WO2007002433A1 - Pyrrolo [2, 3-b] pyridine derivatives as protein kinase inhibitors - Google Patents
Pyrrolo [2, 3-b] pyridine derivatives as protein kinase inhibitors Download PDFInfo
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- WO2007002433A1 WO2007002433A1 PCT/US2006/024524 US2006024524W WO2007002433A1 WO 2007002433 A1 WO2007002433 A1 WO 2007002433A1 US 2006024524 W US2006024524 W US 2006024524W WO 2007002433 A1 WO2007002433 A1 WO 2007002433A1
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Definitions
- the invention concerns compounds of Formula I as described below.
- the invention provides novel use of compounds for therapeutic methods involving modulation of protein kinases, as well as novel compounds that can be used for therapeutic methods involving modulation of protein kinases.
- the compounds of Formula I have the following structure:
- Formula Ia all salts, prodrugs, tautomers, and isomers thereof, wherein Y 3 is a bond, -CR a R b - > -A-Ar-Lr, or L, and Y 5 is a bond, -CR a R b -, or L, and each R 27 is independently halogen, provided that Y 3 or Y 5 is a bond, or R 26 , provided, however, that neither of Y 3 R 27 and Y 5 R 27 are hydrogen, wherein R a , R b , L, L 1 , A, Ar and R 26 are as defined with reference to Formula I.
- Y is -S-(alk) b -, -O-(alk) b -, -OC(O)-(alk) b -, -C(O)O-(alk) b -, -OC(S)-(alk) b -, -C(S)O-(alk) b -, -C(O)-(alk) b -, -C(S)-(alk) b -, -C(O)NR 25 -(alk) b -, -OC(O)NR 25 -(alk) b -, -OC(S)NR 25 -(alk) b -, -C(S)NR 25 -(alk) b -, -S(O)-(alk) b -, -S(O) 2 -(alk) b -, -S(S(O) 2 -(alk) b
- Formula Ir all salts, prodrugs, tautomers, and isomers thereof, wherein Y 2 Y 3 and Y 5 are independently a bond, -CR a R b - or L, and each R 27 is independently halogen, provided that Y 2 , Y 3 or Y 5 is a bond, or R 26 , provided, however, that none of Y 2 R 27 , Y 3 R 27 , and Y 5 R 27 are hydrogen, wherein R a , R b , L and R 26 are as defined with reference to Formula I.
- any two of Y 2 , Y 3 and Y 5 are bonds, and the remaining of Y 2 , Y 3 and Y 5 is -CR a R b - or L. In some embodiments, any two of Y 2 , Y 3 and Y 5 are bonds, and the remaining of Y 2 , Y 3 and Y 5 is L.
- Formula I is all salts, prodrugs, tautomers, and isomers thereof, wherein Y 2 Y 3 and Y 6 are independently a bond, -CR a R b -, or L, and each R 27 is independently halogen, provided that Y 2 , Y 3 or Y 6 is a bond, or R 26 , provided, however, that none of Y 2 R 27 , Y 3 R 27 , and Y 6 R 27 are hydrogen, wherein R a , R b , L and R 26 are as defined with reference to Formula I.
- the compound of Formula I has a structure according to the following sub-generic structure Formula Iu:
- Y 3 , Y 4 and Y 5 are bonds.
- Y 3 , Y 4 and Y 5 are independently -CR a R b - or L.
- Y 3 , Y 4 and Y 5 are independently L.
- any one of Y 3 , Y 4 and Y 5 is a bond, and the remaining of Y 3 , Y 4 and Y 5 are independently -CR a R b - or L.
- any one of Y 3 , Y 4 and Y 5 is a bond, and the remaining of Y 3 , Y 4 and Y 5 are independently L.
- any two of Y 3 , Y 4 and Y 5 are bonds, and the remaining of Y 3 , Y 4 and Y 5 is -CR a R b - or L. In some embodiments, any two ofY 3 , Y 4 and Y 5 are bonds, and the remaining of Y 3 , Y 4 and Y 5 is L.
- Formula Ix all salts, prodrugs, tautomers, and isomers thereof, wherein Y 3 Y 4 and Y 6 are independently a bond, -CR a R b -, or L, and each R 27 is independently halogen, provided that Y 3 , Y 4 or Y 6 is a bond, or R 26 , provided, however, that none of Y 3 R 27 , Y 4 R 27 , and Y 6 R 27 are hydrogen, wherein R a , R b , L and R 26 are as defined with reference to Formula I. [0094] In some embodiments of compounds of Formula Ix, Y 3 , Y 4 and Y 6 are bonds.
- Y 3 , Y 4 and Y 6 are independently -CR a R b - or L. In some embodiments, Y 3 , Y 4 and Y 6 are independently L. In some embodiments, any one of Y 3 , Y 4 and Y 6 is a bond, and the remaining of Y 3 , Y 4 and Y 6 are independently -CR a R b - or L. In some embodiments, any one of Y 3 , Y 4 and Y 6 is a bond, and the remaining of Y 3 , Y 4 and Y 6 are independently L.
- Y 3 , Y 5 and Y 6 are bonds. In some embodiments, Y 3 , Y 5 and Y 6 are independently -CR a R b - or L. In some embodiments, Y 3 , Y 5 and Y 6 are independently L. In some embodiments, any one of Y 3 , Y 5 and Y 6 is a bond, and the remaining of Y 3 , Y 5 and Y 6 are independently -CR a R b - or L. In some embodiments, any one of Y 3 , Y 5 and Y 6 is a bond, and the remaining of Y 3 , Y 5 and Y 6 are independently L.
- R 4 , R 5 , R 6 , R 12 , R 13 , R 14 , R 15 and R 16 are hydrogen and A is -CH 2 -, -S- or -S(O) 2 -;
- R 4 , R 6 , R 12 , R 13 , R 14 , R 15 and R 16 are hydrogen, R 5 is -Br or thiophen-3-yl, and A is -C(O)-;
- R 13 is -OH or -OCH 3
- R 4 , R 6 , R 12 , R 14 , R 15 and R 16 are hydrogen
- R 5 is thiophen-2-yl
- A is -CHOH-;
- R 12 is -F
- R 13 is -OCH 3
- R 4 , R 6 , R 14 , R 15 and R 16 are hydrogen
- R 5 is -Br
- A is -C(O)-;
- ⁇ indicates the bond to the 5-position of the 7-azaindole ring
- R 5 is other than hydrogen and R 4 and R 6 are hydrogen, or R 4 is other than hydrogen and R 5 and R 6 are hydrogen, or R 6 is other than hydrogen and R 4 and R 5 are hydrogen, or R 4 and R 5 are other than hydrogen and R 6 is hydrogen, or R 4 and R 6 are other than hydrogen and R 5 is hydrogen, or R 5 and R 6 are other than hydrogen and R 4 is hydrogen, or R 4 , R 5 and R 6 are other than hydrogen and R 4 is hydrogen, or R 4 , R 5 and R 6 are other than hydrogen.
- R 12 and R 16 are independently -LR 24 , any two of R 13 , R 14 and R 15 are independently hydrogen, halogen, optionally fluoro substituted lower alkyl, optionally fluoro substituted lower alkoxy, or optionally fluoro substituted lower alkylthio, and the remaining of R 13 , R 14 and R 15 is hydrogen.
- R 12 and R 16 are independently -LR 24 , any one of R 13 , R 14 and R 15 is independently hydrogen, halogen, optionally fluoro substituted lower alkyl, optionally fluoro substituted lower alkoxy, or optionally fluoro substituted lower alkylthio, and the remaining of R 13 , R 14 and R 15 are hydrogen.
- R 12 and R 16 are independently -LR 24 , and R 13 , R 14 and R 15 are hydrogen. In some embodiments, R 12 and R 16 are other than hydrogen, and R 13 , R 14 and R 15 are hydrogen. In other embodiments, wherein R 12 and R 16 are other than hydrogen, when R 5 , R 6 , R 13 , R 14 and R 15 are hydrogen and A is -C(O)-, then R 12 and R 16 are not both -F.
- R 12 and R 14 are independently -LR 24 , and any one of R 13 , R 15 and R 16 is independently hydrogen, halogen, optionally fluoro substituted lower alkyl, optionally fluoro substituted lower alkoxy, or optionally fluoro substituted lower alkylthio, and the remaining of R 13 , R 15 and R 16 is hydrogen.
- R 12 and R 14 are independently -LR 24 , and any two of R 13 , R 15 and R 16 are independently hydrogen, halogen, optionally fluoro substituted lower alkyl, optionally fluoro substituted lower alkoxy, or optionally fluoro substituted lower alkylthio and the remaining of R 13 , R 15 and R 16 is hydrogen.
- R 24 when L is -O-, R 24 is not H or CH 3 ; and when L is -OCH 2 -, R 24 is not H.
- one of R 12 , R 13 , R 15 , and R 16 is other than hydrogen and the others are hydrogen. In some embodiments, at least one of R 12 , R 13 , R 15 , and R 16 are other than hydrogen. In some embodiments, two of R 12 , R 13 , R 15 , and R 16 are other than hydrogen and the others are hydrogen. In some embodiments, at least two of R 12 , R 13 , R 15 , and R 16 are other than hydrogen.
- any two of R 12 , R 13 , R 15 and R 16 is hydrogen, halogen, optionally fluoro substituted lower alkyl, optionally fluoro substituted lower alkoxy, or optionally fluoro substituted lower alkylthio and the remaining of R 12 , R 13 , R 15 and R 16 are hydrogen.
- R 14 is -LR 24 , -LR 24 is not -NH 2 , -OH, -OCH 3 , -N(CH 3 )* or
- A is -C(O)-
- R !6 is hydrogen and R 12 is halogen, optionally fluoro substituted lower alkyl, optionally fluoro substituted lower alkoxy, or optionally fluoro substituted lower alkylthio; in further embodiments, R 12 is halogen, optionally fluoro substituted Ci -3 alkyl, optionally fluoro substituted C 1-3 alkoxy, or optionally fluoro substituted C 1-3 alkylthio.
- A is -CH 2 -, two of R 12 , R 14 , R 15 and R 16 are independently halogen, optionally fluoro substituted lower alkyl, optionally fluoro substituted lower alkoxy, or optionally fluoro substituted lower alkylthio and the other two of R 12 , R 14 , R 15 and R 15 are hydrogen.
- A is -CH 2 -, R 14 and R 15 are hydrogen and R 12 and R 16 are independently halogen, optionally fluoro substituted lower alkyl, optionally fluoro substituted lower alkoxy, or optionally fluoro substituted lower alkylthio.
- A is -C(O)-, any one of R 12 , R 14 , R 15 and R 16 is halogen, optionally fluoro substituted lower alkyl, optionally fluoro substituted lower alkoxy, or optionally fluoro substituted lower alkylthio and the remaining of R 12 , R 14 , R 15 and R 16 are hydrogen.
- L is -O- or -NH-
- each R 24 is independently hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl
- R 12 and R 16 are independently hydrogen, halogen, optionally fluoro substituted lower alkyl, optionally fluoro substituted lower alkoxy, or optionally fluoro substituted lower alkylthio and R 14 is hydrogen; in further embodiments, A is -CH 2 - or -C(O)-.
- the compounds of Formula III may be used to treat a subject suffering from or at risk for any of the protein kinase mediated diseases or conditions contemplated herein.
- R 57 is selected from the group consisting of lower alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, wherein lower alkyl is optionally substituted with one or more substituents selected from the group consisting of fluoro, lower alkoxy, fluoro substituted lower alkoxy, lower alkylthio, fluoro substituted lower alkylthio, mono-alkylamino, di-alkylamino, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl, provided, however, that any substitution of the alkyl carbon bound to O, S, or N of -OR 57 , -SR 57 , -NR 48 R 57 , -C(O)OR 57 , -C(O)NR 48 R 57 , or -S(O) 2 NR 48 R 57 is fluoro, cycloalkyl, heterocycloalkyl, aryl or heteroaryl, wherein cycl
- Cy is selected from the group consisting of aryl, heteroaryl, cycloalkyl, and heterocycloalkyl;
- R 68 is selected from the group consisting of optionally substituted lower alkyl, optionally substituted lower alkenyl, provided, however, that when R 68 is optionally substituted lower alkenyl, no alkene carbon thereof is bound to N, S, O, S(O), S(O) 2 , C(O) or C(S) of -OR 68 , -SR 68 , -NR 69 R 68 , -C(O)R 68 , -C(S)R 68 , -C(O)OR 68 , -C(O)NR 69 R 68 , -C(S)NR 69 R 68 , -S(O) 2 NR 69 R 68 , -NR 69 C(O)R 68 , -NR 69 C(S)R 68 , -NR 69 S(O) 2 R 68 , -NR 69 C(O)NH 2 , -NR 69 C(O)NR
- R 70 is selected from the group consisting of optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, and optionally substituted heteroaryl;
- R 68 is selected from the group consisting of optionally substituted lower alkyl, optionally substituted lower alkenyl, provided, however, that when R 68 is optionally substituted lower alkenyl, no alkene carbon thereof is bound to N, S, O, S(O), S(O) 2 , C(O) or C(S) of -OR 68 , -SR 68 , -NR 69 R 68 , -C(O)R 68 , -C(S)R 68 , -C(O)OR 68 , -C(O)NR 69 R 68 , -C(S)NR 69 R 68 , -S(O) 2 NR 69 R 68 , -NR 69 C(O)R 68 , -NR 69 C(S)R 68 , -NR 69 S(O) 2 R 68 , -NR 69 C(O)NH 2 , -NR 69 C(O)NR
- R 69 is hydrogen or optionally substituted lower alkyl
- compounds of Formula VIII have the structure according to the following sub-generic structure Formula Villa:
- R 84 is hydrogen.
- a Jnk mediated disease or condition includes a disease or condition for which Jnk inhibition provides a therapeutic benefit, e.g. wherein treatment with Jnk inhibitors, including compounds described herein, provides a therapeutic benefit to the subject suffering from or at risk of the disease or condition.
- the method involves administering to the subject an effective amount of a compound of Formula I in combination with one or more other therapies for the disease or condition.
- the Jnk protein kinase includes, but is not limited to, Jnkl, Jnk2, or Jnk3.
- a compound of Formula HI will selectively inhibit one Jnk kinase relative to one or more other Jnk kinases, such as selectively inhibiting Jnk 1 relative to Jnk 2 and/or Jnk3, selectively inhibiting Jnk2 relative to Jnk3 and/or Jnkl, or selectively inhibiting Jnk3 relative to Jnkl and/or Jnk 2.
- IC 50 for the one kinase may be at least about 2-fold, also 5-fold, also 10-fold, also 20-fold, also 50-fold, or at least about 100-fold less than the IC 50 for any of the other kinases as determined in a generally accepted kinase activity assay.
- kits that include a composition as described herein.
- the composition is packaged, e.g., in a vial, bottle, flask, which may be further packaged, e.g., within a box, envelope, or bag; the composition is approved by the U.S.
- PBD polycystic kidney disease
- IBD inflammatory bowel disease
- ulcerative colitis Crohn's disease
- systemic lupus erythematosis Sjogren's Syndrome
- Wegener's granulomatosis psoriasis
- scleroderma chronic thyroiditis
- Grave's disease myasthenia gravis, multiple sclerosis, osteoarthritis, endometriosis, scarring (e.g.
- compounds of Formula III can be used in the preparation of a medicament for the treatment of a Jnk2-mediated disease or condition, such as atherosclerosis.
- CHKl related to DNA damage repair, sensitizes cells to chemotherapeutic agents
- COPD Chronic Obstructive Pulmonary Disease
- emphysema emphysema
- atherosclerosis emphysema
- metabolic disorders including insulin resistance, hyperglycemia, and lipolysis
- disorders of bone structure or mineralization including osteoporosis, increased risk of fracture, hypercalcemia, and bone metastases
- kidney diseases including nephritis (e.g.
- IKK beta related to leukemia of T-cells, necrosis, insulin resistance, and malignant neoplasms
- Jak2 related to myeloproliferative disorders such as polycythaemia vera, myelofibrosis, essential thrombocythemia, myeloid metaplasia and leukemias, including acute lymphoblastic leukemia, chronic neutrophilic leukemia, juvenile myelomonocytic leukemia, CMML, Philadelphia chromosome-negative CML, megakaryocytic leukemia, and acute erythroid leukemia;
- myeloproliferative disorders such as polycythaemia vera, myelofibrosis, essential thrombocythemia, myeloid metaplasia and leukemias, including acute lymphoblastic leukemia, chronic neutrophilic leukemia, juvenile myelomonocytic leukemia, CMML, Philadelphia chromosome-negative CML, megakaryocytic leukemia, and acute erythroid leukemia;
- PKC-theta related to insulin resistance, T-cell lymphoma
- Halogen refer to all halogens, that is, chloro (Cl), fluoro (F), bromo (Br), or iodo (I).
- substitutions include subsets of these substitutions, such as are indicated herein, for example, in the description of compounds of Formula III, attached at any available atom to produce a stable compound.
- fluoro substituted lower alkynyl denotes a lower alkynyl group substituted with one or more fluoro atoms, where preferably the lower alkynyl is substituted with 1, 2, 3, 4 or 5 fluoro atoms, also 1, 2, or 3 fluoro atoms.
- a “substituted heterocycloalkyl” is a heterocycloalkyl that is independently substituted, unless indicated otherwise, with one or more, preferably 1, 2, 3, 4 or 5, also 1, 2, or 3 substituents, attached at any available atom to produce a stable compound, wherein the substituents are selected from the group consisting of halogen, -OH, -NH 2 , -NO 2 , -CN, -C(O)OH, -C(S)OH, -C(O)NH 2 , -C(S)NH 2 , -S(O) 2 NH 2 , -NHC(O)NH 2 , -NHC(O)NH 2 , -NHC(S)NH 2 , -NHS(O) 2 NH 2 , -C(NH)NH 2 , -OR 0 , -SR 0 , -OC(O)R 0 , -OC(S)R 0 , -C(O)R
- heteroaryl groups include, but are not limited to, pyridinyl, pyridazinyl, pyrazinyl, quinaoxalyl, indolizinyl, benzo[b]thienyl, quinazolinyl, purinyl, indolyl, quinolinyl, pyrimidinyl, pyrrolyl, pyrazolyl, oxazolyl, thiazolyl, thienyl, isoxazolyl, oxathiadiazolyl, isothiazolyl, tetrazolyl, imidazolyl, triazolyl, furanyl, benzofuryl, and indolyl.
- each R g is independently selected from the group consisting of cycloalkyl, heterocycloalkyl, aryl, and heteroaryl, wherein cycloalkyl, heterocycloalkyl, aryl, and heteroaryl are optionally substituted with one or more, preferably 1, 2, 3, 4 or 5, also 1, 2 or 3 substituents selected from the group consisting of halogen, -OH, -NH 2 , -NO 2 , -CN, -C(O)OH, -C(S)OH 5 -C(O)NH 2 , -C(S)NH 2 , -S(O) 2 NH 2 , -NHC(O)NH 2 , -NHC(O)NH 2 , -NHC(S)NH 2 , -NHS(O) 2 NH 2 , -C(NH)NH 2 , -0R k , -SR k , -OC(O)R k , -OC(S)R
- each R u is independently selected from the group consisting of lower alkyl, C 3-6 alkenyl, C 3-6 alkynyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl, wherein lower alkyl is optionally substituted with one or more, preferably 1 , 2, 3, 4 or 5, also 1, 2, or 3 substituents selected from the group consisting of-R y , fluoro, -OH, -NH 2 , lower alkoxy, fluoro substituted lower alkoxy, lower alkylthio, fluoro substituted lower alkylthio, mono-alkylamino, di-alkylamino, and cycloalkylamino, provided, however, that any substitution of the lower alkyl carbon bound to the O of ⁇ OR U , S of -SR U , or N of -NHR" is fluoro or -R y , and wherein C 3-6 alkenyl or C 3-6 alkynyl are optional
- the terms “synergistically effective” or “synergistic effect” indicate that two or more compounds that are therapeutically effective, when used in combination, provide improved therapeutic effects greater than the additive effect that would be expected based on the effect of each compound used by itself.
- the term “modulating” or “modulate” refers to an effect of altering a biological activity, especially a biological activity associated with a particular biomolecule such as a protein kinase.
- a biological activity associated with a particular biomolecule such as a protein kinase.
- an agonist or antagonist of a particular biomolecule modulates the activity of that biomolecule, e.g., an enzyme, by either increasing (e.g. agonist, activator), or decreasing (e.g. antagonist, inhibitor) the activity of the biomolecule, such as an enzyme.
- Such activity is typically indicated in terms of an inhibitory concentration (IC 50 ) or excitation concentration (Ji ( J 5 O) of the compound for an inhibitor or activator, respectively, with respect to, for example, an enzyme.
- Akt3 may contribute to the more aggressive clinical phenotype of the estrogen receptor-negative breast cancers and androgen-insensitive prostate carcinomas and inhibitors may provide therapeutic benefits in treating these cancers.
- Akt3 inhibitors may be useful in treating cancer, including estrogen receptor-negative breast cancers, androgen- insensitive prostate carcinomas, and melanomas.
- Anaplastic large cell lymphoma comprises 10-15% of childhood non-Hodgkin lymphomas (NHL) (Perkins et al., Br J Haematol 2005, 131(5):624-7).
- Marzec et al. states aberrant expression of the ALK tyrosine kinase as a chimeric protein with nucleophosmin (NPM) and other partners plays a key role in malignant cell transformation of T-lymphocytes and other cells.
- thrombotic microangiopathy syndromes thrombotic microangiopathy syndromes
- atherosclerosis reperfusion injury
- inflammation including, but not limited to, psoriasis, polycystic kidney disease (PKD), arthritis and autoimmune diseases and conditions, osteoarthritis, endometriosis, scarring, vascular restenosis, fibrotic disorders, rheumatoid arthritis, inflammatory bowel disease (IBD); immunodeficiency diseases, organ transplant rejection, graft versus host disease; renal or prostatic diseases including diabetic nephropathy, nephrosclerosis, glomerulonephritis, prostate hyperplasia; metabolic disorders, obesity; infection, including, but not limited to Helicobacter pylori and Influenza virus, fever, sepsis; pulmonary diseases including chronic obstructive pulmonary disease (COPD) and acute respiratory distress syndrome (ARDS); genetic developmental diseases such as Noonan's syndrome, Costello syndrome, (faciocutaneoskeletal syndrome), leopard
- Cdk2 Target kinase Cdk2 (i.e., Cyclin dependent kinase 2) is a 33.9 kDa serine/threonine kinase (STK) encoded by chromosome 12ql3 (symbol: CDK2).
