ES2659397T3 - 2-azabicíclicos sustituidos y su uso como moduladores receptores de orexinas - Google Patents
2-azabicíclicos sustituidos y su uso como moduladores receptores de orexinas Download PDFInfo
- Publication number
- ES2659397T3 ES2659397T3 ES14717576.4T ES14717576T ES2659397T3 ES 2659397 T3 ES2659397 T3 ES 2659397T3 ES 14717576 T ES14717576 T ES 14717576T ES 2659397 T3 ES2659397 T3 ES 2659397T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- pyridyl
- oxadiazolyl
- pyridazinyl
- pyrimidinyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
Classifications
-
- 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
-
- 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
- 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
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/4709—Non-condensed quinolines 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
- A61K31/435—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
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
- A61K31/4965—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
- C07D471/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Un compuesto de fórmula I**Fórmula** o un enantiómero, diastereómero, tautómero o variante isotópica de los mismos; o una sal o solvato farmacéuticamente aceptable del mismo; donde X es N o CR1; Y es N o CR2; R1 es H, alcoxi, halo, triazolilo, tiazolilo, piridazinilo, pirimidinilo, oxazolilo, isoxazolilo, oxadiazolilo, piridilo, fenilo o pirazolilo, en donde triazolilo, tiazolilo, piridazinilo, pirimidinilo, oxazolilo, isoxazolilo, oxadiazolilo, piridilo, fenilo o pirazolilo está opcionalmente sustituido con hasta dos sustituyentes seleccionados de entre el grupo constituido por halo y alquilo; R2 es H, alquilo, alcoxi, o halo; Z es NH, N-CH3, N-CH2CH3, N-CH2-ciclopropilo, NC(>=O)CH3, N-CH2CH2OCH3 o O; R3 es H, alquilo, alcoxi, halo, triazolilo, tiazolilo, piridazinilo, pirimidinilo, oxazolilo, isoxazolilo, oxadiazolilo, piridilo, fenilo o pirazolilo, en donde triazolilo, tiazolilo, piridazinilo, pirimidinilo, oxazolilo, isoxazolilo, oxadiazolilo, piridilo, fenilo o pirazolilo está opcionalmente sustituido con hasta dos sustituyentes seleccionados de entre el grupo constituido por halo y alquilo; R4 es H o alquilo; o R3 y R4, junto con los átomos a los que están unidos, forman un anillo arilo de 6 miembros o un anillo heteroarilo de 5 ó 6 miembros; R5 es fenilo, piridilo, pirazinilo, benzoxazolilo, piridazinilo, naftiridinilo o pirimidinilo, en el que el piridilo, pirazinilo, benzoxazolilo, piridazinilo, naftiridinilo o pirimidinilo está opcionalmente sustituido con hasta dos grupos seleccionados de entre el grupo constituido por halo, alcoxi, hidroximetilo y alquilo; y n es 1 o 2, en donde "alquilo" es un grupo de cadena lineal o ramificada de alquilo que tiene de 1 a 12 átomos de carbono en la cadena o un grupo hidrocarburo mono-cíclico no aromático que tiene de 3 a 7 átomos de carbono y está opcionalmente sustituido con uno o más átomos de halógeno.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361780378P | 2013-03-13 | 2013-03-13 | |
