EA022323B1 - Арил- и гетероарилкарбонильные производные гексагидроинденопиридина и октагидробензохинолина - Google Patents

Арил- и гетероарилкарбонильные производные гексагидроинденопиридина и октагидробензохинолина Download PDF

Info

Publication number
EA022323B1
EA022323B1 EA201270562A EA201270562A EA022323B1 EA 022323 B1 EA022323 B1 EA 022323B1 EA 201270562 A EA201270562 A EA 201270562A EA 201270562 A EA201270562 A EA 201270562A EA 022323 B1 EA022323 B1 EA 022323B1
Authority
EA
Eurasian Patent Office
Prior art keywords
group
cis
compound
acid
quinoline
Prior art date
Application number
EA201270562A
Other languages
English (en)
Russian (ru)
Other versions
EA201270562A1 (ru
Inventor
Маттиас Экхардт
Штефан Петерс
Герберт Нар
Франк Химмелсбах
Линхан Чжуан
Original Assignee
Вайтаи Фармасьютиклз, Инк.
Берингер Ингельхайм Интернэшнл Гмбх
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41683136&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA022323(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Вайтаи Фармасьютиклз, Инк., Берингер Ингельхайм Интернэшнл Гмбх filed Critical Вайтаи Фармасьютиклз, Инк.
Publication of EA201270562A1 publication Critical patent/EA201270562A1/ru
Publication of EA022323B1 publication Critical patent/EA022323B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • C07D221/10—Aza-phenanthrenes
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • 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
    • 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
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • C07D221/16—Ring systems of three rings containing carbocyclic rings other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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
    • C07D417/02—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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D498/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
EA201270562A 2009-11-06 2010-11-05 Арил- и гетероарилкарбонильные производные гексагидроинденопиридина и октагидробензохинолина EA022323B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09175233 2009-11-06
PCT/US2010/055586 WO2011057054A1 (en) 2009-11-06 2010-11-05 Aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridine and octahydrobenzoquinoline

Publications (2)

Publication Number Publication Date
EA201270562A1 EA201270562A1 (ru) 2012-09-28
EA022323B1 true EA022323B1 (ru) 2015-12-30

Family

ID=41683136

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201270562A EA022323B1 (ru) 2009-11-06 2010-11-05 Арил- и гетероарилкарбонильные производные гексагидроинденопиридина и октагидробензохинолина

Country Status (27)