- Cdk2 is also known as p33 protein kinase, and cell division protein kinase 2.
- De Bondt et al. reported the X-ray crystallographic structure of Cdk2 (De Bondt et al., Nature 1993, 363: 595-602).
- Cdk2 is involved in control of the human cell cycle. Cdk2 activation requires association with cyclins and leads to cell proliferation.
- Cdk6 Target kinase Cdk6 (i.e., Cyclin dependent kinase 6) is a 36.9 kDa STK encoded by chromosome 7q21-q22 (symbol: CDK6).
- Lam et al. reported expression of CDK4 and CDK6 was elevated relative to matched normal brain tissue in eight of 18 glioblastoma multiforme (GBM) tumours (44%). Their data attests to the functional importance of both CDK4 and CDK6 in astrocytic tumourigenesis, particularly during the later stages of tumour progression (Lam et al., Br J Neurosurg 2000, 14(l):28-32).
- Csk Target kinase
- Csk i.e., c Src kinase
- CSK Chromogene kinase
- Csk cloned by Partanen et al. (Oncogene 1991, 6: 2013- 2018), is a cytoplasmic tyrosine kinase that downregulates the tyrosine kinase activity of the Src oncoprotein through tyrosine phosphorylation of the Src carboxy terminus.
- EPH gene mRNA was detected in liver, lung, kidney, and testes of rat; screening of 25 human cancers of various cell types showed preferential expression in cells of epithelial origin. Overexpression of EPH mRNA was found in a hepatoma and a lung cancer without gene amplification.
- Southern blot analysis of DNAs from human-mouse hybrid clones with an EPH probe showed that this gene is present on human chromosome 7.
- Two other receptor tyrosine kinase genes, MET and EGFR are on the same chromosome.
- Yoshida et al. (1989) assigned the EPH locus to 7q32-q36.
Priority Applications (11)
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EP06773861A EP1893612B1 (en) | 2005-06-22 | 2006-06-21 | Pyrrolo [2, 3-b]pyridine derivatives as protein kinase inhibitors |
AU2006261993A AU2006261993B2 (en) | 2005-06-22 | 2006-06-21 | Pyrrolo (2, 3-B) pyridine derivatives as protein kinase inhibitors |
DK06773861.7T DK1893612T3 (da) | 2005-06-22 | 2006-06-21 | Pyrrol [2,3-B]pyridin-derivater som proteinkinasehæmmere |
ES06773861T ES2371397T3 (es) | 2005-06-22 | 2006-06-21 | Derivados de pirrolo[2,3-b]piridina como inhibidores de proteínas cinasas. |
CA2613015A CA2613015C (en) | 2005-06-22 | 2006-06-21 | Pyrrolo [2, 3-b] pyridine derivatives as protein kinase inhibitors |
AT06773861T ATE518860T1 (de) | 2005-06-22 | 2006-06-21 | Pyrroloä2,3-büpyridinderivate als proteinkinaseinhibitoren |
PL06773861T PL1893612T3 (pl) | 2005-06-22 | 2006-06-21 | Pochodne pirolo-[2,3-b]pirydyny jako inhibitory kinazy białkowej |
HK08109870.8A HK1114610A1 (en) | 2005-06-22 | 2008-09-05 | Pyrrolo [2, 3-b]pyridine derivatives as protein kinase inhibitors |
DE201212000043 DE122012000043I1 (de) | 2005-06-22 | 2012-06-26 | Pyrrolo[2,3-B]pyridinderivate als proteinkinaseinhibitoren. |
LU92035C LU92035I2 (fr) | 2005-06-22 | 2012-06-28 | Vemurafenib et les sels pharmaceutiquement acceptables de celui-ci, sous toutes les formes bénéficiant de la protection conférée par le brevet de base |
CY2012021C CY2012021I2 (el) | 2005-06-22 | 2012-07-31 | Παραγωγα πυρρολο[2,3-β]πυριδινης ως αναστολεις κινασης προτεϊνης |
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Cited By (223)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2007084667A2 (en) * | 2006-01-19 | 2007-07-26 | Osi Pharmaceutical, Inc. | Fused heterobicyclic kinase inhibitors |
WO2007116866A1 (ja) | 2006-04-03 | 2007-10-18 | Astellas Pharma Inc. | ヘテロ化合物 |
WO2008003736A1 (en) * | 2006-07-06 | 2008-01-10 | Solvay Pharmaceuticals B.V. | Azaindole derivatives with a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition |
WO2008025947A1 (en) * | 2006-08-31 | 2008-03-06 | Vernalis (R & D) Ltd. | 1h-pyrrolo[2,3-b]pyridine derivatives useful as hsp90 inhibitors |
WO2008079903A1 (en) * | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Pyrrolo [2, 3-b] pyridine derivatives as kinase modulators |
WO2008080015A2 (en) * | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
WO2008079909A1 (en) * | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Pyrrolo [2,3-b] pyridines as kinase modulators |
WO2009026239A1 (en) * | 2007-08-17 | 2009-02-26 | University Of Maryland, Baltimore | Small molecule inhibitors of lck sh2 domain binding |
EP2036990A1 (en) | 2007-09-11 | 2009-03-18 | Roche Diagnostics GmbH | Diagnostic test for susceptibility to B-Raf kinase inhibitors |
US7507826B2 (en) | 2004-03-30 | 2009-03-24 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of JAK and other protein kinases |
DE102007045919A1 (de) | 2007-09-26 | 2009-04-09 | Bayer Cropscience Ag | Wirkstoffkombinationen mit insektiziden und akariziden Eigenschaften |
DE102007045956A1 (de) | 2007-09-26 | 2009-04-09 | Bayer Cropscience Ag | Wirkstoffkombination mit insektiziden und akariziden Eigenschaften |
WO2009089352A1 (en) | 2008-01-08 | 2009-07-16 | Array Biopharma Inc. | Pyrrolopyridines as kinase inhibitors |
WO2009111280A1 (en) | 2008-02-29 | 2009-09-11 | Array Biopharma Inc. | N- (6-aminopyridin-3-yl) -3- (sulfonamido) benzamide derivatives as b-raf inhibitors for the treatment of cancer |
WO2009141274A1 (en) * | 2008-05-21 | 2009-11-26 | Basf Se | Substituted pyridin-4 -yl-methyl sulfonamides as fungicides |
WO2009144159A1 (en) * | 2008-05-28 | 2009-12-03 | Basf Se | Substituted pyridin-4-yl-methyl sulfonamidesas fungicides |
WO2009157196A1 (ja) | 2008-06-25 | 2009-12-30 | 武田薬品工業株式会社 | アミド化合物 |
DE102008052943A1 (de) | 2008-10-23 | 2010-04-29 | Merck Patent Gmbh | Azaindolderivate |
US7767816B2 (en) | 2006-01-17 | 2010-08-03 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of janus kinases |
WO2010104945A1 (en) | 2009-03-11 | 2010-09-16 | Plexxikon, Inc. | Pyrrolo [2, 3-b] pyridine derivatives for the inhibition of raf kinases |
WO2010104973A1 (en) * | 2009-03-11 | 2010-09-16 | Plexxikon, Inc. | Pyrrolo [2, 3-b] pyridine derivatives for the inhibition of raf kinases |
WO2010111527A1 (en) * | 2009-03-26 | 2010-09-30 | Plexxikon, Inc. | Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use |
US7846941B2 (en) | 2005-05-17 | 2010-12-07 | Plexxikon, Inc. | Compounds modulating c-kit and c-fms activity and uses therefor |
US7863288B2 (en) | 2005-06-22 | 2011-01-04 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
US7879844B2 (en) | 2005-12-28 | 2011-02-01 | Astellas Pharma Inc. | Heterocyclic janus kinase 3 inhibitors |
WO2011015522A2 (en) | 2009-08-03 | 2011-02-10 | F. Hoffmann-La Roche Ag | Process for the manufacture of pharmaceutically active compounds |
US7893075B2 (en) * | 2006-11-22 | 2011-02-22 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
WO2011025938A2 (en) | 2009-08-28 | 2011-03-03 | Array Biopharma Inc. | Raf inhibitor compounds and methods of use thereof |
WO2011025951A1 (en) | 2009-08-28 | 2011-03-03 | Array Biopharma Inc. | Raf inhibitor compounds and methods of use thereof |
WO2011025940A1 (en) | 2009-08-28 | 2011-03-03 | Array Biopharma Inc. | Raf inhibitor compounds and methods of use thereof |
WO2011025968A1 (en) | 2009-08-28 | 2011-03-03 | Array Biopharma Inc. | 1h-pyrazolo [ 3, 4-b] pyridine compounds for inhibiting raf kinase |
WO2011025947A1 (en) | 2009-08-28 | 2011-03-03 | Array Biopharma Inc. | Raf inhibitor compounds and methods of use thereof |
WO2011025965A1 (en) | 2009-08-28 | 2011-03-03 | Genentech, Inc. | Raf inhibitor compounds and methods of use thereof |
JP2011510004A (ja) * | 2008-01-22 | 2011-03-31 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | タンパク質キナーゼ阻害剤及びその使用 |
WO2011057022A1 (en) | 2009-11-06 | 2011-05-12 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
WO2011057974A1 (en) | 2009-11-11 | 2011-05-19 | F. Hoffmann-La Roche Ag | Propane-i-sulfonic acid {3-[5-(4-chloro-phenyl)-1h-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide compositions and uses thereof |
US7947708B2 (en) | 2004-06-17 | 2011-05-24 | Plexxikon, Inc. | Compounds modulating C-kit activity |
WO2011063159A1 (en) | 2009-11-18 | 2011-05-26 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
US7964728B2 (en) | 2006-07-06 | 2011-06-21 | Solvay Pharmaceuticals B.V. | Azaindole derivatives with a combination of partial nicotinic acetyl-choline receptor agonism and dopamine reuptake inhibition |
WO2011085129A3 (en) * | 2010-01-06 | 2011-09-01 | Errico Joseph P | Methods and compositions of targeted drug development |
WO2011128455A1 (en) | 2010-04-16 | 2011-10-20 | Ac Immune S.A. | Novel compounds for the treatment of diseases associated with amyloid or amyloid-like proteins |
WO2011143645A1 (en) | 2010-05-14 | 2011-11-17 | OSI Pharmaceuticals, LLC | Fused bicyclic kinase inhibitors |
WO2011143646A1 (en) | 2010-05-14 | 2011-11-17 | OSI Pharmaceuticals, LLC | Fused bicyclic kinase inhibitors |
US8067434B2 (en) | 2003-12-19 | 2011-11-29 | Plexxikon Inc. | Compounds and methods for development of Ret modulators |
WO2012010538A2 (en) | 2010-07-21 | 2012-01-26 | F. Hoffmann-La Roche Ag | Novel processes for the manufacture of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1h-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide |
US8110576B2 (en) | 2008-06-10 | 2012-02-07 | Plexxikon Inc. | Substituted pyrrolo[2,3b]pyrazines and methods for treatment of raf protein kinase-mediated indications |
US8119637B2 (en) | 2008-06-10 | 2012-02-21 | Plexxikon Inc. | Substituted pyrrolo[2,3-b]pyrazines and methods for kinase modulation, and indications therefor |
US8153641B2 (en) | 2008-05-19 | 2012-04-10 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
US8158636B2 (en) | 2008-05-19 | 2012-04-17 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
US8163767B2 (en) | 2005-07-14 | 2012-04-24 | Astellas Pharma Inc. | Heterocyclic Janus Kinase 3 inhibitors |
US8183245B2 (en) | 2007-10-25 | 2012-05-22 | Merck Sharp & Dohme Corp. | Pyrazine substituted pyrrolopyridines as inhibitors of JAK and PDK1 |
WO2012075327A1 (en) | 2010-12-02 | 2012-06-07 | University Of Pittsburgh-Of The Commonwealth System Of Higher Education | Methods for treating a tumor using an antibody that specifically binds grp94 |
US8198273B2 (en) | 2009-05-06 | 2012-06-12 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
WO2012109075A1 (en) | 2011-02-07 | 2012-08-16 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
US8247421B2 (en) | 2006-12-21 | 2012-08-21 | Vertex Pharmaceuticals Incorporated | 5-cyano-4-(pyrrolo [2,3B] pyridine-3-yl)-pyrimidine derivatives useful as protein kinase inhibitors |
WO2012158658A1 (en) | 2011-05-16 | 2012-11-22 | OSI Pharmaceuticals, LLC | Fused bicyclic kinase inhibitors |
WO2012161776A1 (en) | 2011-02-21 | 2012-11-29 | Plexxikon Inc. | Solid forms of a pharmaceutically active substance |
WO2012170752A1 (en) * | 2011-06-10 | 2012-12-13 | Glaxo Wellcome Manufacturing Pte Ltd | Novel compounds |
US8338452B2 (en) | 2008-02-29 | 2012-12-25 | Array Biopharma Inc. | Raf inhibitor compounds and methods of use thereof |
US8372842B2 (en) | 2008-01-09 | 2013-02-12 | Array Biopharma Inc. | Pyrazolopyridines as kinase inhibitors |
US8394795B2 (en) | 2008-02-29 | 2013-03-12 | Array Biopharma Inc. | Pyrazole [3, 4-B] pyridine Raf inhibitors |
EP2566481A1 (en) * | 2010-05-06 | 2013-03-13 | Merck Sharp & Dohme Corp. | Aza-indole derivatives useful as modulators of faah |
WO2013043715A1 (en) | 2011-09-19 | 2013-03-28 | Genentech, Inc. | Combination treatments comprising c-met antagonists and b-raf antagonists |
JP2013513627A (ja) * | 2009-12-14 | 2013-04-22 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | 癌などの疾患を処置するためのチアゾール誘導体 |
JP2013519684A (ja) * | 2010-02-11 | 2013-05-30 | ヴァンダービルト ユニバーシティー | mGluR4アロステリック増強剤としてのピラゾロピリジン、ピラゾロピラジン、ピラゾロピリミジン、ピラゾロチオフェンおよびピラゾロチアゾール化合物、組成物、および神経機能不全を治療する方法 |
WO2013142427A1 (en) | 2012-03-19 | 2013-09-26 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
US8592448B2 (en) | 2008-11-20 | 2013-11-26 | OSI Pharmaceuticals, LLC | Substituted pyrrolo[2,3-b]-pyridines and -pyrazines |
WO2013181415A1 (en) | 2012-05-31 | 2013-12-05 | Plexxikon Inc. | Synthesis of pyrrolo [2, 3 - b] pyridines |
US8648086B2 (en) | 2009-08-24 | 2014-02-11 | Ascepion Pharmaceuticals, Inc. | 5,6-bicyclic heteroaryl-containing urea compounds as kinase inhibitors |
US8658170B2 (en) | 2010-01-06 | 2014-02-25 | Joseph P. Errico | Combination therapy with MDM2 and EFGR inhibitors |
JP2014040460A (ja) * | 2008-02-25 | 2014-03-06 | F. Hoffmann-La Roche Ag | ピロロピラジンキナーゼ阻害剤 |
US8691807B2 (en) | 2011-06-20 | 2014-04-08 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors |
US8722693B2 (en) | 2007-06-13 | 2014-05-13 | Incyte Corporation | Salts of the Janus kinase inhibitor (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
WO2014130856A2 (en) * | 2013-02-21 | 2014-08-28 | Wayne Rothbaum | Treatment of skeletal-related disorders |
WO2014128235A1 (en) | 2013-02-22 | 2014-08-28 | F. Hoffmann-La Roche Ag | Methods of treating cancer and preventing drug resistance |
EP2771011A1 (en) * | 2011-10-24 | 2014-09-03 | Glaxosmithkline Intellectual Property (No. 2) Limited | Chemical compounds |
US8829007B2 (en) | 2009-06-17 | 2014-09-09 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
WO2014144850A1 (en) | 2013-03-15 | 2014-09-18 | Genentech, Inc. | Methods of treating cancer and preventing cancer drug resistance |
US8871774B2 (en) | 2010-12-16 | 2014-10-28 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
WO2014194127A1 (en) | 2013-05-30 | 2014-12-04 | Plexxikon Inc. | Compounds for kinase modulation, and indications therefor |
WO2014206344A1 (en) | 2013-06-28 | 2014-12-31 | Beigene, Ltd. | Fused tricyclic amide compounds as multiple kinase inhibitors |
US8933085B2 (en) | 2010-11-19 | 2015-01-13 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
US8933086B2 (en) | 2005-12-13 | 2015-01-13 | Incyte Corporation | Heteroaryl substituted pyrrolo[2,3-B]pyridines and pyrrolo[2,3-B]pyrimidines as Janus kinase inhibitors |
US8937088B2 (en) | 2011-01-06 | 2015-01-20 | Astar Biotech Llc | Ureas for the treatment and prevention of cancer |
JP2015052009A (ja) * | 2008-11-25 | 2015-03-19 | ユニバーシティー オブ ロチェスター | Mlk阻害剤および使用方法 |
US8987443B2 (en) | 2013-03-06 | 2015-03-24 | Incyte Corporation | Processes and intermediates for making a JAK inhibitor |
US9034884B2 (en) | 2010-11-19 | 2015-05-19 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors |
US20150141428A1 (en) * | 2012-05-22 | 2015-05-21 | Merck Sharp & Dohme Corp. | TrkA Kinase Inhibitors, Compositions and Methods Thereof |
WO2015078424A1 (en) | 2013-11-27 | 2015-06-04 | Zentiva, K.S. | Crystalline forms of vemurafenib |
US9051319B2 (en) | 2011-08-01 | 2015-06-09 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
US9163021B2 (en) | 2012-10-04 | 2015-10-20 | Pfizer Limited | Pyrrolo[3,2-c]pyridine tropomyosin-related kinase inhibitors |
US9193733B2 (en) | 2012-05-18 | 2015-11-24 | Incyte Holdings Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
US9200004B2 (en) | 2013-01-15 | 2015-12-01 | Incyte Holdings Corporation | Thiazolecarboxamides and pyridinecarboxamide compounds useful as Pim kinase inhibitors |
WO2015191986A1 (en) | 2014-06-13 | 2015-12-17 | Genentech, Inc. | Methods of treating and preventing cancer drug resistance |
US9216984B2 (en) | 2009-05-22 | 2015-12-22 | Incyte Corporation | 3-[4-(7H-pyrrolo[2,3-D]pyrimidin-4-yl)-1H-pyrazol-1-yl]octane—or heptane-nitrile as JAK inhibitors |
WO2016011160A1 (en) | 2014-07-15 | 2016-01-21 | Genentech, Inc. | Compositions for treating cancer using pd-1 axis binding antagonists and mek 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 |
JP2016504316A (ja) * | 2012-12-14 | 2016-02-12 | アーリーン ファーマシューティカルズ エルエルシー | 塩誘導性キナーゼ2(SIK2)阻害剤としての置換された1H−ピロロ[2,3−b]ピリジン及び1H−ピラゾロ[3,4−b]ピリジン誘導体 |
US20160046636A1 (en) * | 2009-12-29 | 2016-02-18 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
US9278950B2 (en) | 2013-01-14 | 2016-03-08 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
EP2282636B1 (en) | 2008-05-06 | 2016-03-23 | Novartis AG | Benzene sulfonamide thiazole and oxazole compounds |
WO2016057367A1 (en) | 2014-10-06 | 2016-04-14 | Dana-Farber Cancer Institute, Inc. | Angiopoietin-2 biomarkers predictive of anti-immune checkpoint response |
US9334274B2 (en) | 2009-05-22 | 2016-05-10 | Incyte Holdings 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 |
US9359445B2 (en) | 2010-03-25 | 2016-06-07 | The J. David Gladstone Institutes | Compositions and methods for treating neurological disorders |
US9358229B2 (en) | 2011-08-10 | 2016-06-07 | Novartis Pharma Ag | JAK PI3K/mTOR combination therapy |
US9359358B2 (en) | 2011-08-18 | 2016-06-07 | Incyte Holdings Corporation | Cyclohexyl azetidine derivatives as JAK inhibitors |
US9382241B2 (en) | 2012-05-31 | 2016-07-05 | Genentech, Inc. | Aminoquinazoline and pyridopyrimidine derivatives |
US9399639B2 (en) | 2012-08-27 | 2016-07-26 | Calitor Sciences, Llc | Substituted azaindole compounds, salts, pharmaceutical compositions thereof and methods of use |
US9440969B2 (en) | 2009-12-23 | 2016-09-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
US9464088B2 (en) | 2010-03-10 | 2016-10-11 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as JAK1 inhibitors |
US9469640B2 (en) | 2007-07-17 | 2016-10-18 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
WO2016165676A1 (en) | 2015-04-14 | 2016-10-20 | Zentiva, K.S. | Amorphous forms of vemurafenib |
US9487521B2 (en) | 2011-09-07 | 2016-11-08 | Incyte Holdings Corporation | Processes and intermediates for making a JAK inhibitor |
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 |
WO2016191295A1 (en) | 2015-05-22 | 2016-12-01 | Plexxikon Inc. | Solid forms of a compound for modulating kinases |
JP2016540045A (ja) * | 2013-11-15 | 2016-12-22 | ザ ウィスター インスティテュート オブ アナトミー アンド バイオロジー | Ebna1阻害剤およびそれらの使用方法 |
US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
WO2017011776A1 (en) | 2015-07-16 | 2017-01-19 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
