KR20190025943A - 피리미딘-기재 항증식제 - Google Patents

피리미딘-기재 항증식제 Download PDF

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Publication number
KR20190025943A
KR20190025943A KR1020197002845A KR20197002845A KR20190025943A KR 20190025943 A KR20190025943 A KR 20190025943A KR 1020197002845 A KR1020197002845 A KR 1020197002845A KR 20197002845 A KR20197002845 A KR 20197002845A KR 20190025943 A KR20190025943 A KR 20190025943A
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formula
alkylene
pharmaceutically acceptable
compound
alkyl
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English (en)
Korean (ko)
Inventor
제이 코프랜드 스트럼
데이비드 정
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쥐원 쎄라퓨틱스, 인크.
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Withdrawn legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains four or more hetero rings
    • 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
    • C07D491/12—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 three hetero rings
    • C07D491/14—Ortho-condensed systems
    • C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • 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
    • C07D491/22—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 four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems
    • 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
    • C07D498/22—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 four or more hetero rings
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
KR1020197002845A 2016-07-01 2017-06-29 피리미딘-기재 항증식제 Withdrawn KR20190025943A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662357630P 2016-07-01 2016-07-01
US62/357,630 2016-07-01
PCT/US2017/040093 WO2018005860A1 (en) 2016-07-01 2017-06-29 Pyrimidine-based antiproliferative agents

Publications (1)

Publication Number Publication Date
KR20190025943A true KR20190025943A (ko) 2019-03-12

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KR1020197002845A Withdrawn KR20190025943A (ko) 2016-07-01 2017-06-29 피리미딘-기재 항증식제

Country Status (13)

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US (2) US10829490B2 (https=)
EP (2) EP3478294A4 (https=)
JP (1) JP2019520379A (https=)
KR (1) KR20190025943A (https=)
CN (1) CN109789143A (https=)
AU (1) AU2017290748A1 (https=)
BR (1) BR112018077136A2 (https=)
CA (1) CA3028751A1 (https=)
EA (1) EA201990187A1 (https=)
IL (1) IL263910A (https=)
MX (1) MX2019000200A (https=)
RU (1) RU2019102647A (https=)
WO (1) WO2018005860A1 (https=)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018005863A1 (en) * 2016-07-01 2018-01-04 G1 Therapeutics, Inc. Pyrimidine-based compounds for the treatment of cancer
RU2019102647A (ru) * 2016-07-01 2020-08-03 Г1 Терапьютикс, Инк. Антипролиферационные средства на основе пиримидина
JOP20170169A1 (ar) 2016-08-29 2019-01-30 Novartis Ag مركبات بيريدازين ثلاثية الحلقة مندمجة تفيد في علاج العدوى بفيروس أورثوميكسو
KR20190092478A (ko) 2016-12-05 2019-08-07 쥐원 쎄라퓨틱스, 인크. 화학요법 레지멘 동안의 면역 반응의 보존
MX2019008158A (es) 2017-01-06 2019-12-09 G1 Therapeutics Inc Terapia de combinacion para el tratamiento del cancer.
