[go: up one dir, main page]

PE20061018A1 - Sales de adicion de acido de piperidin-4-ilamina del acido 4-(2,6-dicloro-benzoil-amino)-1h-pirazol-3-carboxilico como inhibidores de quinasa - Google Patents

Sales de adicion de acido de piperidin-4-ilamina del acido 4-(2,6-dicloro-benzoil-amino)-1h-pirazol-3-carboxilico como inhibidores de quinasa

Info

Publication number
PE20061018A1
PE20061018A1 PE2006000078A PE2006000078A PE20061018A1 PE 20061018 A1 PE20061018 A1 PE 20061018A1 PE 2006000078 A PE2006000078 A PE 2006000078A PE 2006000078 A PE2006000078 A PE 2006000078A PE 20061018 A1 PE20061018 A1 PE 20061018A1
Authority
PE
Peru
Prior art keywords
acid
salt
ilamine
pirazol
piperidin
Prior art date
Application number
PE2006000078A
Other languages
English (en)
Inventor
David Charles Rees
Gary Trewartha
Mladen Vinkovic
Paul Graham Wyatt
Original Assignee
Astex Therapeutics Ltd
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
Priority claimed from GB0501475A external-priority patent/GB0501475D0/en
Application filed by Astex Therapeutics Ltd filed Critical Astex Therapeutics Ltd
Publication of PE20061018A1 publication Critical patent/PE20061018A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or 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
    • C07D231/38Nitrogen atoms
    • C07D231/40Acylated on said nitrogen atom
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • 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
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)

Abstract

SE REFIERE A SALES DE ADICION DE ACIDO DE PIPERIDIN-4-ILAMINA DEL ACIDO 4-(2,6-DICLORO-BENZOIL-AMINO)-1H-PIRAZOL-3-CARBOXILICO, FORMANDOSE LA SAL CON UN ACIDO SELECCIONADO A PARTIR DE ACIDO METANSULFONICO Y ACIDO ACETICO Y MEZCLAS DE LOS MISMOS; SIENDO ESTA SAL SUSTANCIALMENTE CRISTALINA; LA SAL MESILATO ES ANHIDRA Y EXHIBE UN PICO ENDOTERMICO A 379-380°C CUANDO SE SOMETE A CALORIMETRIA DIFERENCIAL; Y LA SAL DE ACIDO ACETICO EXHIBE PICOS EXOTERMICOS A 231-232°C Y 292 A 293°C, Y ADEMAS CONTIENE UNA SOLA FORMA CRISTALINA Y NO MAS DEL 5% DE OTRAS FORMAS CRISTALINAS. TAMBIEN SE REFIERE A COMPUESTOS INTERMEDIARIOS Y UN PROCESO DE PREPARACION. ESTOS COMPUESTOS SON INHIBIDORES DE QUINASA CDK (CDK1 O CDK2) O QUINASA-3 DE SINTASA DE GLICOGENO, POR LO QUE INHIBEN EL CRECIMIENTO CELULAR ANORMAL Y SON UTILES EN EL TRATAMIENTO DE LINFOMA DE CELULAS-B
PE2006000078A 2005-01-21 2006-01-20 Sales de adicion de acido de piperidin-4-ilamina del acido 4-(2,6-dicloro-benzoil-amino)-1h-pirazol-3-carboxilico como inhibidores de quinasa PE20061018A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US64597305P 2005-01-21 2005-01-21
GB0501475A GB0501475D0 (en) 2005-01-22 2005-01-22 Pharmaceutical compounds

Publications (1)

Publication Number Publication Date
PE20061018A1 true PE20061018A1 (es) 2006-10-31

Family

ID=36129898

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2009001082A PE20091785A1 (es) 2005-01-21 2006-01-20 Sales de adicion de acido de piperidin-4-ilamida del acido 4-(2,6-dicloro-benzoil-amino)-1h-pirazol-3-carboxilico
PE2006000078A PE20061018A1 (es) 2005-01-21 2006-01-20 Sales de adicion de acido de piperidin-4-ilamina del acido 4-(2,6-dicloro-benzoil-amino)-1h-pirazol-3-carboxilico como inhibidores de quinasa

