CY1118721T1 - Παραγωγα 2,3 διϋδρο-1η-ινδεν-1-υλ-2,7-διαζασπειρο[3.6]εννεανιου και η χρηση αυτων ως ανταγωνιστες ή αντιστροφοι αγωνιστες του υποδοχεα γκρελινης - Google Patents
Παραγωγα 2,3 διϋδρο-1η-ινδεν-1-υλ-2,7-διαζασπειρο[3.6]εννεανιου και η χρηση αυτων ως ανταγωνιστες ή αντιστροφοι αγωνιστες του υποδοχεα γκρελινηςInfo
- Publication number
- CY1118721T1 CY1118721T1 CY20151101105T CY151101105T CY1118721T1 CY 1118721 T1 CY1118721 T1 CY 1118721T1 CY 20151101105 T CY20151101105 T CY 20151101105T CY 151101105 T CY151101105 T CY 151101105T CY 1118721 T1 CY1118721 T1 CY 1118721T1
- Authority
- CY
- Cyprus
- Prior art keywords
- diazaspier
- diazapeiro
- derydro
- inden
- dyn
- Prior art date
Links
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 102000012004 Ghrelin Human genes 0.000 abstract 1
- 101800001586 Ghrelin Proteins 0.000 abstract 1
- 102000000393 Ghrelin Receptors Human genes 0.000 abstract 1
- 108010016122 Ghrelin Receptors Proteins 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- GNKDKYIHGQKHHM-RJKLHVOGSA-N ghrelin Chemical compound C([C@H](NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)CN)COC(=O)CCCCCCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)C1=CC=CC=C1 GNKDKYIHGQKHHM-RJKLHVOGSA-N 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
- C07D471/10—Spiro-condensed systems
-
- 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
-
- 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
- A61K31/4747—Quinolines; Isoquinolines spiro-condensed
-
- 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
- A61K31/4965—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
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- A61P3/08—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- 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)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Η παρούσα εφεύρεση παρέχει μια ένωση του Χημικού Τύπου (I) ή ένα φαρμακευτικώς αποδεκτό άλας εξ' αυτής όπου τα R1, R2, Ra, L, Ζ, Ζ1 και Ζ2 καθορίζονται ως εις το παρόν, που δρουν ως ανταγωνιστές ή αντίστροφοι αγωνιστές της Γκρελίνης· φαρμακευτικές συνθέσεις εξ' αυτής· και μεθόδους αγωγής παθήσεων, διαταραχών, ή καταστάσεων που μεσολαβούνται μέσω του ανταγωνισμού του υποδοχέα Γκρελίνης.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31552210P | 2010-03-19 | 2010-03-19 | |
| US201161444401P | 2011-02-18 | 2011-02-18 | |
| PCT/IB2011/051035 WO2011114271A1 (en) | 2010-03-19 | 2011-03-11 | 2,3 dihydro-1h-inden-1-yl- 2,7-diazaspiro [3.6] nonane derivatives and their use as antagonists or inverse agonists of the ghrelin receptor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CY1118721T1 true CY1118721T1 (el) | 2017-07-12 |
Family
ID=44647714
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY20151101105T CY1118721T1 (el) | 2010-03-19 | 2015-12-04 | Παραγωγα 2,3 διϋδρο-1η-ινδεν-1-υλ-2,7-διαζασπειρο[3.6]εννεανιου και η χρηση αυτων ως ανταγωνιστες ή αντιστροφοι αγωνιστες του υποδοχεα γκρελινης |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US8609680B2 (el) |
| EP (1) | EP2547679B1 (el) |
| JP (1) | JP5496409B2 (el) |
| KR (1) | KR101455917B1 (el) |
| CN (1) | CN102939290B (el) |
| AR (1) | AR080688A1 (el) |
| AU (1) | AU2011228699B2 (el) |
| BR (1) | BR112012023664B1 (el) |
| CA (1) | CA2792234C (el) |
| CY (1) | CY1118721T1 (el) |
| DK (1) | DK2547679T3 (el) |
| ES (1) | ES2557895T3 (el) |
| HR (1) | HRP20151232T1 (el) |
| HU (1) | HUE025774T2 (el) |
| IL (1) | IL221952A (el) |
| ME (1) | ME02330B (el) |
| MX (1) | MX2012010772A (el) |
| PH (1) | PH12012501800A1 (el) |
| PL (1) | PL2547679T3 (el) |
| PT (1) | PT2547679E (el) |
| RS (1) | RS54383B1 (el) |
| RU (1) | RU2524341C2 (el) |
| SG (1) | SG183812A1 (el) |
| SI (1) | SI2547679T1 (el) |
| TW (1) | TWI410423B (el) |
| WO (1) | WO2011114271A1 (el) |
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| HRP20191937T1 (hr) | 2012-09-25 | 2020-01-10 | F. Hoffmann - La Roche Ag | Derivati heksahidropirolo [3,4-c]pirola i srodni spojevi kao inhibitori autotaksina (atx) i kao inhibitori proizvodnje lizofosfatidne kiseline (lpa) za liječenje npr. bubrežnih bolesti |
