CN1642929B - 含有2-苯基苯并噻唑啉衍生物的κ-阿片样物质受体激动剂 - Google Patents
含有2-苯基苯并噻唑啉衍生物的κ-阿片样物质受体激动剂 Download PDFInfo
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- CN1642929B CN1642929B CN038072750A CN03807275A CN1642929B CN 1642929 B CN1642929 B CN 1642929B CN 038072750 A CN038072750 A CN 038072750A CN 03807275 A CN03807275 A CN 03807275A CN 1642929 B CN1642929 B CN 1642929B
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- Prior art keywords
- phenyl
- methoxy
- ethanoyl
- alkyl
- propoxy
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- 239000002632 kappa opiate receptor agonist Substances 0.000 title abstract description 24
- 229940126470 kappa opioid receptor agonist Drugs 0.000 title abstract description 24
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- 150000001875 compounds Chemical class 0.000 claims abstract description 368
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract description 33
- 125000002252 acyl group Chemical group 0.000 claims abstract description 25
- 150000003839 salts Chemical class 0.000 claims abstract description 24
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract description 15
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- 125000001424 substituent group Chemical group 0.000 claims abstract 4
- BZGWZLIKWOCPLN-UHFFFAOYSA-N 1,3-benzothiazole;quinoline Chemical compound C1=CC=C2SC=NC2=C1.N1=CC=CC2=CC=CC=C21 BZGWZLIKWOCPLN-UHFFFAOYSA-N 0.000 claims description 152
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- 239000000018 receptor agonist Substances 0.000 abstract 2
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- 230000000694 effects Effects 0.000 description 22
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- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 20
- 238000000605 extraction Methods 0.000 description 20
- 238000002386 leaching Methods 0.000 description 20
- 239000011780 sodium chloride Substances 0.000 description 19
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- CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 description 18
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- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 17
- 238000002425 crystallisation Methods 0.000 description 16
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Classifications
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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
-
- 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
- A61K31/428—Thiazoles condensed with carbocyclic rings
-
- 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
- A61P17/04—Antipruritics
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- 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
- A61P19/02—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
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric 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
- A61P25/04—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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
- C07D277/62—Benzothiazoles
- C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
- C07D277/66—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2 with aromatic rings or ring systems directly attached in position 2
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Dermatology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Biomedical Technology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2002097500 | 2002-03-29 | ||
| JP097500/2002 | 2002-03-29 | ||
| PCT/JP2003/003928 WO2003082840A1 (en) | 2002-03-29 | 2003-03-28 | κ-OPIOID RECEPTOR AGONIST COMPRISING 2-PHENYLBENZOTHIAZOLINE DERIVATIVE |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2006101392068A Division CN100522954C (zh) | 2002-03-29 | 2003-03-28 | 含有2-苯基苯并噻唑啉衍生物的к-阿片样物质受体激动剂 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1642929A CN1642929A (zh) | 2005-07-20 |
| CN1642929B true CN1642929B (zh) | 2010-05-12 |
Family
ID=28671920
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN038072750A Expired - Fee Related CN1642929B (zh) | 2002-03-29 | 2003-03-28 | 含有2-苯基苯并噻唑啉衍生物的κ-阿片样物质受体激动剂 |
| CNB2006101392068A Expired - Fee Related CN100522954C (zh) | 2002-03-29 | 2003-03-28 | 含有2-苯基苯并噻唑啉衍生物的к-阿片样物质受体激动剂 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2006101392068A Expired - Fee Related CN100522954C (zh) | 2002-03-29 | 2003-03-28 | 含有2-苯基苯并噻唑啉衍生物的к-阿片样物质受体激动剂 |
Country Status (10)
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI334349B (en) * | 2003-07-04 | 2010-12-11 | Santen Pharmaceutical Co Ltd | Pain threshold reduction depressant |
| US7642274B2 (en) | 2004-07-02 | 2010-01-05 | Santen Pharmaceutical Co., Ltd. | Inhibitor of pain threshold decrease |
| WO2006088246A1 (ja) * | 2005-02-18 | 2006-08-24 | Takeda Pharmaceutical Company Limited | Ｇｐｒ３４受容体機能調節剤 |