| US201361780378P | 2013-03-13 | ||
| PCT/US2014/024293 WO2014165070A1 (en) | 2013-03-13 | 2014-03-12 | Substituted 2-azabicycles and their use as orexin receptor modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2659397T3 true ES2659397T3 (es) | 2018-03-15 |
Family
ID=50487148
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES19193122T Active ES2950032T3 (es) | 2013-03-13 | 2014-03-12 | 2-Azabiciclos sustituidos y su uso como moduladores del receptor de orexina |
| ES14717576.4T Active ES2659397T3 (es) | 2013-03-13 | 2014-03-12 | 2-azabicíclicos sustituidos y su uso como moduladores receptores de orexinas |
| ES17206491T Active ES2760564T3 (es) | 2013-03-13 | 2014-03-12 | 2-azabicíclicos sustituidos y su uso como moduladores receptores de orexinas |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES19193122T Active ES2950032T3 (es) | 2013-03-13 | 2014-03-12 | 2-Azabiciclos sustituidos y su uso como moduladores del receptor de orexina |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES17206491T Active ES2760564T3 (es) | 2013-03-13 | 2014-03-12 | 2-azabicíclicos sustituidos y su uso como moduladores receptores de orexinas |
Country Status (38)
| Country | Link |
|---|---|
| US (5) | US9611277B2 (es) |
| EP (4) | EP3363438B1 (es) |
| JP (1) | JP6275815B2 (es) |
| KR (1) | KR102209424B1 (es) |
| CN (3) | CN108864093A (es) |
| AR (1) | AR095423A1 (es) |
| AU (2) | AU2014248680B2 (es) |
| BR (1) | BR112015022294B1 (es) |
| CA (1) | CA2904618C (es) |
| CL (1) | CL2015002609A1 (es) |
| CR (2) | CR20210523A (es) |
| CY (3) | CY1120024T1 (es) |
| DK (2) | DK2970314T3 (es) |
| EA (1) | EA029276B1 (es) |
| ES (3) | ES2950032T3 (es) |
| HR (3) | HRP20180303T1 (es) |
| HU (3) | HUE036193T2 (es) |
| IL (2) | IL240466B (es) |
| JO (1) | JOP20140092B1 (es) |
| LT (2) | LT2970314T (es) |
| ME (2) | ME03011B (es) |
| MX (2) | MX368466B (es) |
| MY (1) | MY183725A (es) |
| NI (1) | NI201500130A (es) |
| NO (1) | NO3107630T3 (es) |
| PE (1) | PE20151599A1 (es) |
| PH (1) | PH12015501929B1 (es) |
| PL (3) | PL3363438T3 (es) |
| PT (2) | PT3363438T (es) |
| RS (3) | RS56875B1 (es) |
| SG (1) | SG11201507415QA (es) |
| SI (2) | SI3363438T1 (es) |
| SM (3) | SMT201800056T1 (es) |
| TW (1) | TWI621618B (es) |
| UA (1) | UA118669C2 (es) |
| UY (1) | UY35409A (es) |
| WO (1) | WO2014165070A1 (es) |
| ZA (1) | ZA201507562B (es) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2585806T3 (es) | 2009-10-23 | 2016-10-10 | Janssen Pharmaceutica N.V. | Octahidropirrolo [3,4-c] pirroles disustituidos como moduladores de receptores de orexina |
| EP2937345B1 (en) | 2009-12-29 | 2018-03-21 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| WO2013074986A1 (en) | 2011-11-17 | 2013-05-23 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
| TW201444849A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途 |
| TWI621618B (zh) * | 2013-03-13 | 2018-04-21 | 比利時商健生藥品公司 | 經取代2-氮雜雙環類及其作為食慾素受體調控劑之用途 |
