ME01537B - Spojevi spiropiperidona kao antagonisti receptora orl-1 - Google Patents
Spojevi spiropiperidona kao antagonisti receptora orl-1Info
- Publication number
- ME01537B ME01537B MEP-2013-118A MEP11813A ME01537B ME 01537 B ME01537 B ME 01537B ME P11813 A MEP11813 A ME P11813A ME 01537 B ME01537 B ME 01537B
- Authority
- ME
- Montenegro
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- methyl
- compound according
- ylmethyl
- Prior art date
Links
- 239000002464 receptor antagonist Substances 0.000 title description 3
- 229940044551 receptor antagonist Drugs 0.000 title description 3
- JUXAVSAMVBLDKO-UHFFFAOYSA-N 1-(1-azabicyclo[2.2.2]octan-3-yl)-3-[3-(1h-indol-3-yl)-1-oxo-1-spiro[1,2-dihydroindene-3,4'-piperidine]-1'-ylpropan-2-yl]urea Chemical class C1N(CC2)CCC2C1NC(=O)NC(C(=O)N1CCC2(C3=CC=CC=C3CC2)CC1)CC1=CNC2=CC=CC=C12 JUXAVSAMVBLDKO-UHFFFAOYSA-N 0.000 title description 2
- 108010020615 nociceptin receptor Proteins 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims description 14
- -1 cyano, cyanomethyl Chemical group 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 13
- 229910052731 fluorine Inorganic materials 0.000 claims 6
- 239000011737 fluorine Substances 0.000 claims 6
- 125000001153 fluoro group Chemical group F* 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 5
- 229910052801 chlorine Chemical group 0.000 claims 3
- 239000000460 chlorine Chemical group 0.000 claims 3
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- NKQHBJNRBKHUQR-UHFFFAOYSA-N [2-[4-[(2-chloro-4,4-difluorospiro[5h-thieno[2,3-c]pyran-7,4'-piperidine]-1'-yl)methyl]-3-methylpyrazol-1-yl]pyridin-3-yl]methanol Chemical compound C1=C(CN2CCC3(CC2)C=2SC(Cl)=CC=2C(F)(F)CO3)C(C)=NN1C1=NC=CC=C1CO NKQHBJNRBKHUQR-UHFFFAOYSA-N 0.000 claims 2
- 125000004849 alkoxymethyl group Chemical group 0.000 claims 2
- 239000004615 ingredient Substances 0.000 claims 2
- 230000001225 therapeutic effect Effects 0.000 claims 2
- 125000001607 1,2,3-triazol-1-yl group Chemical group [*]N1N=NC([H])=C1[H] 0.000 claims 1
- 125000003626 1,2,4-triazol-1-yl group Chemical group [*]N1N=C([H])N=C1[H] 0.000 claims 1
- XTVMMUUMUBGOPK-UHFFFAOYSA-N 2-chloro-4,4-difluoro-1'-[[3-methyl-1-[3-(pyrazol-1-ylmethyl)pyridin-2-yl]pyrazol-4-yl]methyl]spiro[5h-thieno[2,3-c]pyran-7,4'-piperidine] Chemical compound C1=C(CN2CCC3(CC2)C=2SC(Cl)=CC=2C(F)(F)CO3)C(C)=NN1C1=NC=CC=C1CN1C=CC=N1 XTVMMUUMUBGOPK-UHFFFAOYSA-N 0.000 claims 1
- TVSCFMXJYNZEER-UHFFFAOYSA-N 7-methoxy-11a-methyl-1,9b,10,11-tetrahydronaphtho[1,2-g]indole Chemical compound C1CC2(C)CC=NC2=C2C=CC3=CC(OC)=CC=C3C21 TVSCFMXJYNZEER-UHFFFAOYSA-N 0.000 claims 1
- 208000020401 Depressive disease Diseases 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical group CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010033307 Overweight Diseases 0.000 claims 1
- ZAOZBWZTMUTPSX-UHFFFAOYSA-N [4-[(2-chloro-4,4-difluorospiro[5h-thieno[2,3-c]pyran-7,4'-piperidine]-1'-yl)methyl]-1-(3-fluoropyridin-2-yl)pyrazol-3-yl]methanol Chemical compound C1=C(CN2CCC3(CC2)C=2SC(Cl)=CC=2C(F)(F)CO3)C(CO)=NN1C1=NC=CC=C1F ZAOZBWZTMUTPSX-UHFFFAOYSA-N 0.000 claims 1
