AU2012245971A1 - A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation - Google Patents

A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation Download PDF

Info

Publication number
AU2012245971A1
AU2012245971A1 AU2012245971A AU2012245971A AU2012245971A1 AU 2012245971 A1 AU2012245971 A1 AU 2012245971A1 AU 2012245971 A AU2012245971 A AU 2012245971A AU 2012245971 A AU2012245971 A AU 2012245971A AU 2012245971 A1 AU2012245971 A1 AU 2012245971A1
Authority
AU
Australia
Prior art keywords
compound
cancer
crystalline form
solvent
process according
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.)
Abandoned
Application number
AU2012245971A
Other languages
English (en)
Other versions
AU2012245971A8 (en
Inventor
Suneel Manohar Babu Chennamsetty
Yogesh CHINCHWADE
Sivaramakrishnan Hariharan
Yogesh HULAWALE
Kishor JOSHI
Selvam PARAMASIVAN
Meenakshi Sivakumar
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.)
Piramal Enterprises Ltd
Original Assignee
Piramal Healthcare 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
Application filed by Piramal Healthcare Ltd filed Critical Piramal Healthcare Ltd
Publication of AU2012245971A1 publication Critical patent/AU2012245971A1/en
Publication of AU2012245971A8 publication Critical patent/AU2012245971A8/en
Abandoned legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical 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)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2012245971A 2011-04-21 2012-04-19 A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation Abandoned AU2012245971A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161477937P 2011-04-21 2011-04-21
US61/477,937 2011-04-21
PCT/IB2012/051967 WO2012143879A1 (en) 2011-04-21 2012-04-19 A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation

Publications (2)

Publication Number Publication Date
AU2012245971A1 true AU2012245971A1 (en) 2013-10-17
AU2012245971A8 AU2012245971A8 (en) 2013-11-07

Family

ID=46026953

Family Applications (2)

Application Number Title Priority Date Filing Date
AU2012245455A Abandoned AU2012245455A1 (en) 2011-04-21 2012-04-19 Insulin-Like Growth Factor-1 Receptor inhibitors
AU2012245971A Abandoned AU2012245971A1 (en) 2011-04-21 2012-04-19 A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation

Family Applications Before (1)

Application Number Title Priority Date Filing Date
AU2012245455A Abandoned AU2012245455A1 (en) 2011-04-21 2012-04-19 Insulin-Like Growth Factor-1 Receptor inhibitors

Country Status (9)

Country Link
US (3) US20140046059A1 (enExample)
EP (2) EP2699568A1 (enExample)
JP (1) JP2014514321A (enExample)
CN (1) CN103732592A (enExample)
AU (2) AU2012245455A1 (enExample)
CA (2) CA2833009A1 (enExample)
IL (1) IL228810A0 (enExample)
IN (1) IN2013MN02170A (enExample)
WO (3) WO2012145471A1 (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2014514321A (ja) * 2011-04-21 2014-06-19 メルク・シャープ・アンド・ドーム・コーポレーション インスリン様増殖因子1受容体阻害剤
WO2014002007A1 (en) * 2012-06-26 2014-01-03 Piramal Enterprises Limited Method of predicting or monitoring response to igf-1r and ir inhibitors using biomarkers
KR102196374B1 (ko) 2012-11-29 2020-12-31 케모센트릭스, 인크. Cxcr7 길항제
WO2014177915A1 (en) 2013-05-01 2014-11-06 Piramal Enterprises Limited Cancer combination therapy using imidazo[4,5-c]quinoline derivatives
CN104098498A (zh) * 2014-07-30 2014-10-15 天津市斯芬克司药物研发有限公司 一种吲唑类化合物及其制备方法
WO2016041953A1 (en) 2014-09-15 2016-03-24 Dmitry Gorilovsky A system comprising multiple digital cameras viewing a large scene
CN105218475A (zh) * 2015-10-15 2016-01-06 湖南华腾制药有限公司 1,2-吗啉盐酸盐的合成方法
CA3085481A1 (en) 2017-12-15 2019-06-20 Inthera Bioscience AG 1 -(piperidinocarbonylmethyl)-2-oxopiperazine derivatives for treating cancer
BR112021011222A2 (pt) 2018-12-12 2021-08-24 Chemocentryx, Inc. Inibidores de cxcr7 para o tratamento de câncer
CN113149941A (zh) * 2020-01-22 2021-07-23 中国科学院上海药物研究所 醚类化合物及其在防治糖尿病及代谢综合征中的药学用途
WO2025014774A1 (en) 2023-07-07 2025-01-16 Viridian Therapeutics, Inc. Methods of treating active and chronic thyroid eye disease

