FI114098B - Tricykliska pyrimidinderivat som kan inhibera tyrosinkinaser av en epidermisk växtfaktorreceptorfamilj och farmaceutiska sammansättningar som innehåller dem - Google Patents

Tricykliska pyrimidinderivat som kan inhibera tyrosinkinaser av en epidermisk växtfaktorreceptorfamilj och farmaceutiska sammansättningar som innehåller dem Download PDF

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FI114098B
FI114098B FI962855A FI962855A FI114098B FI 114098 B FI114098 B FI 114098B FI 962855 A FI962855 A FI 962855A FI 962855 A FI962855 A FI 962855A FI 114098 B FI114098 B FI 114098B
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pyrimidine
alkyl
nitrogen
atoms
amino
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FI962855A (sv
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Howard Daniel Hollis Showalter
Alexander James Bridges
William Alexander Denny
David Fry
Alan Kraker
Robert Frederick Meyer
Andrew Mark Thompson
Gordon William Rewcastle
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Warner Lambert Co
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Claims (17)

1. Pyrimidinderivat med formeln
5 Rt -Ri RS ^ X^fenylO^)» * "ώΐά, R* f T ™ Ri° R* ETT Rio
10. Re R7 Re kannetecknat därav, att Y och Z är N, O eller S, A, B, D och E kan alla vara kol, eller högst tvä av 15 dem kan vara kvave, till följd av vilket de äterstäende atomerna mäste vara koi, eller vilka som heist tvä när-liggande positioner i A-E kan vara en heteroatom, N eller S, sä att de bildar en fusionerad ring med fem medlemmar, varvid den ena av de tvä äterstäende atomema mäste vara 20 koi och den andra kan vara antingen koi eller kväve; X = NH; R1 = H eller C^-C^-alkyl; f n = 0, 1 eller 2; om n = 2, R1 kan oberoende av andra vara H eller Cj.-25 C4-alkyl i nägondera förenande kolatomen och bäde R- och : S-stereocenter i nägondera linker hör tili uppfinningen; R2 är halogen, och * * m = 0-3, i vilken formel Ar är fenyl, ' R3, R4, R5 och Rs är H, en lägalkyl (1-4 kolatomer) , 30 en lägalkoxi (1-4 kolatomer), amino eller en lägalkyla-*;;; mino, R7 och R8 kan oberoende av varandra enligt situatio-; : nen vara H eller en lägalkyl (1-4 kolatomer) eller en di- ; C^-C^-alkylamino-C^-C^-alkyl ; ,' , 3 5 R10 är H eller amino; ’ · om vilken som heist av substituenterna R1, R2, R3 \ eller R4 innehäller kirala centra eller om R1 skapar 114098 73 kirala centra i förenande atomer, da hör deras alia stereoisomerer bade separat och som racemiska och/eller diastereoisomera blandningar till uppfinningen; eller ett farmaceutiskt salt eller hydrat därav. 5
2. Pyrimidinderivat enligt patentkravet 1, kännetecknat därav, att det har formeln la eller lb R1 la 10 {*5 τ>3 JL S JL fenyl-(R2)m R« 15 eller R» lb R* X-flyV R* ^Jv. fenyl-(R2)» · ,ΐ$Τοϊο; R* » * väri R1, R2, R3, R4, R5, R6, X, m och n betecknar detsamma V 25 som i patentkravet 1. > · » »
3. Pyrimidinderivat enligt patentkravet 1, kännetecknat ;därav, att det är 4 -(3-bromanilino)bensotieno[3,2-d]pyrimidin; , :, 30 4-(3-bromanilino)-8-nitrobensotieno [3,2-d] pyrimidin,· , ’ 8-amino-4 -(3-bromanilino)bensotieno[3,2-d]pyrimidin; ” 4-(3-bromanilino)-9-metoxibensotieno[3,2-d]pyrimidin; *:‘2 eller 4- (3-bromanilino) tiazolo [4 1,5 ' :4,5] tieno [3,2-d]pyrimidin. 35 . 4. Farmaceutisk sammansättning, som innehäller en tera- peutiskt effektiv mängd av ett pyrimidinderivat med 74 114098 följande struktur, i en blandning med ett farmaceutiskt godtagbart fyllmedel, utspädningsmedel eller bärarmedel Rt Rt
5 Rs X^fenyKR.)- Rs Ra cncr IUA‘ryV\, FU^tT Re R7 Rs 10 väri Y och Z är N, O eller S, A, B; D och E kan alla vara koi, eller högst tvä av dem kan vara kväve, tili följd av vilket de äterstäende atomema mäste vara koi, eller vilka sora heist tvä när-15 liggande positioner i A-E kan vara en heteroatom, N eller S, sd att de bildar en fusionerad ring med fem raedlemmar, varvid den ena av de tvä äterstäende atoraerna mäste vara koi och den andra kan vara antingen koi eller kväve; X = NH;
20 R1 = H eller Cj-C^-alkyl; n = 0, 1 eller 2; om n = 2, R1 kan oberoende av andra vara H eller Cx-: C4-alkyl i nägondera förenande kolatomen och bade R- och S-stereocentra i nägondera linker hör tili uppfinningen;
25 R2 är halogen, och , : m = 0-3, i vilken forrael Ar är fenyl, , R3, R4, R5 och Rs är H, en lägalkyl (1-4 kolatomer) , _ en lägalkoxi (1-4 kolatomer), amino eller en lägalkyla- mino,
3. R7 och R8 kan oberoende av varandra vara H eller en lägalkyl (1-4 kolatomer) eller en di-C^-C^-alkylamino-Cx-'··.* C4-alkyl ; • R10 är H eller amino; • * » » om vilken som heist av substituenterna R1, R2, R3 35 eller R4 innehäller kirala centra eller om R1 skapar t · I kirala centra i förenande atomer, dä deras alla ste- 114098 75 reoisomerer bade separat och som racemiska och/eller diastereoisomera blandningar hör till uppfinningen,- eller ett farmaceutiskt salt eller hydrat av före-ningen. 5
5. Farmaceutisk sammansättning, sorti är lämpad för dosering som inhibitor för familjen epidermala tillväxtfak-torreceptorer av tyrosinkinaser för behandling av cancer, psoriasis, njursjukdom eller pankreatit, eller for inhi-10 bition av blastocyt-implantation, och som innehäller en terapeutiskt effektiv rnangd av pyrimidinderivat med följande struktur i en blandning med ett farmaceutiskt godtagbart fyllmedel, utspädningsmedel eller bärarmedel
15 Fh Rt R5 ^ ^^fenyKRj). R5 RS ^ ^^fenyt(Ri)» * dler N n - iOf li · . 110.1 ii R4." "Έ jTwfljo ^^r^Rto
20 Re R7 . Re väri Y och Z är N, 0 eller S, ,: I A, B, D och E kan alla vara kol, eller högst tvä av dem kan vara kväve, till följd av vilket de äterstäende 25 atomerna mäste vara kol, eller vilka som heist tvä när- . : liggande positioner i A-E kan vara en heteroatom, N eller , ,·. S, sä att de bildar en fusionerad ring med fern medlemmar, ·" varvid den ena av de tvä äterstäende atomerna mäste vara » t · kol och den andra kan vara antingen kol eller kväve;
