MX2019015068A - Compuestos de tetrahidroquinolina como inhibidores del bromodominio extra terminal y bromo ( bet ) y el uso de los mismos en el tratamiento de cancer. - Google Patents

Compuestos de tetrahidroquinolina como inhibidores del bromodominio extra terminal y bromo ( bet ) y el uso de los mismos en el tratamiento de cancer.

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Publication number
MX2019015068A
MX2019015068A MX2019015068A MX2019015068A MX2019015068A MX 2019015068 A MX2019015068 A MX 2019015068A MX 2019015068 A MX2019015068 A MX 2019015068A MX 2019015068 A MX2019015068 A MX 2019015068A MX 2019015068 A MX2019015068 A MX 2019015068A
Authority
MX
Mexico
Prior art keywords
bromodomain inhibitors
bet bromodomain
tetrahydroquinoline
compositions
tetrahydroquinoline compositions
Prior art date
Application number
MX2019015068A
Other languages
English (en)
Inventor
Herbertz Torsten
Stryker Kauffman Goss
J Kayser-Bricker Katherine
P Luke George
W Martin Matthew
S Millan David
E R Schiller Shawn
c talbot Adam
W Bair Kenneth
Original Assignee
Forma Therapeutics 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 Forma Therapeutics Inc filed Critical Forma Therapeutics Inc
Publication of MX2019015068A publication Critical patent/MX2019015068A/es

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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
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    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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    • 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
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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Abstract

La presente invención se refiere a inhibidores de bromodominios de terminal extra y bromo (BET) que son útiles para el tratamiento de cáncer, enfermedades inflamatorias, diabetes, y obesidad, que tienen la fórmula (I): (ver Fórmula) en donde W, X, Y, Z, R1, R2, R5, y R8 son como se describe aquí.
MX2019015068A 2013-11-18 2016-05-17 Compuestos de tetrahidroquinolina como inhibidores del bromodominio extra terminal y bromo ( bet ) y el uso de los mismos en el tratamiento de cancer. MX2019015068A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361905639P 2013-11-18 2013-11-18
US201462054811P 2014-09-24 2014-09-24

Publications (1)

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MX2019015068A true MX2019015068A (es) 2020-02-13

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MX2016006438A MX370535B (es) 2013-11-18 2014-11-18 Compuestos de tetrahidroquinolina como inhibidores del bromodominio extra terminal y bromo (bet) y el uso de los mismos en el tratamiento de cáncer.
MX2019015068A MX2019015068A (es) 2013-11-18 2016-05-17 Compuestos de tetrahidroquinolina como inhibidores del bromodominio extra terminal y bromo ( bet ) y el uso de los mismos en el tratamiento de cancer.

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MX2016006438A MX370535B (es) 2013-11-18 2014-11-18 Compuestos de tetrahidroquinolina como inhibidores del bromodominio extra terminal y bromo (bet) y el uso de los mismos en el tratamiento de cáncer.

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Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2802608A4 (en) 2012-01-12 2015-08-05 Univ Yale COMPOUNDS AND METHODS FOR ENHANCED DEGRADATION OF TARGET PROTEINS AND OTHER POLYPEPTIDES BY E3 UBIQUITIN LIGASE
KR20150096794A (ko) 2012-12-21 2015-08-25 제니쓰 에피제네틱스 코포레이션 브로모도메인 저해제로서의 신규한 헤테로사이클릭 화합물
US9636328B2 (en) 2013-06-21 2017-05-02 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
CN109939113B (zh) 2013-06-21 2022-02-15 恒翼生物医药科技(上海)有限公司 双环溴结构域抑制剂
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
CA2919948C (en) 2013-07-31 2020-07-21 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
CN106029076B (zh) 2013-11-18 2019-06-07 福马疗法公司 作为bet溴域抑制剂的苯并哌嗪组合物
MX370535B (es) * 2013-11-18 2019-12-17 Forma Therapeutics Inc Compuestos de tetrahidroquinolina como inhibidores del bromodominio extra terminal y bromo (bet) y el uso de los mismos en el tratamiento de cáncer.
