AR102019A1 - (r)-3-((3s,4s)-3-fluoro-4-(4-hidroxifenil)piperidin-1-il)-1-(4-metilbencil)pirrolidin-2-ona y sus profármacos para el tratamiento de trastornos psiquiátricos - Google Patents
(r)-3-((3s,4s)-3-fluoro-4-(4-hidroxifenil)piperidin-1-il)-1-(4-metilbencil)pirrolidin-2-ona y sus profármacos para el tratamiento de trastornos psiquiátricosInfo
- Publication number
- AR102019A1 AR102019A1 ARP150100067A ARP150100067A AR102019A1 AR 102019 A1 AR102019 A1 AR 102019A1 AR P150100067 A ARP150100067 A AR P150100067A AR P150100067 A ARP150100067 A AR P150100067A AR 102019 A1 AR102019 A1 AR 102019A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- substituted
- esters
- halo
- substituents selected
- Prior art date
Links
- 208000020016 psychiatric disease Diseases 0.000 title 1
- -1 amino acid esters Chemical class 0.000 abstract 6
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000001475 halogen functional group Chemical group 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 1
- 125000005907 alkyl ester group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000002393 azetidinyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 abstract 1
- 150000003009 phosphonic acids Chemical class 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- IIACRCGMVDHOTQ-UHFFFAOYSA-N sulfamic acid Chemical class NS(O)(=O)=O IIACRCGMVDHOTQ-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/576—Six-membered rings
- C07F9/59—Hydrogenated pyridine rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurosurgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
Reivindicación 1: Un compuesto caracterizado por la fórmula (1) en donde: Ar¹ es fenilo o indanilo y se sustituye con 0 - 3 sustituyentes seleccionados de ciano, halo, alquilo, haloalquilo y haloalcoxi; Ar² es fenilo sustituido con 1 sustituyente OR y también sustituido con 0 - 3 sustituyentes seleccionados de ciano, halo, alquilo, haloalquilo y haloalcoxi; R es una porción de profármaco seleccionada del grupo que consiste en alquilésteres, ésteres de aminoácidos, alcoxiésteres, ácidos fosfónicos, alquilésteres fosfónicos, alcoxifosfononato ácido, alquilésteres de alcoxifosfonato, alquilcarabamatos, carbamatos de aminoácidos, fosforamidatos de alquilo, fosforamidatos de arilo y sulfamatos; X es un enlace o C₁₋₃ alquileno; n es 1 ó 2; y el anillo A es azetidinilo, pirrolidinilo, piperidinilo, piperazinilo, homopiperidinilo u homopiperazinilo y se sustituye con 0 - 4 sustituyentes seleccionados de halo, alquilo, hidroxi o alcoxi; o una sal de aquel aceptable desde el punto de vista farmacéutico.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461925405P | 2014-01-09 | 2014-01-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR102019A1 true AR102019A1 (es) | 2017-02-01 |
Family
ID=52444626
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150100067A AR102019A1 (es) | 2014-01-09 | 2015-01-09 | (r)-3-((3s,4s)-3-fluoro-4-(4-hidroxifenil)piperidin-1-il)-1-(4-metilbencil)pirrolidin-2-ona y sus profármacos para el tratamiento de trastornos psiquiátricos |
Country Status (26)
| Country | Link |
|---|---|
| US (10) | US9187506B2 (es) |
| EP (2) | EP3092223B1 (es) |
| JP (1) | JP6629738B2 (es) |
| KR (1) | KR102331120B1 (es) |
| AR (1) | AR102019A1 (es) |
| AU (1) | AU2015204785A1 (es) |
| CA (1) | CA2936338A1 (es) |
| CL (1) | CL2016001744A1 (es) |
| CY (1) | CY1122768T1 (es) |
| DK (1) | DK3092223T3 (es) |
| EA (1) | EA201691133A1 (es) |
| ES (1) | ES2771825T3 (es) |
| HR (1) | HRP20200161T1 (es) |
| HU (1) | HUE048750T2 (es) |
| IL (1) | IL246596A0 (es) |
| LT (1) | LT3092223T (es) |
| MX (1) | MX2016008715A (es) |
| PE (1) | PE20160898A1 (es) |
| PL (1) | PL3092223T3 (es) |
| PT (1) | PT3092223T (es) |
| RS (1) | RS59858B1 (es) |
| SG (1) | SG11201605620QA (es) |
| SI (1) | SI3092223T1 (es) |
| TW (1) | TW201612169A (es) |
| UY (1) | UY35946A (es) |
| WO (1) | WO2015105929A1 (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9187506B2 (en) * | 2014-01-09 | 2015-11-17 | Bristol-Myers Squibb Company | (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one and its prodrugs for the treatment of psychiatric disorders |
| CA3001894A1 (en) * | 2015-10-14 | 2017-04-20 | Bristol-Myers Squibb Company | Selective nr2b antagonists |
