AR024379A1 - Gamma-carbolinas fusionadas heterociclicas sustituidas - Google Patents

Gamma-carbolinas fusionadas heterociclicas sustituidas

Info

Publication number
AR024379A1
AR024379A1 ARP000102981A ARP000102981A AR024379A1 AR 024379 A1 AR024379 A1 AR 024379A1 AR P000102981 A ARP000102981 A AR P000102981A AR P000102981 A ARP000102981 A AR P000102981A AR 024379 A1 AR024379 A1 AR 024379A1
Authority
AR
Argentina
Prior art keywords
disorders
carbolins
heterociclic
gamma
fused
Prior art date
Application number
ARP000102981A
Other languages
English (en)
Original Assignee
Du Pont Pharm 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 Du Pont Pharm Co filed Critical Du Pont Pharm Co
Publication of AR024379A1 publication Critical patent/AR024379A1/es

Links

Classifications

    • 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
    • C07D471/06—Peri-condensed systems
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/22—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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/18—Ring systems of four or more rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/32—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems containing carbocyclic rings other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/06—Peri-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Anesthesiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente se refiere a ciertos compuestos novedosos representados por la formula estructural (1) o sus sales aceptables para uso farmacéutico, donde R1,R5, R6a, R6b, R7, R8, R9, X, b, k, m, y n, y las líneas de puntos se describen en la presente. También se relaciona con formulaciones farmacéuticas quecomprenden estos nuevos compuestos como ingredientes activos y con el uso de estos nuevos compuestos en el tratamiento de determinadas afecciones. Loscompuestos de la presente son agonistas y antagonistas de serotonina que son utiles en el control o prevencion de trastornos del sistema nervioso central queincluyen obesidad, ansiedad, depresion, psicosis, esquizofrenia, trastornos del sueno, trastornos de la sexualidad, migrana, trastornos asociados con dolorescefálicos, fobias sociales y trastornos gastrointestinales tales como disfuncion de la motilidad del tracto gastrointestinal.
ARP000102981A 1999-06-15 2000-06-15 Gamma-carbolinas fusionadas heterociclicas sustituidas AR024379A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US13932199P 1999-06-15 1999-06-15

Publications (1)

Publication Number Publication Date
AR024379A1 true AR024379A1 (es) 2002-10-02

Family

ID=22486095

Family Applications (3)

Application Number Title Priority Date Filing Date
ARP000102979A AR024377A1 (es) 1999-06-15 2000-06-15 Gamma-carbolinas fusionadas heterociclicas sustituidas
ARP000102981A AR024379A1 (es) 1999-06-15 2000-06-15 Gamma-carbolinas fusionadas heterociclicas sustituidas
ARP000102980A AR024378A1 (es) 1999-06-15 2000-06-15 Gamma-carbolinas fusionadas heterociclicas sustituidas

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP000102979A AR024377A1 (es) 1999-06-15 2000-06-15 Gamma-carbolinas fusionadas heterociclicas sustituidas

Family Applications After (1)

Application Number Title Priority Date Filing Date
ARP000102980A AR024378A1 (es) 1999-06-15 2000-06-15 Gamma-carbolinas fusionadas heterociclicas sustituidas

Country Status (19)

Country Link
US (7) US6552017B1 (es)
EP (3) EP1189904B1 (es)
JP (3) JP4762465B2 (es)
CN (3) CN1370169A (es)
AR (3) AR024377A1 (es)
AT (3) ATE277048T1 (es)
AU (3) AU5738000A (es)
BR (3) BR0012086A (es)
CA (3) CA2374239A1 (es)
DE (3) DE60014083T2 (es)
ES (3) ES2223536T3 (es)
HK (3) HK1043112A1 (es)
IL (3) IL147108A0 (es)
MX (3) MXPA01012914A (es)
NO (3) NO20016115L (es)
NZ (1) NZ516031A (es)
TR (1) TR200103658T2 (es)
WO (3) WO2000077001A1 (es)
ZA (1) ZA200109735B (es)