Family Cites Families (309)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3126375A (en) 1964-03-24 Chioacyl
US2789118A (en) 1956-03-30 1957-04-16 American Cyanamid Co 16-alpha oxy-belta1, 4-pregnadienes
US2990401A (en) 1958-06-18 1961-06-27 American Cyanamid Co 11-substituted 16alpha, 17alpha-substituted methylenedioxy steroids
US3048581A (en) 1960-04-25 1962-08-07 Olin Mathieson Acetals and ketals of 16, 17-dihydroxy steroids
US3749712A (en) 1970-09-25 1973-07-31 Sigma Tau Ind Farmaceuti Triamcinolone acetonide esters and process for their preparation
SE378110B (enExample) 1972-05-19 1975-08-18 Bofors Ab
US3996359A (en) 1972-05-19 1976-12-07 Ab Bofors Novel stereoisomeric component A of stereoisomeric mixtures of 2'-unsymmetrical 16,17-methylenedioxy steroid 21-acylates, compositions thereof, and method of treating therewith
SE378109B (enExample) 1972-05-19 1975-08-18 Bofors Ab
US4319039A (en) 1979-06-15 1982-03-09 Merck & Co., Inc. Preparation of ammonium salt of hypocholesteremic fermentation product
US4231938A (en) 1979-06-15 1980-11-04 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4294926A (en) 1979-06-15 1981-10-13 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4444784A (en) 1980-08-05 1984-04-24 Merck & Co., Inc. Antihypercholesterolemic compounds
DK149080C (da) 1980-06-06 1986-07-28 Sankyo Co Fremgangsmaade til fremstilling af derivater af ml-236b-carboxylsyre
JPS5889191A (ja) 1981-11-20 1983-05-27 Sankyo Co Ltd 3−ヒドロキシ−ml−236b誘導体の製造法
US5354772A (en) 1982-11-22 1994-10-11 Sandoz Pharm. Corp. Indole analogs of mevalonolactone and derivatives thereof
US4911165A (en) 1983-01-12 1990-03-27 Ethicon, Inc. Pliabilized polypropylene surgical filaments
US4681893A (en) 1986-05-30 1987-07-21 Warner-Lambert Company Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis
US4782084A (en) 1987-06-29 1988-11-01 Merck & Co., Inc. HMG-COA reductase inhibitors
US4885314A (en) 1987-06-29 1989-12-05 Merck & Co., Inc. Novel HMG-CoA reductase inhibitors
US4820850A (en) 1987-07-10 1989-04-11 Merck & Co., Inc. Process for α-C-alkylation of the 8-acyl group on mevinolin and analogs thereof
US5030447A (en) 1988-03-31 1991-07-09 E. R. Squibb & Sons, Inc. Pharmaceutical compositions having good stability
US5180589A (en) 1988-03-31 1993-01-19 E. R. Squibb & Sons, Inc. Pravastatin pharmaceuatical compositions having good stability
US4916239A (en) 1988-07-19 1990-04-10 Merck & Co., Inc. Process for the lactonization of mevinic acids and analogs thereof
EP0360390A1 (en) 1988-07-25 1990-03-28 Glaxo Group Limited Spirolactam derivatives
US5118853A (en) 1988-10-13 1992-06-02 Sandoz Ltd. Processes for the synthesis of 3-disubstituted aminoacroleins
US5290946A (en) 1988-10-13 1994-03-01 Sandoz Ltd. Processes for the synthesis of 3-(substituted indolyl-2-yl)propenaldehydes
WO1990005525A1 (en) 1988-11-23 1990-05-31 Pfizer Inc. Quinuclidine derivatives as substance p antagonists
US4929437A (en) 1989-02-02 1990-05-29 Merck & Co., Inc. Coenzyme Q10 with HMG-CoA reductase inhibitors
US5164372A (en) 1989-04-28 1992-11-17 Fujisawa Pharmaceutical Company, Ltd. Peptide compounds having substance p antagonism, processes for preparation thereof and pharmaceutical composition comprising the same
US5189164A (en) 1989-05-22 1993-02-23 Sandoz Ltd. Processes for the synthesis of syn-(E)-3,5-dihydroxy-7-substituted hept-6-enoic and heptanoic acids and derivatives and intermediates thereof
FI94339C (fi) 1989-07-21 1995-08-25 Warner Lambert Co Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi
PH27357A (en) 1989-09-22 1993-06-21 Fujisawa Pharmaceutical Co Pyrazole derivatives and pharmaceutical compositions comprising the same
IE903957A1 (en) 1989-11-06 1991-05-08 Sanofi Sa Aromatic amine compounds, their method of preparation and¹pharmaceutical compositions in which they are present
FR2654726B1 (fr) 1989-11-23 1992-02-14 Rhone Poulenc Sante Nouveaux derives de l'isoindolone et leur preparation.
FR2654725B1 (fr) 1989-11-23 1992-02-14 Rhone Poulenc Sante Nouveaux derives de l'isoindolone, leur preparation et les compositions pharmaceutiques qui les contiennent.
GB8929070D0 (en) 1989-12-22 1990-02-28 Fujisawa Pharmaceutical Co Peptide compounds,processes for preparation thereof and pharmaceutical composition comprising the same
US5232929A (en) 1990-11-28 1993-08-03 Pfizer Inc. 3-aminopiperidine derivatives and related nitrogen containing heterocycles and pharmaceutical compositions and use
UA41251C2 (uk) 1990-01-04 2001-09-17 Пфайзер, Інк. Гідровані азотвмісні гетероциклічні сполуки, похідні піперидину, фармацевтична композиція та спосіб пригнічення активності речовини р в організмі
WO1991012266A1 (fr) 1990-02-15 1991-08-22 Fujisawa Pharmaceutical Co., Ltd. Compose peptidique
US5420245A (en) 1990-04-18 1995-05-30 Board Of Regents, The University Of Texas Tetrapeptide-based inhibitors of farnesyl transferase
HUT62891A (en) 1990-06-01 1993-06-28 Pfizer Process for producing 3-amino-2-arylquinuclidine compounds and pharmaceuticql composition comprising such compounds
CA2086434C (en) 1990-07-23 1998-09-22 John A. Lowe, Iii Quinuclidine derivatives
CZ387492A3 (en) 1990-09-28 1994-02-16 Pfizer Analogs of non-aromatic hetero cycles containing nitrogen with a condensed ring, process of their preparation and use
GB9023116D0 (en) 1990-10-24 1990-12-05 Fujisawa Pharmaceutical Co Peptide compounds,processes for preparation thereof and pharmaceutical composition comprising the same
DK0498069T3 (da) 1990-12-21 1995-12-04 Fujisawa Pharmaceutical Co Ny anvendelse af peptidderivat
JPH0733385B2 (ja) 1991-01-10 1995-04-12 フアイザー・インコーポレイテツド 物質pの拮抗薬としてのn−アルキルキヌクリジニウム塩
US5242930A (en) 1991-02-11 1993-09-07 Merck Sharp & Dohme Ltd. Azabicyclic compounds, pharmaceutical compositions containing them and their use in therapy
JPH082901B2 (ja) 1991-03-01 1996-01-17 ファイザー・インコーポレーテッド 1−アザビシクロ[3.2.2ノナン−3−アミン誘導体類