US9550768B2 (en) | 2011-05-17 | 2017-01-24 | Plexxikon Inc. | Kinase modulation and indications therefor |
US9556197B2 (en) | 2013-08-23 | 2017-01-31 | Incyte Corporation | Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors |
EP3124472A1 (en) | 2011-12-31 | 2017-02-01 | BeiGene, Ltd. | Fused tricyclic compounds as raf kinase inhibitors |
US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
US9580416B2 (en) | 2014-07-02 | 2017-02-28 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase |
US9593317B2 (en) | 2010-06-09 | 2017-03-14 | Bayer Cropscience Nv | Methods and means to modify a plant genome at a nucleotide sequence commonly used in plant genome engineering |
US9655854B2 (en) | 2013-08-07 | 2017-05-23 | Incyte Corporation | Sustained release dosage forms for a JAK1 inhibitor |
WO2017087851A1 (en) | 2015-11-19 | 2017-05-26 | Genentech, Inc. | Methods of treating cancer using b-raf inhibitors and immune checkpoint inhibitors |
JP2017516814A (ja) * | 2014-06-03 | 2017-06-22 | ギリアード サイエンシーズ, インコーポレイテッド | Tank結合キナーゼインヒビター化合物 |
US9758522B2 (en) | 2012-10-19 | 2017-09-12 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
US9771361B2 (en) | 2013-11-13 | 2017-09-26 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
WO2017176751A1 (en) | 2016-04-04 | 2017-10-12 | Loxo Oncology, Inc. | Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
WO2017176744A1 (en) | 2016-04-04 | 2017-10-12 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
WO2017180581A1 (en) | 2016-04-15 | 2017-10-19 | Genentech, Inc. | Diagnostic and therapeutic methods for cancer |
US9822124B2 (en) | 2014-07-14 | 2017-11-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors |
WO2018002415A1 (en) | 2016-07-01 | 2018-01-04 | Fermion Oy | New processes for the preparation of vemurafenib |
US9862705B2 (en) | 2015-09-09 | 2018-01-09 | Incyte Corporation | Salts of a pim kinase inhibitor |
US9862688B2 (en) | 2014-04-23 | 2018-01-09 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged janus kinase inhibitors and uses thereof |
US9920032B2 (en) | 2015-10-02 | 2018-03-20 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
WO2018050286A1 (en) * | 2016-09-16 | 2018-03-22 | Helmholtz Zentrum Muenchen - Deutsches Forschungszentrum Für Gesundheit Und Umwelt (Gmbh) | Traf 6 inhibitors |
WO2018071454A1 (en) | 2016-10-10 | 2018-04-19 | Andrews Steven W | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
WO2018071447A1 (en) | 2016-10-10 | 2018-04-19 | Andrews Steven W | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
US9993480B2 (en) | 2011-02-18 | 2018-06-12 | Novartis Pharma Ag | mTOR/JAK inhibitor combination therapy |
US10000483B2 (en) | 2012-10-19 | 2018-06-19 | Dana-Farber Cancer Institute, Inc. | Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof |
US10017477B2 (en) | 2014-04-23 | 2018-07-10 | Dana-Farber Cancer Institute, Inc. | Janus kinase inhibitors and uses thereof |
US10023569B2 (en) | 2013-11-13 | 2018-07-17 | Vertex Pharmaceuticals Incorporated | Methods of preparing inhibitors of influenza viruses replication |
WO2018136661A1 (en) | 2017-01-18 | 2018-07-26 | Andrews Steven W | SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS |
WO2018134254A1 (en) | 2017-01-17 | 2018-07-26 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
US10040781B2 (en) | 2014-09-26 | 2018-08-07 | Gilead Sciences, Inc. | Tank-binding kinase inhibitor compounds |
US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
WO2018146253A1 (en) | 2017-02-10 | 2018-08-16 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the mapk pathway |
WO2018170381A1 (en) | 2017-03-16 | 2018-09-20 | Andrews Steven W | Macrocyclic compounds as ros1 kinase inhibitors |
WO2018175324A1 (en) | 2017-03-20 | 2018-09-27 | The Broad Institute, Inc. | Compounds and methods for regulating insulin secretion |
US10112927B2 (en) | 2012-10-18 | 2018-10-30 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
WO2018210661A1 (en) * | 2017-05-15 | 2018-11-22 | Basf Se | Heteroaryl compounds as agrochemical fungicides |
WO2018213810A1 (en) * | 2017-05-19 | 2018-11-22 | Nflection Therapeutics, Inc. | Pyrrolopyridine-aniline compounds for treatment of dermal disorders |
US10144730B2 (en) | 2011-11-17 | 2018-12-04 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-Jun-N-terminal kinase (JNK) |
US10166191B2 (en) | 2012-11-15 | 2019-01-01 | Incyte Corporation | Sustained-release dosage forms of ruxolitinib |
WO2019051296A1 (en) | 2017-09-08 | 2019-03-14 | Genentech, Inc. | DIAGNOSTIC AND THERAPEUTIC METHODS OF CANCER |
US10251889B2 (en) | 2009-07-09 | 2019-04-09 | Array BioPharm Inc. | Substituted pyrazolo[1,5-a]pyrimidine compounds as Trk kinase inhibitors |
WO2019075108A1 (en) | 2017-10-10 | 2019-04-18 | Metcalf Andrew T | CRYSTALLINE FORMS |
WO2019075114A1 (en) | 2017-10-10 | 2019-04-18 | Mark Reynolds | FORMULATIONS COMPRISING 6- (2-HYDROXY-2-METHYLPROPOXY) -4- (6- (6 - ((6-METHOXYPYRIDIN-3-YL) METHYL) -3,6-DIAZABICYCLO [3.1.1] HEPTAN-3- YL) PYRIDIN-3-YL) PYRAZOLO [1,5-A] pYRIDINE-3-carbonitrile |
US10273233B2 (en) | 2015-05-13 | 2019-04-30 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
US10316049B2 (en) | 2015-12-17 | 2019-06-11 | Gilead Sciences, Inc. | Tank-binding kinase inhibitor compounds |
WO2019133810A1 (en) | 2017-12-28 | 2019-07-04 | Tract Pharmaceuticals, Inc. | Stem cell culture systems for columnar epithelial stem cells, and uses related thereto |
WO2019143977A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
WO2019143994A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
WO2019149738A1 (en) | 2018-01-31 | 2019-08-08 | Heparegenix Gmbh | Protein kinase mkk4 inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
WO2019158579A1 (en) | 2018-02-13 | 2019-08-22 | Vib Vzw | Targeting minimal residual disease in cancer with rxr antagonists |
EP3550031A1 (en) | 2012-07-24 | 2019-10-09 | Pharmacyclics, LLC | Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk) |
US10442763B2 (en) | 2015-05-14 | 2019-10-15 | The Wistar Institute Of Anatomy And Biology | EBNA1 inhibitors and methods using same |
WO2019243315A1 (en) | 2018-06-21 | 2019-12-26 | Heparegenix Gmbh | Tricyclic protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
US10533004B2 (en) | 2015-05-13 | 2020-01-14 | Vertex Pharmaceuticals Incorporated | Methods of preparing inhibitors of influenza viruses replication |
WO2020016243A1 (en) | 2018-07-16 | 2020-01-23 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
US10550121B2 (en) | 2015-03-27 | 2020-02-04 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
WO2020028258A1 (en) | 2018-07-31 | 2020-02-06 | Loxo Oncology, Inc. | Spray-dried dispersions and formulations of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoro propan-2-yl)-1h-pyrazole-4-carboxamide |
WO2020055672A1 (en) | 2018-09-10 | 2020-03-19 | Array Biopharma Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
US10596161B2 (en) | 2017-12-08 | 2020-03-24 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
WO2020070390A1 (en) | 2018-10-03 | 2020-04-09 | Jyväskylän Yliopisto | Vemurafenib and salts thereof for use in the treatment of enteroviral infections |
WO2020079581A1 (en) | 2018-10-16 | 2020-04-23 | Novartis Ag | Tumor mutation burden alone or in combination with immune markers as biomarkers for predicting response to targeted therapy |
US10646567B2 (en) | 2011-08-01 | 2020-05-12 | Genentech, Inc. | Methods of treating cancer using PD-1 axis binding antagonists and MEK inhibitors |
WO2020102686A1 (en) * | 2018-11-16 | 2020-05-22 | California Institute Of Technology | Erk inhibitors and uses thereof |
WO2020131674A1 (en) | 2018-12-19 | 2020-06-25 | Array Biopharma Inc. | 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer |
WO2020131627A1 (en) | 2018-12-19 | 2020-06-25 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases |
US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
US10724102B2 (en) | 2015-10-26 | 2020-07-28 | Loxo Oncology, Inc. | Point mutations in TRK inhibitor-resistant cancer and methods relating to the same |
US10758543B2 (en) | 2010-05-21 | 2020-09-01 | Incyte Corporation | Topical formulation for a JAK inhibitor |
US10849980B2 (en) | 2014-12-23 | 2020-12-01 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
WO2020239124A1 (en) * | 2019-05-31 | 2020-12-03 | Fochon Pharmaceuticals, Ltd. | SUBSTITUTED PYRROLO [2, 3-b] PYRIDINE AND PYRAZOLO [3, 4-b] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS |
WO2020243519A1 (en) * | 2019-05-29 | 2020-12-03 | Ifm Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
US10870651B2 (en) | 2014-12-23 | 2020-12-22 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
US10899736B2 (en) | 2018-01-30 | 2021-01-26 | Incyte Corporation | Processes and intermediates for making a JAK inhibitor |
US10906889B2 (en) | 2013-10-18 | 2021-02-02 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7) |
WO2021018820A1 (en) | 2019-07-29 | 2021-02-04 | Heparegenix Gmbh | Heteroaryl-substituted pyrazolo-pyridine protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
AU2016297558B2 (en) * | 2015-07-20 | 2021-03-25 | Genzyme Corporation | Colony stimulating factor-1 receptor (CSF-1R) inhibitors |
KR20210035236A (ko) * | 2018-07-19 | 2021-03-31 | 메드샤인 디스커버리 아이엔씨. | 아자인돌 유도체 및 이의 FGFR과 C-Met 억제제로서의 용도 |
US10988483B2 (en) | 2017-05-19 | 2021-04-27 | Nflection Therapeutics, Inc. | Fused heteroaromatic-aniline compounds for treatment of dermal disorders |
US11040957B2 (en) | 2013-10-18 | 2021-06-22 | Dana-Farber Cancer Institute, Inc. | Heteroaromatic compounds useful for the treatment of proliferative diseases |
WO2021134004A1 (en) | 2019-12-27 | 2021-07-01 | Schrodinger, Inc. | Cyclic compounds and methods of using same |
US11059801B2 (en) | 2014-12-23 | 2021-07-13 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
WO2021144287A1 (en) | 2020-01-15 | 2021-07-22 | Heparegenix Gmbh | 3-benzoyl-1h-pyrrolo[2,3-b]pyridine derivatives as mkk4 inhibitors for treating liver diseases |
WO2021152005A1 (en) | 2020-01-28 | 2021-08-05 | Universite De Strasbourg | Antisense oligonucleotide targeting linc00518 for treating melanoma |
US11087354B2 (en) | 2012-08-17 | 2021-08-10 | Genentech, Inc. | Combination therapies |
US11091486B2 (en) | 2016-10-26 | 2021-08-17 | Array Biopharma, Inc | Process for the preparation of pyrazolo[1,5-a]pyrimidines and salts thereof |
US11142507B2 (en) | 2015-09-09 | 2021-10-12 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
US11214571B2 (en) | 2016-05-18 | 2022-01-04 | Array Biopharma Inc. | Process for the preparation of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide and salts thereof |
US11242338B2 (en) | 2018-05-17 | 2022-02-08 | The Wistar Institute | EBNA1 inhibitor crystalline forms, and methods of preparing and using same |
WO2022055963A1 (en) | 2020-09-10 | 2022-03-17 | Schrödinger, Inc. | Heterocyclic pericondensed cdc7 kinase inhibitors for the treatment of cancer |
WO2022063101A1 (zh) * | 2020-09-23 | 2022-03-31 | 劲方医药科技(上海)有限公司 | 芳甲酰取代的三环化合物及其制法和用途 |
US11304949B2 (en) | 2018-03-30 | 2022-04-19 | Incyte Corporation | Treatment of hidradenitis suppurativa using JAK inhibitors |
US11312714B2 (en) | 2017-06-30 | 2022-04-26 | The Regents Of The University Of California | Compositions and methods for modulating hair growth |
WO2022105746A1 (en) * | 2020-11-17 | 2022-05-27 | Fochon Pharmaceuticals, Ltd. | SUBSTITUTED PYRROLO [2, 3-b] PYRIDINE AND PYRAZOLO [3, 4-b] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS |
WO2022125524A1 (en) * | 2020-12-07 | 2022-06-16 | Lieber Institute, Inc. | Compounds for inhibiting inositol hexakisphosphate kinase (ip6k) and methods of use thereof |
WO2022121900A1 (zh) * | 2020-12-07 | 2022-06-16 | 南京明德新药研发有限公司 | 吡咯并吡啶类化合物及其应用 |
WO2022164789A1 (en) | 2021-01-26 | 2022-08-04 | Schrödinger, Inc. | Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disoders |
WO2022197898A1 (en) | 2021-03-18 | 2022-09-22 | Schrödinger, Inc. | Cyclic compounds and methods of using same |
WO2022195551A1 (en) | 2021-03-18 | 2022-09-22 | Novartis Ag | Biomarkers for cancer and methods of use thereof |
US11524963B2 (en) | 2018-01-18 | 2022-12-13 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidines as RET kinase inhibitors |
US11530216B2 (en) | 2020-12-23 | 2022-12-20 | Genzyme Corporation | Deuterated colony stimulating factor-1 receptor (CSF-1R) inhibitors |
US11572344B2 (en) | 2018-11-20 | 2023-02-07 | Nflection Therapeutics, Inc. | Cyanoaryl-aniline compounds for treatment of dermal disorders |
WO2023174300A1 (zh) * | 2022-03-15 | 2023-09-21 | 劲方医药科技(上海)有限公司 | Btk抑制剂的晶型及其酸式盐和其酸式盐的晶型 |
US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
WO2024003350A1 (en) | 2022-06-30 | 2024-01-04 | Universite De Strasbourg | Combination therapy for melanoma |
WO2024033381A1 (en) | 2022-08-10 | 2024-02-15 | Vib Vzw | Inhibition of tcf4/itf2 in the treatment of cancer |
Families Citing this family (185)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1797881B1 (en) | 2004-09-17 | 2009-04-15 | Eisai R&D Management Co., Ltd. | Medicinal composition with improved stability and reduced gelation properties |
EP2281901B1 (en) | 2005-08-02 | 2013-11-27 | Eisai R&D Management Co., Ltd. | Anti-tumour pharmaceutical composition with angiogenesis inhibitors |
JP5209966B2 (ja) * | 2005-09-01 | 2013-06-12 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 崩壊性の改善された医薬組成物の製造方法 |
EP2036557B1 (en) | 2006-05-18 | 2015-10-21 | Eisai R&D Management Co., Ltd. | Antitumor agent for thyroid cancer |
JP2009537621A (ja) * | 2006-05-22 | 2009-10-29 | アストラゼネカ アクチボラグ | インドール誘導体 |
BRPI0622054B8 (pt) | 2006-09-22 | 2021-05-25 | Oxford Amherst Llc | composto e composição farmacêutica |
MX2009010284A (es) * | 2007-03-28 | 2010-01-29 | Pharmacyclics Inc | Inhibidores de la tirosina-cinasa de bruton. |
US20120101113A1 (en) | 2007-03-28 | 2012-04-26 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase |
DK2076289T3 (da) | 2007-04-13 | 2015-02-09 | Dana Farber Cancer Inst Inc | Fremgangsmåder til behandling af cancerresistens over for ErbB-lægemider |
GB0710528D0 (en) * | 2007-06-01 | 2007-07-11 | Glaxo Group Ltd | Novel compounds |
MX2010001636A (es) * | 2007-08-14 | 2010-03-15 | Hoffmann La Roche | Derivados de pirazolo[3,4-d]-pirimidina como agentes antiproliferativos. |
US8426396B2 (en) * | 2008-01-08 | 2013-04-23 | Shriners Hospitals For Children | Treatment for achondroplasia |
AR072008A1 (es) * | 2008-06-13 | 2010-07-28 | Merck & Co Inc | Compuestos heterobiciclicos como agentes de inhibicion de quinasa p38 |
US9447049B2 (en) | 2010-03-01 | 2016-09-20 | University Of Tennessee Research Foundation | Compounds for treatment of cancer |
MX2011000661A (es) | 2008-07-16 | 2011-05-25 | Pharmacyclics Inc | Inhibidores de tirosina cinasa de bruton para el tratamiento de tumores solidos. |
US8318446B2 (en) * | 2008-12-05 | 2012-11-27 | California Institute Of Technology | DNA-damage-induced proteolysis |
PL2396321T3 (pl) * | 2009-02-10 | 2015-10-30 | Monsanto Technology Llc | Kompozycje i sposoby zwalczania nicieni |
US8546399B2 (en) * | 2009-05-26 | 2013-10-01 | Abbvie Inc. | Apoptosis inducing agents for the treatment of cancer and immune and autoimmune diseases |
TWI537269B (zh) | 2009-05-26 | 2016-06-11 | 艾伯維巴哈馬有限公司 | 用於治療癌症及免疫及自體免疫疾病之細胞凋亡誘發劑 |
US9034875B2 (en) | 2009-05-26 | 2015-05-19 | Abbvie Inc. | Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases |
US20220315555A1 (en) | 2009-05-26 | 2022-10-06 | Abbvie Inc. | Apoptosis inducing agents for the treatment of cancer and immune and autoimmune diseases |
AU2010310468A1 (en) | 2009-10-23 | 2012-05-24 | Mannkind Corporation | Cancer immunotherapy and method of treatment |
WO2011060216A1 (en) | 2009-11-12 | 2011-05-19 | Concert Pharmaceuticals Inc. | Substituted azaindoles |
US11084811B2 (en) | 2010-03-01 | 2021-08-10 | Oncternal Therapeutics, Inc. | Compounds for treatment of cancer |
TWI619713B (zh) | 2010-04-21 | 2018-04-01 | 普雷辛肯公司 | 用於激酶調節的化合物和方法及其適應症 |
HUE035337T2 (en) | 2010-05-20 | 2018-05-02 | Array Biopharma Inc | Macrocyclic compounds as TRK kinase inhibitors |
US8669256B2 (en) | 2010-05-28 | 2014-03-11 | Merck Sharp & Dohme B.V. | Substituted thieno[2,3-b]pyrazine compounds as modulators of B-Raf kinase activity |
IL300955A (en) | 2010-06-03 | 2023-04-01 | Pharmacyclics Llc | (R)-1-(3-(4-amino-3-(4-phenoxyphenyl)-H1-pyrazolo[4,3-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1- Indicated for use as a drug to treat chronic lymphocytic leukemia or small lymphocytic lymphoma |
EP2598661B1 (en) | 2010-07-26 | 2017-09-27 | Biomatrica, INC. | Compositions for stabilizing dna, rna and proteins in saliva and other biological samples during shipping and storage at ambient temperatures |
US9376709B2 (en) | 2010-07-26 | 2016-06-28 | Biomatrica, Inc. | Compositions for stabilizing DNA and RNA in blood and other biological samples during shipping and storage at ambient temperatures |
US8709419B2 (en) * | 2010-08-17 | 2014-04-29 | Hoffmann-La Roche, Inc. | Combination therapy |
US20120045433A1 (en) | 2010-08-17 | 2012-02-23 | Kapil Dhingra | Combination therapy |
WO2012037060A1 (en) | 2010-09-13 | 2012-03-22 | Concert Pharmaceuticals Inc. | Substituted azaindoles |
UA113500C2 (xx) | 2010-10-29 | 2017-02-10 | Одержані екструзією розплаву тверді дисперсії, що містять індукуючий апоптоз засіб | |
EP2632436B1 (en) | 2010-10-29 | 2018-08-29 | Abbvie Inc. | Solid dispersions containing an apoptosis-inducing agent |
KR101236731B1 (ko) | 2010-11-02 | 2013-02-25 | 한국과학기술원 | 아자인돌 화합물, 이를 포함하는 pi3k 저해제용 약학 조성물 및 pi3k와 연관된 질환 치료용 약학 조성물 |
US8722657B2 (en) | 2010-11-23 | 2014-05-13 | Abbvie Inc. | Salts and crystalline forms of an apoptosis-inducing agent |
WO2012071374A1 (en) | 2010-11-23 | 2012-05-31 | Abbott Laboratories | Methods of treatment using selective bcl-2 inhibitors |
US9295669B2 (en) * | 2010-12-14 | 2016-03-29 | Hoffman La-Roche Inc. | Combination therapy for proliferative disorders |
US20140031383A1 (en) | 2011-02-08 | 2014-01-30 | Dana-Farber Cancer Institute, Inc. | Methods for treatment of melanoma |