US20160256448A1 (en) * 2013-11-18 2016-09-08 Forma Therapeutics, Inc. Tetrahydroquinoline compositions as bet bromodomain inhibitors
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
EP3227280B1 (en) 2014-12-01 2019-04-24 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
CA2966449A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
EP3233846A4 (en) 2014-12-17 2018-07-18 Zenith Epigenetics Ltd. Inhibitors of bromodomains
EP3270917A4 (en) 2015-03-18 2018-08-08 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
CA2995036A1 (en) 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Tunable endogenous protein degradation
WO2017030814A1 (en) 2015-08-19 2017-02-23 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
EP3454856A4 (en) 2016-05-10 2019-12-25 C4 Therapeutics, Inc. HETEROCYCLIC DEGRONIMERS FOR TARGET PROTEIN REDUCTION
WO2017197046A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation
WO2017197036A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療
ES2919558T3 (es) * 2016-09-14 2022-07-27 Bayer Cropscience Ag Método para producir compuestos bicíclicos halogenados
EP4119552A1 (en) 2017-02-08 2023-01-18 Dana-Farber Cancer Institute, Inc. Regulating chimeric antigen receptors
WO2018207882A1 (ja) * 2017-05-12 2018-11-15 武田薬品工業株式会社 複素環化合物
CN107216331B (zh) * 2017-07-07 2019-06-18 华南理工大学 一种四氢萘啶并四氢喹唑啉衍生物及其合成方法和应用
MX2020000693A (es) 2017-07-18 2020-07-29 Nuvation Bio Inc Compuestos de 1,8-naftiridinona, y usos de los mismos.
JP2020527588A (ja) 2017-07-18 2020-09-10 ニューベイション・バイオ・インコーポレイテッドＮｕｖａｔｉｏｎ Ｂｉｏ Ｉｎｃ． アデノシンアンタゴニストとしてのヘテロ環式化合物
EP3681885B1 (en) 2017-09-15 2024-02-28 Forma Therapeutics, Inc. Tetrahydro-imidazo quinoline compositions as cbp/p300 inhibitors
WO2019089412A1 (en) 2017-11-01 2019-05-09 Merck Sharp & Dohme Corp. Novel substituted tetrahydroquinolin compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
WO2019148055A1 (en) 2018-01-26 2019-08-01 Yale University Imide-based modulators of proteolysis and methods of use
WO2019152440A1 (en) 2018-01-30 2019-08-08 Foghorn Therapeutics Inc. Methods and compounds for treating disorders
AU2019251223A1 (en) 2018-04-13 2020-11-26 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2020006329A1 (en) * 2018-06-29 2020-01-02 Forma Therapeutics, Inc. Salts of (s)-(5-cyclobutoxy-2-methyl-6-(1-(piperidin-4-yl)-1h-pyrazol-4-yl)-3,4-dihydroquinolin-1(2h)-yl)(cyclopropyl)methanone and solid forms thereof
MX2023013508A (es) 2018-06-29 2023-12-13 Forma Therapeutics Inc Inhibicion de la proteina de union a creb (cbp).
CA3110788A1 (en) * 2018-09-13 2020-03-19 Zenith Epigenetics Ltd. Combination therapy for the treatment of estrogen-receptor positive breast cancer
AU2019372121A1 (en) 2018-10-30 2021-05-27 Nuvation Bio Inc. Heterocyclic compounds as BET inhibitors
WO2020132561A1 (en) 2018-12-20 2020-06-25 C4 Therapeutics, Inc. Targeted protein degradation
MX2021008650A (es) 2019-01-18 2021-11-03 Nuvation Bio Inc Compuestos heterociclicos como antagonistas de adenosina.
CN113939291A (zh) 2019-01-18 2022-01-14 诺维逊生物股份有限公司 1,8-萘啶酮化合物及其用途
EP3917529A4 (en) * 2019-01-29 2022-11-02 Foghorn Therapeutics Inc. CONNECTIONS AND USES THEREOF
US20230065463A1 (en) * 2019-01-29 2023-03-02 Foghorn Therapeutics Inc. Compounds and uses thereof
JP2022523073A (ja) * 2019-01-29 2022-04-21 フォグホーン セラピューティクス インコーポレイテッド 化合物及びその使用
EP3938365A4 (en) * 2019-03-15 2023-01-25 Forma Therapeutics, Inc. COMPOSITIONS AND METHODS OF TREATMENT OF ANDROGEN RECEPTOR POSITIVE FORMS OF CANCER
WO2021003163A1 (en) 2019-07-01 2021-01-07 Forma Therapeutics, Inc. Treating cancer with a bromodomain and extra-terminal (bet) family inhibitor