US5747469A (en) 1991-03-06 1998-05-05 Board Of Regents, The University Of Texas System Methods and compositions comprising DNA damaging agents and p53
EP0581777A1 (en) 1991-03-26 1994-02-09 Pfizer Inc. Stereoselective preparation of substituted piperidines
FR2677361A1 (fr) 1991-06-04 1992-12-11 Adir Nouveaux peptides et pseudopeptides, derives de tachykinines, leur procede de preparation et les compositions pharmaceutiques qui les contiennent.
FR2676053B1 (fr) 1991-05-03 1993-08-27 Sanofi Elf Nouveaux composes dialkylenepiperidino et leurs enantiomeres, procede pour leur preparation et compositions pharmaceutiques les contenant.
FR2676055B1 (fr) 1991-05-03 1993-09-03 Sanofi Elf Composes polycycliques amines et leurs enantiomeres, procede pour leur preparation et compositions pharmaceutiques les contenant.
FR2676443B1 (fr) 1991-05-17 1993-08-06 Rhone Poulenc Rorer Sa Nouveaux derives de perhydroisoindole et leur preparation.
FR2676447B1 (fr) 1991-05-17 1993-08-06 Rhone Poulenc Rorer Sa Nouveaux derives du thiopyranopyrrole et leur preparation.
FR2676442B1 (fr) 1991-05-17 1993-08-06 Rhone Poulenc Rorer Sa Nouveau derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent.
FR2676446B1 (fr) 1991-05-17 1993-08-06 Rhone Poulenc Rorer Sa Nouveaux derives du thiopyranopyrrole, leur preparation et les compositions pharmaceutiques qui les contiennent.
WO1992020661A1 (en) 1991-05-22 1992-11-26 Merck & Co., Inc. N, n-diacylpiperazines
PL170513B1 (en) 1991-05-22 1996-12-31 Pfizer Method of obtaining novel derivatives of 3-amino quinuclidine
WO1992021677A1 (en) 1991-05-31 1992-12-10 Pfizer Inc. bibNUCLIDINE DERIVATIVES
GB9113219D0 (en) 1991-06-19 1991-08-07 Fujisawa Pharmaceutical Co Peptide compound,processes for preparation thereof and pharmaceutical composition comprising the same
PL170516B1 (en) 1991-06-20 1996-12-31 Pfizer Method of obtaining novel derivatives of fluoroalkoxy benzylaminic compounds of piperidine
TW202432B (enExample) 1991-06-21 1993-03-21 Pfizer
US5288730A (en) 1991-06-24 1994-02-22 Merck Sharp & Dohme Limited Azabicyclic compounds, pharmaceutical compositions containing them and their use in therapy
DE69208088T2 (de) 1991-07-05 1996-11-14 Merck Sharp & Dohme Aromatische verbindungen, diese enthaltende pharmazeutische zusammensetzungen und ihre therapeutische anwendung
EP0593559A1 (en) 1991-07-05 1994-04-27 MERCK SHARP & DOHME LTD. Aromatic compounds, pharmaceutical compositions containing them and their use in therapy
EP0536817A1 (en) 1991-07-05 1993-04-14 MERCK SHARP & DOHME LTD. Azabicyclic compounds as tachykinin antagonists
US5495047A (en) 1991-07-10 1996-02-27 Merck, Sharp & Dohme (Ltd.) Fused tricyclic compounds, pharmaceutical compositions containing them and their use in therapy
US5610183A (en) 1991-07-10 1997-03-11 Merck, Sharp & Dohme Ltd. Phenylglycine derivatives pharmaceutical compositions containing them and their use in therapy
MY110227A (en) 1991-08-12 1998-03-31 Ciba Geigy Ag 1-acylpiperindine compounds.
EP0528495A1 (en) 1991-08-20 1993-02-24 Merck Sharp & Dohme Ltd. Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them
PT533280E (pt) 1991-09-20 2001-01-31 Glaxo Group Ltd Novas utilizacoes medicas para antagonistas de taquiquinina
US5527808A (en) 1991-09-26 1996-06-18 Pfizer Inc. Fused tricyclic nitrogen containing heterocycles
JP2553020B2 (ja) 1991-11-07 1996-11-13 吉富製薬株式会社 キヌクリジン化合物およびその医薬用途
ATE161821T1 (de) 1991-11-12 1998-01-15 Pfizer Azyklische ethylendiaminderivate als 'substance p rezeptor' antagonisten
EP0545478A1 (en) 1991-12-03 1993-06-09 MERCK SHARP & DOHME LTD. Heterocyclic compounds as tachykinin antagonists
HU9203780D0 (en) 1991-12-12 1993-03-29 Sandoz Ag Stabilized pharmaceutical products of hmg-coa reductase inhibitor and method for producing them
GB9200535D0 (en) 1992-01-10 1992-02-26 Fujisawa Pharmaceutical Co New compound
GB9201179D0 (en) 1992-01-21 1992-03-11 Glaxo Group Ltd Chemical compounds
US5328927A (en) 1992-03-03 1994-07-12 Merck Sharpe & Dohme, Ltd. Hetercyclic compounds, processes for their preparation and pharmaceutical compositions containing them
JP2656702B2 (ja) 1992-03-23 1997-09-24 ファイザー製薬株式会社 ペプチド性キヌクリジン
FR2689888B1 (fr) 1992-04-10 1994-06-10 Rhone Poulenc Rorer Sa Nouveaux derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent.
WO1993021181A1 (en) 1992-04-15 1993-10-28 Merck Sharp & Dohme Limited Azacyclic compounds
GB2266529A (en) 1992-05-01 1993-11-03 Merck Sharp & Dohme Tetrahydroisoquinoline derivatives
CA2134964C (en) 1992-05-18 1997-12-30 Manoj C. Desai Bridged aza-bicyclic derivatives as substance p antagonists
GB9211193D0 (en) 1992-05-27 1992-07-08 Merck Sharp & Dohme Therapeutic agents
CA2099233A1 (en) 1992-06-29 1993-12-30 Conrad P. Dorn Morpholine and thiomorpholine tachykinin receptor antagonists
US5637699A (en) 1992-06-29 1997-06-10 Merck & Co., Inc. Process for preparing morpholine tachykinin receptor antagonists
US5719147A (en) 1992-06-29 1998-02-17 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
US5612336A (en) 1992-07-13 1997-03-18 Merck, Sharp & Dohme Ltd. Heterocyclic amide derivatives as tachykinin antagonists
CA2140343A1 (en) 1992-07-17 1994-02-03 Sean M. Sullivan Method and reagent for treatment of animal diseases
GB2268931A (en) 1992-07-22 1994-01-26 Merck Sharp & Dohme Azabicyclic tachykinin-receptor antagonists
ES2124318T3 (es) 1992-07-28 1999-02-01 Merck Sharp & Dohme Compuestos azaciclicos.
GB2269170A (en) 1992-07-29 1994-02-02 Merck Sharp & Dohme Azatricyclic tachykinin antagonists
WO1994003429A1 (en) 1992-07-31 1994-02-17 Merck Sharp & Dohme Limited Substituted amines as tachykinin receptor antagonists
AU4396193A (en) 1992-08-04 1994-03-03 Pfizer Inc. 3-benzylamino-2-phenyl-piperidine derivatives as substance p receptor antagonists
GB9216911D0 (en) 1992-08-10 1992-09-23 Merck Sharp & Dohme Therapeutic agents
