JP2013529210A - Sstr5アンタゴニストとしてのスピロイソオキサゾリン化合物 - Google Patents
Sstr5アンタゴニストとしてのスピロイソオキサゾリン化合物 Download PDFInfo
- Publication number
- JP2013529210A JP2013529210A JP2013511232A JP2013511232A JP2013529210A JP 2013529210 A JP2013529210 A JP 2013529210A JP 2013511232 A JP2013511232 A JP 2013511232A JP 2013511232 A JP2013511232 A JP 2013511232A JP 2013529210 A JP2013529210 A JP 2013529210A
- Authority
- JP
- Japan
- Prior art keywords
- halogen
- substituted
- mmol
- alkyl
- methyl
- 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.)
- Withdrawn
Links
- 0 CC(C=C*CC(C)=C)NC Chemical compound CC(C=C*CC(C)=C)NC 0.000 description 10
- TTWKJIPWEKNXMQ-FRKPEAEDSA-N CC(C)(C)N/N=C(\C)/c(ccc(F)c1F)c1F Chemical compound CC(C)(C)N/N=C(\C)/c(ccc(F)c1F)c1F TTWKJIPWEKNXMQ-FRKPEAEDSA-N 0.000 description 1
- SCWSQIVPMOKPNA-UHFFFAOYSA-N CC(C)(C)c1cc(CN(CCC2C3)CCC2ON=C3c(cc2)ccc2C(O)=[U])ccc1-c(cn1)ccc1F Chemical compound CC(C)(C)c1cc(CN(CCC2C3)CCC2ON=C3c(cc2)ccc2C(O)=[U])ccc1-c(cn1)ccc1F SCWSQIVPMOKPNA-UHFFFAOYSA-N 0.000 description 1
- MRUZCKAZDXUCAQ-UHFFFAOYSA-N CC(C)[n](cc(C=O)c1c2)c1c(C)cc2Cl Chemical compound CC(C)[n](cc(C=O)c1c2)c1c(C)cc2Cl MRUZCKAZDXUCAQ-UHFFFAOYSA-N 0.000 description 1
- XQXALTVKZWLQRE-UHFFFAOYSA-N CC(CCSc(c(Cl)c1)ccc1Br)=C Chemical compound CC(CCSc(c(Cl)c1)ccc1Br)=C XQXALTVKZWLQRE-UHFFFAOYSA-N 0.000 description 1
- UWWYATUQDWTDGU-UHFFFAOYSA-N CC1(CN(CC2)CCC2(C2)ON=C2c(cc2)ccc2C(O)=O)C=C(C(F)(F)F)C=CC1C1=CNCC=C1 Chemical compound CC1(CN(CC2)CCC2(C2)ON=C2c(cc2)ccc2C(O)=O)C=C(C(F)(F)F)C=CC1C1=CNCC=C1 UWWYATUQDWTDGU-UHFFFAOYSA-N 0.000 description 1
- TVVJUZLIHJFTQP-UHFFFAOYSA-N CCOC(C(C)C1C)=CC(C=O)=C1c(ccc(F)c1F)c1F Chemical compound CCOC(C(C)C1C)=CC(C=O)=C1c(ccc(F)c1F)c1F TVVJUZLIHJFTQP-UHFFFAOYSA-N 0.000 description 1
- FXAMBHANNFAZDZ-UHFFFAOYSA-N OCc(cc1Cl)cc(Cl)c1I Chemical compound OCc(cc1Cl)cc(Cl)c1I FXAMBHANNFAZDZ-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- 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
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34568310P | 2010-05-18 | 2010-05-18 | |
| US61/345,683 | 2010-05-18 | ||
| PCT/US2011/036367 WO2011146324A1 (en) | 2010-05-18 | 2011-05-13 | Spiro isoxazoline compounds as sstr5 antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013529210A true JP2013529210A (ja) | 2013-07-18 |
| JP2013529210A5 JP2013529210A5 (cg-RX-API-DMAC7.html) | 2014-06-26 |
Family
ID=44991994
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013511232A Withdrawn JP2013529210A (ja) | 2010-05-18 | 2011-05-13 | Sstr5アンタゴニストとしてのスピロイソオキサゾリン化合物 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20130040978A1 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2571356A4 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2013529210A (cg-RX-API-DMAC7.html) |
| AR (1) | AR081401A1 (cg-RX-API-DMAC7.html) |
| AU (1) | AU2011256444B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2799414A1 (cg-RX-API-DMAC7.html) |