CN111163780A (zh) 2017-07-18 2020-05-15 诺维逊生物股份有限公司 作为腺苷拮抗剂的杂环化合物
CA3070073A1 (en) 2017-07-18 2019-01-24 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
JP2021514359A (ja) 2018-02-15 2021-06-10 ニューベイション・バイオ・インコーポレイテッドＮｕｖａｔｉｏｎ Ｂｉｏ Ｉｎｃ． キナーゼ阻害剤としての複素環式化合物
CN118878544A (zh) 2018-02-28 2024-11-01 诺华股份有限公司 作为正粘病毒复制抑制剂用于治疗流感的化合物
WO2019222521A1 (en) * 2018-05-16 2019-11-21 G1 Therapeutics, Inc. Cdk inhibitors for the treatment of neoplastic disorders
CN109836400B (zh) * 2018-09-17 2022-12-09 南通华祥医药科技有限公司 杂环化合物及其盐的制备方法
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
WO2020140054A1 (en) 2018-12-28 2020-07-02 Spv Therapeutics Inc. Cyclin-dependent kinase inhibitors
CN111377921A (zh) * 2018-12-29 2020-07-07 武汉光谷通用名药物研究院有限公司 Cdk4-flt3抑制剂及其用途
AU2020208644A1 (en) 2019-01-18 2021-08-26 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
WO2020150676A1 (en) 2019-01-18 2020-07-23 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
TW202100520A (zh) 2019-03-05 2021-01-01 美商英塞特公司 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
WO2020206034A1 (en) * 2019-04-01 2020-10-08 G1 Therapeutics, Inc. Cell cycle inhibiting compounds for the treatment of medical disorders
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
WO2020260252A1 (en) 2019-06-24 2020-12-30 Boehringer Ingelheim International Gmbh New macrocyclic compounds and derivatives as egfr inhibitors
CA3150681A1 (en) 2019-08-14 2021-02-18 Incyte Corporation Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
US12570660B2 (en) 2019-08-16 2026-03-10 Cyclacel Pharmaceuticals, Inc Process for the preparation of a pyrimidino-diazepine derivative
US11851426B2 (en) 2019-10-11 2023-12-26 Incyte Corporation Bicyclic amines as CDK2 inhibitors
KR20230012547A (ko) 2020-05-19 2023-01-26 쥐원 쎄라퓨틱스, 인크. 의학적 장애의 치료를 위한 시클린-의존성 키나제 억제 화합물
US10988479B1 (en) 2020-06-15 2021-04-27 G1 Therapeutics, Inc. Morphic forms of trilaciclib and methods of manufacture thereof
KR20230112605A (ko) * 2020-08-07 2023-07-27 에이비엠 쎄라퓨틱스 코포레이션 키나아제 억제제 및 그의 용도
US20240000782A1 (en) * 2020-12-02 2024-01-04 Telios Pharma, Inc. Methods and compositions for treating an ophthalmic condition
IL308318A (en) * 2021-05-11 2024-01-01 Abbvie Inc Dosage regimens of VENETOCLAX for use in the treatment of MYELODYSPLASTIC syndromes in combination with a CYP3A inhibitor and AZACITIDINE
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
CN113788837B (zh) * 2021-08-02 2022-08-26 深圳湾实验室坪山生物医药研发转化中心 Trilaciclib的合成方法
CN113786491B (zh) * 2021-10-08 2023-03-28 中国医学科学院医药生物技术研究所 一种含汉防己甲素、二氢槲皮素或槲皮素的抗肿瘤联用制剂
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
IL317242A (en) * 2022-06-20 2025-01-01 Incyclix Bio Llc Cyclin-dependent kinase 2 inhibitors for medical treatment
IT202300001971A1 (it) * 2023-02-07 2024-08-07 Olon Spa Processo per la preparazione di trilaciclib o un suo sale.
WO2025238662A1 (en) * 2024-05-15 2025-11-20 Msn Laboratories Private Limited, R&D Center Improved process for the preparation of 4-amino-n-[(1s)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinecarboxamide and its salts

Family Cites Families (108)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4418068A (en) 1981-04-03 1983-11-29 Eli Lilly And Company Antiestrogenic and antiandrugenic benzothiophenes
TW366342B (en) 1992-07-28 1999-08-11 Lilly Co Eli The use of 2-phenyl-3-aroylbenzothiophenes in inhibiting bone loss
US5565215A (en) 1993-07-23 1996-10-15 Massachusettes Institute Of Technology Biodegradable injectable particles for imaging