US20140199292A1 (en) * | 2011-03-15 | 2014-07-17 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Compositions and methods for inhibiting tumor development caused by chemotherapy induced senescence |
CN103874689B (zh) * | 2011-04-01 | 2016-04-27 | 基因泰克公司 | Akt抑制剂化合物和威罗菲尼的组合及使用方法 |
WO2012138809A1 (en) * | 2011-04-05 | 2012-10-11 | Dawei Zhang | Heterocyclic compounds as kinase inhibitors |
WO2012144463A1 (ja) * | 2011-04-18 | 2012-10-26 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 腫瘍治療剤 |
EP2707508A4 (en) * | 2011-05-10 | 2015-07-29 | Brunangelo Falini | BIOMARKERS OF TRICHOLEUCOCYTE LEUKEMIA AND METHODS OF USE THEREOF |
JP2014515368A (ja) | 2011-05-26 | 2014-06-30 | 第一三共株式会社 | プロテインキナーゼ阻害剤としての複素環化合物 |
US9945862B2 (en) | 2011-06-03 | 2018-04-17 | Eisai R&D Management Co., Ltd. | Biomarkers for predicting and assessing responsiveness of thyroid and kidney cancer subjects to lenvatinib compounds |
KR20140048968A (ko) | 2011-07-13 | 2014-04-24 | 파마시클릭스, 인코포레이티드 | 브루톤형 티로신 키나제의 억제제 |
WO2013029043A1 (en) * | 2011-08-25 | 2013-02-28 | Reaction Biology Corp. | Selective kinase inhibitors |
WO2013032951A1 (en) | 2011-08-26 | 2013-03-07 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
JP6093768B2 (ja) | 2011-09-14 | 2017-03-08 | ニューファーマ, インコーポレイテッド | 特定の化学的実体、組成物、および方法 |
EP2570127A1 (en) | 2011-09-16 | 2013-03-20 | Sanofi | Compositions and methods for treating cancer using PI3KB beta inhibitor and MAPK pathway inhibitor, including MEK and RAF inhibitors |
US8377946B1 (en) | 2011-12-30 | 2013-02-19 | Pharmacyclics, Inc. | Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors |
WO2013109142A1 (en) | 2012-01-16 | 2013-07-25 | Stichting Het Nederlands Kanker Instituut | Combined pdk and mapk/erk pathway inhibition in neoplasia |
CN102603734A (zh) * | 2012-01-19 | 2012-07-25 | 盛世泰科生物医药技术(苏州)有限公司 | 一种蛋白激酶抑制剂及其应用 |
WO2013112950A2 (en) | 2012-01-25 | 2013-08-01 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
US9216170B2 (en) | 2012-03-19 | 2015-12-22 | Hoffmann-La Roche Inc. | Combination therapy for proliferative disorders |
JP6159388B2 (ja) | 2012-03-28 | 2017-07-05 | ニューロポア セラピーズ,インコーポレイティド | タンパク質凝集の阻害剤としてのフェニル−尿素及びフェニル−カルバメート誘導体 |
CN104395311B (zh) * | 2012-04-23 | 2017-04-19 | 基因泰克公司 | 制备化合物的中间体和方法 |
US10077474B2 (en) * | 2012-05-29 | 2018-09-18 | Abbott Molecular, Inc. | Method of designing primers, method of detecting single nucleotide polymorphisms (SNPs), method of distinguishing SNPs, and related primers, detectable oligonucleotides, and kits |
UA114421C2 (uk) | 2012-06-04 | 2017-06-12 | Фармасайклікс Ллс | Кристалічна форма інгібітору тирозинкінази брутона |
JP2015522037A (ja) | 2012-07-03 | 2015-08-03 | ラシオファルム ゲーエムベーハー | ベムラフェニブコリン塩の固体形態 |
US20150183781A1 (en) * | 2012-08-07 | 2015-07-02 | Um Pharmauji Sdn. Bhd. | 5-(1H-Pyrazol-4-yl)-1H-Pyrrolo[2,3-b]Pyridine Derivatives as Kinase Inhibitors |
CN103626765B (zh) * | 2012-08-27 | 2016-08-10 | 广东东阳光药业有限公司 | 取代的氮杂吲哚化合物及其盐、组合物和用途 |
US10227357B2 (en) | 2012-09-06 | 2019-03-12 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
WO2014047648A1 (en) | 2012-09-24 | 2014-03-27 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
CN105712992B (zh) * | 2012-09-29 | 2018-10-26 | 上海科州药物研发有限公司 | 作为cMet抑制剂的化合物及其制备方法和用途 |
KR102174576B1 (ko) * | 2012-10-08 | 2020-11-06 | 아트리바 테라퓨틱스 게엠베하 | 바이러스 질환 치료에서의 mek 억제제 |
EP2916838B1 (en) | 2012-11-12 | 2019-03-13 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
MX2015006168A (es) | 2012-11-15 | 2015-08-10 | Pharmacyclics Inc | Compuestos de pirrolopirimidina como inhibidores de quinasas. |
US9725703B2 (en) | 2012-12-20 | 2017-08-08 | Biomatrica, Inc. | Formulations and methods for stabilizing PCR reagents |
BR112015009004A8 (pt) | 2012-12-21 | 2021-07-20 | Eisai R&D Man Co Ltd | forma amorfa de derivado de quinolina e método de produção da mesma |
KR102212923B1 (ko) | 2012-12-21 | 2021-02-04 | 플렉시콘 인코퍼레이티드 | 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증 |
JP6835472B2 (ja) * | 2013-03-05 | 2021-02-24 | ユニバーシティ オブ テネシー リサーチ ファウンデーション | 癌の処置のための組成物 |
EP2970270A1 (en) | 2013-03-14 | 2016-01-20 | ratiopharm GmbH | Solid state forms of vemurafenib hydrochloride |
US20140275082A1 (en) | 2013-03-14 | 2014-09-18 | Abbvie Inc. | Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases |
US20140303121A1 (en) | 2013-03-15 | 2014-10-09 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
CN105188707A (zh) | 2013-03-15 | 2015-12-23 | 赛诺菲 | 包含PI3Kβ抑制剂和RAF抑制剂以克服癌细胞抵抗的抗肿瘤组合物 |
KR102244719B1 (ko) | 2013-03-15 | 2021-04-26 | 플렉시콘 인코퍼레이티드 | 헤테로시클릭 화합물 및 그의 용도 |
US9206188B2 (en) | 2013-04-18 | 2015-12-08 | Arrien Pharmaceuticals Llc | Substituted pyrrolo[2,3-b]pyridines as ITK and JAK inhibitors |
MX368099B (es) | 2013-05-14 | 2019-09-19 | Eisai R&D Man Co Ltd | Biomarcadores para predecir y evaluar el grado de respuesta de sujetos con cancer de endometrio a compuestos de tipo lenvatinib. |
CN105491883B (zh) | 2013-06-13 | 2018-11-02 | 生物马特里卡公司 | 细胞稳定化 |
US11007174B2 (en) * | 2013-07-12 | 2021-05-18 | Piramal Enterprises Limited | Pharmaceutical combination for the treatment of melanoma |
TWI649081B (zh) | 2013-08-02 | 2019-02-01 | 製藥公司 | 治療固態腫瘤之方法 |
US9415050B2 (en) | 2013-08-12 | 2016-08-16 | Pharmacyclics Llc | Methods for the treatment of HER2 amplified cancer |
WO2015041533A1 (en) | 2013-09-20 | 2015-03-26 | Stichting Het Nederlands Kanker Instituut | Rock in combination with mapk-pathway |
WO2015041534A1 (en) | 2013-09-20 | 2015-03-26 | Stichting Het Nederlands Kanker Instituut | P90rsk in combination with raf/erk/mek |
MA38961A1 (fr) | 2013-09-30 | 2018-05-31 | Pharmacyclics Llc | Composés 3-phenyl-1h-pyrazolo[3,4-d]pyrimidin-4-ylamine substitués inhibiteurs de la tyrosine kinase de bruton utilisés pour traiter par exemple les maladies auto-immunes, respiratoires et inflammatoires, cancer, mastocytose et osteoporose |
WO2015075749A1 (en) * | 2013-11-22 | 2015-05-28 | Laurus Labs Private Limited | Novel processes for the preparation of vemurafenib |
CN104710417B (zh) * | 2013-12-11 | 2020-09-08 | 上海科州药物研发有限公司 | 氮杂吲哚类衍生物及其合成方法 |
MX2016008201A (es) * | 2013-12-20 | 2017-04-27 | Biomed Valley Discoveries Inc | Tratamiento del cancer usando combinaciones de inhibidores de erk y raf. |
CN104739823A (zh) * | 2013-12-28 | 2015-07-01 | 复旦大学附属华山医院 | 淫羊藿素在制备维罗非尼增敏剂中的用途 |
US9771369B2 (en) | 2014-03-04 | 2017-09-26 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
WO2015143400A1 (en) | 2014-03-20 | 2015-09-24 | Pharmacyclics, Inc. | Phospholipase c gamma 2 and resistance associated mutations |
US20170027940A1 (en) | 2014-04-10 | 2017-02-02 | Stichting Het Nederlands Kanker Instituut | Method for treating cancer |
CN106535900A (zh) * | 2014-05-06 | 2017-03-22 | 加利福尼亚大学董事会 | 使用braf抑制剂的伤口愈合 |
WO2015178770A1 (en) | 2014-05-19 | 2015-11-26 | Stichting Het Nederlands Kanker Instituut | Compositions for cancer treatment |
WO2015181628A1 (en) * | 2014-05-27 | 2015-12-03 | Eisai R&D Management Co., Ltd. | Treatment of acute myeloid leukemia with an hck inhibitor |
JP6661554B2 (ja) | 2014-06-10 | 2020-03-11 | バイオマトリカ,インク. | 周囲温度における血小板の安定化 |
JP2017517558A (ja) * | 2014-06-13 | 2017-06-29 | ジェネンテック, インコーポレイテッド | 癌薬剤耐性の治療方法及び防止方法 |
WO2016000615A1 (en) * | 2014-07-02 | 2016-01-07 | Sunshine Lake Pharma Co., Ltd. | Heteroaryl compounds and pharmaceutical applications thereof |
CA2959602A1 (en) | 2014-08-01 | 2016-02-04 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
BR112017002231A2 (pt) | 2014-08-07 | 2018-07-17 | Pharmacyclics Llc | novas formulações de um inibidor de tirosina cinase de bruton |
HRP20221047T1 (hr) | 2014-08-28 | 2022-11-11 | Eisai R&D Management Co., Ltd. | Derivat kinolina visoke čistoće i postupak za njegovu proizvodnju |
EP3194392B1 (en) | 2014-09-15 | 2020-01-01 | Plexxikon, Inc. | Heterocyclic compounds and uses thereof |
US10611765B2 (en) | 2014-11-06 | 2020-04-07 | Ohio State Innovation Foundation | Pyrrolopyrimidine derivatives as Mps1/TTK kinase inhibitors |
US10414764B2 (en) | 2014-11-29 | 2019-09-17 | Shilpa Medicare Limited | Substantially pure vemurafenib and its salts |
CN107427505A (zh) | 2015-02-25 | 2017-12-01 | 卫材R&D管理有限公司 | 用于抑制喹啉衍生物的苦味的方法 |
SG11201707122QA (en) | 2015-03-03 | 2017-09-28 | Pharmacyclics Llc | Pharmaceutical formulations of bruton's tyrosine kinase inhibtor |
WO2016140717A1 (en) | 2015-03-04 | 2016-09-09 | Merck Sharp & Dohme Corp. | Combination of a pd-1 antagonist and a vegfr/fgfr/ret tyrosine kinase inhibitor for treating cancer |
US10160755B2 (en) | 2015-04-08 | 2018-12-25 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
US9802932B2 (en) | 2015-05-06 | 2017-10-31 | Plexxikon Inc. | Solid forms of a compound modulating kinases |
HUE047657T2 (hu) | 2015-05-06 | 2020-05-28 | Plexxikon Inc | Kináz-moduláló hatású 1H-pirrolo[2,3-b]piridin származékok szintézise |
US9814714B2 (en) | 2015-05-22 | 2017-11-14 | Plexxikon Inc. | Kinase modulation, and indications therefor |
RS59934B1 (sr) * | 2015-06-09 | 2020-03-31 | Abbvie Inc | Modulatori nuklearnih receptora (ror) za lečenje inflamatornih i autoimunih oboljenja |
US11369623B2 (en) | 2015-06-16 | 2022-06-28 | Prism Pharma Co., Ltd. | Anticancer combination of a CBP/catenin inhibitor and an immune checkpoint inhibitor |
EP3328372A4 (en) | 2015-07-28 | 2019-03-20 | University Of Iowa Research Foundation | COMPOSITIONS AND METHODS OF TREATING CANCER |
WO2017019804A2 (en) | 2015-07-28 | 2017-02-02 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
KR20180052757A (ko) | 2015-09-21 | 2018-05-18 | 플렉시콘 인코퍼레이티드 | 헤테로시클릭 화합물 및 그의 용도 |
WO2017066193A1 (en) * | 2015-10-15 | 2017-04-20 | Princeton Drug Discovery, Llc | Novel inhibitors of protein kinases |
US9938273B2 (en) | 2015-12-07 | 2018-04-10 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
SG11201804776SA (en) | 2015-12-08 | 2018-07-30 | Biomatrica Inc | Reduction of erythrocyte sedimentation rate |
US10116776B2 (en) | 2015-12-14 | 2018-10-30 | Red.Com, Llc | Modular digital camera and cellular phone |
US10513528B2 (en) * | 2016-02-25 | 2019-12-24 | Taxis Pharmaceuticals, Inc. | Synthetic processes and intermediates |
EP3430005B1 (en) | 2016-03-16 | 2021-12-08 | Plexxikon Inc. | Compounds and methods for kinase modulation and indications therefore |
AU2017283491B2 (en) * | 2016-06-13 | 2021-06-03 | Chemocentryx, Inc. | Methods of treating pancreatic cancer |
WO2017223565A1 (en) | 2016-06-24 | 2017-12-28 | University Of Iowa Research Foundation | Compositions and methods of treating melanoma |
CN116478132A (zh) | 2016-07-12 | 2023-07-25 | 锐新医药公司 | 作为变构shp2抑制剂的2,5-双取代型及2,5,6-三取代型3-甲基吡嗪 |
TW201815766A (zh) | 2016-09-22 | 2018-05-01 | 美商普雷辛肯公司 | 用於ido及tdo調節之化合物及方法以及其適應症 |
EP3308773A1 (en) | 2016-10-11 | 2018-04-18 | Recordati Industria Chimica E Farmaceutica SPA | Formulations of cysteamine and cysteamine derivatives |
CA3040348A1 (en) | 2016-10-19 | 2018-04-26 | United States Government As Represented By The Department Of Veterans Affairs | Compositions and methods for treating cancer |
AU2017363299B2 (en) | 2016-11-23 | 2022-12-22 | Chemocentryx, Inc. | Method of treating focal segmental glomerulosclerosis |
AU2017376922B2 (en) | 2016-12-15 | 2022-12-01 | Société des Produits Nestlé S.A. | Compositions and methods that modulate phosphorus or enzymes in a companion animal |
US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
KR102564201B1 (ko) * | 2016-12-23 | 2023-08-07 | 아비나스 오퍼레이션스, 인코포레이티드 | 급속 진행성 섬유육종 폴리펩티드의 표적화 분해를 위한 화합물 및 방법 |
CA3047580A1 (en) * | 2016-12-23 | 2018-07-26 | Plexxikon Inc. | Compounds and methods for cdk8 modulation and indications therefor |
MX2019008696A (es) | 2017-01-23 | 2019-09-13 | Revolution Medicines Inc | Compuestos de piridina como inhibidores de shp2 alostericos. |
MX2019008695A (es) | 2017-01-23 | 2019-09-11 | Revolution Medicines Inc | Compuestos biciclicos como inhibidores alostericos de shp2. |
US10577366B2 (en) | 2017-03-20 | 2020-03-03 | Plexxikon Inc. | Crystalline forms of a compound that inhibits bromodomain |
WO2018183762A1 (en) * | 2017-03-29 | 2018-10-04 | United States Government As Represented By The Department Of Veterans Affairs | Methods and compositions for treating cancer |
US10774093B2 (en) | 2017-03-30 | 2020-09-15 | Taxis Pharmaceuticals, Inc. | Synthetic processes and synthetic intermediates |
TW201902517A (zh) * | 2017-04-28 | 2019-01-16 | 美商石英醫療公司 | Raf降解結合物化合物 |
US10428067B2 (en) | 2017-06-07 | 2019-10-01 | Plexxikon Inc. | Compounds and methods for kinase modulation |
US10435404B2 (en) | 2017-07-25 | 2019-10-08 | Plexxikon Inc. | Formulations of a compound modulating kinases |
CN109384785B (zh) * | 2017-08-10 | 2021-09-28 | 浙江海正药业股份有限公司 | 吡咯并吡啶酮类衍生物、其制备方法及其在医药上的用途 |
JP2020536919A (ja) | 2017-10-11 | 2020-12-17 | ケモセントリックス, インコーポレイテッド | Ccr2アンタゴニストによる巣状分節性糸球体硬化症の治療 |
EP3694848A1 (en) | 2017-10-12 | 2020-08-19 | Revolution Medicines, Inc. | Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors |
WO2019075243A1 (en) | 2017-10-13 | 2019-04-18 | Plexxikon Inc. | SOLID FORMS OF A COMPOUND FOR MODULATING KINASES |
ES2947411T3 (es) | 2017-10-26 | 2023-08-08 | Xynomic Pharmaceuticals Inc | Sales cristalinas de un campo inhibidor de quinasa B-RAF |
CA3080197C (en) | 2017-10-27 | 2023-12-19 | Plexxikon Inc. | Formulations of a compound modulating kinases |
EP3724189B1 (en) | 2017-12-15 | 2023-10-04 | Revolution Medicines, Inc. | Polycyclic compounds as allosteric shp2 inhibitors |
CN112119072A (zh) | 2018-03-20 | 2020-12-22 | 普莱希科公司 | 用于ido和tdo调节的化合物和方法,以及其适应症 |
WO2019195682A1 (en) * | 2018-04-05 | 2019-10-10 | Beth Israel Deaconess Medical Center, Inc. | Aryl hydrocarbon receptor modulators and uses thereof |
EP3560516A1 (en) * | 2018-04-27 | 2019-10-30 | Bergen Teknologioverforing AS | Combination therapy including beta-sitosterol in combination with at least one of a braf inhibitor, a mek inhibitor or an erk inhibitor and methods and use thereof |
GB201808321D0 (en) * | 2018-05-21 | 2018-07-11 | Univ College Dublin Nat Univ Ireland Dublin | Compositions and uses thereof |
RU2687107C1 (ru) * | 2018-06-18 | 2019-05-07 | федеральное государственное автономное образовательное учреждение высшего образования "Московский физико-технический институт (государственный университет)" | Ингибитор braf киназы n-(3-(5-(4-хлорофенил)-1h-пиразоло[3,4-b]пиридин-3-карбонил)-2,4-дифторофенил) пропан-1-сульфонамид |
CN116875518A (zh) * | 2018-07-06 | 2023-10-13 | 科罗拉多州立大学董事会法人团体 | 用于构建和检测生物活性剂的基因编码系统 |
US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
CN113166097A (zh) * | 2018-12-03 | 2021-07-23 | 默克专利股份公司 | 作为端锚聚合酶抑制剂的4-杂芳基羰基-n-(苯基或杂芳基)哌啶-1-甲酰胺 |
EP3924340A1 (en) * | 2019-02-11 | 2021-12-22 | Merck Patent GmbH | Indazolyl-isoxazole derivatives for the treatment of diseases such as cancer |
WO2020168197A1 (en) | 2019-02-15 | 2020-08-20 | Incyte Corporation | Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors |
TW202100520A (zh) | 2019-03-05 | 2021-01-01 | 美商英塞特公司 | 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物 |
US11919904B2 (en) | 2019-03-29 | 2024-03-05 | Incyte Corporation | Sulfonylamide compounds as CDK2 inhibitors |
EP3953351A1 (en) | 2019-04-09 | 2022-02-16 | Plexxikon Inc. | Condensed azines for ep300 or cbp modulation and indications therefor |
US11440914B2 (en) | 2019-05-01 | 2022-09-13 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
US11447494B2 (en) | 2019-05-01 | 2022-09-20 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
MX2022001940A (es) | 2019-08-14 | 2022-05-10 | Incyte Corp | Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2. |
US20220347182A1 (en) * | 2019-10-02 | 2022-11-03 | The Board Of Trustees Of The Leland Stanford Junior University | Methods and compositions for the treatment of osteoarthritis |
PE20221905A1 (es) | 2019-10-11 | 2022-12-23 | Incyte Corp | Aminas biciclicas como inhibidoras de la cdk2 |
CN111004210A (zh) * | 2019-10-23 | 2020-04-14 | 中山大学 | 化合物单晶及其制备方法 |
KR20220119094A (ko) | 2019-12-19 | 2022-08-26 | 아비나스 오퍼레이션스, 인코포레이티드 | 안드로겐 수용체의 표적화된 분해를 위한 화합물 및 방법 |
US20230090552A1 (en) | 2020-01-08 | 2023-03-23 | Synthis Therapeutics, Inc. | Alk5 inhibitor conjugates and uses thereof |
CA3172681A1 (en) * | 2020-04-15 | 2021-10-21 | Kollol Pal | Methods for preparing tyrosine receptor kinase inhibitors |
EP4139296A1 (en) | 2020-04-23 | 2023-03-01 | Opna Immuno Oncology, SA | Compounds and methods for cd73 modulation and indications therefor |
US11529335B2 (en) | 2020-07-31 | 2022-12-20 | University Of Iowa Research Foundation | Compositions and methods for treating cancer |
WO2022040512A1 (en) | 2020-08-21 | 2022-02-24 | Plexxikon Inc. | Combinational drug anticancer therapies |
CN114478528A (zh) * | 2020-10-28 | 2022-05-13 | 劲方医药科技(上海)有限公司 | 芳甲酰取代的三环化合物及其制法和用途 |
CN112574200B (zh) * | 2021-02-26 | 2021-06-11 | 安润医药科技(苏州)有限公司 | Btk和/或btk的突变体c481s的小分子抑制剂 |
CN115073469B (zh) * | 2021-03-15 | 2023-12-22 | 药雅科技(上海)有限公司 | 吡咯并嘧啶类化合物作为激酶抑制剂的制备及其应用 |
TW202304890A (zh) * | 2021-04-14 | 2023-02-01 | 美商百歐克斯製藥公司 | Klk5雙環雜芳香族抑制劑 |
WO2023059786A1 (en) * | 2021-10-06 | 2023-04-13 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Inhibitors of ulk1 and methods of use |
US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
WO2023178240A2 (en) * | 2022-03-16 | 2023-09-21 | The Children's Medical Center Corporation | Pyk2 inhibition modulates immune cell function |
CN115141197B (zh) * | 2022-07-27 | 2024-03-26 | 安徽医科大学 | 一种3-芳杂环取代苯基衍生物及其制备方法与用途 |
US11957759B1 (en) | 2022-09-07 | 2024-04-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use |
Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2234705A (en) * | 1940-04-12 | 1941-03-11 | Eastman Kodak Co | Cellulose organic derivative composition containing esters of monoalkoxy benzoic acids |
DE2413258A1 (de) * | 1974-03-20 | 1975-10-02 | Bayer Ag | Alkoxycarbonylphenylharnstoffe, verfahren zu ihrer herstellung und ihre verwendung als herbizide |
WO2004016610A1 (en) | 2002-08-14 | 2004-02-26 | Astrazeneca Ab | Substituted pyrrolopyridines |
WO2004024895A2 (en) | 2002-09-16 | 2004-03-25 | Plexxikon, Inc. | Crystal structure of pim-1 kinase |
