ECSP12011695A - Derivados de (tio) morfolina como moduladores de s1p - Google Patents
Derivados de (tio) morfolina como moduladores de s1pInfo
- Publication number
- ECSP12011695A ECSP12011695A ECSP12011695A ECSP12011695A EC SP12011695 A ECSP12011695 A EC SP12011695A EC SP12011695 A ECSP12011695 A EC SP12011695A EC SP12011695 A ECSP12011695 A EC SP12011695A
- Authority
- EC
- Ecuador
- Prior art keywords
- alkyl
- optionally substituted
- atoms
- halogen
- fluoro
- Prior art date
Links
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 title 2
- 125000000217 alkyl group Chemical group 0.000 abstract 14
- 125000001153 fluoro group Chemical group F* 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 102000011011 Sphingosine 1-phosphate receptors Human genes 0.000 abstract 2
- 108050001083 Sphingosine 1-phosphate receptors Proteins 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000002911 monocyclic heterocycle group Chemical group 0.000 abstract 2
- -1 phenoxy, benzyl Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- DZCBKUAAGVVLOX-UHFFFAOYSA-N 1-morpholin-4-ylethanol Chemical compound CC(O)N1CCOCC1 DZCBKUAAGVVLOX-UHFFFAOYSA-N 0.000 abstract 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 abstract 1
- 125000004860 4-ethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])C([H])([H])[H] 0.000 abstract 1
- 229910018828 PO3H2 Inorganic materials 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 1
- 150000001602 bicycloalkyls Chemical group 0.000 abstract 1
- 235000010290 biphenyl Nutrition 0.000 abstract 1
- 239000004305 biphenyl Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000002993 cycloalkylene group Chemical group 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 125000005647 linker group Chemical group 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 1
- 125000004312 morpholin-2-yl group Chemical group [H]N1C([H])([H])C([H])([H])OC([H])(*)C1([H])[H] 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000004299 tetrazol-5-yl group Chemical group [H]N1N=NC(*)=N1 0.000 abstract 1
- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical class C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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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
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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
-
- 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
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
- C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
- C07D279/12—1,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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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
- C07D417/02—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 two hetero rings
- C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6527—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
- C07F9/6533—Six-membered rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurology (AREA)
- Animal Behavior & Ethology (AREA)
- Neurosurgery (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente invención se refiere a derivados de (tio)morfolina que tienen la fórmula (I) (I)en dondeR1 se selecciona de ciano, alquinilo (2-4C), alquilo (1-4C), cicloalquilo (3-6C), cicloalquenilo (4-6C),bicicloalquilo (6-8C),, grupo bicíclico (8-10C), cada uno sustituido en forma opcional con alquilo (1-4C),fenilo, bifenilo, naftilo, cada uno sustituido en forma opcional con uno o más sustituyentes se selecciona en forma independiente de halógeno, alquilo (C1-4C) sustituido en forma