[go: up one dir, main page]

PE20141409A1 - Derivados de piridin-2(1h)-ona como inhibidores de jak - Google Patents

Derivados de piridin-2(1h)-ona como inhibidores de jak

Info

Publication number
PE20141409A1
PE20141409A1 PE2014000084A PE2014000084A PE20141409A1 PE 20141409 A1 PE20141409 A1 PE 20141409A1 PE 2014000084 A PE2014000084 A PE 2014000084A PE 2014000084 A PE2014000084 A PE 2014000084A PE 20141409 A1 PE20141409 A1 PE 20141409A1
Authority
PE
Peru
Prior art keywords
independently
ilamino
haloalkyl
hydroxyalkyl
halogen
Prior art date
Application number
PE2014000084A
Other languages
English (en)
Inventor
Paul Robert Eastwood
Tana Jordi Bach
Santacana Lluis Miquel Pages
Original Assignee
Almirall Sa
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=44512745&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20141409(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Almirall Sa filed Critical Almirall Sa
Publication of PE20141409A1 publication Critical patent/PE20141409A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19—Cytokines; Lymphokines; Interferons
    • A61K38/21—Interferons [IFN]
    • A61K38/212—IFN-alpha
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19—Cytokines; Lymphokines; Interferons
    • A61K38/21—Interferons [IFN]
    • A61K38/215—IFN-beta
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychiatry (AREA)
  • Otolaryngology (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA (I) DONDE: m ES 0, 1, 2 O 3; X E Y SON INDEPENDIENTEMENTE N O -CR6; A Y B SON INDEPENDIENTEMENTE N O -CR7; D ES N O -CR5; W ES UN GRUPO ENLAZADOR SELECCIONADO DE O, S, -NR8-, ENTRE OTROS; R5 Y R6 SON INDEPENDIENTEMENTE H, HALOGENO, CIANO, HALOALQUILO C1-C4, CICLOALQUILO C3-C10, ENTRE OTROS; R7 ES H, HALOGENO, CIANO, CICLOALQUILO C3-C10, ENTRE OTROS; R8 ES H, HALOALQUILO C1-C4, HIDROXIALQUILO C1-C4, ENTRE OTROS; R1 ES H, HIDROXIALQUILO C1-C4, ALCOXI C1-C4, ENTRE OTROS; R2 ES H, HALOGENO, CICLOALQUENILO C3-C10, ENTRE OTROS; R3 Y R4 SON INDEPENDIENTEMENTE H, HALOALQUILO C1-C4, HIDROXIALQUILO C1-C4 O ALQUILO LINEAL O RAMIFICADO C1-C6. SON COMPUESTOS PREFERIDOS: (S)-3-(4-(1-(5-FLUOROPIRIDIN-2-IL)ETILAMINO)PIRIMIDIN-2-ILAMINO)PIRIDIN-2(1H)-ONA; (R)-3-OXO-3-(3-(2-(2-OXO-1,2-DIHIDROPIRIDIN-3-ILAMINO)PIRIMIDIN-4-ILAMINO)PIPERIDIN-1-IL)PROPANONITRILO; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UNA COMBINACION. DICHOS COMPUESTO SON UTILES PARA EL TRATAMIENTO DE ARTRITIS REUMATOIDES, ESCLEROSIS MULTIPLE, ASMA, PSORIASIS, DERMATITIS ATOPICA
PE2014000084A 2011-08-01 2012-07-23 Derivados de piridin-2(1h)-ona como inhibidores de jak PE20141409A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11382263A EP2554544A1 (en) 2011-08-01 2011-08-01 Pyridin-2(1h)-one derivatives as jak inhibitors
US201161556948P 2011-11-08 2011-11-08

Publications (1)

Publication Number Publication Date
PE20141409A1 true PE20141409A1 (es) 2014-10-01