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2009001082A PE20091785A1 (es) 2005-01-21 2006-01-20 Sales de adicion de acido de piperidin-4-ilamida del acido 4-(2,6-dicloro-benzoil-amino)-1h-pirazol-3-carboxilico

Country Status (18)

Country Link
US (2) US8013163B2 (es)
EP (1) EP1846393B1 (es)
JP (1) JP5184892B2 (es)
KR (1) KR101344691B1 (es)
AR (1) AR054425A1 (es)
AU (1) AU2006207323B2 (es)
BR (1) BRPI0606594A2 (es)
CA (1) CA2593560C (es)
IL (1) IL184504A (es)
MA (1) MA29256B1 (es)
MX (1) MX2007008783A (es)
NO (1) NO340738B1 (es)
NZ (1) NZ556471A (es)
PE (2) PE20091785A1 (es)
RU (1) RU2410385C2 (es)
SA (1) SA06260465B1 (es)
TN (1) TNSN07277A1 (es)
WO (1) WO2006077426A2 (es)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0412259B1 (pt) 2003-07-22 2019-08-20 Astex Therapeutics Limited Compostos de 1H-pirazol 3,4-dissubstituídos como moduladores de quinases dependentes de ciclina (CDK), seus usos, processo para a preparação dos mesmos e composição farmacêutica
JP5475234B2 (ja) * 2005-01-21 2014-04-16 アステックス・セラピューティクス・リミテッド 医薬化合物
US20080139620A1 (en) * 2005-01-21 2008-06-12 Astex Therapeutics Limited Pyrazole Derivatives For The Inhibition Of Cdk's And Gsk's
AR054425A1 (es) * 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
AU2006207325B2 (en) * 2005-01-21 2012-08-16 Astex Therapeutics Limited Pharmaceutical compounds
US8404718B2 (en) * 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
AR052559A1 (es) * 2005-01-21 2007-03-21 Astex Therapeutics Ltd Derivados de pirazol para inhibir cdk's y gsk's
JP2008528469A (ja) * 2005-01-21 2008-07-31 アステックス・セラピューティクス・リミテッド ピラゾールキナーゼ阻害剤およびさらなる抗癌剤の組合せ剤
US20090036607A1 (en) * 2005-03-03 2009-02-05 Mitsubishi Rayon Co., Ltd. Polymer particle, resin composition containing same, and molded body
WO2006109075A2 (en) 2005-04-13 2006-10-19 Astex Therapeutics Limited Hydroxybenzamide derivatives and their use as inhibitors of hsp90
JP2009536187A (ja) * 2006-05-05 2009-10-08 アステックス・セラピューティクス・リミテッド 癌の処置のための4−(2,6−ジクロロ−ベンゾイルアミノ)−1h−ピラゾール−3−カルボン酸(1−メタンスルホニル−ピペリジン−4−イル)−アミド
EP2026805A1 (en) * 2006-05-08 2009-02-25 Astex Therapeutics Limited Pharmaceutical combinations of diazole derivatives for cancer treatment
US20100004243A1 (en) * 2006-07-14 2010-01-07 Astex Therapeutics Limited Pharmaceutical compounds
WO2008044045A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
EP2073803B1 (en) 2006-10-12 2018-09-19 Astex Therapeutics Limited Pharmaceutical combinations
EP2073804B1 (en) 2006-10-12 2017-09-13 Astex Therapeutics Limited Hydroxy-substituted benzoic acid amide compounds for use in the treatment of pain
GB0620259D0 (en) 2006-10-12 2006-11-22 Astex Therapeutics Ltd Pharmaceutical compounds
US7858663B1 (en) * 2007-10-31 2010-12-28 Pisgah Laboratories, Inc. Physical and chemical properties of thyroid hormone organic acid addition salts
EP2228378B1 (en) 2007-12-27 2015-09-09 Kissei Pharmaceutical Co., Ltd. Monosebacate of pyrazole derivative
UY32297A (es) * 2008-12-22 2010-05-31 Almirall Sa Sal mesilato de 5-(2-{[6-(2,2-difluoro-2-fenilitoxi) hexil]amino}-1-hidroxietil)-8-hidroxiquinolin-2( 1h)-ona como agonista del receptor b(beta)2 acrenérgico
PT3430010T (pt) 2016-03-17 2020-09-10 Hoffmann La Roche Derivado de 5-etiol-4-metil-pirazol-3-carboxamida com atividade de agonista de taar
US11077110B2 (en) 2016-03-18 2021-08-03 Tufts Medical Center Compositions and methods for treating and preventing metabolic disorders
JP7190425B2 (ja) 2016-08-23 2022-12-15 エーザイ・アール・アンド・ディー・マネジメント株式会社 肝細胞癌の治療のための併用療法
KR102517650B1 (ko) 2017-03-16 2023-04-05 에자이 알앤드디 매니지먼트 가부시키가이샤 유방암의 치료를 위한 조합물 요법

