KR20100097224A - 접합된 항-정신병 약물 및 그의 용도 - Google Patents

접합된 항-정신병 약물 및 그의 용도 Download PDF

Info

Publication number
KR20100097224A
KR20100097224A KR1020107016372A KR20107016372A KR20100097224A KR 20100097224 A KR20100097224 A KR 20100097224A KR 1020107016372 A KR1020107016372 A KR 1020107016372A KR 20107016372 A KR20107016372 A KR 20107016372A KR 20100097224 A KR20100097224 A KR 20100097224A
Authority
KR
South Korea
Prior art keywords
residues
group
acid
psychotic
chemical
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.)
Ceased
Application number
KR1020107016372A
Other languages
English (en)
Korean (ko)
Inventor
아브라함 누델만
아다 레파엘리
이릿 길-애드
아브라함 웨즈만
Original Assignee
라모트 앳 텔 아비브 유니버시티 리미티드
바-일란 유니버시티
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 라모트 앳 텔 아비브 유니버시티 리미티드, 바-일란 유니버시티 filed Critical 라모트 앳 텔 아비브 유니버시티 리미티드
Publication of KR20100097224A publication Critical patent/KR20100097224A/ko
Ceased legal-status Critical Current

Links

Images

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic 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
    • A61K31/5415Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/542Carboxylic acids, e.g. a fatty acid or an amino acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/55Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis

Landscapes

  • 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)
KR1020107016372A 2001-09-27 2002-09-29 접합된 항-정신병 약물 및 그의 용도 Ceased KR20100097224A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US32493601P 2001-09-27 2001-09-27
US60/324,936 2001-09-27

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
KR1020097024590A Division KR20090130150A (ko) 2001-09-27 2002-09-29 접합된 항-정신병 약물 및 그의 용도

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020127002565A Division KR101238452B1 (ko) 2001-09-27 2002-09-29 접합된 항-정신병 약물 및 그의 용도

Publications (1)

Publication Number Publication Date
KR20100097224A true KR20100097224A (ko) 2010-09-02

Family

ID=23265759

Family Applications (4)

Application Number Title Priority Date Filing Date
KR1020107016372A Ceased KR20100097224A (ko) 2001-09-27 2002-09-29 접합된 항-정신병 약물 및 그의 용도
KR1020127002565A Expired - Fee Related KR101238452B1 (ko) 2001-09-27 2002-09-29 접합된 항-정신병 약물 및 그의 용도
KR1020047004581A Expired - Fee Related KR100996239B1 (ko) 2001-09-27 2002-09-29 접합된 항-정신병 약물 및 그의 용도
KR1020097024590A Ceased KR20090130150A (ko) 2001-09-27 2002-09-29 접합된 항-정신병 약물 및 그의 용도

Family Applications After (3)

Application Number Title Priority Date Filing Date
KR1020127002565A Expired - Fee Related KR101238452B1 (ko) 2001-09-27 2002-09-29 접합된 항-정신병 약물 및 그의 용도
KR1020047004581A Expired - Fee Related KR100996239B1 (ko) 2001-09-27 2002-09-29 접합된 항-정신병 약물 및 그의 용도
KR1020097024590A Ceased KR20090130150A (ko) 2001-09-27 2002-09-29 접합된 항-정신병 약물 및 그의 용도

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

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL227699A (https=) 1957-09-11 1900-01-01
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
US4138484A (en) 1976-08-16 1979-02-06 Nelson Research & Development Company Method for treating schizophrenia and method and composition for potentiating neuroleptic drugs
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
JPH0672868A (ja) * 1992-08-26 1994-03-15 Maruha Corp 抗精神病薬
US5795909A (en) * 1996-05-22 1998-08-18 Neuromedica, Inc. DHA-pharmaceutical agent conjugates of taxanes
US6197764B1 (en) * 1997-11-26 2001-03-06 Protarga, Inc. Clozapine compositions and uses thereof
IL139975A0 (en) 2000-11-29 2002-02-10 Univ Ramot Anti proliferative drugs
CN1375287A (zh) * 2001-03-16 2002-10-23 王玉万 含氯氰碘柳胺或其钠盐的兽用混悬注射剂
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
CN101445494A (zh) 2009-06-03
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
WO2003026563A2 (en) 2003-04-03

Similar Documents

Publication Publication Date Title
US7939525B2 (en) Conjugated psychotropic drugs and uses thereof
KR101238452B1 (ko) 접합된 항-정신병 약물 및 그의 용도
JP5284779B2 (ja) 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
IL161083A (en) Conjugated anti-psychotic drugs of the phenothiazine family and uses thereof
AU2004201240B2 (en) Conjugated Psychotropic Drugs and Uses Thereof

Legal Events

Date Code Title Description
A107 Divisional application of patent
A201 Request for examination
PA0104 Divisional application for international application

Comment text: Divisional Application for International Patent

Patent event code: PA01041R01D

Patent event date: 20100721

PA0201 Request for examination
PG1501 Laying open of application
E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20101028

Patent event code: PE09021S01D

AMND Amendment
E601 Decision to refuse application
PE0601 Decision on rejection of patent

Patent event date: 20110530

Comment text: Decision to Refuse Application

Patent event code: PE06012S01D

Patent event date: 20101028

Comment text: Notification of reason for refusal

Patent event code: PE06011S01I

J201 Request for trial against refusal decision
PJ0201 Trial against decision of rejection

Patent event date: 20110630

Comment text: Request for Trial against Decision on Refusal

Patent event code: PJ02012R01D

Patent event date: 20110530

Comment text: Decision to Refuse Application

Patent event code: PJ02011S01I

Appeal kind category: Appeal against decision to decline refusal

Decision date: 20120920

Appeal identifier: 2011101004420

Request date: 20110630

AMND Amendment
PB0901 Examination by re-examination before a trial

Comment text: Amendment to Specification, etc.

Patent event date: 20110727

Patent event code: PB09011R02I

Comment text: Request for Trial against Decision on Refusal

Patent event date: 20110630

Patent event code: PB09011R01I

Comment text: Amendment to Specification, etc.

Patent event date: 20101227

Patent event code: PB09011R02I

E90F Notification of reason for final refusal
PE0902 Notice of grounds for rejection

Comment text: Final Notice of Reason for Refusal

Patent event date: 20110831

Patent event code: PE09021S02D

A107 Divisional application of patent
PA0104 Divisional application for international application

Comment text: Divisional Application for International Patent

Patent event code: PA01041R01D

Patent event date: 20120130

B601 Maintenance of original decision after re-examination before a trial
PB0601 Maintenance of original decision after re-examination before a trial
J301 Trial decision

Free format text: TRIAL DECISION FOR APPEAL AGAINST DECISION TO DECLINE REFUSAL REQUESTED 20110630

Effective date: 20120920

PJ1301 Trial decision

Patent event code: PJ13011S01D

Patent event date: 20120920

Comment text: Trial Decision on Objection to Decision on Refusal

Appeal kind category: Appeal against decision to decline refusal

Request date: 20110630

Decision date: 20120920

Appeal identifier: 2011101004420