HRP20190842T1 - Kristalni oblici 2-((4s)-6-(4-hlorofenil)-1-metil-4h-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamida - Google Patents

Kristalni oblici 2-((4s)-6-(4-hlorofenil)-1-metil-4h-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamida Download PDF

Info

Publication number
HRP20190842T1
HRP20190842T1 HRP20190842TT HRP20190842T HRP20190842T1 HR P20190842 T1 HRP20190842 T1 HR P20190842T1 HR P20190842T T HRP20190842T T HR P20190842TT HR P20190842 T HRP20190842 T HR P20190842T HR P20190842 T1 HRP20190842 T1 HR P20190842T1
Authority
HR
Croatia
Prior art keywords
water
isoxazolo
azepin
chlorophenyl
benzo
Prior art date
Application number
HRP20190842TT
Other languages
English (en)
Inventor
Michael L. Hall
Original Assignee
Constellation Pharmaceuticals, Inc.
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 Constellation Pharmaceuticals, Inc. filed Critical Constellation Pharmaceuticals, Inc.
Publication of HRP20190842T1 publication Critical patent/HRP20190842T1/hr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Claims (13)

1. Kristalni monohidrat oblika A 2-((4S)-6-(4-hlorofenil)-1-metil-4H-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamida, pri čemu je kristalni oblik naznačen time što se najmanje tri najviše vrijednosti rendgenske difrakcije praha dostiže pod 2Θkutevima odabranim od 4,73°, 18,09°, 18,48°, 18,80°, 19,70°, i 25,17°.
2. Kristalni monohidrat oblika A sukladno patentnom zahtjevu 1, pri čemu je taj kristalni oblik naznačen time što se najmanje četiri najviših vrijednosti rendgenske difrakcije praha dostiže pod 2Θ kutevima odabranim od 4,73°, 18,.09°, 18,48°, 18,80°, 19,70°, i 25,17°.
3. Kristalni monohidrat oblika A sukladno patentnom zahtjevu 1 ili 2, pri čemu je taj kristalni oblik naznačen time što se najmanje pet najviših vrijednosti rendgenske difrakcije praha dostiže pod 2Θ kutevima odabranim od 4,73°, 18,09°, 18,48°, 18,80°, 19,70°, i 25,17°.
4. Kristalni monohidrat oblika A sukladno bilo kojem od patentnih zahtjeva 1 do 3, pri čemu je, taj kristalni oblik naznačen time što se najviše vrijednosti rendgenske difrakcije praha dostižu pod 2Θkutevima 4,73°, 18,09°, 18,48°, 18,80°, 19,70°, i 25,17°.
5. Kristalni monohidrat oblika A sukladno bilo kojem od patentnih zahtjeva 1 do 4, pri čemu je taj kristalni oblik naznačen time što se najviše vrijednosti rendgenske difrakcije praha dostižu pod 2Θ kutevima 4,73°, 9,42°, 12,91°, 18,09°, 18,48°, 18,80°, 19,70°, 21,42°, i 25,17°.
6. Kristalni monohidrat oblika A sukladno bilo kojem od patentnih zahtjeva 1 do 5, pri čemu je taj kristalni oblik naznačen time što se najviše vrijednosti rendgenske difrakcije praha dostižu pod 2Θ kutevima 4,73°, 8,11°, 9,42°, 12,91°, 14,10°, 14,97°, 18,09°, 18,48°, 18,80°, 19,70°, 21,42°, i 25,17°, 26,07°, i 26,53°.
7. Farmaceutski pripravak koji sadrži oblik kristalnog monohidrata sukladno bilo kojem od patentnih zahtjeva 1 do 6; i farmacutski prihvatljiv nosač ili otapalo.
8. Kristalni monohidrat oblika A 2-((4S)-6-(4-klorofenil)-1-metil-4H-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamida sukladno bilo kojem od patentnih zahtjeva radi liječenja proliferativnog poremećaja, bolesti upale, sepse, autoimunih bolesti, ili virusne infekcije.
9. Kristalni monohidrat oblika A 2-((4S)-6-(4-klorofenil)-1-metil-4H-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamida za uporabu sukladno patentnom zahtjevu 8, pri čemu je taj poremećaj karcinom.
10. Postupak dobivanja kristalnog monohidrata oblika A 2-((4S)-6-(4-klorofenil)-1-metil-4H-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamida, taj postupak obuhvaća: stvaranje kristalnog monohidrata oblika A iz otopine koja sadrži amorfni 2-((4S)-6-(4-klorofenil)-1-metil-4H-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamid i vodu; ili iz mješavine koja sadrži amorfni 2-((4S)-6-(4-klorofenil)-1-metil-4H-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamid, i kombinaciju vode i organskog otapala.
11. Postupak sukladno patentnom zahtjevu 10, pri čemu se kombinacija vode i organskog otapala izabire od etanola/vode, izopropanola/vode, tetrahidrofurana/vode, acetona/vode, metanola/vode, i acetonitrila/vode.
12. Postupak sukladno patentnom zahtjevu 10 ili 11, pri čemu je kombinacija vode i organskog otapala etanol/voda.
13. Postupak sukladno bilo kojem od patentnih zahtjeva 10 do 12, pri čemu je kombinacija vode i organskog otapala u odnosu od 60:40 mješavine etanola/vode
HRP20190842TT 2014-06-20 2019-05-07 Kristalni oblici 2-((4s)-6-(4-hlorofenil)-1-metil-4h-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamida HRP20190842T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462014782P 2014-06-20 2014-06-20
EP15733597.7A EP3157928B1 (en) 2014-06-20 2015-06-18 Crystalline forms of 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
PCT/US2015/036347 WO2015195862A1 (en) 2014-06-20 2015-06-18 Crystalline forms of 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4s5-e]azepin-4-yl)acetamide

