CN101445494A - 共轭的精神抑制药及其用途 - Google Patents

共轭的精神抑制药及其用途 Download PDF

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Publication number
CN101445494A
CN101445494A CNA200810190781XA CN200810190781A CN101445494A CN 101445494 A CN101445494 A CN 101445494A CN A200810190781X A CNA200810190781X A CN A200810190781XA CN 200810190781 A CN200810190781 A CN 200810190781A CN 101445494 A CN101445494 A CN 101445494A
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CN
China
Prior art keywords
residue
antipsychotic drug
acid
chemical
organic acid
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CNA200810190781XA
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English (en)
Chinese (zh)
Inventor
A·努德曼
A·雷哈里
I·吉-阿德
A·维兹曼
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Ramot at Tel Aviv University Ltd
Bar Ilan University
Original Assignee
Ramot at Tel Aviv University Ltd
Bar Ilan University
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 Ramot at Tel Aviv University Ltd, Bar Ilan University filed Critical Ramot at Tel Aviv University Ltd
Publication of CN101445494A publication Critical patent/CN101445494A/zh
Pending legal-status Critical Current

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    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
    • 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
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Cephalosporin Compounds (AREA)
CNA200810190781XA 2001-09-27 2002-09-29 共轭的精神抑制药及其用途 Pending CN101445494A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US32493601P 2001-09-27 2001-09-27
US60/324936 2001-09-27

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CNB028236009A Division CN100558365C (zh) 2001-09-27 2002-09-29 共轭的精神抑制药及其用途

Publications (1)

Publication Number Publication Date
CN101445494A true CN101445494A (zh) 2009-06-03

Family

ID=23265759

Family Applications (2)

Application Number Title Priority Date Filing Date
CNA200810190781XA Pending CN101445494A (zh) 2001-09-27 2002-09-29 共轭的精神抑制药及其用途
CNB028236009A Expired - Fee Related CN100558365C (zh) 2001-09-27 2002-09-29 共轭的精神抑制药及其用途

Family Applications After (1)

Application Number Title Priority Date Filing Date
CNB028236009A Expired - Fee Related CN100558365C (zh) 2001-09-27 2002-09-29 共轭的精神抑制药及其用途

Country Status (10)

Country Link
EP (2) EP1429844B1 (https=)
JP (3) JP4521187B2 (https=)
KR (4) KR20100097224A (https=)
CN (2) CN101445494A (https=)
AT (1) ATE541588T1 (https=)
CA (1) CA2461663A1 (https=)
ES (2) ES2399977T3 (https=)
IL (2) IL161083A0 (https=)
MX (1) MXPA04002912A (https=)
WO (1) WO2003026563A2 (https=)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4521187B2 (ja) * 2001-09-27 2010-08-11 ラモト アット テル アヴィヴ ユニヴァーシティ リミテッド コンジュゲートされた抗精神病薬およびこれらの使用
US7544681B2 (en) * 2001-09-27 2009-06-09 Ramot At Tel Aviv University Ltd. Conjugated psychotropic drugs and uses thereof
EP2272537A3 (en) 2005-06-07 2014-10-22 Ramot at Tel-Aviv University Ltd. Salts of conjugated psychotropic drugs and processes of preparing same
JP5284779B2 (ja) * 2005-06-07 2013-09-11 ラモット・アット・テル・アビブ・ユニバーシテイ・リミテッド コンジュゲート化された向精神薬の新規な塩およびその調製方法
CN101506188B (zh) * 2006-06-22 2014-01-15 雷蒙特亚特特拉维夫大学有限公司 作为具外周系统限制活性药物的五羟色胺再摄取抑制剂
US9278947B2 (en) 2006-06-22 2016-03-08 Ramot At Tel-Aviv University Ltd. Serotonin reuptake inhibitors as drugs having peripheral-system-restricted activity
EP2051735B1 (en) * 2006-07-17 2012-08-29 Ramot, at Tel Aviv University Ltd. Conjugates comprising a psychotropic drug or a gaba agonist and an organic acid and their use treating pain and other cns disorders
EP2101585A4 (en) * 2006-11-30 2011-06-15 Cenerx Biopharma Inc PIVAGABIN DIALKYLAMINOAL CYLTERS AS A MEDICAMENT FOR THE TREATMENT OF DISORDERS OF THE CENTRAL NERVOUS SYSTEM
WO2009101616A1 (en) 2008-02-11 2009-08-20 Ramot At Tel Aviv University Ltd. Novel conjugates for treating neurodegenerative diseases and disorders
MX2010014203A (es) 2008-06-20 2011-02-22 Astrazeneca Ab Derivados de dibenzotiazepina y sus usos - 424.
CN105330603A (zh) * 2008-10-08 2016-02-17 凯飞药业公司 Gaba偶联物及其使用方法
WO2011070579A1 (en) * 2009-12-09 2011-06-16 Biolinerx Ltd. Methods of improving cognitive functions
AU2014202425B2 (en) * 2009-12-31 2015-11-19 Kempharm, Inc. Amino acid conjugates of quetiapine, process for making and using the same
CN107714703A (zh) * 2009-12-31 2018-02-23 凯姆制药公司 喹硫平的氨基酸缀合物、其制备和使用方法
US8377929B2 (en) 2010-02-24 2013-02-19 Ramot At Tel-Aviv University Ltd. Crystalline forms of the tri-mesylate salt of perphenazine-GABA and process of producing the same
EP3476218A1 (en) 2010-03-11 2019-05-01 Kempharm, Inc. Fatty acid conjugates of quetiapine, process for making and using the same
WO2012038963A1 (en) 2010-09-22 2012-03-29 Ramot At Tel-Aviv University Ltd. An acid addition salt of a nortriptyline-gaba conjugate and a process of preparing same
CN111329865A (zh) * 2020-03-30 2020-06-26 华东理工大学 奋乃静在制备治疗子宫内膜癌的药物中的应用