Families Citing this family (148)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6407092B1 (en) 1999-04-23 2002-06-18 Pharmacia & Upjohn Company Tetracyclic azepinoindole compounds
JP4762465B2 (ja) * 1999-06-15 2011-08-31 ブリストル−マイヤーズ スクイブ ファーマ カンパニー 置換複素環縮合ガンマーカルボリン
US6583135B2 (en) 2000-09-20 2003-06-24 Pharmacia & Upjohn Company Substituted azepino[4,5b]indole derivatives
US6858604B2 (en) 2000-11-03 2005-02-22 Wyeth Cyclohepta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives
AR031202A1 (es) 2000-11-03 2003-09-10 Wyeth Corp Ciclopenta(b) (1,4)diazepino(6,7,1-hi) indoles y derivados
US6759405B2 (en) 2000-11-03 2004-07-06 Wyeth Cycloocta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives
CN1227237C (zh) 2000-11-20 2005-11-16 比奥维特罗姆股份公司 作为五羟色胺5－ht2受体拮抗剂的哌嗪基吡嗪化合物
SE0004245D0 (sv) 2000-11-20 2000-11-20 Pharmacia Ab Novel compounds and their use
US6849619B2 (en) 2000-12-20 2005-02-01 Bristol-Myers Squibb Company Substituted pyridoindoles as serotonin agonists and antagonists
HUP0303432A3 (en) 2000-12-20 2012-09-28 Bristol Myers Squibb Co Substituted pyridoindoles as serotonin agonists and antagonists and pharmaceutical compositions containing the compounds and their use
JP2004534781A (ja) * 2001-06-01 2004-11-18 アルコン，インコーポレイテッド 新規なアリールアミノプロパン類似体および緑内障治療へのこれらの使用
WO2002098860A1 (en) * 2001-06-01 2002-12-12 Alcon, Inc. Novel fused indazoles and indoles and their use for the treatment of glaucoma
BR0210241A (pt) * 2001-06-01 2004-08-10 Alcon Inc Piranoindazóis e seu uso no tratamento de glaucoma
WO2003014125A1 (en) * 2001-08-06 2003-02-20 Pharmacia & Upjohn Company Therapeutically useful tetracyclic ligands
US20030060462A1 (en) * 2001-08-06 2003-03-27 Hoffman Robert L. Therapeutic compounds
WO2003024976A2 (en) * 2001-09-21 2003-03-27 Pharmacia & Upjohn Company Tricyclic indole derivatives as 5-ht ligands
WO2003033497A1 (en) * 2001-10-18 2003-04-24 Pharmacia & Upjohn Company Tetracyclic azaindoles and -indolines having serotonin 5-ht2c activity
TW200307682A (en) 2002-04-25 2003-12-16 Wyeth Corp 1,2,3,4,7,8-Hexahydro-6H-[1,4]diazepino[6,7,1-ij]quinoline derivatives as antipsychotic and antiobesity agents
TWI312781B (en) 2002-04-25 2009-08-01 [1,4]diazepino[6,7,1-ij]quinoline derivatives as antipsychotic and antiobesity agents
TW200307540A (en) 2002-04-25 2003-12-16 Wyeth Corp [1, 4]Diazocino[7, 8, 1-hi] indole derivatives as antipsychotic and antiobesity agents
BR0311970A (pt) 2002-06-19 2005-03-29 Biovitrum Ab Novos compostos, seu uso e preparação
US6958420B2 (en) * 2002-07-19 2005-10-25 Board Of Trustees Of Michigan State University Synthesis of aminoarylboronic esters and substituted anilines from arenes via catalytic C-H activation/borylation/amination and uses thereof
CN1678302A (zh) * 2002-08-30 2005-10-05 爱尔康公司 取代的5－苯并二氢吡喃－5－基－乙胺化合物及其在治疗青光眼中的用途
EP1581209A4 (en) 2002-12-13 2009-03-11 Alcon Inc NEW BENZOPYRAN ANALOGUE AND ITS USE FOR THE TREATMENT OF GLAUKOM
EP1581221B1 (en) * 2002-12-19 2011-05-18 Bristol-Myers Squibb Company Substituted tricyclic gamma-carbolines as serotonin receptor agonists and antagonists
CL2004000826A1 (es) 2003-04-25 2005-03-04 Pfizer Uso de un agonista para el receptor 5-ht2c para preparar un medicamento util en el tratamiento de la incontinencia urinaria provocada por estres, con la condicion de que el agonista no sea 1-[6-cloro-5-(trifluorometil)-2-piridinil]piperazina (org-129
US7728155B2 (en) 2003-10-24 2010-06-01 Wyeth Llc Dihydrobenzofuranyl alkanamines and methods for using same as cns agents
WO2005053688A1 (en) 2003-11-26 2005-06-16 Alcon, Inc. Substituted furo[2,3-g] indazoles for the treatment of glaucoma
