ES2569539T3 - Derivados de piperidin-4-il azetidina como inhibidores de JAK1 - Google Patents
Derivados de piperidin-4-il azetidina como inhibidores de JAK1 Download PDFInfo
- Publication number
- ES2569539T3 ES2569539T3 ES11711709T ES11711709T ES2569539T3 ES 2569539 T3 ES2569539 T3 ES 2569539T3 ES 11711709 T ES11711709 T ES 11711709T ES 11711709 T ES11711709 T ES 11711709T ES 2569539 T3 ES2569539 T3 ES 2569539T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- cycloalkyl
- heteroaryl
- heterocycloalkyl
- aryl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- DDOFLXMWWKLMSZ-UHFFFAOYSA-N 4-(azetidin-1-yl)piperidine Chemical class C1CCN1C1CCNCC1 DDOFLXMWWKLMSZ-UHFFFAOYSA-N 0.000 title 1
- 229940116839 Janus kinase 1 inhibitor Drugs 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 30
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 16
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 12
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 12
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 12
- 125000005115 alkyl carbamoyl group Chemical group 0.000 abstract 12
- 125000001072 heteroaryl group Chemical group 0.000 abstract 12
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 12
- -1 cyano, amino Chemical group 0.000 abstract 9
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 8
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 7
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 7
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 7
- 125000005843 halogen group Chemical group 0.000 abstract 7
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 6
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 abstract 6
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 6
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 6
- 229910052799 carbon Inorganic materials 0.000 abstract 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 5
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 4
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 4
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 4
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 abstract 3
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 3
- 125000000446 sulfanediyl group Chemical group *S* 0.000 abstract 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 125000004750 (C1-C6) alkylaminosulfonyl group Chemical group 0.000 abstract 2
- 125000005915 C6-C14 aryl group Chemical group 0.000 abstract 2
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 2
- 150000001721 carbon Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000005311 halosulfanyl group Chemical group 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 abstract 1
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 abstract 1
- 102100038417 Cytoplasmic FMR1-interacting protein 1 Human genes 0.000 abstract 1
- 101710181791 Cytoplasmic FMR1-interacting protein 1 Proteins 0.000 abstract 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000011737 fluorine Chemical group 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
- A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
-
- 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
- A61P11/06—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
- A61P17/04—Antipruritics
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- 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
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Physics & Mathematics (AREA)
- Condensed Matter Physics & Semiconductors (AREA)
- Crystallography & Structural Chemistry (AREA)
- General Physics & Mathematics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
un compuesto de la Fórmula (I):**Fórmula** o una sal del mismo farmacéuticamente aceptable; donde: X es N o CR2; Y es N o CR3; Z es H, ciano, halo, C1-3 alquilo o C1-3 haloalquilo; L es C(R4)2, C(>=O), C(>=O)N(R4a),C(>=O)C(R4b)2, S(>=O)2, C(>=O)O, C(>=O)OC(R4b)2 O C(>=O)N(R4a)C(R4b)2); A es C1-6 alquilo, C3-14 cicloalquilo, C2-13 heterocicloalquilo, C6-14 arilo o C1-14 heteroarilo; donde dicho C1-6 alquilo, C3-14 cicloalquilo, C2-13 heterocicloalquilo, C6-14 arilo y C1-14 heteroarilo se sustituyen individualmente y opcionalmente por 1, 2, 3, 4, 5 o 6 grupos R5 independientemente seleccionados; o cada R1 es, independientemente C1-4 alquilo, hidroxilo, C1-4 alcoxi, flúor, hidroxil- C1-4 alquilo o C1-4 alcoxi- C1-4 alquilo; dos grupos R1 juntos forman un puente de 2- 3-carbonos o un puente de fórmula -CH2-O-CH2; R2 es H, halo, hidroxilo, ciano, C1-4 alquilo, C1-4 haloalcoxi o C1-4 alcoxi; R3 es H, ciano, amino, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C3-7 cicloalquilo, C1-6 haloalquilo, C1-6 alcoxi, C1-6 haloalcoxi, amino, C1-6 alquilamino, di-C1-6-alquilamino, C1-6 alquilsulfonilo, carbamilo, C1-6 alquilcarbamilo, di-C1-6 alquilcarbamilo, caboxi, C1-6 alquilcabonilo o C1-6 alcoxicarbonilo; cada R4 es independientemente H o C1-4 alquilo; o dos grupos R4 juntos con el átomo de carbono al que están unidos forman un anillo cicloaqluilo con 3, 4, 5 o 6 miembros; R4a es H o C1-4 alquilo; cada R4b es, independientemente, H o C1-4 alquilo; o dos grupos R4b, junto con el átomo de carbono al que están unidos, forma un anillo cicloaquilo con 3, 4, 5 o 6 miembros; cada R5 es, independientemente, halo, ciano, nitro, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C1-6 haloalquilo, halosulfanilo, C3-10 cicloalquilo, C3-10 cicloalquilo-C1-3 alquilo, C2-10 heterocicloalquilo, C2-10 heteroarilo-C1-3 alquilo, C6-10 arilo, C6-10 arilo-C3-10 alquilo, C1-10 heteroarilo, C1-10 heteroarilo-C1-3 alquilo, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, C(>=NRe)Rb, C(>=NRe)NRcRd, NRcC(>=NRe)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rd, S(O)2Rd, S(O)2Rb o S(O)2NRcRd; donde C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C1-6 haloalquilo, C3-10 ciclooalquilo, C3-10 cicloalquilo-C1-3 alquilo, C2-10 heterocicloalquilo,C2-10 heterocicloalquilo- C1-3 alquilo, C6-10 arilo, C6-10 arilo-C1-3 alquilo, C1-10 heteroarilo, y C1-10 heteroarilo-C1-3 alquilo se sustituyen individualmente y opcionalmente por 1, 2, 3, 4 ó 5 grupos R6 independientemente seleccionados; cada R6 es, independientemente, halo, ciano, nitro, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C1-6 haloalquilo, halosulfanilo, C3-10 cicloalquilo, C3-10 cicloalquilo-C1-3 alquilo, C2-10 heterocicloalquilo, C2-10 heterocicloalquilo- C1-3 alquilo, C6-10 arilo, C6-10 arilo-C1-3 alquilo, C1-10 heteroarilo, C1-10 heteroarilo-C1-3 alquilo, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(>=NRe1)NRe1Rd1, NRc1C(>=NRe1)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, o S(O)2NRc1Rd1; donde dicho C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C1-6 haloalquilo, C3-10 cicloalquilo, C3-10 cicloalquilo-C1-3 alquilo, C2-10 heterocicloalquilo, C2-10 heterocicloalquilo-C1-3 alquilo, C6-10 arilo, C6-10 arilo-C1-3 alquilo, C1-10 heteroarilo y C1-10 heteroarilo-C1-3 alquilo se sustituyen individualmente y opcionalmente por 1, 2, 3, 4 ó 5 grupos Rh independientemente seleccionados; cada Ra, Rb, Rc y Rd es, independientemente, H, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C1-6 haloalquilo, C3- 10 cicloalquilo, C3-10 cicloalquilo-C1-3 alquilo, C2-10 heterocicloalquilo, C2-10 heterocicloalquilo-C1-3 alquilo, C6-10 arilo, C6-10 arilo-C1-3 alquilo, C1-10 heteroarilo, o C1-10 heteroarilo-C1-3 alquilo; donde dicho C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C1-6 haloalquilo, C3-10 cicloalquilo, C3-10 cicloalquilo-C1-3 alquilo, C2-10 heterocicloalquilo, C2-10 heterocicloalquilo-C1-3 alquilo, C6-10 arilo, C6-10 arilo-C1-3 alquilo, C1-10 heteroarilo, y C1-10 heteroarilo-C1-3 alquilo se sustituye individualmente y opcionalmente por 1, 2, 3, 4 ó 5 grupos Rg independientemente seleccionados; o cualquier Rc and Rd junto con el átomo N al que están unidos forman un grupo heterocicloalquilo o un grupo heteroarilo de 3, 4, 5, 6 ó 7 miembros, cada uno opcionalmente sustituido por 1, 2, 3 ó 4 sustituyentes