Publications (1)

Publication Number Publication Date
HRP20190842T1 true HRP20190842T1 (hr) 2019-08-09

Family

ID=53499102

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20190842TT HRP20190842T1 (hr) 2014-06-20 2019-05-07 Kristalni oblici 2-((4s)-6-(4-hlorofenil)-1-metil-4h-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamida

Country Status (17)

Country Link
US (1) US9969747B2 (hr)
EP (1) EP3157928B1 (hr)
JP (1) JP6682522B2 (hr)
CN (1) CN106687463B (hr)
CA (1) CA2952830C (hr)
CY (1) CY1121997T1 (hr)
DK (1) DK3157928T3 (hr)
ES (1) ES2725928T3 (hr)
HR (1) HRP20190842T1 (hr)
HU (1) HUE043441T2 (hr)
LT (1) LT3157928T (hr)
PL (1) PL3157928T3 (hr)
PT (1) PT3157928T (hr)
RS (1) RS58730B1 (hr)
SI (1) SI3157928T1 (hr)
TR (1) TR201906788T4 (hr)
WO (1) WO2015195862A1 (hr)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI719464B (zh) 2013-03-15 2021-02-21 美商英塞特控股公司 作為bet蛋白抑制劑之三環雜環
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
DK3674302T3 (da) 2014-04-23 2023-04-03 Incyte Holdings Corp 1h-pyrrolo[2,3-c]pyridin-7(6h)-oner og pyrazolo[3,4-c]pyridin-7(6h)-oner som inhibitorer af bet-proteiner
KR102643344B1 (ko) 2016-06-20 2024-03-07 인사이트 코포레이션 Bet 저해제의 결정질 고체 형태
EP3539960A4 (en) 2016-11-10 2020-03-18 Luoxin Pharmaceutical (Shanghai) Co., Ltd. NITROGEN MACROCYCLIC COMPOUND, ITS PREPARATION METHOD, ITS PHARMACEUTICAL COMPOSITION AND ITS APPLICATION
US20210000815A1 (en) * 2017-12-28 2021-01-07 Constellation Pharmaceuticals, Inc. Pharmacokinetic enhancement of ezh2 inhibitors through combination therapies
WO2021091532A1 (en) 2019-11-05 2021-05-14 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
KR20210095904A (ko) 2018-11-27 2021-08-03 콘스텔레이션 파마슈티칼스, 인크. 골수증식 장애의 치료 방법
WO2020112939A1 (en) 2018-11-27 2020-06-04 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
WO2020256739A1 (en) 2019-06-21 2020-12-24 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
WO2020257644A1 (en) 2019-06-21 2020-12-24 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
WO2021091535A1 (en) 2019-11-05 2021-05-14 Constellation Pharmaceuticals, Inc. Treating myeloproliferative disorders with cpi-0610 and a jak inhibitor
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
KR20230048042A (ko) 2020-08-04 2023-04-10 콘스텔레이션 파마슈티칼스, 인크. 혈소판 증가증의 치료를 위한 2-((4s)-6-(4-클로로페닐)-1-메틸-4h-벤조[c]이속사졸로[4,5-e]아제핀-4-일)아세트아미드
CA3218297A1 (en) 2021-05-11 2022-11-17 Gozde Colak Use of pelabresib for treating anemias
WO2023147149A1 (en) * 2022-01-31 2023-08-03 Constellation Pharmaceuticals, Inc. Anhydrous crystalline forms of 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide

