AR124662A2 - Formulaciones inmunosupresoras - Google Patents
Formulaciones inmunosupresorasInfo
- Publication number
- AR124662A2 AR124662A2 ARP220100086A ARP220100086A AR124662A2 AR 124662 A2 AR124662 A2 AR 124662A2 AR P220100086 A ARP220100086 A AR P220100086A AR P220100086 A ARP220100086 A AR P220100086A AR 124662 A2 AR124662 A2 AR 124662A2
- Authority
- AR
- Argentina
- Prior art keywords
- carbon atoms
- alkyl
- halogen
- substituted
- cycloalkyl
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title abstract 3
- 229960003444 immunosuppressant agent Drugs 0.000 title 1
- 230000001861 immunosuppressant effect Effects 0.000 title 1
- 239000003018 immunosuppressive agent Substances 0.000 title 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 18
- 239000008186 active pharmaceutical agent Substances 0.000 abstract 10
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 229910052736 halogen Inorganic materials 0.000 abstract 9
- 150000002367 halogens Chemical class 0.000 abstract 9
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 229910052799 carbon Inorganic materials 0.000 abstract 5
- 150000003839 salts Chemical class 0.000 abstract 5
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 3
- 239000002253 acid Substances 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 3
- -1 1H -tetrazol-5-yl Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 150000007514 bases Chemical class 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 239000007790 solid phase Substances 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- KIHYPELVXPAIDH-UHFFFAOYSA-N 1-[[4-[n-[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]-c-methylcarbonimidoyl]-2-ethylphenyl]methyl]azetidine-3-carboxylic acid Chemical compound CCC1=CC(C(C)=NOCC=2C=C(C(C3CCCCC3)=CC=2)C(F)(F)F)=CC=C1CN1CC(C(O)=O)C1 KIHYPELVXPAIDH-UHFFFAOYSA-N 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004450 alkenylene group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000002245 particle Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- 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
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Transplantation (AREA)
- Physical Education & Sports Medicine (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Communicable Diseases (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Abstract
La presente invención se refiere a una composición farmacéutica en fase sólida, la cual comprende uno o más excipientes farmacéuticamente aceptables, y un ingrediente farmacéutico activo (API), el cual es un compuesto de la fórmula (1) o (2), o una sal, solvato o hidrato farmacológicamente aceptable del mismo, en donde el ingrediente farmacéutico activo (API) no se expone a un compuesto básico. Reivindicación 1: Una composición farmacéutica en fase sólida, la cual comprende uno o más excipientes farmacéuticamente aceptables, y un ingrediente farmacéutico activo (API), el cual es un compuesto de la fórmula (1) o (2), o una sal, solvato o hidrato farmacológicamente aceptable del mismo, en donde el ingrediente farmacéutico activo (API) no se expone a un compuesto básico, en donde: A es COOR⁵, OPO(OR⁵)₂, PO(OR⁵)₂, SO₂OR⁵, POR⁵OR⁵ ó 1H-tetrazol-5-ilo, en donde R⁵ es H o un grupo formador de éster; W es un enlace, alquileno de 1 a 3 átomos de carbono, o alquenileno de 2 a 3 átomos de carbono; Y es arilo de 6 a 10 átomos de carbono, o heteroarilo de 3 a 9 átomos de carbono opcionalmente sustituido por 1 a 3 radicales seleccionados a partir de halógeno, NO₂, alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono; alquilo de 1 a 6 átomos de carbono sustituido por halógeno, y alcoxilo de 1 a 6 átomos de carbono sustituido por halógeno; Z se selecciona a partir de: los compuestos del grupo de fórmulas (3); en donde los asteriscos de Z indican el punto de unión entre -C(R³)-(R⁴)- y A de la fórmula (1) o (2), respectivamente; R⁶ se selecciona a partir de hidrógeno y alquilo de 1 a 6 átomos de carbono; y J¹ y J² son independientemente metileno o un heteroátomo seleccionado a partir de S, O y NR⁵; en donde R⁵ se selecciona a partir de hidrógeno y alquilo de 1 a 6 átomos de carbono; y cualquier alquileno de Z puede estar adicionalmente sustituido por uno a tres radicales seleccionados a partir de halógeno, hidroxilo, alquilo de 1 a 6 átomos de carbono; o R⁶ se puede unir a un átomo de carbono de Y para formar un anillo de 5 a 7 miembros; R¹ es arilo de 6 a 10 átomos de carbono, o heteroarilo de 3 a 9 átomos de carbono opcionalmente sustituido por alquilo de 1 a 6 átomos de carbono, arilo de 6 a 10 átomos de carbono, arilo de 6 a 10 átomos de carbono-alquilo de 1 a 4 átomos de carbono, heteroarilo de 3 a 9 átomos de carbono, heteroarilo de 3 a 9 átomos de carbono-alquilo de 1 a 4 átomos de carbono, cicloalquilo de 3 a 8 átomos de carbono, cicloalquilo de 3 a 8 átomos de carbono-alquilo de 1 a 4 átomos de carbono, hetero-cicloalquilo de 3 a 8 átomos de carbono, o hetero-cicloalquilo de 3 a 8 átomos de carbono-alquilo de 1 a 4 átomos de carbono; en donde cualquier arilo, heteroarilo, cicloalquilo o hetero-cicloalquilo de R¹ puede estar sustituido por 1 a 5 grupos seleccionados a partir de halógeno, alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono, y alquilo de 1 a 6 átomos de carbono o alcoxilo de 1 a 6 átomos de carbono sustituido por halógeno; R² es H, alquilo de 1 a 6 átomos de carbono, alquilo de 1 a 6 átomos de carbono sustituido por halógeno, alquenilo de 2 a 6 átomos de carbono, o alquinilo de 2 a 6 átomos de carbono; y cada uno de R³ ó R⁴ es independientemente H, halógeno, OH, alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono, o alquilo de 1 a 6 átomos de carbono o alcoxilo de 1 a 6 átomos de carbono sustituido por halógeno. Reivindicación 3: Una composición de la reivindicación 1, en donde el ingrediente farmacéutico activo (API) es el ácido 1-{4-[1-(4-ciclohexil-3-trifluoro-metil-benciloxi-imino)-etil]-2-etil-bencil}-azetidin-3-carboxílico, o una sal farmacéuticamente aceptable. Reivindicación 10: Una tableta que comprende una mezcla comprimida que consiste en ácido 1-{4-[1-(4-ciclohexil-3-trifluoro-metil-benciloxi-imino)-etil]-2-etil-bencil}-azetidin-3-carboxílico, o una sal farmacéuticamente aceptable del mismo, y uno o más excipientes no básicos, estando el ácido 1-{4-[1-(4-ciclohexil-3-trifluoro-metil-benciloxi-imino)-etil]-2-etil-bencil}-azetidin-3-carboxílico, o una sal farmacéuticamente aceptable, en la forma de partículas que tienen un diámetro X₉₀ de 10 micras a 200 micras.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11150431 | 2011-01-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR124662A2 true AR124662A2 (es) | 2023-04-19 |
Family
ID=44022942
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120100047A AR084801A1 (es) | 2011-01-07 | 2012-01-06 | Formulaciones inmunosupresoras |
| ARP220100086A AR124662A2 (es) | 2011-01-07 | 2022-01-17 | Formulaciones inmunosupresoras |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120100047A AR084801A1 (es) | 2011-01-07 | 2012-01-06 | Formulaciones inmunosupresoras |
Country Status (36)
| Country | Link |
|---|---|
| US (4) | US20130273161A1 (es) |
| EP (2) | EP2661261B1 (es) |
| JP (2) | JP6111202B2 (es) |
| KR (2) | KR102166885B1 (es) |
| CN (1) | CN103458877B (es) |
| AR (2) | AR084801A1 (es) |
| AU (1) | AU2012204835B2 (es) |
| BR (1) | BR112013017302B1 (es) |
| CA (1) | CA2823616C (es) |
| CL (1) | CL2013001979A1 (es) |
| CO (1) | CO6761402A2 (es) |
| CY (1) | CY1122182T1 (es) |
| DK (1) | DK2661261T3 (es) |
| EA (1) | EA026144B9 (es) |
| EC (1) | ECSP13012812A (es) |
| ES (1) | ES2751920T3 (es) |
| GT (1) | GT201300178A (es) |
| HR (1) | HRP20191842T1 (es) |
| HU (1) | HUE045612T2 (es) |
| IL (1) | IL227094B (es) |
