AR087752A1 - Compuestos y composiciones como inhibidores de la quinasa c-kit - Google Patents
Compuestos y composiciones como inhibidores de la quinasa c-kitInfo
- Publication number
- AR087752A1 AR087752A1 ARP120103222A ARP120103222A AR087752A1 AR 087752 A1 AR087752 A1 AR 087752A1 AR P120103222 A ARP120103222 A AR P120103222A AR P120103222 A ARP120103222 A AR P120103222A AR 087752 A1 AR087752 A1 AR 087752A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- independently selected
- membered
- unsubstituted
- alkyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title 1
- 125000005842 heteroatom Chemical group 0.000 abstract 19
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 10
- 125000001072 heteroaryl group Chemical group 0.000 abstract 10
- KIWSYRHAAPLJFJ-DNZSEPECSA-N n-[(e,2z)-4-ethyl-2-hydroxyimino-5-nitrohex-3-enyl]pyridine-3-carboxamide Chemical compound [O-][N+](=O)C(C)C(/CC)=C/C(=N/O)/CNC(=O)C1=CC=CN=C1 KIWSYRHAAPLJFJ-DNZSEPECSA-N 0.000 abstract 10
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 7
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 abstract 6
- 125000005843 halogen group Chemical group 0.000 abstract 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 5
- 125000003003 spiro group Chemical group 0.000 abstract 5
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 2
- WNXJIVFYUVYPPR-UHFFFAOYSA-N 1,3-dioxolane Chemical compound C1COCO1 WNXJIVFYUVYPPR-UHFFFAOYSA-N 0.000 abstract 2
- IZXIZTKNFFYFOF-UHFFFAOYSA-N 2-Oxazolidone Chemical compound O=C1NCCO1 IZXIZTKNFFYFOF-UHFFFAOYSA-N 0.000 abstract 2
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 abstract 2
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 abstract 2
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 abstract 2
- 230000002159 abnormal effect Effects 0.000 abstract 2
- SHQSVMDWKBRBGB-UHFFFAOYSA-N cyclobutanone Chemical compound O=C1CCC1 SHQSVMDWKBRBGB-UHFFFAOYSA-N 0.000 abstract 2
- BGTOWKSIORTVQH-UHFFFAOYSA-N cyclopentanone Chemical compound O=C1CCCC1 BGTOWKSIORTVQH-UHFFFAOYSA-N 0.000 abstract 2
- 229910052805 deuterium Inorganic materials 0.000 abstract 2
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 abstract 1
- 101000692455 Homo sapiens Platelet-derived growth factor receptor beta Proteins 0.000 abstract 1
- 101150038994 PDGFRA gene Proteins 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 108010051742 Platelet-Derived Growth Factor beta Receptor Proteins 0.000 abstract 1
- 102000018967 Platelet-Derived Growth Factor beta Receptor Human genes 0.000 abstract 1
- 102100026547 Platelet-derived growth factor receptor beta Human genes 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- KTHXBEHDVMTNOH-UHFFFAOYSA-N cyclobutanol Chemical compound OC1CCC1 KTHXBEHDVMTNOH-UHFFFAOYSA-N 0.000 abstract 1
- 230000002074 deregulated effect Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- AHHWIHXENZJRFG-UHFFFAOYSA-N oxetane Chemical compound C1COC1 AHHWIHXENZJRFG-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/04—Drugs for disorders of the respiratory system for throat disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Otolaryngology (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Transplantation (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Enzymes And