Family Cites Families (133)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2917432A (en) 1954-10-05 1959-12-15 Burroughs Wellcome Co Leukemia treatment
US3046301A (en) 1959-10-29 1962-07-24 Burroughs Wellcome Co Method of making chlorambucil
GB1354939A (en) 1971-10-28 1974-06-05 Ici Ltd Process for the manufacture of 1,1,2-triphenylalk-1-enes
US4005063A (en) 1973-10-11 1977-01-25 Abbott Laboratories [Des-gly]10 -GnRH nonapeptide anide analogs in position 6 having ovulation-inducing activity
GB1524747A (en) 1976-05-11 1978-09-13 Ici Ltd Polypeptide
US4282361A (en) 1978-03-16 1981-08-04 Massachusetts Institute Of Technology Synthesis for 7-alkylamino-3-methylpyrazolo [4,3-d]pyrimidines
DE2845574A1 (de) 1978-10-19 1980-04-24 Deutsches Krebsforsch Durch heterocyclische ringe oder alkylreste substituierte analoga von ccnu und verfahren zu deren herstellung
EP0100172B1 (en) 1982-07-23 1987-08-12 Imperial Chemical Industries Plc Amide derivatives
US4978672A (en) 1986-03-07 1990-12-18 Ciba-Geigy Corporation Alpha-heterocyclc substituted tolunitriles
JPS6425763A (en) 1987-04-24 1989-01-27 Mitsubishi Chem Ind Pyrazoles and insecticide and acaricide containing said pyrazoles as active ingredient
US5164196A (en) 1987-05-19 1992-11-17 Ventech Research, Inc. Crotoxin complex as cytotoxic agent
US5002755A (en) 1988-02-18 1991-03-26 Vanderbilt University Method of controlling nephrotoxicity of anti-tumor plaintum compounds
EP0531369A1 (de) 1990-05-26 1993-03-17 Byk Gulden Lomberg Chemische Fabrik Gmbh 1,4-dihydropyridine zur anwendung bei der überwindung von arzneimittelresistenzen
IL100110A0 (en) 1990-12-26 1992-08-18 American Cyanamid Co Insecticidal and synergistic miticidal compositions
SK44894A3 (en) 1991-10-18 1995-04-12 Monsanto Co Trisubstituted aromatic compounds, method of their preparation and fungicidal agents
ATE139900T1 (de) 1992-11-13 1996-07-15 Idec Pharma Corp Therapeutische verwendung von chimerischen und markierten antikörper gegen menschlichen b lymphozyt beschränkter differenzierung antigen für die behandlung von b-zell-lymphoma
PL175831B1 (pl) 1992-12-17 1999-02-26 Pfizer Pochodna pirazolu
US5773001A (en) 1994-06-03 1998-06-30 American Cyanamid Company Conjugates of methyltrithio antitumor agents and intermediates for their synthesis
ES2219670T3 (es) 1994-11-10 2004-12-01 Millennium Pharmaceuticals, Inc. Utilizacion de compuestos de pirazola para el tratamiento de la glomerulonefritis, cancer, ateroesclerosis o restenosis.
US5502068A (en) 1995-01-31 1996-03-26 Synphar Laboratories, Inc. Cyclopropylpyrroloindole-oligopeptide anticancer agents
US5675024A (en) 1995-11-22 1997-10-07 Allergan Aryl or heteroaryl amides of tetrahydronaphthalene, chroman, thiochroman and 1,2,3,4,-tetrahydroquinoline carboxylic acids, having an electron withdrawing substituent in the aromatic or heteroaromatic moiety, having retinoid-like biological activity
US5663357A (en) 1995-11-22 1997-09-02 Allergan Substituted heteroarylamides having retinoid-like biological activity
AU703203B2 (en) 1996-01-30 1999-03-18 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP0904076A1 (en) 1996-04-03 1999-03-31 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU716381B2 (en) 1996-04-03 2000-02-24 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JP2000507592A (ja) 1996-04-03 2000-06-20 メルク エンド カンパニー インコーポレーテッド ファルネシル―タンパク質トランスフェラーゼ阻害剤
HU224827B1 (hu) 1996-05-03 2006-02-28 Abbott Lab Új antiangiogén peptidek, azokat kódoló polinukleotidok, és eljárások angiogenezis gátlására
EP0915825B1 (en) 1996-06-21 2004-05-06 Allergan, Inc. Substituted tetrahydronaphthalene and dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity
TW523506B (en) 1996-12-18 2003-03-11 Ono Pharmaceutical Co Sulfonamide or carbamide derivatives and drugs containing the same as active ingredients