AU2020299592A1 (en) 2019-07-02 2022-02-17 Nuvation Bio Inc. Heterocyclic compounds as BET inhibitors
JPWO2021065980A1 (es) 2019-09-30 2021-04-08
JP2023504249A (ja) 2019-11-28 2023-02-02 バイエル・アクチエンゲゼルシヤフト 免疫活性化のためのｄｇｋアルファ阻害剤としての置換アミノキノロン類
PE20221582A1 (es) 2019-12-19 2022-10-06 Arvinas Operations Inc Compuestos y metodos para la degradacion dirigida de receptor de androgenos
BR112022014968A2 (pt) 2020-01-29 2022-09-20 Foghorn Therapeutics Inc Composto, composição farmacêutica e métodos de inibição do nível de brd9 em uma célula, de inibição da atividade de brd9 em uma célula, de tratamento de um distúrbio, de tratamento de um câncer em um sujeito em necessidade e de tratamento de infecção em um sujeito em necessidade
CN111617305B (zh) * 2020-04-23 2021-05-11 杭州千芝雅卫生用品有限公司 一种亲肤性吸液材料的制备方法
US11787800B2 (en) 2020-07-29 2023-10-17 Foghorn Therapeutics Inc. BRD9 degraders and uses thereof
US11795168B2 (en) 2020-09-23 2023-10-24 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP)
US11801243B2 (en) 2020-09-23 2023-10-31 Forma Therapeutics, Inc. Bromodomain inhibitors for androgen receptor-driven cancers
WO2022271801A1 (en) * 2021-06-23 2022-12-29 Blueprint Medicines Corporation Process for preparing egfr inhibitors
WO2023283263A1 (en) 2021-07-06 2023-01-12 Foghorn Therapeutics Inc. Citrate salt, pharmaceutical compositions, and methods of making and using the same
WO2023185986A1 (en) * 2022-03-31 2023-10-05 Beigene , Ltd. Bcl-xl inhibitors

Family Cites Families (169)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0028765B1 (de) 1979-11-09 1983-05-04 Bayer Ag Alkylharnstoffderivate zur Behandlung von Erkrankungen des Fettstoffwechsels; Verfahren zu deren Herstellung, deren Verwendung in Arzneimitteln zur Behandlung von Fettstoffwechselstörungen, diese enthaltende Arzneimittel, Verfahren zur Herstellung der Arzneimittel sowie einige Alkylharnstoffverbindungen
FR2541680B1 (fr) 1983-02-24 1985-06-14 Rhone Poulenc Sante Nouveaux derives de l'amino-5 dithiole-1,2 one-3, leur preparation et les compositions medicinales qui les contiennent
EP0190105A3 (de) 1985-01-31 1988-10-26 Ciba-Geigy Ag Herbizides Mittel
JPS61227506A (ja) 1985-04-01 1986-10-09 Nippon Tokushu Noyaku Seizo Kk カルバモイルイミダゾ−ル類、その中間体、それらの製法並びに除草剤又は農園芸用殺菌剤
DE3600288A1 (de) 1986-01-08 1987-07-16 Bayer Ag Verwendung von amiden zur verbesserung der kulturpflanzen-vertraeglichkeit von herbizid wirksamen sulfonylharnstoff-derivaten
DE3618004A1 (de) 1986-05-28 1987-12-03 Bayer Ag Verwendung von amiden zur verbesserung der kulturpflanzen-vertraeglichkeit von herbizid wirksamen sulfonyliso(thio)-harnstoff-derivaten
JPS6434982A (en) 1987-07-30 1989-02-06 Nissan Chemical Ind Ltd Condensed heterocyclic derivative, production thereof and herbicide containing said derivative as active ingredient
US5256625A (en) 1987-08-13 1993-10-26 Monsanto Company Safening imidazolinone herbicides
US5502025A (en) 1987-08-13 1996-03-26 Monsanto Company Safening herbicidal pyrazolylsulfonylureas
US5041454A (en) 1987-09-25 1991-08-20 Janssen Pharmaceutica N.V. Novel substituted N-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides
US5201933A (en) 1988-08-01 1993-04-13 Monsanto Company Safening herbicidal benzoic acid derivatives
US5063230A (en) 1988-11-29 1991-11-05 Rhone-Poulenc Rorer Pharmaceuticals Inc. Substituted saturated and unsaturated indole quinoline and benzazepine carboxamides and their use as pharmacological agents
JP2955634B2 (ja) 1990-04-12 1999-10-04 株式会社リコー 電子写真感光体
KR900016822A (ko) 1990-04-20 1990-11-14 하라 레이노스께 슬라이드 프로젝터