Country Link
US (3) US8497281B2 (cg-RX-API-DMAC7.html)
EP (1) EP2496559B1 (cg-RX-API-DMAC7.html)
JP (1) JP5796015B2 (cg-RX-API-DMAC7.html)
KR (1) KR20120102688A (cg-RX-API-DMAC7.html)
CN (2) CN105037326A (cg-RX-API-DMAC7.html)
AP (1) AP2012006248A0 (cg-RX-API-DMAC7.html)
AR (1) AR078887A1 (cg-RX-API-DMAC7.html)
AU (1) AU2010315077B2 (cg-RX-API-DMAC7.html)
BR (1) BR112012010792A2 (cg-RX-API-DMAC7.html)
CA (1) CA2778161A1 (cg-RX-API-DMAC7.html)
CL (1) CL2012001043A1 (cg-RX-API-DMAC7.html)
CO (1) CO6531441A2 (cg-RX-API-DMAC7.html)
EA (1) EA022323B1 (cg-RX-API-DMAC7.html)
GE (1) GEP20156330B (cg-RX-API-DMAC7.html)
IL (1) IL218652A0 (cg-RX-API-DMAC7.html)
IN (1) IN2012DN02807A (cg-RX-API-DMAC7.html)
MA (1) MA33776B1 (cg-RX-API-DMAC7.html)
MX (1) MX2012005309A (cg-RX-API-DMAC7.html)
MY (1) MY159922A (cg-RX-API-DMAC7.html)
NZ (1) NZ598950A (cg-RX-API-DMAC7.html)
PE (1) PE20121182A1 (cg-RX-API-DMAC7.html)
PH (1) PH12012500904A1 (cg-RX-API-DMAC7.html)
SG (1) SG179569A1 (cg-RX-API-DMAC7.html)
TW (1) TWI531571B (cg-RX-API-DMAC7.html)
UA (1) UA109643C2 (cg-RX-API-DMAC7.html)
UY (1) UY33001A (cg-RX-API-DMAC7.html)
WO (1) WO2011057054A1 (cg-RX-API-DMAC7.html)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE554078T1 (de) 2007-07-26 2012-05-15 Vitae Pharmaceuticals Inc Synthese von 11-beta-hydroxysteroid-dehydrogenase-1-hemmern
AR069207A1 (es) 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
WO2009063061A2 (en) * 2007-11-16 2009-05-22 Boehringer Ingelheim International Gmbh Aryl- and heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use
WO2009075835A1 (en) 2007-12-11 2009-06-18 Vitae Pharmaceutical, Inc CYCLIC UREA INHIBITORS OF 11β-HYDROXYSTEROID DEHYDROGENASE 1
TW200934490A (en) 2008-01-07 2009-08-16 Vitae Pharmaceuticals Inc Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1
JP5490020B2 (ja) 2008-01-24 2014-05-14 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状カルバゼート及びセミカルバジドインヒビター
US20110028445A1 (en) * 2008-02-12 2011-02-03 Boehringer Ingelheim International Gmbh Urea derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use
EP2254872A2 (en) 2008-02-15 2010-12-01 Vitae Pharmaceuticals, Inc. Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
AU2009241727B2 (en) 2008-05-01 2013-05-02 Vitae Pharmaceuticals, Inc Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US8592410B2 (en) 2008-05-01 2013-11-26 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11BETA-hydroxysteroid dehydrogenase 1
CL2009001058A1 (es) 2008-05-01 2010-09-10 Vitae Pharmaceuticals Inc Compuestos derivados de oxazinas sustituidas, inhibidores de la 11b-hidroxiesteroide deshidrogenasa de tipo-1; composicion farmaceutica; y uso del compuesto para inhibir la actividad de 11b-hsd1, como en el tratamiento de la diabetes, dislipidemia, hipertension, obesidad, cancer, glaucoma, entre otras.