Family

ID=44512745

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2014000084A PE20141409A1 (es) 2011-08-01 2012-07-23 Derivados de piridin-2(1h)-ona como inhibidores de jak

Country Status (20)

Country Link
US (1) US9034311B2 (es)
EP (2) EP2554544A1 (es)
JP (1) JP2014521673A (es)
KR (1) KR20140044865A (es)
CN (1) CN103702991A (es)
AR (1) AR087355A1 (es)
AU (1) AU2012292276A1 (es)
BR (1) BR112014002245A2 (es)
CA (1) CA2839805A1 (es)
CL (1) CL2014000203A1 (es)
CO (1) CO6852079A2 (es)
CR (1) CR20140031A (es)
EA (1) EA201400182A1 (es)
GT (1) GT201400017A (es)
MX (1) MX2014000635A (es)
PE (1) PE20141409A1 (es)
PH (1) PH12014500103A1 (es)
UY (1) UY34212A (es)
WO (1) WO2013017461A1 (es)
ZA (1) ZA201309187B (es)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY33213A (es) 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
EP2463289A1 (en) 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
SG11201700777VA (en) 2014-08-04 2017-02-27 Nuevolution As Optionally fused heterocyclyl-substituted derivatives of pyrimidine useful for the treatment of inflammatory, metabolic, oncologic and autoimmune diseases
US10059689B2 (en) * 2014-10-14 2018-08-28 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
KR101778004B1 (ko) * 2015-06-22 2017-09-15 (주) 에빅스젠 이마티닙을 유효성분으로 포함하는 안구 건조 질환 예방 및 치료용 약학 조성물
EA202092442A3 (ru) 2016-06-07 2021-08-31 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
EP4190318A1 (en) * 2016-12-14 2023-06-07 Biora Therapeutics, Inc. Treatment of a disease of the gastrointestinal tract with a jak inhibitor and devices
KR102317480B1 (ko) 2017-03-23 2021-10-25 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체
US11344549B2 (en) 2017-09-21 2022-05-31 Beijing Scitech-Mq Pharmaceuticals Limited 2-substituted pyrazole amino-4-substituted amino-5-pyrimidine formamide compound, composition, and application thereof
ES2925450T3 (es) 2017-11-06 2022-10-18 Bristol Myers Squibb Co Compuestos de isofuranona útiles como inhibidores de HPK1
CN110372664A (zh) * 2018-04-13 2019-10-25 华东理工大学 选择性jak2抑制剂及其应用
EP3846793B1 (en) 2018-09-07 2024-01-24 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
WO2020063760A1 (en) 2018-09-26 2020-04-02 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
KR20220088699A (ko) 2019-09-27 2022-06-28 디스크 메디슨, 인크. 골수섬유증 및 관련 상태의 치료 방법
EP4076657A1 (en) 2019-12-20 2022-10-26 Nuevolution A/S Compounds active towards nuclear receptors
EP4076661A1 (en) 2019-12-20 2022-10-26 Nuevolution A/S Compounds active towards nuclear receptors
BR112022017727A2 (pt) 2020-03-03 2022-11-16 Pic Therapeutics Inc Inibidores de eif4e e usos dos mesmos
EP4126875A1 (en) 2020-03-31 2023-02-08 Nuevolution A/S Compounds active towards nuclear receptors
WO2021198955A1 (en) 2020-03-31 2021-10-07 Nuevolution A/S Compounds active towards nuclear receptors
KR20230012539A (ko) 2020-05-13 2023-01-26 디스크 메디슨, 인크. 골수섬유증을 치료하기 위한 항-헤모주벨린 (hjv) 항체
EP4392421A1 (en) 2021-08-25 2024-07-03 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
JP2024534127A (ja) 2021-08-25 2024-09-18 ピク セラピューティクス， インコーポレイテッド ｅＩＦ４Ｅ阻害剤及びその使用
KR102503968B1 (ko) 2022-09-22 2023-02-28 이진석 실꼬리 절단장치 및 그를 구비하는 양말 편직기