| TW (1) | TW201200524A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2011146324A1 (cg-RX-API-DMAC7.html) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015146561A1 (ja) * | 2014-03-26 | 2015-10-01 | 住友精化株式会社 | 臭化芳香族エステル化合物の製造方法 |
| JP2022501342A (ja) * | 2018-09-18 | 2022-01-06 | クリネティックス ファーマシューティカルズ,インク. | ソマトスタチンモジュレーターとその使用 |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8742110B2 (en) | 2010-08-18 | 2014-06-03 | Merck Sharp & Dohme Corp. | Spiroxazolidinone compounds |
| US20150166528A1 (en) | 2012-06-14 | 2015-06-18 | Basf Se | Pesticidal methods using substituted 3-pyridyl thiazole compounds and derivatives for combating animal pests |
| FR3000064A1 (fr) | 2012-12-21 | 2014-06-27 | Univ Lille Ii Droit & Sante | Composes de type spiroisoxazoline ayant une activite potentialisatrice de l'activite d'un antibiotique-composition et produit pharmaceutiques comprenant de tels composes |
| JP6247697B2 (ja) * | 2013-03-14 | 2017-12-13 | 武田薬品工業株式会社 | スピロアゼチジンイソキサゾール誘導体及びそのsstr5アンタゴニストとしての使用 |
| EP3083642B1 (en) * | 2013-12-17 | 2018-09-05 | Merck Sharp & Dohme Corp. | Fused bicyclic isoxazolines as inhibitors of cholesterol ester transfer protein |
| CN104945416B (zh) * | 2014-03-24 | 2017-11-17 | 中国科学院上海药物研究所 | 一类螺异噁唑啉衍生物、其制备方法及医药用途 |
| EP3174537B1 (en) * | 2014-07-29 | 2021-06-23 | Merck Sharp & Dohme Corp. | Monocyclic isoxazolines as inhibitors of cholesterol ester transfer protein |
| TW201712012A (zh) | 2015-06-16 | 2017-04-01 | 美國禮來大藥廠 | 2-側氧基-1,3,8-三氮雜螺[4.5]癸-3-基羧酸衍生物 |
| CN110088089B (zh) | 2016-10-25 | 2023-08-29 | 勃林格殷格翰国际有限公司 | 苄基氨基吡啶基环丙烷甲酸、药物组合物及其用途 |
| US10793530B2 (en) | 2017-01-26 | 2020-10-06 | Boehringer Ingelheim International Gmbh | Benzylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof |
| JP7023969B2 (ja) | 2017-01-26 | 2022-02-22 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ベンジルアミノピリジルシクロプロパンカルボン酸、その医薬組成物及び使用 |
| EP3596062A4 (en) | 2017-03-16 | 2020-08-26 | Crinetics Pharmaceuticals, Inc. | SOMATOSTATIN MODULATORS AND THEIR USES |
| EP3752498B1 (en) | 2018-02-12 | 2023-06-28 | Crinetics Pharmaceuticals, Inc. | Somatostatin modulators and uses thereof |
| TWI841768B (zh) | 2019-08-14 | 2024-05-11 | 美商克林提克斯醫藥股份有限公司 | 非肽生長抑制素(somatostatin)5型受體激動劑及其用途 |
| IL291985A (en) | 2019-10-07 | 2022-06-01 | Kallyope Inc | Gpr119 agonists |
| EP4073075A4 (en) * | 2019-12-03 | 2023-12-27 | Kallyope, Inc. | Sstr5 antagonists |
| PH12022552277A1 (en) | 2020-02-28 | 2024-03-04 | Kallyope Inc | Gpr40 agonists |
| UY39222A (es) | 2020-05-19 | 2021-11-30 | Kallyope Inc | Activadores de la ampk |
| EP4172162A4 (en) | 2020-06-26 | 2024-08-07 | Kallyope, Inc. | AMPK ACTIVATORS |
| WO2022177974A1 (en) | 2021-02-17 | 2022-08-25 | Crinetics Pharmaceuticals, Inc. | Crystalline forms of a somatostatin modulator |
| CN115215787A (zh) * | 2021-04-19 | 2022-10-21 | 中国科学院上海药物研究所 | 生长抑素受体5拮抗剂及其用途 |
| CN116354961B (zh) * | 2021-12-27 | 2025-07-25 | 中国科学院上海药物研究所 | 生长抑素受体5拮抗剂及其药物组合物及用途 |
| CN114230552B (zh) * | 2021-12-29 | 2023-11-03 | 江苏广域化学有限公司 | 三氟甲氧基二苯并噻吩、其制备方法及相关中间体的制备方法 |