DK0655055T3 (da) 1992-08-13 2001-01-02 Warner Lambert Co Tachykininantagonister
EP1114823A3 (en) 1992-08-19 2001-07-18 Pfizer Inc. Substituted benzylamino nitrogen containing non-aromatic heterocycles
US5387595A (en) 1992-08-26 1995-02-07 Merck & Co., Inc. Alicyclic compounds as tachykinin receptor antagonists
ATE161530T1 (de) 1992-09-04 1998-01-15 Takeda Chemical Industries Ltd Kondensierte heterozyklische verbindungen, deren herstellung und verwendung
AU4973693A (en) 1992-09-10 1994-03-29 Merck Sharp & Dohme Limited Alcohols and ethers with aromatic substituents as tachykinin-antagonists
GB9220286D0 (en) 1992-09-25 1992-11-11 Merck Sharp & Dohme Therapeutic agents
JP2656699B2 (ja) 1992-10-21 1997-09-24 ファイザー製薬株式会社 置換ベンジルアミノキヌクリジン
GB9222262D0 (en) 1992-10-23 1992-12-09 Merck Sharp & Dohme Therapeutic agents
GB9222486D0 (en) 1992-10-26 1992-12-09 Merck Sharp & Dohme Therapeutic agents
AU678409B2 (en) 1992-10-28 1997-05-29 Merck Sharp & Dohme Limited 4-arylmethyloxymethyl piperidines as tachykinin antagonists
JP2656700B2 (ja) 1992-10-28 1997-09-24 ファイザー製薬株式会社 置換キヌクリジン誘導体
US5554627A (en) 1992-10-30 1996-09-10 Merck, Sharp & Dohme Ltd. Tachykinin antagonists
KR950704311A (ko) 1992-11-12 1995-11-17 알렌 제이. 스피겔 물질 p 길항체로서의 퀴누클리딘 유도체(quinuclidine derivative as substance p antagonist)
US5261188A (en) 1992-11-23 1993-11-16 The Standard Products Company Belt weatherstrip with bulb
CA2150123C (en) 1992-12-10 2004-12-07 Harry R. Howard Aminomethylene substituted non-aromatic heterocycles
US5604260A (en) 1992-12-11 1997-02-18 Merck Frosst Canada Inc. 5-methanesulfonamido-1-indanones as an inhibitor of cyclooxygenase-2
AU682838B2 (en) 1992-12-14 1997-10-23 Merck Sharp & Dohme Limited 4-aminomethyl/thiomethyl/sulfonylmethyl-4-phenylpiperidines as tachykinin receptor antagonists
GB9226581D0 (en) 1992-12-21 1993-02-17 Merck Sharp & Dohme Therapeutic agents
CA2111902A1 (en) 1992-12-21 1994-06-22 Jack Beuford Campbell Antitumor compositions and methods of treatment
GB9300051D0 (en) 1993-01-04 1993-03-03 Merck Sharp & Dohme Therapeutic agents
ES2111288T3 (es) 1993-01-15 1998-03-01 Searle & Co Nuevos 3,4-diaril tiofenos y analogos de los mismos utiles como agentes antiinflamatorios.
EP0610793A1 (en) 1993-02-08 1994-08-17 Takeda Chemical Industries, Ltd. Tetracyclic morpholine derivatives and their use or analgesics
JPH08506823A (ja) 1993-02-18 1996-07-23 メルク シヤープ エンド ドーム リミテツド アザ環式化合物、該化合物を含む組成物及びタキキニン拮抗剤としての該化合物の使用
US5674889A (en) 1993-02-22 1997-10-07 Merck, Sharp & Dohme, Ltd. Aromatic compounds, compositions containing them and their use in therapy
WO1994019357A1 (en) 1993-02-23 1994-09-01 Merrell Dow Pharmaceuticals Inc. Farnesyl:protein transferase inhibitors as anticancer agents
US5298627A (en) 1993-03-03 1994-03-29 Warner-Lambert Company Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
DK0687268T3 (da) 1993-03-04 1998-10-12 Pfizer Spiroazacykliske derivater som substans P-antagonister
US5409944A (en) 1993-03-12 1995-04-25 Merck Frosst Canada, Inc. Alkanesulfonamido-1-indanone derivatives as inhibitors of cyclooxygenase
CA2118985A1 (en) 1993-04-02 1994-10-03 Dinesh V. Patel Heterocyclic inhibitors of farnesyl protein transferase
US5496833A (en) 1993-04-13 1996-03-05 Merck Sharp & Dohme Limited Piperidine tachykinin receptor antagonists
AU678023B2 (en) 1993-05-06 1997-05-15 Aventis Inc. Substituted pyrrolidin-3-yl-alkyl-piperidines useful as tachykinin antagonists
US5843941A (en) 1993-05-14 1998-12-01 Genentech, Inc. Ras farnesyl transferase inhibitors
US5602098A (en) 1993-05-18 1997-02-11 University Of Pittsburgh Inhibition of farnesyltransferase
IL109646A0 (en) 1993-05-19 1994-08-26 Pfizer Heteroatom substituted alkyl benzylamino-quinuclidines
US5380738A (en) 1993-05-21 1995-01-10 Monsanto Company 2-substituted oxazoles further substituted by 4-fluorophenyl and 4-methylsulfonylphenyl as antiinflammatory agents
WO1994029309A1 (en) 1993-06-07 1994-12-22 Merck & Co., Inc. Spiro-substituted azacycles as neurokinin antagonists
US5474995A (en) 1993-06-24 1995-12-12 Merck Frosst Canada, Inc. Phenyl heterocycles as cox-2 inhibitors
US5436265A (en) 1993-11-12 1995-07-25 Merck Frosst Canada, Inc. 1-aroyl-3-indolyl alkanoic acids and derivatives thereof useful as anti-inflammatory agents
GB9602877D0 (en) 1996-02-13 1996-04-10 Merck Frosst Canada Inc 3,4-Diaryl-2-hydroxy-2,5- dihydrofurans as prodrugs to cox-2 inhibitors
EP0634402A1 (en) 1993-07-14 1995-01-18 Takeda Chemical Industries, Ltd. Isochinolinone derivatives, their production and use
EP0708771B1 (en) 1993-07-15 1998-10-07 Pfizer Inc. Benzyloxyquinuclidines as substance p antagonists
TW365603B (en) 1993-07-30 1999-08-01 Rhone Poulenc Rorer Sa Novel perhydroisoindole derivatives, their preparation and pharmaceutical compositions which contain them
GB9315808D0 (en) 1993-07-30 1993-09-15 Merck Sharp & Dohme Therapeutic agents
GB9317987D0 (en) 1993-08-26 1993-10-13 Glaxo Group Ltd Chemical compounds
AU7082194A (en) 1993-09-17 1995-04-03 Pfizer Inc. Heteroarylamino and heteroarylsulfonamido substituted 3-benzylaminomethyl piperidines and related compounds
DE69433744T2 (de) 1993-09-17 2004-10-14 Pfizer Inc. 3-amino-5-carboxy-substituierte piperidine und 3-amino-4-carboxy-substituierte pyrrolidine als tachykinin-antagonisten
US5728830A (en) 1993-09-22 1998-03-17 Kyowa Hakko Kogyo Co., Ltd. Farnesyltransferase inhibitor
IL111002A (en) 1993-09-22 1998-09-24 Glaxo Group Ltd Piperidine derivatives their preparation and pharmaceutical compositions containing them
US5719148A (en) 1993-10-15 1998-02-17 Schering Corporation Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
IL111257A0 (en) 1993-10-15 1994-12-29 Schering Corp Tricyclic sulfonamide compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
US5661152A (en) 1993-10-15 1997-08-26 Schering Corporation Tricyclic sulfonamide compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
