PE20161444A1 - 1,2-ciclopentanos sustituidos como antagonistas del receptor de orexina - Google Patents

1,2-ciclopentanos sustituidos como antagonistas del receptor de orexina

Info

Publication number
PE20161444A1
PE20161444A1 PE2016001443A PE2016001443A PE20161444A1 PE 20161444 A1 PE20161444 A1 PE 20161444A1 PE 2016001443 A PE2016001443 A PE 2016001443A PE 2016001443 A PE2016001443 A PE 2016001443A PE 20161444 A1 PE20161444 A1 PE 20161444A1
Authority
PE
Peru
Prior art keywords
orexin receptor
cyclopentanes
substituted
receptor antagonists
compounds
Prior art date
Application number
PE2016001443A
Other languages
English (en)
Inventor
Tatsuhiko Fujimoto
Stephanie Maine
Charlotte Fieldhouse
John Stephen Robinson
Angela Glen
Original Assignee
Takeda Pharmaceuticals Co
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Takeda Pharmaceuticals Co filed Critical Takeda Pharmaceuticals Co
Publication of PE20161444A1 publication Critical patent/PE20161444A1/es

Links

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
    • 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
    • A61K31/495—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
    • 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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • 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
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/20—Nitrogen 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
    • C07D401/02—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
    • C07D403/02—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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/12—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 linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE 1,2-CICLOPENTANO DE FORMULA (I) DONDE R1 ES HETEROARILO DE 5 O 6 MIEMBROS OPCIONALMENTE SUSTITUIDO; L ES UN ENLACE, CH2, ENTRE OTROS; Ra Y Rb SON CADA UNO H, ALQUILO C1-C3 O HALOALQUILO C1-C3; R2 ES H, ALQUILO C1-C6 O CICLOALQUILO C3-C6; R3 ES FENILO O HETEROARILO DE 5 O 6 MIEMBROS OPCIONALMENTE SUSTITUIDOS; X ES CH2, CHF O CF2. SON COMPUESTOS PREFERIDOS: 2,6-DIMETOXI-N-[(1S,2S)-2-{[5-(TRIFLUOROMETIL)PIRIDIN-2-IL]AMINO}CICLOPENTIL]BENZAMIDA; 2,6-DIMETOXI-N-[(1S,2S)-2-{[5-(TRIFLUOROMETIL)PIRIMIDIN-2-IL]AMINO}CICLOPENTIL]BENZAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR DE OREXINA SIENDO UTILES EN EL TRATAMIENTO DE LA ESQUIZOFRENIA
PE2016001443A 2014-02-20 2015-02-19 1,2-ciclopentanos sustituidos como antagonistas del receptor de orexina PE20161444A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP14156011 2014-02-20

Publications (1)

Publication Number Publication Date
PE20161444A1 true PE20161444A1 (es) 2017-01-06

Family

ID=50115776

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016001443A PE20161444A1 (es) 2014-02-20 2015-02-19 1,2-ciclopentanos sustituidos como antagonistas del receptor de orexina

Country Status (27)