independientemente seleccionados de halo, ciano, nitro, hidroxilo, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C3- 7 cicloalquilo, C1-6 haloalquilo, C1-6 alcoxi, C1-6 haloalcoxi, amino, C1-6 alquiloamino, di-C1-6 alquiloamino, tio, C1- 6 alquilotio, C1-6 alquilosulfinilo, C1-6 alquilosulfonilo, carbamilo, C1-6 alquilocarbamilo, di-C1-6 alquilocarbamilo, carboxi, C1-6 alquilocarbonilo, y C1-6 alcoxicarbonilo; cada Re es, independientemente, H, C1-6 alquilo, CN, hidroxilo, C1-6 alcoxi, C1-6 alquilosulfonilo, carboxi, C1-6 alquilocarbonilo, aminosulfonilo, C1-6 alquiloaminosulfonilo, di-C1-6 alquiloaminosulfonilo, carbamilo, C1-6 alquilocarbamilo, o di-C1-6 alquilocarbamilo; cada Ra1, Rb1, Rc1, y Rd1 es, independientemente, H, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C1-6 haloalquilo, C3-10 cicloalquilo, C3-10 cicloalquilo-C1-3 alquilo, C2-10 heterocicloalquilo, C2-10 heterocicloalquilo-C1-3 alquilo, C6-10 arilo, C6-10 arilo-C1-3 alquilo, C1-10 heteroarilo, o C1-10 heteroarilo-C1-3 alquilo; donde dicho C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C1-6 haloalquilo, C3-10 cicloalquilo, C3-10 cicloalquilo-C1-3 alquilo, C2-10 heterocicloalquilo, C2-10 heterocicloalquilo-C1-3 alquilo, C6-10 arilo, C6-10 arilo-C1-3 alquilo, C1-10 heteroarilo, y C1-10 heteroarilo-C1-3 alquilo se sustituye individualmente y opcionalmente por 1, 2, 3, 4 ó 5 grupos Rg' independientemente seleccionados; o cualquier Rc1 and Rd1 junto con el átomo N al que están unidos forman un grupo heterocicloalquilo o un grupo heteroarilo de 3, 4, 5, 6 ó 7 miembros, cada uno opcionalmente sustituido por 1, 2, 3 ó 4 sustituyentes independientemente seleccionados de halo, ciano, nitro, hidroxilo, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C3- 7 cicloalquilo, C1-6 haloalquilo, C1-6 alcoxi, C1-6 haloalcoxi, amino, C1-6 alquiloamino, di-C1-6 alquiloamino, tio, C1- 6 alquilotio, C1-6 alquilosulfinilo, C1-6 alquilosulfonilo, carbamilo, C1-6 alquilocarbamilo, di-C1-6 alquilocarbamilo, carboxi, C1-6 alquilocarbonilo, C1-6 alcoxicarbonilo, y C1-6 alquilocarboniloamino; cada Re1 es, independientemente, H, C1-6 alquilo, CN, hidroxilo, C1-6 alcoxi, C1-6 alquilosulfonilo, carboxi, C1-6 alquilocarbonilo, aminosulfonilo, C1-6 alquiloaminosulfonilo, di-C1-6 alquiloaminosulfonilo, carbamilo, C1-6 alquilocarbamilo, o di-C1-6 alquilocarbamilo; each Rg, Rg', y Rh es, independientemente, halo, ciano, nitro, hidroxilo, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C3-7 cicloalquilo, C1-6 haloalquilo, C1-6 alcoxi, C1-6 haloalcoxi, amino, C1-6 alquiloamino, di-C1-6 alquiloamino, tio, C1-6 alquilotio, C1-6 alquilosulfinilo, C1-6 alquilosulfonilo, carbamilo, C1-6 alquilocarbamilo, di- C1-6 alquilocarbamilo, carboxi, C1-6 alquilocarbonilo, C1-6 alcoxicarbonilo, o C1-6 alquilocarboniloamino; y n es 0, 1, 2, 3 ó 4.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US31258810P | 2010-03-10 | 2010-03-10 | |
US312588P | 2010-03-10 | ||
US41560210P | 2010-11-19 | 2010-11-19 | |
US415602P | 2010-11-19 | ||
PCT/US2011/027665 WO2011112662A1 (en) | 2010-03-10 | 2011-03-09 | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
ES2569539T3 true ES2569539T3 (es) | 2016-05-11 |
Family
ID=44065466
Family Applications (4)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES15195698.4T Active ES2662588T3 (es) | 2010-03-10 | 2011-03-09 | Derivados de piperidin-4-IL azetidina como inhibidores de JAK1 |
ES17211097T Active ES2796377T3 (es) | 2010-03-10 | 2011-03-09 | Derivados de piperidin-4-IL azetidina como inhibidores de JAK1 |
ES11711709T Active ES2569539T3 (es) | 2010-03-10 | 2011-03-09 | Derivados de piperidin-4-il azetidina como inhibidores de JAK1 |
ES20158754T Active ES2908412T3 (es) | 2010-03-10 | 2011-03-09 | Derivados de piperidin-4-IL azetidina como inhibidores de JAK1 |
Family Applications Before (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES15195698.4T Active ES2662588T3 (es) | 2010-03-10 | 2011-03-09 | Derivados de piperidin-4-IL azetidina como inhibidores de JAK1 |
ES17211097T Active ES2796377T3 (es) | 2010-03-10 | 2011-03-09 | Derivados de piperidin-4-IL azetidina como inhibidores de JAK1 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES20158754T Active ES2908412T3 (es) | 2010-03-10 | 2011-03-09 | Derivados de piperidin-4-IL azetidina como inhibidores de JAK1 |
Country Status (38)
Country | Link |
---|---|
US (6) | US8765734B2 (es) |
EP (6) | EP2545045B1 (es) |
JP (6) | JP5858484B2 (es) |
KR (7) | KR102283091B1 (es) |
CN (1) | CN102985417B (es) |
AR (1) | AR081315A1 (es) |
AU (1) | AU2011224484A1 (es) |
BR (1) | BR112012022513A2 (es) |
CA (1) | CA2792508C (es) |
CL (1) | CL2012002501A1 (es) |
CO (1) | CO6602158A2 (es) |
CR (1) | CR20120510A (es) |
CY (2) | CY1120154T1 (es) |
DK (3) | DK3050882T3 (es) |
EA (1) | EA030376B1 (es) |
EC (1) | ECSP12012218A (es) |
ES (4) | ES2662588T3 (es) |
HK (2) | HK1177741A1 (es) |
HR (3) | HRP20160326T1 (es) |
HU (3) | HUE049914T2 (es) |
IL (1) | IL221823A (es) |
LT (2) | LT3050882T (es) |
ME (2) | ME02386B (es) |
MX (5) | MX336932B (es) |
MY (2) | MY175156A (es) |
NO (1) | NO3050882T3 (es) |
NZ (1) | NZ602313A (es) |
PE (1) | PE20130038A1 (es) |
PH (1) | PH12015502575A1 (es) |
PL (3) | PL3050882T3 (es) |
PT (2) | PT3354652T (es) |
RS (3) | RS54823B1 (es) |
SG (1) | SG183551A1 (es) |
SI (3) | SI3354652T1 (es) |
SM (1) | SMT201600085B (es) |
TW (5) | TWI592413B (es) |
WO (1) | WO2011112662A1 (es) |
ZA (1) | ZA201207420B (es) |
Families Citing this family (124)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PL2426129T3 (pl) | 2005-12-13 | 2017-04-28 | Incyte Holdings Corporation | Podstawione heteroarylem pirolo[2,3-b]pirydyny i pirolo[2,3-b]pirymidyny jako inhibitory kinazy Janusowej |
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. |
ME00960B (me) | 2007-06-13 | 2012-06-20 | Incyte Corp | Soli inhibitora janus kinaze, (r)-3-(4-(7h-pirol[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropannitrila |
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. |
JOP20190230A1 (ar) | 2009-01-15 | 2017-06-16 | Incyte Corp | طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به |
LT2432472T (lt) * | 2009-05-22 | 2020-02-10 | Incyte Holdings Corporation | 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- arba heptan-nitrilas, kaip jak inhibitoriai |
US8716303B2 (en) | 2009-05-22 | 2014-05-06 | Incyte Corporation | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
EP2845856A1 (en) | 2009-06-29 | 2015-03-11 | Incyte Corporation | Pyrimidinones as PI3K inhibitors |
US9249145B2 (en) | 2009-09-01 | 2016-02-02 | Incyte Holdings Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
PL3050882T3 (pl) * | 2010-03-10 | 2018-08-31 | Incyte Holdings Corporation | Piperydyn-4-ylowe pochodne azetydyny jako inhibitory JAK1 |
BR112012029653B1 (pt) | 2010-05-21 | 2021-01-12 | Incyte Holdings Corporation | formulação farmacêutica para aplicação tópica em pele e seu uso |
CN103415515B (zh) | 2010-11-19 | 2015-08-26 | 因塞特公司 | 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物 |
ES2536415T3 (es) | 2010-11-19 | 2015-05-25 | Incyte Corporation | Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK |
EP3660016A1 (en) | 2010-12-20 | 2020-06-03 | Incyte Holdings Corporation | N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors |
ES2547916T3 (es) | 2011-02-18 | 2015-10-09 | Novartis Pharma Ag | Terapia de combinación de inhibidores de mTOR/JAK |
CA2839767A1 (en) | 2011-06-20 | 2012-12-27 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
EP2741747A1 (en) | 2011-08-10 | 2014-06-18 | 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 |
SG11201400232WA (en) | 2011-09-02 | 2014-03-28 | Incyte Corp | Heterocyclylamines as pi3k inhibitors |
UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
AU2012312303B2 (en) * | 2011-09-22 | 2016-09-15 | Merck Sharp & Dohme Corp. | Cyanomethylpyrazole carboxamides as janus kinase inhibitors |
AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