Family Cites Families (147)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3523939A (en) 1967-07-03 1970-08-11 Hoffmann La Roche 5-(2,6-disubstituted phenyl)-1,4-benzodiazepines and methods for their preparation
CH498846A (de) 1967-08-09 1970-11-15 Hoffmann La Roche Verfahren zur Herstellung von Benzodiazepin-Derivaten
US3709898A (en) 1971-02-09 1973-01-09 Upjohn Co Process for the production of triazolobenzodiazepines and intermediates
US3781289A (en) 1971-02-09 1973-12-25 Upjohn Co 7-chloro-1-methyl-5-phenyl-s-triazolo (4,3-a)quinolines
US3681343A (en) 1971-05-11 1972-08-01 Upjohn Co 6-phenyl-s-triazolo{8 4,3-a{9 {8 1,4{9 {0 benzodiazepines
DE2242918A1 (de) 1971-09-15 1973-03-22 Upjohn Co Neue 4-amino-s-triazolo eckige klammer auf 4,3-a eckige klammer zu eckige klammer auf 1,4 eckige klammer zu benzodiazepine
US3903103A (en) 1971-09-15 1975-09-02 Upjohn Co 4-Amino-s-triazolo-{8 4,3-a{9 {8 1,4{9 benzodiazepine
US3886141A (en) 1971-10-07 1975-05-27 Hoffmann La Roche Preparation of 5-pyridyl benzodiazepine utilizing hexamethylenetetramine
BE795790A (fr) 1972-02-22 1973-08-22 Upjohn Co Dibenzo-triazolo-azepine
US4155904A (en) 1973-02-08 1979-05-22 Schering Corporation Process for the preparation of 1,4-benzo-diazepines and 1,4-benzodiazepinones
FR2220257A1 (en) 1973-03-09 1974-10-04 Lipha 5,6-Dihydro-(4H)-s-triazolo-(4,3-a) (1,5)benzodiazepines - as antiinflam-matory and analgesic agents without tranquillising effects
IE38931B1 (en) 1973-03-09 1978-07-05 Lipha Triazolobenzodiazepines
US3966736A (en) 1975-04-07 1976-06-29 The Upjohn Company 2,9-Dihydro-3H-pyrido[3,2-c]-s-triazolo[4,3-a][1,5]-benzodiazepin-3-ones
AT350056B (de) 1975-11-04 1979-05-10 Degussa Verfahren zur herstellung von neuen pyrido- (2,3-f)-(1,4)-diazepinen, deren optischen isomeren und salzen
DE2640599A1 (de) 1976-09-09 1978-03-16 Scherico Ltd Verfahren zur herstellung von 1,4- benzodiazepinen
CA1152066A (en) 1980-02-08 1983-08-16 Hoffmann-La Roche Limited Benzodiazepine derivatives
CA1163266A (en) 1980-07-31 1984-03-06 Albert E. Fischli Benzodiazepine derivatives
CA1157855A (en) 1980-07-31 1983-11-29 Albert E. Fischli Benzodiazepine derivatives
US4455307A (en) 1982-01-04 1984-06-19 The Upjohn Company Antihypertensive use of triazolobenzodiazepines
US4820834A (en) 1984-06-26 1989-04-11 Merck & Co., Inc. Benzodiazepine analogs
US4663321A (en) 1984-06-26 1987-05-05 Merck & Co., Inc. Triazolobenzodiazepines and pharmaceutical use
US5004741A (en) 1984-06-26 1991-04-02 Merck & Co., Inc. Methods of antagonizing CCK or gastrin with benzodiazepine analogs
ATE86256T1 (de) 1987-05-28 1993-03-15 Yoshitomi Pharmaceutical Thieno(triazolo)diazepinverbindungen, und medizinische verwendung derselben.
MC1999A1 (fr) 1987-12-18 1990-01-26 Hoffmann La Roche Composes tricycliques
US4959361A (en) 1987-12-18 1990-09-25 Hoffmann-La Roche Inc. Triazolo(4,3-A)(1,4)benzodiazepines and thieno (3,2-F)(1,2,4)triazolo(4,3-A)(1,4)diazepine compounds which have useful activity as platelet activating factor (PAF) antagonists
WO1989005812A1 (en) 1987-12-22 1989-06-29 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compounds and their medicinal use
CA1324863C (en) 1988-01-30 1993-11-30 Minoru Moriwaki Thienotriazolodiazepine compounds and pharmaceutical uses thereof