WO2004078923A2 (en) | 2003-02-28 | 2004-09-16 | Plexxikon, Inc. | Pyk2 crystal structure and uses |
WO2005028624A2 (en) | 2003-09-15 | 2005-03-31 | Plexxikon, Inc. | Molecular scaffolds for kinase ligand development |
WO2005062795A2 (en) | 2003-12-19 | 2005-07-14 | Plexxikon, Inc. | Compounds and methods for development of ret modulators |
Family Cites Families (159)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3124610A (en) * | 1964-03-10 | Preparation of intermediates | ||
US2413258A (en) | 1942-07-07 | 1946-12-24 | United Gas Improvement Co | Polystyrene-type resins plasticized with high boiling fatty acid alkyl esters |
US3067237A (en) * | 1959-04-14 | 1962-12-04 | Sterling Drug Inc | Lower-alkyl mono-or bis-(alkanesulfonamido) benzoate esters |
GB1141949A (en) | 1966-02-23 | 1969-02-05 | Sterling Drug Inc | 7-azaindole derivatives |
DE1668420B2 (de) * | 1966-10-21 | 1976-11-25 | Minnesota Mining and Manufacturing Co., Saint Paul, Minn. (V.StA.) | Trifluormethylsulfonanilide, verfahren zu ihrer herstellung und ihre verwendung |
IL46853A0 (en) * | 1974-03-20 | 1975-05-22 | Bayer Ag | Novel alkoxycarbonylphenylureas,their preparation and their use as herbicides |
GB1573212A (en) | 1976-04-15 | 1980-08-20 | Technicon Instr | Immunoassay for gentamicin |
US4301159A (en) * | 1980-06-20 | 1981-11-17 | Shionogi & Co., Ltd. | N-(Diethylaminoethyl)-2-alkoxy-benzamide derivatives |
AU547405B2 (en) * | 1981-07-08 | 1985-10-17 | Sanofi | Amidobenzamides |
US4664504A (en) * | 1983-01-20 | 1987-05-12 | Tokyo Shibaura Denki Kabushiki Kaisha | Image forming apparatus |
US4568649A (en) | 1983-02-22 | 1986-02-04 | Immunex Corporation | Immediate ligand detection assay |
US4626513A (en) | 1983-11-10 | 1986-12-02 | Massachusetts General Hospital | Method and apparatus for ligand detection |
EP0142152B1 (en) * | 1983-11-14 | 1991-03-20 | The Dow Chemical Company | Novel substituted 1,2,4-triazolo- [1,5-a] pyrimidine-2-sulfonamides and compositions and methods of controlling undesired vegetation and suppressing the nitrification of ammonium nitrogen in soil |
AU567140B2 (en) * | 1984-01-06 | 1987-11-12 | Shionogi & Co., Ltd. | Sulphonamido-benzamide derivatives |
ATE56096T1 (de) | 1984-03-15 | 1990-09-15 | Immunex Corp | Test zur sofortigen feststellung von liganden, testsatz und seine herstellung. |
IT1196133B (it) * | 1984-06-06 | 1988-11-10 | Ausonia Farma Srl | Derivati furanici con attivita' antiulcera |
US4714693A (en) | 1986-04-03 | 1987-12-22 | Uop Inc. | Method of making a catalyst composition comprising uniform size metal components on carrier |
US5688655A (en) | 1988-02-10 | 1997-11-18 | Ict Pharmaceuticals, Inc. | Method of screening for protein inhibitors and activators |
US6054270A (en) | 1988-05-03 | 2000-04-25 | Oxford Gene Technology Limited | Analying polynucleotide sequences |
US5700637A (en) | 1988-05-03 | 1997-12-23 | Isis Innovation Limited | Apparatus and method for analyzing polynucleotide sequences and method of generating oligonucleotide arrays |
US5658775A (en) | 1988-05-17 | 1997-08-19 | Sloan-Kettering Institute For Cancer Research | Double copy retroviral vector |
CA1339354C (en) | 1988-09-01 | 1997-08-26 | The Whitehead Institute For Biomedical Research | Recombinant retroviruses with amphotropic and ecotropic host ranges |
US5703055A (en) | 1989-03-21 | 1997-12-30 | Wisconsin Alumni Research Foundation | Generation of antibodies through lipid mediated DNA delivery |
US5800992A (en) | 1989-06-07 | 1998-09-01 | Fodor; Stephen P.A. | Method of detecting nucleic acids |
US5744101A (en) | 1989-06-07 | 1998-04-28 | Affymax Technologies N.V. | Photolabile nucleoside protecting groups |
US5527681A (en) | 1989-06-07 | 1996-06-18 | Affymax Technologies N.V. | Immobilized molecular synthesis of systematically substituted compounds |
US5143854A (en) | 1989-06-07 | 1992-09-01 | Affymax Technologies N.V. | Large scale photolithographic solid phase synthesis of polypeptides and receptor binding screening thereof |
US5360822A (en) * | 1990-02-07 | 1994-11-01 | Nippon Shinyaku Co. Ltd. | Sulfonanilide derivatives and medicine |
WO1991018088A1 (en) | 1990-05-23 | 1991-11-28 | The United States Of America, Represented By The Secretary, United States Department Of Commerce | Adeno-associated virus (aav)-based eucaryotic vectors |
DE4022414A1 (de) | 1990-07-13 | 1992-01-16 | Bayer Ag | Substituierte pyrrolo-pyridine |
US5124335A (en) | 1991-01-30 | 1992-06-23 | Merck & Co., Inc. | Substituted pyrollo-fused 6 membered heterocycles as angiotensin ii antagonists |
CA2113990A1 (en) | 1991-07-26 | 1993-02-18 | Frederick L. Moolten | Cancer therapy utilizing malignant cells |
US5632957A (en) | 1993-11-01 | 1997-05-27 | Nanogen | Molecular biological diagnostic systems including electrodes |
FR2687402B1 (fr) | 1992-02-14 | 1995-06-30 | Lipha | Nouveaux azaindoles, procedes de preparation et medicaments les contenant. |
JPH05236997A (ja) | 1992-02-28 | 1993-09-17 | Hitachi Ltd | ポリヌクレオチド捕捉用チップ |
PL310443A1 (en) | 1993-03-01 | 1995-12-11 | Merck Sharp & Dohme | Derivatives of pyrolo-pyridine |
US5576319A (en) * | 1993-03-01 | 1996-11-19 | Merck, Sharp & Dohme Ltd. | Pyrrolo-pyridine derivatives |
ES2134929T3 (es) | 1993-03-01 | 1999-10-16 | Merck Sharp & Dohme | Derivados de pirrolo-piridina como ligandos para receptores de dopamina. |
US5549614A (en) * | 1993-03-18 | 1996-08-27 | Tunis; Scott W. | Apparatus for folding flexible intraocular lenses |
DE69434998T2 (de) | 1993-05-27 | 2008-03-13 | Aventis Pharmaceuticals Inc. | Topologisch getrennte, kodierende Festphasen-Bibliotheken |
US5840485A (en) | 1993-05-27 | 1998-11-24 | Selectide Corporation | Topologically segregated, encoded solid phase libraries |
US5631236A (en) | 1993-08-26 | 1997-05-20 | Baylor College Of Medicine | Gene therapy for solid tumors, using a DNA sequence encoding HSV-Tk or VZV-Tk |
US5426039A (en) | 1993-09-08 | 1995-06-20 | Bio-Rad Laboratories, Inc. | Direct molecular cloning of primer extended DNA containing an alkane diol |
JP3545461B2 (ja) | 1993-09-10 | 2004-07-21 | エーザイ株式会社 | 二環式ヘテロ環含有スルホンアミド誘導体 |
US6045996A (en) | 1993-10-26 | 2000-04-04 | Affymetrix, Inc. | Hybridization assays on oligonucleotide arrays |
US6468742B2 (en) | 1993-11-01 | 2002-10-22 | Nanogen, Inc. | Methods for determination of single nucleic acid polymorphisms using bioelectronic microchip |
US5965452A (en) | 1996-07-09 | 1999-10-12 | Nanogen, Inc. | Multiplexed active biologic array |
US5486525A (en) * | 1993-12-16 | 1996-01-23 | Abbott Laboratories | Platelet activating factor antagonists: imidazopyridine indoles |
US5807522A (en) | 1994-06-17 | 1998-09-15 | The Board Of Trustees Of The Leland Stanford Junior University | Methods for fabricating microarrays of biological samples |
US5763198A (en) | 1994-07-22 | 1998-06-09 | Sugen, Inc. | Screening assays for compounds |
GB9416162D0 (en) | 1994-08-10 | 1994-09-28 | Merck Sharp & Dohme | Therapeutic agents |
GB9416189D0 (en) | 1994-08-10 | 1994-09-28 | Merck Sharp & Dohme | Therapeutic agents |
DE4430212A1 (de) * | 1994-08-28 | 1996-02-29 | Merck Patent Gmbh | Ortho-substituierte Benzoesäure-Derivate |
US5556752A (en) | 1994-10-24 | 1996-09-17 | Affymetrix, Inc. | Surface-bound, unimolecular, double-stranded DNA |
US5830645A (en) | 1994-12-09 | 1998-11-03 | The Regents Of The University Of California | Comparative fluorescence hybridization to nucleic acid arrays |
GB9503400D0 (en) | 1995-02-21 | 1995-04-12 | Merck Sharp & Dohme | Therpeutic agents |
GB2298199A (en) | 1995-02-21 | 1996-08-28 | Merck Sharp & Dohme | Synthesis of azaindoles |
US5959098A (en) | 1996-04-17 | 1999-09-28 | Affymetrix, Inc. | Substrate preparation process |
US6117681A (en) | 1995-03-29 | 2000-09-12 | Bavarian Nordic Research Inst. A/S | Pseudotyped retroviral particles |
GB2299581A (en) | 1995-04-07 | 1996-10-09 | Merck Sharp & Dohme | 3-(Tetrahydropyridin-1-yl-methyl)pyrrolo[2,3-b]pyridine derivatives as ligands for dopamine receptor subtypes |
GB9507291D0 (en) * | 1995-04-07 | 1995-05-31 | Merck Sharp & Dohme | Therapeutic agents |
US6110456A (en) | 1995-06-07 | 2000-08-29 | Yale University | Oral delivery or adeno-associated viral vectors |
US5856174A (en) | 1995-06-29 | 1999-01-05 | Affymetrix, Inc. | Integrated nucleic acid diagnostic device |
US5866411A (en) | 1995-09-08 | 1999-02-02 | Pedersen; Finn Skou | Retroviral vector, a replication system for said vector and avian or mammalian cells transfected with said vector |
US5747276A (en) | 1995-09-15 | 1998-05-05 | The Scripps Research Institute | Screening methods for the identification of novel antibiotics |
US5721118A (en) | 1995-10-31 | 1998-02-24 | The Regents Of The University Of California, San Diego | Mammalian artificial chromosomes and methods of using same |
US6022963A (en) | 1995-12-15 | 2000-02-08 | Affymetrix, Inc. | Synthesis of oligonucleotide arrays using photocleavable protecting groups |
US6013440A (en) | 1996-03-11 | 2000-01-11 | Affymetrix, Inc. | Nucleic acid affinity columns |
US6025155A (en) | 1996-04-10 | 2000-02-15 | Chromos Molecular Systems, Inc. | Artificial chromosomes, uses thereof and methods for preparing artificial chromosomes |
US5804585A (en) | 1996-04-15 | 1998-09-08 | Texas Biotechnology Corporation | Thieno-pyridine sulfonamides derivatives thereof and related compounds that modulate the activity of endothelin |
DE69728688T2 (de) * | 1996-11-19 | 2004-08-19 | Amgen Inc., Thousand Oaks | Aryl und heteroaryl substituierte kondensierte pyrrole als entzündunghemmende mittel |
US6294330B1 (en) | 1997-01-31 | 2001-09-25 | Odyssey Pharmaceuticals Inc. | Protein fragment complementation assays for the detection of biological or drug interactions |
EP0972071A4 (en) | 1997-03-07 | 2004-04-21 | Tropix Inc | TEST ARRANGEMENT FOR PROTEAS INHIBITORS |
US5977131A (en) | 1997-04-09 | 1999-11-02 | Pfizer Inc. | Azaindole-ethylamine derivatives as nicotinic acetylcholine receptor binding agents |
US6096718A (en) | 1997-06-05 | 2000-08-01 | Gene Targeting Corp. | Tissue specific adenovirus vectors for breast cancer treatment |
CA2295239A1 (en) | 1997-06-27 | 1999-01-07 | Fujisawa Pharmaceutical Co., Ltd. | Sulfonamide compounds and medicinal use thereof |
US6235769B1 (en) | 1997-07-03 | 2001-05-22 | Sugen, Inc. | Methods of preventing and treating neurological disorders with compounds that modulate the function of the C-RET receptor protein tyrosine kinase |
US6826296B2 (en) | 1997-07-25 | 2004-11-30 | Affymetrix, Inc. | Method and system for providing a probe array chip design database |
US6161776A (en) | 1997-08-12 | 2000-12-19 | Nibco Inc. | Multi-layered, porous mat turf irrigation apparatus and method |
DK1012564T3 (da) | 1997-09-11 | 2003-07-21 | Bioventures Inc | Fremgangsmåde til at fremstille højtæthedsarrays |
US6178384B1 (en) | 1997-09-29 | 2001-01-23 | The Trustees Of Columbia University In The City Of New York | Method and apparatus for selecting a molecule based on conformational free energy |
US6465178B2 (en) | 1997-09-30 | 2002-10-15 | Surmodics, Inc. | Target molecule attachment to surfaces |
US6048695A (en) | 1998-05-04 | 2000-04-11 | Baylor College Of Medicine | Chemically modified nucleic acids and methods for coupling nucleic acids to solid support |
AU4543899A (en) | 1998-06-08 | 1999-12-30 | Advanced Medicine, Inc. | Multibinding inhibitors of microsomal triglyceride transferase protein |
US6113913A (en) | 1998-06-26 | 2000-09-05 | Genvec, Inc. | Recombinant adenovirus |
AU772477B2 (en) | 1998-08-28 | 2004-04-29 | Scios Inc. | Inhibitors of p38-alpha kinase |
US6184226B1 (en) | 1998-08-28 | 2001-02-06 | Scios Inc. | Quinazoline derivatives as inhibitors of P-38 α |
US6350786B1 (en) * | 1998-09-22 | 2002-02-26 | Hoffmann-La Roche Inc. | Stable complexes of poorly soluble compounds in ionic polymers |
US6277628B1 (en) | 1998-10-02 | 2001-08-21 | Incyte Genomics, Inc. | Linear microarrays |
US6277489B1 (en) | 1998-12-04 | 2001-08-21 | The Regents Of The University Of California | Support for high performance affinity chromatography and other uses |
US20010001449A1 (en) | 1998-12-30 | 2001-05-24 | Thomas R. Kiliany | Low-pressure hydrocracking process |
KR100757282B1 (ko) * | 1999-03-17 | 2007-09-11 | 아스트라제네카 아베 | 아미드 유도체 |
GB9906566D0 (en) | 1999-03-23 | 1999-05-19 | Zeneca Ltd | Chemical compounds |
US6221653B1 (en) | 1999-04-27 | 2001-04-24 | Agilent Technologies, Inc. | Method of performing array-based hybridization assays using thermal inkjet deposition of sample fluids |
FR2793793B1 (fr) | 1999-05-19 | 2004-02-27 | Adir | Nouveaux derives dimeriques substitues, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
TWI234557B (en) * | 1999-05-26 | 2005-06-21 | Telik Inc | Novel naphthalene ureas as glucose uptake enhancers |
US6653151B2 (en) | 1999-07-30 | 2003-11-25 | Large Scale Proteomics Corporation | Dry deposition of materials for microarrays using matrix displacement |
US20010008765A1 (en) | 1999-12-06 | 2001-07-19 | Fuji Photo Film Co., Ltd. | DNA chip and reactive solid carrier |
US20020010203A1 (en) | 1999-12-22 | 2002-01-24 | Ken Lipson | Methods of modulating c-kit tyrosine protein kinase function with indolinone compounds |
MXPA02006474A (es) | 1999-12-28 | 2002-11-29 | Eisai Co Ltd | Compuestos heterociclicos que contienen sulfonamida. |
JP2001278886A (ja) * | 2000-03-28 | 2001-10-10 | Dai Ichi Seiyaku Co Ltd | ベンゾオキサジン誘導体及びこれを含有する医薬 |
GB0007934D0 (en) * | 2000-03-31 | 2000-05-17 | Darwin Discovery Ltd | Chemical compounds |
ES2317368T3 (es) | 2001-02-21 | 2009-04-16 | EISAI R&D MANAGEMENT CO., LTD. | Metodo para evaluar el efecto de un inhibidor de la angiogenesis a traves de la inhibicion de la expresion de la integrina. |
CA2707827A1 (en) | 2001-04-11 | 2002-10-24 | Senju Pharmaceutical Co., Ltd. | Visual function disorder improving agents containing rho kinase inhibitors |
US6559169B2 (en) | 2001-04-24 | 2003-05-06 | Wyeth | Antidepressant azaheterocyclymethyl derivatives of 2,3-dihydro-1,4-benzodioxan |
GB0114417D0 (en) | 2001-06-13 | 2001-08-08 | Boc Group Plc | Lubricating systems for regenerative vacuum pumps |
US20040171630A1 (en) | 2001-06-19 | 2004-09-02 | Yuntae Kim | Tyrosine kinase inhibitors |
US7291639B2 (en) | 2001-06-20 | 2007-11-06 | Wyeth | Aryloxy-acetic acid compounds useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1) |
GB0115109D0 (en) | 2001-06-21 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
UA75425C2 (en) | 2001-07-09 | 2006-04-17 | Piperazine oxime derivatives with antagonistic activity to nk-1 receptor, use thereof, a pharmaceutical composition based thereon, a method for producing and a method for producing intermediary compounds | |
GB0117583D0 (en) | 2001-07-19 | 2001-09-12 | Astrazeneca Ab | Novel compounds |
US6858860B2 (en) | 2001-07-24 | 2005-02-22 | Seiko Epson Corporation | Apparatus and method for measuring natural period of liquid |
GB0118479D0 (en) | 2001-07-28 | 2001-09-19 | Astrazeneca Ab | Novel compounds |
WO2003028724A1 (en) | 2001-10-04 | 2003-04-10 | Smithkline Beecham Corporation | Chk1 kinase inhibitors |
JPWO2003037862A1 (ja) | 2001-10-30 | 2005-02-17 | 日本新薬株式会社 | アミド誘導体及び医薬 |
US20030236277A1 (en) | 2002-02-14 | 2003-12-25 | Kadow John F. | Indole, azaindole and related heterocyclic pyrrolidine derivatives |
US6884889B2 (en) | 2002-03-25 | 2005-04-26 | Bristol-Myers Squibb Co. | Processes for the preparation of antiviral 7-azaindole derivatives |
JP2005534618A (ja) | 2002-03-28 | 2005-11-17 | エーザイ株式会社 | 神経変性疾患用の、c−junn−末端キナーゼ阻害剤としての7−アザインドール |
WO2003082869A1 (en) | 2002-03-28 | 2003-10-09 | Eisai Co., Ltd. | Azaindoles as inhibitors of c-jun n-terminal kinases |
GB0212785D0 (en) * | 2002-05-31 | 2002-07-10 | Glaxo Group Ltd | Compounds |
UA78999C2 (en) | 2002-06-04 | 2007-05-10 | Wyeth Corp | 1-(aminoalkyl)-3-sulfonylazaindoles as ligands of 5-hydroxytryptamine-6 |
TW200403243A (en) | 2002-07-18 | 2004-03-01 | Wyeth Corp | 1-Heterocyclylalkyl-3-sulfonylazaindole or-azaindazole derivatives as 5-hydroxytryptamine-6 ligands |
TWI329112B (en) | 2002-07-19 | 2010-08-21 | Bristol Myers Squibb Co | Novel inhibitors of kinases |
US6878887B2 (en) * | 2002-08-07 | 2005-04-12 | Matsushita Electric Industrial Co., Ltd. | Anti-malfunction mechanism for variable output device |
KR101476067B1 (ko) | 2002-09-06 | 2014-12-23 | 인설트 테라페틱스, 인코퍼레이티드 | 공유결합된 치료제 전달을 위한 사이클로덱스트린-기초 중합체 |
BR0317230A (pt) * | 2002-12-13 | 2005-10-25 | Smithkline Beecham Corp | Composto, composição, métodos de antagonizar uma atividade do receptor de quimiocina ccr-5, e de tratar uma infecção viral em um paciente, e, uso de um composto |
DE60323133D1 (de) * | 2002-12-13 | 2008-10-02 | Smithkline Beecham Corp | Cyclohexylverbindungen als ccr5-antagonisten |
US7696225B2 (en) | 2003-01-06 | 2010-04-13 | Osi Pharmaceuticals, Inc. | (2-carboxamido)(3-Amino) thiophene compounds |
SE0300120D0 (sv) | 2003-01-17 | 2003-01-17 | Astrazeneca Ab | Novel compounds |
SE0300119D0 (sv) | 2003-01-17 | 2003-01-17 | Astrazeneca Ab | Novel compounds |
US20050085463A1 (en) | 2003-01-23 | 2005-04-21 | Weiner David M. | Use of N-desmethylclozapine to treat human neuropsychiatric disease |
BRPI0407493A (pt) | 2003-02-14 | 2006-02-14 | Wyeth Corp | derivados heterociclil-3-sulfinilazaindol ou -azaindazol como ligantes de 5-hidroxitriptamina-6 |
DE10357510A1 (de) | 2003-12-09 | 2005-07-07 | Bayer Healthcare Ag | Heteroarylsubstituierte Benzole |
WO2005066347A1 (en) | 2003-12-24 | 2005-07-21 | Danisco A/S | Proteins |
GB0330042D0 (en) | 2003-12-24 | 2004-01-28 | Pharmacia Italia Spa | Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions them |
GB0330043D0 (en) | 2003-12-24 | 2004-01-28 | Pharmacia Italia Spa | Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions comprising them |
GB0403635D0 (en) | 2004-02-18 | 2004-03-24 | Devgen Nv | Pyridinocarboxamides with improved activity as kinase inhibitors |
GB0405055D0 (en) | 2004-03-05 | 2004-04-07 | Eisai London Res Lab Ltd | JNK inhibitors |