Country Link
US (3) US10011588B2 (es)
EP (1) EP3107898B1 (es)
JP (1) JP6433505B2 (es)
KR (1) KR20160121572A (es)
CN (1) CN106164047B (es)
AR (1) AR099495A1 (es)
AU (1) AU2015220551B2 (es)
CA (1) CA2938855C (es)
CL (1) CL2016002084A1 (es)
CR (1) CR20160374A (es)
EA (1) EA033758B1 (es)
EC (1) ECSP16074478A (es)
ES (1) ES2855499T3 (es)
GE (1) GEP20186910B (es)
IL (1) IL247194B (es)
MA (1) MA39152B1 (es)
MX (1) MX2016010848A (es)
MY (1) MY182564A (es)
PE (1) PE20161444A1 (es)
PH (1) PH12016501624A1 (es)
PL (1) PL3107898T3 (es)
SG (2) SG11201605298RA (es)
TN (1) TN2016000263A1 (es)
TW (1) TW201613864A (es)
UA (1) UA119552C2 (es)
UY (1) UY36003A (es)
WO (1) WO2015124932A1 (es)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5759470B2 (ja) 2009-10-23 2015-08-05 ヤンセン ファーマシューティカ エヌ．ベー． オレキシン受容体調節因子としての二置換オクタヒドロピロロ［３，４−ｃ］ピロール
TW201613864A (en) 2014-02-20 2016-04-16 Takeda Pharmaceutical Novel compounds
KR102559922B1 (ko) 2016-03-10 2023-07-25 얀센 파마슈티카 엔.브이. 오렉신-2 수용체 길항제를 사용한 우울증의 치료 방법
AU2017326253B2 (en) 2016-09-13 2021-10-21 Allergan, Inc. Stabilized non-protein clostridial toxin compositions
CN106580998B (zh) * 2016-12-08 2017-11-07 青岛市市立医院 一种治疗肾性高血压的药物组合物
CN107434788B (zh) * 2017-09-11 2018-06-15 威海迪素制药有限公司 一种格列吡嗪的制备方法
SG11202005016SA (en) 2017-12-05 2020-06-29 Sunovion Pharmaceuticals Inc Nonracemic mixtures and uses thereof
WO2019113084A1 (en) 2017-12-05 2019-06-13 Sunovion Pharmaceuticals Inc. Crystal forms and production methods thereof
KR20220018004A (ko) 2019-06-04 2022-02-14 선오비온 파마슈티컬스 인코포레이티드 조절 방출 제형 및 이의 용도
EP4088721A4 (en) * 2020-01-08 2024-01-10 Neuroventi COMPOSITION FOR TREATMENT OF FRAGILE X SYNDROME OR ASSOCIATED DEVELOPMENTAL DISORDERS, COMPRISING A LISURIDE COMPOUND AS ACTIVE INGREDIENT
CN113999142B (zh) * 2021-11-29 2023-01-24 蚌埠中实化学技术有限公司 一种手性N-Boc-反式-1,2-环己二胺的制备方法