US5721236A (en) 1993-10-15 1998-02-24 Schering Corporation Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
IL111235A (en) 1993-10-15 2001-03-19 Schering Plough Corp Medicinal preparations for inhibiting protein G activity and for the treatment of malignant diseases, containing tricyclic compounds, some such new compounds and a process for the preparation of some of them
AU699043B2 (en) 1993-10-15 1998-11-19 Schering Corporation Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
WO1995011917A1 (en) 1993-10-25 1995-05-04 Parke, Davis & Company Substituted tetra- and pentapeptide inhibitors of protein:farnesyl transferase
WO1995011880A1 (en) 1993-10-27 1995-05-04 Merck Sharp & Dohme Limited Substituted amides as tachykinin antagonists
US5344991A (en) 1993-10-29 1994-09-06 G.D. Searle & Co. 1,2 diarylcyclopentenyl compounds for the treatment of inflammation
US5783593A (en) 1993-11-04 1998-07-21 Abbott Laboratories Inhibitors of squalene synthetase and protein farnesyltransferase
WO1995012572A1 (en) 1993-11-04 1995-05-11 Abbott Laboratories Cyclobutane derivatives as inhibitors of squalene synthetase and protein farnesyltransferase
CA2170766A1 (en) 1993-11-05 1995-05-11 Gary Louis Bolton Substituted di- and tripeptide inhibitors of protein:farnesyl transferase
US6403577B1 (en) 1993-11-17 2002-06-11 Eli Lilly And Company Hexamethyleneiminyl tachykinin receptor antagonists
US5466823A (en) 1993-11-30 1995-11-14 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides
IT1271462B (it) 1993-12-03 1997-05-28 Menarini Farma Ind Antagonisti delle tachichinine,procedimento per la loro preparazione e loro impiego in formulazioni farmaceutiche.
US5484799A (en) 1993-12-09 1996-01-16 Abbott Laboratories Antifungal dorrigocin derivatives
IL111960A (en) 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
WO1995017382A1 (en) 1993-12-21 1995-06-29 Eli Lilly And Company Non-peptide tachykinin receptor antagonists
ES2164758T3 (es) 1993-12-29 2002-03-01 Merck Sharp & Dohme Derivados de morfolina sustituidos y su uso como agentes terapeuticos.
ES2127946T3 (es) 1993-12-29 1999-05-01 Pfizer Antagonistas de neurocinina diazabiciclica.
EP0739336B1 (en) 1994-01-13 1998-08-26 MERCK SHARP & DOHME LTD. Gem-disubstituted azacyclic tachykinin antagonists
WO1995020575A1 (en) 1994-01-28 1995-08-03 Merck Sharp & Dohme Limited Aralkylamino substituted azacyclic therapeutic agents
US5393790A (en) 1994-02-10 1995-02-28 G.D. Searle & Co. Substituted spiro compounds for the treatment of inflammation
GB9402688D0 (en) 1994-02-11 1994-04-06 Merck Sharp & Dohme Therapeutic agents
US5610165A (en) 1994-02-17 1997-03-11 Merck & Co., Inc. N-acylpiperidine tachykinin antagonists
TW385308B (en) 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
WO1995024612A1 (de) 1994-03-07 1995-09-14 International Business Machines Corporation Verfahren und vorrichtung zur schnellen interpolation von zwischenwerten aus periodischen phasenverschobenen signalen und zur erkennung von defekten in einem drehkörper
CN1151156A (zh) 1994-03-15 1997-06-04 卫材株式会社 异戊二烯基转移酶抑制剂
FR2718136B1 (fr) 1994-03-29 1996-06-21 Sanofi Sa Composés aromatiques aminés, procédé pour leur obtention et compositions pharmaceutiques les contenant.
RU95104898A (ru) 1994-03-31 1996-12-27 Бристоль-Мейерз Сквибб Компани (US) Имидазолсодержащие ингибиторы фарнезид-протеинтрансферазы, способ лечения связанных с ней заболеваний
US5523430A (en) 1994-04-14 1996-06-04 Bristol-Myers Squibb Company Protein farnesyl transferase inhibitors
US5610145A (en) 1994-04-15 1997-03-11 Warner-Lambert Company Tachykinin antagonists
US5362718A (en) 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
IL113472A0 (en) 1994-04-29 1995-07-31 Lilly Co Eli Non-peptidyl tachykinin receptor antogonists
JPH10500944A (ja) 1994-05-05 1998-01-27 メルク シヤープ エンド ドーム リミテツド モルホリン誘導体及びタキキニンのアンタゴニストとしてのそれらの使用
SK142696A3 (en) 1994-05-07 1997-06-04 Boehringer Ingelheim Kg Amino acids derivative, method for preparation thereof, pharmaceutical compositions containing said compounds (ii) and their use
US5510510A (en) 1994-05-10 1996-04-23 Bristol-Meyers Squibb Company Inhibitors of farnesyl protein transferase
US5563255A (en) 1994-05-31 1996-10-08 Isis Pharmaceuticals, Inc. Antisense oligonucleotide modulation of raf gene expression
ATE206710T1 (de) 1994-06-06 2001-10-15 Warner Lambert Co Tachykinin (nk1) rezeptor antagonisten
EP0686629A3 (en) 1994-06-10 1999-02-10 Eli Lilly And Company Cyclohexyl tachykinine receptor antagonists
DE69507476D1 (de) 1994-06-10 1999-03-04 Rhone Poulenc Rorer Sa Farnesyl-transferase-inhibitoren, ihre herstellung und sie enthaltende pharmazeutische zusammensetzungen
US5571792A (en) 1994-06-30 1996-11-05 Warner-Lambert Company Histidine and homohistidine derivatives as inhibitors of protein farnesyltransferase
CN1067067C (zh) 1994-07-12 2001-06-13 伊莱利利公司 杂环速激肽受体拮抗物
CA2154116A1 (en) 1994-07-22 1996-01-23 Philip Arthur Hipskind 1-aryl-2-acetamidopentanone derivatives for use as tachykinin receptor antagonists
GB9415997D0 (en) 1994-08-08 1994-09-28 Merck Sharp & Dohme Therapeutic agents
GB9415996D0 (en) 1994-08-08 1994-09-28 Merck Sharp & Dohme Therapeutic agents
WO1996005529A1 (en) 1994-08-09 1996-02-22 Micron Optics, Inc. Temperature compensated fiber fabry-perot filters
TW432061B (en) 1994-08-09 2001-05-01 Pfizer Res & Dev Lactams
CA2155448A1 (en) 1994-08-11 1996-02-12 Katerina Leftheris Inhibitors of farnesyl protein transferase
EP0776884B1 (en) 1994-08-11 2000-01-05 Banyu Pharmaceutical Co., Ltd. Substituted amide derivative
AU3192495A (en) 1994-08-12 1996-03-07 Banyu Pharmaceutical Co., Ltd. N,n-disubstituted amic acid derivative
DK0777659T3 (da) 1994-08-15 2001-09-03 Merck Sharp & Dohme Morpholinderivater og deres anvendelse som terapeutiske midler
DE4429506B4 (de) 1994-08-19 2007-09-13 Degussa Gmbh Verfahren zur Extraktion natürlicher Carotinoid-Farbstoffe