| TW201444821A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代之哌啶化合物及其作為食慾素受體調節劑之用途 |
| JP6262885B2 (ja) * | 2014-03-06 | 2018-01-17 | シャンハイ ハイヤン ファーマシューティカル テクノロジー カンパニー リミテッドShanghai Haiyan Pharmaceutical Technology Co., Ltd. | オレキシン受容体拮抗剤としてのピペリジン誘導体 |
| AU2015314851B2 (en) * | 2014-09-11 | 2020-01-02 | Janssen Pharmaceutica Nv | Substituted 2-azabicycles and their use as orexin receptor modulators |
| US9938276B2 (en) * | 2014-12-19 | 2018-04-10 | Merck Sharp & Dohme Corp. | 6,5-bicyclic octahydropyrrolopyridine orexin receptor antagonists |
| AU2015371251B2 (en) | 2014-12-23 | 2020-06-11 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| CN107427521B (zh) | 2015-03-27 | 2021-08-03 | 达纳-法伯癌症研究所股份有限公司 | 细胞周期蛋白依赖性激酶的抑制剂 |
| WO2017012502A1 (en) | 2015-07-17 | 2017-01-26 | Sunshine Lake Pharma Co., Ltd. | Substituted quinazoline compounds and preparation and uses thereof |
| WO2017028732A1 (zh) * | 2015-08-14 | 2017-02-23 | 上海海雁医药科技有限公司 | 食欲素受体拮抗剂化合物的晶型及其制备方法和应用 |
| JP7028766B2 (ja) | 2015-09-09 | 2022-03-02 | ダナ-ファーバー キャンサー インスティテュート, インコーポレイテッド | サイクリン依存性キナーゼの阻害剤 |
| SG11201804223TA (en) | 2015-11-23 | 2018-06-28 | Sunshine Lake Pharma Co Ltd | OCTAHYDROPYRROLO [3, 4-c] PYRROLE DERIVATIVES AND USES THEREOF |
| HRP20220642T1 (hr) | 2016-03-10 | 2022-06-24 | Janssen Pharmaceutica Nv | Postupci za liječenje depresije uporabom antagonista receptora oreksina 2 |
| CA3252823A1 (en) | 2016-06-13 | 2025-02-25 | Gilead Sciences, Inc. | Substituted tert-butyl-3-(2-chloro-phenyl)-3-hydroxyazetidine-1-carboxylate compounds |
| BR112018075734A2 (pt) | 2016-06-13 | 2019-04-02 | Gilead Sciences, Inc. | composto, composição farmacêutica, método para tratar um paciente com uma doença ou condição mediada pelo menos em parte por fxr, e, uso de um composto. |
| EP3544971B1 (en) | 2016-11-22 | 2022-07-06 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 12 (cdk12) and uses thereof |
| CN110461328A (zh) | 2017-03-28 | 2019-11-15 | 吉利德科学公司 | 治疗肝疾病的治疗组合 |
| GB2558975B (en) * | 2017-09-01 | 2019-01-23 | Chronos Therapeutics Ltd | Substituted 2-azabicyclo[3.1.1]heptane and 2-azabicyclo[3.2.1]octane derivatives as orexin receptor antagonists |
| EP3676261B1 (en) * | 2017-09-01 | 2024-12-18 | Chronos Therapeutics Limited | Substituted 2-azabicyclo[3.1.1]heptane and 2-azabicyclo[3.2.1]octane derivatives as orexin receptor antagonists |
| JP7590185B2 (ja) | 2018-06-25 | 2024-11-26 | ダナ-ファーバー キャンサー インスティテュート, インコーポレイテッド | Taireファミリーキナーゼインヒビターおよびそれらの使用 |
| AU2019395255B2 (en) * | 2018-12-14 | 2025-02-27 | Dana-Farber Cancer Institute, Inc. | Pyrazolopyridine inhibitors of c-Jun-N-terminal kinases and uses thereof |
| WO2020140098A1 (en) | 2018-12-28 | 2020-07-02 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 and uses thereof |
| EP4360632B1 (en) | 2019-01-15 | 2025-10-29 | Gilead Sciences, Inc. | Fxr (nr1h4) modulating compounds |
| US11524005B2 (en) | 2019-02-19 | 2022-12-13 | Gilead Sciences, Inc. | Solid forms of FXR agonists |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3674793A (en) | 1967-03-29 | 1972-07-04 | Sterling Drug Inc | 6-hydroxy-2-azabicyclo(2.2.2)octan-3-ones and 2-azabicyclo(2.2.2.)octane-3,6-diones |