US5478847A (en) 1994-03-02 1995-12-26 Eli Lilly And Company Methods of use for inhibiting bone loss and lowering serum cholesterol
GB9412273D0 (en) 1994-06-18 1994-08-10 Univ Nottingham Administration means
US6007845A (en) 1994-07-22 1999-12-28 Massachusetts Institute Of Technology Nanoparticles and microparticles of non-linear hydrophilic-hydrophobic multiblock copolymers
US6413539B1 (en) 1996-10-31 2002-07-02 Poly-Med, Inc. Hydrogel-forming, self-solvating absorbable polyester copolymers, and methods for use thereof
US5628984A (en) 1995-07-31 1997-05-13 University Of North Carolina At Chapel Hill Method of detecting lung disease
US5998402A (en) 1996-04-19 1999-12-07 American Home Products Corporation 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents
US5780497A (en) 1996-04-19 1998-07-14 American Home Products Corporation 2-phenyl-1- 4-(amino-1-yl-alk-1-ynyl)-benzyl!-1H-indol-5-ols as estrogenic agents
TW397821B (en) 1996-04-19 2000-07-11 American Home Produits Corp 3-[4-(2-phenyl-indole-1-ylmethyl)-phenyl]-acrylamides and 2-phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol as well as pharmaceutical compositions of estrogenic agents thereof
US5880137A (en) 1996-04-19 1999-03-09 American Home Products Corporation 2-phenyl-1- 4-(amino-1-yl-alk-1-ynyl)-benzyl!-1H-indol-5-ols as estrogenic agents
US6005102A (en) 1997-10-15 1999-12-21 American Home Products Corporation Aryloxy-alkyl-dialkylamines
ID24568A (id) 1997-11-06 2000-07-27 American Home Prod Kontrasepsi oral yang mengandung anti-estrogen plus progestin
US6326392B1 (en) 1997-11-06 2001-12-04 American Home Products Corporation Anti-estrogen plus progestin containing oral contraceptives
US6583170B1 (en) 1998-05-15 2003-06-24 Wyeth 2-Phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol and estrogen formulations
US6479535B1 (en) 1998-05-15 2002-11-12 Wyeth 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole and estrogen formulations
US6287588B1 (en) 1999-04-29 2001-09-11 Macromed, Inc. Agent delivering system comprised of microparticle and biodegradable gel with an improved releasing profile and methods of use thereof
CO5271696A1 (es) 2000-01-12 2003-04-30 Pfizer Prod Inc Procedimiento para reducir la morbilidad y el riesgo de mortalidad
CO5271709A1 (es) 2000-01-12 2003-04-30 Pfizer Prod Inc Composiciones y procedimientos para el y tratamiento de afecciones que responden a estrogenos
CO5271697A1 (es) 2000-01-12 2003-04-30 Pfizer Prod Inc Composiciones y procedimientos para el tratamiento de afecciones que responden a un aumento de testosterona
CO5251465A1 (es) 2000-01-26 2003-02-28 Pfizer Prod Inc Composiciones y procedimientos para tratar la osteoporosis y reducir el colesterol
EP1268477B1 (en) 2000-03-15 2010-04-21 Sanofi-Aventis Deutschland GmbH Substituted beta-carbolines with ikb-kinase inhibiting activity
US20020013327A1 (en) 2000-04-18 2002-01-31 Lee Andrew G. Compositions and methods for treating female sexual dysfunction
US6589549B2 (en) 2000-04-27 2003-07-08 Macromed, Incorporated Bioactive agent delivering system comprised of microparticles within a biodegradable to improve release profiles
US6495164B1 (en) 2000-05-25 2002-12-17 Alkermes Controlled Therapeutics, Inc. I Preparation of injectable suspensions having improved injectability
AU2001271785A1 (en) 2000-07-06 2002-01-21 American Home Products Corporation Combinations of statins, estrogenic agents and optionally estrogens
MXPA03000170A (es) 2000-07-06 2003-05-27 Wyeth Corp Combinaciones de un inhibidor de recaptacion de serotonina selectivo y agentes estrogenicos.