US9193733B2 (en) | 2012-05-18 | 2015-11-24 | Incyte Holdings Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
PL3023415T3 (pl) | 2012-10-02 | 2018-06-29 | Gilead Sciences, Inc. | Inhibitory demetylaz histonowych |
EP2917221A1 (en) | 2012-11-01 | 2015-09-16 | Incyte Corporation | Tricyclic fused thiophene derivatives as jak inhibitors |
HUE055894T2 (hu) | 2012-11-15 | 2021-12-28 | Incyte Holdings Corp | A ruxolitinib nyújtott felszabadulású dózisformái |
EP2943485B1 (en) | 2013-01-14 | 2017-09-20 | Incyte Holdings Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
NZ749911A (en) | 2013-01-15 | 2020-02-28 | Incyte Holdings Corp | Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors |
MD20150085A2 (ro) | 2013-02-27 | 2016-02-29 | Epitherapeutics Aps | Inhibitori ai histon-demetilazelor |
BR112015021458B1 (pt) * | 2013-03-06 | 2022-06-07 | Incyte Holdings Corporation | "processos e intermediários para preparar {1-{1-[3-flúor2-(trifluormetil)isonicotinoil] piperidin-4-il}-3-[4-(7hpirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]azetidin-3-il}acetonitrila, útil no tratamento de doenças relacionadas com a atividade de janus quinases |
US8669281B1 (en) | 2013-03-14 | 2014-03-11 | Alkermes Pharma Ireland Limited | Prodrugs of fumarates and their use in treating various diseases |
CN105452213B (zh) | 2013-03-14 | 2017-09-22 | 阿尔克梅斯制药爱尔兰有限公司 | 富马酸酯前体药物及其在治疗多种疾病中的应用 |
WO2014146249A1 (en) * | 2013-03-19 | 2014-09-25 | Merck Sharp & Dohme Corp. | Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors |
US10059705B2 (en) | 2013-03-19 | 2018-08-28 | Merck Sharp & Dohme Corp. | Acyclic cyanoethylpyrazolo pyridones as janus kinase inhibitors |
WO2014146246A1 (en) * | 2013-03-19 | 2014-09-25 | Merck Sharp & Dohme Corp. | Cycloalkyl nitrile pyrazolo pyridones as janus kinase inhibitors |
RU2669922C2 (ru) | 2013-03-19 | 2018-10-17 | Мерк Шарп И Доум Корп. | N-(2-цианогетероциклил)пиразолопиридоны в качестве ингибиторов янус-киназы |
US20160045498A1 (en) * | 2013-04-04 | 2016-02-18 | The Walter And Eliza Hall Institute Of Medical Research | Methods of treating diseases characterized by excessive wnt signalling |
HUE043573T2 (hu) | 2013-05-17 | 2019-08-28 | Incyte Corp | Bipirazol só, amely JAK-gátlóként alkalmazható |
KR20160045081A (ko) | 2013-08-07 | 2016-04-26 | 인사이트 코포레이션 | Jak1 억제제용 지속 방출 복용 형태 |
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 |
SG11201601259YA (en) | 2013-08-23 | 2016-03-30 | Incyte Corp | Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors |
JP6367545B2 (ja) * | 2013-12-17 | 2018-08-01 | コンサート ファーマシューティカルズ インコーポレイテッド | ルキソリチニブの重水素化誘導体 |
WO2015127450A1 (en) | 2014-02-24 | 2015-08-27 | Alkermes Pharma Ireland Limited | Sulfonamide and sulfinamide prodrugs of fumarates and their use in treating various diseases |
PL3110409T3 (pl) | 2014-02-28 | 2018-12-31 | Incyte Corporation | Inhibitory jak1 do leczenia zespołów mielodysplastycznych |
PT3129021T (pt) * | 2014-04-08 | 2020-11-16 | Incyte Corp | Ratamento de doenças malignas das células b por uma associação de inibidores de jak e pi3k |
CN106687462A (zh) | 2014-04-30 | 2017-05-17 | 因赛特公司 | Jak1抑制剂的制备方法以及其新形式 |
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 |
WO2015191677A1 (en) | 2014-06-11 | 2015-12-17 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors |
US9822124B2 (en) | 2014-07-14 | 2017-11-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors |
US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
MA40470A (fr) * | 2014-08-27 | 2016-03-03 | Gilead Sciences Inc | Composés et procédés d'inhibition des histones déméthylases |
US9586949B2 (en) | 2015-02-09 | 2017-03-07 | Incyte Corporation | Aza-heteroaryl compounds as PI3K-gamma inhibitors |
EP3262046B1 (en) | 2015-02-27 | 2020-11-04 | Incyte Corporation | Salts of pi3k inhibitor and processes for their preparation |
US9732097B2 (en) | 2015-05-11 | 2017-08-15 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
US9988401B2 (en) | 2015-05-11 | 2018-06-05 | Incyte Corporation | Crystalline forms of a PI3K inhibitor |
WO2016183071A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Hetero-tricyclic compounds and their use for the treatment of cancer |
WO2016196244A1 (en) | 2015-05-29 | 2016-12-08 | Incyte Corporation | Pyridineamine compounds useful as pim kinase inhibitors |
WO2017013270A1 (en) | 2015-07-23 | 2017-01-26 | Universite De Strasbourg | Use of leptin signaling inhibitor for protecting kidneys from patients having ciliopathy |
WO2017027717A1 (en) | 2015-08-12 | 2017-02-16 | Incyte Corporation | Bicyclic fused pyrimidine compounds as tam inhibitors |
WO2017035366A1 (en) | 2015-08-26 | 2017-03-02 | Incyte Corporation | Pyrrolopyrimidine derivatives as tam inhibitors |
TWI734699B (zh) | 2015-09-09 | 2021-08-01 | 美商英塞特公司 | Pim激酶抑制劑之鹽 |
TW201718546A (zh) | 2015-10-02 | 2017-06-01 | 英塞特公司 | 適用作pim激酶抑制劑之雜環化合物 |
US11780848B2 (en) | 2015-10-16 | 2023-10-10 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1- carboxamide and solid state forms thereof |
US10550126B2 (en) | 2015-10-16 | 2020-02-04 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
US11365198B2 (en) | 2015-10-16 | 2022-06-21 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
SG11201802990RA (en) | 2015-10-16 | 2018-05-30 | Abbvie Inc | PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF |
EP4086259A1 (en) | 2015-11-06 | 2022-11-09 | Incyte Corporation | Heterocyclic compounds as pi3k-gamma inhibitors |
ES2830446T3 (es) * | 2015-12-11 | 2021-06-03 | Sichuan Kelun Biotech Biopharmaceutical Co Ltd | Derivado de azetidina, método de preparación del mismo y uso del mismo |
EP3400221B1 (en) | 2016-01-05 | 2020-08-26 | Incyte Corporation | Pyrazol / imidazol substituted pyridines as pi3k-gamma inhibitors |
JP6770580B2 (ja) * | 2016-01-26 | 2020-10-14 | 杭州華東医薬集団生物医薬有限公司Hangzhou Huadong Medicine Group Biopharmaceutical Co., Ltd. | ピロロピリミジン5員環アザ環状誘導体およびその利用 |
WO2017162604A1 (en) | 2016-03-21 | 2017-09-28 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for diagnosis and treatment of solar lentigo |
CN114456175B (zh) | 2016-03-28 | 2024-09-03 | 因赛特公司 | 作为tam抑制剂的吡咯并三嗪化合物 |
TW201803871A (zh) | 2016-06-24 | 2018-02-01 | 英塞特公司 | 作為PI3K-γ抑制劑之雜環化合物 |
EP3504532B1 (en) * | 2016-08-24 | 2024-08-21 | Royal Melbourne Institute Of Technology | Diagnostic methods and device |
GB201617871D0 (en) * | 2016-10-21 | 2016-12-07 | Sareum Limited | Pharmaceutical compounds |
US20180153922A1 (en) | 2016-12-06 | 2018-06-07 | New York Society For The Ruptured And Crippled Maintaining The Hospital For Special Surgery | Inhibition of expansion and function of pathogenic age-associated b cells and use for the prevention and treatment of autoimmune disease |
US10961228B2 (en) | 2017-01-17 | 2021-03-30 | Astrazeneca Ab | JAK1 selective inhibitors |
WO2018167283A1 (en) | 2017-03-17 | 2018-09-20 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling |
CN109422753B (zh) * | 2017-09-03 | 2021-12-31 | 上海美志医药科技有限公司 | 一类具有抑制并降解酪氨酸蛋白激酶jak1或jak2活性的化合物 |
WO2019067594A1 (en) | 2017-09-27 | 2019-04-04 | Incyte Corporation | SALTS OF PYRROLOTRIAZINE DERIVATIVES USEFUL AS TAM INHIBITORS |
BR112020007593A2 (pt) | 2017-10-18 | 2020-09-24 | Incyte Corporation | derivados de imidazol condensados substituídos por grupos hidróxi terciários como inibidores de pi3k-gama |
CN109867676B (zh) * | 2017-12-01 | 2020-10-30 | 北京普祺医药科技有限公司 | 一种吡咯并嘧啶衍生的化合物、药物组合物以及其用途 |
AR113922A1 (es) | 2017-12-08 | 2020-07-01 | Incyte Corp | Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas |
SG11202007072RA (en) | 2018-01-26 | 2020-08-28 | Rapt Therapeutics Inc | Chemokine receptor modulators and uses thereof |
TWI797242B (zh) * | 2018-01-30 | 2023-04-01 | 美商英塞特公司 | 製備jak抑制劑之方法及中間物 |
CN118557580A (zh) * | 2018-02-16 | 2024-08-30 | 因赛特公司 | 用于治疗细胞因子相关的病症的jak1通路抑制剂 |
MX2020009305A (es) | 2018-03-08 | 2020-11-24 | Novartis Ag | Uso de un anticuerpo anti-p-selectina. |
SG11202009441PA (en) * | 2018-03-30 | 2020-10-29 | Incyte Corp | Treatment of hidradenitis suppurativa using jak inhibitors |
WO2019191679A1 (en) | 2018-03-30 | 2019-10-03 | Incyte Corporation | Biomarkers for inflammatory skin disease |
