AR039329A1 - Derivados de triazol, antagonistas de receptor de taquicinina - Google Patents
Derivados de triazol, antagonistas de receptor de taquicininaInfo
- Publication number
- AR039329A1 AR039329A1 ARP030101377A ARP030101377A AR039329A1 AR 039329 A1 AR039329 A1 AR 039329A1 AR P030101377 A ARP030101377 A AR P030101377A AR P030101377 A ARP030101377 A AR P030101377A AR 039329 A1 AR039329 A1 AR 039329A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- independently
- group
- phenyl
- halo
- Prior art date
Links
- QWENRTYMTSOGBR-UHFFFAOYSA-N 1H-1,2,3-Triazole Chemical class C=1C=NNN=1 QWENRTYMTSOGBR-UHFFFAOYSA-N 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 7
- -1 cyano, difluoromethyl Chemical group 0.000 abstract 5
- 125000005843 halogen group Chemical group 0.000 abstract 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 4
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 150000001335 aliphatic alkanes Chemical class 0.000 abstract 3
- 125000004429 atom Chemical group 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000004076 pyridyl group Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- RNQOHYCJKWDINT-UHFFFAOYSA-N N-phenoxy-N-phenylsulfanylaniline Chemical compound O(C1=CC=CC=C1)N(C1=CC=CC=C1)SC1=CC=CC=C1 RNQOHYCJKWDINT-UHFFFAOYSA-N 0.000 abstract 1
- 102000007124 Tachykinin Receptors Human genes 0.000 abstract 1
- 108010072901 Tachykinin Receptors Proteins 0.000 abstract 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000005554 pyridyloxy group Chemical group 0.000 abstract 1
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 1
- 229940042055 systemic antimycotics triazole derivative Drugs 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
Classifications
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
- C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
-
- 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
- C07D403/02—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 two hetero rings
- C07D403/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
- C07D487/04—Ortho-condensed systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Pulmonology (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Se refiere a derivados de triazol, o a una sal farmacéuticamente aceptable del mismo, a composiciones farmacéuticas del mismo y a su uso como inhibidor del subtipo NK-1 de receptores de taquicinina, así como a un proceso para su preparación y a los intermedios del mismo. Reivindicación 1: Un compuesto de fórmula (1) en la que: D es un alcano (C1-3)diilo; R1 es fenilo, que está opcionalmente sustituido con uno a tres sustituyentes independientemente seleccionados del grupo constituido por halo, alquilo C1-4, alcoxi C1-4, ciano, difluorometilo, trifluorometilo y trifluorometoxi; R4 es un radical seleccionado del grupo constituido por el grupo de fórmula (2) en el que A1-A2-A3-A4-, junto con los átomos a los que están unidos, forma un anillo carbocíclico o heterocíclico aromático en el que cada uno de A1, A2, A3 y A4 es independientemente -CR8- o N, debiendo ser -CR8- al menos uno de A1, A2, A3 y A4, -G1-G2-G3-, junto con los átomos a los que están unidos, forma un anillo heterocíclico aromático en el que cada uno de G1, G2 y G3 es independientemente -CR8-, N, O, o S, pudiendo ser O o S sólo uno de G1, G2 y G3, -G4-G5-G6-, junto con los átomos a los que están unidos, forma un anillo heterocíclico en el que cada uno de G4, G5 y G6 es independientemente -CR8- o N; cada R8 está independientemente seleccionado del grupo constituido por H, halo, alquilo C1-4, alquilo C1-4 sustituido, cicloalquilo C3-6, -NR12R13, trifluorometilo y trifluorometoxi; R12 y R13 son cada uno independientemente