US7338972B1 (en) 2003-12-15 2008-03-04 Alcon, Inc. Substituted 1-alkylamino-1H-indazoles for the treatment of glaucoma
US7129257B1 (en) 2003-12-15 2006-10-31 Alcon, Inc. Pyrazolo[3,4- e]benzoxazoles for the treatment of glaucoma
WO2005058911A2 (en) 2003-12-15 2005-06-30 Alcon, Inc. Substituted [1,4]oxazino[2,3-g]indazoles for the treatment of glaucoma
CA2559408C (en) 2004-03-15 2014-05-13 Ptc Therapeutics, Inc. Carboline derivatives useful in the inhibition of angiogenesis
US8076352B2 (en) 2004-03-15 2011-12-13 Ptc Therapeutics, Inc. Administration of carboline derivatives useful in the treatment of cancer and other diseases
US7767689B2 (en) 2004-03-15 2010-08-03 Ptc Therapeutics, Inc. Carboline derivatives useful in the treatment of cancer
US8076353B2 (en) 2004-03-15 2011-12-13 Ptc Therapeutics, Inc. Inhibition of VEGF translation
JP2008503482A (ja) 2004-06-18 2008-02-07 ワイス ６−アルキル−５−アリールスルホニル−ジヒドロフェナントリジンの製造方法
US8685924B2 (en) 2004-08-25 2014-04-01 Takeda Pharmaceutical Company Limited Preventives/remedies for stress urinary incontinence and method of screening the same
GT200500317A (es) 2004-11-05 2006-10-27 Proceso para preparar compuestos de quinolina y productos obtenidos de los mismos
US7425572B2 (en) 2004-12-08 2008-09-16 Alcon, Inc. Use of dioxindoindazoles and dioxoloindazoles for treating glaucoma
AR054849A1 (es) 2005-07-26 2007-07-18 Wyeth Corp Diazepinoquinolinas, sintesis de las mismas, e intermediarios para obtenerlas
KR101503681B1 (ko) * 2006-01-19 2015-03-19 아더시스 인코포레이티드 세로토닌 5-ｈｔ2ｃ 수용체 리간드로서의 티오페닐 및 피롤릴 아제핀 및 이의 용도
EP2742936A1 (en) 2006-05-16 2014-06-18 Takeda Pharmaceutical Company Limited Fused heterocyclic compound and use thereof
CA2666193A1 (en) 2006-08-08 2008-02-14 Sanofi-Aventis Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, process for preparing them, medicaments comprising these compounds, and their use
WO2008112280A1 (en) 2007-03-12 2008-09-18 Intra-Cellular Therapies, Inc. Substituted heterocycle fused gamma-carbolines synthesis
MX354786B (es) 2007-06-04 2018-03-21 Synergy Pharmaceuticals Inc Agonistas de guanilato ciclasa utiles para el tratamiento de trastornos gastrointestinales, inflamacion, cancer y otros trastornos.
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
US20100266504A1 (en) 2007-11-15 2010-10-21 Takahiro Matsumoto Condensed pyridine derivative and use thereof
CA2727055C (en) 2008-01-11 2016-12-20 Albany Molecular Research, Inc. (1-azinone) -substituted pyridoindoles as mch antagonists
PL2262505T3 (pl) * 2008-03-12 2015-04-30 Intra Cellular Therapies Inc Podstawione heterocykliczne skondensowane gamma-karboliny w postaci stałej
US8598119B2 (en) 2008-05-27 2013-12-03 Intra-Cellular Therapies, Inc. Methods and compositions for sleep disorders and other disorders
AU2015218433B2 (en) * 2008-05-27 2017-07-27 Intra-Cellular Therapies, Inc. Methods and compositions for sleep disorders and other disorders
EP3239170B1 (en) 2008-06-04 2019-03-20 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
UY31968A (es) 2008-07-09 2010-01-29 Sanofi Aventis Nuevos derivados heterocíclicos, sus procesos para su preparación, y sus usos terapéuticos
EP3241839B1 (en) 2008-07-16 2019-09-04 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
TW201018694A (en) * 2008-09-29 2010-05-16 Abbott Lab Indole and indoline derivatives and methods of use thereof
US9625475B2 (en) * 2008-09-29 2017-04-18 Abbvie Inc. Indole and indoline derivatives and methods of use thereof
WO2010068601A1 (en) 2008-12-08 2010-06-17 Sanofi-Aventis A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof
WO2011003007A1 (en) * 2009-07-01 2011-01-06 Albany Molecular Research, Inc. Azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine mch-1 antagonists, methods of making, and use thereof
US8618299B2 (en) * 2009-07-01 2013-12-31 Albany Molecular Research, Inc. Azinone-substituted azapolycycle MCH-1 antagonists, methods of making, and use thereof
WO2011003005A1 (en) * 2009-07-01 2011-01-06 Albany Molecular Research, Inc. Azinone-substituted azepino[b]indole and pyrido-pyrrolo-azepine mch-1 antagonists, methods of making, and use thereof
WO2011003021A1 (en) * 2009-07-01 2011-01-06 Albany Molecular Research, Inc. Azinone-substituted azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine mch-1 antagonists, methods of making, and use thereof
AU2010273732A1 (en) 2009-07-14 2012-02-09 Albany Molecular Research, Inc. 5-HT3 receptor modulators, methods of making, and use thereof
EP2470552B1 (en) 2009-08-26 2013-11-13 Sanofi Novel crystalline heteroaromatic fluoroglycoside hydrates, pharmaceuticals comprising these compounds and their use
US8575186B2 (en) 2009-10-05 2013-11-05 Albany Molecular Research, Inc. Epiminocycloalkyl[b] indole derivatives as serotonin sub-type 6 (5-HT6) modulators and uses thereof
US20120253036A1 (en) 2009-12-11 2012-10-04 Yukinori Nagakura Agent for treating fibromyalgia
US9040519B2 (en) 2010-02-18 2015-05-26 Medivation Technologies, Inc. Fused tetracyclic pyrido [4,3-B] indole and pyrido [3,4-B] indole derivatives and methods of use
US9034865B2 (en) 2010-02-18 2015-05-19 Medivation Technologies, Inc. Pyrido [4,3-B] indole and pyrido [3,4-B] indole derivatives and methods of use
WO2011103460A1 (en) * 2010-02-18 2011-08-25 Medivation Technologies, Inc. Fused tetracyclic pyrido[4,3-b]indole and pyrido[3,4-b]ondole derivatives and methods of use
JP5894574B2 (ja) 2010-04-22 2016-03-30 イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． 有機化合物
WO2012030953A1 (en) 2010-09-01 2012-03-08 Arena Pharmaceuticals, Inc. 5-ht2c receptor agonists in the treatment of disorders ameliorated by reduction of norepinephrine level
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
WO2012088124A2 (en) 2010-12-21 2012-06-28 Albany Molecular Research, Inc. Tetrahydro-azacarboline mch-1 antagonists, methods of making, and uses thereof
US8697700B2 (en) 2010-12-21 2014-04-15 Albany Molecular Research, Inc. Piperazinone-substituted tetrahydro-carboline MCH-1 antagonists, methods of making, and uses thereof
EP2668191A4 (en) 2011-01-19 2014-08-20 Albany Molecular Res Inc BENZOFURO- [3,2-C-] PYRIDINES AND RELATED ANALOGS AS SEROTONIN-SUBTYPE-6 (5-HT6) MODULATORS FOR THE TREATMENT OF ADIPOSITAS, METABOLISM SYNDROME, COGNITION AND SCHIZOPHRENIA
US9434747B2 (en) 2011-02-18 2016-09-06 Medivation Technologies, Inc. Methods of treating diabetes
DK2681236T3 (en) 2011-03-01 2018-04-16 Synergy Pharmaceuticals Inc PROCEDURE FOR MANUFACTURING GUANYLATE CYCLASE-C-AGONISTS
EP2683701B1 (de) 2011-03-08 2014-12-24 Sanofi Mit benzyl- oder heteromethylengruppen substituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
US8828995B2 (en) 2011-03-08 2014-09-09 Sanofi Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
EP2683699B1 (de) 2011-03-08 2015-06-24 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
US8809324B2 (en) 2011-03-08 2014-08-19 Sanofi Substituted phenyl-oxathiazine derivatives, method for producing them, drugs containing said compounds and the use thereof
WO2012120056A1 (de) 2011-03-08 2012-09-13 Sanofi Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
US8901114B2 (en) 2011-03-08 2014-12-02 Sanofi Oxathiazine derivatives substituted with carbocycles or heterocycles, method for producing same, drugs containing said compounds, and use thereof
