CN103717069B - 有机化合物 - Google Patents

有机化合物 Download PDF

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Publication number
CN103717069B
CN103717069B CN201280035785.5A CN201280035785A CN103717069B CN 103717069 B CN103717069 B CN 103717069B CN 201280035785 A CN201280035785 A CN 201280035785A CN 103717069 B CN103717069 B CN 103717069B
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compound
formula
disease
disorder
compounds
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English (en)
Chinese (zh)
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CN103717069A (zh
Inventor
P·李
Y·彭
J·托麦施
L·P·文诺格勒
Q·张
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Intra Cellular Therapies Inc
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Intra Cellular Therapies Inc
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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
    • C07D401/12—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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/243—Platinum; Compounds thereof
    • 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
    • A61P11/00—Drugs for disorders of the respiratory 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Inorganic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Virology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Hospice & Palliative Care (AREA)
  • Toxicology (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201280035785.5A 2011-06-24 2012-06-22 有机化合物 Active CN103717069B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
USPCT/US2011/041866 2011-06-24
PCT/US2011/041866 WO2012177263A1 (en) 2011-06-24 2011-06-24 Compounds and methods of prophylaxis and treatment regarding nictonic receptor antagonists
US201161501207P 2011-06-25 2011-06-25
US61/501,207 2011-06-25
PCT/US2012/043880 WO2012178112A1 (en) 2011-06-24 2012-06-22 Organic compounds

Publications (2)

Publication Number Publication Date
CN103717069A CN103717069A (zh) 2014-04-09
CN103717069B true CN103717069B (zh) 2018-06-05

Family

ID=47422974

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201280035785.5A Active CN103717069B (zh) 2011-06-24 2012-06-22 有机化合物

Country Status (13)

Country Link
US (4) US9469625B2 (enExample)
EP (1) EP2723173B1 (enExample)
JP (1) JP6087911B2 (enExample)
KR (1) KR20140036305A (enExample)
CN (1) CN103717069B (enExample)
AU (2) AU2012272680A1 (enExample)
BR (1) BR112013033306A2 (enExample)
CA (2) CA2840047A1 (enExample)
ES (1) ES2627338T3 (enExample)
IL (1) IL230036A (enExample)
MX (1) MX342322B (enExample)
RU (1) RU2610094C2 (enExample)
WO (3) WO2012177263A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012177263A1 (en) * 2011-06-24 2012-12-27 Intra-Cellular Therapies, Inc. Compounds and methods of prophylaxis and treatment regarding nictonic receptor antagonists
US11491150B2 (en) 2017-05-22 2022-11-08 Intra-Cellular Therapies, Inc. Organic compounds
WO2019152680A1 (en) * 2018-01-31 2019-08-08 Flagship Pioneering Innovations V, Inc. Methods and compositions for treating cancer using chrna6 inhibitors
WO2020146384A1 (en) 2019-01-07 2020-07-16 Intra-Cellular Therapies, Inc. Organic compounds
WO2021008565A1 (zh) * 2019-07-16 2021-01-21 清华大学 乙酰胆碱通路调节剂在治疗癌症中的用途
EP4238970A1 (en) * 2022-03-03 2023-09-06 InterAx Biotech AG Modulators of ackr3 and uses thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009112459A1 (en) * 2008-03-11 2009-09-17 Neurosearch A/S Novel 1,2,3-triazole derivatives useful as modulators of nicotinic acetylcholine receptors
US20100179186A1 (en) * 2008-10-10 2010-07-15 University Of Kentucky Research Foundation USE OF A NOVEL ALPHA-7 nAChR ANTAGONIST TO SUPPRESS PATHOGENIC SIGNAL TRANSDUCTION IN CANCER AND AIDS

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US6953855B2 (en) * 1998-12-11 2005-10-11 Targacept, Inc. 3-substituted-2(arylalkyl)-1-azabicycloalkanes and methods of use thereof
PE20021019A1 (es) * 2001-04-19 2002-11-13 Upjohn Co Grupos azabiciclicos sustituidos
ES2338539T3 (es) * 2001-11-01 2010-05-10 Icagen, Inc. Pirazolamidas para uso en el tratamiento del dolor.
BR0315056A (pt) 2002-11-01 2005-08-16 Pharmacia & Upjohn Co Llc Compostos tendo tanto atividade agonista nicotìnica de alfa7 quanto atividade antagonista de 5ht3 para o tratamento de doenças do sistema nervoso central
MXPA05007689A (es) * 2003-01-22 2005-09-30 Pharmacia & Upjohn Co Llc Tratamiento de enfermedades con agonistas completos del receptor alfa-7 de nach.
US7135575B2 (en) * 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
JP2006525355A (ja) * 2003-05-01 2006-11-09 アボット・ラボラトリーズ ナトリウムチャンネルモジュレーターとしてのピラゾール−アミドおよびスルホンアミド
US20040220170A1 (en) * 2003-05-01 2004-11-04 Atkinson Robert N. Pyrazole-amides and sulfonamides as sodium channel modulators
EP1638944A1 (en) * 2003-06-12 2006-03-29 Eli Lilly And Company Tachykinin receptor antagonists
WO2012177263A1 (en) 2011-06-24 2012-12-27 Intra-Cellular Therapies, Inc. Compounds and methods of prophylaxis and treatment regarding nictonic receptor antagonists

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009112459A1 (en) * 2008-03-11 2009-09-17 Neurosearch A/S Novel 1,2,3-triazole derivatives useful as modulators of nicotinic acetylcholine receptors
US20100179186A1 (en) * 2008-10-10 2010-07-15 University Of Kentucky Research Foundation USE OF A NOVEL ALPHA-7 nAChR ANTAGONIST TO SUPPRESS PATHOGENIC SIGNAL TRANSDUCTION IN CANCER AND AIDS

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Discovery of novel alpha7 nicotinic receptor antagonists;Youyi Peng等;《Bioorganic & Medicinal Chemistry Letters 20》;20100625;第4825、4827页 *
Ligand-Induced Conformational Change in the a7 Nicotinic Receptor Ligand Binding Domain;Richard H. Henchman等;《Biophysical Journal》;20050430;第88卷(第4期);第2564-2576页 *

Also Published As

Publication number Publication date
US20160237061A1 (en) 2016-08-18
WO2012177263A1 (en) 2012-12-27
WO2012178112A1 (en) 2012-12-27
AU2012272646A1 (en) 2014-02-20
US9708294B2 (en) 2017-07-18
MX342322B (es) 2016-09-23
MX2014000255A (es) 2014-08-21
WO2012178057A1 (en) 2012-12-27
US9469625B2 (en) 2016-10-18
IL230036A (en) 2016-10-31
US9452160B2 (en) 2016-09-27
JP6087911B2 (ja) 2017-03-01
AU2012272646B2 (en) 2016-09-08
CA2840047A1 (en) 2012-12-27
EP2723173B1 (en) 2017-04-19
US20140205596A1 (en) 2014-07-24
US20140205595A1 (en) 2014-07-24
CN103717069A (zh) 2014-04-09
KR20140036305A (ko) 2014-03-25
US9108949B2 (en) 2015-08-18
BR112013033306A2 (pt) 2016-08-16
RU2610094C2 (ru) 2017-02-07
JP2014517078A (ja) 2014-07-17
US20160008343A1 (en) 2016-01-14
EP2723173A1 (en) 2014-04-30
AU2012272680A1 (en) 2014-02-20
CA2840373A1 (en) 2012-12-27
ES2627338T3 (es) 2017-07-27
EP2723173A4 (en) 2015-02-18
RU2014102191A (ru) 2015-07-27

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