EP2786995A1 (en) | 2004-03-30 | 2014-10-08 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of JAK and other protein kinases |
US7498342B2 (en) | 2004-06-17 | 2009-03-03 | Plexxikon, Inc. | Compounds modulating c-kit activity |
AU2005265017A1 (en) * | 2004-06-17 | 2006-01-26 | Plexxikon, Inc. | Azaindoles modulating c-kit activity and uses therefor |
CA2572058A1 (en) | 2004-06-30 | 2006-01-12 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of protein kinases |
US7709645B2 (en) | 2004-07-27 | 2010-05-04 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
BRPI0513916A (pt) | 2004-07-27 | 2008-05-20 | Sgx Pharmaceuticals Inc | moduladores de pirrol-piridina cinase |
US7361764B2 (en) | 2004-07-27 | 2008-04-22 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
AU2005269387A1 (en) | 2004-07-27 | 2006-02-09 | Sgx Pharmaceuticals, Inc. | Fused ring heterocycle kinase modulators |
US7626021B2 (en) | 2004-07-27 | 2009-12-01 | Sgx Pharmaceuticals, Inc. | Fused ring heterocycle kinase modulators |
GB0419192D0 (en) * | 2004-08-27 | 2004-09-29 | Merck Sharp & Dohme | Therapeutic agents |
JP5033119B2 (ja) | 2005-04-25 | 2012-09-26 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | キナーゼ阻害剤としての新規アザ複素環化合物 |
MX2007014377A (es) | 2005-05-17 | 2008-02-06 | Plexxikon Inc | Inhibidores de proteina cinasa de derivados de pirrol (2,3-b) piridina. |
EP1881983B1 (en) | 2005-05-20 | 2012-01-11 | Vertex Pharmaceuticals, Inc. | Pyrrolopyridines useful as inhibitors of protein kinase |
BRPI0611863B1 (pt) * | 2005-06-22 | 2021-11-23 | Plexxikon, Inc | Composto, bem como composição e kit compreendendo o mesmo, composto intermediário na preparação do mesmo, método para tratamento e uso do mesmo |
GB0516156D0 (en) | 2005-08-05 | 2005-09-14 | Eisai London Res Lab Ltd | JNK inhibitors |
AU2007226983A1 (en) * | 2006-03-20 | 2007-09-27 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions |
WO2008063888A2 (en) * | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
WO2008079909A1 (en) * | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Pyrrolo [2,3-b] pyridines as kinase modulators |
PE20121126A1 (es) * | 2006-12-21 | 2012-08-24 | Plexxikon Inc | Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa |
CL2008001540A1 (es) | 2007-05-29 | 2009-05-22 | Sgx Pharmaceuticals Inc | Compuestos derivados de pirrolopiridinas y pirazolopiridinas; composicion farmaceutica; y uso en el tratamiento del cancer. |
TW201041888A (en) * | 2009-05-06 | 2010-12-01 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
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Patent Citations (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2234705A (en) * | 1940-04-12 | 1941-03-11 | Eastman Kodak Co | Cellulose organic derivative composition containing esters of monoalkoxy benzoic acids |
DE2413258A1 (de) * | 1974-03-20 | 1975-10-02 | Bayer Ag | Alkoxycarbonylphenylharnstoffe, verfahren zu ihrer herstellung und ihre verwendung als herbizide |
WO2004016610A1 (en) | 2002-08-14 | 2004-02-26 | Astrazeneca Ab | Substituted pyrrolopyridines |
WO2004024895A2 (en) | 2002-09-16 | 2004-03-25 | Plexxikon, Inc. | Crystal structure of pim-1 kinase |
US20040142864A1 (en) | 2002-09-16 | 2004-07-22 | Plexxikon, Inc. | Crystal structure of PIM-1 kinase |
WO2004078923A2 (en) | 2003-02-28 | 2004-09-16 | Plexxikon, Inc. | Pyk2 crystal structure and uses |
US20050170431A1 (en) | 2003-02-28 | 2005-08-04 | Plexxikon, Inc. | PYK2 crystal structure and uses |
WO2005028624A2 (en) | 2003-09-15 | 2005-03-31 | Plexxikon, Inc. | Molecular scaffolds for kinase ligand development |
US20050164300A1 (en) | 2003-09-15 | 2005-07-28 | Plexxikon, Inc. | Molecular scaffolds for kinase ligand development |
WO2005062795A2 (en) | 2003-12-19 | 2005-07-14 | Plexxikon, Inc. | Compounds and methods for development of ret modulators |
Non-Patent Citations (30)
Title |
---|
"Encyclopaedia of human biology", vol. 2, 1991, ACADEMIC PRESS, pages: 371 - 9 |
"Remington's Pharmaceutical Sciencess, 19th ed.,", vol. 2, 1995, MACK FUBJISBING CO., pages: 1457 |
"Synergism and Antagonism in Chemotherapy", 1991, ACADEMIC PRESS, pages: 61 - 102 |
"The Science and Practice of Pharmacy, 21 st edition,", 2005, LIPPINCOTT, WILLIAMS AND WILLDNS |
BAGSHAWE, DI-UG DEV RES, vol. 34, 1995, pages 220 - 230 |
BARTON ET AL.: "The chemistry of pentavalent organobismuth reagents. Part X. Studies on the phenylation and oxidation of phenols", TETRAHEDRON, vol. 43, no. 2, 1987, pages 323 - 332, XP002402100 * |
BERTOLINI ET AL., J MED CHEM, vol. 40, 1997, pages 2011 - 2016 |
BUCHWALD, J AM. CHEM. SOC., vol. 125, 2003, pages 2890 - 2891 |
BUCHWALD, J. AM. CHEM. SOC., vol. 125, 2003, pages 2890 - 2891 |
CHOU ET AL., ADV. ENZYME REGUL., vol. 22, 1984, pages 27 - 55 |
CHOU ET AL., J. NAT1. CANCER INST., vol. 86, 1994, pages 1517 - 24 |
CHOU; TALALAY, ADV. ENZYME REGUL., vol. 22, 1984, pages 27 - 55 |
COSTE, J. ORG. CHEM., vol. 59, 1994, pages 2437 |
CRUMP, CURR PHARM DES, vol. 8, no. 25, 2002, pages 2243 - 8 |
CURTIN ET AL.: "Discovery and Evaluation of a Series of 3-Acylindole Imidazopyridine Platelet-Activating Factor Antagonists", J. MED. CHEM., vol. 41, 1998, pages 74 - 95, XP002402103 * |
GREENE, T. W.; WUTS, P.G.M.: "Protective Groups in Organic Synthesis I, 3rd ed.", 1981, JOHN WILEY & SONS |
HEACOCK ET AL.: "Orientation and Relative Reaction rate Factors in aromatic Substitution by the Benzensulfonimido Radical", J. AM. CHEM. SOC., vol. 82, 1960, pages 3460 - 3463, XP002402102 * |
HOOD, J.D. ET AL., SCIENCE, vol. 296, 2002, pages 2404 |
KUNNIMALAIYAAN ET AL., ANTICANCER DRUGS, vol. 17, no. 2, 2005, pages 139 - 42 |
LANGHAM ET AL.: "Metalationof Halogen-Metal Interconversion Reactions of Some Halogenated Phenyl Ethers", J. AM. CHEM. SOC., vol. 63, 1941, pages 545 - 549, XP002402101 * |
MARCH: "Advanced Organic Chemistry: Reactions, Mechanisms and Stzucture", 1994, MCGRAW HILL |
MUYAURA; SUZUKI, CHEM. REV., vol. 95, 1995, pages 2457 |
NIIHORI ET AL., NAT GENET., vol. 38, no. 3, 2006, pages 294 - 6 |
ORG. SYN. COLLECTIVE, vol. 2, 1943, pages 292 |
PIERCE ET AL.: "Local anaesthetics. I. beta-Monoalkylaminoethyl Esters of Alkoxybenzoic Acids", J. AM. CHEM. SOC., vol. 64, 1942, pages 1691 - 1694, XP002402104 * |
SHAN ET AL., J PHARM SCI, vol. 86, pages 756 - 757 |
T. HAYASHI; M.KONISHI; Y. KOBORI; M. KUMADA; T. HIGUCHI; K. HIROTSU, J. AM . CHEM. SOC., vol. 106, 1984, pages 158 - 163 |
T. W. GREENE; P. G. M. WUTS: "Protective Groups in Organic Synthesis", 1991, JOHN WILEY & SONS |
THOMAS, J. AM. CHEM. SOC., vol. 123, 2001, pages 9404 |
WERMUTH: "The Practice of Medicinal Cbemistry", 2001, ACADEMIC PRESS |
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US8841304B2 (en) | 2008-01-08 | 2014-09-23 | Array Biopharma, Inc. | Pyrrolopyridines as kinase inhibitors |
US8372842B2 (en) | 2008-01-09 | 2013-02-12 | Array Biopharma Inc. | Pyrazolopyridines as kinase inhibitors |
JP2011510004A (ja) * | 2008-01-22 | 2011-03-31 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | タンパク質キナーゼ阻害剤及びその使用 |
JP2014040460A (ja) * | 2008-02-25 | 2014-03-06 | F. Hoffmann-La Roche Ag | ピロロピラジンキナーゼ阻害剤 |
US8394795B2 (en) | 2008-02-29 | 2013-03-12 | Array Biopharma Inc. | Pyrazole [3, 4-B] pyridine Raf inhibitors |
WO2009111280A1 (en) | 2008-02-29 | 2009-09-11 | Array Biopharma Inc. | N- (6-aminopyridin-3-yl) -3- (sulfonamido) benzamide derivatives as b-raf inhibitors for the treatment of cancer |
US8338452B2 (en) | 2008-02-29 | 2012-12-25 | Array Biopharma Inc. | Raf inhibitor compounds and methods of use thereof |
EP2282636B1 (en) | 2008-05-06 | 2016-03-23 | Novartis AG | Benzene sulfonamide thiazole and oxazole compounds |
US8912204B2 (en) | 2008-05-19 | 2014-12-16 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
US8153641B2 (en) | 2008-05-19 | 2012-04-10 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
US8158636B2 (en) | 2008-05-19 | 2012-04-17 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
US9260437B2 (en) | 2008-05-19 | 2016-02-16 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
WO2009141274A1 (en) * | 2008-05-21 | 2009-11-26 | Basf Se | Substituted pyridin-4 -yl-methyl sulfonamides as fungicides |
WO2009144159A1 (en) * | 2008-05-28 | 2009-12-03 | Basf Se | Substituted pyridin-4-yl-methyl sulfonamidesas fungicides |
US8119637B2 (en) | 2008-06-10 | 2012-02-21 | Plexxikon Inc. | Substituted pyrrolo[2,3-b]pyrazines and methods for kinase modulation, and indications therefor |
US8110576B2 (en) | 2008-06-10 | 2012-02-07 | Plexxikon Inc. | Substituted pyrrolo[2,3b]pyrazines and methods for treatment of raf protein kinase-mediated indications |
WO2009157196A1 (ja) | 2008-06-25 | 2009-12-30 | 武田薬品工業株式会社 | アミド化合物 |
DE102008052943A1 (de) | 2008-10-23 | 2010-04-29 | Merck Patent Gmbh | Azaindolderivate |
US8592448B2 (en) | 2008-11-20 | 2013-11-26 | OSI Pharmaceuticals, LLC | Substituted pyrrolo[2,3-b]-pyridines and -pyrazines |
JP2015052009A (ja) * | 2008-11-25 | 2015-03-19 | ユニバーシティー オブ ロチェスター | Mlk阻害剤および使用方法 |
AU2010224245B2 (en) * | 2009-03-11 | 2016-07-21 | Plexxikon, Inc. | Pyrrolo [2, 3-b] pyridine derivatives for the inhibition of Raf kinases |
KR101663339B1 (ko) * | 2009-03-11 | 2016-10-06 | 플렉시콘 인코퍼레이티드 | Raf 키나제의 억제를 위한 피롤로[2,3-b]피리딘 유도체 |
US8901301B2 (en) | 2009-03-11 | 2014-12-02 | Plexxikon Inc. | Pyrrolo[2,3-]pyridine kinase inhibitors |
JP2012520311A (ja) * | 2009-03-11 | 2012-09-06 | プレキシコン インコーポレーテッド | Rafキナーゼの阻害のためのピロロ[2,3−b]ピリジン誘導体 |
WO2010104945A1 (en) | 2009-03-11 | 2010-09-16 | Plexxikon, Inc. | Pyrrolo [2, 3-b] pyridine derivatives for the inhibition of raf kinases |
US8129404B2 (en) | 2009-03-11 | 2012-03-06 | Plexxikon Inc. | Compounds and uses thereof |
KR20110125670A (ko) * | 2009-03-11 | 2011-11-21 | 플렉시콘, 인코퍼레이티드 | Raf 키나제의 억제를 위한 피롤로[2,3-b]피리딘 유도체 |
WO2010104973A1 (en) * | 2009-03-11 | 2010-09-16 | Plexxikon, Inc. | Pyrrolo [2, 3-b] pyridine derivatives for the inhibition of raf kinases |
WO2010111527A1 (en) * | 2009-03-26 | 2010-09-30 | Plexxikon, Inc. | Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use |
KR101739994B1 (ko) | 2009-04-03 | 2017-05-25 | 에프. 호프만-라 로슈 아게 | 프로판-1-술폰산 {3-[5-(4-클로로-페닐)-1H-피롤로[2,3-b]피리딘-3-카르보닐]-2,4-디플루오로-페닐}-아미드 조성물 및 그의 용도 |
US9447089B2 (en) | 2009-04-03 | 2016-09-20 | Plexxikon Inc. | Compositions and uses thereof |
US9663517B2 (en) | 2009-04-03 | 2017-05-30 | Plexxikon Inc. | Compositions and uses thereof |
JP2012526127A (ja) * | 2009-05-06 | 2012-10-25 | プレキシコン インコーポレーテッド | Rafプロテインキナーゼを阻害するピロロ[2,3.b]ピリジン類 |
US8198273B2 (en) | 2009-05-06 | 2012-06-12 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
US20120245174A1 (en) * | 2009-05-06 | 2012-09-27 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
US9334274B2 (en) | 2009-05-22 | 2016-05-10 | Incyte Holdings 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 |
US9216984B2 (en) | 2009-05-22 | 2015-12-22 | Incyte Corporation | 3-[4-(7H-pyrrolo[2,3-D]pyrimidin-4-yl)-1H-pyrazol-1-yl]octane—or heptane-nitrile as JAK inhibitors |
US9623029B2 (en) | 2009-05-22 | 2017-04-18 | Incyte Holdings Corporation | 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octane- or heptane-nitrile as JAK inhibitors |
US9345708B2 (en) | 2009-06-17 | 2016-05-24 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
US9808459B2 (en) | 2009-06-17 | 2017-11-07 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
US9518056B2 (en) | 2009-06-17 | 2016-12-13 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
US10874673B2 (en) | 2009-06-17 | 2020-12-29 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
US10039762B2 (en) | 2009-06-17 | 2018-08-07 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
US8829007B2 (en) | 2009-06-17 | 2014-09-09 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
US10251889B2 (en) | 2009-07-09 | 2019-04-09 | Array BioPharm Inc. | Substituted pyrazolo[1,5-a]pyrimidine compounds as Trk kinase inhibitors |
US10758542B2 (en) | 2009-07-09 | 2020-09-01 | Array Biopharma Inc. | Substituted pyrazolo[l,5-a]pyrimidine compounds as Trk kinase inhibitors |
WO2011015522A2 (en) | 2009-08-03 | 2011-02-10 | F. Hoffmann-La Roche Ag | Process for the manufacture of pharmaceutically active compounds |
US8741920B2 (en) | 2009-08-03 | 2014-06-03 | Hoffmann-La Roche, Inc. | Process for the manufacture of pharmaceutically active compounds |
US8530661B2 (en) | 2009-08-03 | 2013-09-10 | Hoffmann-La Roche, Inc. | Process for the manufacture of pharmaceutically active compounds |
US8329724B2 (en) | 2009-08-03 | 2012-12-11 | Hoffmann-La Roche Inc. | Process for the manufacture of pharmaceutically active compounds |
US8648086B2 (en) | 2009-08-24 | 2014-02-11 | Ascepion Pharmaceuticals, Inc. | 5,6-bicyclic heteroaryl-containing urea compounds as kinase inhibitors |
WO2011025968A1 (en) | 2009-08-28 | 2011-03-03 | Array Biopharma Inc. | 1h-pyrazolo [ 3, 4-b] pyridine compounds for inhibiting raf kinase |
WO2011025940A1 (en) | 2009-08-28 | 2011-03-03 | Array Biopharma Inc. | Raf inhibitor compounds and methods of use thereof |
WO2011025951A1 (en) | 2009-08-28 | 2011-03-03 | Array Biopharma Inc. | Raf inhibitor compounds and methods of use thereof |
WO2011025938A2 (en) | 2009-08-28 | 2011-03-03 | Array Biopharma Inc. | Raf inhibitor compounds and methods of use thereof |
WO2011025947A1 (en) | 2009-08-28 | 2011-03-03 | Array Biopharma Inc. | Raf inhibitor compounds and methods of use thereof |
WO2011025965A1 (en) | 2009-08-28 | 2011-03-03 | Genentech, Inc. | Raf inhibitor compounds and methods of use thereof |
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 |
WO2011057022A1 (en) | 2009-11-06 | 2011-05-12 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
US9096593B2 (en) | 2009-11-06 | 2015-08-04 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
WO2011057974A1 (en) | 2009-11-11 | 2011-05-19 | F. Hoffmann-La Roche Ag | Propane-i-sulfonic acid {3-[5-(4-chloro-phenyl)-1h-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide compositions and uses thereof |
US8673928B2 (en) | 2009-11-18 | 2014-03-18 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
WO2011063159A1 (en) | 2009-11-18 | 2011-05-26 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
US9617267B2 (en) | 2009-11-18 | 2017-04-11 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
JP2013513627A (ja) * | 2009-12-14 | 2013-04-22 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | 癌などの疾患を処置するためのチアゾール誘導体 |
US9440969B2 (en) | 2009-12-23 | 2016-09-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
US11826365B2 (en) | 2009-12-29 | 2023-11-28 | Dana-Farber Cancer Institute, Inc. | Type II raf kinase inhibitors |
AU2016201096B2 (en) * | 2009-12-29 | 2017-08-31 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
US20160046636A1 (en) * | 2009-12-29 | 2016-02-18 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
AU2010343102B2 (en) * | 2009-12-29 | 2016-03-24 | Dana-Farber Cancer Institute, Inc. | Type II Raf kinase inhibitors |
US9358231B2 (en) | 2009-12-29 | 2016-06-07 | Dana-Farber Cancer Institute, Inc. | Type II RAF kinase inhibitors |
US9023354B2 (en) | 2010-01-06 | 2015-05-05 | Joseph P. Errico | Combination therapy with MDM2 and EFGR inhibitors |
US20150105412A1 (en) | 2010-01-06 | 2015-04-16 | Joseph P. Errico | Combination therapy with mdm2 and efgr inhibitors |
US8658170B2 (en) | 2010-01-06 | 2014-02-25 | Joseph P. Errico | Combination therapy with MDM2 and EFGR inhibitors |
US9273031B2 (en) | 2010-01-06 | 2016-03-01 | Joseph P. Errico | Combination therapy with MDM2 and EFGR inhibitors |
US9073858B2 (en) | 2010-01-06 | 2015-07-07 | Joseph P. Errico | Methods of targeted drug development |
US8618302B2 (en) | 2010-01-06 | 2013-12-31 | Joseph P. Errico | Methods and compositions of targeted drug development |
WO2011085129A3 (en) * | 2010-01-06 | 2011-09-01 | Errico Joseph P | Methods and compositions of targeted drug development |
US9108963B2 (en) | 2010-02-11 | 2015-08-18 | Vanderbilt University | Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
JP2013519684A (ja) * | 2010-02-11 | 2013-05-30 | ヴァンダービルト ユニバーシティー | mGluR4アロステリック増強剤としてのピラゾロピリジン、ピラゾロピラジン、ピラゾロピリミジン、ピラゾロチオフェンおよびピラゾロチアゾール化合物、組成物、および神経機能不全を治療する方法 |
US9163015B2 (en) | 2010-02-11 | 2015-10-20 | Vanderbilt University | Pyrazolopyridine, pyrarolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
US11285140B2 (en) | 2010-03-10 | 2022-03-29 | Incyte Corporation | Piperidin-4-yl azetidine derivatives as JAK1 inhibitors |
US10695337B2 (en) | 2010-03-10 | 2020-06-30 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as JAK1 inhibitors |
US9999619B2 (en) | 2010-03-10 | 2018-06-19 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as JAK1 inhibitors |
US9464088B2 (en) | 2010-03-10 | 2016-10-11 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as JAK1 inhibitors |
US9359445B2 (en) | 2010-03-25 | 2016-06-07 | The J. David Gladstone Institutes | Compositions and methods for treating neurological disorders |
US9221812B2 (en) | 2010-04-16 | 2015-12-29 | Ac Immune Sa | Compounds for the treatment of diseases associated with amyloid or amyloid-like proteins |
WO2011128455A1 (en) | 2010-04-16 | 2011-10-20 | Ac Immune S.A. | Novel compounds for the treatment of diseases associated with amyloid or amyloid-like proteins |
JP2013525297A (ja) * | 2010-04-16 | 2013-06-20 | エーシー・イミューン・エス・アー | アミロイドまたはアミロイド様タンパク質と関連する疾患を治療するための新規化合物 |
JP2013525490A (ja) * | 2010-05-06 | 2013-06-20 | メルク・シャープ・エンド・ドーム・コーポレイション | Faahのモジュレータとして有用なアザインドール誘導体 |
EP2566481A4 (en) * | 2010-05-06 | 2014-01-22 | Merck Sharp & Dohme | AS FAAH MODULATORS SUITABLE AZA-INDOL DERIVATIVES |
EP2566481A1 (en) * | 2010-05-06 | 2013-03-13 | Merck Sharp & Dohme Corp. | Aza-indole derivatives useful as modulators of faah |
JP2013526569A (ja) * | 2010-05-14 | 2013-06-24 | オーエスアイ・ファーマシューティカルズ,エルエルシー | 縮合二環式キナーゼ阻害剤 |
CN102971316A (zh) * | 2010-05-14 | 2013-03-13 | Osi药物有限责任公司 | 稠双环激酶抑制剂 |
WO2011143645A1 (en) | 2010-05-14 | 2011-11-17 | OSI Pharmaceuticals, LLC | Fused bicyclic kinase inhibitors |
WO2011143646A1 (en) | 2010-05-14 | 2011-11-17 | OSI Pharmaceuticals, LLC | Fused bicyclic kinase inhibitors |