DE4429653C2 (de) 1994-08-20 1997-04-03 Anton Dr More Konverter und Verfahren zum Frischen von Metallschmelzen insbesondere von Roheisen zu Stahl
AU693936B2 (en) 1994-08-25 1998-07-09 Merrell Pharmaceuticals Inc. Novel substituted piperidines useful for the treatment of allergic diseases
ATE158568T1 (de) 1994-08-29 1997-10-15 Akzo Nobel Nv Verfahren zur herstellung von quaternären diestern
GB9417956D0 (en) 1994-09-02 1994-10-26 Merck Sharp & Dohme Therapeutic agents
GB9418545D0 (en) 1994-09-15 1994-11-02 Merck Sharp & Dohme Therapeutic agents
US5457107A (en) 1994-09-16 1995-10-10 Merck & Co., Inc. Polymorphic form of a tachykinin receptor antagonist
ATE212981T1 (de) 1994-09-30 2002-02-15 Novartis Erfind Verwalt Gmbh 1-acyl-4-aliphatische aminopiperidin verbindungen
TW397825B (en) 1994-10-14 2000-07-11 Novartis Ag Aroyl-piperidine derivatives
FR2725986B1 (fr) 1994-10-21 1996-11-29 Adir Nouveaux derives de piperidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
EP0709375B1 (en) 1994-10-25 2005-05-18 AstraZeneca AB Therapeutic heterocycles
GB9421709D0 (en) 1994-10-27 1994-12-14 Zeneca Ltd Therapeutic compounds
JP4319251B2 (ja) 1994-11-22 2009-08-26 エヌエックスピー ビー ヴィ 半導体素子を有し導体トラックが形成されている基板が接着層により結合されている支持本体を有する半導体装置
EP0714891A1 (en) 1994-11-22 1996-06-05 Eli Lilly And Company Heterocyclic tachykinin receptor antagonists
FR2727411B1 (fr) 1994-11-30 1997-01-03 Rhone Poulenc Rorer Sa Nouveaux derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent
JPH10510261A (ja) 1994-12-09 1998-10-06 ワーナー−ランバート・カンパニー タンパク質:ファルネシルトランスフェラーゼの置換テトラーおよびペンタペプチド阻害剤
PE38997A1 (es) 1994-12-13 1997-10-02 Novartis Ag Antagonista de taquicinina
GB9426103D0 (en) 1994-12-23 1995-02-22 Merck Sharp & Dohme Therapeutic agents
CN1176652A (zh) 1995-01-09 1998-03-18 马格拉国际有限公司 胶乳表面的耐磨图象印刷
AU4437896A (en) 1995-01-12 1996-07-31 Glaxo Group Limited Piperidine derivatives having tachykinin antagonist activity
EP0794789A4 (en) 1995-01-12 1999-05-26 Univ Pittsburgh Inhibitors of prenyl transferases
FR2729390A1 (fr) 1995-01-18 1996-07-19 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2729951B1 (fr) 1995-01-30 1997-04-18 Sanofi Sa Nouveaux composes heterocycliques, procede pour leur preparation et compositions pharmaceutiques en contenant
FR2730492B1 (fr) 1995-02-09 1997-03-14 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2730491B1 (fr) 1995-02-09 1997-03-14 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
US5633272A (en) 1995-02-13 1997-05-27 Talley; John J. Substituted isoxazoles for the treatment of inflammation
GB9505491D0 (en) 1995-03-18 1995-05-03 Merck Sharp & Dohme Therapeutic agents
GB9505492D0 (en) 1995-03-18 1995-05-03 Merck Sharp & Dohme Therapeutic agents
US5554641A (en) 1995-03-20 1996-09-10 Horwell; David C. Nonpeptides as tachykinin antagonists
GB9505692D0 (en) 1995-03-21 1995-05-10 Glaxo Group Ltd Chemical compounds
US5700806A (en) 1995-03-24 1997-12-23 Schering Corporation Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
US5684013A (en) 1995-03-24 1997-11-04 Schering Corporation Tricyclic compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
EP0733632B1 (en) 1995-03-24 2003-06-04 Takeda Chemical Industries, Ltd. Cyclic compounds, their production and use as tachykinin receptor antagonists
IL117580A0 (en) 1995-03-29 1996-07-23 Merck & Co Inc Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them
US5565568A (en) 1995-04-06 1996-10-15 Eli Lilly And Company 2-acylaminopropanamides as tachykinin receptor antagonists
US5891872A (en) 1995-04-07 1999-04-06 Schering Corporation Tricyclic compounds
US5712280A (en) 1995-04-07 1998-01-27 Schering Corporation Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
IL117805A0 (en) 1995-04-07 1996-08-04 Schering Corp Carbonyl piperazinyl and piperidinyl compounds
IL117798A (en) 1995-04-07 2001-11-25 Schering Plough Corp Tricyclic compounds useful for inhibiting the function of protein - G and for the treatment of malignant diseases, and pharmaceutical preparations containing them
JP3950170B2 (ja) 1995-04-13 2007-07-25 アベンティス・ファーマスーティカルズ・インコーポレイテッド タキキニン受容体アンタゴニスト活性を有する新規な置換されたピペラジン誘導体
US5831115A (en) 1995-04-21 1998-11-03 Abbott Laboratories Inhibitors of squalene synthase and protein farnesyltransferase
IL118101A0 (en) 1995-05-03 1996-09-12 Abbott Lab Inhibitors of farnesyltransferase
WO1996037489A1 (en) 1995-05-25 1996-11-28 Fujisawa Pharmaceutical Co., Ltd. 1-benzoyl-2-(indolyl-3-alkyl)-piperazine derivatives as neurokinin receptor antagonists
US5919780A (en) 1995-06-16 1999-07-06 Warner Lambert Company Tricyclic inhibitors of protein farnesyltransferase
GB9513118D0 (en) 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
GB9513121D0 (en) 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
GB9513117D0 (en) 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
DK0840732T3 (da) 1995-07-07 2001-04-17 Pfizer Substituerede benzolactamforbindelser som substans P-antagonister
FR2736641B1 (fr) 1995-07-10 1997-08-22 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
AT402617B (de) 1995-07-11 1997-07-25 Datacon Schweitzer & Zeindl Gm Anlage zum automatisierten, hermetischen anlage zum automatisierten, hermetischen verschliessen von gehäusen verschliessen von gehäusen
FR2736638B1 (fr) 1995-07-12 1997-08-22 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
CH690163A5 (fr) 1995-07-28 2000-05-31 Symphar Sa Dérivés gem-diphosphonates substitués utiles en tant qu'agents anti-cancers.
TW340842B (en) 1995-08-24 1998-09-21 Pfizer Substituted benzylaminopiperidine compounds
US6020343A (en) 1995-10-13 2000-02-01 Merck Frosst Canada, Inc. (Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors
AU722883B2 (en) 1995-10-18 2000-08-10 Merck & Co., Inc. Cyclopentyl tachykinin receptor antagonists
DE19541283A1 (de) 1995-11-06 1997-05-07 Boehringer Ingelheim Kg Neue Aminosäurederivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