| US6505492B2 (en) | 2001-04-11 | 2003-01-14 | Bethlehem Steel Corporation | Method and apparatus for forming deep-drawn articles |
| EP1396488A1 (en) | 2001-05-23 | 2004-03-10 | Mitsubishi Pharma Corporation | Fused heterocyclic compound and medicinal use thereof |
| WO2004069816A1 (en) | 2003-02-07 | 2004-08-19 | Ranbaxy Laboratories Limited | Oxazolidinone derivatives as antimicrobials |
| BRPI0407714A (pt) | 2003-02-21 | 2006-02-14 | Pharmacia & Up John Company Ll | "exo-2r (+)-2-amino-7-azabiciclo[2.2.1]heptano-7-carboxilato de t-butila, intermediário, e processo para os preparar e isolar |
| AR058554A1 (es) | 2005-12-20 | 2008-02-13 | Novartis Ag | Compuestos heterociclicos nitrogenados de 6 miembros sustituidos, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades mediadas por mglur5. |
| EP2272509A1 (en) | 2006-09-11 | 2011-01-12 | Novartis AG | New Uses of metabotropic glutamate receptors |
| US8133901B2 (en) | 2006-12-01 | 2012-03-13 | Actelion Pharmaceuticals Ltd. | 3-heteroaryl (amino or amido)-1-(biphenyl or phenylthiazolyl) carbonylpiperidine derivatives as orexin receptor inhibitors |
| TW200833328A (en) | 2006-12-28 | 2008-08-16 | Actelion Pharmaceuticals Ltd | 2-aza-bicyclo[3.1.0]hexane derivatives |
| US8030495B2 (en) | 2007-05-23 | 2011-10-04 | Coleman Paul J | Cyclopropyl pyrrolidine orexin receptor antagonists |
| TW200904440A (en) | 2007-07-17 | 2009-02-01 | Bristol Myers Squibb Co | Method for modulating GPR119 G protein-coupled receptor and selected compounds |
| CA2705411A1 (en) | 2007-12-21 | 2009-07-02 | F. Hoffmann-La Roche Ag | Heteroaryl derivatives as orexin receptor antagonists |
| BRPI0908096A2 (pt) * | 2008-02-21 | 2015-08-25 | Actelion Pharmaceuticals Ltd | Derivado de 2-aza-biciclo [2.2.1] heptano |
| CN102015645B (zh) | 2008-04-30 | 2012-11-14 | 埃科特莱茵药品有限公司 | 哌啶和吡咯烷化合物 |
| MX2011000664A (es) | 2008-07-16 | 2011-02-24 | Schering Corp | Derivados biciclicos heterociclicos y uso de los mismos como moduladores de gpr119. |
| WO2010048016A1 (en) | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,3-disubstituted piperidine orexin receptor antagonists |
| JP2012506375A (ja) | 2008-10-21 | 2012-03-15 | メルク・シャープ・エンド・ドーム・コーポレイション | 2,5−二置換ピペリジンオレキシン受容体アンタゴニスト |
| CA2745433A1 (en) | 2008-12-02 | 2010-06-10 | Glaxo Group Ltd. | N-{[(ir,4s,6r-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0]hept-4-yl] methyl}-2-heteroarylamine derivatives and uses thereof |
| AR076024A1 (es) | 2009-04-03 | 2011-05-11 | Schering Corp | Derivados de heterociclos biciclicos puenteados y metodos de uso de los mismos |
| US20120040991A1 (en) | 2009-04-24 | 2012-02-16 | Glaxo Group Limited | 3-azabicyclo [4.1.0] heptanes used as orexin antagonists |
| WO2011050202A1 (en) | 2009-10-23 | 2011-04-28 | Janssen Pharmaceutica Nv | Fused heterocyclic compounds as orexin receptor modulators |
| EP2491034B1 (en) | 2009-10-23 | 2013-12-18 | Janssen Pharmaceutica, N.V. | Fused heterocyclic compounds as orexin receptor modulators |