AU2001271784A1 (en) 2000-07-06 2002-01-21 Wyeth Therapy for prosthesis-related bone degeneration
WO2002003989A2 (en) 2000-07-06 2002-01-17 Wyeth Use of substituted indole compounds for treating sphincter incontinence
AU2001273144A1 (en) 2000-07-06 2002-01-21 Wyeth Use of substituted indole compounds for treating neuropeptide y-related conditions
WO2002003990A2 (en) 2000-07-06 2002-01-17 Wyeth Use of substituted insole compounds for treating excessive intraocular pressure
AU2001273125A1 (en) 2000-07-06 2002-01-21 American Home Products Corporation Combinations of bisphosphonates, estrogenic agents and optionally estrogens
WO2002003986A2 (en) 2000-07-06 2002-01-17 Wyeth Use of substituted indole compounds for treating breast disorders
AR030064A1 (es) 2000-07-06 2003-08-13 Wyeth Corp Metodos para inhibir los efectos uterotroficos de los agentes estrogenicos
AU7178301A (en) 2000-07-06 2002-01-21 American Home Prod Methods for increasing nitric oxide synthase activity
EP1177787A3 (en) 2000-07-28 2003-09-10 Pfizer Products Inc. Use of an estrogen agonist/antagonist for treating cataracts
JP2004507465A (ja) 2000-08-11 2004-03-11 ワイス エストロゲン受容体陽性癌腫の治療方法
EP1192945A3 (en) 2000-09-21 2004-03-03 Pfizer Products Inc. Use of an estrogen agonist/antagonist for treating osteoarthritis
IL145838A (en) 2000-10-16 2008-11-03 Pfizer Prod Inc Use of an estrogen agonist/antagonist for the manufacture of a medicament for treating vaginitis
CN1507357A (zh) 2000-10-31 2004-06-23 PRҩƷ���޹�˾ 提高生物活性分子传递的方法和组合物
AU781168B2 (en) 2001-01-26 2005-05-12 Pfizer Products Inc. Method of treating certain cancers using an estrogen agonist/antagonist
GB0122318D0 (en) 2001-09-14 2001-11-07 Novartis Ag Organic compounds
MXPA04005939A (es) 2002-01-22 2005-01-25 Warner Lambert Co 2-(piridin-2-ilamino)-pirido[2,3-d]pirimidin-7-onas.
MXPA05007503A (es) * 2003-01-17 2005-09-21 Warner Lambert Co Heterociclicos 2-aminopiridina sustituidos como inhibidores de proliferacion celular.
US20050009910A1 (en) 2003-07-10 2005-01-13 Allergan, Inc. Delivery of an active drug to the posterior part of the eye via subconjunctival or periocular delivery of a prodrug
ES2246694B1 (es) 2004-04-29 2007-05-01 Instituto Cientifico Y Tecnologico De Navarra, S.A. Nanoparticulas pegiladas.
US7771742B2 (en) 2004-04-30 2010-08-10 Allergan, Inc. Sustained release intraocular implants containing tyrosine kinase inhibitors and related methods
US20050244469A1 (en) 2004-04-30 2005-11-03 Allergan, Inc. Extended therapeutic effect ocular implant treatments
WO2005107708A1 (en) 2004-04-30 2005-11-17 Allergan, Inc. Biodegradable intravitreal tyrosine kinase inhibitors implants
CN1956982A (zh) 2004-05-21 2007-05-02 万有制药株式会社 具有氨基噻唑骨架的Cdk4、6选择性抑制剂
AU2006206446A1 (en) 2005-01-21 2006-07-27 Janssen Pharmaceutica N.V. Novel heterocyclic benzo[c]chromene derivatives useful as modulators of the estrogen receptors
US20070071756A1 (en) 2005-09-26 2007-03-29 Peyman Gholam A Delivery of an agent to ameliorate inflammation
US7946916B2 (en) 2006-01-12 2011-05-24 Waterleaf Ltd. Variable payout wager games
JP5819579B2 (ja) 2006-01-13 2015-11-24 サーモディクス，インコーポレイティド 薬物送達のためのマトリックスを含む微粒子