Family Cites Families (80)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS54128591A (en) 1978-03-25 1979-10-05 Kyowa Hakko Kogyo Co Ltd Cephalosporin analog
IT7920688U1 (it) 1979-02-05 1980-08-05 Chiesi Paolo Inalatore per sostanze medicamentose pulverulente, con combinata funzione di dosatore
DE3274065D1 (de) 1981-07-08 1986-12-11 Draco Ab Powder inhalator
US4570630A (en) 1983-08-03 1986-02-18 Miles Laboratories, Inc. Medicament inhalation device
FI69963C (fi) 1984-10-04 1986-09-12 Orion Yhtymae Oy Doseringsanordning
DE3927170A1 (de) 1989-08-17 1991-02-21 Boehringer Ingelheim Kg Inhalator
IT1237118B (it) 1989-10-27 1993-05-18 Miat Spa Inalatore multidose per farmaci in polvere.
US5201308A (en) 1990-02-14 1993-04-13 Newhouse Michael T Powder inhaler
GB9004781D0 (en) 1990-03-02 1990-04-25 Glaxo Group Ltd Device
SG45171A1 (en) 1990-03-21 1998-01-16 Boehringer Ingelheim Int Atomising devices and methods
GB9015522D0 (en) 1990-07-13 1990-08-29 Braithwaite Philip W Inhaler
WO1992003175A1 (en) 1990-08-11 1992-03-05 Fisons Plc Inhalation device
DE4027391A1 (de) 1990-08-30 1992-03-12 Boehringer Ingelheim Kg Treibgasfreies inhalationsgeraet
ATE209938T1 (de) 1990-09-26 2001-12-15 Pharmachemie Bv Wirbelkammer-pulverinhalator
GB9026025D0 (en) 1990-11-29 1991-01-16 Boehringer Ingelheim Kg Inhalation device
AU650953B2 (en) 1991-03-21 1994-07-07 Novartis Ag Inhaler
DE4239402A1 (de) 1992-11-24 1994-05-26 Bayer Ag Pulverinhalator
UA27961C2 (uk) 1992-12-18 2000-10-16 Шерінг Корпорейшн Інгалятор для порошкових ліків
EP1908488A3 (en) 1995-04-14 2008-04-16 SmithKline Beecham Corporation Metered dose inhaler for salmeterol
AU719449B2 (en) 1995-06-21 2000-05-11 Astrazeneca Ab Pharmaceutical powder cartridge with integrated metering device and inhaler for powdered medicaments
GB9518953D0 (en) 1995-09-15 1995-11-15 Pfizer Ltd Pharmaceutical formulations
DE19536902A1 (de) 1995-10-04 1997-04-10 Boehringer Ingelheim Int Vorrichtung zur Hochdruckerzeugung in einem Fluid in Miniaturausführung
WO2000035298A1 (en) 1996-11-27 2000-06-22 Wm. Wrigley Jr. Company Chewing gum containing medicament active agents
GB9919778D0 (en) 1999-08-21 1999-10-27 Zeneca Ltd Chemical compounds
PE20020506A1 (es) 2000-08-22 2002-07-09 Glaxo Group Ltd Derivados de pirazol fusionados como inhibidores de la proteina cinasa
EP1382603B1 (en) 2001-04-26 2008-07-23 Eisai R&D Management Co., Ltd. Nitrogenous fused-ring compound having pyrazolyl group as substituent and medicinal composition thereof
DE10129703A1 (de) 2001-06-22 2003-01-02 Sofotec Gmbh & Co Kg Zerstäubungssystem für eine Pulvermischung und Verfahren für Trockenpulverinhalatoren
WO2003000682A1 (en) 2001-06-25 2003-01-03 Merck & Co., Inc. (pyrimidyl)(phenyl)substituted fused heteroaryl p38 inhibiting and pkg kinase inhibiting compounds
EP1503757B1 (en) 2002-05-02 2007-12-19 Merck & Co., Inc. Tyrosine kinase inhibitors
ES2195785B1 (es) 2002-05-16 2005-03-16 Almirall Prodesfarma, S.A. Nuevos derivados de piridazin-3(2h)-ona.
GB0216383D0 (en) 2002-07-13 2002-08-21 Astrazeneca Ab Compounds