WO1997017070A1 (en) 1995-11-06 1997-05-15 University Of Pittsburgh Inhibitors of protein isoprenyl transferases
GB9523244D0 (en) 1995-11-14 1996-01-17 Merck Sharp & Dohme Therapeutic agents
JP4183099B2 (ja) 1995-11-17 2008-11-19 ゲゼルシャフト・フュア・ビオテヒノロジッシェ・フォルシュング・ミット・ベシュレンクテル・ハフツング(ゲー・ベー・エフ) エポチロンcおよびd、製造法ならびに組成物
AU704139B2 (en) 1995-11-22 1999-04-15 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JP2000500760A (ja) 1995-11-23 2000-01-25 メルク シヤープ エンド ドーム リミテツド スピロピペリジン誘導体およびタキキニン拮抗薬としてのその使用
GB9524157D0 (en) 1995-11-25 1996-01-24 Pfizer Ltd Therapeutic agents
RU2135494C1 (ru) 1995-12-01 1999-08-27 Санкио Компани Лимитед Гетероциклические соединения и композиция на их основе, проявляющая антагонистическое действие в отношении рецепторов тахикинина
IL123568A (en) 1995-12-08 2001-08-08 Janssen Pharmaceutica Nv History (Imidazole - 5Il) Methyl-2-quinolinone inhibitors of Prenzyl transferase, their preparation, pharmaceutical preparations containing them and their preparation and drugs containing them
GB9525296D0 (en) 1995-12-11 1996-02-07 Merck Sharp & Dohme Therapeutic agents
TW350844B (en) 1995-12-22 1999-01-21 Schering Corp Tricyclic amides useful to inhibition of G-protein function and for treatment of proliferative diseases
AU1529997A (en) 1996-01-16 1997-08-11 Warner-Lambert Company Substituted histidine inhibitors of protein farnesyltransferase
US6673927B2 (en) 1996-02-16 2004-01-06 Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. Farnesyl transferase inhibitors
EP0944388A4 (en) 1996-04-03 2001-08-16 Merck & Co Inc INHIBITORS OF FARNESYL PROTEIN TRANSFERASE
EP1288206B1 (en) 1996-04-12 2008-09-17 G.D. Searle LLC Substituted benzenesulfonamide derivatives as prodrugs of COX-2 inhibitors
CA2253934A1 (en) 1996-05-22 1997-11-27 Warner-Lambert Company Inhibitors of protein farnesyl transferase
WO1998002436A1 (en) 1996-07-15 1998-01-22 Bristol-Myers Squibb Company Thiadioxobenzodiazepine inhibitors of farnesyl protein transferase
US5861419A (en) 1996-07-18 1999-01-19 Merck Frosst Canad, Inc. Substituted pyridines as selective cyclooxygenase-2 inhibitors
JP4579351B2 (ja) 1996-12-03 2010-11-10 スローン−ケッタリング インスティトュート フォア キャンサー リサーチ エポチロンの合成とその中間体及びその類似物並びにその使用
WO1998028980A1 (en) 1996-12-30 1998-07-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU5719598A (en) 1996-12-30 1998-07-31 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU3475100A (en) 1999-01-29 2000-08-18 Imclone Systems Incorporated Antibodies specific to kdr and uses thereof
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
AU4972900A (en) 1999-04-08 2000-11-14 Arch Development Corporation Use of anti-vegf antibody to enhance radiation in cancer therapy
CA2388646C (en) 1999-10-27 2009-01-27 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
US6545004B1 (en) 1999-10-27 2003-04-08 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
US6958334B2 (en) 2001-04-10 2005-10-25 Merck & Co., Inc. Inhibitors of Akt activity
AU2002251266A1 (en) 2001-04-10 2002-10-28 Merck Sharp And Dohme Limited Inhibitors of akt activity
ATE400274T1 (de) 2001-04-10 2008-07-15 Merck & Co Inc Hemmstoffe der akt aktivität
WO2002083139A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
WO2003013526A1 (en) 2001-08-08 2003-02-20 Merck & Co. Inc. Anticoagulant compounds
EP1444209A4 (en) 2001-11-07 2005-02-16 Merck & Co Inc INHIBITORS OF MITOTIC KINESINS
AU2002351183B2 (en) 2001-12-06 2008-05-08 Merck Sharp & Dohme Corp. Mitotic kinesin inhibitors
US7244723B2 (en) 2001-12-06 2007-07-17 Merck & Co., Inc. Substituted furopyrimidinones as a mitotic kinesin inhibitors
AU2002363960B2 (en) 2001-12-06 2008-07-10 Merck Sharp & Dohme Corp. Mitotic kinesin inhibitors
WO2003049678A2 (en) 2001-12-06 2003-06-19 Merck & Co., Inc. Mitotic kinesin inhibitors
WO2003050064A2 (en) 2001-12-06 2003-06-19 Merck & Co., Inc. Mitotic kinesin inhibitors
WO2003105855A1 (en) 2002-01-11 2003-12-24 Merck & Co., Inc. Mitotic kinesin inhibitors
WO2003064383A2 (en) 2002-02-01 2003-08-07 Ariad Gene Therapeutics, Inc. Phosphorus-containing compounds & uses thereof
DE60329990D1 (de) 2002-03-08 2009-12-24 Merck & Co Inc Mitotische kinesin-hemmer
CA2481229C (en) 2002-04-08 2010-09-21 Merck & Co., Inc. Substituted pyrazine inhibitors of akt
WO2003086403A1 (en) 2002-04-08 2003-10-23 Merck & Co., Inc. Inhibitors of akt activity
AU2003223467B2 (en) 2002-04-08 2007-10-04 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
US7273869B2 (en) 2002-04-08 2007-09-25 Merck & Co., Inc. Inhibitors of Akt activity
WO2004039774A2 (en) 2002-05-23 2004-05-13 Merck & Co., Inc. Mitotic kinesin inhibitors
US20050234080A1 (en) 2002-05-23 2005-10-20 Coleman Paul J Mitotic kinesin inhibitors
CA2486215A1 (en) 2002-06-14 2003-12-24 Merck & Co., Inc. Mitotic kinesin inhibitors
DE60334386D1 (de) * 2002-08-09 2010-11-11 Merck Sharp & Dohme Tyrosinkinaseinhibitoren
AR046639A1 (es) 2003-11-21 2005-12-14 Schering Corp Combinaciones terapeuticas de anticuerpo anti- igfr1
MX2007010973A (es) 2005-03-09 2007-09-19 Schering Corp Compuestos para inhibir la actividad de cinesina de ksp.
CA2599899A1 (en) 2005-03-09 2006-09-21 Schering Corporation Fused thieno [2, 3-b] pyridine and thiazolo [5, 4-b] pyridine compounds for inhibiting ksp kinesin activity
CN101258130B (zh) * 2005-09-09 2012-11-28 阿纳里特康股份有限公司 作为胰岛素样生长因子-1受体抑制剂的异喹啉
WO2007029107A1 (en) * 2005-09-09 2007-03-15 Analytecon Sa Isoquinolines derivatives as igf-1r inhibitors
ATE527240T1 (de) 2005-12-13 2011-10-15 Schering Corp Polyzyklische indazol-derivate als erk-hemmer
MX2008010635A (es) 2006-02-16 2008-10-28 Schering Corp Derivados de pirrolidina como inhibidores de cinasa regulada por señales extracelulares.
US20110038876A1 (en) 2007-06-18 2011-02-17 Robert Sun Heterocyclic compounds and use thereof as erk inhibitors
JP2014514321A (ja) * 2011-04-21 2014-06-19 メルク・シャープ・アンド・ドーム・コーポレーション インスリン様増殖因子1受容体阻害剤