EP2683703B1 (de) 2011-03-08 2015-05-27 Sanofi Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
US8809325B2 (en) 2011-03-08 2014-08-19 Sanofi Benzyl-oxathiazine derivatives substituted with adamantane and noradamantane, medicaments containing said compounds and use thereof
US8828994B2 (en) 2011-03-08 2014-09-09 Sanofi Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
US9428506B2 (en) * 2012-04-14 2016-08-30 Intra-Cellular Therapies, Inc. Substituted pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalines for the treatment of nervous system disorders
JP6440625B2 (ja) 2012-11-14 2018-12-19 ザ・ジョンズ・ホプキンス・ユニバーシティー 精神***病を処置するための方法および組成物
EP2981266B1 (en) * 2013-03-04 2018-01-03 Daya CNS LLC Pentacyclic pyridoindolobenz[b,d]azepine derivatives and uses thereof
JP2016514671A (ja) 2013-03-15 2016-05-23 シナジー ファーマシューティカルズ インコーポレイテッド グアニル酸シクラーゼのアゴニストおよびその使用
WO2014145192A1 (en) 2013-03-15 2014-09-18 Intra-Cellular Therapies, Inc. Organic compounds
EP3004138B1 (en) 2013-06-05 2024-03-13 Bausch Health Ireland Limited Ultra-pure agonists of guanylate cyclase c, method of making and using same
WO2015066344A1 (en) 2013-11-01 2015-05-07 Arena Pharmaceuticals, Inc. 5-ht2c receptor agonists and compositions and methods of use
KR102373288B1 (ko) 2013-12-03 2022-03-10 인트라-셀룰라 써래피스, 인코퍼레이티드. 신규한 방법
CN111689966A (zh) 2014-04-04 2020-09-22 细胞内治疗公司 有机化合物
KR20170012209A (ko) 2014-04-04 2017-02-02 인트라-셀룰라 써래피스, 인코퍼레이티드. 유기 화합물
WO2016172496A1 (en) 2015-04-23 2016-10-27 Constellation Pharmaceuticals, Inc. Lsd1 inhibitors and uses thereof
IL296884B2 (en) * 2016-01-26 2024-05-01 Intra Cellular Therapies Inc Condensed heterocyclic converted gamma carbonyls for use in the treatment of central nervous system disorders
HUE055334T2 (hu) 2016-03-25 2021-11-29 Intra Cellular Therapies Inc Szerves vegyületek és azok alkalmazása központi idegrendszeri betegségek kezelésében vagy megelõzésében
JP6997718B2 (ja) * 2016-03-28 2022-01-18 イントラ－セルラー・セラピーズ・インコーポレイテッド 新規共結晶
WO2017172784A1 (en) 2016-03-28 2017-10-05 Intra-Cellular Therapies, Inc. Novel salts and crystals
US10682354B2 (en) 2016-03-28 2020-06-16 Intra-Cellular Therapies, Inc. Compositions and methods
US11331316B2 (en) 2016-10-12 2022-05-17 Intra-Cellular Therapies, Inc. Amorphous solid dispersions
FI3532459T3 (fi) 2016-10-26 2023-10-23 Constellation Pharmaceuticals Inc Lsd1-estäjiä ja niiden lääkinnällisiä käyttöjä
WO2018106916A1 (en) * 2016-12-07 2018-06-14 Concert Pharmaceuticals, Inc. Deuterated quinoxaline compounds
US10961245B2 (en) 2016-12-29 2021-03-30 Intra-Cellular Therapies, Inc. Substituted heterocycle fused gamma-carbolines for treatment of central nervous system disorders
JP6987868B2 (ja) * 2016-12-29 2022-01-05 イントラ−セルラー・セラピーズ・インコーポレイテッドIntra−Cellular Therapies, Inc. 有機化合物
CN116327770A (zh) 2017-03-24 2023-06-27 细胞内治疗公司 新组合物和方法
CN110636845A (zh) 2017-04-10 2019-12-31 雷迪博士实验室有限公司 卢美哌隆对甲苯磺酸盐的无定形形式和固体分散体
MX2020000967A (es) 2017-07-26 2020-09-28 Intra Cellular Therapies Inc Compuestos organicos.
CA3071119A1 (en) * 2017-07-26 2019-01-31 Intra-Cellular Therapies, Inc. Substituted heterocycle fused gamma-carbolines for treatment or prophylaxis of central nervous system disorders
US10513515B2 (en) 2017-08-25 2019-12-24 Biotheryx, Inc. Ether compounds and uses thereof
MX2020007271A (es) 2017-09-26 2020-08-17 Intra Cellular Therapies Inc Sales y cristales novedosos.
WO2019102240A1 (en) * 2017-11-27 2019-05-31 Egis Gyógyszergyár Zrt. Method for the manufacture of lumateperone and its salts