US6020357A (en) 1996-12-23 2000-02-01 Dupont Pharmaceuticals Company Nitrogen containing heteroaromatics as factor Xa inhibitors
ATE443698T1 (de) 1996-12-23 2009-10-15 Bristol Myers Squibb Pharma Co Stickstoffhaltige heterocyclen als faktor xa- hemmer
US6306393B1 (en) 1997-03-24 2001-10-23 Immunomedics, Inc. Immunotherapy of B-cell malignancies using anti-CD22 antibodies
KR100390612B1 (ko) 1997-04-25 2003-07-07 화이자 인코포레이티드 타입 5 시클릭 구아노신 3',5'-모노포스페이트포스포디에스테라제를 억제하는 성기능 장애 치료용피라졸로피리미디논 제조용 중간체의 제조 방법
CA2288787A1 (en) 1997-05-22 1998-11-26 G.D. Searle And Co. Pyrazole derivatives as p38 kinase inhibitors
ATE296805T1 (de) 1997-06-19 2005-06-15 Bristol Myers Squibb Pharma Co Inhibitoren des faktors xa mit einer neutralen gruppe mit p1-spezifität
IL135536A0 (en) 1997-12-19 2001-05-20 Schering Ag Ortho-anthranilamide derivatives and pharmaceutical compositions containing the same
WO1999032454A1 (en) 1997-12-22 1999-07-01 Du Pont Pharmaceuticals Company Nitrogen containing heteroaromatics with ortho-substituted p1's as factor xa inhibitors
WO1999067235A1 (en) 1998-06-25 1999-12-29 Sumitomo Pharmaceuticals Co., Ltd. Five-membered ring compounds
JP2000186092A (ja) 1998-12-22 2000-07-04 Kyowa Hakko Kogyo Co Ltd Ucn−01の製造法
WO2000039102A1 (en) 1998-12-23 2000-07-06 Du Pont Pharmaceuticals Company THROMBIN OR FACTOR Xa INHIBITORS
AU4327600A (en) 1999-04-02 2000-10-23 Du Pont Pharmaceuticals Company Aryl sulfonyls as factor xa inhibitors
ES2391550T3 (es) 1999-04-15 2012-11-27 Bristol-Myers Squibb Company Inhibidores cíclicos de la proteína tirosina quinasa
US6166244A (en) 1999-05-07 2000-12-26 Allergan Sales, Inc. Oxygen, sulfur and nitrogen substituted cyclohexene and cyclohexane derivatives having retinoid-like biological activity
AU5283600A (en) 1999-05-24 2000-12-12 Cor Therapeutics, Inc. Inhibitors of factor xa
FR2795726A1 (fr) 1999-06-30 2001-01-05 Aventis Cropscience Sa Nouveaux pyrazoles fongicides
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
WO2001014331A2 (en) 1999-08-24 2001-03-01 Regents Of The University Of California Non-quinoline inhibitors of malaria parasites
RU2002110295A (ru) 1999-09-17 2003-12-10 Милленниум Фармасьютикалс, Инк. (Us) Ингибиторы фактора Ха
BR0014076A (pt) 1999-09-17 2002-10-15 Millennium Pharm Inc Benzamidas e inibidores correlatos do fator xa
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
US6485907B1 (en) 2000-01-11 2002-11-26 Syngenta Participations Ag PCR-based detection of Rhizoctonia cerealis
HN2001000008A (es) 2000-01-21 2003-12-11 Inc Agouron Pharmaceuticals Compuesto de amida y composiciones farmaceuticas para inhibir proteinquinasas, y su modo de empleo
CA2399791A1 (en) 2000-02-11 2001-08-16 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases
AU2001245353A1 (en) 2000-02-29 2001-09-12 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
EP1264820A4 (en) 2000-03-14 2004-09-15 Fujisawa Pharmaceutical Co amide compounds
WO2001081345A1 (en) 2000-04-20 2001-11-01 Mitsubishi Pharma Corporation Aromatic amide compounds
JP2004509064A (ja) 2000-04-27 2004-03-25 アボット・ラボラトリーズ 置換フェニルファルネシルトランスフェラーゼ阻害剤
US6414013B1 (en) 2000-06-19 2002-07-02 Pharmacia & Upjohn S.P.A. Thiophene compounds, process for preparing the same, and pharmaceutical compositions containing the same background of the invention
WO2002000651A2 (en) 2000-06-27 2002-01-03 Bristol-Myers Squibb Pharma Company Factor xa inhibitors
KR20030059084A (ko) 2000-07-31 2003-07-07 스미스크라인 비참 피.엘.시. 카르복사미드 화합물 및 이것의 사람 11cby 수용체의길항제로서의 용도
CZ2003468A3 (cs) 2000-08-31 2004-05-12 Pfizeráproductsáinc Deriváty pyrazolu a jejich použití jako inhibitorů proteinkinázy
ES2242771T5 (es) 2000-09-15 2011-10-14 Vertex Pharmaceuticals Incorporated Compuestos de pirazol útiles como inhibidores de proteína quinasas.