AU8400891A (en) 1990-08-13 1992-03-17 G.D. Searle & Co. Use of heterocyclic amino-alcohol compounds for treatment of cns diseases
IL100643A (en) 1991-01-25 1996-10-31 Nippon Kayaku Kk History of hydrazine and pesticides containing these histories as an active ingredient
CA2066104C (en) 1991-04-19 2003-05-27 Hidenori Ogawa Benzazepine derivatives as vasopressin antagonists
US5194571A (en) 1991-08-19 1993-03-16 Eastman Kodak Company Colored polyester compositions
TW222276B (es) 1992-01-27 1994-04-11 Fujisawa Pharmaceutical Co
EP0555183A1 (de) 1992-02-07 1993-08-11 Ciba-Geigy Ag Schädlingsbekämpfungsmittel
US5262564A (en) 1992-10-30 1993-11-16 Octamer, Inc. Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents
GB9307527D0 (en) 1993-04-13 1993-06-02 Fujisawa Pharmaceutical Co New venzamide derivatives,processes for the preparation thereof and pharmaceutical composition comprising the same
GB9307833D0 (en) 1993-04-15 1993-06-02 Glaxo Inc Modulators of cholecystokinin and gastrin
KR100345046B1 (ko) 1993-08-19 2002-12-05 얀센 파마슈티카 엔.브이. 혈관수축성치환된아릴옥시알킬디아민
WO1995017398A1 (en) 1993-12-21 1995-06-29 Smithkline Beecham Plc Indole, indoline and quinoline derivatives with 5ht1d (anti-depressive) activity
US5739129A (en) 1994-04-14 1998-04-14 Glaxo Wellcome Inc. CCK or gastrin modulating 5-heterocyclic-1, 5 benzodiazepines
EP0758330A1 (en) 1994-05-06 1997-02-19 Smithkline Beecham Plc Biphenylcarboxamides useful as 5-ht1d antagonists
GB9416972D0 (en) 1994-08-23 1994-10-12 Smithkline Beecham Plc Carbon side chain/indole/indolene
EP0702004A2 (de) 1994-09-15 1996-03-20 Ciba-Geigy Ag 2,9-Diamino- und 2-amino-8-carbamoyl-4-hydroxy-alkansäureamid-derivative
US5910495A (en) 1994-10-14 1999-06-08 Glaxo Wellcome Inc. Use of 1,5-benzo b!1,4-diazepines to control gastric emptying
US5780464A (en) 1994-10-14 1998-07-14 Glaxo Wellcome Inc. Enteric coated compositions of 1,5-benzodiazepine derivatives having CCK antagonistic or agonistic activity
GB9420763D0 (en) 1994-10-14 1994-11-30 Glaxo Inc Acetamide derivatives
US5688810A (en) 1994-12-22 1997-11-18 Ligand Pharmaceuticals Incorporated Steroid receptor modulator compounds and methods
GB9508637D0 (en) 1995-04-28 1995-06-14 Fujisawa Pharmaceutical Co New use
US5654316A (en) 1995-06-06 1997-08-05 Schering Corporation Piperidine derivatives as neurokinin antagonists
US5767129A (en) 1995-08-24 1998-06-16 Warner-Lambert Company Substituted quinolines and isoquinolines as calcium channel blockers, their preparation and the use thereof
US6696448B2 (en) 1996-06-05 2004-02-24 Sugen, Inc. 3-(piperazinylbenzylidenyl)-2-indolinone compounds and derivatives as protein tyrosine kinase inhibitors
WO1998008818A1 (en) 1996-08-26 1998-03-05 Genetics Institute, Inc. Inhibitors of phospholipase enzymes
DE19638486A1 (de) 1996-09-20 1998-03-26 Basf Ag Hetaroylderivate
DE19638484A1 (de) 1996-09-20 1998-03-26 Basf Ag Hetaroylderivate
WO1998035939A1 (fr) 1997-02-18 1998-08-20 Sanwa Kagaku Kenkyusho Co., Ltd. Derives de diamide malonique et utilisation de ces derniers
AU7526798A (en) 1997-04-18 1998-11-27 Smithkline Beecham Plc Acetamide and urea derivatives, process for their preparation and their use in the treatment of cns disorders
US6011031A (en) 1997-05-30 2000-01-04 Dr. Reddy's Research Foundation Azolidinediones useful for the treatment of diabetes, dyslipidemia and hypertension: process for their preparation and pharmaceutical compositions containing them
DE19727117A1 (de) 1997-06-26 1999-01-07 Boehringer Ingelheim Pharma Phenylalkylderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
AU735366B2 (en) 1997-09-29 2001-07-05 Bristol-Myers Squibb Company Inhibitors of farnesyl protein transferase