| EP3362441B1 (en) | 2015-10-14 | 2020-08-12 | Bristol-Myers Squibb Company | Selective nr2b antagonists |
| US20210110275A1 (en) * | 2019-10-11 | 2021-04-15 | Royal Bank Of Canada | System and method of machine learning using embedding networks |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6476041B1 (en) | 1999-10-29 | 2002-11-05 | Merck & Co., Inc. | 1,4 substituted piperidinyl NMDA/NR2B antagonists |
| EA200200952A1 (ru) | 2000-04-26 | 2003-02-27 | Уорнер-Ламберт Компани | Производные циклогексиламина в качестве селективных антагонистов подтипов nmda-рецепторов |
| WO2003035641A1 (fr) | 2001-10-22 | 2003-05-01 | Shionogi & Co., Ltd. | Nouveau derive carbamoyl-pyrrolidone |
| CA2527093C (en) | 2003-06-04 | 2009-10-20 | Merck & Co., Inc. | 3-fluoro-piperidines as nmda/nr2b antagonists |
| EP1673367A1 (en) * | 2003-10-08 | 2006-06-28 | Pfizer, Inc. | Fused lactam compounds |
| WO2007099828A1 (ja) * | 2006-02-23 | 2007-09-07 | Shionogi & Co., Ltd. | 環式基で置換された含窒素複素環誘導体 |
| EP2170334B1 (en) | 2007-06-29 | 2021-03-17 | Emory University | Nmda receptor antagonists for neuroprotection |
| NZ585332A (en) * | 2007-11-13 | 2012-05-25 | Vertex Pharma | 4(-3-(-2-(phenyl)morpholino)-2-oxopyrrolidin-1-yl)-n-(thiazol-2-yl)benzenesulfonamide derivati ves and related compounds as modulators of ion channels for the treatment of pain |
| US9187506B2 (en) * | 2014-01-09 | 2015-11-17 | Bristol-Myers Squibb Company | (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one and its prodrugs for the treatment of psychiatric disorders |
-
2015
- 2015-01-07 US US14/591,372 patent/US9187506B2/en active Active
- 2015-01-08 WO PCT/US2015/010552 patent/WO2015105929A1/en active Application Filing
- 2015-01-08 MX MX2016008715A patent/MX2016008715A/es unknown
- 2015-01-08 TW TW104100590A patent/TW201612169A/zh unknown
- 2015-01-08 CA CA2936338A patent/CA2936338A1/en not_active Abandoned
- 2015-01-08 AU AU2015204785A patent/AU2015204785A1/en not_active Abandoned
- 2015-01-08 JP JP2016545818A patent/JP6629738B2/ja active Active
- 2015-01-08 SI SI201531064T patent/SI3092223T1/sl unknown
- 2015-01-08 PT PT157023128T patent/PT3092223T/pt unknown
- 2015-01-08 EP EP15702312.8A patent/EP3092223B1/en active Active
- 2015-01-08 KR KR1020167021355A patent/KR102331120B1/ko active IP Right Grant
- 2015-01-08 PE PE2016001105A patent/PE20160898A1/es unknown
- 2015-01-08 SG SG11201605620QA patent/SG11201605620QA/en unknown
- 2015-01-08 HU HUE15702312A patent/HUE048750T2/hu unknown
- 2015-01-08 ES ES15702312T patent/ES2771825T3/es active Active
- 2015-01-08 DK DK15702312.8T patent/DK3092223T3/da active
- 2015-01-08 EA EA201691133A patent/EA201691133A1/ru unknown
- 2015-01-08 LT LTEP15702312.8T patent/LT3092223T/lt unknown
- 2015-01-08 RS RS20200109A patent/RS59858B1/sr unknown
- 2015-01-08 EP EP19212924.5A patent/EP3677578A1/en not_active Withdrawn
- 2015-01-08 PL PL15702312T patent/PL3092223T3/pl unknown
- 2015-01-09 UY UY0001035946A patent/UY35946A/es unknown
- 2015-01-09 AR ARP150100067A patent/AR102019A1/es unknown
- 2015-10-13 US US14/881,932 patent/US20160030456A1/en not_active Abandoned
-
2016
- 2016-07-04 IL IL246596A patent/IL246596A0/en unknown
- 2016-07-07 CL CL2016001744A patent/CL2016001744A1/es unknown
- 2016-11-21 US US15/357,102 patent/US20170065573A1/en not_active Abandoned
-
2017
- 2017-04-18 US US15/490,558 patent/US20170216325A1/en not_active Abandoned
- 2017-08-17 US US15/679,847 patent/US20170340653A1/en not_active Abandoned
- 2017-12-19 US US15/846,914 patent/US20180104265A1/en not_active Abandoned
-
2018
- 2018-05-04 US US15/971,049 patent/US20180250316A1/en not_active Abandoned
- 2018-12-19 US US16/225,631 patent/US20190125770A1/en not_active Abandoned
-
2019
- 2019-06-27 US US16/454,843 patent/US20190314392A1/en not_active Abandoned
-
2020
- 2020-01-31 HR HRP20200161TT patent/HRP20200161T1/hr unknown
- 2020-01-31 US US16/778,960 patent/US20200297742A1/en not_active Abandoned
- 2020-02-07 CY CY20201100120T patent/CY1122768T1/el unknown
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| Date | Code | Title | Description |
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| FB | Suspension of granting procedure |