Family Cites Families (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3708962B2 (ja) 1994-08-24 2005-10-19 アストラゼネカ・アクチエボラーグ 治療に有用なスピロ−アザ二環式化合物
SE9504661D0 (sv) 1995-12-22 1995-12-22 Astra Pharma Inc New compounds
SE9600683D0 (sv) 1996-02-23 1996-02-23 Astra Ab Azabicyclic esters of carbamic acids useful in therapy
AR013184A1 (es) 1997-07-18 2000-12-13 Astrazeneca Ab Aminas heterociclicas espiroazobiciclicas, composicion farmaceutica, uso de dichas aminas para preparar medicamentos y metodo de tratamiento o profilaxis
SE9702799D0 (sv) 1997-07-25 1997-07-25 Astra Ab New compounds
SE9900100D0 (sv) 1999-01-15 1999-01-15 Astra Ab New compounds
SE9903760D0 (sv) 1999-10-18 1999-10-18 Astra Ab New compounds
SE9904176D0 (sv) 1999-11-18 1999-11-18 Astra Ab New use
SE0000540D0 (sv) 2000-02-18 2000-02-18 Astrazeneca Ab New compounds
SE0002729D0 (sv) 2000-07-20 2000-07-20 Astrazeneca Ab Novel compound form
MY140070A (en) 2001-05-18 2009-11-30 Astrazeneca Ab 4-(phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders
ATE353332T1 (de) 2001-06-01 2007-02-15 Astrazeneca Ab Neuer, für die therapie geeigneter ligand für nikotinische acetylcholinrezeptoren
ES2266549T3 (es) * 2001-06-28 2007-03-01 Smithkline Beecham Plc Derivados de n-aroil-amina ciclicos como antagonistas del receptor de orexina.
GB0130341D0 (en) * 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
WO2003087103A1 (en) 2002-04-18 2003-10-23 Astrazeneca Ab Thienyl compounds
US7417049B2 (en) 2002-04-18 2008-08-26 Astrazeneca Ab Furyl compounds
CA2482313A1 (en) 2002-04-18 2003-10-23 Astrazeneca Ab Heterocyclic compounds
AU2003273179A1 (en) 2002-05-10 2003-12-12 Bristol-Myers Squibb Company 1,1-disubstituted cycloalkyl derivatives as factor xa inhibitors
SE0202430D0 (sv) 2002-08-14 2002-08-14 Astrazeneca Ab New Compounds
SE0202465D0 (sv) 2002-08-14 2002-08-14 Astrazeneca Ab New compounds
SE0202598D0 (sv) 2002-09-02 2002-09-02 Astrazeneca Ab Alpha-7 Nicotinic receptor agonists and statins in combination
US20080090863A1 (en) * 2004-09-30 2008-04-17 Taisho Pharmaceutical Co., Ltd. Pyridine Derivatives and Their Use as Medicaments for Treating Diseases Related to Mch Receptor
DK1846354T3 (da) 2005-01-14 2010-08-16 Allergan Inc Substituterede cyclopentaner eller cyclopentanoner til behandling af okular hypertensive tilstande
US20090118200A1 (en) * 2005-05-23 2009-05-07 Bergman Jeffrey M Proline bis-amide orexin receptor antagonists
MEP1008A (xx) 2005-12-21 2010-02-10 Incyte Corp 3-aminociklopentankarboksamidi kao modulatori receptora hemokina
JP2009543785A (ja) * 2006-07-14 2009-12-10 メルク エンド カムパニー インコーポレーテッド 架橋ジアゼパンオレキシン受容体アンタゴニスト
WO2008038841A1 (fr) * 2006-09-30 2008-04-03 Japan Tobacco Inc. Dérivé de thiadiazolone et utilisation de celui-ci
EP2125808A2 (en) 2006-12-15 2009-12-02 Bayer Schering Pharma Aktiengesellschaft 3-h-pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
EP2120575A4 (en) 2006-12-21 2011-04-27 Abbott Lab AGONISTS AND ANTAGONISTS OF SPHINGOSINE-1-PHOSPHATE RECEPTORS
AR064561A1 (es) 2006-12-28 2009-04-08 Actelion Pharmaceuticals Ltd Derivados de 2-aza-biciclo[3.1.0]hexano y su uso en la preparacion de un medicamento para el tratamiento de enfermedades relacionadas con disfunciones generales del sistema de la orexina.
CN101796053A (zh) * 2007-07-03 2010-08-04 葛兰素集团有限公司 用作食欲素受体拮抗剂的哌啶衍生物
WO2009080533A1 (en) * 2007-12-21 2009-07-02 F. Hoffmann-La Roche Ag Heteroaryl derivatives as orexin receptor antagonists
JP2010155827A (ja) * 2008-12-04 2010-07-15 Takeda Chem Ind Ltd スピロ環化合物
ES2428288T3 (es) * 2009-05-12 2013-11-06 Actelion Pharmaceuticals Ltd. Novedosos derivados de oxazolidinona y su uso como antagonistas del receptor de la orexina
US8080541B2 (en) * 2009-08-27 2011-12-20 Hoffman-La Roche Inc. Carbocyclic GlyT-1 receptor antagonists
CA2821893A1 (en) * 2010-12-17 2012-06-21 Taisho Pharmaceutical Co., Ltd. Pyrazole derivative
EP2675801B1 (en) * 2011-02-18 2015-04-08 Actelion Pharmaceuticals Ltd. Novel pyrazole and imidazole derivatives useful as orexin antagonists
CN104334544B (zh) * 2012-06-04 2016-10-19 埃科特莱茵药品有限公司 苯并咪唑脯氨酸衍生物
WO2014124230A2 (en) * 2013-02-08 2014-08-14 Celgene Avilomics Research, Inc. Erk inhibitors and uses thereof
GB201318222D0 (en) * 2013-10-15 2013-11-27 Takeda Pharmaceutical Novel compounds
MX2016010745A (es) 2014-02-20 2017-02-02 Takeda Pharmaceuticals Co Ciclopentanos, tetrahidrofuranos y pirrolidinas sustituidas como antagonistas del receptor de orexina.
TWI651310B (zh) 2014-02-20 2019-02-21 日商日本煙草產業股份有限公司 三化合物及其醫藥用途
TW201613864A (en) 2014-02-20 2016-04-16 Takeda Pharmaceutical Novel compounds