Modification Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se proporcionan compuestos y composiciones farmacéuticas, los cuales son útiles como inhibidores de las proteínas quinasas, así como también métodos para utilizar tales compuestos y así tratar, aliviar o prevenir una condición asociada con actividad anormal o desregulada de las quinasas, que involucran activación anormal de la c-kit o quinasas c-kit y PDGFR (PDGFRa, PDGFRb). Reivindicación 1: Un compuesto de la fórmula (1) o de la fórmula (2), o una sal farmacéuticamente aceptable del mismo, en donde: m es 1 y R²⁰ se selecciona a partir de H, halo, alquilo C₁₋₆, haloalquilo C₁₋₆, haloalcoxilo C₁₋₆, deuterio, alquilo C₁₋₆ deuterado, -CN, -(CR⁹₂)ₙOR⁴, -C(O)R⁴, -(CR⁹₂)ₙC(=O)OR⁴, R¹⁰, -(CR⁹₂)ₙR¹⁰, -((CR⁹₂)O)ₜR⁴, -(CR⁹₂)ₙO(CR⁹₂)ₙR⁷, -(CR⁹₂)ₙC(=O)R⁴, -C(=O)N(R⁴)₂, -OR⁴ y -(CR⁹₂)ₙCN; ó m es 4 y R²⁰ es deuterio; R¹ se selecciona a partir de alquilo C₁₋₆ y halo; cada R¹¹ se selecciona independientemente a partir de H, halo, y alquilo C₁₋₆; L¹ es un enlace, -NH- ó -C(=O)NH-; L² es -(CR⁹₂)ₙ-, -CHR⁶-, -(CR⁹₂)ₙO-, -NH-, -(CR⁹₂)ₙC(=O)-, -C(=O)O(CR⁹₂)ₙ-, -(CR⁹₂)ₙOC(=O)NR⁴-, -(CR⁹₂)ₙNR⁴C(=O)(CR⁹₂)ₙ-, -(CR⁹₂)ₙNR⁴C(=O)- ó -(CR⁹₂)ₙNR⁴C(=O)O-; R² es R³ ó L²R³; R³ se selecciona a partir de un cicloalquilo C₃₋₈ no sustituido, una ciclobutanona, una ciclopentanona y un cicloalquilo C₃₋₈ sustituido, en donde el cicloalquilo C₃₋₈ sustituido de R² es sustituido por 1 - 4 sustituyentes independientemente seleccionados a partir de alquilo C₁₋₆, halo, haloalquilo C₁₋₆, -OR⁴, -CN, -C(=O)OR⁴, -C(=O)R⁴, -C(=O)R⁷, -C(=O)OR⁵, -(CR⁹₂)ₙOR⁴, -O(CR⁹₂)ₙOR⁴, -C(=O)O(CR⁹₂)ₙOR⁴, -N(R⁴)₂, =N-OR⁴, =N-O-(CR⁹₂)ₙR⁵, -C(=O)NR⁴₂, -NR⁴C(=O)OR⁴, -NR⁴C(=O)(CR⁹₂)ₙOR⁴, -NR⁴(CR⁹₂)OR⁴, -NR⁴S(=O)₂R⁴, -N(C(=O)OR⁴)₂, =CH₂, =CH(CR⁹₂)ₙOR⁴, R⁸, -(CR⁹₂)ₙR⁸, alcoxilo C₁₋₆ deuterado, -S(=O)₂R⁴, -S(=O)₂R⁷, -S(=O)₂R⁸, -S(=O)₂N(R⁴)₂, -S(=O)₂NHC(=O)OR⁴, -S(=O)₂(CR⁹₂)ₙC(=O)OR⁴, -S(=O)₂(CR⁹₂)ₙOR⁴, un dioxolano espiro unido, un dioxolano espiro unido el cual es sustituido por alquilo C₁₋₆, un dioxano espiro unido, un tetrahidrofuranilo espiro unido, un oxetano espiro unido, una ciclobutanona espiro unida, un ciclobutanol espiro unido, un puente de alquilo C₁, un heterocicloalquilo no sustituido de 5 - 6 miembros con 1 - 2 heteroátomos independientemente seleccionados a partir de N, O y S, un heterocicloalquilo de 5 - 6 miembros con 1 - 2 heteroátomos independientemente seleccionados a partir de N, O y S sustituidos por 1 - 3 sustituyentes independientemente seleccionados a partir de alquilo C₁₋₆, halo, haloalquilo C₁₋₆, haloalcoxilo C₁₋₆, -OR⁴ y R⁸; cada R⁴ se selecciona independientemente a partir de H y alquilo C₁₋₆; R⁵ es un cicloalquilo C₃₋₈ no sustituido, un heterocicloalquilo no sustituido de 5 - 6 miembros con 1 - 2 heteroátomos independientemente seleccionados a partir de N u O ó un cicloalquilo C₃₋₈ sustituido por 1 - 3 sustituyentes independientemente seleccionados a partir de alquilo C₁₋₆; cada R⁶ se selecciona independientemente a partir de -NHC(O)OR⁴, -OR⁴ y -(CR⁹₂)ₙOR⁴; cada R⁷ se selecciona independientemente a partir de haloalquilo C₁₋₆; R⁸ se selecciona a partir de un fenilo no sustituido, heteroarilo no sustituido de 5 - 6 miembros con 1 - 3 heteroátomos independientemente seleccionados a partir de N, O ó S, un