KR20210018218A (ko) | 2018-04-13 | 2021-02-17 | 인사이트 코포레이션 | 이식편대숙주질환용 바이오마커 |
CA3101323A1 (en) | 2018-06-01 | 2019-12-05 | Incyte Corporation | Dosing regimen for the treatment of pi3k related disorders |
MX2021000127A (es) | 2018-06-29 | 2021-03-29 | Incyte Corp | Formulaciones de un inhibidor de axl/mer. |
WO2020039401A1 (en) | 2018-08-24 | 2020-02-27 | Novartis Ag | Treatment comprising il-1βeta binding antibodies and combinations thereof |
IL309869A (en) | 2018-09-05 | 2024-02-01 | Incyte Corp | Crystal forms of phosphoinositide 3-kinase inhibitor (PI3K) |
MX2021004946A (es) | 2018-10-31 | 2021-07-15 | Incyte Corp | Terapia combinada para tratamiento de enfermedades hematológicas. |
WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
KR101992148B1 (ko) | 2018-11-30 | 2019-06-25 | 한승훈 | 안전벨트의 꼬임방지장치 |
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 |
KR20210134738A (ko) | 2019-03-14 | 2021-11-10 | 상하이 시너지 파마슈티컬 사이언시스 코., 엘티디. | Jak 억제제 및 그 제조방법과 의약분야에서의 응용 |
EP3941474A2 (en) | 2019-03-19 | 2022-01-26 | Incyte Corporation | Biomarkers for vitiligo |
WO2021091535A1 (en) | 2019-11-05 | 2021-05-14 | Constellation Pharmaceuticals, Inc. | Treating myeloproliferative disorders with cpi-0610 and a jak inhibitor |
WO2020256739A1 (en) | 2019-06-21 | 2020-12-24 | Constellation Pharmaceuticals, Inc. | Methods of treating myeloproliferative disorders |
WO2020257644A1 (en) | 2019-06-21 | 2020-12-24 | Constellation Pharmaceuticals, Inc. | Methods of treating myeloproliferative disorders |
TW202124443A (zh) | 2019-09-16 | 2021-07-01 | 瑞士商諾華公司 | 高親和力的、配位基阻斷性、人源化的抗T細胞免疫球蛋白結構域和黏蛋白結構域3(TIM-3)IgG4抗體用於治療骨髓纖維化之用途 |
WO2021053489A1 (en) | 2019-09-16 | 2021-03-25 | Novartis Ag | Use of an mdm2 inhibitor for the treatment of myelofibrosis |
EP4041204A1 (en) | 2019-10-10 | 2022-08-17 | Incyte Corporation | Biomarkers for graft-versus-host disease |
US20210123931A1 (en) | 2019-10-10 | 2021-04-29 | Incyte Corporation | Biomarkers for graft-versus-host disease |
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) |
JP7518900B2 (ja) * | 2019-10-16 | 2024-07-18 | インサイト・コーポレイション | 皮膚エリテマトーデス及び扁平苔癬(lp)の治療のためのjak1阻害剤の使用 |
MX2022006176A (es) | 2019-11-22 | 2022-08-17 | Incyte Corp | Terapia combinada que comprende un inhibidor de alk2 y un inhibidor de jak2. |
AR122505A1 (es) | 2020-06-02 | 2022-09-14 | Incyte Corp | Procesos para preparar un inhibidor de jak1 |
US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
IL300557A (en) | 2020-08-18 | 2023-04-01 | Incyte Corp | Process and intermediates for preparing a JAK1 inhibitor |
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 |
EP4225317A1 (en) | 2020-10-08 | 2023-08-16 | Novartis AG | Use of an erk inhibitor for the treatment of myelofibrosis |
WO2022120131A1 (en) | 2020-12-04 | 2022-06-09 | Incyte Corporation | Jak inhibitor with a vitamin d analog for treatment of skin diseases |
KR20230118118A (ko) | 2020-12-08 | 2023-08-10 | 인사이트 코포레이션 | 백반증의 치료를 위한 jak1 경로 저해제 |
CA3207859A1 (en) | 2021-01-11 | 2022-07-14 | Incyte Corporation | Combination therapy comprising jak pathway inhibitor and rock inhibitor |
TWI820622B (zh) | 2021-03-04 | 2023-11-01 | 美商美國禮來大藥廠 | Fgfr3抑制劑化合物 |
WO2022235613A1 (en) | 2021-05-03 | 2022-11-10 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of prurigo nodularis |
WO2023288197A1 (en) | 2021-07-12 | 2023-01-19 | Incyte Corporation | Process and intermediates for preparing baricitinib |
CN114149437A (zh) * | 2021-12-24 | 2022-03-08 | 安徽大学 | 一种吡咯并嘧啶五元氮杂环衍生物及其制备方法和用途 |
WO2024030600A1 (en) | 2022-08-05 | 2024-02-08 | Incyte Corporation | Treatment of urticaria using jak inhibitors |
Family Cites Families (309)
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 |
US3632836A (en) | 1968-10-25 | 1972-01-04 | Dow Chemical Co | Solid curable polyepoxides modified with hydrolyzed liquid polyepoxides |
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 |
US4404335A (en) | 1982-08-16 | 1983-09-13 | The Dow Chemical Company | Hydrolyzing epoxy resins in absence of solvent and in presence of oxalic acid and a phosphonium compound |
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 |
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 |
US5378700A (en) | 1989-10-11 | 1995-01-03 | Teijin Limited | Fused pyrimidine derivative, process for preparation of same and pharmaceutical preparation comprising same as active ingredient |
US5403593A (en) | 1991-03-04 | 1995-04-04 | Sandoz Ltd. | Melt granulated compositions for preparing sustained release dosage forms |
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 |
USH1439H (en) | 1993-10-18 | 1995-05-02 | The Dow Chemical Company | Method to increase the level of α-glycol in liquid epoxy resin |
EP0727217A3 (en) | 1995-02-10 | 1997-01-15 | Suntory Ltd | Pharmaceutical and cosmetic compositions containing God-type ellagitannin as an active ingredient |
US5856326A (en) | 1995-03-29 | 1999-01-05 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
IL117580A0 (en) | 1995-03-29 | 1996-07-23 | Merck & Co Inc | Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them |
ES2167586T3 (es) | 1995-07-05 | 2002-05-16 | Du Pont | Pirimidinonas fungicidas. |
PT836605E (pt) | 1995-07-06 | 2002-07-31 | Novartis Ag | Pirrolopirimidinas e processos para a sua preparacao |
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 |
EP0906099A4 (en) | 1996-04-03 | 2001-02-07 | Merck & Co Inc | CANCER TREATMENT METHOD |
AU2802297A (en) | 1996-04-18 | 1997-11-07 | Merck & Co., Inc. | A method of treating cancer |
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 |
EP0973396A4 (en) | 1997-04-07 | 2001-02-07 | Merck & Co Inc | METHOD FOR 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 |
US5908841A (en) | 1997-08-11 | 1999-06-01 | Boehringer Ingelheim Pharmaceuticals, Inc. | 5,11-dihydro-6H-dipyrido 3,2-b:2',3'-e!azepine-6-ones and their use in the prevention of treatment of HIV infection |
US7153845B2 (en) | 1998-08-25 | 2006-12-26 | Columbia Laboratories, Inc. | Bioadhesive progressive hydration tablets |
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 |
KR20010052570A (ko) | 1998-06-04 | 2001-06-25 | 스티븐 에프. 웨인스톡 | 세포 유착을 억제하는 소염성 화합물 |
US6232320B1 (en) | 1998-06-04 | 2001-05-15 | Abbott Laboratories | Cell adhesion-inhibiting antiinflammatory compounds |
PA8474101A1 (es) | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
PL198640B1 (pl) | 1998-06-19 | 2008-07-31 | Pfizer Prod Inc | Związki pirolo[2,3-d]pirymidynowe, środek farmaceutyczny i zastosowanie tych związków |
ES2342240T3 (es) | 1998-08-11 | 2010-07-02 | Novartis Ag | Derivados de isoquinolina con actividad que inhibe la angiogenia. |
JP2000119271A (ja) | 1998-08-12 | 2000-04-25 | Hokuriku Seiyaku Co Ltd | 1h―イミダゾピリジン誘導体 |
CA2343148C (en) | 1998-09-10 | 2005-11-15 | Nycomed Danmark A/S | Quick release pharmaceutical compositions of drug substances |
US6375839B1 (en) | 1998-10-29 | 2002-04-23 | Institut Francais Du Petrole | Process and device for separation with variable-length chromatographic zones |
FR2785196B1 (fr) | 1998-10-29 | 2000-12-15 | Inst Francais Du Petrole | Procede et dispositif de separation avec des zones chromatographiques a longueur variable |
US6413419B1 (en) | 1998-10-29 | 2002-07-02 | Institut Francais Du Petrole | Process and device for separation with variable-length chromatographic |
US6133031A (en) | 1999-08-19 | 2000-10-17 | Isis Pharmaceuticals Inc. | Antisense inhibition of focal adhesion kinase expression |
JP2002538121A (ja) | 1999-03-03 | 2002-11-12 | メルク エンド カムパニー インコーポレーテッド | プレニルタンパク質トランスフェラーゼの阻害剤 |
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 |
AU3565999A (en) | 1999-04-16 | 2000-11-02 | Coelacanth Chemical Corporation | Synthesis of azetidine derivatives |
US6915718B2 (en) | 1999-09-02 | 2005-07-12 | United Parts Fhs Automobil Systeme Gmbh | Selector handle in a motor vehicle |
US6921763B2 (en) | 1999-09-17 | 2005-07-26 | Abbott Laboratories | Pyrazolopyrimidines as therapeutic agents |
