AR095280A1 - Derivados heterocíclicos de imidazo[1,2-a]piridina - Google Patents
Derivados heterocíclicos de imidazo[1,2-a]piridinaInfo
- Publication number
- AR095280A1 AR095280A1 ARP140100893A ARP140100893A AR095280A1 AR 095280 A1 AR095280 A1 AR 095280A1 AR P140100893 A ARP140100893 A AR P140100893A AR P140100893 A ARP140100893 A AR P140100893A AR 095280 A1 AR095280 A1 AR 095280A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- independently selected
- halo
- optionally substituted
- alkoxy
- Prior art date
Links
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 13
- 125000005843 halogen group Chemical group 0.000 abstract 12
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 5
- 125000005842 heteroatom Chemical group 0.000 abstract 5
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 4
- 125000004366 heterocycloalkenyl group Chemical group 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 125000006546 (C4-C10) cycloalkyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000006580 bicyclic heterocycloalkyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000002207 metabolite Substances 0.000 abstract 1
- 125000006578 monocyclic heterocycloalkyl group Chemical group 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61P11/06—Antiasthmatics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Obesity (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Endocrinology (AREA)
- Dermatology (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Reivindicación 1: Un compuesto de acuerdo con la fórmula (1), donde R¹ᵃ es H, halo o alquilo C₁₋₄; R¹ᵇ es: halo, alquilo C₁₋₄ (alquilo que está opcionalmente sustituido con uno o varios halo independientemente seleccionados), o alcoxi C₁₋₄ (alcoxi que está opcionalmente sustituido con uno o varios halo independientemente seleccionados); X es -S-, -O-, -N=CH-, -CH=N- o -CH=CH-; W es N o CR³, cuando W es N, R² es: H, -CN, halo, alquilo C₁₋₄ (alquilo que está opcionalmente sustituido con uno o varios OH o CN independientemente seleccionados), -C(=O)CH₃, -C(=O)CF₃, -C(=O)OCH₃, -C(=O)NH₂, o -NHC(=O)CH₃, o cuando W es CR³, uno de R² o R³ es: H, -CN, halo, alquilo C₁₋₄ (alquilo que esta opcionalmente sustituido con uno o varios OH o CN independientemente seleccionados), -C(=O)CH₃, C(=O)CF₃, -C(=O)OCH₃, -C(=O)NH₂, -NHC(=O)CH₃, y el otro es H o alquilo C₁₋₄; R⁴ es alquilo C₁₋₄; R⁵ es alquilo C₁₋₄ opcionalmente sustituido con uno o varios CN, OH, halo o -C(=O)NH₂ independientemente seleccionados; uno de R⁶ᵃ o R⁶ᵇ se selecciona de H, -CH₃ y halo, y el otro es H; Cy es: cicloalquilo C₄₋₁₀, heterocicloalquilo mono o bicíclico de 4 - 10 miembros que contiene uno o varios heteroátomos independientemente seleccionados de O, N y S, o heterocicloalquenilo de 4 - 7 miembros que contiene 1 enlace doble, que contiene uno o varios heteroátomos independientemente seleccionados de O, N y S; cada R⁷ se selecciona independientemente de: OH, oxo, halo, y alquilo C₁₋₄ (alquilo que está opcionalmente sustituido con uno o varios OH o alcoxi C₁₋₄ independientemente seleccionados); el índice a es 0, 1 ó 2; R⁸ es -(L¹-W¹)ₘ-L²-G¹, donde L¹ este ausente o bien es -O-, -C(=O)-, -NRⁱ, -NRʰC(=O)- o -SO₂-; W¹ es alquileno C₁₋₄; el índice m es 0 ó 1; L² está ausente o bien es -O-, -C(=O)-, -C(=O)O-, -OC(=O)-, -C(=O)-C(=O)-, -C(=O)-C(=O)NRᵃ-, -NRᵇ-, -C(=O)NRᶜ-, -NRᵈC(=O)-, -NRʲC(=O)O-, -SO₂-, -SO₂NRᵉ- o -NRᶠSO₂-; G¹ es: H, -CN, alquilo C₁₋₄ (alquilo que está opcionalmente sustituido con uno o varios -CN, OH, halo o fenilo