Also Published As

Publication number Publication date
EP2699568A1 (en) 2014-02-26
CA2831730A1 (en) 2012-10-26
JP2014514321A (ja) 2014-06-19
WO2012145471A1 (en) 2012-10-26
US20140045832A1 (en) 2014-02-13
WO2012143874A1 (en) 2012-10-26
AU2012245455A8 (en) 2013-11-07
IN2013MN02170A (enExample) 2015-06-12
US20140045847A1 (en) 2014-02-13
AU2012245971A8 (en) 2013-11-07
IL228810A0 (en) 2013-12-31
CA2833009A1 (en) 2012-10-26
CN103732592A (zh) 2014-04-16
AU2012245455A1 (en) 2013-10-31
EP2699567A1 (en) 2014-02-26
US20140046059A1 (en) 2014-02-13
WO2012143879A1 (en) 2012-10-26

Similar Documents

Publication Publication Date Title
AU2012245971A1 (en) A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
JP7383652B2 (ja) B-rafキナーゼのマレイン酸塩、結晶形、調整方法、及びその使用
JP7007302B2 (ja) メニン-mll相互作用の阻害剤
KR102086871B1 (ko) Fgfr 키나제의 억제를 통한 항암 벤조피라진
JP6169583B2 (ja) Fgfrキナーゼの阻害を介した抗癌ピリドピラジン
DK2763992T3 (en) NOVEL CHIRAL N-acyl-5,6,7, (8-substituted) -tetrahydro [1,2,4] triazolo [4,3-a] pyrazines as selective NK-3 receptor antagonists, PHARMACEUTICAL COMPOSITION AND METHODS FOR THE use in the NK-3 receptor mediated diseases
AU2014309788B2 (en) Novel quinoline-substituted compound
EP2528920A2 (en) Bicyclic heteroaryl derivatives having inhibitory activity for protein kinase
JP2008514628A (ja) 蛋白質キナーゼ類のイミダゾ{4,5−b}ピラジノン阻害剤
EP3459952B1 (en) Pyrimidine derivative, method for preparing same and use thereof in medicine
TW201236684A (en) Pharmaceutically acceptable salts of (E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide, preparation process and pharmaceutical use there of
AU2012292649B8 (en) N-(Benzimidazol-2-yl)-cyclopropane carboxamides as lysophosphatidic acid antagonists
EP2509980A1 (en) Heterocyclic compounds containing an indole core
CN102918029B (zh) 4-苯胺-6-丁烯酰胺-7-烷醚喹唑啉衍生物及其制备方法和用途
CN111909157A (zh) Ezh2抑制剂及其用途
CN120418237A (zh) 芳香酰胺类衍生物及其制备方法和用途
CN105209454A (zh) 用作激酶活性调节剂的6-[4-(1h-咪唑-2-基)哌啶-1-基]嘧啶-4-胺衍生物
CN103717590A (zh) 喹唑啉-7-醚化合物及使用方法
CN118684666A (zh) Kif18a抑制剂及其用途
CN120787223A (zh) 芳香酰胺类衍生物及其制备方法和用途
CN114746419B (zh) N-(3-(5-(嘧啶-4-基)噻唑-4-基)苯基)磺酰胺化合物及其用作braf抑制剂的用途
CN117177975A (zh) 嘧啶并[5,4,d]嘧啶化合物、包含其的组合物及其用途
WO2025172707A1 (en) Heterocyclic compounds modulating exonuclease 1 (exo1)
WO2025003429A1 (en) Pyrazole derivatives as pd-1/pd-l1 interaction inhibitors
CN120035595A (zh) 噻唑并[5,4-d]嘧啶化合物、包含其的组合物及其用途

Legal Events

Date Code Title Description
TH Corrigenda

Free format text: IN VOL 27 , NO 40 , PAGE(S) 5845 UNDER THE HEADING PCT APPLICATIONS THAT HAVE ENTERED THE NATIONAL PHASE - NAME INDEX UNDER THE NAME PIRAMAL HEALTHCARE LIMITED, APPLICATION NO. 2012245971, UNDER INID (71) CORRECT THE APPLICANT NAME TO PIRAMAL ENTERPRISES LIMITED

MK1 Application lapsed section 142(2)(a) - no request for examination in relevant period