CA2307068C (en) 1997-10-27 2007-04-10 Dr. Reddy's Research Foundation Bicyclic compounds, process for their preparation and pharmaceutical compositions containing them
AU1687699A (en) 1997-12-25 1999-07-19 Yamanouchi Pharmaceutical Co., Ltd. Nitrogenous heterocyclic derivatives
US5994379A (en) 1998-02-13 1999-11-30 Merck Frosst Canada, Inc. Bisaryl COX-2 inhibiting compounds, compositions and methods of use
EE200000522A (et) 1998-02-25 2002-02-15 Genetics Institute, Inc. Fosfolipaas A2 ensüümi inhibiitor, seda sisaldav farmatseutiline kompositsioon ning meetod fosfolipaasensüümi toime pärssimiseks
WO1999043670A1 (en) 1998-02-26 1999-09-02 Neurogen Corporation Benzylpiperazinyl- and benzylpiperidinyl ethanone derivatives, their preparation and their use as dopamine d4 receptor antagonists
US6084098A (en) 1999-02-26 2000-07-04 Neurogen Corporation Benzylpiperazinyl and piperidinyl ethanone derivatives: dopamine receptor subtype specific ligands
EP1070054A1 (en) 1998-04-08 2001-01-24 Takeda Chemical Industries, Ltd. Amine compounds, their production and their use as somatostatin receptor antagonists or agonists
WO1999067234A1 (de) 1998-06-19 1999-12-29 Optische Werke G. Rodenstock Photochrome naphthopyrane
DE19827855A1 (de) 1998-06-23 1999-12-30 Hoechst Schering Agrevo Gmbh Kombinationen aus Herbiziden und Safenern
DE19838011C2 (de) 1998-08-21 2000-01-13 Christoph Syldatk Verfahren zur biotechnischen Herstellung von Fettsäuremethylestern ("Biodiesel") auf Molkebasis
JP4548642B2 (ja) * 1998-09-29 2010-09-22 アメリカン・サイアナミド・カンパニー プロテインチロシンキナーゼインヒビターとしての置換３−シアノキノリン
US6048873A (en) 1998-10-01 2000-04-11 Allergan Sales, Inc. Tetrahdroquinolin-2-one 6 or 7-yl, tetrahdroquinilin-2-thione 6 or 7-yl pentadienoic acid and related derivatives having retinoid-like biological activity
AU1881900A (en) 1998-12-23 2000-07-31 Aventis Pharma Limited Dihydro-benzo(1,4)oxazines and tetrahydroquinoxalines
WO2000078716A1 (fr) 1999-06-24 2000-12-28 Toray Industries, Inc. ANTAGONISTES DU RECEPTEUR ADRENERGIQUE-α¿1B?
WO2001002384A1 (de) 1999-07-02 2001-01-11 Optische Werke G. Rodenstock Spirofluorenopyrane
WO2001032610A1 (fr) 1999-10-29 2001-05-10 Kaken Pharmaceutical Co., Ltd. Derive d'uree, son procede de production, et produit pharmaceutique contenant ce derive d'uree
US7101869B2 (en) 1999-11-30 2006-09-05 Pfizer Inc. 2,4-diaminopyrimidine compounds useful as immunosuppressants
TWI245761B (en) 2001-03-01 2005-12-21 Telik Inc Antagonists of MCP-1 function and methods of use thereof
US20030216398A1 (en) 2001-04-05 2003-11-20 Mitsuru Kakihana Soluble beta amyloid precursor protein secretion promoters
AU2002257114A1 (en) 2001-04-06 2002-10-21 Schering Corporation Treatment of malaria with farsenyl protein transferase inhibitors
EP1382598A4 (en) 2001-04-26 2005-03-23 Takeda Pharmaceutical NEW HETEROCYCLIC DERIVATIVES
US6720420B2 (en) 2001-12-21 2004-04-13 Johnson & Johnson Vision Care, Inc. Photochromic oxazine compounds and methods for their manufacture
TW200301698A (en) 2001-12-21 2003-07-16 Bristol Myers Squibb Co Acridone inhibitors of IMPDH enzyme
AU2003249534A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc 6,6-fused heteroaryl derivatives as matrix metalloproteinase inhibitors
GB0224557D0 (en) 2002-10-22 2002-11-27 Glaxo Group Ltd Novel compounds
AU2003303231A1 (en) 2002-12-20 2004-07-14 Warner-Lambert Company Llc Benzoxazines and derivatives thereof as inhibitors of pi3ks
TWI322012B (en) * 2002-12-20 2010-03-21 Organon Nv Tetrahydroquinoline derivatives