ES2211344B1 (es) 2002-12-26 2005-10-01 Almirall Prodesfarma, S.A. Nuevos derivados de piridazin-3(2h)-ona.
ES2232306B1 (es) 2003-11-10 2006-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de piridazin-3(2h)-ona.
WO2005095400A1 (en) 2004-03-30 2005-10-13 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of jak and other protein kinases
ES2251866B1 (es) 2004-06-18 2007-06-16 Laboratorios Almirall S.A. Nuevos derivados de piridazin-3(2h)-ona.
ES2251867B1 (es) 2004-06-21 2007-06-16 Laboratorios Almirall S.A. Nuevos derivados de piridazin-3(2h)-ona.
UA93031C2 (uk) 2004-07-16 2011-01-10 Алміралл, С.А. Інгалятор для порошкових медикаментів, фармацевтичний порошковий картридж для використання з інгалятором та спосіб використання інгалятора
WO2006038001A1 (en) 2004-10-06 2006-04-13 Celltech R & D Limited Aminopyrimidine derivatives as jnk inhibitors
DE602005014382D1 (de) 2004-12-21 2009-06-18 Smithkline Beecham Corp 2-pyrimidinyl-pyrazolopyridin-erbb-kinaseinhibitoren
AU2006248780B2 (en) 2005-05-16 2010-06-03 Astrazeneca Ab Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors
ES2265276B1 (es) 2005-05-20 2008-02-01 Laboratorios Almirall S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico.
WO2007049041A1 (en) * 2005-10-28 2007-05-03 Astrazeneca Ab 4- (3-aminopyrazole) pyrimidine derivatives for use as tyrosine kinase inhibitors in the treatment of cancer
ES2296516B1 (es) 2006-04-27 2009-04-01 Laboratorios Almirall S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico.
BRPI0712381A2 (pt) 2006-06-06 2012-07-10 Avigen Inc compostos de pirazolo[1,5-a]piridina substituìda e seus métodos de uso
AR063142A1 (es) 2006-10-04 2008-12-30 Pharmacopeia Inc Derivados de 2-(bencimidazolil) purina y purinonas 6-sustituidas utiles como inmunosupresores,y composiciones farmaceuticas que los contienen.
AU2007307031B2 (en) 2006-10-11 2011-11-24 Amgen Inc. Imidazo- and triazolo-pyridine compounds and methods of use therof
ES2302447B1 (es) 2006-10-20 2009-06-12 Laboratorios Almirall S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico.
JP5512274B2 (ja) * 2006-10-23 2014-06-04 セファロン、インク． ＡＬＫ阻害剤およびｃ−ＭＥＴ阻害剤としての２，４−ジアミノピリミジンの縮合二環式誘導体
HRP20151398T1 (hr) 2006-12-22 2016-02-12 Astex Therapeutics Limited Tricikliäśni derivati amina kao inhibitori protein tirozin kinaze
ES2319596B1 (es) 2006-12-22 2010-02-08 Laboratorios Almirall S.A. Nuevos derivados de los acidos amino-nicotinico y amino-isonicotinico.
US7977336B2 (en) 2006-12-28 2011-07-12 Banyu Pharmaceutical Co. Ltd Aminopyrimidine derivatives as PLK1 inhibitors
ES2306595B1 (es) 2007-02-09 2009-09-11 Laboratorios Almirall S.A. Sal de napadisilato de 5-(2-((6-(2,2-difluoro-2-feniletoxi)hexil)amino)-1-hidroxietil)-8-hidroxiquinolin-2(1h)-ona como agonista del receptor adrenergico beta2.
US7834024B2 (en) * 2007-03-26 2010-11-16 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
UY31048A1 (es) * 2007-04-25 2008-11-28 Astrazeneca Ab Nuevos compuestos de pirimidina y usos de los mismos