| ES2585806T3 (es) | 2009-10-23 | 2016-10-10 | Janssen Pharmaceutica N.V. | Octahidropirrolo [3,4-c] pirroles disustituidos como moduladores de receptores de orexina |
| CA2778684A1 (en) | 2009-10-29 | 2011-05-05 | Schering Corporation | Bridged bicyclic piperidine derivatives and methods of use thereof |
| WO2011066137A1 (en) | 2009-11-24 | 2011-06-03 | Schering Corporation | Substituted biaryl derivatives and methods of use thereof |
| AU2010332010A1 (en) | 2009-12-14 | 2012-08-02 | Inspire Pharmaceuticals, Inc. | Bridged bicyclic Rho kinase inhibitor compounds, composition and use |
| WO2011087812A1 (en) | 2009-12-21 | 2011-07-21 | Vanderbilt University | Alkyl 3-((2-amidoethyl)amino)-8-azabicyclo[3.2.1]octane-8-carboxylate analogs as selective m1 agonists and methods of making and using same |
| UY33227A (es) | 2010-02-19 | 2011-09-30 | Novartis Ag | Compuestos de pirrolopirimidina como inhibidores de la cdk4/6 |
| US20130096141A1 (en) | 2010-06-18 | 2013-04-18 | Bernard R. Neustadt | Bicyclic heterocycle derivatives and methods of use thereof |
| WO2012089606A1 (en) | 2010-12-28 | 2012-07-05 | Glaxo Group Limited | Azabicyclo [4.1.0] hept - 4 - yl derivatives as human orexin receptor antagonists |
| WO2012145581A1 (en) | 2011-04-20 | 2012-10-26 | Janssen Pharmaceutica Nv | Disubstituted octahy-dropyrrolo [3,4-c] pyrroles as orexin receptor modulators |
| AR088352A1 (es) | 2011-10-19 | 2014-05-28 | Merck Sharp & Dohme | Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina |
| WO2014066196A1 (en) | 2012-10-23 | 2014-05-01 | Merck Sharp & Dohme Corp. | 2-pyridyloxy-3-substituted-4-nitrile orexin receptor antagonists |
| MX2015006191A (es) | 2012-11-16 | 2015-08-10 | Merck Sharp & Dohme | Inhibidores de purina de fosfatidilinositol 3-quinasa delta humana. |
| TW201444849A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途 |
| TWI621618B (zh) | 2013-03-13 | 2018-04-21 | 比利時商健生藥品公司 | 經取代2-氮雜雙環類及其作為食慾素受體調控劑之用途 |
| JP6532474B2 (ja) | 2014-02-06 | 2019-06-19 | アッヴィ・インコーポレイテッド | 6−ヘテロアリールオキシ−および6−アリールオキシ−キノリン−2−カルボキシアミドならびにその使用 |
| AU2015314851B2 (en) | 2014-09-11 | 2020-01-02 | Janssen Pharmaceutica Nv | Substituted 2-azabicycles and their use as orexin receptor modulators |
-
2014
- 2014-03-11 TW TW103108293A patent/TWI621618B/zh not_active IP Right Cessation
- 2014-03-12 SM SM20180056T patent/SMT201800056T1/it unknown
- 2014-03-12 EP EP17206491.7A patent/EP3363438B1/en active Active
- 2014-03-12 BR BR112015022294-3A patent/BR112015022294B1/pt active IP Right Grant
- 2014-03-12 PL PL17206491T patent/PL3363438T3/pl unknown
- 2014-03-12 MX MX2018015165A patent/MX368466B/es unknown
- 2014-03-12 AU AU2014248680A patent/AU2014248680B2/en active Active
- 2014-03-12 PL PL19193122.9T patent/PL3622956T3/pl unknown
- 2014-03-12 PL PL14717576T patent/PL2970314T3/pl unknown
- 2014-03-12 ME MEP-2018-46A patent/ME03011B/me unknown
- 2014-03-12 SM SM20190655T patent/SMT201900655T1/it unknown
- 2014-03-12 EA EA201591703A patent/EA029276B1/ru unknown
- 2014-03-12 JO JOP/2014/0092A patent/JOP20140092B1/ar active