EP1414804A1 (en) 2000-10-20 2004-05-06 Bristol-Myers Squibb Pharma Company Acylsemicarbazides and their use as cyclin dependent kinase (cdk) inhibitors
US6455559B1 (en) 2001-07-19 2002-09-24 Pharmacia Italia S.P.A. Phenylacetamido-pyrazole derivatives, process for their preparation and their use as antitumor agents
CN102250071A (zh) 2000-12-21 2011-11-23 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的吡唑化合物
DE10064823A1 (de) 2000-12-22 2002-06-27 Knoll Ag Integrinrezeptorliganden
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
GB0102687D0 (en) * 2001-02-02 2001-03-21 Pharmacia & Upjohn Spa Oxazolyl-pyrazole derivatives active as kinase inhibitors,process for their preparation and pharmaceutical compositions comprising them
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
MXPA03007783A (es) 2001-02-28 2005-08-16 Brian C Giles Metodo y formula para efecto anti-tumor y anti-metastatico.
BR0207996A (pt) 2001-03-05 2004-03-02 Du Pont Composto, método de controle de pragas invertebradas e composição para controle das mesmas
MXPA03006310A (es) 2001-03-16 2003-09-16 Pfizer Compuestos farmaceuticamente activos.
GB0106661D0 (en) 2001-03-16 2001-05-09 Pfizer Ltd Pharmaceutically active compounds
WO2002074298A1 (en) 2001-03-21 2002-09-26 Ono Pharmaceutical Co., Ltd. Il-6 production inhibitors
RU2344123C9 (ru) 2001-04-16 2009-05-20 Шеринг Корпорейшн 3,4-дизамещенные циклобутен-1,2-дионы как лиганды схс-хемокинового рецептора
US6905669B2 (en) 2001-04-24 2005-06-14 Supergen, Inc. Compositions and methods for reestablishing gene transcription through inhibition of DNA methylation and histone deacetylase
RU2332415C2 (ru) * 2001-04-27 2008-08-27 Вертекс Фармасьютикалз Инкорпорейтед Производные пиразола, полезные в качестве ингибиторов протеинкиназы
EP1480597A4 (en) 2001-05-11 2005-02-02 Burnham Inst SCREENING, DIAGNOSTIC AND THERAPY PROCEDURES IN CONNECTION WITH RIZ
WO2002094183A2 (en) 2001-05-18 2002-11-28 Tap Pharmaceutical Products Inc. A method for tumor treatment with fumagillol derivatives
BR0209912A (pt) 2001-05-21 2004-04-06 Du Pont Composto, método de controle de pragas invertebradas e composição para controle das mesmas
AU2002312370A1 (en) 2001-06-13 2002-12-23 Roland W. Burli Antipathogenic benzamide compounds
WO2003011287A1 (en) 2001-08-03 2003-02-13 Vertex Pharmaceuticals Incorporated Pyrazolon derivatives as inhibitors of gsk-3
AUPR738301A0 (en) 2001-08-30 2001-09-20 Starpharma Limited Chemotherapeutic agents
JP2005507875A (ja) 2001-08-31 2005-03-24 ユニバーシティ オブ コネチカット カンナビノイド受容体に作用する新規なピラゾール類似体
KR20100107509A (ko) 2001-09-14 2010-10-05 9222-9129 퀘벡 인코포레이티드 히스톤 데아세틸라아제의 억제제
HN2002000317A (es) * 2001-11-02 2003-05-21 Pfizer Inhibidores de pde9 para tratamiento de trastornos cardiovasculares
US6919359B2 (en) 2001-11-08 2005-07-19 Pfizer Inc Azabicyclic-substituted-heteroaryl compounds for the treatment of disease
WO2003048081A2 (en) 2001-12-04 2003-06-12 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
ES2251677T3 (es) 2002-01-22 2006-05-01 Warner-Lambert Company Llc 2-(piridin-2-ilamino)-pirido(2,3-d)pirimidin-7-onas.
US7205307B2 (en) 2002-02-14 2007-04-17 Icagen, Inc. Pyrimidines as novel openers of potassium ion channels
BR0308250A (pt) 2002-03-04 2005-01-11 Aton Pharma Inc Métodos de indução de diferenciação terminal
CA2478799C (en) 2002-03-12 2009-12-29 Merck & Co., Inc. Di-aryl substituted tetrazole modulators of metabotropic glutamate receptor-5
EP1348707B1 (en) 2002-03-28 2010-08-25 Ustav Experimentalni Botaniky AV CR, v.v.i. (Institute of Experimental Botany Academy of Sciences of the Czech Republic, PRO) Pyrazolo[4,3-d]pyrimidines, processes for their preparation and methods for therapy
US6995168B2 (en) 2002-05-31 2006-02-07 Euro-Celtique S.A. Triazaspiro compounds useful for treating or preventing pain