US8765780B2 (en) 2008-05-13 2014-07-01 Boehringer Ingelheim International Gmbh Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use
JP5379160B2 (ja) 2008-07-25 2013-12-25 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 １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状インヒビター
CA2729998A1 (en) 2008-07-25 2010-01-28 Boehringer Ingelheim International Gmbh Inhibitors of 11beta-hydroxysteroid dehydrogenase 1
WO2010046445A2 (en) 2008-10-23 2010-04-29 Boehringer Ingelheim International Gmbh Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use
CA2744946A1 (en) 2009-02-04 2010-08-12 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
MA33216B1 (fr) 2009-04-30 2012-04-02 Boehringer Ingelheim Int Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1
WO2010139673A1 (en) 2009-06-02 2010-12-09 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2440537A1 (en) 2009-06-11 2012-04-18 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure
UY33001A (es) * 2009-11-06 2011-05-31 Boehringer Ingelheim Int Derivados arilo y heteroarilcarbonilo de hexahidroindenopiridina y octahidrobenzoquinolina
JP5860042B2 (ja) 2010-06-16 2016-02-16 ヴァイティー ファーマシューティカルズ，インコーポレイテッド 置換５、６及び７員複素環、そのような化合物を含有する医薬及びそれらの使用
JP5813106B2 (ja) 2010-06-25 2015-11-17 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 代謝障害の処置のための１１−β−ＨＳＤ１のインヒビターとしてのアザスピロヘキサノン
CA2813671A1 (en) 2010-11-02 2012-05-10 Boehringer Ingelheim International Gmbh Pharmaceutical combinations for the treatment of metabolic disorders
TWI537258B (zh) * 2010-11-05 2016-06-11 百靈佳殷格翰國際股份有限公司 六氫茚并吡啶及八氫苯并喹啉之芳基－及雜環芳基羰基衍生物
EP2744783A1 (en) 2011-08-17 2014-06-25 Boehringer Ingelheim International GmbH Indenopyridine derivatives
BR112014027884A2 (pt) * 2012-05-09 2017-06-27 Boehringer Ingelheim Int combinações farmacêuticas para tratamento de distúrbios metabólicos
JO3407B1 (ar) 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
US20150141651A1 (en) * 2013-11-20 2015-05-21 Boehringer Ingelheim International Gmbh Hexahydroindenopyridine derivatives
CN109045035B (zh) * 2018-07-19 2020-07-28 广西科技大学 7-(2,2-二甲基-3-丁烯酰胺基)-八氢苯喹啉乙酸酯在制备治疗肝病药物的应用
AR127706A1 (es) * 2021-11-19 2024-02-21 Hoffmann La Roche Síntesis de 2’-(7,7-dimetil-1’h,7h-espiro[furo[3,4-b]piridin-5,4’-piperidin]-1’-il)-1,3-dihidro-4’h-espiro[inden-2,5’-[1,3]oxazol]-4’-ona
CN116554000B (zh) * 2023-04-28 2025-07-25 南京林业大学 一种金属铑不对称催化二烷基取代的内炔制备茚醇的方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004089896A1 (en) * 2003-04-11 2004-10-21 Novo Nordisk A/S 11β-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ACTIVE COMPOUNDS
WO2009063061A2 (en) * 2007-11-16 2009-05-22 Boehringer Ingelheim International Gmbh Aryl- and heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use
WO2009100872A1 (en) * 2008-02-12 2009-08-20 Boehringer Ingelheim International Gmbh Urea derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use