CA1322367C (en) 1988-05-17 1993-09-21 Yoshitomi Pharmaceutical Industries Ltd. Thienotriazolodiazepine compounds and pharmaceutical uses thereof
US5382579A (en) 1988-10-31 1995-01-17 Eisai Co., Ltd. Triazolo-1,4-diazepine derivatives and their use in pharmaceuticals
US5221671A (en) 1988-10-31 1993-06-22 Eisai Co., Ltd. Triazolo-1,4-diazepine derivatives and their use in pharmaceuticals
FI95708C (fi) 1988-10-31 1996-03-11 Eisai Co Ltd Analogiamenetelmä 1,4-diatsepiinijohdannaisen ja sen farmaseuttisesti sopivan suolan valmistamiseksi
DE3936828A1 (de) 1988-11-06 1990-05-10 Boehringer Ingelheim Kg Neue hetrazepine
DE4006471A1 (de) 1989-03-03 1990-09-06 Boehringer Ingelheim Kg Neue thienodiazepine
YU133090A (sh) 1989-07-12 1993-10-20 Boehringer Ingelheim Kg. Novi heteroazepini s paf-antaganostičnim učinkom in postopek za njihovo pripravo
EP0411668B2 (en) 1989-08-04 1998-11-11 MERCK SHARP & DOHME LTD. Central cholecystokinin antagonists for treatment of psychiatric disorders
US5175159A (en) 1989-10-05 1992-12-29 Merck & Co., Inc. 3-substituted-1,4-benzodiazepines as oxytocin antagonists
IE904560A1 (en) 1989-12-18 1991-06-19 Merck & Co Inc New benzodiazepine analogs
IL96613A0 (en) 1989-12-18 1991-09-16 Merck & Co Inc Pharmaceutical compositions containing benzodiazepine analogs
JP2971901B2 (ja) 1990-03-15 1999-11-08 エーザイ株式会社 トリアゾロ―１，４―ジアゼピン系化合物
JP2971902B2 (ja) 1990-03-15 1999-11-08 エーザイ株式会社 トリアゾロ―１，４―ジアゼピン系化合物
JP2959591B2 (ja) 1990-05-23 1999-10-06 吉富製薬株式会社 チエノトリアゾロジアゼピン化合物
WO1994006801A1 (en) 1990-05-23 1994-03-31 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compound and medicinal use thereof
DE4027470A1 (de) 1990-08-30 1992-03-05 Boehringer Ingelheim Kg Neue hetrazepinoide amide
JP2959598B2 (ja) 1990-10-12 1999-10-06 吉富製薬株式会社 光学活性なチエノトリアゾロジアゼピン化合物
US5206234A (en) 1990-10-22 1993-04-27 Merck & Co., Inc. Benzolactam analogs as antagonists of cck
CA2056809A1 (en) 1990-12-07 1992-06-08 Mark G. Bock Benzodiazepine analogs
DE4101146A1 (de) 1991-01-16 1992-07-23 Boehringer Ingelheim Kg Neue in 6-position substituierte diazepine, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
DE4107521A1 (de) 1991-03-08 1992-09-10 Boehringer Ingelheim Kg Neue acylaminosubstituierte hetrazepine
US5683998A (en) 1991-04-23 1997-11-04 Toray Industries, Inc. Tricyclic triazolo derivatives, processes for producing the same and the uses of the same
US5185331A (en) 1991-05-14 1993-02-09 Merck & Co., Inc. Triazolobenzodiazepines
EP0523846A3 (en) 1991-06-14 1993-03-17 Merck & Co. Inc. 1,4-benzodiazepines with 5-membered heterocyclic rings
GB9117852D0 (en) 1991-08-19 1991-10-09 Merck Sharp & Dohme Therapeutic agents
US5153191A (en) 1991-08-20 1992-10-06 Warner-Lambert Company Cholecystokinin antagonists useful for treating depression
DE4128581A1 (de) 1991-08-28 1993-03-04 Boehringer Ingelheim Kg Verwendung von paf-antagonisten hetrazepinoider struktur zur behandlung der allergischen rhinitis
KR970002640B1 (ko) 1991-09-30 1997-03-07 요시또미세이야꾸 가부시끼가이샤 티에노디아제핀 화합물 및 그의 용도
WO1993007129A1 (en) 1991-10-11 1993-04-15 Yoshitomi Pharmaceutical Industries, Ltd. Remedy for osteoporosis and diazepine compound