EP3733204A4 (en) 2017-12-27 2021-09-15 Takeda Pharmaceutical Company Limited THERAPEUTIC FOR EXERCISE INCONTINENCE AND STAIR INCONTINENCE
CA3094204A1 (en) 2018-03-16 2019-09-19 Intra-Cellular Therapies, Inc. Novel methods
CN112040940A (zh) 2018-03-23 2020-12-04 细胞内治疗公司 有机化合物
CA3102948A1 (en) 2018-06-08 2019-12-12 Intra-Cellular Therapies, Inc. Novel methods
WO2019241278A1 (en) 2018-06-11 2019-12-19 Intra-Cellular Therapies, Inc. Substituted heterocycle fused gamma-carbolines synthesis
WO2019246384A1 (en) 2018-06-21 2019-12-26 Aquestive Therapeutics, Inc. System and method for making personalized individual unit doses containing pharmaceutical actives
CN109100437A (zh) * 2018-07-22 2018-12-28 邯郸学院 仲胺类抗抑郁药物的质谱检测方法
WO2020023782A1 (en) 2018-07-27 2020-01-30 Biotheryx, Inc. Bifunctional compounds as cdk modulators
AU2019328528A1 (en) 2018-08-31 2021-03-18 Intra-Cellular Therapies, Inc. Novel methods
KR20210052472A (ko) 2018-08-31 2021-05-10 인트라-셀룰라 써래피스, 인코퍼레이티드. 신규한 방법
WO2020051317A1 (en) 2018-09-07 2020-03-12 Aquestive Therapeutics, Inc. Oral film compositions and dosage forms having precise active dissolution profiles
US20220024924A1 (en) 2018-11-27 2022-01-27 Teva Czech Industries S.R.O Solid state forms of lumateperone salts and processes for preparation of lumateperone and salts thereof
WO2020131895A1 (en) * 2018-12-17 2020-06-25 Intra-Cellular Therapies, Inc. Substituted heterocycle fused gamma-carbolines synthesis
US20220064166A1 (en) * 2018-12-17 2022-03-03 Intra-Cellular Therapies, Inc. Substituted heterocycle fused gamma-carbolines synthesis
WO2020131899A1 (en) * 2018-12-17 2020-06-25 Intra-Cellular Therapies, Inc. Organic compound
EP3897643B1 (en) * 2018-12-21 2023-11-15 Intra-Cellular Therapies, Inc. A pyridopyrroloquinoxaline compound and its medical use
JP2022518495A (ja) * 2019-01-23 2022-03-15 イントラ－セルラー・セラピーズ・インコーポレイテッド 嗜癖の治療方法
JP2022521789A (ja) 2019-02-27 2022-04-12 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 脳障害を治療するためのアゼピノ－インドール及び他の複素環化合物
CA3134674A1 (en) * 2019-04-04 2020-10-08 Intra-Cellular Therapies, Inc. Methods of treating neuropathic pain
US20210000822A1 (en) 2019-07-07 2021-01-07 Intra-Cellular Therapies, Inc. Novel methods
JP2022554293A (ja) 2019-11-01 2022-12-28 アクエスティブ セラピューティクス インコーポレイテッド プロドラッグ組成物及び治療方法
EP4058029A1 (en) 2019-11-14 2022-09-21 Aquestive Therapeutics, Inc. Multimodal compositions and methods of treatment
JP7261942B2 (ja) * 2019-12-11 2023-04-20 イントラ－セルラー・セラピーズ・インコーポレイテッド 有機化合物
EP4143329A2 (en) 2020-04-28 2023-03-08 Anwita Biosciences, Inc. Interleukin-2 polypeptides and fusion proteins thereof, and their pharmaceutical compositions and therapeutic applications
EP4227306A4 (en) * 2020-10-09 2024-02-28 Shujing Biopharma Co., Ltd HETEROCYCLIC SUBSTITUTED CONDENSED GAMMA-CARBOLINE DERIVATIVE, PREPARATION METHOD THEREFOR, RELATED INTERMEDIATE AND USE THEREOF
CN112062767B (zh) * 2020-10-20 2022-03-11 杭州科巢生物科技有限公司 一种卢美哌隆的制备方法及其中间体
CN116940351A (zh) 2021-01-15 2023-10-24 阿奎斯蒂弗医疗股份有限公司 前药组合物和治疗方法
WO2022192476A1 (en) 2021-03-09 2022-09-15 Aquestive Therapeutics, Inc. Dosage forms having equivalent biocomparable profiles
CN116444520A (zh) * 2022-01-14 2023-07-18 上海科技大学 并环哌啶类化合物及其制备方法和用途
CN114456149A (zh) * 2022-02-24 2022-05-10 中国科学技术大学 一种多巴胺drd2受体拮抗剂及其用途
WO2023178113A2 (en) * 2022-03-14 2023-09-21 Intra-Cellular Therapies, Inc. Organic compounds
WO2023178111A2 (en) * 2022-03-14 2023-09-21 Intra-Cellular Therapies, Inc. Organic compounds
WO2023225620A1 (en) 2022-05-18 2023-11-23 Intra-Cellular Therapies, Inc. Novel methods
WO2024145659A1 (en) 2022-12-30 2024-07-04 Intra-Cellular Therapies, Inc. Heterocycle fused gamma-carbolines acting on the serotonine 5-ht2a receptor