ATE521609T1 (de) * 2007-05-04 2011-09-15 Astrazeneca Ab Aminothiazolylpyrimidinderivate und ihre verwendung bei der behandlung von krebs
UY31272A1 (es) 2007-08-10 2009-01-30 Almirall Lab Nuevos derivados de ácido azabifenilaminobenzoico
WO2009021990A1 (en) 2007-08-14 2009-02-19 Bayer Schering Pharma Aktiengesellschaft Fused imidazoles for cancer treatment
CN101842011A (zh) 2007-08-17 2010-09-22 安克进药物公司 作为钾通道调节剂的杂环
WO2009027736A2 (en) * 2007-08-27 2009-03-05 Astrazeneca Ab 2,4 diaminopyrimid'lnes for the treatment of myeloproliferative disorders and cancer
MX2010004244A (es) 2007-10-17 2010-04-30 Novartis Ag Derivados de imidazo [i,2-a]-piridina utiles como inhibidores de cinasa tipo activina (alk).
WO2009054941A1 (en) 2007-10-25 2009-04-30 Merck & Co., Inc. Therapeutic compounds
ES2320961B1 (es) 2007-11-28 2010-03-17 Laboratorios Almirall, S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor adrenergico beta2.
NZ586662A (en) 2007-12-19 2012-08-31 Vertex Pharma PYRAZOLO[1,5-a]PYRIMIDINES USEFUL AS JANUS KINASE 2 INHIBITORS
CA2710452A1 (en) 2007-12-21 2009-07-09 Wyeth Llc Imidazo [1,2-a] pyridine compounds
CN101939324B (zh) 2008-02-25 2014-10-15 霍夫曼-拉罗奇有限公司 吡咯并吡嗪激酶抑制剂
US8258144B2 (en) 2008-04-22 2012-09-04 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
UY31929A (es) * 2008-06-25 2010-01-05 Irm Llc Compuestos y composiciones como inhibidores de cinasa
CA2731368C (en) 2008-08-06 2013-05-14 Pfizer Inc. 6 substituted 2-heterocyclylamino pyrazine compounds as chk-1 inhibitors
UY32055A (es) * 2008-08-19 2010-03-26 Astrazeneca Ab Derivados sustituidos de la 5-Halo-N2-[sustituido](1-metil-1H-imidazol-4-il)pirimidin-2,-diamina y sus sales farmacéuticamente aceptables, procesos de preparación, composiciones y aplicaciones.
EP2196465A1 (en) 2008-12-15 2010-06-16 Almirall, S.A. (3-oxo)pyridazin-4-ylurea derivatives as PDE4 inhibitors
UY32297A (es) 2008-12-22 2010-05-31 Almirall Sa Sal mesilato de 5-(2-{[6-(2,2-difluoro-2-fenilitoxi) hexil]amino}-1-hidroxietil)-8-hidroxiquinolin-2( 1h)-ona como agonista del receptor b(beta)2 acrenérgico
AR074870A1 (es) 2008-12-24 2011-02-16 Palau Pharma Sa Derivados de pirazolo (1,5-a ) piridina
HRP20151325T1 (hr) * 2009-01-23 2016-01-01 Rigel Pharmaceuticals, Inc. Pripravci i postupci za inhibiciju jak puta
RU2535217C2 (ru) * 2009-02-06 2014-12-10 Ниппон Синяку Ко., Лтд. Производные аминопиразина и лекарственные средства
BR112012010186B8 (pt) 2009-10-29 2021-05-25 Palau Pharma Sa derivados de heteroarila contendo n como inibidores de quinase jak3 e composição farmacêutica compreendendo os mesmos
EP2338888A1 (en) 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
UY33213A (es) 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
EP2397482A1 (en) 2010-06-15 2011-12-21 Almirall, S.A. Heteroaryl imidazolone derivatives as jak inhibitors
EP2463289A1 (en) 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
EP2527344A1 (en) 2011-05-25 2012-11-28 Almirall, S.A. Pyridin-2(1H)-one derivatives useful as medicaments for the treatment of myeloproliferative disorders, transplant rejection, immune-mediated and inflammatory diseases