heteroarilo no sustituido de 5 miembros con 1 - 4 heteroátomos seleccionados a partir de N, un heterocicloalquilo no sustituido de 4 - 6 miembros con 1 - 2 heteroátomos independientemente seleccionados a partir de N, O ó S, un cicloalquilo C₃₋₈ no sustituido, un heteroarilo sustituido de 5 - 6 miembros con 1 - 3 heteroátomos independientemente seleccionados a partir de N, O ó S, un fenilo sustituido, un heteroarilo sustituido de 5 miembros con 1 - 4 heteroátomos seleccionados a partir de N, un heterocicloalquilo sustituido de 4 - 6 miembros con 1 - 2 heteroátomos independientemente seleccionados a partir de N, O ó S, un cicloalquilo C₃₋₈ sustituido, una oxazolidin-2-ona, pirrolidinona y una pirrolidin-2-ona, en donde el fenilo sustituido, el heteroarilo sustituido de 5 - 6 miembros con 1 - 3 heteroátomos independientemente seleccionados a partir de N, O ó S, el heteroarilo sustituido de 5 miembros con 1 - 4 heteroátomos seleccionados a partir de N, el cicloalquilo C₃₋₈ sustituido y el heterocicloalquilo sustituido de 4 - 6 miembros de R⁸ son sustituidos por 1 - 3 sustituyentes independientemente seleccionados a partir de alquilo C₁₋₆, -(C(R⁹)₂)ₙOR⁴, -(C(R⁹)₂)ₙR⁵, -(C(R⁹)₂)ₙC(O)OR⁴, -C(O)OR⁴ y -S(O)₂R⁴; cada R⁹ se selecciona independientemente a partir de H y alquilo C₁₋₆; cada R⁹ se selecciona a partir de un fenilo no sustituido, un heteroarilo no sustituido de 5 - 6 miembros con 1 - 2 heteroátomos independientemente seleccionados a partir de N, O ó S, un heteroarilo no sustituido de 5 miembros con 1 - 4 heteroátomos seleccionados a partir de N, un heterocicloalquilo no sustituido de 4 - 6 miembros con 1 - 2 heteroátomos independientemente seleccionados a partir de N, O ó S, un cicloalquilo C₃₋₈ no sustituido, un heteroarilo sustituido de 5 - 6 miembros con 1 - 2 heteroátomos independientemente seleccionados a partir de N, O ó S, un fenilo sustituido, un heteroarilo sustituido de 5 miembros con 1 - 4 heteroátomos seleccionados a partir de N, un heterocicloalquilo sustituido de 4 - 6 miembros con 1 - 2 heteroátomos independientemente seleccionados a partir de N, O ó S, un cicloalquilo C₃₋₈ sustituido, una oxazolidin-2-ona, pirrolidinona y una pirrolidin-2-ona, en donde el fenilo sustituido, heteroarilo sustituido de 5 - 6 miembros con 1 - 2 heteroátomos independientemente seleccionados a partir de N, O ó S, el heteroarilo sustituido de 5 miembros con 1 - 4 heteroátomos seleccionados a partir de N, cicloalquilo C₃₋₈ sustituido y heterocicloalquilo sustituido de 4 - 6 miembros de R⁸ son sustituidos por 1 - 3 sustituyentes independientemente seleccionados a partir de alquilo C₁₋₆, -(C(R⁹)₂)ₙOR⁴, -(C(R⁹)₂)ₙR⁵, -(C(R⁹)₂)ₙC(O)OR⁴ y -S(O)₂R⁴; t es 1, 2 ó 3, y cada n se selecciona independientemente a partir de 1, 2, 3 y 4.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161530028P | 2011-09-01 | 2011-09-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR087752A1 true AR087752A1 (es) | 2014-04-16 |
Family
ID=46829898
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120103222A AR087752A1 (es) | 2011-09-01 | 2012-08-31 | Compuestos y composiciones como inhibidores de la quinasa c-kit |
Country Status (42)
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX339937B (es) | 2011-09-01 | 2016-06-17 | Novartis Ag * | Compuestos y composiciones como inhibidores de la quinasa c-kit. |