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3299078A (en) * 1962-10-01 1967-01-17 Smith Kline French Lab Pyrido [3', 4': 4, 5] pyrrolo [3, 2, 1-hi] indoles and-[3, 2, 1-ij] quinolines
US3813392A (en) 1969-06-09 1974-05-28 J Sellstedt Pyrrolo(1,2,3-alpha epsilon)quinoxalin-2(3h)-ones and related compounds
US3892746A (en) * 1969-06-09 1975-07-01 American Home Prod Pyrrolo{8 1,2,3-de{9 quinoxalin-2(3H)-ones and related compounds
US3891643A (en) * 1972-05-15 1975-06-24 American Home Prod Pyrrolo{8 1,2,3-de{9 quinoxalin-2-(3H)-ones and related compounds
US4238607A (en) 1972-06-19 1980-12-09 Endo Laboratories Inc. Pyridopyrrolo benzheterocycles
US4013652A (en) 1972-06-19 1977-03-22 Endo Laboratories, Inc. Pyridopyrrolobenzoxazine
US3914421A (en) 1972-06-19 1975-10-21 Endo Lab Pyridopyrrolobenzheterocycles for combatting depression
US4115577A (en) 1972-06-19 1978-09-19 Endo Laboratories, Inc. Pyridopyrrolobenzheterocycles
US4183936A (en) 1972-06-19 1980-01-15 Endo Laboratories, Inc. Pyridopyrrolobenzheterocycles
FR2213283A1 (en) 1973-11-15 1974-08-02 Inst Im Ordzhonikidze Pyrazino(1,2,3-ab)beta carbolines and homologues - antidepressants not acting by MAO inhibition
US4088647A (en) 1976-02-04 1978-05-09 Glushkov Robert Georgievich Pyrazino (1,2,3-ab)-β-carboline derivatives and salts thereof and method of preparing same
US4219550A (en) * 1978-11-09 1980-08-26 E. I. Du Pont De Nemours And Company Cis- and trans- octahydropyridopyrrolobenzheterocycles
DE3855147D1 (de) 1987-07-20 1996-05-02 Duphar Int Res 8,9-Anellierte 1,2,3,4-Tetrahydro-beta-carbolin-Derivate
US5328905A (en) 1987-07-20 1994-07-12 Duphar International Research B.V. 8,9-anellated-1,2,3,4-tetrahydro-β-carboline derivatives
EP0347980A1 (en) * 1988-06-20 1989-12-27 Duphar International Research B.V 8,9-Annelated beta-carbolines and 8,9-anelated-3,4-dihydro-beta-carbolines
US4997831A (en) 1988-09-01 1991-03-05 Glaxo Group Limited Lactam derivatives
US5223625A (en) 1988-12-22 1993-06-29 Duphar International Research B.V. Annelated indolo [3,2,-C]lactams
EP0377238A1 (en) * 1988-12-22 1990-07-11 Duphar International Research B.V New annelated indolo (3,2-c)-lactams
CA2011107A1 (en) 1990-02-28 1991-08-31 David E. Bays Lactam derivatives
US5512575A (en) 1991-08-15 1996-04-30 Zeneca Limited Methanoanthraceneyl methyl piperidinyl compounds
KR960705824A (ko) 1993-10-20 1996-11-08 아사이 이페이 인돌 유도체(Indole Derivative)
US5654139A (en) 1994-09-21 1997-08-05 The United States Of America As Represented By The Department Of Health And Human Services Allelic variation of the serotonin 5HT2c receptor
US5902815A (en) 1996-09-03 1999-05-11 Washington University Use of 5HT-2A serotonin agonists to prevent adverse effects of NMDA receptor hypofunction
US5908830A (en) 1996-10-31 1999-06-01 Merck & Co., Inc. Combination therapy for the treatment of diabetes and obesity
DE1071701T1 (de) 1998-04-14 2001-08-23 Arena Pharmaceuticals, Inc. Non-endogene, konstitutiv aktivierte humane serotonin-rezeptoren und kleine molekülmodulatoren davon
US6140509A (en) 1998-06-26 2000-10-31 Arena Pharmaceuticals, Inc. Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof
US6407092B1 (en) 1999-04-23 2002-06-18 Pharmacia & Upjohn Company Tetracyclic azepinoindole compounds
AR023574A1 (es) 1999-04-23 2002-09-04 Pharmacia & Upjohn Co Llc Compuestos de azepinindol tetraciclico,composiciones farmaceuticas y el uso de dichos compuestos para preparar un medicamento, e intermediarios
JP4762465B2 (ja) * 1999-06-15 2011-08-31 ブリストル−マイヤーズ スクイブ ファーマ カンパニー 置換複素環縮合ガンマーカルボリン