30 X = NH; *;;; R1 = H eller Ci-C^-alkyl; • I >·.' n = 0, 1 eller 2; : om n s 2, R1 kan oberoende av andra vara H eller Cx- . C4-alkyl i nägondera förenande kolatomen och bade R- och
35 S-stereocentra i nägondera linker hör till uppfinningen; '· ; R2 är halogen, och m = 0-3, i vilken formel Ar är fenyl, 114098 76 R3, R4, R5 och Rs är H, en lägalkyl (1-4 kolatomer) , en lägalkoxi (1-4 kolatomer), amino eller en lägalkyla-mino, R7 och R3 kan oberoende av varandra vara H eller en 5 lägalkyl (1-4 kolatomer) eller en di-C1-C4-alkyl ami no-Cj-C4- alkyl; R10 är H eller amino/ om vilken som heist av substituentema R1, R2, R3 eller R4 innehäller kirala centra eller om R1 skapar 10 kirala centra i forenande atomer, dä deras alia stereo-isomerer bäde separat och som racemiska och/eller dias-tereoisomera blandningar hor till uppfinningen; eller ett farmaceutiskt salt eller hydrat av före-ningen. 15
6. Kontraceptiv sammansättning som innehäller en kontra-ceptivt effektiv mängd av ett pyrimidinderivat med föl-jande formel i en blandning med kontraceptivt godtagbart fyllmedel, utspädningsmedel eller bärarmedel 20 Rt Ri :,.. Rs X\^fe“yl(R*w Rs Ra x (^feny,(Ri)“ V: 2S lkAfVV\, R4."D-=E^ ^Ν^Η,ο *, · Re R? Ra ·;·, väri Y och Z är N, O eller· S, A, B, D och E kan alla vara koi, eller högst tvä av , 30 dem kan vara kväve, tili följd av vilket de äterstäende atomema mäste vara koi, eller vilka som heist tvä närli- > t *;·’ gande positioner i A-E kan vara en heteroatom, N, 0 eller j S, sä att de bildar en fusionerad ring med fem medlemmar, varvid den ena av de tvä äterstäende atomema mäste vara . 35 koi och den andra kan vara antingen koi eller kväve; : x = NH; R1 = H eller Cx-C^-alkyl; / 114098 77 n = O, 1 eller 2; om n = 2, R1 kan oberoende av andra vara H eller Cx-C4-alkyl i nägondera förendande kolatomen och bade R- och S-stereocentra i nägondera linker hör tili uppfinningen;
5 R2 är halogen, och m = 0-3, i vilken formel Ar är fenyl, R3, R4, R5 och R6 är H, en lägalkyl (1-4 kolatomer) , en lägalkoxi (1-4 kolatomer), amino eller en lägalkyl-amino,
10 R7 och R8 kan oberoende av varandra vara H eller en lägalkyl (1-4 kolatomer) eller en di-C1-C4-alkylamino-C1-C4-alkyl ; R10 är H eller amino; om vilken som heist av substituenterna R1, R2, R3 15 eller R4 innehäller kirala centra eller om R1 skapar kirala centra i förenande atomer, dä alla deras stere-oisomerer bäde separat och som racemiska och/eller dias-tereoisomera blandningar hör tili uppfinningen; eller ett farmaceutiskt sait eller hydrat av före-20 ningen. t t * S i > t * f
FI962855A 1994-01-25 1996-07-15 Tricykliska pyrimidinderivat som kan inhibera tyrosinkinaser av en epidermisk växtfaktorreceptorfamilj och farmaceutiska sammansättningar som innehåller dem FI114098B (sv)

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Application Number Priority Date Filing Date Title
US18674594A 1994-01-25 1994-01-25
US18673594A 1994-01-25 1994-01-25
US18673594 1994-01-25
US18674594 1994-01-25
US08/358,352 US5679683A (en) 1994-01-25 1994-12-23 Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
US35835294 1994-12-23
US9500911 1995-01-23
PCT/US1995/000911 WO1995019970A1 (en) 1994-01-25 1995-01-23 Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family

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FI962855A0 FI962855A0 (sv) 1996-07-15
FI962855A FI962855A (sv) 1996-09-13
FI114098B true FI114098B (sv) 2004-08-13

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Families Citing this family (384)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK0682027T3 (da) * 1994-05-03 1998-05-04 Ciba Geigy Ag Pyrrolopyrimidinderivater med antiproliferativ virkning
US5476851A (en) * 1994-09-08 1995-12-19 Rhone-Poulenc Rorer Pharmaceuticals, Inc. Pyrazolo[3,4-g]quinoxaline compounds which inhibit PDGF receptor protein tyrosine kinase
TW321649B (sv) * 1994-11-12 1997-12-01 Zeneca Ltd
GB9424233D0 (en) * 1994-11-30 1995-01-18 Zeneca Ltd Quinazoline derivatives
AU5108196A (en) * 1995-03-20 1996-10-08 Dr. Karl Thomae Gmbh Imidazoquinazolines, drugs containing these compounds, their use and process for their preparation
EP0819129B1 (en) * 1995-04-03 2000-08-02 Novartis AG Pyrazole derivatives and processes for the preparation thereof
GB9508537D0 (en) * 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
GB9508565D0 (en) * 1995-04-27 1995-06-14 Zeneca Ltd Quiazoline derivative
EP0824525B1 (en) * 1995-04-27 2001-06-13 AstraZeneca AB Quinazoline derivatives
GB9508538D0 (en) * 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
GB9508535D0 (en) * 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivative
IL122855A (en) * 1995-07-06 2004-08-31 Novartis Ag History of N-Phenyl (Alkyl) - 7H-Pyrolo [-3,2d] Pyrimidine - 4 Amine, their preparation and pharmaceutical preparations containing them
GB9520822D0 (en) * 1995-10-11 1995-12-13 Wellcome Found Therapeutically active compounds
GB9624482D0 (en) * 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
US5760041A (en) * 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
ATE237596T1 (de) 1996-02-13 2003-05-15 Astrazeneca Ab Chinazolinderivate und deren verwendung als vegf hemmer
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
GB9603097D0 (en) * 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline compounds
ATE211134T1 (de) 1996-03-05 2002-01-15 4-anilinochinazolin derivate
US6344459B1 (en) 1996-04-12 2002-02-05 Warner-Lambert Company Irreversible inhibitors of tyrosine kinases
GB9607729D0 (en) * 1996-04-13 1996-06-19 Zeneca Ltd Quinazoline derivatives
ES2249800T3 (es) * 1996-06-24 2006-04-01 Pfizer Inc. Derivados triciclicos sustituidos con fenilamino para el tratamento de enfermedades hiperproliferativas.