H, alquilo C1-4 o -C(O)-CH3, o R12 y R13, junto con el N al que están unidos, forman un anillo de 4 a 7 miembros; Q1, Q2, Q5 y Q6 son cada uno independientemente -CH- o N; Q3 y Q4 son cada uno independientemente O, o N, debiendo ser N al menos uno de Q3 y Q4; R6 es alquilo C1-6, cicloalquilo C3-6, fenilo o piridilo; estando opcionalmente sustituido dicho fenilo o piridilo con 1 a 3 sustituyentes independientemente seleccionados del grupo constituido por halo, ciano, alquilo C1-4, alcoxi C1-4, trifluorometilo, trifluorometoxi, morfolino y -NR14R15; R14 y R15 son cada uno independientemente, H, o alquilo C1-4, o R14 y R15 conjuntamente con el N al que están unidos forman un anillo de 4-7 miembros; X es un enlace, alcano (C1-3)diilo, -CH(OH)-, -C(O)-, -O-, S(O)p-, o -C=N-OR9-; p es 0, 1 o 2; R9 es H, alquilo C1-4 o bencilo; Y es un enlace, alcano (C1-3)diilo o -C(O)-; n es 0, 1 o 2; cada R7 es independientemente alquilo C1-4; R5 es H, halo, trifluorometilo, alquilo C1-4, cicloalquilo C3-6, furilo, tienilo, pirrolilo, imidazolilo, -NR16R17, piridiloxi, fenilo, fenoxi, feniltio, anilino, pudiendo estar opcionalmente sustituido dicho grupo fenilo, fenoxi, feniltio o anilino en el anillo de fenilo con 1 o 2 sustituyentes independientemente seleccionados del grupo constituido por halo, alquilo C1-4, alcoxi C1-4 y -S(O)qalquilo (C1-4), o un radical seleccionado del grupo constituido por el grupo de las fórmulas (3) en el que W es un enlace, -CH2-, -O-, -NR11- o -S(O)q-; q es 0, 1 o 2; R11 se selecciona del grupo constituido por H, alquilo C1-4, acetilo, fenilo, bencilo y -S(O)2CH3; Z1, Z2 y Z3 son cada uno independientemente -CH- o N; R16 y R17 son cada uno independientemente H, o alquilo C1-4; o una sal farmacéuticamente aceptable de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US37612102P | 2002-04-26 | 2002-04-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR039329A1 true AR039329A1 (es) | 2005-02-16 |
Family
ID=29270766
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030101377A AR039329A1 (es) | 2002-04-26 | 2003-04-22 | Derivados de triazol, antagonistas de receptor de taquicinina |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US7320994B2 (es) |
| EP (1) | EP1501809B1 (es) |
| JP (1) | JP4559087B2 (es) |
| KR (1) | KR100755577B1 (es) |
| CN (1) | CN1312136C (es) |
| AR (1) | AR039329A1 (es) |
| AT (1) | ATE384053T1 (es) |
| AU (1) | AU2003230829B8 (es) |
| BR (1) | BRPI0309534B8 (es) |
| CA (1) | CA2483159C (es) |
| CR (1) | CR7548A (es) |
| CY (1) | CY1107221T1 (es) |
| DE (1) | DE60318697T2 (es) |
| DK (1) | DK1501809T3 (es) |
| EA (1) | EA007720B1 (es) |
| EC (1) | ECSP045391A (es) |
| ES (1) | ES2298513T3 (es) |
| HR (1) | HRP20041008B1 (es) |
| IL (2) | IL164675A0 (es) |
| MX (1) | MXPA04010622A (es) |
| MY (1) | MY141559A (es) |
| NO (1) | NO333647B1 (es) |
| NZ (1) | NZ535886A (es) |
| PE (1) | PE20040600A1 (es) |
| PL (1) | PL212090B1 (es) |
| PT (1) | PT1501809E (es) |
| TW (1) | TWI265807B (es) |
| UA (1) | UA79113C2 (es) |
| WO (1) | WO2003091226A1 (es) |
| ZA (1) | ZA200408670B (es) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR039241A1 (es) | 2002-04-04 | 2005-02-16 | Biogen Inc | Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos |
| EP1638944A1 (en) * | 2003-06-12 | 2006-03-29 | Eli Lilly And Company | Tachykinin receptor antagonists |
| ATE462700T1 (de) | 2003-10-24 | 2010-04-15 | Lilly Co Eli | Neue kristalline formen von ä2-ä1-(3,5- bistrifluormethylbenzyl)-5-pyridin-4-yl-1h-ä1,2 3üütriazol-4-ylü-pyridin-3-ylü-(2- chlorphenyl)methanon |
| CA2581454A1 (en) | 2004-09-23 | 2006-03-30 | Reddy Us Therapeutics, Inc. | Novel pyrimidine compounds, process for their preparation and compositions containing them |