- 2014-03-12 ES ES19193122T patent/ES2950032T3/es active Active
- 2014-03-12 LT LTEP14717576.4T patent/LT2970314T/lt unknown
- 2014-03-12 PT PT172064917T patent/PT3363438T/pt unknown
- 2014-03-12 EP EP23176328.5A patent/EP4272824A3/en not_active Withdrawn
- 2014-03-12 MY MYPI2015703021A patent/MY183725A/en unknown
- 2014-03-12 LT LT17206491T patent/LT3363438T/lt unknown
- 2014-03-12 HU HUE14717576A patent/HUE036193T2/hu unknown
- 2014-03-12 MX MX2015011815A patent/MX361529B/es active IP Right Grant
- 2014-03-12 ES ES14717576.4T patent/ES2659397T3/es active Active
- 2014-03-12 HR HRP20180303TT patent/HRP20180303T1/hr unknown
- 2014-03-12 SG SG11201507415QA patent/SG11201507415QA/en unknown
- 2014-03-12 CN CN201810842686.7A patent/CN108864093A/zh active Pending
- 2014-03-12 EP EP19193122.9A patent/EP3622956B9/en active Active
- 2014-03-12 CR CR20210523A patent/CR20210523A/es unknown
- 2014-03-12 CN CN201910948604.1A patent/CN110669052B/zh active Active
- 2014-03-12 CA CA2904618A patent/CA2904618C/en active Active
- 2014-03-12 RS RS20180158A patent/RS56875B1/sr unknown
- 2014-03-12 WO PCT/US2014/024293 patent/WO2014165070A1/en not_active Ceased
- 2014-03-12 ES ES17206491T patent/ES2760564T3/es active Active
- 2014-03-12 PT PT147175764T patent/PT2970314T/pt unknown
- 2014-03-12 CN CN201480027437.2A patent/CN105308048B/zh active Active
- 2014-03-12 RS RS20230703A patent/RS64551B9/sr unknown
- 2014-03-12 DK DK14717576.4T patent/DK2970314T3/en active
- 2014-03-12 US US14/774,555 patent/US9611277B2/en active Active
- 2014-03-12 JP JP2016501487A patent/JP6275815B2/ja active Active
- 2014-03-12 SI SI201431351T patent/SI3363438T1/sl unknown
- 2014-03-12 SM SM20230223T patent/SMT202300223T1/it unknown
- 2014-03-12 EP EP14717576.4A patent/EP2970314B1/en active Active
- 2014-03-12 UA UAA201509932A patent/UA118669C2/uk unknown
- 2014-03-12 HU HUE19193122A patent/HUE063608T2/hu unknown
- 2014-03-12 PE PE2015001954A patent/PE20151599A1/es active IP Right Grant
- 2014-03-12 US US14/206,722 patent/US8969352B2/en active Active
- 2014-03-12 KR KR1020157028720A patent/KR102209424B1/ko not_active Expired - Fee Related
- 2014-03-12 HU HUE17206491A patent/HUE047592T2/hu unknown
- 2014-03-12 DK DK17206491T patent/DK3363438T3/da active
- 2014-03-12 ME MEP-2019-314A patent/ME03572B/me unknown
- 2014-03-12 HR HRP20230633TT patent/HRP20230633T1/hr unknown
- 2014-03-12 RS RSP20191419 patent/RS59466B1/sr unknown
- 2014-03-12 SI SI201430542T patent/SI2970314T1/en unknown
- 2014-03-13 AR ARP140100967A patent/AR095423A1/es active IP Right Grant
- 2014-03-13 UY UY0001035409A patent/UY35409A/es not_active Application Discontinuation
- 2014-11-19 NO NO14808529A patent/NO3107630T3/no unknown
-
2015
- 2015-01-26 US US14/605,387 patent/US9447117B2/en active Active
- 2015-08-10 IL IL240466A patent/IL240466B/en active IP Right Grant
- 2015-08-24 CR CR20150433A patent/CR20150433A/es unknown
- 2015-09-02 PH PH12015501929A patent/PH12015501929B1/en unknown
- 2015-09-10 NI NI201500130A patent/NI201500130A/es unknown