ATE384062T1 (de) 1996-08-23 2008-02-15 Novartis Pharma Gmbh Substituierte pyrrolopyrimidine und verfahren zu ihrer herstellung
AU724809B2 (en) * 1996-08-30 2000-09-28 Kyowa Hakko Kogyo Co. Ltd. Imidazoquinazoline derivatives
EP0929553B1 (en) 1996-10-02 2005-03-16 Novartis AG Pyrimidine derivatives and processes for the preparation thereof
US6225318B1 (en) 1996-10-17 2001-05-01 Pfizer Inc 4-aminoquinazolone derivatives
WO1998028281A1 (en) * 1996-12-23 1998-07-02 Celltech Therapeutics Limited Fused polycyclic 2-aminopyrimidine derivatives, their preparation and their use as protein tyrosine kinase inhibitors
US6002008A (en) * 1997-04-03 1999-12-14 American Cyanamid Company Substituted 3-cyano quinolines
US5929080A (en) * 1997-05-06 1999-07-27 American Cyanamid Company Method of treating polycystic kidney disease
ZA986732B (en) * 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitiors of tyrosine kinases
US6251912B1 (en) 1997-08-01 2001-06-26 American Cyanamid Company Substituted quinazoline derivatives
US6323209B1 (en) 1997-11-06 2001-11-27 American Cyanamid Company Method of treating or inhibiting colonic polyps
US6686366B1 (en) 1998-06-02 2004-02-03 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A3 receptor and uses thereof
US6878716B1 (en) 1998-06-02 2005-04-12 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptor and uses thereof
IL139787A0 (en) * 1998-06-02 2002-02-10 Osi Pharm Inc PYRROLO [2, 3d] PYRIMIDINE COMPOSITIONS AND THEIR USE
BRPI9914164B8 (pt) 1998-09-29 2021-05-25 American Cyanamid Co compostos de 3-ciano quinolina
US6288082B1 (en) 1998-09-29 2001-09-11 American Cyanamid Company Substituted 3-cyanoquinolines
US6297258B1 (en) 1998-09-29 2001-10-02 American Cyanamid Company Substituted 3-cyanoquinolines
EA200100687A1 (ru) * 1998-12-22 2001-12-24 Варнер Ламберт Компани Комбинированная химиотерапия
US6432979B1 (en) 1999-08-12 2002-08-13 American Cyanamid Company Method of treating or inhibiting colonic polyps and colorectal cancer
EE05330B1 (et) 1999-11-05 2010-08-16 Astrazeneca Ab Kinasoliini derivaadid kui VEGF-i inhibiitorid
JP2003513075A (ja) * 1999-11-05 2003-04-08 スミスクライン ビーチャム パブリック リミテッド カンパニー 複合５ｈｔ１ａ、５ｈｔ１ｂおよび５ｈｔ１ｄ受容体活性を有するイソキノリンおよびキナゾリン誘導体
UA74803C2 (uk) 1999-11-11 2006-02-15 Осі Фармасьютікалз, Інк. Стійкий поліморф гідрохлориду n-(3-етинілфеніл)-6,7-біс(2-метоксіетокси)-4-хіназолінаміну, спосіб його одержання (варіанти) та фармацевтичне застосування
US7160890B2 (en) 1999-12-02 2007-01-09 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A3 receptor and uses thereof
US6664252B2 (en) 1999-12-02 2003-12-16 Osi Pharmaceuticals, Inc. 4-aminopyrrolo[2,3-d]pyrimidine compounds specific to adenosine A2a receptor and uses thereof
US6680322B2 (en) 1999-12-02 2004-01-20 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptors and uses thereof
US6638929B2 (en) 1999-12-29 2003-10-28 Wyeth Tricyclic protein kinase inhibitors
US6838484B2 (en) 2000-08-24 2005-01-04 University Of Tennessee Research Foundation Formulations comprising selective androgen receptor modulators
US6673802B2 (en) 2000-12-01 2004-01-06 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A3 receptor and uses thereof
US6680324B2 (en) 2000-12-01 2004-01-20 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptors and uses thereof
US7365197B2 (en) 2000-12-29 2008-04-29 Wyeth Method for the regioselective preparation of substituted benzo[g]quinoline-3-carbonitriles and benzo[g]quinazolines
PL217921B1 (pl) 2001-01-05 2014-09-30 Amgen Fremont Inc Przeciwciało przeciw receptorowi insulinopodobnego czynnika wzrostu I, zawierająca go kompozycja farmaceutyczna, sposób jego wytwarzania, zastosowania, linia komórkowa, wyizolowana cząsteczka kwasu nukleinowego, wektor, komórka gospodarza oraz zwierzę transgeniczne
WO2003000194A2 (en) 2001-06-21 2003-01-03 Pfizer Inc. Thienopyridine and thienopyrimidine anticancer agents
JP2005515173A (ja) * 2001-10-31 2005-05-26 バイエル・ヘルスケア・アクチェンゲゼルシャフト ピリミド［４，５−ｂ］インドール誘導体
