ME02066B - Kristalni oblici hidrohloridne soli ( 4a-r,9a-s)- 1-( 1h-benzoimidazol- s-karbonil)- 2,3,4,4a,9,9a-heksahidr0- 1h-inden0[2,1-b]piridin-6-karbonitrila i njihova upotreba kao inhibitora hsd 1 - Google Patents
Kristalni oblici hidrohloridne soli ( 4a-r,9a-s)- 1-( 1h-benzoimidazol- s-karbonil)- 2,3,4,4a,9,9a-heksahidr0- 1h-inden0[2,1-b]piridin-6-karbonitrila i njihova upotreba kao inhibitora hsd 1Info
- Publication number
- ME02066B ME02066B MEP-2015-42A MEP4215A ME02066B ME 02066 B ME02066 B ME 02066B ME P4215 A MEP4215 A ME P4215A ME 02066 B ME02066 B ME 02066B
- Authority
- ME
- Montenegro
- Prior art keywords
- compound
- diffraction peaks
- ray diffraction
- crystalline form
- angles
- Prior art date
Links
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 title 1
- 101100451537 Caenorhabditis elegans hsd-1 gene Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 25
- 238000002441 X-ray diffraction Methods 0.000 claims 14
- 238000000034 method Methods 0.000 claims 10
- 239000012458 free base Substances 0.000 claims 9
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 6
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 6
- 239000013078 crystal Substances 0.000 claims 6
- 238000002360 preparation method Methods 0.000 claims 5
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 3
- 230000015572 biosynthetic process Effects 0.000 claims 3
- 238000001816 cooling Methods 0.000 claims 3
- 230000005588 protonation Effects 0.000 claims 3
- 102000004277 11-beta-hydroxysteroid dehydrogenases Human genes 0.000 claims 2
- 108090000874 11-beta-hydroxysteroid dehydrogenases Proteins 0.000 claims 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000000725 suspension Substances 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 238000003756 stirring Methods 0.000 claims 1
Classifications
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- 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
-
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/US2010/055586 WO2011057054A1 (en) | 2009-11-06 | 2010-11-05 | Aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridine and octahydrobenzoquinoline |
| US201161484995P | 2011-05-11 | 2011-05-11 | |
| EP11785232.7A EP2635563B1 (en) | 2010-11-05 | 2011-11-04 | 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 |
| PCT/US2011/059331 WO2012061708A1 (en) | 2010-11-05 | 2011-11-04 | 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02066B true ME02066B (me) | 2015-05-20 |
Family
ID=44999935
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2015-42A ME02066B (me) | 2010-11-05 | 2011-11-04 | Kristalni oblici hidrohloridne soli ( 4a-r,9a-s)- 1-( 1h-benzoimidazol- s-karbonil)- 2,3,4,4a,9,9a-heksahidr0- 1h-inden0[2,1-b]piridin-6-karbonitrila i njihova upotreba kao inhibitora hsd 1 |
Country Status (36)
Families Citing this family (12)
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| TW200927115A (en) | 2007-11-16 | 2009-07-01 | Boehringer Ingelheim Int | Aryl-and heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use |
| AR071719A1 (es) | 2008-05-13 | 2010-07-07 | Boehringer Ingelheim Int | Derivados aliciclicos de acido carboxilico de benzomorfanos y estructuras relacionadas, medicamentos que contienen dichos compuestos y su uso.procesos de obtencion |
| US8703765B2 (en) | 2009-06-02 | 2014-04-22 | Boehringer Ingelheim International Gmbh | Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1 |
| US8927539B2 (en) | 2009-06-11 | 2015-01-06 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1 based on the 1,3-oxazinan-2-one structure |
| WO2011159760A1 (en) | 2010-06-16 | 2011-12-22 | Vitae Pharmaceuticals, Inc. | Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use |