US8445510B2 (en) | 2010-05-14 | 2013-05-21 | OSI Pharmaceuticals, LLC | Fused bicyclic kinase inhibitors |
US11571425B2 (en) | 2010-05-21 | 2023-02-07 | Incyte Corporation | Topical formulation for a JAK inhibitor |
US10869870B2 (en) | 2010-05-21 | 2020-12-22 | Incyte Corporation | Topical formulation for a JAK inhibitor |
US11590136B2 (en) | 2010-05-21 | 2023-02-28 | Incyte Corporation | Topical formulation for a JAK inhibitor |
US10758543B2 (en) | 2010-05-21 | 2020-09-01 | Incyte Corporation | Topical formulation for a JAK inhibitor |
US11219624B2 (en) | 2010-05-21 | 2022-01-11 | Incyte Holdings Corporation | Topical formulation for a JAK inhibitor |
US9593317B2 (en) | 2010-06-09 | 2017-03-14 | Bayer Cropscience Nv | Methods and means to modify a plant genome at a nucleotide sequence commonly used in plant genome engineering |
US9150594B2 (en) | 2010-07-21 | 2015-10-06 | Hoffmann-La Roche Inc. | Processes for the manufacture of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide |
US8779150B2 (en) | 2010-07-21 | 2014-07-15 | Hoffmann-La Roche Inc. | Processes for the manufacture of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1 H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide |
US9556172B2 (en) | 2010-07-21 | 2017-01-31 | Hoffman La-Roche Inc. | Processes for the manufacture of propane-1-sulfonic acid (3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl)-amide |
WO2012010538A2 (en) | 2010-07-21 | 2012-01-26 | F. Hoffmann-La Roche Ag | Novel processes for the manufacture of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1h-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide |
US9034884B2 (en) | 2010-11-19 | 2015-05-19 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors |
US10640506B2 (en) | 2010-11-19 | 2020-05-05 | Incyte Holdings Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidines derivatives as JAK inhibitors |
US8933085B2 (en) | 2010-11-19 | 2015-01-13 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
WO2012075327A1 (en) | 2010-12-02 | 2012-06-07 | University Of Pittsburgh-Of The Commonwealth System Of Higher Education | Methods for treating a tumor using an antibody that specifically binds grp94 |
US8871774B2 (en) | 2010-12-16 | 2014-10-28 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
US8937088B2 (en) | 2011-01-06 | 2015-01-20 | Astar Biotech Llc | Ureas for the treatment and prevention of cancer |
JP2016138119A (ja) * | 2011-02-07 | 2016-08-04 | プレキシコン インコーポレーテッドPlexxikon Inc. | キナーゼ調節のための化合物および方法、ならびにそれに対する適応症 |
US9624213B2 (en) | 2011-02-07 | 2017-04-18 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
US11337976B2 (en) | 2011-02-07 | 2022-05-24 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
WO2012109075A1 (en) | 2011-02-07 | 2012-08-16 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
US9993480B2 (en) | 2011-02-18 | 2018-06-12 | Novartis Pharma Ag | mTOR/JAK inhibitor combination therapy |
WO2012161776A1 (en) | 2011-02-21 | 2012-11-29 | Plexxikon Inc. | Solid forms of a pharmaceutically active substance |
EP3281675A1 (en) | 2011-02-21 | 2018-02-14 | Plexxikon Inc. | Solid forms of a pharmaceutically active substance |
US8865735B2 (en) | 2011-02-21 | 2014-10-21 | Hoffman-La Roche Inc. | Solid forms of a pharmaceutically active substance |
WO2012158658A1 (en) | 2011-05-16 | 2012-11-22 | OSI Pharmaceuticals, LLC | Fused bicyclic kinase inhibitors |
US9550768B2 (en) | 2011-05-17 | 2017-01-24 | Plexxikon Inc. | Kinase modulation and indications therefor |
WO2012170752A1 (en) * | 2011-06-10 | 2012-12-13 | Glaxo Wellcome Manufacturing Pte Ltd | Novel compounds |
US8877742B2 (en) | 2011-06-10 | 2014-11-04 | Glaxosmithkline Intellectual Property Limited | Compounds |
US9023840B2 (en) | 2011-06-20 | 2015-05-05 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors |
US11214573B2 (en) | 2011-06-20 | 2022-01-04 | Incyte Holdings Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors |
US9611269B2 (en) | 2011-06-20 | 2017-04-04 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors |
US8691807B2 (en) | 2011-06-20 | 2014-04-08 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors |
US10513522B2 (en) | 2011-06-20 | 2019-12-24 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors |
US10875855B2 (en) | 2011-08-01 | 2020-12-29 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
US9051319B2 (en) | 2011-08-01 | 2015-06-09 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
US10646567B2 (en) | 2011-08-01 | 2020-05-12 | Genentech, Inc. | Methods of treating cancer using PD-1 axis binding antagonists and MEK inhibitors |
US9908878B2 (en) | 2011-08-01 | 2018-03-06 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
US9394302B2 (en) | 2011-08-01 | 2016-07-19 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
US9358229B2 (en) | 2011-08-10 | 2016-06-07 | Novartis Pharma Ag | JAK PI3K/mTOR combination therapy |
US9359358B2 (en) | 2011-08-18 | 2016-06-07 | Incyte Holdings Corporation | Cyclohexyl azetidine derivatives as JAK inhibitors |
US9718834B2 (en) | 2011-09-07 | 2017-08-01 | Incyte Corporation | Processes and intermediates for making a JAK inhibitor |
US9487521B2 (en) | 2011-09-07 | 2016-11-08 | Incyte Holdings Corporation | Processes and intermediates for making a JAK inhibitor |
WO2013043715A1 (en) | 2011-09-19 | 2013-03-28 | Genentech, Inc. | Combination treatments comprising c-met antagonists and b-raf antagonists |
US20140296204A1 (en) * | 2011-10-24 | 2014-10-02 | Glaxosmithkline Intellectual Property (No.2) Limited | Chemical compounds |
EP2771011A4 (en) * | 2011-10-24 | 2015-04-15 | Glaxosmithkline Ip No 2 Ltd | CHEMICAL COMPOUNDS |
EP2771011A1 (en) * | 2011-10-24 | 2014-09-03 | Glaxosmithkline Intellectual Property (No. 2) Limited | Chemical compounds |
US9174984B2 (en) | 2011-10-24 | 2015-11-03 | Glaxosmithkline Intellectual Property (No.2) Limited | Chemical compounds |
US10981903B2 (en) | 2011-11-17 | 2021-04-20 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-Jun-N-terminal kinase (JNK) |
US10144730B2 (en) | 2011-11-17 | 2018-12-04 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-Jun-N-terminal kinase (JNK) |
EP3124472A1 (en) | 2011-12-31 | 2017-02-01 | BeiGene, Ltd. | Fused tricyclic compounds as raf kinase inhibitors |
WO2013142427A1 (en) | 2012-03-19 | 2013-09-26 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
US9358235B2 (en) | 2012-03-19 | 2016-06-07 | Plexxikon Inc. | Kinase modulation, and indications therefor |
EP4295912A2 (en) | 2012-03-19 | 2023-12-27 | Daiichi Sankyo, Inc. | Compounds and methods for kinase modulation, and indications therefor |
US10123998B2 (en) | 2012-03-19 | 2018-11-13 | Plexxikon Inc. | Kinase modulation, and indications therefor |
US9730918B2 (en) | 2012-03-19 | 2017-08-15 | Plexxikon Inc. | Kinase modulation, and indications therefor |
US9193733B2 (en) | 2012-05-18 | 2015-11-24 | Incyte Holdings Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
US20150141428A1 (en) * | 2012-05-22 | 2015-05-21 | Merck Sharp & Dohme Corp. | TrkA Kinase Inhibitors, Compositions and Methods Thereof |
US9181261B2 (en) * | 2012-05-22 | 2015-11-10 | Merck Sharp & Dohme Corp. | TrkA kinase inhibitors, compositions and methods thereof |
US20140094611A1 (en) * | 2012-05-31 | 2014-04-03 | Plexxikon Inc. | Synthesis of heterocyclic compounds |
WO2013181415A1 (en) | 2012-05-31 | 2013-12-05 | Plexxikon Inc. | Synthesis of pyrrolo [2, 3 - b] pyridines |
US9150570B2 (en) * | 2012-05-31 | 2015-10-06 | Plexxikon Inc. | Synthesis of heterocyclic compounds |
US9382241B2 (en) | 2012-05-31 | 2016-07-05 | Genentech, Inc. | Aminoquinazoline and pyridopyrimidine derivatives |
JP2015518051A (ja) * | 2012-05-31 | 2015-06-25 | プレキシコン インコーポレーテッドPlexxikon Inc. | ピロロ[2,3−b]ピリジンの合成 |
US9592235B2 (en) | 2012-05-31 | 2017-03-14 | Genentech, Inc. | Aminoquinazoline and pyridopyrimidine derivatives |
US9695169B2 (en) | 2012-05-31 | 2017-07-04 | Plexxikon Inc. | Synthesis of heterocyclic compounds |
EP3550031A1 (en) | 2012-07-24 | 2019-10-09 | Pharmacyclics, LLC | Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk) |
US11783366B2 (en) | 2012-08-17 | 2023-10-10 | Genentech, Inc. | Combination therapies |
US11087354B2 (en) | 2012-08-17 | 2021-08-10 | Genentech, Inc. | Combination therapies |
US9399639B2 (en) | 2012-08-27 | 2016-07-26 | Calitor Sciences, Llc | Substituted azaindole compounds, salts, pharmaceutical compositions thereof and methods of use |
US9163021B2 (en) | 2012-10-04 | 2015-10-20 | Pfizer Limited | Pyrrolo[3,2-c]pyridine tropomyosin-related kinase inhibitors |
US10787436B2 (en) | 2012-10-18 | 2020-09-29 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
US10112927B2 (en) | 2012-10-18 | 2018-10-30 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
US9758522B2 (en) | 2012-10-19 | 2017-09-12 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
USRE48175E1 (en) | 2012-10-19 | 2020-08-25 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
US10000483B2 (en) | 2012-10-19 | 2018-06-19 | Dana-Farber Cancer Institute, Inc. | Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof |
US10874616B2 (en) | 2012-11-15 | 2020-12-29 | Incyte Corporation | Sustained-release dosage forms of ruxolitinib |
US11896717B2 (en) | 2012-11-15 | 2024-02-13 | Incyte Holdings Corporation | Sustained-release dosage forms of ruxolitinib |
US11337927B2 (en) | 2012-11-15 | 2022-05-24 | Incyte Holdings Corporation | Sustained-release dosage forms of ruxolitinib |
US11576865B2 (en) | 2012-11-15 | 2023-02-14 | Incyte Corporation | Sustained-release dosage forms of ruxolitinib |
US10166191B2 (en) | 2012-11-15 | 2019-01-01 | Incyte Corporation | Sustained-release dosage forms of ruxolitinib |
US11576864B2 (en) | 2012-11-15 | 2023-02-14 | Incyte Corporation | Sustained-release dosage forms of ruxolitinib |
EP2931722A4 (en) * | 2012-12-14 | 2016-09-21 | Arrien Pharmaeuticals Llc | SUBSTITUTED 1H-PYRROLO- [2,3-B] PYRIDINE AND 1H-PYRAZOLO- [3,4-B] PYRIDINE DERIVATIVES AS SALT-INDUCIBLE KINASE-2 (SIK2) INHIBITORS |
US9890153B2 (en) | 2012-12-14 | 2018-02-13 | Arrien Pharmaceuticals Llc | Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors |
JP2016504316A (ja) * | 2012-12-14 | 2016-02-12 | アーリーン ファーマシューティカルズ エルエルシー | 塩誘導性キナーゼ2(SIK2)阻害剤としての置換された1H−ピロロ[2,3−b]ピリジン及び1H−ピラゾロ[3,4−b]ピリジン誘導体 |
US9951062B2 (en) | 2012-12-14 | 2018-04-24 | Arrien Pharmaceuticals Llc | Substituted 1 H-pyrrolo [2, 3-b] pyridine and 1 H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors |
US9676750B2 (en) | 2013-01-14 | 2017-06-13 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
US9278950B2 (en) | 2013-01-14 | 2016-03-08 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
US9550765B2 (en) | 2013-01-15 | 2017-01-24 | Incyte Holdings Corporation | Thiazolecarboxamides and pyridinecarboxamide compounds useful as Pim kinase inhibitors |
US9200004B2 (en) | 2013-01-15 | 2015-12-01 | Incyte Holdings Corporation | Thiazolecarboxamides and pyridinecarboxamide compounds useful as Pim kinase inhibitors |
US10265307B2 (en) | 2013-01-15 | 2019-04-23 | Incyte Corporation | Thiazolecarboxamides and pyridinecarboxamide compounds useful as Pim kinase inhibitors |
US10828290B2 (en) | 2013-01-15 | 2020-11-10 | Incyte Corporation | Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors |
US9849120B2 (en) | 2013-01-15 | 2017-12-26 | Incyte Holdings Corporation | Thiazolecarboxamides and pyridinecarboxamide compounds useful as Pim kinase inhibitors |
US11229631B2 (en) | 2013-01-15 | 2022-01-25 | Incyte Corporation | Thiazolecarboxamides and pyridinecarboxamide compounds useful as Pim kinase inhibitors |
US10517858B2 (en) | 2013-01-15 | 2019-12-31 | Incyte Holdings Corporation | Thiazolecarboxamides and pyridinecarboxamide compounds useful as PIM kinase inhibitors |
WO2014130856A2 (en) * | 2013-02-21 | 2014-08-28 | Wayne Rothbaum | Treatment of skeletal-related disorders |
WO2014130856A3 (en) * | 2013-02-21 | 2014-10-16 | Wayne Rothbaum | Treatment of skeletal-related disorders |
WO2014128235A1 (en) | 2013-02-22 | 2014-08-28 | F. Hoffmann-La Roche Ag | Methods of treating cancer and preventing drug resistance |
US8987443B2 (en) | 2013-03-06 | 2015-03-24 | Incyte Corporation | Processes and intermediates for making a JAK inhibitor |
US9221845B2 (en) | 2013-03-06 | 2015-12-29 | Incyte Holdings Corporation | Processes and intermediates for making a JAK inhibitor |
US9714233B2 (en) | 2013-03-06 | 2017-07-25 | Incyte Corporation | Processes and intermediates for making a JAK inhibitor |
WO2014144850A1 (en) | 2013-03-15 | 2014-09-18 | Genentech, Inc. | Methods of treating cancer and preventing cancer drug resistance |
WO2014194127A1 (en) | 2013-05-30 | 2014-12-04 | Plexxikon Inc. | Compounds for kinase modulation, and indications therefor |
WO2014206344A1 (en) | 2013-06-28 | 2014-12-31 | Beigene, Ltd. | Fused tricyclic amide compounds as multiple kinase inhibitors |
US11045421B2 (en) | 2013-08-07 | 2021-06-29 | Incyte Corporation | Sustained release dosage forms for a JAK1 inhibitor |
US10561616B2 (en) | 2013-08-07 | 2020-02-18 | Incyte Corporation | Sustained release dosage forms for a JAK1 inhibitor |
US9655854B2 (en) | 2013-08-07 | 2017-05-23 | Incyte Corporation | Sustained release dosage forms for a JAK1 inhibitor |
US9556197B2 (en) | 2013-08-23 | 2017-01-31 | Incyte Corporation | Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors |
US10000507B2 (en) | 2013-08-23 | 2018-06-19 | Incyte Corporation | Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors |
US11040957B2 (en) | 2013-10-18 | 2021-06-22 | Dana-Farber Cancer Institute, Inc. | Heteroaromatic compounds useful for the treatment of proliferative diseases |
US10906889B2 (en) | 2013-10-18 | 2021-02-02 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7) |
US10640501B2 (en) | 2013-11-13 | 2020-05-05 | Vertex Pharmaceuticals Incorporated | Methods of preparing inhibitors of influenza viruses replication |
US10023569B2 (en) | 2013-11-13 | 2018-07-17 | Vertex Pharmaceuticals Incorporated | Methods of preparing inhibitors of influenza viruses replication |
US11345700B2 (en) | 2013-11-13 | 2022-05-31 | Vertex Pharmaceuticals Incorporated | Methods of preparing inhibitors of influenza viruses replication |
US9771361B2 (en) | 2013-11-13 | 2017-09-26 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
JP2020196723A (ja) * | 2013-11-15 | 2020-12-10 | ザ ウィスター インスティテュート オブ アナトミー アンド バイオロジー | Ebna1阻害剤およびそれらの使用方法 |
JP2016540045A (ja) * | 2013-11-15 | 2016-12-22 | ザ ウィスター インスティテュート オブ アナトミー アンド バイオロジー | Ebna1阻害剤およびそれらの使用方法 |
US11242317B2 (en) | 2013-11-15 | 2022-02-08 | The Wistar Institute Of Anatomy And Biology | EBNA1 inhibitors and their method of use |
US10421718B2 (en) | 2013-11-15 | 2019-09-24 | The Wistar Institute Of Anatomy And Biology | EBNA1 inhibitors and their method of use |
WO2015078424A1 (en) | 2013-11-27 | 2015-06-04 | Zentiva, K.S. | Crystalline forms of vemurafenib |
US10017477B2 (en) | 2014-04-23 | 2018-07-10 | Dana-Farber Cancer Institute, Inc. | Janus kinase inhibitors and uses thereof |
US9862688B2 (en) | 2014-04-23 | 2018-01-09 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged janus kinase inhibitors and uses thereof |
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 |
JP2017516814A (ja) * | 2014-06-03 | 2017-06-22 | ギリアード サイエンシーズ, インコーポレイテッド | Tank結合キナーゼインヒビター化合物 |
US10259811B2 (en) | 2014-06-03 | 2019-04-16 | Gilead Sciences, Inc. | Tank-binding kinase inhibitor compounds |
US10072001B2 (en) | 2014-06-03 | 2018-09-11 | Gilead Sciences, Inc. | Tank-binding kinase inhibitor compounds |
WO2015191986A1 (en) | 2014-06-13 | 2015-12-17 | Genentech, Inc. | Methods of treating and preventing cancer drug resistance |
US9580416B2 (en) | 2014-07-02 | 2017-02-28 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase |
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 |
US9890162B2 (en) | 2014-07-14 | 2018-02-13 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
EP3563870A1 (en) | 2014-07-15 | 2019-11-06 | F. Hoffmann-La Roche AG | Methods of treating cancer using pd-1 axis binding antagonists and mek inhibitors |
WO2016011160A1 (en) | 2014-07-15 | 2016-01-21 | Genentech, Inc. | Compositions for treating cancer using pd-1 axis binding antagonists and mek inhibitors |
US10946093B2 (en) | 2014-07-15 | 2021-03-16 | Genentech, Inc. | Methods of treating cancer using PD-1 axis binding antagonists and MEK inhibitors |
US10253019B2 (en) | 2014-09-26 | 2019-04-09 | Gilead Sciences, Inc. | Tank-binding kinase inhibitor compounds |
US10040781B2 (en) | 2014-09-26 | 2018-08-07 | Gilead Sciences, Inc. | Tank-binding kinase inhibitor compounds |
WO2016057367A1 (en) | 2014-10-06 | 2016-04-14 | Dana-Farber Cancer Institute, Inc. | Angiopoietin-2 biomarkers predictive of anti-immune checkpoint response |
US10870651B2 (en) | 2014-12-23 | 2020-12-22 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
US11583586B2 (en) | 2014-12-23 | 2023-02-21 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
US10849980B2 (en) | 2014-12-23 | 2020-12-01 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
US11059801B2 (en) | 2014-12-23 | 2021-07-13 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
US10550121B2 (en) | 2015-03-27 | 2020-02-04 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
US11325910B2 (en) | 2015-03-27 | 2022-05-10 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
WO2016165676A1 (en) | 2015-04-14 | 2016-10-20 | Zentiva, K.S. | Amorphous forms of vemurafenib |
US10533004B2 (en) | 2015-05-13 | 2020-01-14 | Vertex Pharmaceuticals Incorporated | Methods of preparing inhibitors of influenza viruses replication |
US10273233B2 (en) | 2015-05-13 | 2019-04-30 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
US10442763B2 (en) | 2015-05-14 | 2019-10-15 | The Wistar Institute Of Anatomy And Biology | EBNA1 inhibitors and methods using same |
US11912659B2 (en) | 2015-05-14 | 2024-02-27 | The Wistar Institute Of Anatomy And Biology | EBNA1 inhibitors and methods using same |