- 239000002585 base Substances 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000004859 cyclopropyloxymethyl group Chemical group C1(CC1)OC* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 125000004284 isoxazol-3-yl group Chemical group [H]C1=C([H])C(*)=NO1 0.000 claims 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 125000004304 oxazol-5-yl group Chemical group O1C=NC=C1* 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004353 pyrazol-1-yl group Chemical group [H]C1=NN(*)C([H])=C1[H] 0.000 claims 1
- 239000012896 selective serotonin reuptake inhibitor Substances 0.000 claims 1
- 125000004192 tetrahydrofuran-2-yl group Chemical group [H]C1([H])OC([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 241000884009 Hyporhamphus unifasciatus Species 0.000 description 1
- 241001417524 Pomacanthidae Species 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/20—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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
- A61K31/435—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
- A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
-
- 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
-
- 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
- A61P25/06—Antimigraine 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
- A61P25/24—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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (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)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09382246 | 2009-11-16 | ||
| US29862910P | 2010-01-27 | 2010-01-27 | |
| PCT/US2010/056180 WO2011060035A1 (en) | 2009-11-16 | 2010-11-10 | Spiropiperidine compounds as orl-1 receptor antagonists |
| EP10782482.3A EP2501703B1 (en) | 2009-11-16 | 2010-11-10 | Spiropiperidine compounds as orl-1 receptor antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME01537B true ME01537B (me) | 2014-04-20 |
Family
ID=41728051
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2013-118A ME01537B (me) | 2009-11-16 | 2010-11-10 | Spojevi spiropiperidona kao antagonisti receptora orl-1 |
Country Status (34)
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG10201401661RA (en) | 2009-12-04 | 2014-07-30 | Sunovion Pharmaceuticals Inc | Multicycle compounds and pharmaceutical compositions useful for the treatment of neurological disorders |
| JP2013540145A (ja) * | 2010-10-21 | 2013-10-31 | ウニベルシテート デス ザールランデス | コルチゾール依存性疾患の治療用の選択的cyp11b1阻害剤 |
| TWI582096B (zh) * | 2011-12-06 | 2017-05-11 | 美國禮來大藥廠 | 用於酒精依賴及濫用處理之4',5'-二氫螺[哌啶-4,7'-噻吩并[2,3-c]哌喃]化合物 |
| TW201416370A (zh) | 2012-07-31 | 2014-05-01 | Lilly Co Eli | 用於治療焦慮之orl-1受體拮抗劑 |
| NZ739834A (en) | 2012-10-02 | 2018-11-30 | Bayer Cropscience Ag | Heterocyclic compounds as pesticides |
| JP6440625B2 (ja) | 2012-11-14 | 2018-12-19 | ザ・ジョンズ・ホプキンス・ユニバーシティー | 精神分裂病を処置するための方法および組成物 |
| TW201607923A (zh) | 2014-07-15 | 2016-03-01 | 歌林達有限公司 | 被取代之氮螺環(4.5)癸烷衍生物 |
| JO3638B1 (ar) * | 2015-09-09 | 2020-08-27 | Lilly Co Eli | مركبات مفيدة في تثبيط ror - جاما- t |
| CA3032302A1 (en) | 2016-07-29 | 2018-02-01 | Taleen G. Hanania | Compounds and compositions and uses thereof |