| JO (1) | JO3619B1 (es) |
| LT (1) | LT2661261T (es) |
| MA (1) | MA34897B1 (es) |
| MX (2) | MX371290B (es) |
| MY (1) | MY161162A (es) |
| PE (1) | PE20140216A1 (es) |
| PH (1) | PH12013501442B1 (es) |
| PL (1) | PL2661261T3 (es) |
| PT (1) | PT2661261T (es) |
| SG (1) | SG191286A1 (es) |
| SI (1) | SI2661261T1 (es) |
| TN (1) | TN2013000257A1 (es) |
| TW (2) | TWI583380B (es) |
| UA (1) | UA114283C2 (es) |
| WO (1) | WO2012093161A1 (es) |
| ZA (1) | ZA201304465B (es) |
Families Citing this family (14)
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|---|---|---|---|---|
| PH12013501442B1 (en) | 2011-01-07 | 2018-04-20 | Novartis Ag | Immunosuppressant formulations |
| EP3129006B1 (en) * | 2014-04-10 | 2021-01-27 | Novartis AG | Immunosuppressant formulation |
| EP4074312B1 (en) * | 2014-04-10 | 2026-02-25 | Novartis AG | Siponimod immediate release dosage regimen for treating autoimmune diseases |
| US20180042895A1 (en) | 2015-02-26 | 2018-02-15 | Novartis Ag | Treatment of autoimmune disease in a patient receiving additionally a beta-blocker |
| SI3318259T1 (sl) * | 2015-07-03 | 2023-06-30 | Astellas Pharma Inc. | Stabilni farmacevtski sestavki za oralno dajanje |
| US11629124B2 (en) | 2017-03-09 | 2023-04-18 | Novartis Ag | Solid forms comprising an oxime ether compound, compositions and methods of use thereof |
| US11434200B2 (en) | 2017-03-09 | 2022-09-06 | Novartis Ag | Solid forms comprising an oxime ether compound and a coformer, compositions and methods of use thereof |
| AU2018341136A1 (en) | 2017-09-27 | 2020-03-12 | Novartis Ag | Parenteral formulation comprising siponimod |
| EP3687530A1 (en) | 2017-09-29 | 2020-08-05 | Novartis AG | Dosing regimen of siponimod |
| RU2020114751A (ru) | 2017-09-29 | 2021-10-29 | Новартис Аг | Схема введения доз сипонимода |
| CN109908095A (zh) * | 2019-04-08 | 2019-06-21 | 肇庆学院 | 一种西尼莫德片剂及制备方法 |
| WO2021214717A1 (en) | 2020-04-23 | 2021-10-28 | Novartis Ag | Dosing regimen for the use of siponimod for the treatment of acute respiratory distress syndrome |
| EP4489787A1 (en) * | 2022-03-09 | 2025-01-15 | ISP Investments LLC | Co-processed excipient composition |
| WO2024126409A1 (en) | 2022-12-12 | 2024-06-20 | Synthon B.V. | Pharmaceutical composition of siponimod |
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| ES2478842T3 (es) | 2008-12-18 | 2014-07-23 | Novartis Ag | Sal clorhidrato del ácido 1-(4-(1-((E)-4-ciclohexil-3-trifluorometil-benziloxiimino)-etil)-2-etil-benzil)-azetidina-3-carboxílico |
| KR20160064245A (ko) * | 2008-12-18 | 2016-06-07 | 노파르티스 아게 | 1-［4-［1-(4-시클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸］-2-에틸-벤질］-아제티딘-3-카르복실산의 헤미푸마레이트 염 |
| MX2011006610A (es) | 2008-12-18 | 2011-06-30 | Novartis Ag | Nueva forma polimorfica de acido 1-(4-{l-[(e)-4-ciclohexil-3 -trifluorometil-benciloxi-imino]-etil)-2-etil-bencil)-azetidin-3 carboxilico. |
| US20110247617A1 (en) | 2008-12-19 | 2011-10-13 | Thomas Nilsson | Mouthpiece for an inhaler |
| CA2747992C (en) | 2008-12-22 | 2017-11-07 | Novartis Ag | Dosage regimen of an s1p receptor agonist |
| AR074826A1 (es) | 2008-12-22 | 2011-02-16 | Novartis Ag | Regimen de dosificacion para un agonista de los receptores de s1p |
| AU2010300919A1 (en) | 2009-09-29 | 2012-03-22 | Novartis Ag | Dosage regimen of an S1P receptor modulator |
| PH12013501442B1 (en) | 2011-01-07 | 2018-04-20 | Novartis Ag | Immunosuppressant formulations |
| WO2012095853A1 (en) | 2011-01-10 | 2012-07-19 | Novartis Pharma Ag | Modified release formulations comprising sip receptor modulators |
| TW201320994A (zh) | 2011-10-11 | 2013-06-01 | Novartis Ag | 投藥療程 |
| EP3199947A3 (en) | 2013-04-04 | 2017-09-13 | Novartis AG | Identifying patient response to s1p receptor modulator administration |
| EP3129006B1 (en) | 2014-04-10 | 2021-01-27 | Novartis AG | Immunosuppressant formulation |
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