ES2143993T3 (es) 1991-12-11 2000-06-01 Yoshitomi Pharmaceutical Farmaco para tratar una enfermedad autoinmune.
JPH07507993A (ja) 1991-12-20 1995-09-07 メルク　シヤープ　エンド　ドーム　リミテツド 医薬活性を有する中枢神経系コレシストキニンアンタゴニスト
DE4200610A1 (de) 1992-01-13 1993-07-15 Boehringer Ingelheim Kg Verwendung von paf-antagonisten zur behandlung der dysmenorrhea
CA2130196A1 (en) 1992-03-24 1993-09-30 Jose Luis Castro Pineiro Benzodiazepine derivatives
DE4219659A1 (de) 1992-06-16 1993-12-23 Boehringer Ingelheim Kg Die Verwendung von PAF-Antagonisten in Kombination mit Anticholinergika
WO1994006802A1 (en) 1992-09-18 1994-03-31 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compound and medicinal use thereof
US5302590A (en) 1992-12-18 1994-04-12 Hoffmann-La Roche Inc. Compounds useful as dual antagonists of platelet activating factor and leukotriene D4
CA2159344A1 (en) 1993-03-30 1994-10-13 Minoru Moriwaki Cell adhesion inhibitor and thienotriazolodiazepine compound
EP0763537A3 (en) 1993-05-14 1997-10-22 Genentech Inc Non-peptides farnesyl transfer inhibitors
US5760031A (en) 1993-07-29 1998-06-02 American Cyanamid Company Tricyclic benzazepine vasopressin antagonists
US5869483A (en) 1993-07-29 1999-02-09 American Cyanamid Company Tricyclic benzazepine vasopressin antagonists
US5733905A (en) 1993-07-29 1998-03-31 American Cyanamid Company Tricyclic diazepine vasopressin antagonists and oxytocin antagonists
US5516774A (en) 1993-07-29 1996-05-14 American Cyanamid Company Tricyclic diazepine vasopressin antagonists and oxytocin antagonists
JP3633008B2 (ja) 1993-11-15 2005-03-30 三菱ウェルファーマ株式会社 チエノトリアゾロジアゼピン化合物
US5679672A (en) 1993-11-22 1997-10-21 Merck & Co., Inc. Benzodiazepines
WO1995018130A1 (fr) 1993-12-28 1995-07-06 Meiji Seika Kabushiki Kaisha Derives tricycliques de benzazepine et benzothiazepine
US5739129A (en) 1994-04-14 1998-04-14 Glaxo Wellcome Inc. CCK or gastrin modulating 5-heterocyclic-1, 5 benzodiazepines
US5795887A (en) 1994-04-15 1998-08-18 Glaxo Wellcome Inc. Method of inducing cholecystokinin agonist activity using 1,4- Benzodiazepine compounds
JP3264588B2 (ja) 1994-08-23 2002-03-11 松下電器産業株式会社 電子地図データの生成装置
JP3264589B2 (ja) 1994-09-07 2002-03-11 東芝機械株式会社 研磨装置
CN1121395C (zh) 1995-09-21 2003-09-17 药物分子设计研究所株式会社 类视色素作用增强性化合物
CN1227555A (zh) 1996-06-12 1999-09-01 日本烟草产业株式会社 细胞因子生成抑制剂、三氮䓬化合物及其中间体
JP3094453B2 (ja) 1996-09-13 2000-10-03 ウェルファイド株式会社 チエノトリアゾロジアゼピン化合物およびその医薬用途
EA002100B1 (ru) 1996-12-23 2001-12-24 Элан Фармасьютикалз, Инк. ЦИКЛОАЛКИЛЬНЫЕ СОЕДИНЕНИЯ, ЛАКТАМЫ, ЛАКТОНЫ И РОДСТВЕННЫЕ СОЕДИНЕНИЯ, СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ И СПОСОБЫ ИНГИБИРОВАНИЯ ВЫСВОБОЖДЕНИЯ И/ИЛИ СИНТЕЗА β-АМИЛОИДНОГО ПЕПТИДА С ПОМОЩЬЮ УКАЗАННЫХ СОЕДИНЕНИЙ
US6433167B1 (en) 1997-06-25 2002-08-13 Nikken Chemicals Co., Ltd. Triazolo-1,4-diazepine compounds and medicinal composition containing the same
JP4204657B2 (ja) 1997-12-05 2009-01-07 有限会社ケムフィズ 糖尿病の予防・治療剤
JPH11228576A (ja) 1997-12-10 1999-08-24 Japan Tobacco Inc アポトーシス抑制剤
FR2779652B1 (fr) 1998-06-15 2001-06-08 Sod Conseils Rech Applic Utilisation de diazepines pour la preparation de medicaments destines a traiter les etats pathologiques ou les maladies dans lesquels un des recepteurs de la somatostatine est implique