WO2004072041A1 (en) 2003-02-12 2004-08-26 Care X S.A. Tetrahydroquinolines as agonists of liver- x receptors
US20040204450A1 (en) 2003-03-28 2004-10-14 Pfizer Inc Quinoline and quinoxaline compounds
KR100729883B1 (ko) 2003-03-28 2007-06-18 화이자 프로덕츠 인코포레이티드 죽상경화증 및 비만증을 치료하기 위한 ｃｅｔｐ억제제로서의 1,2,4-치환된 1,2,3,4-테트라하이드로- 및1,2-디하이드로-퀴놀린 및1,2,3,4-테트라하이드로-퀴녹살린 유도체
WO2005041684A2 (en) 2003-08-06 2005-05-12 Senomyx Inc. Novel flavors, flavor modifiers, tastants, taste enhancers, umami or sweet tastants, and/or enhancers and use thereof
EP1653939A2 (en) 2003-08-07 2006-05-10 Allergan, Inc. Method for treating cachexia with retinoid ligands
EP1515192B1 (en) 2003-09-11 2015-07-15 Ricoh Company, Ltd. Electrophotographic photoconductor, electrophotographic process, electrophotographic apparatus, and process cartridge
DE10343098A1 (de) 2003-09-18 2005-04-14 Bayer Healthcare Ag Tetrahydrochinoxaline und ihre Verwendung
EP1680114A4 (en) 2003-10-28 2008-09-24 Amgen Inc TRIAZOL COMPOUNDS AND RELEVANT PROCEDURES
EP1761515B1 (de) 2003-12-20 2008-11-05 MERCK PATENT GmbH 2-(hetero-)aryl substituierte tetrahydrochinolinderivate
BRPI0418255A (pt) 2003-12-31 2007-04-17 Warner Lambert Co derivados de piperazina e piperidina n-substituìdos
WO2005090282A1 (en) 2004-03-12 2005-09-29 Ligand Pharmaceuticals Incorporated Androgen receptor modulator compounds and methods
EP1732541A4 (en) * 2004-04-07 2008-03-05 Takeda Pharmaceutical CYCLIC COMPOUNDS
JP4604086B2 (ja) 2004-05-07 2010-12-22 エグゼリクシス， インコーポレイテッド Ｒａｆモジュレーターおよびその使用方法
US7442693B2 (en) 2004-05-28 2008-10-28 Smithkline Beecham Corporation Diazepine compounds as ligands of the melanocortin 1 and/or 4 receptors
WO2006009819A1 (en) 2004-06-18 2006-01-26 Array Biopharma Inc. Inhibitors of cholesteryl ester transfer protien
JP2008518003A (ja) 2004-10-29 2008-05-29 アストラゼネカ・アクチエボラーグ 医薬品としての不飽和キノリンもしくはナフタレン誘導体の使用
US20090264384A1 (en) 2004-11-01 2009-10-22 Nuada, Inc. Indole, benzimidazole, and benzolactam boronic acid compounds, analogs thereof and methods of use thereof
WO2007134169A2 (en) 2006-05-10 2007-11-22 Nuada, Llc Indole, benzimidazole, and benzolactam boronic acid compounds, analogs thereof and methods of use thereof
WO2006050236A2 (en) 2004-11-01 2006-05-11 Nuada, Llc Compounds and methods of use thereof
CA2585766A1 (en) 2004-11-01 2006-05-11 Nuada, Llc Compounds and methods of use thereof
AR051780A1 (es) 2004-11-29 2007-02-07 Japan Tobacco Inc Compuestos en anillo fusionados que contienen nitrogeno y utilizacion de los mismos
MX2007010215A (es) 2005-02-24 2007-11-07 Millennium Pharm Inc Antagonistas del receptor pgd2 para el tratamiento de enfermedades inflamatorias.
JP2008531559A (ja) 2005-02-25 2008-08-14 イーライ リリー アンド カンパニー スピロ−複素環式クロマン、チオクロマン及びジヒドロキノリン
WO2006094210A2 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. Tetrahydroquinoxalinone sirtuin modulators
EP1888575A2 (en) 2005-05-09 2008-02-20 Hydra Biosciences, Inc. Compounds for modulating trpv3 function
JP4862042B2 (ja) 2005-05-11 2012-01-25 アボット・ラボラトリーズ バニロイド受容体サブタイプ１（ｖｒ１）のアンタゴニスト及びその使用
JP5145037B2 (ja) 2005-06-14 2013-02-13 日本化薬株式会社 色素増感光電変換素子
EP1896461A2 (en) 2005-06-30 2008-03-12 Amgen Inc. Bis-aryl kinase inhibitors and their use in the treatment of inflammation, angiogenesis and cancer
KR101373535B1 (ko) 2005-07-26 2014-03-12 사노피 Ｒｈｏ-키나제 억제제로서의 피페리디닐-치환된 이소퀴놀론유도체
JP2009510114A (ja) 2005-09-30 2009-03-12 ビテ ファーマシューティカルズ， インコーポレイテッド 特定のｒｘｒアゴニストによる癌治療
US7741317B2 (en) 2005-10-21 2010-06-22 Bristol-Myers Squibb Company LXR modulators
JP2009517434A (ja) 2005-11-30 2009-04-30 エフ．ホフマン−ラ ロシュ アーゲー ５−置換インドール−２−カルボキサミド誘導体
KR101124156B1 (ko) 2005-11-30 2012-03-23 에프. 호프만-라 로슈 아게 1,5-치환된 인돌-2-일 아마이드 유도체
