JP5735634B2 - スフィンゴシン−1−リン酸受容体1アゴニストとしての4−(5−イソオキサゾリルまたは5−ピラゾリル−1,2,4−オキサジアゾール−3−イル)−マンデル酸アミド化合物 - Google Patents
スフィンゴシン−1−リン酸受容体1アゴニストとしての4−(5−イソオキサゾリルまたは5−ピラゾリル−1,2,4−オキサジアゾール−3−イル)−マンデル酸アミド化合物 Download PDFInfo
- Publication number
- JP5735634B2 JP5735634B2 JP2013506294A JP2013506294A JP5735634B2 JP 5735634 B2 JP5735634 B2 JP 5735634B2 JP 2013506294 A JP2013506294 A JP 2013506294A JP 2013506294 A JP2013506294 A JP 2013506294A JP 5735634 B2 JP5735634 B2 JP 5735634B2
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- Japan
- Prior art keywords
- phenyl
- hydroxy
- trifluoromethyl
- acetamide
- oxadiazol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
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- 0 CC(*)(C1)C*1NC Chemical compound CC(*)(C1)C*1NC 0.000 description 2
- AWRSDLWBHOVPLM-UHFFFAOYSA-N CC(C1)(CN1C(CCNC(C(c(cc1)ccc1-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1)O)=O)=O)O Chemical compound CC(C1)(CN1C(CCNC(C(c(cc1)ccc1-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1)O)=O)=O)O AWRSDLWBHOVPLM-UHFFFAOYSA-N 0.000 description 1
- WVRKHFSDURCGFL-GKOGFXNCSA-N C[C@H](C#N)NC(C(c(cc1)ccc1-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1)O)=O Chemical compound C[C@H](C#N)NC(C(c(cc1)ccc1-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1)O)=O WVRKHFSDURCGFL-GKOGFXNCSA-N 0.000 description 1
- LDGOTHYJHKJQQI-UHFFFAOYSA-N N#CC1(CC1)NC(C(c(cc1)ccc1-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1)O)=O Chemical compound N#CC1(CC1)NC(C(c(cc1)ccc1-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1)O)=O LDGOTHYJHKJQQI-UHFFFAOYSA-N 0.000 description 1
- YXCQSMKIRXQDHI-UHFFFAOYSA-N NC(C(C#N)NC(C(c(cc1)ccc1-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1)O)=O)=O Chemical compound NC(C(C#N)NC(C(c(cc1)ccc1-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1)O)=O)=O YXCQSMKIRXQDHI-UHFFFAOYSA-N 0.000 description 1
- GYHKODORJRRYBU-CLFYSBASSA-N O/N=C(/c1ccccc1)\Cl Chemical compound O/N=C(/c1ccccc1)\Cl GYHKODORJRRYBU-CLFYSBASSA-N 0.000 description 1
- HXJUTPCZVOIRIF-UHFFFAOYSA-N O=S1(CCCC1)=O Chemical compound O=S1(CCCC1)=O HXJUTPCZVOIRIF-UHFFFAOYSA-N 0.000 description 1
- ICDIVHMFUVHALM-UHFFFAOYSA-N OC(C(NCCc1c[nH]cn1)=O)c(cc1)ccc1-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1 Chemical compound OC(C(NCCc1c[nH]cn1)=O)c(cc1)ccc1-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1 ICDIVHMFUVHALM-UHFFFAOYSA-N 0.000 description 1
- ORYAMGWVNJOICC-UHFFFAOYSA-N OC(C(NCCc1c[s]cn1)=O)c(cc1)ccc1-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1 Chemical compound OC(C(NCCc1c[s]cn1)=O)c(cc1)ccc1-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1 ORYAMGWVNJOICC-UHFFFAOYSA-N 0.000 description 1
- RBCGLLBOGZKJQQ-UHFFFAOYSA-N OC(C(NCc1c[s]cc1)=O)c(cc1)ccc1-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1 Chemical compound OC(C(NCc1c[s]cc1)=O)c(cc1)ccc1-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1 RBCGLLBOGZKJQQ-UHFFFAOYSA-N 0.000 description 1
- WATWRRWJXMTBSG-UHFFFAOYSA-N OC(c1n[o]c(-c2ccccc2)c1C(F)(F)F)=O Chemical compound OC(c1n[o]c(-c2ccccc2)c1C(F)(F)F)=O WATWRRWJXMTBSG-UHFFFAOYSA-N 0.000 description 1
- QXCJZOWWTZPCDU-UHFFFAOYSA-N OCCCNC(C(c(cc1)ccc1-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1)O)=O Chemical compound OCCCNC(C(c(cc1)ccc1-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1)O)=O QXCJZOWWTZPCDU-UHFFFAOYSA-N 0.000 description 1
Classifications
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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
-
- 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
- A61K31/4245—Oxadiazoles
-
- 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
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- 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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
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- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
-
- A—HUMAN NECESSITIES
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- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
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- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
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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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- 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]
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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
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- A61P37/02—Immunomodulators