AU766233B2 (en) * | 1999-10-13 | 2003-10-09 | Banyu Pharmaceutical Co., Ltd. | Substituted imidazolidinone derivatives |
US7235258B1 (en) | 1999-10-19 | 2007-06-26 | Nps Pharmaceuticals, Inc. | Sustained-release formulations for treating CNS-mediated disorders |
ATE380031T1 (de) | 1999-12-10 | 2007-12-15 | Pfizer Prod Inc | Pyrrolo 2,3-d pyrimidinderivate enthaltende zusammensetzungen |
KR100755622B1 (ko) | 1999-12-24 | 2007-09-04 | 아벤티스 파마 리미티드 | 아자인돌 |
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 |
DK1142566T3 (da) | 2000-04-07 | 2004-02-09 | Medidom Lab | Oftalmologiske formuleringer på basis af ciclosporin, hyaluronsyre og polysorbat |
AU4878601A (en) | 2000-04-20 | 2001-11-07 | Mitsubishi Corporation | Aromatic amide compounds |
JP4642309B2 (ja) | 2000-04-25 | 2011-03-02 | イコス・コーポレイション | ヒトホスファチジル−イノシトール3−キナーゼデルタの阻害剤 |
US7498304B2 (en) | 2000-06-16 | 2009-03-03 | Curis, Inc. | Angiogenesis-modulating compositions and uses |
WO2001098344A2 (en) | 2000-06-16 | 2001-12-27 | 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 |
WO2001097849A1 (fr) | 2000-06-23 | 2001-12-27 | Mitsubishi Pharma Corporation | Potentialisateurs d'effet antitumoral |
HUP0301114A3 (en) | 2000-06-26 | 2004-11-29 | Pfizer Prod Inc | Pyrrolo[2,3-d]pyrimidine compounds as immunosuppressive agents and pharmaceutical compositions containing them |
AU2002215608B2 (en) | 2000-06-28 | 2004-12-09 | Smithkline Beecham P.L.C. | Wet milling process |
WO2002016370A1 (fr) | 2000-08-22 | 2002-02-28 | Hokuriku Seiyaku Co., Ltd. | Derives de 1h-imidazopyridine |
AU2002228783A1 (en) | 2000-12-05 | 2002-06-18 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
GB0100622D0 (en) | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds V111 |
US20040077654A1 (en) | 2001-01-15 | 2004-04-22 | Bouillot Anne Marie Jeanne | Aryl piperidine and piperazine derivatives as inducers of ldl-receptor expression |
WO2002060492A1 (en) | 2001-01-30 | 2002-08-08 | Cytopia Pty Ltd | Methods of inhibiting kinases |
CA2446864C (en) | 2001-05-16 | 2011-02-15 | Vertex Pharmaceuticals Incorporated | 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 |
DE60216115T2 (de) | 2001-08-01 | 2007-05-31 | Merck & Co., Inc. | BENZIMIDAZO 4,5-föISOCHINOLINON-DERIVATE |
CA2466243A1 (en) | 2001-09-19 | 2003-03-27 | 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 |
HU230798B1 (hu) | 2001-10-30 | 2018-06-28 | Novartis Ag | Staurosporin-származékok mint az FLT3 receptor tirozin-kináz aktivitás inhibitorai |
JP2003155285A (ja) | 2001-11-19 | 2003-05-27 | Toray Ind Inc | 環状含窒素誘導体 |
WO2003048111A1 (en) | 2001-11-30 | 2003-06-12 | Teijin Limited | Process for producing 5-(3-cyanophenyl)-3-formylbenzoic acid compound |
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 |
MXPA04010225A (es) | 2002-04-15 | 2005-07-05 | Adams Lab Inc | Liberacion sostenida de la combinacion de guaifenesina con farmacos. |
TW200403058A (en) | 2002-04-19 | 2004-03-01 | Bristol Myers Squibb Co | Heterocyclo inhibitors of potassium channel function |
WO2003091246A1 (en) | 2002-04-26 | 2003-11-06 | Vertex Pharmaceuticals Incorporated | Pyrrole derivatives as inhibitors of erk2 and uses thereof |
US7125888B2 (en) | 2002-05-02 | 2006-10-24 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
BR0309844A (pt) | 2002-05-07 | 2005-02-15 | Control Delivery Sys Inc | Processos para formação de um dispositivo para a distribuição de droga |
ATE377004T1 (de) | 2002-05-23 | 2007-11-15 | Cytopia Pty Ltd | Proteinkinaseinhibitoren |
PE20040522A1 (es) | 2002-05-29 | 2004-09-28 | Novartis Ag | Derivados de diarilurea dependientes de la cinasa de proteina |
EP1535934A4 (en) | 2002-06-26 | 2005-11-02 | Idemitsu Kosan Co | HYDROGEN COPOLYMER, PROCESS FOR PRODUCING THE SAME, AND THERMOFUSIBLE ADHESIVE COMPOSITION CONTAINING 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 |
EP1541563A4 (en) | 2002-07-10 | 2007-11-07 | Ono Pharmaceutical Co | ANTAGONIST OF CCR4 AND CORRESPONDING MEDICINAL USE |
AU2003278727A1 (en) | 2002-09-20 | 2004-04-08 | Alcon, Inc. | Use of cytokine synthesis inhibitors for the treatment of dry eye disorders |
US20040204404A1 (en) | 2002-09-30 | 2004-10-14 | Robert Zelle | Human N-type calcium channel blockers |
US7259161B2 (en) | 2002-11-04 | 2007-08-21 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of JAK and other protein kinases |
US8034831B2 (en) | 2002-11-06 | 2011-10-11 | Celgene Corporation | Methods for the treatment and management of myeloproliferative diseases using 4-(amino)-2-(2,6-Dioxo(3-piperidyl)-isoindoline-1,3-dione in combination with other therapies |
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 |
PL378246A1 (pl) | 2002-11-26 | 2006-03-20 | Pfizer Products Inc. | Sposób leczenia odrzucania przeszczepu |
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 |
TW200418806A (en) | 2003-01-13 | 2004-10-01 | Fujisawa Pharmaceutical Co | HDAC inhibitor |
US7444183B2 (en) | 2003-02-03 | 2008-10-28 | Enteromedics, Inc. | Intraluminal electrode apparatus and method |
EP1611125A1 (en) | 2003-02-07 | 2006-01-04 | Vertex Pharmaceuticals Incorporated | Heteroaryl substituted pyrolls useful as inhibitors of protein kinases |
GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
AU2004230841A1 (en) | 2003-04-03 | 2004-10-28 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of protein kinases |
SE0301373D0 (sv) | 2003-05-09 | 2003-05-09 | Astrazeneca Ab | Novel compounds |
SE0301372D0 (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 |
AU2004268621C1 (en) | 2003-08-29 | 2011-08-18 | Exelixis, Inc. | c-Kit modulators and methods of use |
WO2005026129A1 (en) | 2003-09-15 | 2005-03-24 | Gpc Biotech Ag | Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases |
AR045944A1 (es) | 2003-09-24 | 2005-11-16 | Novartis Ag | Derivados de isoquinolina 1.4-disustituidas |
TWI343256B (en) | 2003-10-24 | 2011-06-11 | Santen Pharmaceutical Co Ltd | Cornea-conjunctiva disorder treating agent |
US7387793B2 (en) | 2003-11-14 | 2008-06-17 | Eurand, Inc. | Modified release dosage forms of skeletal muscle relaxants |
MY141220A (en) | 2003-11-17 | 2010-03-31 | Astrazeneca Ab | Pyrazole derivatives as inhibitors of receptor tyrosine kinases |
BRPI0416909A (pt) | 2003-11-25 | 2007-01-16 | Pfizer Prod Inc | método de tratamento de aterosclerose |
AU2004305317A1 (en) | 2003-12-17 | 2005-07-07 | Pfizer Products Inc. | Pyrrolo [2,3-D] pyrimidine compounds for treating transplant rejection |
AU2004308299B2 (en) | 2003-12-19 | 2011-11-24 | Plexxikon, Inc. | Compounds and methods for development of Ret modulators |
DE602004016211D1 (en) | 2003-12-19 | 2008-10-09 | Schering Corp | Thiadiazole als cxc- und cc-chemokinrezeptorliganden |
AU2004303602C1 (en) | 2003-12-23 | 2009-05-28 | Astex Therapeutics Limited | Pyrazole derivatives as protein kinase modulators |
US20050165029A1 (en) | 2004-01-13 | 2005-07-28 | Ambit Biosciences Corporation | Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases |
US20050277629A1 (en) | 2004-03-18 | 2005-12-15 | The Brigham And Women's Hospital, Inc. | Methods for the treatment of synucleinopathies (Lansbury) |
NZ584499A (en) | 2004-03-30 | 2011-08-26 | Vertex Pharma | Azaindoles Useful as Inhibitors of Jak and Other Protein Kinases |
US8076338B2 (en) | 2004-04-23 | 2011-12-13 | Exelixis, Inc. | Kinase modulators and methods of use |
US7558717B2 (en) | 2004-04-28 | 2009-07-07 | Vertex Pharmaceuticals Incorporated | Crystal structure of human JAK3 kinase domain complex and binding pockets thereof |
WO2005105814A1 (en) | 2004-04-28 | 2005-11-10 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
CA2563569A1 (en) | 2004-05-03 | 2005-11-10 | Novartis Ag | Combinations comprising a s1p receptor agonist and a jak3 kinase inhibitor |
WO2005110410A2 (en) | 2004-05-14 | 2005-11-24 | Abbott Laboratories | Kinase inhibitors as therapeutic agents |
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 |
WO2006001463A1 (ja) | 2004-06-23 | 2006-01-05 | Ono Pharmaceutical Co., Ltd. | S1p受容体結合能を有する化合物およびその用途 |