Family Cites Families (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL127995C (cg-RX-API-DMAC7.html) 1963-12-20 Geigy Ag J R
US3341538A (en) * 1965-06-18 1967-09-12 Geigy Chem Corp Certain 2, 6-methano-3-benzazocines
DE1785124A1 (de) * 1968-08-13 1971-11-11 Prym Werke William Reissverschluss
DE2108954A1 (en) 1971-02-25 1972-09-07 Boehringer Sohn Ingelheim 2-(furylmethyl)-6,7-benzomorphans - useful as cns active agents
GB1304175A (cg-RX-API-DMAC7.html) * 1969-03-31 1973-01-24
DE2105743C3 (de) 1971-02-08 1979-11-29 Boehringer Sohn Ingelheim 2-(Furylmethyl)- a -5,9-dialkyl -6,7benzomorphane, Verfahren zu ihrer Herstellung und deren Verwendung
US3681349A (en) * 1970-03-05 1972-08-01 Morton Norwich Products Inc 1-(substituted benzyl) tetrahydro-2-(1h) pyrimidones
US3657257A (en) * 1970-08-31 1972-04-18 Robins Co Inc A H 3-aryl-8-carbamoyl nortropanes
DE2229695A1 (de) 1972-06-19 1974-01-31 Boehringer Sohn Ingelheim 2-(heteroaryl-methyl)-5,9 beta-dialkyl6,7-benzomorphane, deren saeureadditionssalze sowie verfahren zu deren herstellung
DE2338369A1 (de) * 1973-07-26 1975-02-13 Schering Ag Mikrobiologische hydroxylierung von 2,6-methano-3-benzazocinen
SU510999A3 (ru) * 1973-10-27 1976-04-15 К.Х.Берингер Зон, (Фирма) Способ получени (метоксиметил-фурилметил)6,7-бензоморфанов илиморфинанов
US4009171A (en) * 1974-02-21 1977-02-22 Sterling Drug Inc. N-acylated-11-oxygenated-2,6-methano-3-benzazocine intermediates
DE2411382C3 (de) 1974-03-09 1979-09-06 C.H. Boehringer Sohn, 6507 Ingelheim 2-Tetrahydrofurfuryl-6,7-benzomorphane, Verfahren zur Herstellung und deren Verwendung
US4087532A (en) * 1974-03-09 1978-05-02 Boehringer Ingelheim Gmbh Analgesically useful 2-tetrahydrofurfuryl-5-lower alkyl-2-oxy-6,7-benzomorphans and salts thereof
DE2437610A1 (de) 1974-08-05 1976-02-26 Boehringer Sohn Ingelheim Neue 5,9-beta-disubstituierte 2-tetrahydrofurfuryl-6,7-benzomorphane, deren saeureadditionssalze, ihre verwendung als arzneimittel und verfahren zu deren herstellung
US4108857A (en) * 1975-08-18 1978-08-22 Sterling Drug Inc. Imidazolylmethyl methanobenzazocines
DE2828039A1 (de) * 1978-06-26 1980-01-10 Boehringer Sohn Ingelheim 2-(2-alkoxyethyl)-2'-hydroxy-6,7-benzomorphane deren saeureadditionssalze diese enthaltende arzneimittel und verfahren zu deren herstellung
GB9510459D0 (en) 1995-05-24 1995-07-19 Zeneca Ltd Bicyclic amines
GB9517622D0 (en) * 1995-08-29 1995-11-01 Univ Edinburgh Regulation of intracellular glucocorticoid concentrations
JP3192662B2 (ja) 1996-07-31 2001-07-30 日研化学株式会社 ６―フェニルテトラヒドロ―１，３―オキサジン―２―オン誘導体及びそれを含む医薬組成物
GB9623944D0 (en) 1996-11-15 1997-01-08 Zeneca Ltd Bicyclic amine derivatives
DE69816758T2 (de) 1997-05-20 2004-06-03 Heraeus Quarzglas Gmbh & Co. Kg Synthetisches quarzglas zur verwendung in uv-strahlung und verfahren zu seiner herstellung
US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
YU54202A (sh) 2000-01-18 2006-01-16 Agouron Pharmaceuticals Inc. Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije
WO2001055063A1 (en) 2000-01-25 2001-08-02 Idemitsu Petrochemical Co., Ltd. Novel bisadamantane compounds, process for preparing the same, and novel biadamantane derivatives
DE10034623A1 (de) 2000-07-17 2002-01-31 Bayer Ag Heterocyclisch substituierte Pyridine als Cytokin-Inhibitoren
AU2003234621A1 (en) 2002-05-17 2003-12-02 Jenken Biosciences, Inc. Opioid and opioid-like compounds and uses thereof
AU2004226452B2 (en) * 2003-03-26 2008-07-24 Merck Sharp & Dohme Corp. Bicyclic piperidine derivatives as melanocortin-4 receptor agonists
US7700583B2 (en) * 2003-04-11 2010-04-20 High Point Pharmaceuticals, Llc 11β-hydroxysteroid dehydrogenase type 1 active compounds
EP1862181A3 (en) * 2003-04-11 2010-09-15 High Point Pharmaceuticals, LLC New pyrazolo[1,5-a] pyrimidine derivatives and pharmaceutical use thereof
CN101001842B (zh) * 2004-05-07 2015-10-07 因塞特公司 酰氨基化合物及其作为药物的应用