Also Published As

Publication number Publication date
CA2374239A1 (en) 2000-12-21
NO20016115D0 (no) 2001-12-14
AU5738000A (en) 2001-01-02
JP2003502336A (ja) 2003-01-21
WO2000077010A2 (en) 2000-12-21
ES2223536T3 (es) 2005-03-01
AU5737900A (en) 2001-01-02
BR0012411A (pt) 2002-04-16
USRE39680E1 (en) 2007-06-05
US20040209864A1 (en) 2004-10-21
ZA200109735B (en) 2004-01-27
MXPA01012970A (es) 2003-10-14
EP1189905B1 (en) 2004-09-29
EP1192165B1 (en) 2004-09-22
NZ516031A (en) 2003-10-31
NO20016116D0 (no) 2001-12-14
ES2223537T3 (es) 2005-03-01
ATE277055T1 (de) 2004-10-15
CA2381322A1 (en) 2000-12-21
CN1370169A (zh) 2002-09-18
US20060178362A1 (en) 2006-08-10
DE60014083D1 (de) 2004-10-28
US20040034015A1 (en) 2004-02-19
WO2000077002A1 (en) 2000-12-21
CN1370176A (zh) 2002-09-18
DE60014370D1 (de) 2004-11-04
US6552017B1 (en) 2003-04-22
BR0012086A (pt) 2002-04-02
JP4762465B2 (ja) 2011-08-31
DE60014079T2 (de) 2006-03-02
AR024377A1 (es) 2002-10-02
IL147109A0 (en) 2002-08-14
EP1189904B1 (en) 2004-09-22
ATE277928T1 (de) 2004-10-15
IL147108A0 (en) 2002-08-14
MXPA01012969A (es) 2003-10-14
NO20016116L (no) 2002-02-11
JP4916633B2 (ja) 2012-04-18
DE60014083T2 (de) 2006-03-02
NO20016128L (no) 2002-02-11
EP1189904A1 (en) 2002-03-27
DE60014079D1 (de) 2004-10-28
ATE277048T1 (de) 2004-10-15
HK1042480A1 (zh) 2002-08-16
NO20016128D0 (no) 2001-12-14
JP2003502331A (ja) 2003-01-21
US7081455B2 (en) 2006-07-25
JP2003502330A (ja) 2003-01-21
JP4863591B2 (ja) 2012-01-25
IL145998A0 (en) 2002-07-25
BR0012084A (pt) 2002-04-02
CA2373920A1 (en) 2000-12-21
US6548493B1 (en) 2003-04-15
US7238690B2 (en) 2007-07-03
EP1189905A1 (en) 2002-03-27
CN1371374A (zh) 2002-09-25
ES2228549T3 (es) 2005-04-16
WO2000077001A1 (en) 2000-12-21
AU5615900A (en) 2001-01-02
AR024378A1 (es) 2002-10-02
MXPA01012914A (es) 2004-04-21
EP1192165A2 (en) 2002-04-03
WO2000077010A3 (en) 2001-06-28
HK1043112A1 (zh) 2002-09-06
HK1042481A1 (zh) 2002-08-16
DE60014370T2 (de) 2006-02-09
US20040127482A1 (en) 2004-07-01
NO20016115L (no) 2002-02-12
TR200103658T2 (tr) 2002-06-21

Similar Documents

Publication Publication Date Title
AR024379A1 (es) Gamma-carbolinas fusionadas heterociclicas sustituidas
BG107863A (en) Substituted pyrroloquinolines and pyridoquinolines as serotonin agonists and antagonists
MXPA03005438A (es) Pirioindoles substituidos como agonistas y antagonistas de serotonina.
ATE509929T1 (de) Substituierte tricyclische gamma-carbolineals serotonin-rezeptor-agonisten und antagonisten
MX2019008690A (es) Compuestos espiro heterociclicos como inhibidores de magl.
BRPI0415657A (pt) derivados de alcanamina de diidrobenzofuranila como agonistas de 5ht2c
ES2132105T3 (es) 2-aminometil-cromanos como principios activos en farmacos para el tratamiento de enfermedades del sistema nervioso central.
AR054786A1 (es) (6-fluor-benzol(1,3) dioxolil)-morfolin-4-il-metanomas, moduladoras del receptor cb1
PA8597301A1 (es) Derivados de imidazol-4-il-etinil-piridina
MX2019015371A (es) Derivados de dihidro-pirrolo-piridina.
NO20032795D0 (no) Substituerte pyrazinokinoksalinderivater som serotonin reseptor agonister og antagonister
HUP0303316A2 (hu) Aril- és amino-aril-szubsztituált szerotoninreceptor agonista és antagonista ligandumok és ezeket tartalmazó gyógyszerkészítmények
CR6968A (es) Un nuevo compuesto derivado de la triptamina y sus analogos.
PE20050352A1 (es) Derivados de 7-indolilsulfonamidas y su preparacion como medicamentos
GB0311349D0 (en) Therapeutic agents, compositions, preparations and uses
ES2161243T3 (es) Imidazolo-quinoxalinonas para el tratamiento de enfermedades del sistema nervioso central.
ES2101646B1 (es) Nuevo compuesto derivado del cromeno.
DOP2001000251A (es) Antagonistas de receptores de taquiquinina zwitterionica.

Legal Events

Date Code Title Description
FA Abandonment or withdrawal