AR039067A1 (es) 2001-11-09 2005-02-09 Pfizer Prod Inc Anticuerpos para cd40
CA2468673C (en) 2001-11-30 2011-01-25 Osi Pharmaceuticals, Inc. Compounds specific to adenosine a1 and a3 receptors and uses thereof
JP2003183283A (ja) * 2001-12-18 2003-07-03 Takeda Chem Ind Ltd 縮合インドール化合物、その製造法および用途
AU2002357621A1 (en) 2001-12-19 2003-06-30 Ube Industries, Ltd. Process for producing quinazolin-4-one and derivative thereof
ATE458483T1 (de) 2001-12-20 2010-03-15 Osi Pharm Inc Selektive pyrimidin-a2b-antagonistenverbindungen, ihre synthese und verwendung
WO2003064399A1 (fr) * 2002-01-28 2003-08-07 Ube Industries, Ltd. Procede de production de derive de quinazolin-4-one
US7078409B2 (en) 2002-03-28 2006-07-18 Beta Pharma, Inc. Fused quinazoline derivatives useful as tyrosine kinase inhibitors
UA77303C2 (en) 2002-06-14 2006-11-15 Pfizer Derivatives of thienopyridines substituted by benzocondensed heteroarylamide useful as therapeutic agents, pharmaceutical compositions and methods for their use
WO2004046147A1 (ja) * 2002-11-18 2004-06-03 Otsuka Pharmaceutical Co., Ltd. ポリヌクレオチド誘導体及びその利用
WO2004056806A1 (en) 2002-12-19 2004-07-08 Pfizer Inc. 2-(1h-indazol-6-ylamino)-benzamide compounds as protein kinases inhibitors useful for the treatment of ophtalmic diseases
RS53118B (en) 2003-02-26 2014-06-30 Sugen Inc. AMINOHETEROARYL UNITS AS PROTEIN KINASE INHIBITORS
EP1637523A4 (en) * 2003-06-18 2009-01-07 Ube Industries PROCESS FOR PRODUCING A PYRIMIDIN-4-ONE COMPOUND
GB0315966D0 (en) * 2003-07-08 2003-08-13 Cyclacel Ltd Compounds
HN2004000285A (es) 2003-08-04 2006-04-27 Pfizer Prod Inc ANTICUERPOS DIRIGIDOS A c-MET
JP2007504122A (ja) 2003-08-29 2007-03-01 ファイザー・インク 新規抗血管形成剤として有用なチエノピリジン−フェニルアセトアミドおよびその誘導体
AR045563A1 (es) 2003-09-10 2005-11-02 Warner Lambert Co Anticuerpos dirigidos a m-csf
US7291733B2 (en) * 2003-10-10 2007-11-06 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted tricyclic heterocycles and their uses
CA2549869C (en) 2003-12-18 2015-05-05 Janssen Pharmaceutica N.V. Pyrido- and pyrimidopyrimidine derivatives as anti- proliferative agents
JP4503022B2 (ja) 2003-12-23 2010-07-14 ファイザー・インク 新規キノリン誘導体
CN1956966B (zh) * 2004-02-19 2012-04-18 雷克斯安公司 喹唑啉衍生物及其治疗用途
MEP8409A (en) 2004-06-02 2011-12-20 Fused heterocyclic compound
EP2322217A3 (en) 2004-07-16 2011-09-28 Pfizer Products Inc. Combination treatment for non-hematologic malignancies using an anti-IGF-1R antibody
WO2006023843A2 (en) * 2004-08-20 2006-03-02 Bayer Pharmaceuticals Corporation Novel heterocycles
RS51362B (en) 2004-08-26 2011-02-28 Pfizer Inc. ENANTIOMERALLY PURE AMINOHETEROARYL UNITS AS PROTEIN KINASE INHIBITORS
US7511048B2 (en) 2004-10-27 2009-03-31 Bayer Pharmaceuticals Corporation Pyrimidothienoindazoles
NI200700147A (es) 2004-12-08 2019-05-10 Janssen Pharmaceutica Nv Derivados de quinazolina inhibidores de cinasas dirigidos a multip
US20090155247A1 (en) * 2005-02-18 2009-06-18 Ashkenazi Avi J Methods of Using Death Receptor Agonists and EGFR Inhibitors
US20060188498A1 (en) * 2005-02-18 2006-08-24 Genentech, Inc. Methods of using death receptor agonists and EGFR inhibitors
WO2006105488A2 (en) 2005-03-31 2006-10-05 Agensys, Inc. Antibodies and related molecules that bind to 161p2f10b proteins
AU2006238930B2 (en) 2005-04-26 2010-12-23 Pfizer Inc. P-cadherin antibodies
HUE025608T2 (en) 2005-09-07 2016-03-29 Amgen Fremont Inc Human monoclonal antibody against activin receptor-like kinase-1 (ALK-1)
EP2372363A1 (en) 2005-09-20 2011-10-05 OSI Pharmaceuticals, Inc. Biological markers predictive of anti-cancer response to insulin-like growth factor-1
US8633201B2 (en) * 2006-04-07 2014-01-21 Boehringer Ingelheim International Gmbh Thienopyrimidines having Mnk1/Mnk2 inhibiting activity for pharmaceutical compositions
MEP43308A (en) 2006-05-09 2011-02-10 Pfizer Prod Inc Cycloalkylamino acid derivatives and pharmaceutical compositions thereof
NL2000613C2 (nl) 2006-05-11 2007-11-20 Pfizer Prod Inc Triazoolpyrazinederivaten.