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Endocrinology (AREA)
- Surgery (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32731510P | 2010-04-23 | 2010-04-23 | |
| US61/327,315 | 2010-04-23 | ||
| PCT/US2011/033364 WO2011133734A1 (en) | 2010-04-23 | 2011-04-21 | 4 - (5 - isoxazolyl or 5 - pyrrazolyl -1,2,4- oxadiazol - 3 - yl) -mandelic acid amides as sphingosin- 1 - phosphate 1 rreceptor agonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013525369A JP2013525369A (ja) | 2013-06-20 |
| JP2013525369A5 JP2013525369A5 (enExample) | 2014-05-22 |
| JP5735634B2 true JP5735634B2 (ja) | 2015-06-17 |
Family
ID=44069927
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013506294A Expired - Fee Related JP5735634B2 (ja) | 2010-04-23 | 2011-04-21 | スフィンゴシン−1−リン酸受容体1アゴニストとしての4−(5−イソオキサゾリルまたは5−ピラゾリル−1,2,4−オキサジアゾール−3−イル)−マンデル酸アミド化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8835470B2 (enExample) |
| EP (1) | EP2560969B1 (enExample) |
| JP (1) | JP5735634B2 (enExample) |
| CN (1) | CN103119038B (enExample) |
| ES (1) | ES2548683T3 (enExample) |
| WO (1) | WO2011133734A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2539256T3 (es) | 2010-07-20 | 2015-06-29 | Bristol-Myers Squibb Company | Compuestos de 3-fenil-1,2,4-oxadiazol sustituidos |
| JP5869579B2 (ja) | 2010-09-24 | 2016-02-24 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 置換オキサジアゾール化合物およびそれらのs1p1アゴニストとしての使用 |
| WO2012061459A1 (en) | 2010-11-03 | 2012-05-10 | Bristol-Myers Squibb Company | Heterocyclic compounds as s1p1 agonists for the treatment of autoimmune and vascular diseases |
| TWI613182B (zh) | 2013-02-21 | 2018-02-01 | 必治妥美雅史谷比公司 | 雙環化合物 |
| BR112015026847A2 (pt) | 2013-04-22 | 2017-07-25 | Abbvie Inc | tiazóis e usos dos mesmos |
| EP2878339A1 (en) * | 2013-12-02 | 2015-06-03 | Siena Biotech S.p.A. | SIP3 antagonists |
| TWI689487B (zh) | 2014-08-20 | 2020-04-01 | 美商必治妥美雅史谷比公司 | 經取代雙環化合物 |
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| US4200750A (en) | 1977-01-07 | 1980-04-29 | Westwood Pharmaceuticals Inc. | 4-Substituted imidazo [1,2-a]quinoxalines |
| DE4102024A1 (de) | 1991-01-24 | 1992-07-30 | Thomae Gmbh Dr K | Biphenylderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung |
| US6069143A (en) | 1994-12-20 | 2000-05-30 | Smithkline Beecham Corporation | Fibrinogen receptor antagonists |
| WO2003061567A2 (en) | 2002-01-18 | 2003-07-31 | Merck & Co., Inc. | Selective s1p1/edg1 receptor agonists |
| DE60330047D1 (en) | 2002-01-18 | 2009-12-24 | Merck & Co Inc | "n-(benzyl)aminoalkyl carboxylate, phosphinate, phosphonate und tetrazole als edg rezeptoragonisten" |
| AU2003207567B2 (en) | 2002-01-18 | 2008-01-24 | Merck Sharp & Dohme Corp. | Edg receptor agonists |
| EP1482895A4 (en) | 2002-03-01 | 2005-04-27 | Merck & Co Inc | AMINO ALKYL PHOSPHONATES AND RELATED COMPOUNDS AS EDG RECEPTOR AGONISTS |
| CA2483164C (en) | 2002-04-23 | 2011-06-07 | Bristol-Myers Squibb Company | Pyrrolo-triazine aniline compounds useful as kinase inhibitors |
| AU2003276043A1 (en) | 2002-06-17 | 2003-12-31 | Merck & Co., Inc. | 1-((5-aryl-1,2,4-oxadiazol-3-yl)benzyl)azetidine-3-carboxylates and 1-((5-aryl-1,2,4-oxadiazol-3-yl)benzyl)pyrrolidine-3-carboxylates as edg receptor agonists |
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| EP1594508B1 (en) | 2003-02-11 | 2012-08-08 | Irm Llc | Novel bicyclic compounds and compositions |
| EP1625123A4 (en) | 2003-05-15 | 2007-08-29 | Merck & Co Inc | 3- (2-AMINO-1-AZACYCLYL) -5-ARYL-1,2,4-OXADIAZOLE AS S1P RECEPTOR AGONISTS |
| AU2004240649A1 (en) | 2003-05-19 | 2004-12-02 | Irm, Llc | Immunosuppressant compounds and compositions |
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-
2011
- 2011-04-21 WO PCT/US2011/033364 patent/WO2011133734A1/en not_active Ceased
- 2011-04-21 ES ES11717430.0T patent/ES2548683T3/es active Active
- 2011-04-21 EP EP11717430.0A patent/EP2560969B1/en not_active Not-in-force
- 2011-04-21 CN CN201180031281.1A patent/CN103119038B/zh not_active Expired - Fee Related
- 2011-04-21 JP JP2013506294A patent/JP5735634B2/ja not_active Expired - Fee Related
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Also Published As
| Publication number | Publication date |
|---|---|
| EP2560969B1 (en) | 2015-08-12 |
| JP2013525369A (ja) | 2013-06-20 |
| EP2560969A1 (en) | 2013-02-27 |
| CN103119038B (zh) | 2016-05-04 |
| US8835470B2 (en) | 2014-09-16 |
| CN103119038A (zh) | 2013-05-22 |
| ES2548683T3 (es) | 2015-10-20 |
| WO2011133734A1 (en) | 2011-10-27 |
| US20130045964A1 (en) | 2013-02-21 |
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