AU2005260689B2 (en) | 2004-06-30 | 2012-05-10 | Vertex Pharmaceuticals Incorporated | 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 |
EP1802625B1 (en) | 2004-10-13 | 2008-06-18 | F. Hoffmann-Roche AG | Disubstituted pyrazolobenzodiazepines useful as inhibitors for cdk2 and angiogesis, 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 |
EP1812440B1 (en) | 2004-11-04 | 2010-09-22 | Vertex Pharmaceuticals, Inc. | Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases |
KR20070085433A (ko) | 2004-11-24 | 2007-08-27 | 노파르티스 아게 | Jak 저해제들과 bcr-abl, flt-3, fak 또는raf 키나제 저해제들 중 하나 이상의 조합물 |
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 |
US20060128803A1 (en) | 2004-12-14 | 2006-06-15 | Alcon, Inc. | Method of treating dry eye disorders using 13(S)-HODE and its analogs |
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. |
TW200635899A (en) | 2004-12-22 | 2006-10-16 | Astrazeneca Ab | Chemical compounds |
EP1844037A1 (en) | 2005-01-20 | 2007-10-17 | Pfizer Limited | Chemical compounds |
KR20070104641A (ko) | 2005-02-03 | 2007-10-26 | 버텍스 파마슈티칼스 인코포레이티드 | 단백질 키나제의 억제제로 유용한 피롤로피리미딘 |
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 |
CA2600144A1 (en) | 2005-03-15 | 2006-09-28 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
RU2007140903A (ru) | 2005-04-05 | 2009-05-20 | Фармакопия, Инк. (Us) | Производные пурина и имидазопиридина для иммуносупрессии |
GB0510139D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B1 |
CA2609126A1 (en) | 2005-05-20 | 2006-11-30 | Vertex Pharmaceuticals Incorporated | Pyrrolopyridines useful as inhibitors of protein kinase |
GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
MX286273B (es) | 2005-06-08 | 2011-05-04 | Rigel Pharmaceuticals Inc | Composiciones y metodos para inhibicion de la via jak. |
WO2006136823A1 (en) | 2005-06-21 | 2006-12-28 | Astex Therapeutics Limited | Heterocyclic containing amines as kinase b inhibitors |
HUE027370T2 (en) | 2005-06-22 | 2016-10-28 | 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 |
US20070149506A1 (en) | 2005-09-22 | 2007-06-28 | Arvanitis Argyrios G | 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 |
AU2006300182B2 (en) | 2005-10-14 | 2012-01-19 | Sumitomo Chemical Company, Limited | Hydrazide compound and pesticidal use of the same |
AU2006307657B2 (en) | 2005-10-28 | 2010-10-28 | Astrazeneca Ab | 4- (3-aminopyrazole) pyrimidine derivatives for use as tyrosine kinase inhibitors in the treatment of cancer |
NZ567851A (en) | 2005-11-01 | 2011-09-30 | Targegen Inc | Bi-aryl meta-pyrimidine inhibitors of kinases |
US9006224B2 (en) | 2005-11-21 | 2015-04-14 | Novartis Ag | Neuroendocrine tumor treatment |
WO2007062459A1 (en) | 2005-11-29 | 2007-06-07 | Cytopia Research Pty Ltd | Selective kinase inhibitors based on pyridine scaffold |
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 |
PL2426129T3 (pl) * | 2005-12-13 | 2017-04-28 | Incyte Holdings Corporation | Podstawione heteroarylem pirolo[2,3-b]pirydyny i pirolo[2,3-b]pirymidyny jako inhibitory kinazy Janusowej |
WO2007076423A2 (en) | 2005-12-22 | 2007-07-05 | Smithkline Beecham Corporation | INHIBITORS OF Akt ACTIVITY |
CA2634787C (en) | 2005-12-23 | 2014-10-21 | Smithkline Beecham Corporation | Azaindole inhibitors of aurora kinases |
JP4643455B2 (ja) | 2006-01-12 | 2011-03-02 | 株式会社ユニバーサルエンターテインメント | 遊技システム |
KR101235103B1 (ko) | 2006-01-17 | 2013-02-21 | 버텍스 파마슈티칼스 인코포레이티드 | 야누스 키나제의 억제제로서 유용한 아자인돌 |
TW200738709A (en) | 2006-01-19 | 2007-10-16 | Osi Pharm Inc | Fused heterobicyclic kinase inhibitors |
US20090018156A1 (en) | 2006-02-01 | 2009-01-15 | Jun Tang | 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 |
PL1842534T3 (pl) | 2006-02-24 | 2012-05-31 | Teva Pharma | Tabletki bursztynianu metoprololu o przedłużonym uwalnianiu oraz sposoby ich wytwarzania |
AU2007225836A1 (en) | 2006-03-10 | 2007-09-20 | Ono Pharmaceutical Co., Ltd. | Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient |
TWI382984B (zh) | 2006-04-03 | 2013-01-21 | Astellas Pharma Inc | 雜環化合物 |
CA2648250A1 (en) * | 2006-04-05 | 2007-10-18 | Vertex Pharmaceuticals Incorporated | Deazapurines useful as inhibitors of janus kinases |
EP2059515A2 (en) | 2006-04-12 | 2009-05-20 | 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 |
AU2007252994A1 (en) | 2006-05-18 | 2007-11-29 | Bayer Healthcare Ag | Pharmaceutical compositions comprising implitapide 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 |
TWI398252B (zh) | 2006-05-26 | 2013-06-11 | Novartis Ag | 吡咯并嘧啶化合物及其用途 |
NZ573174A (en) | 2006-06-01 | 2012-01-12 | Msd Consumer Care Inc | Sustained release pharmaceutical dosage form containing phenylephrine |
EP2044061A2 (en) | 2006-07-20 | 2009-04-08 | Mehmet Kahraman | Benzothiophene inhibitors of rho kinase |
WO2008013622A2 (en) | 2006-07-27 | 2008-01-31 | E. I. Du Pont De Nemours And Company | Fungicidal azocyclic amides |
US8492378B2 (en) | 2006-08-03 | 2013-07-23 | Takeda Pharmaceutical Company Limited | GSK-3β inhibitor |
CA2660560A1 (en) | 2006-08-16 | 2008-02-21 | Boehringer Ingelheim International Gmbh | Pyrazine compounds, their use and methods of preparation |
RU2009112719A (ru) | 2006-09-08 | 2010-10-20 | Новартис АГ (CH) | Производные n-биарил(гетеро)арилсульфонамида, применимые в лечении заболеваний, опосредованных взаимодействием лимфоцитов |
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. |
WO2008043031A1 (en) | 2006-10-04 | 2008-04-10 | 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 |
WO2008058126A2 (en) | 2006-11-06 | 2008-05-15 | 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 |
US7767675B2 (en) | 2006-11-22 | 2010-08-03 | Incyte Corporation | Imidazotriazines and imidazopyrimidines as kinase inhibitors |
WO2008067119A2 (en) | 2006-11-27 | 2008-06-05 | Smithkline Beecham Corporation | Novel compounds |
US7834039B2 (en) | 2006-12-15 | 2010-11-16 | Abbott Laboratories | Oxadiazole compounds |
WO2008079291A2 (en) | 2006-12-20 | 2008-07-03 | Amgen Inc. | Substituted heterocycles and methods of use |
MX2009006543A (es) | 2006-12-20 | 2009-06-26 | Amgen Inc | Compuestos heterociclicos y su uso en el tratamiento de la inflamacion, angiogenesis y cancer. |
AU2007338210B2 (en) | 2006-12-22 | 2013-01-31 | Sigma-Tau Industrie Farmaceutiche Riunite S.P.A. | Gel useful for the delivery of ophthalmic drugs |
CA2673038C (en) | 2006-12-22 | 2015-12-15 | Incyte Corporation | Substituted tricyclic heteroaryl compounds as janus kinase inhibitors |
KR20080062876A (ko) | 2006-12-29 | 2008-07-03 | 주식회사 대웅제약 | 신규한 항진균성 트리아졸 유도체 |
WO2008082840A1 (en) | 2006-12-29 | 2008-07-10 | Abbott Laboratories | Pim kinase inhibitors as cancer chemotherapeutics |
WO2008082839A2 (en) | 2006-12-29 | 2008-07-10 | Abbott Laboratories | Pim kinase inhibitors as cancer chemotherapeutics |
JP5330274B2 (ja) | 2007-03-01 | 2013-10-30 | ノバルティス アーゲー | Pimキナーゼ阻害剤およびその使用方法 |
BRPI0809998B8 (pt) | 2007-04-03 | 2021-05-25 | Array Biopharma Inc | composto de imidazo[1,2-a] piridina como inibidores do receptor tirosina quinase, seus usos, seus processos de preparação e composições farmacêuticas |
US8188178B2 (en) | 2007-05-07 | 2012-05-29 | 3M Innovative Properties Company | Cold shrinkable article including an epichlorohydrin composition |
GB0709031D0 (en) | 2007-05-10 | 2007-06-20 | Sareum Ltd | Pharmaceutical compounds |
WO2008145681A2 (en) | 2007-05-31 | 2008-12-04 | Boehringer Ingelheim International Gmbh | Ccr2 receptor antagonists and uses thereof |
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. |
ME00960B (me) | 2007-06-13 | 2012-06-20 | Incyte Corp | Soli inhibitora janus kinaze, (r)-3-(4-(7h-pirol[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 |
BRPI0815042A2 (pt) | 2007-08-01 | 2015-02-10 | Pfizer | Compostos de pirazol |
WO2009049028A1 (en) | 2007-10-09 | 2009-04-16 | Targegen Inc. | Pyrrolopyrimidine compounds and their use as janus kinase modulators |
EP2217235A4 (en) | 2007-11-15 | 2011-01-12 | Musc Found For Res Dev | PROTEIN INHIBITORS PIM KINASES, COMPOSITIONS AND METHODS FOR TREATING CANCER |