Also Published As

Publication number Publication date
AU2015220551A1 (en) 2016-07-14
PL3107898T3 (pl) 2021-06-14
CN106164047B (zh) 2019-04-16
JP6433505B2 (ja) 2018-12-05
MA39152A1 (fr) 2017-11-30
CA2938855C (en) 2022-06-21
PH12016501624A1 (en) 2016-11-07
MY182564A (en) 2021-01-25
SG11201605298RA (en) 2016-07-28
ES2855499T3 (es) 2021-09-23
ECSP16074478A (es) 2018-07-31
MX2016010848A (es) 2017-01-23
MA39152B1 (fr) 2019-09-30
WO2015124932A1 (en) 2015-08-27
US20170066744A1 (en) 2017-03-09
US9156829B2 (en) 2015-10-13
US20180282309A1 (en) 2018-10-04
EA201691674A1 (ru) 2017-02-28
CN106164047A (zh) 2016-11-23
IL247194B (en) 2019-12-31
SG10201908582TA (en) 2019-11-28
AU2015220551B2 (en) 2018-10-25
KR20160121572A (ko) 2016-10-19
GEP20186910B (en) 2018-10-25
CL2016002084A1 (es) 2017-09-08
US10011588B2 (en) 2018-07-03
CR20160374A (es) 2017-01-27
EP3107898B1 (en) 2021-01-06
TW201613864A (en) 2016-04-16
US10689373B2 (en) 2020-06-23
TN2016000263A1 (en) 2017-10-06
EA033758B1 (ru) 2019-11-22
AR099495A1 (es) 2016-07-27
CA2938855A1 (en) 2015-08-27
IL247194A0 (en) 2016-09-29
JP2017506635A (ja) 2017-03-09
EP3107898A1 (en) 2016-12-28
UA119552C2 (uk) 2019-07-10
UY36003A (es) 2015-09-30
US20150232460A1 (en) 2015-08-20

Similar Documents

Publication Publication Date Title
PE20161444A1 (es) 1,2-ciclopentanos sustituidos como antagonistas del receptor de orexina
PE20161225A1 (es) 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer
ES2770058T3 (es) Compuestos y composiciones destinados a modular las actividades de quinasa de EGFR mutante
PE20161443A1 (es) Compuestos
PE20141404A1 (es) Derivados de tieno[3,2-d]pirimidina que tienen actividad inhibidora por las quinasas de las proteinas
PE20161407A1 (es) Piridina 5,6 disustituida -2-carboxamidas como agonistas del receptor canabinoide
PE20171329A1 (es) Agentes inmunorreguladores
NI201600152A (es) Compuestos de heteroarilo o arilo bicíclicos fusionados y su uso como inhibidores de irak4
PE20141973A1 (es) Compuestos de heterociclilo como inhibidores de mek
PE20170186A1 (es) Nuevos compuestos
PE20170947A1 (es) 2-amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de bace1
PE20181269A1 (es) Agonistas del receptor de apelina y metodos de uso
PE20131343A1 (es) Derivados de acido benzoico
PE20181015A1 (es) 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
PE20161438A1 (es) Inhibidores de desmetilasa 1 especifica a lisina
PE20181074A1 (es) Compuestos heteroaromaticos como inhibidores de btk
PE20161073A1 (es) Amino-heteroaril-benzamidas como inhibidores de cinasa
PE20170444A1 (es) Herbicidas de piperidinona
PE20180024A1 (es) Triazolopirazinonas como inhibidores de pde1
PE20140703A1 (es) Derivados de heteroarilo como moduladores de nachr alfa 7
PE20141202A1 (es) Compuesto de ciclopropanoamina
PE20110196A1 (es) 5-alquinil-pirimidinas
PE20180355A1 (es) Desacetoxitubulisina h y analogos de esta
PE20141828A1 (es) 6-alquinilo piridinas como mimeticos smac
PE20161366A1 (es) Heterociclil-sulfonas sustituidas con heteroarilo