US7713987B2 (en) 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
US20090018118A1 (en) 2005-12-29 2009-01-15 Uros Urleb Heterocyclic compounds
TWI385161B (zh) 2006-02-02 2013-02-11 Mitsubishi Tanabe Pharma Corp 含氮雜雙環化合物
US20070185055A1 (en) 2006-02-06 2007-08-09 Guang Liang Jiang Method for treating cachexia with retinoid ligands
ES2382214T3 (es) 2006-02-13 2012-06-06 F. Hoffmann-La Roche Ag Derivados de sulfonamida heterobicíclicos para el tratamiento de diabetes
JP2009528280A (ja) 2006-02-16 2009-08-06 シェーリング コーポレイション Ｅｒｋインヒビターとしてのピロリジン誘導体
EP2017263A4 (en) 2006-05-09 2011-11-30 Daiichi Sankyo Co Ltd LOWER CARBOXYLIC ACID DERIVATIVE OF HETEROARYLAMIDE
JP2009536953A (ja) 2006-05-11 2009-10-22 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Ｃｅｔｐ阻害剤としての１，２，３，４−テトラヒドロ−キノリン誘導体
US7902184B2 (en) 2006-05-30 2011-03-08 Hoffmann-La Roche Inc. Piperazinyl pyrimidine derivatives
FR2901794A1 (fr) 2006-06-01 2007-12-07 Oreal Composition pour la coloration des fibres keratiniques comprenant un colorant direct diazoique a motif 2-imidazolium
WO2007146230A2 (en) 2006-06-14 2007-12-21 Merck & Co., Inc. Non-nucleoside reverse transcriptase inhibitors
TW200811158A (en) 2006-06-27 2008-03-01 Sanofi Aventis Piperidine or pyrrolidine urea derivatives, their preparation and their therapeutic application
TW200811170A (en) 2006-06-27 2008-03-01 Sanofi Aventis Urea derivatives of tropane, their preparation and their therapeutic application
KR101512477B1 (ko) 2006-07-13 2015-04-15 아칠리온 파르마세우티칼스 인코포레이티드 바이러스 복제 억제제로서 사용되는 4-아미노-4-옥소부타노일 펩티드
GB0618168D0 (en) 2006-09-15 2006-10-25 Babraham Inst Compounds
US20080186971A1 (en) 2007-02-02 2008-08-07 Tarari, Inc. Systems and methods for processing access control lists (acls) in network switches using regular expression matching logic
KR100999592B1 (ko) 2007-02-15 2010-12-08 주식회사 엘지화학 새로운 시클로펜타디에닐 리간드를 갖는 4족 전이금속화합물, 이의 제조방법 및 이를 이용한 올레핀계 중합체의제조방법
TW200848021A (en) 2007-03-06 2008-12-16 Wyeth Corp Sulfonylated heterocycles useful for modulation of the progesterone receptor
GB0706072D0 (en) 2007-03-28 2007-05-09 Sterix Ltd Compound
US20090012045A1 (en) 2007-06-26 2009-01-08 Rigel Pharmaceuticals, Inc. Methods of Treating Cell Proliferative Disorders
US8222417B2 (en) 2007-06-27 2012-07-17 Taisho Pharmaceutical Co., Ltd Compound having 11β-HSD1 inhibitory activity
WO2009020140A1 (ja) 2007-08-06 2009-02-12 Dainippon Sumitomo Pharma Co., Ltd. アダマンチルウレア誘導体
WO2009022746A1 (ja) 2007-08-10 2009-02-19 Nippon Soda Co., Ltd. 含窒素複素環化合物および有害生物防除剤
US9493419B2 (en) 2007-08-21 2016-11-15 The Hong Kong Polytechnic University Quinoline derivatives as anti-cancer agents
WO2009029682A1 (en) 2007-08-28 2009-03-05 Rigel Pharmaceuticals, Inc. Combination therapy with syk kinase inhibitor
EP2203447B1 (en) 2007-09-21 2012-02-29 Janssen Pharmaceutica, N.V. Inhibitors of the interaction between mdm2 and p53
US20100280024A1 (en) 2007-10-15 2010-11-04 Jigar Desai Renin inhibitors
JP2009114107A (ja) 2007-11-06 2009-05-28 Daiichi Sankyo Co Ltd ヘテロアリールアミド低級カルボン酸誘導体を含有する医薬組成物
US8119656B2 (en) 2007-12-07 2012-02-21 The Board Of Regents Of The University Of Texas System Inhibitors of the influenza virus non-structural 1 protein
BRPI0907492A2 (pt) 2008-02-07 2017-06-13 Abbott Lab derivados amida como moduladores alostéricos positivos e métodos de sua utilização
JP2011528369A (ja) 2008-07-16 2011-11-17 シェーリング コーポレイション 二環式ヘテロ環誘導体およびそれらの使用方法
MX2011003951A (es) 2008-10-29 2011-05-03 Hoffmann La Roche Nuevos derivados de fenilamida o de piridilamida y su uso como agonistas de receptor acoplado a proteina g (gpbar1).