US7015227B2 (en) 2002-06-21 2006-03-21 Cgi Pharmaceuticals, Inc. Certain amino-substituted monocycles as kinase modulators
GB0218625D0 (en) 2002-08-10 2002-09-18 Astex Technology Ltd Pharmaceutical compounds
KR20050052500A (ko) 2002-09-19 2005-06-02 쉐링 코포레이션 사이클린 의존성 키나제 억제제로서의 이미다조피리딘
WO2004039795A2 (en) 2002-10-29 2004-05-13 Fujisawa Pharmaceutical Co., Ltd. Amide compounds for the treatment of hyperlipidemia
US20050026877A1 (en) 2002-12-03 2005-02-03 Novacea, Inc. Pharmaceutical compositions comprising active vitamin D compounds
US7144911B2 (en) 2002-12-31 2006-12-05 Deciphera Pharmaceuticals Llc Anti-inflammatory medicaments
US7202257B2 (en) 2003-12-24 2007-04-10 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
US7169797B2 (en) 2003-02-14 2007-01-30 Abbott Laboratories Protein-tyrosine phosphatase inhibitors and uses thereof
US7320989B2 (en) 2003-02-28 2008-01-22 Encysive Pharmaceuticals, Inc. Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists
AR043633A1 (es) 2003-03-20 2005-08-03 Schering Corp Ligandos de receptores de canabinoides
WO2004099127A1 (en) 2003-05-07 2004-11-18 Novo Nordisk A/S Novel compounds as kinase inhibitors
EP1625115A1 (en) 2003-05-09 2006-02-15 Pharmacia & Upjohn Company LLC Substituted pyrimidine derivatives
US20070167500A1 (en) 2003-06-27 2007-07-19 Takayuki Maruyama Remedy for urinary tract diseases
WO2005000309A2 (en) 2003-06-27 2005-01-06 Ionix Pharmaceuticals Limited Chemical compounds
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
BRPI0412259B1 (pt) 2003-07-22 2019-08-20 Astex Therapeutics Limited Compostos de 1H-pirazol 3,4-dissubstituídos como moduladores de quinases dependentes de ciclina (CDK), seus usos, processo para a preparação dos mesmos e composição farmacêutica
SE0303396D0 (sv) 2003-12-16 2003-12-16 Astrazeneca Ab Chemical compounds
CN1960731B (zh) 2004-02-20 2011-12-07 诺华疫苗和诊断公司 调节炎性和转移过程的方法
DK1725528T3 (da) 2004-03-11 2013-09-02 4Sc Ag Sulfonylpyrroler som hdac-inhibitorer
US20060084691A1 (en) 2004-10-18 2006-04-20 Bilal Piperdi Combined treatment with bortezomib and an epidermal growth factor receptor kinase inhibitor
JP5475234B2 (ja) 2005-01-21 2014-04-16 アステックス・セラピューティクス・リミテッド 医薬化合物
AR052559A1 (es) 2005-01-21 2007-03-21 Astex Therapeutics Ltd Derivados de pirazol para inhibir cdk's y gsk's
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
WO2008007113A2 (en) 2006-07-14 2008-01-17 Astex Therapeutics Limited Pharmaceutical combinations
US20080139620A1 (en) 2005-01-21 2008-06-12 Astex Therapeutics Limited Pyrazole Derivatives For The Inhibition Of Cdk's And Gsk's
AU2006207325B2 (en) 2005-01-21 2012-08-16 Astex Therapeutics Limited Pharmaceutical compounds
JP2008528469A (ja) 2005-01-21 2008-07-31 アステックス・セラピューティクス・リミテッド ピラゾールキナーゼ阻害剤およびさらなる抗癌剤の組合せ剤
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
EP1847531A4 (en) 2005-02-09 2009-04-22 Takeda Pharmaceutical PYRAZOLE DERIVATIVE
MX2007016508A (es) 2005-06-30 2008-03-04 Prosidion Ltd Agonistas del receptor acoplado a la proteina g.
JP2009536187A (ja) 2006-05-05 2009-10-08 アステックス・セラピューティクス・リミテッド 癌の処置のための4−(2,6−ジクロロ−ベンゾイルアミノ)−1h−ピラゾール−3−カルボン酸(1−メタンスルホニル−ピペリジン−4−イル)−アミド
EP2026805A1 (en) 2006-05-08 2009-02-25 Astex Therapeutics Limited Pharmaceutical combinations of diazole derivatives for cancer treatment
JP2009542608A (ja) 2006-06-29 2009-12-03 アステックス・セラピューティクス・リミテッド 医薬組合せ剤
US20100004243A1 (en) 2006-07-14 2010-01-07 Astex Therapeutics Limited Pharmaceutical compounds
WO2008007122A2 (en) 2006-07-14 2008-01-17 Astex Therapeutics Limited Combinations of pyrazole derivatives for the inhibition of cdks and gsk's
EP2046327A1 (en) 2006-07-21 2009-04-15 Astex Therapeutics Limited Medical use of cyclin dependent kinases inhibitors
EP2073803B1 (en) 2006-10-12 2018-09-19 Astex Therapeutics Limited Pharmaceutical combinations