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| LT3074400T (lt) | 2013-11-26 | 2018-02-12 | F. Hoffmann-La Roche Ag | Oktahidro-ciklobuta [1,2-c;3,4-c`]dipirolo dariniai kaip autotaksino inhibitoriai |
| JP6574438B2 (ja) * | 2014-03-17 | 2019-09-11 | リマインド エヌヴイRemynd Nv | 2,7−ジアザスピロ[3.5]ノナン化合物 |
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| EA037928B1 (ru) | 2014-03-26 | 2021-06-08 | Ф. Хоффманн-Ля Рош Аг | Бициклические соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa) |
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| MX377277B (es) | 2015-09-04 | 2025-03-07 | Hoffmann La Roche | Derivados de fenoximetilo. |
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| AU2016328535A1 (en) | 2015-09-24 | 2017-11-09 | F. Hoffmann-La Roche Ag | Bicyclic compounds as ATX inhibitors |
| KR102882225B1 (ko) | 2017-02-21 | 2025-11-07 | 엘지전자 주식회사 | 냉장고 |
| BR112019019017A2 (pt) | 2017-03-16 | 2020-04-14 | Hoffmann La Roche | compostos heterocíclicos de utilidade como inibidores duplos de atx/ca |
| JP7090099B2 (ja) | 2017-03-16 | 2022-06-23 | エフ.ホフマン-ラ ロシュ アーゲー | Atxインヒビターとしての新規二環式化合物 |
| AU2018306619B2 (en) * | 2017-07-28 | 2022-06-02 | Chemocentryx, Inc. | Immunomodulator compounds |
| CN108588215A (zh) * | 2018-05-03 | 2018-09-28 | 成都中创清科医学检验所有限公司 | 一种用于检测家族性高胆固醇血症易感性相关的snp位点的引物及其检测方法 |
| CN109970631A (zh) * | 2019-03-26 | 2019-07-05 | 上海吉奉生物科技有限公司 | 一种5-碘-2-吡啶乙酸的合成方法 |
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| CN110172062B (zh) * | 2019-06-21 | 2022-01-07 | 南京药石科技股份有限公司 | 一种单氟代螺环化合物的合成方法及其中间体 |
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| CA2759843A1 (en) | 2009-05-08 | 2010-11-10 | Pfizer Inc. | Gpr 119 modulators |
| US20120083476A1 (en) * | 2009-06-05 | 2012-04-05 | Janssen Pharmaceutica Nv | Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase |
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| WO2011005611A1 (en) | 2009-07-09 | 2011-01-13 | Merck Sharp & Dohme Corp. | Neuromedin u receptor agonists and uses thereof |
-
2011
- 2011-03-11 HU HUE11713083A patent/HUE025774T2/en unknown
- 2011-03-11 RU RU2012137489/04A patent/RU2524341C2/ru not_active IP Right Cessation
- 2011-03-11 DK DK11713083.1T patent/DK2547679T3/en active
- 2011-03-11 HR HRP20151232TT patent/HRP20151232T1/hr unknown
- 2011-03-11 SI SI201130664T patent/SI2547679T1/sl unknown
- 2011-03-11 PH PH1/2012/501800A patent/PH12012501800A1/en unknown
- 2011-03-11 JP JP2013500620A patent/JP5496409B2/ja not_active Expired - Fee Related
- 2011-03-11 CN CN201180014627.7A patent/CN102939290B/zh not_active Expired - Fee Related
- 2011-03-11 PT PT117130831T patent/PT2547679E/pt unknown
- 2011-03-11 AU AU2011228699A patent/AU2011228699B2/en not_active Ceased
- 2011-03-11 RS RS20150808A patent/RS54383B1/sr unknown
- 2011-03-11 WO PCT/IB2011/051035 patent/WO2011114271A1/en not_active Ceased
- 2011-03-11 KR KR1020127027230A patent/KR101455917B1/ko not_active Expired - Fee Related
- 2011-03-11 CA CA2792234A patent/CA2792234C/en not_active Expired - Fee Related
- 2011-03-11 ME MEP-2015-189A patent/ME02330B/me unknown
- 2011-03-11 PL PL11713083T patent/PL2547679T3/pl unknown
- 2011-03-11 MX MX2012010772A patent/MX2012010772A/es active IP Right Grant
- 2011-03-11 BR BR112012023664A patent/BR112012023664B1/pt not_active IP Right Cessation
- 2011-03-11 SG SG2012062667A patent/SG183812A1/en unknown
- 2011-03-11 EP EP11713083.1A patent/EP2547679B1/en active Active
- 2011-03-11 ES ES11713083.1T patent/ES2557895T3/es active Active
- 2011-03-16 TW TW100109022A patent/TWI410423B/zh not_active IP Right Cessation
- 2011-03-16 US US13/049,225 patent/US8609680B2/en active Active
- 2011-03-18 AR ARP110100888A patent/AR080688A1/es not_active Application Discontinuation
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2012
- 2012-09-13 IL IL221952A patent/IL221952A/en not_active IP Right Cessation
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2013
- 2013-11-18 US US14/083,275 patent/US20140080756A1/en not_active Abandoned
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2015
- 2015-12-04 CY CY20151101105T patent/CY1118721T1/el unknown
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