Also Published As

Publication number Publication date
CL2014000203A1 (es) 2014-07-11
JP2014521673A (ja) 2014-08-28
KR20140044865A (ko) 2014-04-15
WO2013017461A1 (en) 2013-02-07
MX2014000635A (es) 2014-04-30
EP2554544A1 (en) 2013-02-06
EP2739616A1 (en) 2014-06-11
CA2839805A1 (en) 2013-02-07
AR087355A1 (es) 2014-03-19
CR20140031A (es) 2014-05-13
EA201400182A1 (ru) 2014-06-30
BR112014002245A2 (pt) 2017-03-07
US9034311B2 (en) 2015-05-19
ZA201309187B (en) 2014-08-27
UY34212A (es) 2013-02-28
GT201400017A (es) 2015-07-13
AU2012292276A1 (en) 2014-02-20
PH12014500103A1 (en) 2019-03-22
CN103702991A (zh) 2014-04-02
NZ618904A (en) 2015-06-26
US20140271543A1 (en) 2014-09-18
CO6852079A2 (es) 2014-01-30

Similar Documents

Publication Publication Date Title
PE20141409A1 (es) Derivados de piridin-2(1h)-ona como inhibidores de jak
PE20130311A1 (es) Composiciones y metodos para modular la via de senalizacion de wnt
ECSP11010830A (es) Derivados de heteroarilo como inhibidores de dgat1
PE20141010A1 (es) Derivados de piridin-2(1h)-ona utiles como medicamentos para el tratamiento de transtornos mieloproliferativos, rechazo de transplantes, enfermedades mediadas por el sistema inmune y enfermedades inflamatorias
PE20141996A1 (es) Compuestos con actividad nematicida
PE20141120A1 (es) Compuestos heterociclicos
PE20120690A1 (es) Derivados de 5-fluoropirimidinona
PE20140832A1 (es) Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
PE20131343A1 (es) Derivados de acido benzoico
PE20130188A1 (es) Pirrolidinonas heteroaromaticas fusionadas como inhibidores de syk
PE20181015A1 (es) 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
PE20141167A1 (es) Piridopirazinas sustituidas como inhibidores novedosos de ptk
PH12013501197B1 (en) Indeno-fused ring compounds
PE20131197A1 (es) Compuestos de pirazolopirimidina como inhibidores de jak y composiciones farmaceuticas que los contienen
PH12014502866A1 (en) Fungicidal heterocyclic carboxamides
PE20170946A1 (es) 2-amino-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
AR091285A1 (es) Inhibidores de bromodominio y sus usos
PE20090775A1 (es) Nuevos derivados de biarilo
PE20161444A1 (es) 1,2-ciclopentanos sustituidos como antagonistas del receptor de orexina
PE20131143A1 (es) Nuevas aminopirazoloquinazolinas
PE20080068A1 (es) Compuestos derivados de pirimidina como inhibidores de la quinasa aurora
PE20120937A1 (es) Compuestos derivados de quinolina y quinoxalina como agentes antivirales
PE20141691A1 (es) Compuestos con actividad nematicida
PE20170947A1 (es) 2-amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de bace1
PH12013501196B1 (en) Indeno- fused ring compounds having photochromic properties

Legal Events

Date Code Title Description
FD Application declared void or lapsed