UA104849C2 (uk) | 2007-11-16 | 2014-03-25 | Інсайт Корпорейшн | 4-піразоліл-n-арилпіримідин-2-аміни і 4-піразоліл-n-гетероарилпіримідин-2-аміни як інгібітори кіназ janus |
GB0723815D0 (en) | 2007-12-05 | 2008-01-16 | Glaxo Group Ltd | Compounds |
PL2231689T3 (pl) | 2008-01-18 | 2017-01-31 | Inst Of Organic Chemistry And Biochemistry Of The Acad Of Sciences Of The Czech Republic | Nowe 7-deazapurynowe nukleozydy o właściwościach cytostatycznych |
US8273744B2 (en) | 2008-02-04 | 2012-09-25 | Mercury Therapeutics, Inc. | AMPK modulators |
PE20091577A1 (es) | 2008-03-03 | 2009-11-05 | Novartis Ag | Inhibidores de cinasa pim y metodos para su uso |
BRPI0909040B8 (pt) * | 2008-03-11 | 2021-05-25 | Incyte Holdings Corp | derivados de azetidina e ciclobutano, seus usos, e composição |
KR101408517B1 (ko) | 2008-03-21 | 2014-06-17 | 노파르티스 아게 | 신규한 헤테로시클릭 화합물 및 그의 용도 |
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 |
WO2010022081A1 (en) | 2008-08-19 | 2010-02-25 | 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 |
NZ605292A (en) | 2008-08-20 | 2014-06-27 | Zoetis Services Llc | Pyrrolo[2,3-d]pyrimidine compounds |
MX2011002362A (es) | 2008-09-02 | 2011-04-04 | Novartis Ag | Inhibidores heterociclicos de cinasa pim. |
EP2342190A1 (en) | 2008-09-02 | 2011-07-13 | Novartis AG | Bicyclic kinase inhibitors |
DK2344474T3 (en) | 2008-09-02 | 2015-12-14 | Novartis Ag | Picolinamidderivater as kinase inhibitors |
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. |
EP2350054A4 (en) | 2008-10-17 | 2012-03-28 | Merck Canada Inc | AZETIDINE DERIVATIVES AS INHIBITORS OF THE STEAROYL COENZYME A DELTA 9 DESATURASE |
JOP20190230A1 (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 |
LT2432472T (lt) | 2009-05-22 | 2020-02-10 | Incyte Holdings Corporation | 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- arba heptan-nitrilas, kaip jak inhibitoriai |
US8716303B2 (en) | 2009-05-22 | 2014-05-06 | Incyte Corporation | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
UA110324C2 (en) | 2009-07-02 | 2015-12-25 | Genentech Inc | Jak inhibitory compounds based on pyrazolo pyrimidine |
CN102574857B (zh) | 2009-07-08 | 2015-06-10 | 利奥制药有限公司 | 作为jak受体和蛋白酪氨酸激酶抑制剂的杂环化合物 |
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 |
US9249145B2 (en) | 2009-09-01 | 2016-02-02 | Incyte Holdings Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
EP2475659B1 (en) | 2009-09-08 | 2015-10-28 | F.Hoffmann-La Roche Ag | 4-substituted pyridin-3-yl-carboxamide compounds and methods of use |
EP2305660A1 (en) | 2009-09-25 | 2011-04-06 | Almirall, S.A. | New thiadiazole derivatives |
MX2012004180A (es) | 2009-10-09 | 2012-07-17 | Incyte Corp | Derivados de hidroxil, ceto y glucuronido de 3-(4-7h-pirrolo[2,3-d ]pirimidin-a-il)-1h-pirazol-1-il)-3-ciclopentilpropanonitrilo. |
MX2012004020A (es) | 2009-10-20 | 2012-05-08 | Cellzome Ltd | Analogos de heterociclilo pirazolopirimidina como inhibidores de jak. |
US20110113416A1 (en) | 2009-11-09 | 2011-05-12 | Bank Of America Corporation | Network-Enhanced Control Of Software Updates Received Via Removable Computer-Readable Medium |
EP2332917B1 (en) | 2009-11-11 | 2012-08-01 | Sygnis Bioscience GmbH & Co. KG | Compounds for PIM kinase inhibition and for treating malignancy |
US9468676B2 (en) | 2009-11-24 | 2016-10-18 | Alderbio Holdings Llc | Antagonists of IL-6 to prevent or treat thrombosis |
US20130129675A1 (en) | 2009-12-04 | 2013-05-23 | Board Of Regents, The University Of Texas System | Interferon therapies in combination with blockade of stat3 activation |
CA2782720A1 (en) | 2009-12-18 | 2011-06-23 | Pfizer Inc. | Pyrrolo[2,3-d]pyrimidine compounds |
KR20140015162A (ko) | 2010-01-12 | 2014-02-06 | 에프. 호프만-라 로슈 아게 | 트라이사이클릭 헤테로사이클릭 화합물, 조성물 및 이의 사용 방법 |
SA111320200B1 (ar) | 2010-02-17 | 2014-02-16 | ديبيوفارم اس ايه | مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة |
EP2536729A1 (en) | 2010-02-18 | 2012-12-26 | Incyte Corporation | Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors |
PL3050882T3 (pl) | 2010-03-10 | 2018-08-31 | Incyte Holdings Corporation | Piperydyn-4-ylowe pochodne azetydyny jako inhibitory JAK1 |
MX2012011941A (es) | 2010-04-14 | 2013-08-27 | Array Biopharma Inc | Imidazo [1, 2-c] pirimidinas 5, 7-substituidas como inhibidores de jak cinasas. |
EP2390252A1 (en) | 2010-05-19 | 2011-11-30 | Almirall, S.A. | New pyrazole derivatives |
BR112012029653B1 (pt) | 2010-05-21 | 2021-01-12 | Incyte Holdings Corporation | formulação farmacêutica para aplicação tópica em pele e seu uso |
US8637529B2 (en) | 2010-06-11 | 2014-01-28 | AbbYie Inc. | Pyrazolo[3,4-d]pyrimidine compounds |
US9351943B2 (en) | 2010-07-01 | 2016-05-31 | Matthew T. McLeay | Anti-fibroblastic fluorochemical emulsion therapies |
WO2012045020A1 (en) | 2010-09-30 | 2012-04-05 | Portola Pharmaceuticals, Inc. | Combinations of 4-(cyclopropylamino)-2-(4-(4-(ethylsulfonyl)piperazin-1-yl)phenylamino)pyrimidine-5-carboxamide and fludarabine |
CN103415515B (zh) | 2010-11-19 | 2015-08-26 | 因塞特公司 | 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物 |
ES2536415T3 (es) | 2010-11-19 | 2015-05-25 | Incyte Corporation | Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK |
US20140073643A1 (en) | 2010-12-03 | 2014-03-13 | Ym Biosciences Australia Pty Ltd | Treatment of jak2-mediated conditions |
ES2547916T3 (es) | 2011-02-18 | 2015-10-09 | Novartis Pharma Ag | Terapia de combinación de inhibidores de mTOR/JAK |
CN102247368B (zh) | 2011-05-19 | 2013-05-29 | 安徽永生堂药业有限责任公司 | 一种复方阿伐斯汀缓释片及其制备方法 |
CN102218042A (zh) | 2011-05-26 | 2011-10-19 | 青岛黄海制药有限责任公司 | 富马酸喹硫平组合物的缓释片剂及其制备方法 |
CA2839767A1 (en) | 2011-06-20 | 2012-12-27 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives 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 |
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 |
EP2741747A1 (en) | 2011-08-10 | 2014-06-18 | 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 |
US9193733B2 (en) | 2012-05-18 | 2015-11-24 | Incyte Holdings 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 |
DK3450434T3 (da) | 2012-06-15 | 2021-05-03 | Concert Pharmaceuticals Inc | Deutererede derivater af ruxolitinib |
EA201590272A1 (ru) | 2012-07-27 | 2015-05-29 | Рациофарм Гмбх | Пероральные дозированные формы для модифицированного высвобождения, содержащие руксолитиниб |
CN102772384A (zh) | 2012-08-07 | 2012-11-14 | 四川百利药业有限责任公司 | 一种盐酸米诺环素缓释片及其制备方法 |
WO2014036016A1 (en) | 2012-08-31 | 2014-03-06 | Principia Biopharma Inc. | Benzimidazole derivatives as itk inhibitors |
EP2917221A1 (en) | 2012-11-01 | 2015-09-16 | Incyte Corporation | Tricyclic fused thiophene derivatives as jak inhibitors |
HUE055894T2 (hu) | 2012-11-15 | 2021-12-28 | Incyte Holdings Corp | A ruxolitinib nyújtott felszabadulású dózisformái |
BR112015021458B1 (pt) | 2013-03-06 | 2022-06-07 | Incyte Holdings Corporation | "processos e intermediários para preparar {1-{1-[3-flúor2-(trifluormetil)isonicotinoil] piperidin-4-il}-3-[4-(7hpirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]azetidin-3-il}acetonitrila, útil no tratamento de doenças relacionadas com a atividade de janus quinases |
HUE043573T2 (hu) | 2013-05-17 | 2019-08-28 | Incyte Corp | Bipirazol só, amely JAK-gátlóként alkalmazható |
KR20160045081A (ko) | 2013-08-07 | 2016-04-26 | 인사이트 코포레이션 | Jak1 억제제용 지속 방출 복용 형태 |
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 |
PL3110409T3 (pl) | 2014-02-28 | 2018-12-31 | Incyte Corporation | Inhibitory jak1 do leczenia zespołów mielodysplastycznych |
PT3129021T (pt) | 2014-04-08 | 2020-11-16 | Incyte Corp | Ratamento de doenças malignas das células b por uma associação de inibidores de jak e pi3k |
CN106687462A (zh) | 2014-04-30 | 2017-05-17 | 因赛特公司 | Jak1抑制剂的制备方法以及其新形式 |
US10363260B2 (en) | 2014-05-28 | 2019-07-30 | Oncotracker, Inc. | Anti-cancer effects of JAK2 inhibitors in combination with thalidomide derivatives and glucocorticoids |
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 |