DE102006029573A1 (de) * 2006-06-22 2007-12-27 Bayer Schering Pharma Ag Neue Quinazoline als Kinase-Inhibitoren
WO2008033782A2 (en) 2006-09-12 2008-03-20 Genentech, Inc. Methods and compositions for the diagnosis and treatment of lung cancer using pdgfra, kit or kdr gene as genetic marker
SG176461A1 (en) 2006-11-06 2011-12-29 Supergen Inc Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
DK2076289T3 (da) 2007-04-13 2015-02-09 Dana Farber Cancer Inst Inc Fremgangsmåder til behandling af cancerresistens over for ErbB-lægemider
WO2008147687A1 (en) * 2007-05-21 2008-12-04 Mayo Foundation For Medical Education And Research Treating pancreatitis
WO2009004329A1 (en) 2007-07-02 2009-01-08 Cancer Research Technology Limited 9h-pyrimido[4,5-b]indoles, 9h-pyrido[4',3':4,5]pyrrolo[2,3-d]pyridines, and 9h-1,3,6,9-tetraaza-fluorenes as chk1 kinase function inhibitors
DK2188313T3 (en) 2007-08-21 2017-12-11 Amgen Inc HUMAN C-FMS ANTI-BINDING PROTEINS
US7960400B2 (en) 2007-08-27 2011-06-14 Duquesne University Of The Holy Ghost Tricyclic compounds having cytostatic and/or cytotoxic activity and methods of use thereof
US7982035B2 (en) 2007-08-27 2011-07-19 Duquesne University Of The Holy Spirit Tricyclic compounds having antimitotic and/or antitumor activity and methods of use thereof
WO2009033094A2 (en) 2007-09-07 2009-03-12 Agensys, Inc. Antibodies and related molecules that bind to 24p4c12 proteins
US20110053991A1 (en) * 2007-11-19 2011-03-03 Gore Lia Treatment of Histone Deacetylase Mediated Disorders
TW200930375A (en) * 2007-12-21 2009-07-16 Exelixis Inc Benzofuropyrimidinones
TWI472339B (zh) 2008-01-30 2015-02-11 Genentech Inc 包含結合至ｈｅｒ２結構域ii之抗體及其酸性變異體的組合物
US8962629B2 (en) 2008-06-10 2015-02-24 Abbvie Inc. Tricyclic compounds
CA2737597C (en) 2008-10-16 2017-03-14 University Of Pittsburgh-Of The Commonwealth System Of Higher Education Fully human antibodies to high molecular weight-melanoma associated antigen and uses thereof
EP2349235A1 (en) 2008-11-07 2011-08-03 Triact Therapeutics, Inc. Use of catecholic butane derivatives in cancer therapy
JP2012517426A (ja) 2009-02-09 2012-08-02 アステックス ファーマシューティカルズ インコーポレイテッド ピロロピリミジニルａｘｌキナーゼ阻害剤
US20120189641A1 (en) 2009-02-25 2012-07-26 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
JP2012519170A (ja) 2009-02-26 2012-08-23 オーエスアイ・ファーマシューティカルズ，エルエルシー 生体内の腫瘍細胞のｅｍｔステータスをモニターするためのｉｎｓｉｔｕ法
WO2010099138A2 (en) 2009-02-27 2010-09-02 Osi Pharmaceuticals, Inc. Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
US20100222381A1 (en) 2009-02-27 2010-09-02 Hariprasad Vankayalapati Cyclopentathiophene/cyclohexathiophene DNA methyltransferase inhibitors
WO2010099363A1 (en) 2009-02-27 2010-09-02 Osi Pharmaceuticals, Inc. Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
EP2401613A2 (en) 2009-02-27 2012-01-04 OSI Pharmaceuticals, LLC Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
JP2012520893A (ja) 2009-03-18 2012-09-10 オーエスアイ・ファーマシューティカルズ，エルエルシー Ｅｇｆｒ阻害薬及びｉｇｆ−１ｒ阻害剤の投与を含む組み合わせ癌治療
CN102356092B (zh) 2009-03-20 2014-11-05 霍夫曼-拉罗奇有限公司 双特异性抗-her抗体
CA2772194A1 (en) 2009-09-01 2011-03-10 Pfizer Inc. Benzimidazole derivatives
PT3575288T (pt) 2009-09-03 2021-12-09 Bristol Myers Squibb Co Quinazolinas como inibidores dos canais iónicos de potássio
MX2012005464A (es) 2009-11-12 2012-06-08 Genentech Inc Un metodo para promover la densidad de espinas dendriticas.
WO2011058164A1 (en) 2009-11-13 2011-05-19 Pangaea Biotech, S.A. Molecular biomarkers for predicting response to tyrosine kinase inhibitors in lung cancer
HUE033099T2 (en) * 2009-12-01 2017-11-28 Abbvie Inc New tricyclic compounds
CN102712640A (zh) 2010-01-12 2012-10-03 弗·哈夫曼-拉罗切有限公司 三环杂环化合物、其组合物和应用方法
RS55487B2 (sr) 2010-02-12 2024-06-28 Pfizer Soli i polimorfi 8-fluoro-2-{4-[(metilamino}metil]fenil}-1,3,4,5-tetrahidro-6h-azepino[5,4,3-cd]indol-6-ona
JP5981853B2 (ja) 2010-02-18 2016-08-31 ジェネンテック， インコーポレイテッド ニューレグリンアンタゴニスト及び癌の治療におけるそれらの使用
AU2011223655A1 (en) 2010-03-03 2012-06-28 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
WO2011109572A2 (en) 2010-03-03 2011-09-09 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
MX2012010265A (es) 2010-03-17 2012-10-01 Hoffmann La Roche Compuestos de imidazopiridina, composiciones y metodos de uso.
WO2011130654A1 (en) 2010-04-16 2011-10-20 Genentech, Inc. Fox03a as predictive biomarker for pi3k/akt kinase pathway inhibitor efficacy
CN104689314B (zh) 2010-06-16 2018-02-02 高等教育联邦系统-匹兹堡大学 内质蛋白的抗体及其用途
US20120089541A1 (en) 2010-08-31 2012-04-12 Genentech, Inc. Biomarkers and methods of treatment
EP2616072A1 (en) 2010-09-15 2013-07-24 F.Hoffmann-La Roche Ag Azabenzothiazole compounds, compositions and methods of use
WO2012052948A1 (en) 2010-10-20 2012-04-26 Pfizer Inc. Pyridine- 2- derivatives as smoothened receptor modulators
JP2013542966A (ja) 2010-11-19 2013-11-28 エフ．ホフマン−ラ ロシュ アーゲー ピラゾロピリジンならびにｔｙｋ２阻害剤としてのピラゾロピリジン及びそれらの使用
EP2468883A1 (en) 2010-12-22 2012-06-27 Pangaea Biotech S.L. Molecular biomarkers for predicting response to tyrosine kinase inhibitors in lung cancer
WO2012085176A1 (en) 2010-12-23 2012-06-28 F. Hoffmann-La Roche Ag Tricyclic pyrazinone compounds, compositions and methods of use thereof as janus kinase inhibitors
US9134297B2 (en) 2011-01-11 2015-09-15 Icahn School Of Medicine At Mount Sinai Method and compositions for treating cancer and related methods
US20120214830A1 (en) 2011-02-22 2012-08-23 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors in hepatocellular carcinoma
EP2492688A1 (en) 2011-02-23 2012-08-29 Pangaea Biotech, S.A. Molecular biomarkers for predicting response to antitumor treatment in lung cancer
BR112013023050A8 (pt) 2011-03-09 2018-09-25 G Pestell Richard antagonista de ccr5, método para determinar se um indivíduo humano tendo câncer de próstata está sofrendo de ou sob o risco de desenvolver metástase, para identificar um antagonista de ccr5, método para determinar se um indivíduo humano tendo câncer de próstata está sofrendo de ou sob o risco de desenvolver metástase, para identificar um composto candidato, para produzir in vitro células epiteliais primárias, para diagnosticar câncer de próstata, para selecionar um tratamento para um indivíduo tendo um câncer/tumor de próstata, linhagem de célula, e, modelo animal
WO2012129145A1 (en) 2011-03-18 2012-09-27 OSI Pharmaceuticals, LLC Nscle combination therapy
WO2012142164A1 (en) 2011-04-12 2012-10-18 The United States Of America, As Represented By The Secretary, Department Of Health & Human Services Human monoclonal antibodies that bind insulin-like growth factor (igf) i and ii
TR201905909T4 (tr) 2011-04-19 2019-05-21 Pfizer Kanser tedavisi için anti-4-1bb antikorlarının ve adcc indükleyici antikorların kombinasyonları.