- 2015-09-11 CL CL2015002609A patent/CL2015002609A1/es unknown
- 2015-10-12 ZA ZA2015/07562A patent/ZA201507562B/en unknown
-
2016
- 2016-08-26 US US15/248,945 patent/US9845333B2/en active Active
-
2017
- 2017-04-04 US US15/478,888 patent/US10183953B2/en active Active
-
2018
- 2018-03-09 CY CY20181100284T patent/CY1120024T1/el unknown
- 2018-07-03 AU AU2018204835A patent/AU2018204835B2/en active Active
-
2019
- 2019-02-03 IL IL264606A patent/IL264606A/en unknown
- 2019-11-08 HR HRP20192032TT patent/HRP20192032T1/hr unknown
- 2019-12-02 CY CY20191101261T patent/CY1122392T1/el unknown
-
2023
- 2023-07-25 CY CY20231100361T patent/CY1126106T1/el unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| NI201500130A (es) | 2-azabiciclo sustituidos y su uso como moduladores del receptor de orexina | |
| AR115662A2 (es) | Derivados de piperidina | |
| ES2659222T3 (es) | 7-azabicíclicos sustituidos y su uso para moduladores de receptores de orexina | |
| AR095422A1 (es) | Compuestos de piperidina sustituidos y su uso como moduladores de receptores de orexina | |
| ES2635318T3 (es) | Moduladores P2X7 | |
| CR20160548A (es) | Nuevos Derivados de Pirazolo Pirimidina y su Uso como Inhibidores de MALT1 | |
| AR088226A1 (es) | Derivados piperidinicos heterociclicos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades neurodegenerativas | |
| AR099677A1 (es) | Compuesto heterocíclico fusionado y su uso para el control de plagas | |
| EA201591429A1 (ru) | 2,3-дизамещенные производные 1-ацил-4-амино-1,2,3,4-тетрагидрохинолинов и их применение в качестве ингибиторов бромодомена | |
| AR097866A1 (es) | Derivados de 4-azaindol | |
| ES2662444T3 (es) | Derivado de piridina | |
| AR110282A1 (es) | Compuestos de amida bicíclica y uso de éstos en el tratamiento de enfermedades mediadas por rip1 | |
| AR103742A1 (es) | Derivados de trifluorometilpropanamida | |
| CL2020002588A1 (es) | Compuestos derivados de indol, composiciones que los contienen, útiles en el tratamiento de infestación por helmintos, preferentemente trematodos, en mamíferos. (divisional de solicitud n° 03258-2016) | |
| MX2016017405A (es) | Compuestos derivados de 2-(3-piridinil)-1h-benzimidazol y medicamentos que los contienen. | |
| AR113811A1 (es) | Sulfonas y sulfóxidos bicíclicos y métodos de uso de los mismos | |
| AR095570A1 (es) | Derivados de urea | |
| AR063374A1 (es) | Derivados de benzoxazina y sus usos | |
| AR083861A1 (es) | OXAZOLIDINONAS COMO MODULADORES DE mGluR5 Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN | |
| ES2667276T3 (es) | Derivados de sulfonilindol y método para prepararlos | |
| ES2721525T3 (es) | Novedosos agonistas de EP4 como compuestos terapéuticos | |
| AR099820A1 (es) | Ciano que contiene compuestos de azabenzofuran para el tratamiento de la hepatitis c | |
| AR094381A1 (es) | Derivados benzodioxano-piperidina y sus aplicaciones terapéuticas para el tratamiento de trastornos neuropsiquiátricos | |
| AR110226A1 (es) | Inhibidores selectivos de hdac1,2 | |
| AR107187A1 (es) | Compuesto de oxadiazol y uso del mismo |