| CN110087687A (zh) | 2016-07-29 | 2019-08-02 | 赛诺维信制药公司 | 化合物、组合物及其用途 |
| JP7146782B2 (ja) | 2017-02-16 | 2022-10-04 | サノビオン ファーマシューティカルズ インク | 統合失調症を処置する方法 |
| LT3589638T (lt) | 2017-03-02 | 2021-06-10 | Eli Lilly And Company | Junginiai, naudingi ror-gama-t slopinimui |
| JP6766274B2 (ja) * | 2017-03-02 | 2020-10-07 | イーライ リリー アンド カンパニー | Ror−ガンマ−tを阻害するのに有用な化合物 |
| CN111183138A (zh) | 2017-08-02 | 2020-05-19 | 赛诺维信制药公司 | 异色满化合物以及用途 |
| KR102746817B1 (ko) | 2018-02-16 | 2024-12-24 | 스미토모 파마 아메리카, 인크. | 염, 결정 형태 및 이들의 제조 방법 |
| CA3121910A1 (en) | 2018-12-17 | 2020-06-25 | Vertex Pharmaceuticals Incorporated | Inhibitors of apol1 and methods of using same |
| MX2021010880A (es) | 2019-03-14 | 2022-01-18 | Sunovion Pharmaceuticals Inc | Sales de un compuesto de isocromanilo y formas cristalinas, procesos de preparacion, usos terapeuticos y composiciones farmaceuticas de las mismas. |
| AU2021257786A1 (en) | 2020-04-14 | 2022-11-03 | Sunovion Pharmaceuticals Inc. | (S)-(4,5-dihydro-7H-thieno[2,3-c]pyran-7-yl)-N-methylmethanamine for treating neurological and psychiatric disorders |
| IL318169A (en) | 2020-08-26 | 2025-03-01 | Vertex Pharma | Apol1 inhibitors and methods of use are the same |
| AU2023218994A1 (en) * | 2022-02-08 | 2024-08-22 | Vertex Pharmaceuticals Incorporated | 2-methyl-4',5'-dihydrospiro[piperidine-4,7'-thieno[2,3-c]pyran] derivatives as inhibitors of apol1 and methods of using same |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL96507A0 (en) | 1989-12-08 | 1991-08-16 | Merck & Co Inc | Nitrogen-containing spirocycles and pharmaceutical compositions containing them |
| JP3989247B2 (ja) * | 1999-12-06 | 2007-10-10 | ユーロ−セルティーク エス.エイ. | ノシセプチン受容体親和性を有するトリアゾスピロ化合物 |
| NZ528978A (en) * | 2001-04-18 | 2004-06-25 | Euro Celtique S | Spiropyrazole compounds |
| WO2002088089A1 (en) | 2001-04-19 | 2002-11-07 | Banyu Pharmaceutical Co., Ltd. | Spiropiperidine derivatives, nociceptin receptor antagonists containing the same as the active ingredient and medicinal compositions |
| ATE396995T1 (de) * | 2001-07-23 | 2008-06-15 | Banyu Pharma Co Ltd | 4-oxoimidazolidin-2-spiro piperidin derivat |
| JP2005519921A (ja) * | 2002-01-28 | 2005-07-07 | ファイザー株式会社 | Orl−1受容体リガンドとしてのn置換スピロピペリジン化合物 |
| JPWO2003095427A1 (ja) | 2002-05-10 | 2005-09-15 | 大正製薬株式会社 | スピロ環化合物 |
| US6995168B2 (en) * | 2002-05-31 | 2006-02-07 | Euro-Celtique S.A. | Triazaspiro compounds useful for treating or preventing pain |
| KR20050043935A (ko) * | 2002-09-09 | 2005-05-11 | 얀센 파마슈티카 엔.브이. | Orl-1 수용체 매개 장애의 치료에 유용한 하이드록시 알킬 치환된 1,3,8-트리아자스피로[4.5]데칸-4-온 유도체 |
| WO2005016913A1 (en) * | 2003-08-19 | 2005-02-24 | Pfizer Japan, Inc. | Tetrahydroisoquinoline or isochroman compounds as orl-1 receptor ligands for the treatment of pain and cns disorders |
| DE10360792A1 (de) * | 2003-12-23 | 2005-07-28 | Grünenthal GmbH | Spirocyclische Cyclohexan-Derivate |
| CA2563164A1 (en) * | 2004-03-29 | 2005-10-06 | Pfizer Inc. | Alpha aryl or heteroaryl methyl beta piperidino propanoic acid compounds as orl1-receptor antagonists |