TW201030007A (en) 2009-02-06 2010-08-16 Gruenenthal Gmbh Substituted spiro-amides as b1r modulators
AU2010226826A1 (en) 2009-03-18 2011-10-13 Merck Sharp & Dohme Corp. Bicyclic compounds as inhibitors of diacylglycerol acyltransferase
US8791090B2 (en) 2009-03-31 2014-07-29 Kowa Company, Ltd. Prophylactic and/or therapeutic agent for anemia comprising tetrahydroquinoline compound as active ingredient
CA2758904C (en) 2009-04-15 2017-04-04 Jw Pharmaceutical Corporation Novel compounds of reverse-turn mimetics, method for manufacturing the same and use thereof
GB0909672D0 (en) 2009-06-04 2009-07-22 Xention Discovery Ltd Compounds
WO2011054851A1 (en) * 2009-11-05 2011-05-12 Glaxosmithkline Llc Novel process
GB0919432D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919434D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
US8420647B2 (en) 2010-01-21 2013-04-16 Hoffmann-La Roche Inc. 4-phenoxy-nicotinamide or 4-phenoxy-pyrimidine-5-carboxamide compounds
EA020528B1 (ru) 2010-02-11 2014-11-28 Бристол-Майерс Сквибб Компани Макроциклы в качестве ингибиторов фактора xia
US8299117B2 (en) 2010-06-16 2012-10-30 Metabolex Inc. GPR120 receptor agonists and uses thereof
JP6063870B2 (ja) 2010-11-08 2017-01-18 ライセラ・コーポレイション ＲＯＲγ活性の阻害用のＮ−スルホニル化テトラヒドロキノリンおよび関連二環化合物および病気の治療
WO2012137224A1 (en) 2011-04-05 2012-10-11 University Of Delhi Coumarin compounds for the treatment of mycobacterial infections
CN103619862A (zh) 2011-04-14 2014-03-05 诺瓦提斯公司 糖苷衍生物及其用途
GB201106750D0 (en) * 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
US9062028B2 (en) 2011-04-28 2015-06-23 Bristol-Myers Squibb Company Bicyclic nitrogen containing heteroaryl TGR5 receptor modulators
GB201107325D0 (en) * 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
CN102816175B (zh) 2011-06-09 2015-12-16 上海汇伦生命科技有限公司 一种杂环并吡啶酮类化合物,其中间体、制备方法和用途
US8962810B2 (en) 2011-06-16 2015-02-24 AB Pharma Ltd. Macrocyclic heterocyclic compound for inhibiting hepatitis C virus and preparation and use thereof
CN102827170A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
WO2013012723A1 (en) 2011-07-13 2013-01-24 Novartis Ag Novel 2-piperidin-1-yl-acetamide compounds for use as tankyrase inhibitors
WO2013036676A1 (en) 2011-09-06 2013-03-14 New York Blood Center, Inc. Hiv inhibitors
US9403800B2 (en) 2012-01-24 2016-08-02 Chemregen, Inc. Compounds for inhibition of cancer cell proliferation
WO2013152687A1 (zh) 2012-04-11 2013-10-17 中国科学院理化技术研究所 一种近红外荧光染料的制备及应用
CA2871514C (en) 2012-05-08 2020-08-25 Merck Sharp & Dohme Corp. Tetrahydronaphthyridine and related bicyclic compounds for inhibition of ror.gamma.activity and the treatment of disease
WO2013184755A2 (en) 2012-06-07 2013-12-12 Georgia State University Research Foundation, Inc. Seca inhibitors and methods of making and using thereof
EP2909214B1 (en) 2012-10-22 2020-07-22 City of Hope Etp derivatives
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
CN106029076B (zh) 2013-11-18 2019-06-07 福马疗法公司 作为bet溴域抑制剂的苯并哌嗪组合物
MX370535B (es) 2013-11-18 2019-12-17 Forma Therapeutics Inc Compuestos de tetrahidroquinolina como inhibidores del bromodominio extra terminal y bromo (bet) y el uso de los mismos en el tratamiento de cáncer.
US20160256448A1 (en) 2013-11-18 2016-09-08 Forma Therapeutics, Inc. Tetrahydroquinoline compositions as bet bromodomain inhibitors
US20160256458A1 (en) 2013-11-18 2016-09-08 Forma Therapeutics, Inc. Benzopiperazine compositions as bet bromodomain inhibitors

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