PE20000944A1 (es) 1998-07-31 2000-09-20 Lilly Co Eli Derivados de sulfonamida
BR9913226A (pt) 1998-09-01 2001-05-22 Innogenetics Nv Benzodiazepinas e derivados de benzotiazepinas e peptìdios de hbsag ligados a anexinas, suas composições e uso
WO2000054778A1 (fr) 1999-03-12 2000-09-21 Welfide Corporation Agents preventifs ou therapeutiques des dermatoses inflammatoires
FR2791980B1 (fr) 1999-04-09 2001-07-06 Sod Conseils Rech Applic Pyrido-thieno-diazepines, leur procede de preparation, et les compositions pharmaceutiques les contenant
GB9911152D0 (en) 1999-05-14 1999-07-14 Glaxo Group Ltd Short-acting benzodiazepines
US7160880B1 (en) 1999-05-14 2007-01-09 Cenes Limited Short-acting benzodiazepines
WO2001047510A2 (en) 1999-12-29 2001-07-05 Glaxo Group Limited Methods and compositions related to modulators of annexin and cartilage homeostasis
CA2412776C (en) 2000-06-16 2011-03-15 Mitsubishi Pharma Corporation Compositions controlling release ph range and/or speed
AU2002317910B2 (en) 2001-06-07 2008-06-19 Via Pharmaceuticals, Inc. Cyclic nucleotide phosphodiesterase inhibitors, preparation and uses thereof
WO2003074525A1 (fr) 2002-03-01 2003-09-12 Yamanouchi Pharmaceutical Co., Ltd. Compose heterocyclique azote
JP2006509832A (ja) 2002-10-30 2006-03-23 ニューロ３デー サイクリックヌクレオチドホスホジエステラーゼ阻害剤、その調製及び使用
DE10251927A1 (de) 2002-11-08 2004-05-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
US7482337B2 (en) 2002-11-08 2009-01-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
KR100562489B1 (ko) 2002-11-11 2006-03-21 삼성전자주식회사 셔터 타이밍 조절 가능한 로우 디코더를 갖는 이미지 센서
NZ541151A (en) 2002-12-18 2008-09-26 Vertex Pharma Triazolopyridazines as protein kinase inhibitors
US7119088B2 (en) 2003-02-19 2006-10-10 Pfizer Inc. Triazole compounds useful in therapy
JPWO2005002590A1 (ja) 2003-07-01 2006-08-10 アステラス製薬株式会社 骨量増加誘導剤
WO2005099759A1 (ja) 2004-04-16 2005-10-27 Institute Of Medicinal Molecular Design. Inc. 動脈硬化症の予防及び／又は治療のための医薬
EP1806070A1 (en) 2004-10-05 2007-07-11 Pioneer Corporation Audio rack
TWI447120B (zh) 2005-05-30 2014-08-01 Mitsubishi Tanabe Pharma Corp 噻吩并三唑并苯二氮呯化合物、其醫藥上之用途
AU2006275981A1 (en) 2005-07-29 2007-02-08 Merck Sharp & Dohme Corp. Heterocyclic benzodiazepine CGRP receptor antagonists
JP2009513644A (ja) 2005-10-26 2009-04-02 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン 治療組成物および方法
US20070105844A1 (en) 2005-10-26 2007-05-10 Regents Of The University Of Michigan Therapeutic compositions and methods
DE102005061840A1 (de) 2005-12-23 2007-06-28 Merck Patent Gmbh Triazolderivate
WO2008023847A1 (fr) 2006-08-25 2008-02-28 Nippon Chemiphar Co., Ltd. Antagoniste du récepteur p2x4
WO2008109856A2 (en) 2007-03-07 2008-09-12 Xenon Pharmaceuticals Inc. Methods of using diazepinone compounds in treating sodium channel-mediated diseases or conditions
US20090111780A1 (en) 2007-10-31 2009-04-30 Everett Laboratories, Inc. Compositions and methods for treatment of ear canal infection and inflammation
ITFI20070288A1 (it) 2007-12-21 2009-06-22 A I L Firenze Sezione Autonoma Inibitori delle deacetilasi istoniche
JP5478262B2 (ja) 2007-12-28 2014-04-23 田辺三菱製薬株式会社 抗癌剤
EP2349257B1 (en) 2008-06-17 2013-11-27 Universidade Federal de Minas Gerais-UFMG Use of paf receptor for treating infections caused by flaviviridae