Also Published As

Publication number Publication date
US8293767B2 (en) 2012-10-23
CA2593560A1 (en) 2006-07-27
JP5184892B2 (ja) 2013-04-17
NO340738B1 (no) 2017-06-06
AU2006207323B2 (en) 2012-06-07
KR101344691B1 (ko) 2013-12-26
US20110274616A1 (en) 2011-11-10
MX2007008783A (es) 2007-09-11
BRPI0606594A2 (pt) 2009-07-07
WO2006077426A3 (en) 2006-09-28
JP2008528470A (ja) 2008-07-31
US20090012124A1 (en) 2009-01-08
KR20070107050A (ko) 2007-11-06
EP1846393A2 (en) 2007-10-24
EP1846393B1 (en) 2020-02-19
WO2006077426A2 (en) 2006-07-27
TNSN07277A1 (en) 2008-12-31
NO20073957L (no) 2007-10-12
AU2006207323A1 (en) 2006-07-27
NZ556471A (en) 2010-12-24
AR054425A1 (es) 2007-06-27
US8013163B2 (en) 2011-09-06
CA2593560C (en) 2014-12-09
PE20091785A1 (es) 2009-12-16
IL184504A0 (en) 2007-10-31
RU2007131100A (ru) 2009-02-27
MA29256B1 (fr) 2008-02-01
RU2410385C2 (ru) 2011-01-27
SA06260465B1 (ar) 2010-06-20
IL184504A (en) 2015-10-29

