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

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19Cytokines; Lymphokines; Interferons
    • A61K38/21Interferons [IFN]
    • A61K38/212IFN-alpha
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19Cytokines; Lymphokines; Interferons
    • A61K38/21Interferons [IFN]
    • A61K38/215IFN-beta
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)
  • Otolaryngology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (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 (19)

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)
UY (1) UY34212A (es)
WO (1) WO2013017461A1 (es)
ZA (1) ZA201309187B (es)

Families Citing this family (14)

* 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
BR112017002214B1 (pt) 2014-08-04 2023-03-07 Nuevolution A/S Composto de fórmula (i), e uso de um composto
EP3206691B1 (en) * 2014-10-14 2018-09-19 Sunshine Lake Pharma Co., Ltd. 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
CA3026784A1 (en) 2016-06-07 2017-12-14 Jacobio Pharmaceuticals Co., Ltd. Heterocyclic pyrazine derivatives useful as shp2 inhibitors
EP3601239A4 (en) 2017-03-23 2020-05-13 Jacobio Pharmaceuticals Co., Ltd. INNOVATIVE HETEROCYCLIC DERIVATIVES USEFUL AS SHP2 INHIBITORS
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
US11166959B2 (en) 2017-11-06 2021-11-09 Bristol-Myers Squibb Company Isofuranone compounds useful as HPK1 inhibitors
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
AU2020405446A1 (en) 2019-12-20 2022-05-26 Nuevolution A/S Compounds active towards nuclear receptors
MX2022012260A (es) 2020-03-31 2022-11-30 Nuevolution As Compuestos activos frente a receptores nucleares.
WO2021198956A1 (en) 2020-03-31 2021-10-07 Nuevolution A/S Compounds active towards nuclear receptors
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
IT7920688V0 (it) 1979-02-05 1979-02-05 Chiesi Paolo Parma 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
DE69132850T2 (de) 1990-09-26 2002-05-29 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
WO1994014492A2 (en) 1992-12-18 1994-07-07 Schering Corporation Inhaler for powdered medications
RO119116B1 (ro) 1995-04-14 2004-04-30 Glaxo Wellcome Inc. Inhalator pentru dozarea salmeterolului
NZ502870A (en) 1995-06-21 2001-06-29 Asta Medica Ag Inhaler for powdered medicaments comprising a visual display device to indicate the discharge status of the inhaler
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
WO2000035296A1 (en) 1996-11-27 2000-06-22 Wm. Wrigley Jr. Company Improved release of medicament active agents from a chewing gum coating
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
WO2002088107A1 (en) 2001-04-26 2002-11-07 Eisai 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
US7125888B2 (en) 2002-05-02 2006-10-24 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.
TWI465437B (zh) 2004-03-30 2014-12-21 Vertex Pharma 適合作為jak及其它蛋白質激酶抑制劑之氮雜吲哚
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.
DE602005023690D1 (de) 2004-07-16 2010-11-04 Almirall Sa Inhalator für die Abgabe von pharmzeutischen Pulver, und ein Pulverkassette zur Verwendung mit diesem Inhalator
WO2006038001A1 (en) 2004-10-06 2006-04-13 Celltech R & D Limited Aminopyrimidine derivatives as jnk inhibitors
JP5132319B2 (ja) 2004-12-21 2013-01-30 スミスクライン ビーチャム コーポレーション 2−ピリミジニルピラゾロピリジンErbBキナーゼ阻害剤
KR20080015409A (ko) 2005-05-16 2008-02-19 아스트라제네카 아베 티로신 키나제 억제제로서 유용한 피라졸릴아미노피리미딘 유도체
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.
JP2009513615A (ja) * 2005-10-28 2009-04-02 アストラゼネカ アクチボラグ 癌の治療においてチロシンキナーゼ阻害剤として使用するための4−(3−アミノピラゾール)ピリミジン誘導体
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.
WO2007146087A2 (en) 2006-06-06 2007-12-21 Avigen, Inc. SUBSTITUTED PYRAZOLO [1,5-α] PYRIDINE COMPOUNDS AND THEIR METHODS OF USE
WO2008043031A1 (en) 2006-10-04 2008-04-10 Pharmacopeia, Inc. 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
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.
CL2007003049A1 (es) * 2006-10-23 2008-05-16 Cephalon Inc Pharmacopeia Drug Compuestos derivados de 2,4-diaminopirimidina; composicion farmaceutica, utiles para tratar trastornos proliferativos.
ES2319596B1 (es) 2006-12-22 2010-02-08 Laboratorios Almirall S.A. Nuevos derivados de los acidos amino-nicotinico y amino-isonicotinico.
PL2121687T3 (pl) 2006-12-22 2016-03-31 Astex Therapeutics Ltd Pochodne amin tricyklicznych jako inhibitory białkowej kinazy tyrozynowej
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.
WO2008118823A2 (en) * 2007-03-26 2008-10-02 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
CN101687863B (zh) * 2007-05-04 2012-09-12 阿斯利康(瑞典)有限公司 氨基-噻唑基-嘧啶衍生物及其治疗癌症的用途
UY31272A1 (es) 2007-08-10 2009-01-30 Almirall Lab Nuevos derivados de ácido azabifenilaminobenzoico
CL2008002397A1 (es) 2007-08-14 2009-09-25 Bayer Schering Pharma Ag Compuestos derivados de imidazoles biciclicos fusionados; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar neoplasia benigna o maligna.
JP5463287B2 (ja) 2007-08-17 2014-04-09 アイカジェン, インコーポレイテッド カリウムチャネル調節物質としての複素環
WO2009027736A2 (en) * 2007-08-27 2009-03-05 Astrazeneca Ab 2,4 diaminopyrimid'lnes for the treatment of myeloproliferative disorders and cancer
EA201000615A1 (ru) 2007-10-17 2010-12-30 Новартис Аг Производные имидазо[1,2-а]пиридина, применимые в качестве ингибиторов апк (активиноподобной киназы)
JP2011500806A (ja) 2007-10-25 2011-01-06 メルク・シャープ・エンド・ドーム・コーポレイション 治療用化合物
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.
CN101932583A (zh) 2007-12-19 2010-12-29 沃泰克斯药物股份有限公司 用作JAK2抑制剂的吡唑并[1,5-a]嘧啶类
JP2011507900A (ja) 2007-12-21 2011-03-10 ワイス・エルエルシー イミダゾ[1,2−a]ピリジン化合物
DK2247592T3 (da) 2008-02-25 2011-09-26 Hoffmann La Roche Pyrrolopyrazinkinaseinhibitors
AU2009238590A1 (en) 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
UY31929A (es) * 2008-06-25 2010-01-05 Irm Llc Compuestos y composiciones como inhibidores de cinasa
ES2378513T3 (es) 2008-08-06 2012-04-13 Pfizer Inc. Compuestos 2-heterociclilamino piracinas sustituidas en posición 6 como inhibidores de CHK-1
TW201011017A (en) * 2008-08-19 2010-03-16 Astrazeneca Ab Chemical compounds 495-1
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
EP2565193B1 (en) * 2009-01-23 2014-03-19 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
JP5263304B2 (ja) * 2009-02-06 2013-08-14 日本新薬株式会社 アミノピラジン誘導体及び医薬
RU2553681C2 (ru) 2009-10-29 2015-06-20 Вектура Лимитед N-содержащие гетероарильные производные в качестве ингибиторов jak3 киназы
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
EA201400182A1 (ru) 2014-06-30
ZA201309187B (en) 2014-08-27
CL2014000203A1 (es) 2014-07-11
US9034311B2 (en) 2015-05-19
US20140271543A1 (en) 2014-09-18
CA2839805A1 (en) 2013-02-07
EP2739616A1 (en) 2014-06-11
CO6852079A2 (es) 2014-01-30
KR20140044865A (ko) 2014-04-15
JP2014521673A (ja) 2014-08-28
NZ618904A (en) 2015-06-26
WO2013017461A1 (en) 2013-02-07
CR20140031A (es) 2014-05-13
UY34212A (es) 2013-02-28
BR112014002245A2 (pt) 2017-03-07
AR087355A1 (es) 2014-03-19
AU2012292276A1 (en) 2014-02-20
MX2014000635A (es) 2014-04-30
EP2554544A1 (en) 2013-02-06
GT201400017A (es) 2015-07-13
CN103702991A (zh) 2014-04-02