MX2011000021A (es) 2008-06-23 2011-02-24 Vertex Pharma Inhibidores de proteina cinasas.
ES2448567T3 (es) 2008-10-30 2014-03-14 Circomed Llc Derivados de la tienotriazoldiazepina activos en apo A
WO2010121164A2 (en) 2009-04-17 2010-10-21 The Regents Of The University Of Michigan 1,4-benzodiazepinone compounds and their use in treating cancer
WO2010128685A1 (en) 2009-05-07 2010-11-11 Prism Biolab Corporation Alpha helix mimetics and methods relating thereto
KR101435729B1 (ko) 2009-09-28 2014-09-01 닛뽕소다 가부시키가이샤 함질소 헤테로 고리 화합물 및 그의 염, 그리고 농원예용 살균제
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
ME02360B (me) 2009-11-05 2016-06-20 Glaxosmithkline Llc Inhibitor bromodomena benzodiazepina
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
KR20120097508A (ko) 2009-11-05 2012-09-04 글락소스미스클라인 엘엘씨 벤조디아제핀 브로모도메인 억제제
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
ES2539964T3 (es) 2009-11-05 2015-07-07 Glaxosmithkline Llc Procedimiento novedoso
CA2785410A1 (en) 2009-12-23 2011-06-30 Carlos F. Barbas, Iii Tyrosine bioconjugation through aqueous ene-like reactions
US8541407B2 (en) 2010-03-31 2013-09-24 Arqule, Inc. Substituted benzo-pyrido-triazolo-diazepine compounds
DK2571503T3 (en) 2010-05-14 2015-04-20 Dana Farber Cancer Inst Inc COMPOSITIONS AND THEIR USE IN THE TREATMENT OF NEOPLASIA, INFLAMMATORY DISEASE AND OTHER DISORDERS
CN103119160B (zh) 2010-05-14 2016-06-01 达那-法伯癌症研究所 用于调节代谢的组合物和方法
CN105582014B (zh) 2010-05-14 2019-06-14 达那-法伯癌症研究所 用于治疗白血病的组合物和方法
US9301962B2 (en) 2010-05-14 2016-04-05 Baylor College Of Medicine Male contraceptive compositions and methods of use
JP5844358B2 (ja) 2010-06-22 2016-01-13 グラクソスミスクライン エルエルシー ベンゾトリアゾロジアゼピン化合物を含むブロモドメイン阻害剤
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
AR084070A1 (es) * 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
EP2705039B1 (en) 2011-05-04 2017-07-26 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
EP2721031B1 (en) 2011-06-17 2016-01-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201114103D0 (en) 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013033269A1 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
WO2013033270A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bromodomain ligands capable of dimerizing in an aqueous solution, and methods of using same
US10071129B2 (en) 2011-08-30 2018-09-11 Whitehead Institute For Biomedical Research Dana-Farber Cancer Institute, Inc. Method for identifying bromodomain inhibitors
DE102011082013A1 (de) 2011-09-01 2013-03-07 Bayer Pharma AG 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
WO2013130573A1 (en) 2012-03-01 2013-09-06 Array Biopharma Inc. Crystalline forms of 1- (3 -tert-butyl- 1 - p-tolyl- 1h- pyrazol- 5 -yl) -3- (5-fluoro-2- (1- ( 2 - hydroxyethyl) - indazol- 5 -yloxy) benzyl) urea hydrochloride
EP4190777A1 (en) 2012-04-13 2023-06-07 Epizyme, Inc. Hbr salt form for ezh2 inhibition
WO2013159006A1 (en) 2012-04-20 2013-10-24 Concert Pharmaceuticals, Inc. Polymorphs of (s)-1-(4,4,6,6,6-pentadeutero-5-hydroxyhexyl)-3,7-dimethyl-1h-purine-2,6(3h,7h)-dione
WO2013184878A1 (en) 2012-06-06 2013-12-12 Constellation Pharmaceuticals, Inc. Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof

Also Published As

Publication number Publication date
EP3157928B1 (en) 2019-02-13
US20170137434A1 (en) 2017-05-18
SI3157928T1 (sl) 2019-06-28
LT3157928T (lt) 2019-05-27
CY1121997T1 (el) 2020-10-14
HUE043441T2 (hu) 2019-08-28
TR201906788T4 (tr) 2019-05-21
DK3157928T3 (da) 2019-05-20
RS58730B1 (sr) 2019-06-28
WO2015195862A8 (en) 2016-01-28
WO2015195862A1 (en) 2015-12-23
CA2952830C (en) 2022-11-01
EP3157928A1 (en) 2017-04-26
CA2952830A1 (en) 2015-12-23
CN106687463A (zh) 2017-05-17
PL3157928T3 (pl) 2019-07-31
JP2017519051A (ja) 2017-07-13
PT3157928T (pt) 2019-05-30
ES2725928T3 (es) 2019-09-30
JP6682522B2 (ja) 2020-04-15
CN106687463B (zh) 2019-04-09
US9969747B2 (en) 2018-05-15

Similar Documents

Publication Publication Date Title
HRP20190842T1 (hr) Kristalni oblici 2-((4s)-6-(4-hlorofenil)-1-metil-4h-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamida
CY1125110T1 (el) Ενωσεις δι-κυκλικου-συντηγμενου ετεροαρυλιου ή αρυλιου και η χρηση αυτων ως αναστολεις irak4
EA201891099A1 (ru) 7-(тиазол-5-ил)пирролопиримида в качестве агониста рецептора tlr7
WO2013171729A3 (en) Aryl and heteroaryl amide compounds as ror gamma t modulator
EA202091115A1 (ru) Производные хиназолина, применяемые для лечения вич
CL2016002310A1 (es) Nuevos compuestos bicíclicos.
EA201790766A1 (ru) Новые соединения метилпиперидина, подходящие для ингибирования микросомальной простагландин-e2-синтазы 1
MX2017007748A (es) Compuestos de heteroarilo anulares fusionados y su uso como inhibidores del receptor de la tirocina cinasa (trk).
HRP20211834T1 (hr) Kristalni čvrsti oblici 6-karboksi-2-(3,5-diklorfenil)benzoksazola
SG11201702498TA (en) Synthesis of ordered microporous carbons by chemical vapor deposition
RU2020110358A (ru) Радиоактивно меченные производные 2-амино-6-фтор-n-[5-фтор- пиридин-3-ил]-пиразоло[1,5-а]пиримидин-3-карбоксамида, используемые в качестве ингибитора atr киназы, препараты на основе этого соединения и его различные твердые формы
AR101403A1 (es) (4s)-4-(4-ciano-2-metoxifenilo)-5-etoxi-2,8-dimetilo-1,4-dihidro-1,6-naftiridin-3-carboxamida, su purificación para su uso como principio activo farmacéutico, un procedimiento para su preparación y su empleo en el tratamiento de enfermedades cardiovasculares
BR112015031619A2 (pt) forma cristalina estável de cloridrato de tipiracil e método de cristalização para a mesma
RU2016146119A (ru) Новый кристалл тетрациклического соединения
HRP20210667T1 (hr) Kristalni oblici antagonista androgenog receptora, postupak pripreme i njihova upotreba
RU2015140619A (ru) Соль производного пиразолохинолина и ее кристалл
TW201613931A (en) Form crystal of bisulfate of janus kinase (JAK) inhibitor and preparation method thereof
CL2016000387A1 (es) Derivados de amida como antagonistas de ácido receptor lisofosfatidico
CY1122468T1 (el) Κρυσταλλικη μορφη διθειικου αναστολεα κινασης jak και μια μεθοδος παρασκευης αυτου
WO2016103262A3 (en) Crystal forms of apomorphine and uses thereof
DK3344684T3 (da) Fremgangsmåde til fremstilling af organosiliciumforbindelser med organyloxygrupper
HRP20192237T1 (hr) Derivati aminohidrotiazina kondenzirani s tetrahidrofuranom, korisni u liječenju alzheimerove bolesti
FR3023177B1 (fr) Procede de preparation de co-cristaux par evaporation flash
EP3391908A4 (en) STABILIZED PHARMACEUTICAL COMPOSITION WITH PEMETREXED OR PHARMACEUTICAL ACCEPTABLE SALT
HRP20190961T1 (hr) Derivat tetrahidropirolo[3,4-d][1,3]tiazina kao inhibitor bace