JP5315060B2 (ja) 2006-02-03 2013-10-16 バイオノミックス リミテッド 置換ベンゾフラン、ベンゾチオフェン、ベンゾセレノフェンおよびインドールおよびそれらのチューブリン重合阻害剤としての使用
US20080166411A1 (en) 2006-04-10 2008-07-10 Pfizer Inc Injectable Depot Formulations And Methods For Providing Sustained Release Of Poorly Soluble Drugs Comprising Nanoparticles
WO2009100176A2 (en) 2008-02-07 2009-08-13 Abbott Laboratories Pharmaceutical dosage form for oral administration of tyrosine kinase inhibitor
KR20110015699A (ko) 2008-06-11 2011-02-16 제넨테크, 인크. 디아자카르바졸 및 사용 방법
ES2522346T3 (es) 2008-08-22 2014-11-14 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de CDK
WO2010043633A1 (en) 2008-10-15 2010-04-22 Palau Pharma, S. A. 2h-pyrazolo [4,3-d]pyrimidin-5-amine derivatives as h4 histamine receptor antagonists for the treatment of allergic, immunological and inflammatory diseases
WO2010091187A2 (en) 2009-02-04 2010-08-12 The Brigham And Women's Hospital, Inc. Polymeric nanoparticles with enhanced drug-loading and methods of use thereof
US10952965B2 (en) 2009-05-15 2021-03-23 Baxter International Inc. Compositions and methods for drug delivery
US9556426B2 (en) 2009-09-16 2017-01-31 Celgene Avilomics Research, Inc. Protein kinase conjugates and inhibitors
UY33227A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de la cdk4/6
WO2011109384A2 (en) 2010-03-02 2011-09-09 Allergan, Inc. Biodegradable polymers for lowering intraocular pressure
RS56042B1 (sr) 2010-06-10 2017-09-29 Seragon Pharmaceuticals Inc Modulatori estrogenih receptora i njihove upotrebe
US8853423B2 (en) 2010-06-17 2014-10-07 Seragon Pharmaceuticals, Inc. Indane estrogen receptor modulators and uses thereof
GB2483736B (en) 2010-09-16 2012-08-29 Aragon Pharmaceuticals Inc Estrogen receptor modulators and uses thereof
US10005750B2 (en) 2010-10-06 2018-06-26 J-Pharma Co., Ltd. Developing potent urate transporter inhibitors: compounds designed for their uricosuric action
US8691830B2 (en) 2010-10-25 2014-04-08 G1 Therapeutics, Inc. CDK inhibitors
MX338327B (es) * 2010-10-25 2016-04-12 G1 Therapeutics Inc Inhibidores de cdk.
US8829102B2 (en) 2010-10-27 2014-09-09 Cabot Corporation High loading carbon black masterbatch for pressure pipe applications
US9840515B2 (en) 2010-12-09 2017-12-12 University of Pittsburgh—of the Commonwealth System of Higher Education Protein kinase D inhibitors
TW201500358A (zh) 2010-12-16 2015-01-01 赫夫門羅氏藥廠股份有限公司 三環ｐｉ３ｋ抑制劑化合物及其使用方法
CA2819299A1 (en) 2010-12-24 2012-06-28 Merck Sharp & Dohme B.V. N-substituted azetidine derivatives
RU2628074C2 (ru) 2011-09-30 2017-08-14 Си энд Си РИСЕРЧ ЛЭБОРЕТРИЗ ТРИЦИКЛИЧЕСКИЕ АЗОТСОДЕРЖАЩИЕ ПРОИЗВОДНЫЕ ИМИДАЗО[4,5-с]ПИРИДИНА, ОБЛАДАЮЩИЕ ИНГИБИРУЮЩЕЙ АКТИВНОСТЬЮ В ОТНОШЕНИИ РЕЦЕПТОРА ГИСТАМИНА 4 (hH4R)
WO2013090829A1 (en) 2011-12-14 2013-06-20 Aragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
EP2791128A4 (en) 2011-12-16 2015-04-22 Olema Pharmaceuticals Inc NOVEL BENZOPYRAN COMPOUNDS, COMPOSITIONS AND USES THEREOF
CA2868966C (en) 2012-03-29 2021-01-26 Francis Xavier Tavares Lactam kinase inhibitors
US20140107025A1 (en) 2012-04-16 2014-04-17 Jade Therapeutics, Llc Ocular drug delivery system
CA2870019C (en) 2012-04-26 2020-08-18 Francis Xavier Tavares Synthesis of lactams