JP2014519813A (ja) 2011-04-25 2014-08-21 オーエスアイ・ファーマシューティカルズ，エルエルシー 癌薬剤発見、診断、および治療におけるｅｍｔ遺伝子シグネチャーの使用
WO2013007768A1 (en) 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Tricyclic heterocyclic compounds, compositions and methods of use thereof as jak inhibitors
WO2013007765A1 (en) 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Fused tricyclic compounds for use as inhibitors of janus kinases
DK2734205T3 (en) 2011-07-21 2018-06-14 Tolero Pharmaceuticals Inc Heterocyclic Protein Kinase Inhibitors
KR20140047160A (ko) 2011-08-12 2014-04-21 에프. 호프만-라 로슈 아게 인다졸 화합물, 조성물 및 사용 방법
CN103890007A (zh) 2011-08-17 2014-06-25 霍夫曼-拉罗奇有限公司 神经调节蛋白抗体及其用途
JP6017559B2 (ja) * 2011-08-19 2016-11-02 ディアクソンヒットＤｉａｘｏｎｈｉｔ Ｄｙｒｋ１阻害剤およびその使用
BR112014004762A2 (pt) 2011-08-31 2018-06-19 Genentech Inc métodos de determinação da sensibilidade de crescimento de célula tumoral á inibição por um inibidor de quinase de egfr, de identificação de um paciente com câncer que provavelmente irá se beneficiar do tratamento com um inibidor de efgr, de tratamento de um câncer em um paciente, de seleção de uma terapia para um paciente com câncer e de determinação de superexpressão de gene erbb2 em uma célula
CA2845409A1 (en) 2011-09-20 2013-03-28 Yingjie Lai Imidazopyridine compounds, compositions and methods of use
MX2014003501A (es) 2011-09-22 2014-07-22 Pfizer Derivados de pirrolopirimidina y purina.
US20130084287A1 (en) 2011-09-30 2013-04-04 Genentech, Inc. Diagnostic markers
EP3275902A1 (en) 2011-10-04 2018-01-31 IGEM Therapeutics Limited Ige anti-hmw-maa antibody
MX2014005570A (es) 2011-11-08 2014-05-30 Pfizer El uso de anticuerpos anti factor estimulante de la colonia de macrofagos para tratar trastornos inflamatorios.
EP2776417B1 (en) 2011-11-09 2018-10-31 Cancer Research Technology Limited 5-(pyridin-2-yl-amino)-pyrazine-2-carbonitrile compounds and their therapeutic use
RU2019103083A (ru) 2011-11-30 2019-03-22 Дженентек, Инк. МУТАЦИИ ErbB3 ПРИ РАКЕ
PL2807165T3 (pl) 2012-01-27 2019-09-30 Université de Montréal Pochodne pirymido[4,5-b]indolu i ich zastosowanie do namnażania hematopoetycznych komórek macierzystych
AR090263A1 (es) 2012-03-08 2014-10-29 Hoffmann La Roche Terapia combinada de anticuerpos contra el csf-1r humano y las utilizaciones de la misma
AU2013240261A1 (en) 2012-03-27 2014-09-18 Genentech, Inc. Diagnosis and treatments relating to HER3 inhibitors
WO2013152252A1 (en) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
EP2861302A4 (en) 2012-05-14 2016-08-24 Prostagene Llc USE OF CCR5 MODULATORS IN THE TREATMENT OF CANCER
NZ702050A (en) 2012-05-15 2016-08-26 Cancer Rec Tech Ltd 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof
CA2873971A1 (en) 2012-05-21 2013-11-28 Bayer Pharma Aktiengesellschaft Substituted pyrrolopyrimidines
WO2013190089A1 (en) 2012-06-21 2013-12-27 Pangaea Biotech, S.L. Molecular biomarkers for predicting outcome in lung cancer
DK2909181T3 (da) 2012-10-16 2017-11-20 Tolero Pharmaceuticals Inc PKM2-modulatorer og fremgangsmåder til anvendelse deraf
CN102875558A (zh) * 2012-11-05 2013-01-16 贵州大学 2-氯-4-取代-8-硝基苯并呋喃[3,2-d]嘧啶类化合物及其制备方法和用途
US9260426B2 (en) 2012-12-14 2016-02-16 Arrien Pharmaceuticals Llc Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
MX2015010791A (es) 2013-02-22 2015-11-26 Hoffmann La Roche Metodos para tratar el cancer y prevenir la resistencia a farmacos.
CA2941010A1 (en) 2013-02-26 2014-09-04 Triact Therapeutics, Inc. Cancer therapy
JP2016510751A (ja) 2013-03-06 2016-04-11 ジェネンテック， インコーポレイテッド 抗がん剤耐性を治療及び予防する方法
US10035801B2 (en) 2013-03-13 2018-07-31 Genentech, Inc. Pyrazolo compounds and uses thereof
CA2905993C (en) 2013-03-14 2022-12-06 Tolero Pharmaceuticals, Inc. Substituted 4-amino-pyrimidinyl-2-amino-phenyl derivatives and pharmaceutical compositions thereof for use as jak2 and alk2 inhibitors
RU2015139054A (ru) 2013-03-14 2017-04-19 Дженентек, Инк. Способы лечения рака и профилактики лекарственной резистентности рака
KR20150127203A (ko) 2013-03-14 2015-11-16 제넨테크, 인크. Mek 억제제 화합물과 her3/egfr 억제제 화합물의 조합물 및 사용 방법
KR20150130451A (ko) 2013-03-15 2015-11-23 제넨테크, 인크. 암 치료 방법 및 항암제 내성 예방을 위한 방법
EP2976085A1 (en) 2013-03-21 2016-01-27 INSERM - Institut National de la Santé et de la Recherche Médicale Method and pharmaceutical composition for use in the treatment of chronic liver diseases associated with a low hepcidin expression
US9206188B2 (en) 2013-04-18 2015-12-08 Arrien Pharmaceuticals Llc Substituted pyrrolo[2,3-b]pyridines as ITK and JAK inhibitors
TW201605896A (zh) 2013-08-30 2016-02-16 安美基股份有限公司 Gitr抗原結合蛋白
RU2016112568A (ru) 2013-09-05 2017-10-06 Дженентек, Инк. Антипролиферативные соединения
CA2923667A1 (en) 2013-09-09 2015-03-12 Triact Therapeutics, Inc. Cancer therapy
AR097894A1 (es) 2013-10-03 2016-04-20 Hoffmann La Roche Inhibidores terapéuticos de cdk8 o uso de los mismos
CA2924584A1 (en) 2013-10-03 2015-04-09 Kura Oncology, Inc. Inhibitors of erk and methods of use
US20150104392A1 (en) 2013-10-04 2015-04-16 Aptose Biosciences Inc. Compositions, biomarkers and their use in the treatment of cancer
MX2016004802A (es) 2013-10-18 2016-07-18 Genentech Inc Anticuerpos anti-r-espondina (anti-rspo) y metodos de uso.