US10766900B2 (en) | 2017-12-29 | 2020-09-08 | Formosa Laboratories, Inc. | Baricitinib intermediate, method for forming Baricitinib intermediate, and method for preparing Baricitinib or pharmaceutically acceptable salt thereof |
KR20210124345A (ko) | 2019-02-06 | 2021-10-14 | 콘서트 파마슈티컬즈, 인크. | 거울상 이성질체 풍부한 jak 억제제를 제조하는 방법 |
-
2011
- 2011-03-09 PL PL15195698T patent/PL3050882T3/pl unknown
- 2011-03-09 PT PT172110975T patent/PT3354652T/pt unknown
- 2011-03-09 TW TW105101410A patent/TWI592413B/zh active
- 2011-03-09 HU HUE17211097A patent/HUE049914T2/hu unknown
- 2011-03-09 ES ES15195698.4T patent/ES2662588T3/es active Active
- 2011-03-09 MX MX2012010344A patent/MX336932B/es active IP Right Grant
- 2011-03-09 MX MX2018002077A patent/MX364636B/es unknown
- 2011-03-09 RS RS20160205A patent/RS54823B1/sr unknown
- 2011-03-09 MY MYPI2012003994A patent/MY175156A/en unknown
- 2011-03-09 KR KR1020207030868A patent/KR102283091B1/ko active IP Right Grant
- 2011-03-09 KR KR1020217023315A patent/KR102354472B1/ko active IP Right Grant
- 2011-03-09 PL PL17211097T patent/PL3354652T3/pl unknown
- 2011-03-09 LT LTEP15195698.4T patent/LT3050882T/lt unknown
- 2011-03-09 CA CA2792508A patent/CA2792508C/en active Active
- 2011-03-09 HU HUE15195698A patent/HUE037077T2/hu unknown
- 2011-03-09 DK DK15195698.4T patent/DK3050882T3/en active
- 2011-03-09 KR KR1020187013055A patent/KR101911697B1/ko active IP Right Grant
- 2011-03-09 KR KR1020187030015A patent/KR20180117206A/ko active Search and Examination
- 2011-03-09 EP EP11711709.3A patent/EP2545045B1/en active Active
- 2011-03-09 TW TW106118905A patent/TWI643857B/zh active
- 2011-03-09 EP EP20158754.0A patent/EP3715347B1/en active Active
- 2011-03-09 PT PT151956984T patent/PT3050882T/pt unknown
- 2011-03-09 LT LTEP17211097.5T patent/LT3354652T/lt unknown
- 2011-03-09 TW TW100107955A patent/TWI531572B/zh active
- 2011-03-09 SG SG2012064457A patent/SG183551A1/en unknown
- 2011-03-09 SI SI201131892T patent/SI3354652T1/sl unknown
- 2011-03-09 AR ARP110100737A patent/AR081315A1/es active IP Right Grant
- 2011-03-09 EP EP24165623.0A patent/EP4400172A2/en active Pending
- 2011-03-09 PL PL11711709T patent/PL2545045T3/pl unknown
- 2011-03-09 TW TW109116080A patent/TWI766281B/zh active
- 2011-03-09 WO PCT/US2011/027665 patent/WO2011112662A1/en active Application Filing
- 2011-03-09 HU HUE11711709A patent/HUE028723T2/en unknown
- 2011-03-09 PH PH12015502575A patent/PH12015502575A1/en unknown
- 2011-03-09 ES ES17211097T patent/ES2796377T3/es active Active
- 2011-03-09 ME MEP-2016-41A patent/ME02386B/me unknown
- 2011-03-09 EA EA201290894A patent/EA030376B1/ru unknown
- 2011-03-09 ES ES11711709T patent/ES2569539T3/es active Active
- 2011-03-09 NZ NZ602313A patent/NZ602313A/en unknown
- 2011-03-09 TW TW107139196A patent/TWI694826B/zh active
- 2011-03-09 KR KR1020127026216A patent/KR101857680B1/ko active IP Right Grant
- 2011-03-09 NO NO15195698A patent/NO3050882T3/no unknown
- 2011-03-09 US US13/043,986 patent/US8765734B2/en active Active
- 2011-03-09 ES ES20158754T patent/ES2908412T3/es active Active
- 2011-03-09 RS RS20180368A patent/RS57219B1/sr unknown
- 2011-03-09 KR KR1020207008092A patent/KR102172742B1/ko active IP Right Grant
- 2011-03-09 SI SI201131432T patent/SI3050882T1/en unknown
- 2011-03-09 SI SI201130747A patent/SI2545045T1/sl unknown
- 2011-03-09 CN CN201180023757.7A patent/CN102985417B/zh active Active
- 2011-03-09 BR BR112012022513A patent/BR112012022513A2/pt not_active Application Discontinuation
- 2011-03-09 RS RS20200725A patent/RS60680B1/sr unknown
- 2011-03-09 AU AU2011224484A patent/AU2011224484A1/en not_active Abandoned
- 2011-03-09 EP EP21213769.9A patent/EP4036088B1/en active Active
- 2011-03-09 DK DK17211097.5T patent/DK3354652T3/da active
- 2011-03-09 PE PE2012001467A patent/PE20130038A1/es active IP Right Grant
- 2011-03-09 MX MX2016001708A patent/MX347851B/es unknown
- 2011-03-09 DK DK11711709.3T patent/DK2545045T3/en active
- 2011-03-09 KR KR1020227001841A patent/KR20220015492A/ko active Application Filing
- 2011-03-09 JP JP2012557194A patent/JP5858484B2/ja active Active
- 2011-03-09 EP EP17211097.5A patent/EP3354652B1/en active Active
- 2011-03-09 MX MX2017006392A patent/MX354212B/es unknown
- 2011-03-09 EP EP15195698.4A patent/EP3050882B1/en not_active Revoked
-
2012
- 2012-09-06 MX MX2019005232A patent/MX2019005232A/es unknown
- 2012-09-06 IL IL221823A patent/IL221823A/en active IP Right Grant
- 2012-09-10 CL CL2012002501A patent/CL2012002501A1/es unknown
- 2012-09-14 CO CO12158921A patent/CO6602158A2/es unknown
- 2012-10-03 ZA ZA2012/07420A patent/ZA201207420B/en unknown
- 2012-10-03 EC ECSP12012218 patent/ECSP12012218A/es unknown
- 2012-10-08 CR CR20120510A patent/CR20120510A/es unknown
- 2012-11-16 MY MYPI2016000078A patent/MY192255A/en unknown
-
2013
- 2013-04-23 HK HK13104880.0A patent/HK1177741A1/zh unknown
-
2014
- 2014-05-28 US US14/289,121 patent/US9464088B2/en active Active
-
2015
- 2015-12-10 JP JP2015241393A patent/JP6158282B2/ja active Active
-
2016
- 2016-03-24 SM SM201600085T patent/SMT201600085B/it unknown
- 2016-04-01 HR HRP20160326TT patent/HRP20160326T1/hr unknown
- 2016-10-07 US US15/288,641 patent/US9999619B2/en active Active
-
2017
- 2017-06-07 JP JP2017112574A patent/JP6318291B2/ja active Active
-
2018
- 2018-03-09 ME MEP-2018-86A patent/ME03002B/me unknown
- 2018-04-02 JP JP2018070780A patent/JP2018118992A/ja active Pending
- 2018-04-05 HR HRP20180552TT patent/HRP20180552T1/hr unknown
- 2018-04-16 CY CY20181100397T patent/CY1120154T1/el unknown
- 2018-06-01 US US15/995,323 patent/US10695337B2/en active Active
-
2019
- 2019-01-28 HK HK19101408.3A patent/HK1258929A1/zh unknown
-
2020
- 2020-04-09 JP JP2020070257A patent/JP2020114868A/ja active Pending
- 2020-05-19 US US16/878,281 patent/US11285140B2/en active Active
- 2020-07-10 HR HRP20201086TT patent/HRP20201086T1/hr unknown
- 2020-07-22 CY CY20201100671T patent/CY1123175T1/el unknown
-
2022
- 2022-02-17 US US17/674,237 patent/US20230043959A1/en active Pending
-
2023
- 2023-05-17 JP JP2023081459A patent/JP2023099660A/ja active Pending
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
ES2569539T3 (es) | Derivados de piperidin-4-il azetidina como inhibidores de JAK1 | |
AR086983A1 (es) | Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak | |
AR083933A1 (es) | Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak | |
ES2616477T3 (es) | Heterociclaminas como inhibidores de pi3k | |
PE20091100A1 (es) | Nuevos compuestos 010 | |
PE20121431A1 (es) | Derivados de pirimidina como inhbidores de la enzima cinasa ptk2 | |
AR085149A1 (es) | Moduladores del receptor de glucagon | |
PE20130279A1 (es) | Compuestos heteroarilo nitrogenados | |
PE20130306A1 (es) | Morfolinopirimidinas y su uso en terapia | |
PE20161475A1 (es) | Pirazolopiridinas y pirazolopirimidinas | |
AR087591A1 (es) | Derivados de ciclohexil azetidina como inhibidores de jak | |
AR070828A1 (es) | Derivados de azetidina y ciclobutano como inhibidores de jak | |
IN2015MN00464A (es) | ||
AR100806A1 (es) | Inhibidores de fosfatidilinositol 3-quinasa | |
AR070535A1 (es) | Compuestos inhibidores de raf y metodos para usarlos | |
PE20141404A1 (es) | Derivados de tieno[3,2-d]pirimidina que tienen actividad inhibidora por las quinasas de las proteinas | |
AR064010A1 (es) | Inhibidores de la actividad de la akt | |
AR085960A1 (es) | 1,3-oxazinas como inhibidores de la bace1 y/o de la bace2 | |
AR083578A1 (es) | INHIBIDORES DE N/N-LACTAMA ACETIL-CoA CARBOXILASA | |
AR077434A1 (es) | Compuestos para la reduccion de produccion de beta - amiloide | |
AR089776A1 (es) | 5,8-dihidro-6h-pirazolo[3,4-h]quinazolinas como inhibidores de igf-1r/ir | |
AR100810A1 (es) | Inhibidores de fosfatidilinositol 3-quinasa | |
PE20150194A1 (es) | Novedosas n-piridinil amidas ciclicas sustituidas como inhibidores de quinasa | |
AR087288A1 (es) | Compuestos de tetrahidropirido-piridina y tetrahidropirido-pirimidina y su uso como moduladores de receptores de c5a | |
AR086552A1 (es) | 4-aril-n-fenil-1,3,5-triazin-2-aminas que contienen un grupo sulfoximina y composicion farmaceutica |