DE602005007344D1 (de) 2004-05-07 2008-07-17 Janssen Pharmaceutica Nv Adamantyl pyrrolidin-2-on-derivate als 11-beta hydroxysteroid dehydrogenas inhibitoren
WO2006024628A1 (en) 2004-08-30 2006-03-09 Janssen Pharmaceutica N.V. Tricyclic lactam derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors
JP2008515956A (ja) 2004-10-12 2008-05-15 ノボ ノルディスク アクティーゼルスカブ １１β−ヒドロキシステロイドデヒドロゲナーゼ１型活性スピロ化合物
JP2008515972A (ja) 2004-10-13 2008-05-15 ニューロジェン・コーポレーション メラニン濃縮ホルモン受容体のリガンドとしてのアリール置換８−アザビシクロ［３．２．１］オクタン化合物
US20090264650A1 (en) 2005-03-31 2009-10-22 Nobuo Cho Prophylactic/Therapeutic Agent for Diabetes
RU2381217C2 (ru) * 2005-04-05 2010-02-10 Ф.Хоффман-Ля Рош Аг Пиразолы
KR20080076916A (ko) 2005-11-01 2008-08-20 트랜스테크 파르마, 인크. 치환된 아미드의 약학적 사용
EP1945207A2 (en) 2005-11-01 2008-07-23 Transtech Pharma, Inc. Pharmaceutical use of substituted amides
JP2007140188A (ja) 2005-11-18 2007-06-07 Fujifilm Corp ポジ型感光性組成物及びそれを用いたパターン形成方法
WO2007076055A2 (en) 2005-12-22 2007-07-05 Entremed, Inc. Compositions and methods comprising proteinase activated receptor antagonists
AU2006335109B2 (en) 2005-12-30 2011-04-07 Merck Sharp & Dohme Corp. Cholesteryl ester transfer protein inhibitors
TW200804341A (en) * 2006-01-31 2008-01-16 Incyte Corp Amido compounds and their use as pharmaceuticals
EP2016047B1 (en) 2006-04-21 2013-08-28 Eli Lilly And Company Biphenyl amide lactam derivatives as inhibitors of 11- beta-hydroxysteroid dehydrogenase 1
EA016959B1 (ru) 2006-04-24 2012-08-30 Эли Лилли Энд Компани Замещенные пирролидиноны в качестве ингибиторов 11-бета-гидроксистероиддегидрогеназы 1 типа
CA2648019C (en) 2006-04-25 2014-04-01 Eli Lilly And Company Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
TW200811170A (en) * 2006-06-27 2008-03-01 Sanofi Aventis Urea derivatives of tropane, their preparation and their therapeutic application
CN101553474B (zh) 2006-10-19 2013-02-27 霍夫曼-拉罗奇有限公司 作为糖尿病用11b-HSD1抑制剂的咪唑啉酮和咪唑烷酮衍生物
TW200829171A (en) * 2006-11-17 2008-07-16 Nihon Nohyaku Co Ltd Haloalkyl sulfonanilide derivatives or salts thereof, herbicide using it as effective constituent and use-method thereof
EP1935420A1 (en) 2006-12-21 2008-06-25 Merck Sante 2-Adamantyl-butyramide derivatives as selective 11beta-HSD1 inhibitors
US8835426B2 (en) 2007-02-26 2014-09-16 Vitae Pharmaceuticals, Inc. Cyclic urea and carbamate inhibitors of 11β-hydroxysteroid dehydrogenase 1
RU64276U1 (ru) 2007-03-01 2007-06-27 Открытое акционерное общество "Татнефть" им. В.Д. Шашина Трубная обвязка устьевой арматуры нагнетательной скважины
CN101652359A (zh) 2007-03-09 2010-02-17 高点制药有限责任公司 作为羟类固醇脱氢酶抑制剂的吲哚-和苯并咪唑酰胺类
ATE554078T1 (de) 2007-07-26 2012-05-15 Vitae Pharmaceuticals Inc Synthese von 11-beta-hydroxysteroid-dehydrogenase-1-hemmern
AR069207A1 (es) 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
JP5734666B2 (ja) 2008-02-11 2015-06-17 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の１，３−オキサアゼパン−２−オン及び１，３−ジアゼパン−２−オン阻害剤
EP2254872A2 (en) 2008-02-15 2010-12-01 Vitae Pharmaceuticals, Inc. Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
JP5538356B2 (ja) 2008-03-18 2014-07-02 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１型の阻害剤
US8592410B2 (en) * 2008-05-01 2013-11-26 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11BETA-hydroxysteroid dehydrogenase 1
AU2009241727B2 (en) 2008-05-01 2013-05-02 Vitae Pharmaceuticals, Inc Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CA2729998A1 (en) 2008-07-25 2010-01-28 Boehringer Ingelheim International Gmbh Inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5379160B2 (ja) 2008-07-25 2013-12-25 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 １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状インヒビター
MA33216B1 (fr) * 2009-04-30 2012-04-02 Boehringer Ingelheim Int Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1
UY33001A (es) * 2009-11-06 2011-05-31 Boehringer Ingelheim Int Derivados arilo y heteroarilcarbonilo de hexahidroindenopiridina y octahidrobenzoquinolina