UA115388C2 (uk) 2013-11-21 2017-10-25 Пфайзер Інк. 2,6-заміщені пуринові похідні та їх застосування в лікуванні проліферативних захворювань
AU2014364601A1 (en) 2013-12-17 2016-07-07 Genentech, Inc. Methods of treating HER2-positive cancers using PD-1 axis binding antagonists and anti-HER2 antibodies
KR20160099092A (ko) 2013-12-17 2016-08-19 제넨테크, 인크. Ox40 결합 효능제 및 pd-1 축 결합 길항제를 포함하는 조합 요법
MA39776A (fr) 2014-03-24 2017-02-01 Hoffmann La Roche Traitement du cancer avec des antagonistes de c-met et corrélation de ces derniers avec l'expression de hgf
CR20160500A (es) 2014-03-31 2016-12-14 Genentech Inc Anticuerpos anti-ox40 y métodos de uso
BR112016022345A2 (pt) 2014-03-31 2017-10-10 Genentech Inc terapia de combinação compreendendo agentes antiangiogênese e agonistas de ligação de ox40
WO2015155624A1 (en) 2014-04-10 2015-10-15 Pfizer Inc. Dihydropyrrolopyrimidine derivatives
WO2015156674A2 (en) 2014-04-10 2015-10-15 Stichting Het Nederlands Kanker Instituut Method for treating cancer
CR20160497A (es) 2014-04-30 2016-12-20 Pfizer Derivados de diheterociclo enlazado a cicloalquilo
US10548911B2 (en) 2014-06-16 2020-02-04 University Of Rochester Small molecule anti-scarring agents
WO2016001789A1 (en) 2014-06-30 2016-01-07 Pfizer Inc. Pyrimidine derivatives as pi3k inhibitors for use in the treatment of cancer
ES2848857T3 (es) 2014-07-31 2021-08-12 Us Gov Health & Human Services Anticuerpos monoclonales humanos contra EphA4 y su uso
CN107074823B (zh) 2014-09-05 2021-05-04 基因泰克公司 治疗性化合物及其用途
EP3193866A1 (en) 2014-09-19 2017-07-26 Genentech, Inc. Use of cbp/ep300 and bet inhibitors for treatment of cancer
CN107912040B (zh) 2014-10-10 2021-04-06 基因泰克公司 作为组蛋白脱甲基酶抑制剂的吡咯烷酰胺化合物
US20160161485A1 (en) 2014-11-03 2016-06-09 Genentech, Inc. Assays for detecting t cell immune subsets and methods of use thereof
CN114381521A (zh) 2014-11-03 2022-04-22 豪夫迈·罗氏有限公司 用于ox40激动剂治疗的功效预测和评估的方法和生物标志物
WO2016073282A1 (en) 2014-11-06 2016-05-12 Genentech, Inc. Combination therapy comprising ox40 binding agonists and tigit inhibitors
MA40940A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
MA40943A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
CN107108613B (zh) 2014-11-10 2020-02-25 基因泰克公司 布罗莫结构域抑制剂及其用途
SG10201807625PA (en) 2014-11-17 2018-10-30 Genentech Inc Combination therapy comprising ox40 binding agonists and pd-1 axis binding antagonists
US9763922B2 (en) 2014-11-27 2017-09-19 Genentech, Inc. Therapeutic compounds and uses thereof
WO2016097918A1 (en) 2014-12-18 2016-06-23 Pfizer Inc. Pyrimidine and triazine derivatives and their use as axl inhibitors
SG11201704707PA (en) 2014-12-23 2017-07-28 Genentech Inc Compositions and methods for treating and diagnosing chemotherapy-resistant cancers
MY188938A (en) 2014-12-24 2022-01-13 Genentech Inc Therapeutic, diagnostic and prognostic methods for cancer of the bladder
CN107208138A (zh) 2014-12-30 2017-09-26 豪夫迈·罗氏有限公司 用于癌症预后和治疗的方法和组合物
JP6855379B2 (ja) 2015-01-09 2021-04-07 ジェネンテック， インコーポレイテッド 癌の処置のためのヒストンデメチラーゼｋｄｍ２ｂのインヒビターとしての（ピペリジン−３−イル）（ナフタレン−２−イル）メタノン誘導体および関連化合物
CN107406418B (zh) 2015-01-09 2021-10-29 基因泰克公司 4,5-二氢咪唑衍生物及其作为组蛋白脱甲基酶(kdm2b)抑制剂的用途
JP6659703B2 (ja) 2015-01-09 2020-03-04 ジェネンテック， インコーポレイテッド ピリダジノン誘導体および癌の処置におけるそれらの使用
JP6709792B2 (ja) 2015-01-29 2020-06-17 ジェネンテック， インコーポレイテッド 治療用化合物およびその使用
JP6636031B2 (ja) 2015-01-30 2020-01-29 ジェネンテック， インコーポレイテッド 治療用化合物およびその使用
MA41598A (fr) 2015-02-25 2018-01-02 Constellation Pharmaceuticals Inc Composés thérapeutiques de pyridazine et leurs utilisations
CN107709364A (zh) 2015-04-07 2018-02-16 豪夫迈·罗氏有限公司 具有激动剂活性的抗原结合复合体及使用方法
RU2717829C2 (ru) 2015-04-20 2020-03-26 Толеро Фармасьютикалз, Инк. Прогнозирование ответа на альвоцидиб с помощью анализа профиля митохондрий
CN107709344B (zh) 2015-05-01 2022-07-15 共晶制药股份有限公司 用于治疗黄病毒科病毒和癌症的核苷类似物
CN107667119A (zh) 2015-05-12 2018-02-06 豪夫迈·罗氏有限公司 用于癌症的治疗和诊断方法
CA2985804A1 (en) 2015-05-18 2016-11-24 Tolero Pharmaceuticals, Inc. Alvocidib prodrugs having increased bioavailability
EP3708681A1 (en) 2015-05-29 2020-09-16 F. Hoffmann-La Roche AG Therapeutic and diagnostic methods for cancer
CN107922926B (zh) 2015-06-05 2021-09-10 赫马魁北克公司 培养和/或使造血干细胞分化为祖细胞的方法及其用途
WO2016200836A1 (en) 2015-06-08 2016-12-15 Genentech, Inc. Methods of treating cancer using anti-ox40 antibodies