| 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 |
| WO2013025664A1 (en) | 2011-08-17 | 2013-02-21 | Boehringer Ingelheim International Gmbh | Indenopyridine derivatives |
| US20130303446A1 (en) * | 2012-05-09 | 2013-11-14 | Boehringer Ingelheim International Gmbh | Pharmaceutical combinations for the treatment of metabolic disorders |
| EP3235813A1 (en) | 2016-04-19 | 2017-10-25 | Cidqo 2012, S.L. | Aza-tetra-cyclo derivatives |
| WO2019043217A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROBENZIMIDAZOLONES |
| ES2995214T3 (en) | 2019-03-06 | 2025-02-07 | C4 Therapeutics Inc | Heterocyclic compounds for medical treatment |
| CN118005644B (zh) * | 2024-01-29 | 2025-12-16 | 中国科学院南海海洋研究所 | 十氢芴型生物碱及其制备方法和在制备抗菌药物中应用 |
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| 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 |
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2011
- 2011-10-18 TW TW100137675A patent/TWI537258B/zh not_active IP Right Cessation
- 2011-11-01 AR ARP110104053A patent/AR083678A1/es unknown
- 2011-11-01 UY UY0001033701A patent/UY33701A/es not_active Application Discontinuation
- 2011-11-04 GE GEAP201113105A patent/GEP20166481B/en unknown
- 2011-11-04 EP EP11785232.7A patent/EP2635563B1/en active Active
- 2011-11-04 CN CN201180053044.5A patent/CN103228642B/zh not_active Expired - Fee Related
- 2011-11-04 AP AP2013006902A patent/AP3521A/xx active
- 2011-11-04 US US13/289,418 patent/US8686149B2/en active Active
- 2011-11-04 PL PL11785232T patent/PL2635563T3/pl unknown
- 2011-11-04 ME MEP-2015-42A patent/ME02066B/me unknown
- 2011-11-04 AU AU2011323164A patent/AU2011323164B2/en not_active Ceased
- 2011-11-04 MX MX2013005069A patent/MX2013005069A/es unknown
- 2011-11-04 NZ NZ609281A patent/NZ609281A/en not_active IP Right Cessation
- 2011-11-04 SG SG2013026430A patent/SG189859A1/en unknown
- 2011-11-04 DK DK11785232.7T patent/DK2635563T3/en active
- 2011-11-04 EA EA201390643A patent/EA022406B1/ru not_active IP Right Cessation
- 2011-11-04 HR HRP20150327TT patent/HRP20150327T1/hr unknown
- 2011-11-04 PE PE2013000949A patent/PE20140123A1/es not_active Application Discontinuation
- 2011-11-04 RS RS20150205A patent/RS53900B1/sr unknown
- 2011-11-04 SI SI201130449T patent/SI2635563T1/sl unknown
- 2011-11-04 BR BR112013011095A patent/BR112013011095A2/pt not_active IP Right Cessation
- 2011-11-04 JP JP2013537864A patent/JP2013541592A/ja active Pending
- 2011-11-04 PH PH1/2013/500879A patent/PH12013500879A1/en unknown
- 2011-11-04 PT PT117852327T patent/PT2635563E/pt unknown
- 2011-11-04 WO PCT/US2011/059331 patent/WO2012061708A1/en not_active Ceased
- 2011-11-04 UA UAA201307042A patent/UA110807C2/uk unknown
- 2011-11-04 ES ES11785232.7T patent/ES2533833T3/es active Active
- 2011-11-04 CA CA2816136A patent/CA2816136A1/en not_active Abandoned
- 2011-11-04 KR KR1020137014295A patent/KR20130119939A/ko not_active Withdrawn
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2012
- 2012-03-16 TN TNP2012000117A patent/TN2012000117A1/en unknown
- 2012-04-05 EC ECSP12011788 patent/ECSP12011788A/es unknown
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2013
- 2013-04-09 IL IL225647A patent/IL225647A0/en unknown
- 2013-05-03 CL CL2013001221A patent/CL2013001221A1/es unknown
- 2013-05-30 CO CO13132839A patent/CO6781480A2/es active IP Right Grant
- 2013-06-05 EC ECSP13012664 patent/ECSP13012664A/es unknown
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2014
- 2014-02-26 US US14/190,899 patent/US9120769B2/en active Active
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2015
- 2015-02-25 CY CY20151100195T patent/CY1116043T1/el unknown
- 2015-04-16 SM SM201500095T patent/SMT201500095B/xx unknown
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