opcional con uno o más átomos de fluoro, alquinilo (2-4C), alcoxi (C1-4C) sustituido en forma opcional con uno o más átomos de fluoro, amino, dialquilamino (C1-4C) , SO2 alquilo (1-4C), CO alquilo (1-4C), CO O alquilo (1-4C), NH-CO alquilo (C1-4C) y cicloalquilo (3-6C), fenilo sustituido con fenoxi, bencilo, benciloxi, feniletilo o heterociclo monocíclico, cada uno sustituido en forma opcional con alquilo (1-4C), heterociclo monocíclico sustituido en forma opcional con halógeno, alquilo (C1-4C) o con fenilo sustituido en forma opcional con alquilo (1-4C), heterociclo bicíclico sustituido en forma opcional con alquilo (C1-4C);A se selecciona de -CO-O-, -O-CO-, -NH-CO-, -CO-NH, -C=C-, -CCH3-O- y el grupo de enlace -Y-(CH2)n-X- en donde Y está unido a R1 y se selecciona de un enlace, -O-, -S-, -SO-, -SO2-, -CH2-O-, CO-, -O-CO-, CO-O-, -CO-NH-, -NH-CO-, -C=C- y C?C- ; n es un número entero desde 1 hasta 10; y X está unido al grupo fenileno / piridilo y se selecciona de un enlace, -O-, S-, -SO-, -SO2-, -NH, -CO-, -C=C- y C?C-;la estructura del anillo B contiene en forma opcional un átomo de nitrógeno;R2 es H, alquilo (C1-4C) sustituido en forma opcional con uno o más átomos de fluoro, alcoxi (C1-4C) sustituido en forma opcional con uno o más átomos de fluoro, o halógeno; yR3 es alquileno (1-4C)-R5 en donde el grupo alquileno puede estar sustituido con (CH2)2 para formar un resto ciclopropilo o uno o dos átomos de halógeno, o R3 es cicloalquileno (3-6C)-R5 o -CO-CH2-R5, en donde R5 es -OH, -PO3H2, OPO3H2, COOH, -COOalquilo (C1-4C) o tetrazol-5-ilo;R4 es H o alquilo (C1-4C);R6 es uno o más sustituyentes se selecciona en forma independiente de H, alquilo (C1-4C) o oxo;W es -O-, -S-, -SO- o -SO2-;o una sal, un solvato o un hidrato aceptables desde el punto de vista farmacéutico de los anteriores; con la salvedad de que el derivado que tiene la fórmula (I) no sea 2 (4 etilfenil) 4 morfolinoetanol o 4 [4 (2 hidroxietil) 2 morfolinil]bencenacetonitriloo una sal, un solvato o un hidrato aceptables desde el punto de vista farmacéutico de los anteriores.Los compuestos de la invención tienen afinidad por los receptores de S1P y pueden usarse en el tratamiento, alivio o prevención de enfermedades y dolencias mediadas por el receptor S1P.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23851809P | 2009-08-31 | 2009-08-31 | |
| EP09169075 | 2009-08-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP12011695A true ECSP12011695A (es) | 2012-03-30 |
Family
ID=41361253
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP12011695 ECSP12011695A (es) | 2009-08-31 | 2012-02-27 | Derivados de (tio) morfolina como moduladores de s1p |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US9045441B2 (es) |
| EP (1) | EP2473490B1 (es) |
| JP (1) | JP5933436B2 (es) |
| KR (1) | KR101767882B1 (es) |
| CN (1) | CN102548976B (es) |
| AR (1) | AR077969A1 (es) |
| AU (1) | AU2010288477B8 (es) |
| CA (1) | CA2772169C (es) |
| CR (1) | CR20120153A (es) |
| DO (1) | DOP2012000053A (es) |
| EC (1) | ECSP12011695A (es) |
| ES (1) | ES2452550T3 (es) |
| HK (1) | HK1172620A1 (es) |
| IL (1) | IL218208A (es) |
| MX (1) | MX2012002534A (es) |
| NZ (1) | NZ598300A (es) |
| PE (1) | PE20121280A1 (es) |
| PL (1) | PL2473490T3 (es) |
| RU (1) | RU2557233C2 (es) |
| SG (1) | SG178902A1 (es) |
| TW (1) | TW201113263A (es) |
| UA (1) | UA106994C2 (es) |
| UY (1) | UY32858A (es) |
| WO (1) | WO2011023795A1 (es) |
| ZA (1) | ZA201201446B (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR077969A1 (es) | 2009-08-31 | 2011-10-05 | Abbott Healthcare Products Bv | Derivados de (tio)morfolina comomoduladores de s1p |