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US3194733A (en) * 1961-04-26 1965-07-13 Olin Mathicson Chemical Corp Phenothiazine compositions and method of treating mental disorders
GB1460713A (en) * 1973-06-08 1977-01-06 Kefalas As 7-fluoro substituted phenothiazines method for preparation thereof and compositions bladed rotor for a gas turbine engine
US3947579A (en) 1974-06-03 1976-03-30 Nelson Research & Development Company Method and composition for potentiating neuroleptic drugs
US3978216A (en) * 1974-06-03 1976-08-31 Nelson Research & Development Company Method for treating schizophrenia and method and composition for potentiating neuroleptic drugs
US3956493A (en) * 1974-10-21 1976-05-11 E. R. Squibb & Sons, Inc. Long acting tranquilizing agent
US4084000A (en) 1975-07-16 1978-04-11 Nelson Research And Development Company Method of treating schizophrenia
US4129652A (en) 1976-08-16 1978-12-12 Nelson Research & Development Company Method for potentiating neuroleptic drugs
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GB1540842A (en) * 1976-08-25 1979-02-14 Kefalas As Phenothiazines
US5525727A (en) * 1982-05-18 1996-06-11 University Of Florida Brain-specific drug delivery
US5104858A (en) * 1988-09-29 1992-04-14 Yale University Sensitizing multidrug resistant cells to antitumor agents
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JP4521187B2 (ja) * 2001-09-27 2010-08-11 ラモト アット テル アヴィヴ ユニヴァーシティ リミテッド コンジュゲートされた抗精神病薬およびこれらの使用

Also Published As

Publication number Publication date
JP4521187B2 (ja) 2010-08-11
EP2275143A2 (en) 2011-01-19
ES2379544T3 (es) 2012-04-27
KR20120032547A (ko) 2012-04-05
EP2275143A3 (en) 2011-01-26
JP2005503423A (ja) 2005-02-03
EP1429844B1 (en) 2012-01-18
KR20090130150A (ko) 2009-12-17
JP2014015472A (ja) 2014-01-30
WO2003026563A9 (en) 2004-04-22
IL161083A0 (en) 2004-08-31
ATE541588T1 (de) 2012-02-15
WO2003026563A3 (en) 2004-03-18
EP1429844A4 (en) 2006-06-07
KR101238452B1 (ko) 2013-02-28
JP2010090170A (ja) 2010-04-22
CN100558365C (zh) 2009-11-11
EP1429844A2 (en) 2004-06-23
KR100996239B1 (ko) 2010-11-23
ES2399977T3 (es) 2013-04-04
CA2461663A1 (en) 2003-04-03
MXPA04002912A (es) 2004-07-05
IL202291A0 (en) 2011-07-31
CN1596141A (zh) 2005-03-16
EP2275143B1 (en) 2012-12-19
KR20040062554A (ko) 2004-07-07
KR20100097224A (ko) 2010-09-02
WO2003026563A2 (en) 2003-04-03

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Application publication date: 20090603