| WO2012012410A2 (en) | 2010-07-19 | 2012-01-26 | Dr. Reddy's Laboratories Ltd. | Kappa opioid receptor agonists |
| US9487510B2 (en) | 2012-03-05 | 2016-11-08 | Dr. Reddy's Laboratories Ltd. | Substituted heterocyclic acetamides as kappa opioid receptor (KOR) agonists |
| WO2014148574A1 (ja) | 2013-03-22 | 2014-09-25 | 参天製薬株式会社 | Ｉｌ－２産生抑制 |
| JP6531330B2 (ja) | 2013-12-18 | 2019-06-19 | 国立大学法人京都大学 | 疼痛に関する化合物及び医薬組成物 |
| JPWO2018230713A1 (ja) | 2017-06-16 | 2020-04-16 | 学校法人同志社 | カスパーゼ阻害活性を有する化合物、これらの化合物を含む、角膜内皮の症状、障害または疾患を治療または予防するための医薬およびその応用 |
| KR102619458B1 (ko) | 2017-06-16 | 2023-12-29 | 학교법인 도시샤 | mTOR 인히비터를 포함하는, 눈의 증상, 장해 또는 질환을 치료 또는 예방하기 위한 의약 및 그 응용 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4479949A (en) * | 1981-09-12 | 1984-10-30 | Santen Pharmaceutical Co., Ltd. | Benzothiazoline compounds |
| US4547513A (en) * | 1983-12-27 | 1985-10-15 | Santen Pharmaceutical Co., Ltd. | 2-Arylbenzothiazoline derivatives and their use in treating angina cordis |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US547513A (en) * | 1895-10-08 | Chell | ||
| JPS4994667A (US20060205796A1-20060914-C00073.png) * | 1973-01-23 | 1974-09-09 | ||
| JPS5967276A (ja) | 1982-09-01 | 1984-04-16 | Santen Pharmaceut Co Ltd | ベンゾチアゾリン誘導体 |
| JPS6183175A (ja) | 1984-09-06 | 1986-04-26 | Santen Pharmaceut Co Ltd | ベンゾチアゾリン誘導体およびそれを主成分とする循環器官用薬剤 |
| JPS62221679A (ja) | 1986-03-19 | 1987-09-29 | Santen Pharmaceut Co Ltd | ベンゾチアゾリン誘導体 |
| JPH066581B2 (ja) | 1986-03-19 | 1994-01-26 | 参天製薬株式会社 | フエノキシアルキルアミン側鎖を有するベンゾチアゾリン誘導体 |
| JPH08231399A (ja) | 1995-02-23 | 1996-09-10 | Shionogi & Co Ltd | モルヒネ禁断抑制作用剤 |
| ATE291429T1 (de) | 1996-11-25 | 2005-04-15 | Toray Industries | Mittel gegen juckreiz |
| JP2000344821A (ja) | 1999-06-01 | 2000-12-12 | Toagosei Co Ltd | オレフィン重合用触媒 |
-
2003
- 2003-03-28 WO PCT/JP2003/003928 patent/WO2003082840A1/ja active Application Filing
- 2003-03-28 EP EP09000611A patent/EP2042173A3/en not_active Withdrawn
- 2003-03-28 KR KR1020047015318A patent/KR101035931B1/ko not_active IP Right Cessation
- 2003-03-28 NZ NZ535987A patent/NZ535987A/en not_active IP Right Cessation
- 2003-03-28 AU AU2003220894A patent/AU2003220894B8/en not_active Ceased
- 2003-03-28 US US10/509,549 patent/US7112598B2/en not_active Expired - Fee Related
- 2003-03-28 CA CA2480560A patent/CA2480560C/en not_active Expired - Fee Related
- 2003-03-28 CN CN038072750A patent/CN1642929B/zh not_active Expired - Fee Related
- 2003-03-28 CN CNB2006101392068A patent/CN100522954C/zh not_active Expired - Fee Related
- 2003-03-28 ES ES03715569T patent/ES2390052T3/es not_active Expired - Lifetime
- 2003-03-28 EP EP03715569A patent/EP1496053B1/en not_active Expired - Lifetime
-
2006
- 2006-05-15 US US11/434,028 patent/US7410987B2/en not_active Expired - Fee Related
-
2009
- 2009-02-02 JP JP2009021413A patent/JP5061134B2/ja not_active Expired - Fee Related
- 2009-03-30 AU AU2009201233A patent/AU2009201233B2/en not_active Ceased
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4479949A (en) * | 1981-09-12 | 1984-10-30 | Santen Pharmaceutical Co., Ltd. | Benzothiazoline compounds |
| US4547513A (en) * | 1983-12-27 | 1985-10-15 | Santen Pharmaceutical Co., Ltd. | 2-Arylbenzothiazoline derivatives and their use in treating angina cordis |
Also Published As
| Publication number | Publication date |
|---|---|
| US20060205796A1 (en) | 2006-09-14 |
| EP1496053A1 (en) | 2005-01-12 |
| JP2009143940A (ja) | 2009-07-02 |
| KR20040095329A (ko) | 2004-11-12 |
| AU2003220894A1 (en) | 2003-10-13 |
| CN1642929A (zh) | 2005-07-20 |
| EP1496053A4 (en) | 2008-01-16 |
| AU2003220894B2 (en) | 2009-02-05 |
| EP2042173A2 (en) | 2009-04-01 |
| US20050113430A1 (en) | 2005-05-26 |
| JP5061134B2 (ja) | 2012-10-31 |
| EP2042173A3 (en) | 2010-02-24 |
| ES2390052T3 (es) | 2012-11-06 |
| AU2009201233A1 (en) | 2009-04-23 |
| CA2480560A1 (en) | 2003-10-09 |
| CA2480560C (en) | 2011-02-15 |
| KR101035931B1 (ko) | 2011-05-23 |
| WO2003082840A1 (en) | 2003-10-09 |
| AU2009201233B2 (en) | 2012-07-05 |
| CN100522954C (zh) | 2009-08-05 |
| US7410987B2 (en) | 2008-08-12 |
| US7112598B2 (en) | 2006-09-26 |
| AU2003220894B8 (en) | 2009-02-19 |
| CN1911918A (zh) | 2007-02-14 |
| EP1496053B1 (en) | 2012-06-20 |
| NZ535987A (en) | 2006-08-31 |
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| Date | Code | Title | Description |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C41 | Transfer of patent application or patent right or utility model | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20160329 Address after: Tokyo, Japan, Japan Patentee after: Step Pharmaceutical Company Limited Address before: Osaka Japan Patentee before: Santen Pharmaceutical Co., Ltd. |
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| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20100512 Termination date: 20180328 |