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004089896A1 (en) * 2003-04-11 2004-10-21 Novo Nordisk A/S 11β-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ACTIVE COMPOUNDS
WO2009063061A2 (en) * 2007-11-16 2009-05-22 Boehringer Ingelheim International Gmbh Aryl- and heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use
WO2009100872A1 (en) * 2008-02-12 2009-08-20 Boehringer Ingelheim International Gmbh Urea derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use

Also Published As

Publication number Publication date
BR112012010792A2 (pt) 2016-03-29
AU2010315077A1 (en) 2012-04-12
US9328072B2 (en) 2016-05-03
US20110136800A1 (en) 2011-06-09
EP2496559B1 (en) 2018-01-10
IL218652A0 (en) 2012-05-31
MX2012005309A (es) 2012-09-28
SG179569A1 (en) 2012-05-30
CO6531441A2 (es) 2012-09-28
PH12012500904A1 (en) 2015-02-20
US20160272590A1 (en) 2016-09-22
AR078887A1 (es) 2011-12-07
NZ598950A (en) 2014-05-30
PE20121182A1 (es) 2012-09-10
US8497281B2 (en) 2013-07-30
TW201132636A (en) 2011-10-01
TWI531571B (zh) 2016-05-01
US20140031544A1 (en) 2014-01-30
AU2010315077B2 (en) 2015-04-16
CL2012001043A1 (es) 2012-08-31
GEP20156330B (en) 2015-07-27
EA201270562A1 (ru) 2012-09-28
EP2496559A1 (en) 2012-09-12
CN102666491A (zh) 2012-09-12
IN2012DN02807A (cg-RX-API-DMAC7.html) 2015-07-24
US9663470B2 (en) 2017-05-30
CN105037326A (zh) 2015-11-11
MA33776B1 (fr) 2012-11-01
WO2011057054A1 (en) 2011-05-12
CN102666491B (zh) 2015-06-24
HK1175470A1 (zh) 2013-07-05
CA2778161A1 (en) 2011-05-12
JP2013510168A (ja) 2013-03-21
UA109643C2 (uk) 2015-09-25
AP2012006248A0 (en) 2012-06-30
MY159922A (en) 2017-02-15
UY33001A (es) 2011-05-31
JP5796015B2 (ja) 2015-10-21
KR20120102688A (ko) 2012-09-18

Similar Documents

Publication Publication Date Title
EA022323B1 (ru) Арил- и гетероарилкарбонильные производные гексагидроинденопиридина и октагидробензохинолина
KR100710402B1 (ko) 3환식 축합 이항환 화합물, 그 제조법 및 그것을 함유하는의약
JP6039585B2 (ja) Ｐｉｍキナーゼ阻害剤としてのトリアゾロピリジン化合物
JP6360915B2 (ja) アザモルフィナン誘導体及びその使用
EA022406B1 (ru) Кристаллические формы гидрохлорида (4a-r,9a-s)-1-(1h-бензоимидазол-5-карбонил)-2,3,4,4a,9,9a-гексагидро-1h-индено[2,1-b]пиридин-6-карбонитрила и их применение в качестве ингибиторов hsd 1
EA024293B1 (ru) СОЕДИНЕНИЯ И КОМПОЗИЦИИ В КАЧЕСТВЕ ИНГИБИТОРОВ с-kit КИНАЗЫ
MX2012014470A (es) Antagonistas d2, metodos de sintesis y metodos de uso.
JP4100865B2 (ja) 三環式縮合異項環化合物、その製造法およびその医薬
HK1184144B (en) Crystalline forms of hydrochloride salt of (4a-r,9a-s) -1- (1h - benzoimidazole- 5 -carbonyl) -2, 3, 4, 4a, 9, 9a - hexahydro -1h- indeno [2, 1 -b] pyridine- 6 -carbonitrile and their use as hsd 1 inhibitors
HK1175470B (en) Aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridine and octahydrobenzoquinoline
OA16399A (en) Crystalline forms of hydrochloride salt of (4AR, 9A-S)-1-(1H-benzoimidazole-5-car-bonyl)-2, 3, 4, 4A 9, 9A-hexahydro-1H-indeno[2, 1-B] pyridine6-carbonitrile and their use as HSD 1 inhibitors.
OA16619A (en) Aryl-and heteroarylcarbonyl derivatives of hexahydroindenopyridine and octahydro benzoquinoline.

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU