 2007-10-18 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
WO2007116313A2 (en) 2006-04-12 2007-10-18 Pfizer Limited Pyrrolidine derivatives as modulators of chemokine ccr5 receptors
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
US20080051427A1 (en) 2006-05-18 2008-02-28 Fritz Schuckler Pharmaceutical Compositions and Methods of Using Same
US7691811B2 (en) 2006-05-25 2010-04-06 Bodor Nicholas S Transporter-enhanced corticosteroid activity and methods and compositions for treating dry eye
JO3235B1 (ar) 2006-05-26 2018-03-08 Astex Therapeutics Ltd مركبات بيررولوبيريميدين و استعمالاتها
JP2009544625A (ja) 2006-07-20 2009-12-17 メーメット・カーラマン Ｒｈｏキナーゼのベンゾチオフェン阻害剤
WO2008013622A2 (en) 2006-07-27 2008-01-31 E. I. Du Pont De Nemours And Company Fungicidal azocyclic amides
WO2008016123A1 (fr) 2006-08-03 2008-02-07 Takeda Pharmaceutical Company Limited INHIBITEUR DE LA GSK-3β
JP5252404B2 (ja) 2006-08-16 2013-07-31 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ピラジン化合物、その使用及び調製方法
AU2007293653B2 (en) 2006-09-08 2011-02-17 Novartis Ag N-biaryl (hetero) arylsulphonamide derivatives useful in the treatment of diseases mediated by lymphocytes interactions
WO2008035376A2 (en) 2006-09-19 2008-03-27 Council Of Scientific & Industrial Research A novel bio-erodible insert for ophthalmic applications and a process for the preparation thereof
CL2007002867A1 (es) 2006-10-04 2008-06-27 Pharmacopeia Inc Compuestos derivados de 2-(bencimidazolil)purina, inhibidores de janus quinasa 3; composicion farmaceutica que los contiene; y su uso para tratar enfermedades autoinmune, inflamatorias, cardiovasculares, rechazo de implante, entre otras.
TW200831104A (en) 2006-10-04 2008-08-01 Pharmacopeia Inc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
US20120225057A1 (en) 2006-10-11 2012-09-06 Deciphera Pharmaceuticals, Llc Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases
MY146474A (en) 2006-11-06 2012-08-15 Supergen Inc Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
US20080119496A1 (en) 2006-11-16 2008-05-22 Pharmacopeia Drug Discovery, Inc. 7-Substituted Purine Derivatives for Immunosuppression
EA026126B1 (ru) 2006-11-22 2017-03-31 Инсайт Холдингс Корпорейшн Имидазотриазины и имидазопиримидины в качестве ингибиторов киназы
WO2008067119A2 (en) 2006-11-27 2008-06-05 Smithkline Beecham Corporation Novel compounds
SG177221A1 (en) 2006-12-15 2012-01-30 Abbott Lab Novel oxadiazole compounds
US7687522B2 (en) 2006-12-20 2010-03-30 Amgen Inc. Substituted pyridines and pyrimidines and their use in treatment of cancer
CA2672903C (en) 2006-12-20 2012-10-23 Amgen Inc. Heterocyclic compounds and their use in treating inflammation, angiogenesis and cancer
CA2673038C (en) 2006-12-22 2015-12-15 Incyte Corporation Substituted tricyclic heteroaryl compounds as janus kinase inhibitors
BRPI0720434A2 (pt) 2006-12-22 2014-01-07 Sigma Tau Ind Farmaceuti Gel útil para liberação de fármacos oftálmicos
WO2008082840A1 (en) 2006-12-29 2008-07-10 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
KR20080062876A (ko) 2006-12-29 2008-07-03 주식회사 대웅제약 신규한 항진균성 트리아졸 유도체
WO2008082839A2 (en) 2006-12-29 2008-07-10 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
EP2132177B1 (en) 2007-03-01 2013-07-17 Novartis AG Pim kinase inhibitors and methods of their use
US8138181B2 (en) 2007-04-03 2012-03-20 Array Biopharma Inc. Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors
GB0709031D0 (en) 2007-05-10 2007-06-20 Sareum Ltd Pharmaceutical compounds
JP5603770B2 (ja) 2007-05-31 2014-10-08 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｃｃｒ２受容体拮抗薬およびその使用
GB0710528D0 (en) 2007-06-01 2007-07-11 Glaxo Group Ltd Novel compounds
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
SI2173752T2 (sl) 2007-06-13 2022-09-30 Incyte Holdings Corporation Soli inhibitorja za janus kinazo (r)-3-(4-(7h-pirolo(2,3-d)pirimidin-4- il)-1h-pirazol-1-il)-3-ciklopentilpropannitrila
WO2009007839A1 (en) 2007-07-11 2009-01-15 Pfizer Inc. Pharmaceutical compositions and methods of treating dry eye disorders
EA201000113A1 (ru) 2007-08-01 2010-08-30 Пфайзер Инк. Пиразольные соединения
WO2009049028A1 (en) 2007-10-09 2009-04-16 Targegen Inc. Pyrrolopyrimidine compounds and their use as janus kinase modulators
WO2009064486A2 (en) 2007-11-15 2009-05-22 Musc Foundation For Research Development Inhibitors of pim protein kinases, compositions, and methods for treating cancer
CN101910152B (zh) * 2007-11-16 2014-08-06 因塞特公司 作为janus激酶抑制剂的4-吡唑基-n-芳基嘧啶-2-胺和4-吡唑基-n-杂芳基嘧啶-2-胺
GB0723815D0 (en) 2007-12-05 2008-01-16 Glaxo Group Ltd Compounds
SI2231689T1 (sl) 2008-01-18 2016-11-30 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Novi citostatski 7-deazapurinski nukleozidi
EA019309B1 (ru) 2008-02-04 2014-02-28 Меркьюри Терапьютикс, Инк. Модуляторы ampk (амф-активируемой протеинкиназы)
AR070531A1 (es) 2008-03-03 2010-04-14 Novartis Ag Inhibidores de cinasa pim y metodos para su uso
KR20120108042A (ko) * 2008-03-11 2012-10-04 인사이트 코포레이션 Ｊａｋ 억제제로서의 아제티딘 및 시클로부탄 유도체
JP5384611B2 (ja) 2008-03-21 2014-01-08 ノバルティス アーゲー 新規ヘテロ環式化合物およびそれらの使用
CA2727928A1 (en) 2008-06-18 2009-12-23 Merck Sharp & Dohme Corp. Inhibitors of janus kinases
WO2009158687A1 (en) 2008-06-26 2009-12-30 Anterios, Inc. Dermal delivery
TWI461423B (zh) 2008-07-02 2014-11-21 Astrazeneca Ab 用於治療Pim激酶相關病狀及疾病之噻唑啶二酮化合物
FR2933409B1 (fr) 2008-07-03 2010-08-27 Centre Nat Rech Scient NOUVEAUX PYRROLO °2,3-a! CARBAZOLES ET LEUR UTILISATION COMME INHIBITEURS DES KINASES PIM
US8557809B2 (en) 2008-08-19 2013-10-15 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
TWI496779B (zh) 2008-08-19 2015-08-21 Array Biopharma Inc 作為ｐｉｍ激酶抑制劑之三唑吡啶化合物
PL2384326T3 (pl) 2008-08-20 2014-09-30 Zoetis Services Llc Związki pirolo[2,3-d]pirymidyonowe
CN103333157A (zh) 2008-09-02 2013-10-02 诺瓦提斯公司 作为激酶抑制剂的吡啶甲酰胺衍生物
WO2010026121A1 (en) 2008-09-02 2010-03-11 Novartis Ag Bicyclic kinase inhibitors
JP5584215B2 (ja) 2008-09-02 2014-09-03 ノバルティス アーゲー ヘテロ環ｐｉｍキナーゼ阻害剤
CL2009001884A1 (es) 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
JOP20190231A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
EP2210890A1 (en) 2009-01-19 2010-07-28 Almirall, S.A. Oxadiazole derivatives as S1P1 receptor agonists
US8263601B2 (en) 2009-02-27 2012-09-11 Concert Pharmaceuticals, Inc. Deuterium substituted xanthine derivatives
MX2011012353A (es) 2009-05-22 2011-12-14 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2, 3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de la cinasa janus.
AR076920A1 (es) 2009-05-22 2011-07-20 Incyte Corp 3-(4-(7h-pirrolo(2,3-d)pirimidin-4-il)-1h-pirazol-1-il)octano-o heptano--nitrilo como inhibidores de jak
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
TW201105674A (en) 2009-07-08 2011-02-16 Leo Pharma As Novel JAK receptor and protein tyrosine kinase inhibitors and pharmaceutical use thereof
WO2011025685A1 (en) 2009-08-24 2011-03-03 Merck Sharp & Dohme Corp. Jak inhibition blocks rna interference associated toxicities
TW201111385A (en) 2009-08-27 2011-04-01 Biocryst Pharm Inc Heterocyclic compounds as janus kinase inhibitors
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
JP5567136B2 (ja) 2009-09-08 2014-08-06 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト ４−置換ピリジン−３−イル−カルボキサミド化合物及び使用方法
EP2305660A1 (en) 2009-09-25 2011-04-06 Almirall, S.A. New thiadiazole derivatives
CN105541847B (zh) 2009-10-09 2019-08-16 因西特控股公司 3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的羟基衍生物、酮基衍生物和葡糖苷酸衍生物
MX2012004020A (es) 2009-10-20 2012-05-08 Cellzome Ltd Analogos de heterociclilo pirazolopirimidina como inhibidores de jak.
EP2332917B1 (en) 2009-11-11 2012-08-01 Sygnis Bioscience GmbH & Co. KG Compounds for PIM kinase inhibition and for treating malignancy
EP2504030A4 (en) 2009-11-24 2013-06-26 Alderbio Holdings Llc IL-6 ANTAGONISTS FOR INCREASING ALBUMIN AND / OR REDUCING CRP
WO2011069141A2 (en) 2009-12-04 2011-06-09 Board Of Regents, The University Of Texas System Interferon therapies in combination with blockade of stat3 activation
WO2011086053A1 (en) 2010-01-12 2011-07-21 F. Hoffmann-La Roche Ag Tricyclic heterocyclic compounds, compositions and methods of use thereof
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
MX2012009541A (es) 2010-02-18 2012-10-01 Incyte Corp Derivados de ciclobutano y metilciclobutano como inhibidores de janus cinasa.
AR081315A1 (es) 2010-03-10 2012-08-08 Incyte Corp Derivados heterociclicos de piperidin y pirimidin -4-il-azetidina, una forma cristalina de la sal del acido acetonitriladipico de un derivado pirimidinico, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades relacionadas con la inhibicion de jak-1, t
CN102985424B (zh) * 2010-04-14 2015-03-11 阵列生物制药公司 5,7-取代的-咪唑并[1,2-c]嘧啶
EP2390252A1 (en) 2010-05-19 2011-11-30 Almirall, S.A. New pyrazole derivatives
CN103002875B (zh) 2010-05-21 2016-05-04 因塞特控股公司 Jak抑制剂的局部用制剂
WO2011156698A2 (en) 2010-06-11 2011-12-15 Abbott Laboratories NOVEL PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS
US9351943B2 (en) 2010-07-01 2016-05-31 Matthew T. McLeay Anti-fibroblastic fluorochemical emulsion therapies
JP5833392B2 (ja) * 2010-09-17 2015-12-16 公益財団法人相模中央化学研究所 （トリフルオロビニル）ベンゼン類およびその製造方法
US20130252917A1 (en) 2010-09-30 2013-09-26 Portola Pharmaceuticals, Inc. Combination therapy of 4-(3-(2h-1,2,3-triazo-2-yl)phenylamino)-2-((1r,2s)-2-aminocyclohexylamino)pyrimidine-5-carboxamide and fludarabine
BR112013012502A2 (pt) 2010-11-19 2019-03-06 Incyte Corporation pirrolopiridina ciclobutil substituída e derivados de pirrolopirimidina derivativos como inibidores de jak
EP2640725B1 (en) 2010-11-19 2015-01-07 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
SG10201509919UA (en) 2010-12-03 2016-01-28 Ym Biosciences Australia Pty Treatment of jak2-mediated conditions
EP2675451B9 (en) 2011-02-18 2017-07-26 Novartis Pharma AG mTOR/JAK INHIBITOR COMBINATION THERAPY
MX344479B (es) 2011-06-20 2016-12-16 Incyte Holdings Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de cinasa janus (jak).
WO2013007768A1 (en) 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Tricyclic heterocyclic compounds, compositions and methods of use thereof as jak inhibitors
WO2013007765A1 (en) 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Fused tricyclic compounds for use as inhibitors of janus kinases
WO2013023119A1 (en) 2011-08-10 2013-02-14 Novartis Pharma Ag JAK P13K/mTOR COMBINATION THERAPY
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
WO2013173720A1 (en) 2012-05-18 2013-11-21 Incyte Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
US10155987B2 (en) 2012-06-12 2018-12-18 Dana-Farber Cancer Institute, Inc. Methods of predicting resistance to JAK inhibitor therapy
WO2014036016A1 (en) 2012-08-31 2014-03-06 Principia Biopharma Inc. Benzimidazole derivatives as itk inhibitors
EA031882B1 (ru) 2012-11-01 2019-03-29 Инсайт Холдингс Корпорейшн Трициклические конденсированные производные тиофена как ингибиторы jak
UA120834C2 (uk) 2012-11-15 2020-02-25 Інсайт Холдінгс Корпорейшн Лікарські форми руксолітинібу зі сповільненим вивільненням
RS58547B1 (sr) 2013-03-06 2019-05-31 Incyte Holdings Corp Postupci i intermedijeri za dobijanje inhibitora jak
MX2015015738A (es) 2013-05-17 2016-03-16 Incyte Corp Derivados del bipirazol como inhibidores de janus cinasa (jak).
MY195091A (en) 2013-08-07 2023-01-10 Incyte Corp Sustained Release Dosage Forms for a JAK1 Inhibitor
CN105555313A (zh) 2013-08-20 2016-05-04 因赛特公司 在c-反应蛋白水平较高的实体肿瘤患者中的存活益处
SI3110409T1 (sl) 2014-02-28 2018-11-30 Incyte Corporation Inhibitorji JAK1 za zdravljenje mielodisplastičnih sindromov
MX2020004398A (es) 2014-04-08 2022-06-06 Incyte Corp Tratamiento de neoplasias malignas de linfocitos b mediante una combinacion de inhibidores de janus cinasa (jak) y fosfatidilinositol 3 cinasa (pi3k).
US9802957B2 (en) 2014-04-30 2017-10-31 Incyte Corporation Processes of preparing a JAK1 inhibitor and new forms thereto
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1

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