| WO2006083711A1 (en) * | 2005-02-01 | 2006-08-10 | Eli Lilly And Company | Tachykinin receptor antagonists |
| US7829585B2 (en) | 2005-03-30 | 2010-11-09 | Eisai R&D Management Co., Ltd. | Antifungal agent containing pyridine derivative |
| EP1894919B1 (en) * | 2005-06-07 | 2012-03-28 | Shionogi & Co., Ltd. | Heterocyclic compound having type i 11 beta hydroxysteroid dehydrogenase inhibitory activity |
| JP4860696B2 (ja) * | 2005-07-25 | 2012-01-25 | エフ．ホフマン−ラ ロシュ アーゲー | 置換トリアゾール誘導体及びそのニューロキニン３レセプターアンタゴニストとしての使用 |
| TWI385169B (zh) | 2005-10-31 | 2013-02-11 | Eisai R&D Man Co Ltd | 經雜環取代之吡啶衍生物及含有彼之抗真菌劑 |
| EP2233136A1 (en) * | 2006-08-18 | 2010-09-29 | Syngenta Limited | Use of HPPD Inhibitors in the Treatment of Depression and/or Withdrawal Symptoms Associated with Addictive Drugs |
| EP2065377B1 (en) | 2006-09-21 | 2011-11-23 | Eisai R&D Management Co., Ltd. | Pyridine derivative substituted by heteroaryl ring, and antifungal agent comprising the same |
| EP2121610B1 (en) * | 2006-12-20 | 2014-04-02 | Eli Lilly & Company | Novel intermediate and process useful in the preparation of {2-[1-(3,5-bis-trifluoromethyl-benzyl)-5-pyridin-4-yl-1h-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone |
| NZ582520A (en) * | 2007-08-08 | 2011-10-28 | Neurosearch As | Novel 1,2,3-triazole derivatives useful as modulators of nicotinic acetylcholine receptors |
| GB0722077D0 (en) * | 2007-11-09 | 2007-12-19 | Smithkline Beecham Corp | Compounds |
| US8513287B2 (en) | 2007-12-27 | 2013-08-20 | Eisai R&D Management Co., Ltd. | Heterocyclic ring and phosphonoxymethyl group substituted pyridine derivatives and antifungal agent containing same |
| WO2009158011A1 (en) * | 2008-06-26 | 2009-12-30 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
| GB0823002D0 (en) * | 2008-12-17 | 2009-01-28 | Syngenta Participations Ag | Isoxazoles derivatives with plant growth regulating properties |
| EP2729147B1 (en) | 2011-07-04 | 2017-09-06 | IRBM - Science Park S.p.A. | Nk-1 receptor antagonists for treating corneal neovascularisation |
| TWI636047B (zh) | 2013-08-14 | 2018-09-21 | 英商卡爾維斯塔製藥有限公司 | 雜環衍生物 |
| GB201421083D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | Enzyme inhibitors |
| GB201421085D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
| WO2016141341A1 (en) | 2015-03-04 | 2016-09-09 | Vanda Pharmaceuticals Inc. | Method of treatment with tradipitant |
| US10287287B2 (en) | 2015-08-17 | 2019-05-14 | Eli Lilly And Company | Process development of a pyridine-containing NK-1 receptor antagonist |
| JP6884801B2 (ja) | 2016-05-31 | 2021-06-09 | カルビスタ・ファーマシューティカルズ・リミテッド | 血漿カリクレインインヒビターとしてのピラゾール誘導体 |
| GB201609607D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts |
| GB201609603D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide |
| KR20200054232A (ko) | 2017-09-13 | 2020-05-19 | 반다 파마슈티칼즈, 인코퍼레이티드. | 트라디피탄트를 이용한 아토피 피부염의 개선된 치료 |
| IL274541B2 (en) * | 2017-11-17 | 2024-10-01 | Vanda Pharmaceuticals Inc | Method of treatment of gastrointestinal diseases with tradipitant |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| HUE057912T2 (hu) | 2017-11-29 | 2022-06-28 | Kalvista Pharmaceuticals Ltd | Plazma kallikrein inhibitort tartalmazó dózisformák |
| CN111918647A (zh) | 2018-02-26 | 2020-11-10 | 圣拉斐尔医院有限公司 | 用于治疗眼痛的nk-1拮抗剂 |
| WO2019236852A1 (en) | 2018-06-08 | 2019-12-12 | Vanda Pharmaceuticals Inc. | Method of treatment with tradipitant |
| US10821099B2 (en) | 2018-09-28 | 2020-11-03 | Vanda Pharmaceuticals Inc. | Use of tradipitant in motion sickness |
| FI3856338T3 (fi) * | 2018-09-28 | 2025-02-03 | Vanda Pharmaceuticals Inc | Tradipitantin käyttö matkapahoinvoinnissa |