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
PE20141996A1 (es) Compuestos con actividad nematicida
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
ECSP11010830A (es) Derivados de heteroarilo como inhibidores de dgat1
PE20181015A1 (es) 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
PE20141120A1 (es) Compuestos heterociclicos
PE20120690A1 (es) Derivados de 5-fluoropirimidinona
PE20131343A1 (es) Derivados de acido benzoico
PE20120135A1 (es) Piperidinas sustituidas como antagonistas de ccr3
PE20170946A1 (es) 2-amino-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
PE20130188A1 (es) Pirrolidinonas heteroaromaticas fusionadas como inhibidores de syk
PH12014502866A1 (en) Fungicidal heterocyclic carboxamides
PE20131197A1 (es) Compuestos de pirazolopirimidina como inhibidores de jak y composiciones farmaceuticas que los contienen
PE20141167A1 (es) Piridopirazinas sustituidas como inhibidores novedosos de ptk
AR091285A1 (es) Inhibidores de bromodominio y sus usos
PE20170947A1 (es) 2-amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de bace1
PE20080068A1 (es) Compuestos derivados de pirimidina como inhibidores de la quinasa aurora
PE20131143A1 (es) Nuevas aminopirazoloquinazolinas
PE20120552A1 (es) Combinaciones que comprenden metotrexato e inhibidores de dhodh
PE20141691A1 (es) Compuestos con actividad nematicida
PE20161368A1 (es) Inhibidores de diacilglicerol aciltranferasa 2
PE20120937A1 (es) Compuestos derivados de quinolina y quinoxalina como agentes antivirales
MX346746B (es) Compuestos de anillo indeno-fusionados.
PE20161444A1 (es) 1,2-ciclopentanos sustituidos como antagonistas del receptor de orexina

Legal Events

Date Code Title Description
FD Application declared void or lapsed