independientemente seleccionados), cicloalquilo C₃₋₇ (cicloalquilo que está opcionalmente sustituido con -NH₂), heterocicloalquenilo de 5 - 6 miembros que contiene 1 enlace doble que contiene uno o varios heteroátomos independientemente seleccionados de O, N y S (heterocicloalquenilo que está opcionalmente sustituido con uno o varios grupos R⁹ independientemente seleccionados), heterocicloalquilo mono, bi o espirocíclico de 4 - 10 miembros que contiene uno o varios heteroátomos independientemente seleccionados de O, N y S (heterocicloalquilo que está opcionalmente sustituido con uno o varios grupos R⁹ independientemente seleccionados), o heteroarilo de 5 - 6 miembros que contiene uno o varios heteroátomos independientemente seleccionados de O, N y S (heteroarilo que está opcionalmente sustituido con uno o varios grupos R¹⁰ independientemente seleccionados); cada R⁹ es oxo o R¹⁰; cada R¹⁰ es: -OH, halo, -CN, alquilo C₁₋₄ (alquilo que está opcionalmente sustituido con uno o varios OH, halo o fenilo independientemente seleccionados), alcoxi C₁₋₄, cicloalquilo C₃₋₇, fenilo, -SO₂CH₃, -C(=O)alcoxi C₁₋₄, -C(=O)alquilo C₁₋₄, o -NRᵍC(=O)alquilo C₁₋₄; y cada Rᵃ, Rᵇ, Rᶜ, Rᵈ, Rᵉ, Rᶠ, Rᵍ, Rʰ, Rⁱ y Rʲ se selecciona independientemente de H y alquilo C₁₋₄; o una sal farmacéuticamente aceptable o un solvato o una sal farmacéuticamente aceptable de un solvato de este; o un metabolito biológicamente activo de este.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US201361781174P | 2013-03-14 | 2013-03-14 |
Publications (1)
Publication Number | Publication Date |
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AR095280A1 true AR095280A1 (es) | 2015-09-30 |
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ID=50236198
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ARP140100893A AR095280A1 (es) | 2013-03-14 | 2014-03-12 | Derivados heterocíclicos de imidazo[1,2-a]piridina |
Country Status (30)
Country | Link |
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US (7) | US8993590B2 (es) |
EP (3) | EP2970255B9 (es) |
JP (2) | JP6339595B2 (es) |
KR (2) | KR20210034098A (es) |
CN (1) | CN105143221B (es) |
AR (1) | AR095280A1 (es) |
AU (3) | AU2014231009B2 (es) |
BR (1) | BR112015020998B1 (es) |
CA (1) | CA2902103C (es) |
CY (2) | CY1119352T1 (es) |
DK (2) | DK3269716T3 (es) |
ES (2) | ES2638980T3 (es) |
HK (2) | HK1219730A1 (es) |
HR (2) | HRP20171219T1 (es) |
HU (2) | HUE051195T2 (es) |
IL (2) | IL240531B (es) |
LT (2) | LT3269716T (es) |
MX (1) | MX358342B (es) |
MY (1) | MY170260A (es) |
NZ (1) | NZ711202A (es) |
PH (1) | PH12015502055A1 (es) |
PL (2) | PL3269716T3 (es) |
PT (2) | PT2970255T (es) |
RU (1) | RU2675818C2 (es) |
SG (1) | SG11201507224RA (es) |
SI (2) | SI3269716T1 (es) |
TW (2) | TWI749290B (es) |
UY (1) | UY35437A (es) |
WO (1) | WO2014139882A1 (es) |
ZA (1) | ZA201505909B (es) |
Families Citing this family (72)
Publication number | Priority date | Publication date | Assignee | Title |
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CN103929963A (zh) | 2011-09-14 | 2014-07-16 | 萨穆梅德有限公司 | 吲唑-3-羧酰胺及其作为WNT/β-CATENIN信号传导通路抑制剂的用途 |
PH12017500997A1 (en) | 2012-04-04 | 2018-02-19 | Samumed Llc | Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof |
JP6339595B2 (ja) | 2013-03-14 | 2018-06-06 | ガラパゴス・ナムローゼ・フェンノートシャップGalapagos N.V. | 炎症性障害の治療のための化合物及びその医薬組成物 |
WO2014202458A1 (en) | 2013-06-19 | 2014-12-24 | Galapagos Nv | Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders |
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