| DE102004039382A1 (de) * | 2004-08-13 | 2006-02-23 | Grünenthal GmbH | Spirocyclische Cyclohexan-Derivate |
| EP2020414A1 (en) | 2007-06-20 | 2009-02-04 | Laboratorios del Dr. Esteve S.A. | spiro[piperidine-4,4'-thieno[3,2-c]pyran] derivatives and related compounds as inhibitors of the sigma receptor for the treatment of psychosis |
| CL2009000731A1 (es) * | 2008-03-27 | 2009-05-15 | Gruenenthal Gmbh | Compuestos derivados de ciclohexano espirociclicos sustituidos, composicion farmaceutica que contiene a dicho compuesto y su uso como moduladores del receptor de opioides µ y el receptor orl-1 para tratar el dolor, ansiedad, depresion, epilepsia, alzheimer, abuso de alcohol, hipertension, anorexia, obesidad y diarrea. |
-
2010
- 2010-10-11 UA UAA201205367A patent/UA107943C2/uk unknown
- 2010-11-02 AR ARP100104035A patent/AR078863A1/es active IP Right Grant
- 2010-11-03 JO JO2010386A patent/JO2887B1/en active
- 2010-11-05 TW TW099138241A patent/TWI465453B/zh not_active IP Right Cessation
- 2010-11-10 MY MYPI2012002117A patent/MY160665A/en unknown
- 2010-11-10 PL PL10782482T patent/PL2501703T3/pl unknown
- 2010-11-10 SI SI201030388T patent/SI2501703T1/sl unknown
- 2010-11-10 PH PH1/2012/500969A patent/PH12012500969A1/en unknown
- 2010-11-10 CA CA2796161A patent/CA2796161C/en not_active Expired - Fee Related
- 2010-11-10 KR KR1020127012498A patent/KR101363830B1/ko not_active Expired - Fee Related
- 2010-11-10 CN CN201080051850.4A patent/CN102612520B/zh not_active Expired - Fee Related
- 2010-11-10 PE PE2012000659A patent/PE20121430A1/es active IP Right Grant
- 2010-11-10 AU AU2010319581A patent/AU2010319581C1/en not_active Ceased
- 2010-11-10 DK DK10782482.3T patent/DK2501703T3/da active
- 2010-11-10 NZ NZ600006A patent/NZ600006A/en not_active IP Right Cessation
- 2010-11-10 MX MX2012005691A patent/MX2012005691A/es active IP Right Grant
- 2010-11-10 HR HRP20130967AT patent/HRP20130967T1/hr unknown
- 2010-11-10 US US12/943,187 patent/US8232289B2/en not_active Expired - Fee Related
- 2010-11-10 EP EP10782482.3A patent/EP2501703B1/en active Active
- 2010-11-10 RS RS20130485A patent/RS53018B/sr unknown
- 2010-11-10 WO PCT/US2010/056180 patent/WO2011060035A1/en not_active Ceased
- 2010-11-10 EA EA201290352A patent/EA020848B1/ru not_active IP Right Cessation
- 2010-11-10 JP JP2012538935A patent/JP5680101B2/ja not_active Expired - Fee Related
- 2010-11-10 ES ES10782482T patent/ES2435814T3/es active Active
- 2010-11-10 PT PT107824823T patent/PT2501703E/pt unknown
- 2010-11-10 ME MEP-2013-118A patent/ME01537B/me unknown
-
2012
- 2012-04-23 IL IL219370A patent/IL219370A/en not_active IP Right Cessation
- 2012-04-23 ZA ZA2012/02967A patent/ZA201202967B/en unknown
- 2012-05-04 CO CO12073055A patent/CO6541545A2/es active IP Right Grant
- 2012-05-11 HN HN2012001011A patent/HN2012001011A/es unknown
- 2012-05-11 DO DO2012000135A patent/DOP2012000135A/es unknown
- 2012-05-14 MA MA34869A patent/MA33751B1/fr unknown
- 2012-05-16 EC ECSP12011902 patent/ECSP12011902A/es unknown
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2013
- 2013-02-26 CR CR20130087A patent/CR20130087A/es unknown
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