WO2014019176A1 (zh) 2012-08-01 2014-02-06 华为技术有限公司 用于同步的方法、装置及系统
EP2895146A1 (en) 2012-09-17 2015-07-22 BIND Therapeutics, Inc. Therapeutic nanoparticles comprising a therapeutic agent and methods of making and using same
KR20150090038A (ko) 2012-09-20 2015-08-05 아키나, 인크. 충전재를 함유한 생분해성 미세캡슐
AU2013337717B2 (en) 2012-11-01 2018-10-25 Infinity Pharmaceuticals, Inc. Treatment of cancers using PI3 kinase isoform modulators
US20140274896A1 (en) * 2013-03-15 2014-09-18 G1 Therapeutics, Inc. Transient Protection of Hematopoietic Stem and Progenitor Cells Against Ionizing Radiation
JP6085391B2 (ja) * 2013-03-15 2017-02-22 ノベリス・インコーポレイテッドＮｏｖｅｌｉｓ Ｉｎｃ． ダル光沢仕上げの圧延肌
ME03557B (me) 2013-03-15 2020-07-20 G1 Therapeutics Inc Privremena zaštiтa normalnih ćelija током hemoterapije
CA2906157C (en) * 2013-03-15 2022-05-17 G1 Therapeutics, Inc. Highly active anti-neoplastic and anti-proliferative agents
AU2014248460B2 (en) 2013-04-01 2019-04-11 Allergan, Inc. Microsphere drug delivery system for sustained intraocular release
UY35590A (es) 2013-05-28 2014-11-28 Astrazeneca Ab Nuevos compuestos para el tratamiento del cáncer
CA2915534A1 (en) 2013-06-19 2014-12-24 Seragon Pharmaceuticals, Inc. Azetidine estrogen receptor modulators and uses thereof
WO2014203132A1 (en) 2013-06-19 2014-12-24 Olema Pharmaceuticals, Inc. Substituted benzopyran compounds, compositions and uses thereof
EA031077B1 (ru) 2013-06-19 2018-11-30 Серагон Фармасьютикалз, Инк. Модулятор рецептора эстрогена и его применения
WO2014203129A1 (en) 2013-06-19 2014-12-24 Olema Pharmaceuticals, Inc. Combinations of benzopyran compounds, compositions and uses thereof
US20160257688A1 (en) 2013-10-24 2016-09-08 Francis Xavier Tavares Process for Synthesis of Lactams
US9481591B1 (en) 2013-12-16 2016-11-01 Barbara Blake Device and process to treat and disinfect sewage, food processing wastewater and other biologically contaminated water
WO2015136016A2 (en) 2014-03-13 2015-09-17 F. Hoffmann-La Roche Ag Therapeutic combinations with estrogen receptor modulators
WO2015161288A1 (en) 2014-04-17 2015-10-22 G1 Therapeutics, Inc. Tricyclic lactams for use as anti-neoplastic and anti-proliferative agents
DK3149008T3 (en) 2014-05-28 2019-04-01 Shanghai Fochon Pharmaceutical Co Ltd Specific protein kinase inhibitors
EP3191098A4 (en) * 2014-09-12 2018-04-25 G1 Therapeutics, Inc. Combinations and dosing regimes to treat rb-positive tumors
WO2016040848A1 (en) 2014-09-12 2016-03-17 G1 Therapeutics, Inc. Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors
TWI874834B (zh) 2014-12-18 2025-03-01 瑞士商赫孚孟拉羅股份公司 四氫-吡啶并[3,4-b]吲哚雌激素受體調節劑及其用途
RU2019102647A (ru) * 2016-07-01 2020-08-03 Г1 Терапьютикс, Инк. Антипролиферационные средства на основе пиримидина
WO2018005863A1 (en) * 2016-07-01 2018-01-04 G1 Therapeutics, Inc. Pyrimidine-based compounds for the treatment of cancer
US11865176B2 (en) 2016-11-08 2024-01-09 Dana-Farber Cancer Institute, Inc. Compositions and methods of modulating anti-tumor immunity
WO2018106870A1 (en) 2016-12-08 2018-06-14 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating cdk4/6-mediated cancer

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