| EP3890735A1 (en) | 2018-12-03 | 2021-10-13 | Vanda Pharmaceuticals Inc. | Method of treatment with tradipitant |
| WO2020132513A1 (en) | 2018-12-21 | 2020-06-25 | Vanda Pharmaceuticals Inc. | Improved treatment of atopic dermatitis with tradipitant |
| WO2021028645A1 (en) | 2019-08-09 | 2021-02-18 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
| IL295327A (en) | 2020-02-25 | 2022-10-01 | Vanda Pharmaceuticals Inc | Improved treatment of atopic dermatitis with tradipitant |
| WO2021180885A1 (en) | 2020-03-11 | 2021-09-16 | Ospedale San Raffaele S.R.L. | Treatment of stem cell deficiency |
| EP4125811A1 (en) | 2020-03-26 | 2023-02-08 | Vanda Pharmaceuticals Inc. | Treatment of lower respiratory tract infection with tradipitant |
| EP4125875A1 (en) | 2020-04-03 | 2023-02-08 | NeRRe Therapeutics Limited | An nk-1 receptor antagonist for treating a disease selecting from sepsis, septic shock,, acute respiratory distress syndrome (ards) or multiple organ dysfunction syndrome (mods) |
| CN113563306B (zh) * | 2020-04-28 | 2022-07-01 | 新发药业有限公司 | 一种2-(4-苯氧基苯基)-6-(哌啶-4-)基烟酰胺的制备方法 |
| MX2022014901A (es) | 2020-06-02 | 2023-01-18 | Nerre Therapeutics Ltd | Antagonistas del receptor de neuroquinina (nk)-1 para su uso en el tratamiento de condiciones de fibrosis pulmonar promovidas por lesion mecanica a los pulmones. |
| CN111662235B (zh) * | 2020-06-23 | 2023-12-22 | 黄淮学院 | 一种苯甲酰基哒嗪衍生物及其制备方法 |
| WO2023019084A1 (en) | 2021-08-12 | 2023-02-16 | Vanda Pharmaceuticals Inc. | Treatment of gastric accommodation with tradipitant |
| US20240350469A1 (en) | 2021-08-31 | 2024-10-24 | Vanda Pharmaceuticals Inc. | Treatment of lower respiratory tract infection with tradipitant |
| WO2024138040A1 (en) | 2022-12-21 | 2024-06-27 | Vanda Pharmaceuticals Inc. | Methods of treatment with tradipitant |
| CN116082253B (zh) * | 2023-02-25 | 2025-04-25 | 浙大城市学院 | 一种1-n-取代的1,2,3-三唑-4-甲酰胺衍生物及其制备方法 |
| WO2024223617A1 (en) * | 2023-04-24 | 2024-10-31 | Fundamental Pharma Gmbh | Effective means to modulate nmda receptor-mediated toxicity |
| US20250255855A1 (en) | 2024-02-09 | 2025-08-14 | Vanda Pharmaceuticals Inc. | Method of treatment with tradipitant |
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| IL50699A0 (en) | 1975-10-28 | 1976-12-31 | Ici America Inc | Triazole derivatives |
| WO1995011880A1 (en) * | 1993-10-27 | 1995-05-04 | Merck Sharp & Dohme Limited | Substituted amides as tachykinin antagonists |
| US6175013B1 (en) * | 1994-06-10 | 2001-01-16 | Eli Lilly And Company | Imidazolinyl tachykinin receptor antagonists |
| US5998444A (en) * | 1995-10-24 | 1999-12-07 | Zeneca Ltd. | Piperidinyl compounds as NK1 or NK2 antagonists |
| WO1997040025A1 (en) | 1996-04-19 | 1997-10-30 | Novo Nordisk A/S | Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles |
| PT915880E (pt) * | 1996-07-24 | 2007-12-31 | Bristol Myers Squibb Pharma Co | Azol triazinas e pirimidinas |
| US6060478A (en) * | 1996-07-24 | 2000-05-09 | Dupont Pharmaceuticals | Azolo triazines and pyrimidines |
| BR9811821A (pt) | 1997-08-06 | 2000-08-15 | Lilly Co Eli | 2-acilaminopropanaminas como antagonistas de receptores de taquicinina |
| CA2393672A1 (en) * | 1999-12-17 | 2001-06-21 | Schering Corporation | Selective neurokinin antagonists |
| TWI287003B (en) | 2000-07-24 | 2007-09-21 | Hoffmann La Roche | 4-phenyl-pyridine derivatives |
| DE10036818A1 (de) * | 2000-07-28 | 2002-02-07 | Solvay Pharm Gmbh | Neue N-Triazolylmethyl-Piperazinderivate als Neurokininrezeptor-Antagonisten |
| JP2002123925A (ja) | 2000-10-13 | 2002-04-26 | Fuji Photo Film Co Ltd | 磁気記録媒体 |
| CN1313450C (zh) * | 2002-04-26 | 2007-05-02 | 伊莱利利公司 | 速激肽受体拮抗剂 |
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