| WO2024129614A1 (en) | 2022-12-13 | 2024-06-20 | Crinetics Pharmaceuticals, Inc. | Somatostatin subtype-2 receptor (sst2r) targeted therapeutics and uses thereof |
| CN115819186B (zh) * | 2023-02-14 | 2023-05-16 | 广东银珠医药科技有限公司 | 一种3,5-二氯苯甲醇的新型制备方法 |
| CN120752056A (zh) | 2023-03-27 | 2025-10-03 | 思可海雅药品株式会社 | 生长激素分泌促进剂 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5939418A (en) * | 1995-12-21 | 1999-08-17 | The Dupont Merck Pharmaceutical Company | Isoxazoline, isothiazoline and pyrazoline factor Xa inhibitors |
| AU6780398A (en) * | 1997-03-28 | 1998-10-22 | Du Pont Merck Pharmaceutical Company, The | Heterocyclic integrin inhibitor prodrugs |
| DE102005044813A1 (de) * | 2005-05-19 | 2007-10-04 | Grünenthal GmbH | Substituierte Spiro-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln |
| AR055395A1 (es) * | 2005-08-26 | 2007-08-22 | Vertex Pharma | Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c |
| BRPI0615449A2 (pt) * | 2005-09-02 | 2011-05-17 | Hoffmann La Roche | compostos, processo para a sua manufatura, composições farmacêuticas que os compreendem, método de tratamento e/ou prevenção de enfermidades que estão associadas com a modulação de receptores de sst do subtipo 5 e uso desses compostos |
| BRPI0617673C1 (pt) * | 2005-10-19 | 2012-05-22 | Ranbaxy Lab Ltd | composições de inibidores de fosfodiesterase do tipo iv |
-
2011
- 2011-05-13 JP JP2013511232A patent/JP2013529210A/ja not_active Withdrawn
- 2011-05-13 WO PCT/US2011/036367 patent/WO2011146324A1/en not_active Ceased
- 2011-05-13 AU AU2011256444A patent/AU2011256444B2/en not_active Expired - Fee Related
- 2011-05-13 CA CA2799414A patent/CA2799414A1/en not_active Abandoned
- 2011-05-13 US US13/641,767 patent/US20130040978A1/en not_active Abandoned
- 2011-05-13 EP EP11783995.1A patent/EP2571356A4/en not_active Withdrawn
- 2011-05-16 TW TW100117097A patent/TW201200524A/zh unknown
- 2011-05-17 AR ARP110101689A patent/AR081401A1/es not_active Application Discontinuation
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015146561A1 (ja) * | 2014-03-26 | 2015-10-01 | 住友精化株式会社 | 臭化芳香族エステル化合物の製造方法 |
| JPWO2015146561A1 (ja) * | 2014-03-26 | 2017-04-13 | 住友精化株式会社 | 臭化芳香族エステル化合物の製造方法 |
| JP2022501342A (ja) * | 2018-09-18 | 2022-01-06 | クリネティックス ファーマシューティカルズ,インク. | ソマトスタチンモジュレーターとその使用 |
| JP7431813B2 (ja) | 2018-09-18 | 2024-02-15 | クリネティックス ファーマシューティカルズ,インク. | ソマトスタチンモジュレーターとその使用 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP2571356A1 (en) | 2013-03-27 |
| US20130040978A1 (en) | 2013-02-14 |
| CA2799414A1 (en) | 2011-11-24 |
| AR081401A1 (es) | 2012-08-29 |
| TW201200524A (en) | 2012-01-01 |
| WO2011146324A1 (en) | 2011-11-24 |
| AU2011256444A1 (en) | 2012-10-18 |
| EP2571356A4 (en) | 2013-11-20 |
| AU2011256444B2 (en) | 2014-07-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20140502 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20140502 |
|
| A761 | Written withdrawal of application |
Free format text: JAPANESE INTERMEDIATE CODE: A761 Effective date: 20140801 |