US10981867B2 (en) | 2015-05-14 | 2021-04-20 | The Wistar Institute Of Anatomy And Biology | EBNA1 inhibitors and methods using same |
WO2016191295A1 (en) | 2015-05-22 | 2016-12-01 | Plexxikon Inc. | Solid forms of a compound for modulating kinases |
US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
US9802918B2 (en) | 2015-05-29 | 2017-10-31 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
US10174027B2 (en) | 2015-07-16 | 2019-01-08 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as RET kinase inhibitors |
US10023570B2 (en) | 2015-07-16 | 2018-07-17 | Array Biopharma Inc. | Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors |
US10174028B2 (en) | 2015-07-16 | 2019-01-08 | Array Biopharma Inc. | Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors |
US10138243B2 (en) | 2015-07-16 | 2018-11-27 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as RET kinase inhibitors |
WO2017011776A1 (en) | 2015-07-16 | 2017-01-19 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
US11274108B2 (en) | 2015-07-20 | 2022-03-15 | Genzyme Corporation | Colony stimulating factor-1 receptor (CSF-1R) inhibitors |
AU2016297558B2 (en) * | 2015-07-20 | 2021-03-25 | Genzyme Corporation | Colony stimulating factor-1 receptor (CSF-1R) inhibitors |
AU2021204116B2 (en) * | 2015-07-20 | 2022-12-01 | Genzyme Corporation | Colony stimulating factor-1 receptor (CSF-1R) inhibitors |
US11505540B2 (en) | 2015-09-09 | 2022-11-22 | Incyte Corporation | Salts of a Pim kinase inhibitor |
US10336728B2 (en) | 2015-09-09 | 2019-07-02 | Incyte Corporation | Salts of a Pim kinase inhibitor |
US11142507B2 (en) | 2015-09-09 | 2021-10-12 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
US9862705B2 (en) | 2015-09-09 | 2018-01-09 | Incyte Corporation | Salts of a pim kinase inhibitor |
US11066387B2 (en) | 2015-09-09 | 2021-07-20 | Incyte Corporation | Salts of a Pim kinase inhibitor |
US9920032B2 (en) | 2015-10-02 | 2018-03-20 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
US10450296B2 (en) | 2015-10-02 | 2019-10-22 | Incyte Corporation | Heterocyclic compounds useful as Pim kinase inhibitors |
US11053215B2 (en) | 2015-10-02 | 2021-07-06 | Incyte Corporation | Heterocyclic compounds useful as Pim kinase inhibitors |
US10724102B2 (en) | 2015-10-26 | 2020-07-28 | Loxo Oncology, Inc. | Point mutations in TRK inhibitor-resistant cancer and methods relating to the same |
US10907215B2 (en) | 2015-10-26 | 2021-02-02 | Loxo Oncology, Inc. | Point mutations in TRK inhibitor-resistant cancer and methods relating to the same |
WO2017087851A1 (en) | 2015-11-19 | 2017-05-26 | Genentech, Inc. | Methods of treating cancer using b-raf inhibitors and immune checkpoint inhibitors |
US10316049B2 (en) | 2015-12-17 | 2019-06-11 | Gilead Sciences, Inc. | Tank-binding kinase inhibitor compounds |
WO2017176744A1 (en) | 2016-04-04 | 2017-10-12 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
US10137127B2 (en) | 2016-04-04 | 2018-11-27 | Loxo Oncology, Inc. | Liquid formulations of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-A]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
US11191766B2 (en) | 2016-04-04 | 2021-12-07 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
US10668072B2 (en) | 2016-04-04 | 2020-06-02 | Loxo Oncology, Inc. | Liquid formulations of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
WO2017176751A1 (en) | 2016-04-04 | 2017-10-12 | Loxo Oncology, Inc. | Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
US11484535B2 (en) | 2016-04-04 | 2022-11-01 | Loxo Oncology, Inc. | Liquid formulations of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a] pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
US10588908B2 (en) | 2016-04-04 | 2020-03-17 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
WO2017180581A1 (en) | 2016-04-15 | 2017-10-19 | Genentech, Inc. | Diagnostic and therapeutic methods for cancer |
US11214571B2 (en) | 2016-05-18 | 2022-01-04 | Array Biopharma Inc. | Process for the preparation of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide and salts thereof |
US10407427B2 (en) | 2016-07-01 | 2019-09-10 | Fermion Oy | Processes for the preparation of Vemurafenib |
WO2018002415A1 (en) | 2016-07-01 | 2018-01-04 | Fermion Oy | New processes for the preparation of vemurafenib |
US11001591B2 (en) | 2016-09-16 | 2021-05-11 | Helmholtz Zentrum Muenchen—Deutsches Forschungszentrum Für Gesundheit Und Umwelt (Gmbh) | TRAF 6 inhibitors |
RU2770404C2 (ru) * | 2016-09-16 | 2022-04-15 | Гельмгольц Центрум Мюнхен - Дойчес Форшунгсцентрум Фюр Гезундхайт Унд Умвельт (Гмбх) | Ингибиторы traf 6 |
CN109715631A (zh) * | 2016-09-16 | 2019-05-03 | 德国亥姆霍兹慕尼黑中心健康与环境研究中心(有限公司) | Traf 6抑制剂 |
CN109715631B (zh) * | 2016-09-16 | 2022-02-18 | 德国亥姆霍兹慕尼黑中心健康与环境研究中心(有限公司) | Traf 6抑制剂 |
WO2018050286A1 (en) * | 2016-09-16 | 2018-03-22 | Helmholtz Zentrum Muenchen - Deutsches Forschungszentrum Für Gesundheit Und Umwelt (Gmbh) | Traf 6 inhibitors |
US10669278B2 (en) | 2016-09-16 | 2020-06-02 | Helmholtz Zentrum Muenchen—Deutsches Forschungszentrum Für Gesundheit Und Umwelt (Gmbh) | TRAF 6 inhibitors |
US10881652B2 (en) | 2016-10-10 | 2021-01-05 | Array Biopharma Inc. | Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors |
US10172851B2 (en) | 2016-10-10 | 2019-01-08 | Array Biopharma Inc. | Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors |
WO2018071454A1 (en) | 2016-10-10 | 2018-04-19 | Andrews Steven W | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
EP3753939A1 (en) | 2016-10-10 | 2020-12-23 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
JP7079303B2 (ja) | 2016-10-10 | 2022-06-01 | アレイ バイオファーマ インコーポレイテッド | Retキナーゼ阻害剤としての置換ピラゾロ[1,5-a]ピリジン化合物 |
JP2021035944A (ja) * | 2016-10-10 | 2021-03-04 | アレイ バイオファーマ、インコーポレイテッド | Retキナーゼ阻害剤としての置換ピラゾロ[1,5−a]ピリジン化合物 |
EP4144735A1 (en) | 2016-10-10 | 2023-03-08 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
US10953005B1 (en) | 2016-10-10 | 2021-03-23 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as RET kinase inhibitors |
US10441581B2 (en) | 2016-10-10 | 2019-10-15 | Array Biopharma Inc. | Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors |
US10144734B2 (en) | 2016-10-10 | 2018-12-04 | Array Biopharma Inc. | Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors |
JP2020503247A (ja) * | 2016-10-10 | 2020-01-30 | アレイ バイオファーマ、インコーポレイテッド | Retキナーゼ阻害剤としての置換ピラゾロ[1,5−a]ピリジン化合物 |
US10112942B2 (en) | 2016-10-10 | 2018-10-30 | Array Biopharma Inc. | Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors |
US10172845B2 (en) | 2016-10-10 | 2019-01-08 | Array Biopharma Inc. | Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors |
US11648243B2 (en) | 2016-10-10 | 2023-05-16 | Array Biopharma Inc. | Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors |
WO2018071447A1 (en) | 2016-10-10 | 2018-04-19 | Andrews Steven W | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
US10555944B2 (en) | 2016-10-10 | 2020-02-11 | Eli Lilly And Company | Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors |
US10137124B2 (en) | 2016-10-10 | 2018-11-27 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as RET kinase inhibitors |
US11091486B2 (en) | 2016-10-26 | 2021-08-17 | Array Biopharma, Inc | Process for the preparation of pyrazolo[1,5-a]pyrimidines and salts thereof |
AU2018209164B2 (en) * | 2017-01-17 | 2021-11-04 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
WO2018134254A1 (en) | 2017-01-17 | 2018-07-26 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
US11040027B2 (en) | 2017-01-17 | 2021-06-22 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
WO2018136661A1 (en) | 2017-01-18 | 2018-07-26 | Andrews Steven W | SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS |
US11168090B2 (en) | 2017-01-18 | 2021-11-09 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors |
US11851434B2 (en) | 2017-01-18 | 2023-12-26 | Array Biopharma Inc. | Substituted pyrazolo[1,5-A]pyrazine compounds as ret kinase inhibitors |
WO2018146253A1 (en) | 2017-02-10 | 2018-08-16 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the mapk pathway |
US10688100B2 (en) | 2017-03-16 | 2020-06-23 | Array Biopharma Inc. | Macrocylic compounds as ROS1 kinase inhibitors |
US10966985B2 (en) | 2017-03-16 | 2021-04-06 | Array Biopharma Inc. | Macrocyclic compounds as ROS1 kinase inhibitors |
WO2018170381A1 (en) | 2017-03-16 | 2018-09-20 | Andrews Steven W | Macrocyclic compounds as ros1 kinase inhibitors |
US11555031B2 (en) | 2017-03-20 | 2023-01-17 | The Broad Institute, Inc. | Compounds and methods for regulating insulin secretion |
WO2018175324A1 (en) | 2017-03-20 | 2018-09-27 | The Broad Institute, Inc. | Compounds and methods for regulating insulin secretion |
EP3601326A4 (en) * | 2017-03-20 | 2020-12-16 | The Broad Institute, Inc. | COMPOUNDS AND METHODS OF REGULATING INSULIN SECRETION |
WO2018210661A1 (en) * | 2017-05-15 | 2018-11-22 | Basf Se | Heteroaryl compounds as agrochemical fungicides |
US11161845B2 (en) | 2017-05-19 | 2021-11-02 | Nflection Therapeutics, Inc. | Pyrrolopyridine-aniline compounds for treatment of dermal disorders |
JP2020520995A (ja) * | 2017-05-19 | 2020-07-16 | エヌフレクション セラピューティクス インコーポレイテッド | 皮膚障害の処置用のピロロピリジン−アニリン化合物 |
KR102642411B1 (ko) * | 2017-05-19 | 2024-02-28 | 엔플렉션 테라퓨틱스, 인코포레이티드 | 피부병 치료를 위한 피롤로피리딘-아닐린 화합물 |
US11542271B2 (en) | 2017-05-19 | 2023-01-03 | Nflection Therapeutics, Inc. | Fused heteroaromatic-aniline compounds for treatment of dermal disorders |
KR20200013239A (ko) * | 2017-05-19 | 2020-02-06 | 엔플렉션 테라퓨틱스, 인코포레이티드 | 피부병 치료를 위한 피롤로피리딘-아닐린 화합물 |
JP7212956B2 (ja) | 2017-05-19 | 2023-01-26 | エヌフレクション セラピューティクス インコーポレイテッド | 皮膚障害の処置用のピロロピリジン-アニリン化合物 |
WO2018213810A1 (en) * | 2017-05-19 | 2018-11-22 | Nflection Therapeutics, Inc. | Pyrrolopyridine-aniline compounds for treatment of dermal disorders |
US10988483B2 (en) | 2017-05-19 | 2021-04-27 | Nflection Therapeutics, Inc. | Fused heteroaromatic-aniline compounds for treatment of dermal disorders |
AU2018270295B2 (en) * | 2017-05-19 | 2022-03-03 | Nflection Therapeutics, Inc. | Pyrrolopyridine-aniline compounds for treatment of dermal disorders |
CN111065393B (zh) * | 2017-05-19 | 2023-08-18 | 恩福莱克逊治疗有限公司 | 用于治疗皮肤疾病的吡咯并吡啶-苯胺类化合物 |
CN111065393A (zh) * | 2017-05-19 | 2020-04-24 | 恩福莱克逊治疗有限公司 | 用于治疗皮肤疾病的吡咯并吡啶-苯胺类化合物 |
US11787804B2 (en) | 2017-06-30 | 2023-10-17 | The Regents Of The University Of California | Compositions and methods for modulating hair growth |
US11312714B2 (en) | 2017-06-30 | 2022-04-26 | The Regents Of The University Of California | Compositions and methods for modulating hair growth |
WO2019051296A1 (en) | 2017-09-08 | 2019-03-14 | Genentech, Inc. | DIAGNOSTIC AND THERAPEUTIC METHODS OF CANCER |
WO2019075108A1 (en) | 2017-10-10 | 2019-04-18 | Metcalf Andrew T | CRYSTALLINE FORMS |
WO2019075114A1 (en) | 2017-10-10 | 2019-04-18 | Mark Reynolds | FORMULATIONS COMPRISING 6- (2-HYDROXY-2-METHYLPROPOXY) -4- (6- (6 - ((6-METHOXYPYRIDIN-3-YL) METHYL) -3,6-DIAZABICYCLO [3.1.1] HEPTAN-3- YL) PYRIDIN-3-YL) PYRAZOLO [1,5-A] pYRIDINE-3-carbonitrile |
US11278541B2 (en) | 2017-12-08 | 2022-03-22 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
US10596161B2 (en) | 2017-12-08 | 2020-03-24 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
WO2019133810A1 (en) | 2017-12-28 | 2019-07-04 | Tract Pharmaceuticals, Inc. | Stem cell culture systems for columnar epithelial stem cells, and uses related thereto |
WO2019143994A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
US11472802B2 (en) | 2018-01-18 | 2022-10-18 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors |
US11524963B2 (en) | 2018-01-18 | 2022-12-13 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidines as RET kinase inhibitors |
WO2019143977A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
US11603374B2 (en) | 2018-01-18 | 2023-03-14 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
US10899736B2 (en) | 2018-01-30 | 2021-01-26 | Incyte Corporation | Processes and intermediates for making a JAK inhibitor |
US11858927B2 (en) | 2018-01-31 | 2024-01-02 | Heparegenix Gmbh | Protein kinase MKK4 inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
WO2019149738A1 (en) | 2018-01-31 | 2019-08-08 | Heparegenix Gmbh | Protein kinase mkk4 inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
WO2019158579A1 (en) | 2018-02-13 | 2019-08-22 | Vib Vzw | Targeting minimal residual disease in cancer with rxr antagonists |
US11304949B2 (en) | 2018-03-30 | 2022-04-19 | Incyte Corporation | Treatment of hidradenitis suppurativa using JAK inhibitors |
US11242338B2 (en) | 2018-05-17 | 2022-02-08 | The Wistar Institute | EBNA1 inhibitor crystalline forms, and methods of preparing and using same |
US11731968B2 (en) | 2018-06-21 | 2023-08-22 | Heparegenix Gmbh | Tricyclic protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
WO2019243315A1 (en) | 2018-06-21 | 2019-12-26 | Heparegenix Gmbh | Tricyclic protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
US11912701B2 (en) | 2018-07-16 | 2024-02-27 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
JP7365393B2 (ja) | 2018-07-16 | 2023-10-19 | ヘパリジェニックス ゲーエムベーハー | 肝再生促進又は肝細胞死の抑制もしくは防止のためのプロテインキナーゼ阻害剤 |
JP2021529815A (ja) * | 2018-07-16 | 2021-11-04 | ヘパリジェニックス ゲーエムベーハー | 肝再生促進又は肝細胞死の抑制もしくは防止のためのプロテインキナーゼ阻害剤 |
WO2020016243A1 (en) | 2018-07-16 | 2020-01-23 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
KR102592556B1 (ko) * | 2018-07-19 | 2023-10-23 | 썬전 링팡 바이오테크 컴퍼니 리미티드 | 아자인돌 유도체 및 이의 FGFR과 C-Met 억제제로서의 용도 |
JP7317938B2 (ja) | 2018-07-19 | 2023-07-31 | シェンチェン リンファン バイオテック カンパニー,リミティド | アザインドール誘導体とFGFR及びC-Met阻害剤としてのその使用 |
JP2021531290A (ja) * | 2018-07-19 | 2021-11-18 | メッドシャイン ディスカバリー インコーポレイテッド | アザインドール誘導体とFGFR及びC−Met阻害剤としてのその使用 |
KR20210035236A (ko) * | 2018-07-19 | 2021-03-31 | 메드샤인 디스커버리 아이엔씨. | 아자인돌 유도체 및 이의 FGFR과 C-Met 억제제로서의 용도 |
EP3825314A4 (en) * | 2018-07-19 | 2022-04-06 | Medshine Discovery Inc. | AZAINDOL DERIVATIVE AND ITS USE AS FGFR AND C-MET INHIBITOR |
WO2020028258A1 (en) | 2018-07-31 | 2020-02-06 | Loxo Oncology, Inc. | Spray-dried dispersions and formulations of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoro propan-2-yl)-1h-pyrazole-4-carboxamide |
US11964988B2 (en) | 2018-09-10 | 2024-04-23 | Array Biopharma Inc. | Fused heterocyclic compounds as RET kinase inhibitors |
WO2020055672A1 (en) | 2018-09-10 | 2020-03-19 | Array Biopharma Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
WO2020070390A1 (en) | 2018-10-03 | 2020-04-09 | Jyväskylän Yliopisto | Vemurafenib and salts thereof for use in the treatment of enteroviral infections |
WO2020079581A1 (en) | 2018-10-16 | 2020-04-23 | Novartis Ag | Tumor mutation burden alone or in combination with immune markers as biomarkers for predicting response to targeted therapy |
WO2020102686A1 (en) * | 2018-11-16 | 2020-05-22 | California Institute Of Technology | Erk inhibitors and uses thereof |
US11572344B2 (en) | 2018-11-20 | 2023-02-07 | Nflection Therapeutics, Inc. | Cyanoaryl-aniline compounds for treatment of dermal disorders |
WO2020131674A1 (en) | 2018-12-19 | 2020-06-25 | Array Biopharma Inc. | 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer |
WO2020131627A1 (en) | 2018-12-19 | 2020-06-25 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases |
WO2020243519A1 (en) * | 2019-05-29 | 2020-12-03 | Ifm Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
CN114008042B (zh) * | 2019-05-31 | 2023-10-03 | 重庆复尚源创医药技术有限公司 | 作为蛋白激酶抑制剂的取代的吡咯并[2,3-b]吡啶及吡唑并[3,4-b]吡啶衍生物 |
CN114008042A (zh) * | 2019-05-31 | 2022-02-01 | 重庆复创医药研究有限公司 | 作为蛋白激酶抑制剂的取代的吡咯并[2,3-b]吡啶及吡唑并[3,4-b]吡啶衍生物 |
WO2020239124A1 (en) * | 2019-05-31 | 2020-12-03 | Fochon Pharmaceuticals, Ltd. | SUBSTITUTED PYRROLO [2, 3-b] PYRIDINE AND PYRAZOLO [3, 4-b] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS |
WO2021018820A1 (en) | 2019-07-29 | 2021-02-04 | Heparegenix Gmbh | Heteroaryl-substituted pyrazolo-pyridine protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
WO2021134004A1 (en) | 2019-12-27 | 2021-07-01 | Schrodinger, Inc. | Cyclic compounds and methods of using same |
WO2021144287A1 (en) | 2020-01-15 | 2021-07-22 | Heparegenix Gmbh | 3-benzoyl-1h-pyrrolo[2,3-b]pyridine derivatives as mkk4 inhibitors for treating liver diseases |
WO2021152005A1 (en) | 2020-01-28 | 2021-08-05 | Universite De Strasbourg | Antisense oligonucleotide targeting linc00518 for treating melanoma |
US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
WO2022055963A1 (en) | 2020-09-10 | 2022-03-17 | Schrödinger, Inc. | Heterocyclic pericondensed cdc7 kinase inhibitors for the treatment of cancer |
WO2022063101A1 (zh) * | 2020-09-23 | 2022-03-31 | 劲方医药科技(上海)有限公司 | 芳甲酰取代的三环化合物及其制法和用途 |
CN116234550A (zh) * | 2020-09-23 | 2023-06-06 | 劲方医药科技(上海)有限公司 | 芳甲酰取代的三环化合物及其制法和用途 |
WO2022105746A1 (en) * | 2020-11-17 | 2022-05-27 | Fochon Pharmaceuticals, Ltd. | SUBSTITUTED PYRROLO [2, 3-b] PYRIDINE AND PYRAZOLO [3, 4-b] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS |
WO2022125524A1 (en) * | 2020-12-07 | 2022-06-16 | Lieber Institute, Inc. | Compounds for inhibiting inositol hexakisphosphate kinase (ip6k) and methods of use thereof |
WO2022121900A1 (zh) * | 2020-12-07 | 2022-06-16 | 南京明德新药研发有限公司 | 吡咯并吡啶类化合物及其应用 |
US11530216B2 (en) | 2020-12-23 | 2022-12-20 | Genzyme Corporation | Deuterated colony stimulating factor-1 receptor (CSF-1R) inhibitors |
WO2022164789A1 (en) | 2021-01-26 | 2022-08-04 | Schrödinger, Inc. | Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disoders |
WO2022195551A1 (en) | 2021-03-18 | 2022-09-22 | Novartis Ag | Biomarkers for cancer and methods of use thereof |
WO2022197898A1 (en) | 2021-03-18 | 2022-09-22 | Schrödinger, Inc. | Cyclic compounds and methods of using same |
WO2023174300A1 (zh) * | 2022-03-15 | 2023-09-21 | 劲方医药科技(上海)有限公司 | Btk抑制剂的晶型及其酸式盐和其酸式盐的晶型 |
WO2024003350A1 (en) | 2022-06-30 | 2024-01-04 | Universite De Strasbourg | Combination therapy for melanoma |
WO2024033381A1 (en) | 2022-08-10 | 2024-02-15 | Vib Vzw | Inhibition of tcf4/itf2 in the treatment of cancer |
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