Similar Documents

Publication Publication Date Title
PE20061018A1 (es) Sales de adicion de acido de piperidin-4-ilamina del acido 4-(2,6-dicloro-benzoil-amino)-1h-pirazol-3-carboxilico como inhibidores de quinasa
CL2021001991A1 (es) Compuestos 3-carbonilamino-5-ciclopentil-1h-pirazol que tienen actividad inhibitoria cdk2.
PH12020550644A1 (en) Crystalline forms of n-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide
MX2019004951A (es) Proceso para la preparacion de pirazolo[1,5-a]pirimidinas y sales de estas.
PE20211756A1 (es) FORMAS POLIMORFICAS NOVEDOSAS DE UN INHIBIDOR DE TGFß
DOP2019000030A (es) Inhibidores de cdk2/4/6
CU20110052A7 (es) Compuestos orgánicos
CY1122468T1 (el) Κρυσταλλικη μορφη διθειικου αναστολεα κινασης jak και μια μεθοδος παρασκευης αυτου
NZ599040A (en) 2,4-disubstituted pyrido[4,3-d]pyrimidin-5(6h)-one compounds for selective inhibitors of lrrk2 and syk kinases
NO20085331L (no) Pyrazolo[1,5-A]pyrimidiner som CDK-inhibitorer
CU20190086A7 (es) Compuestos de heteroarilo bicíclicos 6-6 fusionados útiles como inhibidores de lats
CY1115420T1 (el) Δικυκλικες ενωσεις και οι χρησεις τους ως διπλοι αναστολεις c-src/jak
UA129695C2 (uk) Спосіб отримання та кристалічні форми проміжного продукту в синтезі інгібітора mdm2
CL2008003810A1 (es) Compuestos derivados de 5-anilino imidazol[1,5-a]piridina o pirazina, inhibidores de la actividad mek quinasa; composiciones farmaceuticas que los contienen; y su uso para tratar trastornos hiperproliferativos y una enfermedad inflamatoria.
CO6491081A2 (es) Compuestosy metodos inhibidores de jak de pirazolopirimidina
AR103866A2 (es) Composición farmacéutica para la inhibición de la actividad cinasa her-2, compuesto, formas cristalinas aisladas de monohidrato de maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida, maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida anhidro y maleato parcialmente hidratado de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida y métodos para preparar (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida como una sal de maleato y maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida anhidro
CU20170087A7 (es) Formas cristalinas de 5-(4-ciclopropil-1 h-imidazol-1-il)-n-(6-(4-isopropil-4h-1 , 2, 4- triazol-3-il)piridin-2-il)-2-fluoro-4-metilbenzamida
JP2015514060A5 (es)
PE20080186A1 (es) Derivados 4,6-disustituidos de 2-metoxi-6-etilamino-pirimidina como antagonistas del receptor de prostaglandina d2
TN2010000131A1 (en) Polo-like kinase inhibitors
BRPI0912923A8 (pt) Composto que consiste de um oligonucleotídeo modificadpo composto de 12-30 nucleosídeos ligados, compostos que compreende um oligonucleotídeo modificado que compreende pelo menos 12 nucleosídeos ligados, composto que compreende um oligonucleotídeo modificado que compreende nucleosídeos ligados, e, uso de um composto
WO2012044727A3 (en) Manufacturing process for pyrimidine derivatives
NO20085099L (no) Puritonderivativer som HM74A agonister
MX376500B (es) Forma cristalina del inhibidor de la btk quinasa y método de preparación de la misma.
CY1116043T1 (el) Κρυσταλλικες μορφες υδροχλωρικου αλατος (4α-r,9α-s)-1-(1η-βενζοϊμιδαζολο-5-καρβονυλ)2,3,4,4α,9,9α-εξαϋδρο-1η-ινδενο[2,1-β]πυριδινο-6-καρβονιτριλιου και χρηση τους ως αναστολεις της hsd 1

Legal Events

Date Code Title Description
FC Refusal