| UY34305A (es) | 2011-09-01 | 2013-04-30 | Novartis Ag | Derivados de heterociclos bicíclicos para el tratamiento de la hipertensión arterial pulmonar |
| US9309243B2 (en) | 2012-07-13 | 2016-04-12 | Ucb Biopharma Sprl | Imidazopyridine derivatives as modulators of TNF activity |
| AU2014205483B2 (en) | 2013-01-10 | 2017-11-30 | Gilead Sciences, Inc. | Non-selective kinase inhibitors |
| US9073921B2 (en) | 2013-03-01 | 2015-07-07 | Novartis Ag | Salt forms of bicyclic heterocyclic derivatives |
| JP6483714B2 (ja) | 2013-10-11 | 2019-03-13 | ローレンス エス． ジスマン， | 噴霧乾燥製剤 |
| US20160362408A1 (en) * | 2013-12-05 | 2016-12-15 | Bayer Pharma Aktiengesellschaft | Aryl- and hetaryl-substituted imidazo[1,2-a]pyridine-3-carboxamides and use thereof |
| CN103965190A (zh) * | 2014-05-20 | 2014-08-06 | 定陶县友帮化工有限公司 | 一种咪唑并[1,2-a]吡啶-3-甲酸的合成方法 |
| EP3316968A1 (en) | 2015-07-02 | 2018-05-09 | Janssen Sciences Ireland UC | Antibacterial compounds |
| US10059708B2 (en) * | 2016-04-26 | 2018-08-28 | Northwestern University | Therapeutic targeting of the interleukin 1 receptor-associated kinase 4 (IRAK4) in leukemias characterized by rearrangements in the mixed lineage leukemia gene (MLL-r) |
| AU2017286368B2 (en) | 2016-06-16 | 2021-02-25 | Janssen Sciences Ireland Unlimited Company | Heterocyclic compounds as antibacterials |
| EA201990044A1 (ru) | 2016-06-16 | 2019-05-31 | Янссен Сайенсиз Айрлэнд Анлимитед Компани | Гетероциклические соединения в качестве антибактериальных средств |
| WO2018081567A1 (en) | 2016-10-27 | 2018-05-03 | Pulmokine, Inc. | Combination therapy for treating pulmonary hypertension |
| US11224596B2 (en) | 2017-03-01 | 2022-01-18 | Janssen Sciences Ireland Unlimited Company | PZA and cytochrome bc1 inhibitor combination treatment |
| CN111039946A (zh) * | 2018-10-15 | 2020-04-21 | 上海轶诺药业有限公司 | 一类咪唑并芳环类化合物的制备和应用 |
| JP2022526713A (ja) | 2019-03-21 | 2022-05-26 | オンクセオ | がんの処置のための、キナーゼ阻害剤と組み合わせたＤｂａｉｔ分子 |
| EP3969453A4 (en) * | 2019-05-13 | 2023-01-18 | Novartis AG | CRYSTALLINE FORMS OF N-(5-(5-((1R,2S)-2-FLUOROCYCLOPROPYL)-1,2,4-OXADIAZOL-3-YL)-2-METHYLPHENYL)IMIDAZO[1,2-A]PYRIDINE- 3-CARBOXAMIDE |
| KR20220062564A (ko) | 2019-09-13 | 2022-05-17 | 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 | 항균 화합물 |
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| GB9518993D0 (en) * | 1995-09-16 | 1995-11-15 | Agrevo Uk Ltd | Fungicides |
| US20070072861A1 (en) * | 2000-03-27 | 2007-03-29 | Barbara Roniker | Method of using cyclooxygenase-2 inhibitors in the prevention of cardiovascular disorders |
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| JP2007524596A (ja) | 2003-02-28 | 2007-08-30 | トランスフォーム・ファーマシューティカルズ・インコーポレイテッド | 共結晶医薬組成物 |
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| BR112013012078A2 (pt) * | 2010-11-15 | 2019-09-24 | Abbvie Inc | inibidores de nampt e rock |
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| BR112014003963A2 (pt) * | 2011-09-01 | 2017-03-21 | Irm Llc | compostos e composições como inibidores de quinase c-kit |
| MX339937B (es) * | 2011-09-01 | 2016-06-17 | Novartis Ag * | Compuestos y composiciones como inhibidores de la quinasa c-kit. |
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