| TWI522361B (zh) | 2010-07-09 | 2016-02-21 | 艾伯維公司 | 作為s1p調節劑的稠合雜環衍生物 |
| TW201206893A (en) * | 2010-07-09 | 2012-02-16 | Abbott Healthcare Products Bv | Bisaryl (thio) morpholine derivatives as S1P modulators |
| TWI543984B (zh) | 2010-07-09 | 2016-08-01 | 艾伯維公司 | 作為s1p調節劑的螺-哌啶衍生物 |
| US8802673B2 (en) * | 2011-03-24 | 2014-08-12 | Hoffmann-La Roche Inc | Heterocyclic amine derivatives |
| US9029370B2 (en) * | 2011-06-10 | 2015-05-12 | Hoffmann-La Roche Inc. | Substituted benzamide derivatives |
| MX2015005721A (es) * | 2012-11-07 | 2015-09-08 | Hoffmann La Roche | Derivados de pirazina. |
| US9850206B2 (en) | 2012-11-20 | 2017-12-26 | Biogen Ma Inc. | S1P and/or ATX modulating agents |
| CN105949142B (zh) * | 2016-05-21 | 2018-03-27 | 南华大学 | 具有抗抑郁活性的单一手性化合物及其制备方法和应用 |
| CN114728982A (zh) | 2019-10-31 | 2022-07-08 | 逃逸生物有限公司 | 固体形式的s1p-受体调节剂 |
| AR127592A1 (es) * | 2021-11-08 | 2024-02-07 | Hoffmann La Roche | Hidrogenación catalítica de nitrocompuestos aromáticos |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH072848A (ja) * | 1993-04-23 | 1995-01-06 | Sankyo Co Ltd | モルホリンおよびチオモルホリン誘導体 |
| JP4152002B2 (ja) * | 1996-08-27 | 2008-09-17 | 興和創薬株式会社 | ２−フェニルモルホリン−５−オン誘導体およびそれを含む医薬組成物 |
| US6380387B1 (en) | 1999-12-06 | 2002-04-30 | Hoffmann-La Roche Inc. | 4-Pyrimidinyl-n-acyl-l phenylalanines |
| CA2406685C (en) | 2000-04-21 | 2006-10-31 | Shionogi & Co., Ltd. | Oxadiazole derivatives having anticancer effects |
| AU2004247462B2 (en) * | 2003-06-12 | 2010-09-02 | Btg International Limited | Cyclic hydroxylamine as psychoactive compounds |
| JP4947406B2 (ja) * | 2003-08-29 | 2012-06-06 | 小野薬品工業株式会社 | Ｓ１ｐ受容体結合能を有する化合物およびその医薬用途 |
| RU2390519C2 (ru) * | 2003-08-29 | 2010-05-27 | Оно Фармасьютикал Ко., Лтд. | Соединение, способное к связыванию с рецептором s1p, и его фармацевтическое применение |
| US7550485B2 (en) * | 2003-10-14 | 2009-06-23 | Wyeth | Substituted N-heterocycle derivatives and methods of their use |
| GB0329498D0 (en) * | 2003-12-19 | 2004-01-28 | Novartis Ag | Organic compounds |
| TW200538433A (en) * | 2004-02-24 | 2005-12-01 | Irm Llc | Immunosuppressant compounds and compositiions |
| GB0409744D0 (en) | 2004-04-30 | 2004-06-09 | Pfizer Ltd | Novel compounds |
| BRPI0510453A (pt) * | 2004-04-30 | 2007-10-30 | Warner Lambert Co | composto substituìdos com morfolina para o tratamento de distúrbios do sistema nervoso central |
| WO2006047159A1 (en) * | 2004-10-22 | 2006-05-04 | Agrinomics Llc | Generation of plants with altered oil content |
| CN101043887A (zh) * | 2004-10-22 | 2007-09-26 | 默克公司 | 用作s1p受体激动剂的2－(芳基)氮杂环甲基羧酸酯、磺酸酯、膦酸酯、次膦酸酯和杂环化合物 |
| ES2338716T3 (es) | 2006-01-27 | 2010-05-11 | F.Hoffmann-La Roche Ag | Uso de derivados de 4-imidazol para trastornos del snc. |
| WO2007085557A2 (en) | 2006-01-27 | 2007-08-02 | F. Hoffmann-La Roche Ag | Use of substituted 2-imidazole of imidazoline derivatives |
| CA2644069A1 (en) * | 2006-02-28 | 2007-09-07 | Helicon Therapeutics, Inc. | Therapeutic piperazines as pde4 inhibitors |
| JP2010502675A (ja) * | 2006-09-08 | 2010-01-28 | ノバルティス アクチエンゲゼルシャフト | リンパ球相互作用が介在する疾患または障害を処置するために有用なｎ−ビアリール（ヘテロ）アリールスルホンアミド誘導体 |
| BRPI0720043A2 (pt) * | 2006-12-15 | 2014-01-07 | Abbott Lab | Composto oxadiazol |
| EA200901030A1 (ru) * | 2007-02-02 | 2010-02-26 | Новартис Аг | Антагонист хроменового рецептора s1p1 |
| AR077969A1 (es) | 2009-08-31 | 2011-10-05 | Abbott Healthcare Products Bv | Derivados de (tio)morfolina comomoduladores de s1p |
| CN101812058B (zh) * | 2010-04-13 | 2012-03-21 | 湖南大学 | 吲哚美辛2-芳基吗啉乙酯及其制备方法与应用 |
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