WO2016200835A1 (en) 2015-06-08 2016-12-15 Genentech, Inc. Methods of treating cancer using anti-ox40 antibodies and pd-1 axis binding antagonists
EP3310815A1 (en) 2015-06-17 2018-04-25 F. Hoffmann-La Roche AG Methods of treating locally advanced or metastatic breast cancers using pd-1 axis binding antagonists and taxanes
WO2017009751A1 (en) 2015-07-15 2017-01-19 Pfizer Inc. Pyrimidine derivatives
WO2017024073A1 (en) 2015-08-03 2017-02-09 Tolero Pharmaceuticals, Inc. Combination therapies for treatment of cancer
CN108026110B (zh) 2015-08-26 2022-02-08 国家公共部门基金会卡洛斯三世国家癌症研究中心(F.S.P.Cnio) 作为蛋白激酶抑制剂的稠合三环化合物
IL298355A (en) 2015-09-25 2023-01-01 Genentech Inc Anti-tigit antibodies and methods of use
CN116284011A (zh) 2015-10-16 2023-06-23 艾伯维公司 制备咪唑并[1,2-a]吡咯并[2,3-e]吡嗪类化合物及其固态形式的方法
US11524964B2 (en) 2015-10-16 2022-12-13 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US10550126B2 (en) 2015-10-16 2020-02-04 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11365198B2 (en) 2015-10-16 2022-06-21 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11512092B2 (en) 2015-10-16 2022-11-29 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11773106B2 (en) 2015-10-16 2023-10-03 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US20180371551A1 (en) 2015-12-03 2018-12-27 Agios Pharmaceuticals, Inc. Mat2a inhibitors for treating mtap null cancer
PL3978500T3 (pl) 2015-12-16 2024-03-11 Genentech, Inc. Sposób wytwarzania tricyklicznych związków inhibitorów pi3k
US10596257B2 (en) 2016-01-08 2020-03-24 Hoffmann-La Roche Inc. Methods of treating CEA-positive cancers using PD-1 axis binding antagonists and anti-CEA/anti-CD3 bispecific antibodies
EP4155415A1 (en) 2016-02-29 2023-03-29 Genentech, Inc. Therapeutic and diagnostic methods for cancer
US10730950B2 (en) 2016-03-08 2020-08-04 Janssen Biotech, Inc. GITR antibodies, methods, and uses
RU2625316C1 (ru) * 2016-04-13 2017-07-13 Федеральное государственное бюджетное учреждение науки Институт элементоорганических соединений им. А.Н. Несмеянова Российской академии наук (ИНЭОС РАН) 2-АМИНОЗАМЕЩЕННЫЕ 6-МЕТОКСИ-4-ТРИФТОРМЕТИЛ-9Н-ПИРИМИДО[4,5b]ИНДОЛЫ, СПОСОБ ИХ ПОЛУЧЕНИЯ, ПРИМЕНЕНИЕ И ПРЕДШЕСТВЕННИКИ
EP3865511A1 (en) 2016-04-14 2021-08-18 F. Hoffmann-La Roche AG Anti-rspo3 antibodies and methods of use
EP3443350B1 (en) 2016-04-15 2020-12-09 H. Hoffnabb-La Roche Ag Methods for monitoring and treating cancer
WO2017180581A1 (en) 2016-04-15 2017-10-19 Genentech, Inc. Diagnostic and therapeutic methods for cancer
KR20190003957A (ko) 2016-04-15 2019-01-10 제넨테크, 인크. 암 모니터링 및 치료 방법
EP4067347B1 (en) 2016-05-24 2024-06-19 Genentech, Inc. Heterocyclic inhibitors of cbp/ep300 for the treatment of cancer
MA45146A (fr) 2016-05-24 2021-03-24 Constellation Pharmaceuticals Inc Dérivés de pyrazolopyridine pour le traitement du cancer
US20200129519A1 (en) 2016-06-08 2020-04-30 Genentech, Inc. Diagnostic and therapeutic methods for cancer
KR102474326B1 (ko) 2016-06-22 2022-12-05 반더빌트유니버시티 무스카린성 아세틸콜린 수용체 m4의 양성 알로스테릭 조절제
JP2019530434A (ja) 2016-08-05 2019-10-24 ジェネンテック， インコーポレイテッド アゴニスト活性を有する多価及び多重エピトープ抗体ならびに使用方法
JP7250674B2 (ja) 2016-08-08 2023-04-03 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト がんの治療及び診断方法
AU2017339517B2 (en) 2016-10-06 2024-03-14 Foundation Medicine, Inc. Therapeutic and diagnostic methods for cancer
EP3532091A2 (en) 2016-10-29 2019-09-04 H. Hoffnabb-La Roche Ag Anti-mic antibidies and methods of use
WO2018085803A1 (en) 2016-11-07 2018-05-11 Vanderbilt University Positive allosteric modulators of the muscarinic acetylcholine receptor m4
CN116041365A (zh) 2016-11-07 2023-05-02 范德比尔特大学 毒蕈碱型乙酰胆碱受体m4的正向别构调节剂
CN109862893B (zh) * 2016-11-07 2023-02-17 范德比尔特大学 毒蕈碱型乙酰胆碱受体m4的正向别构调节剂
US11279694B2 (en) 2016-11-18 2022-03-22 Sumitomo Dainippon Pharma Oncology, Inc. Alvocidib prodrugs and their use as protein kinase inhibitors
AU2017379847B2 (en) 2016-12-19 2022-05-26 Sumitomo Pharma Oncology, Inc. Profiling peptides and methods for sensitivity profiling
BR112019012976A2 (pt) 2016-12-22 2019-12-31 Amgen Inc inibidores de kras g12c e métodos de uso dos mesmos
CN106699755B (zh) * 2017-01-10 2018-09-21 清华大学深圳研究生院 一种氮杂吖啶类化合物及其制备方法与用途
ES2953595T3 (es) 2017-03-01 2023-11-14 Hoffmann La Roche Procedimientos diagnósticos y terapéuticos para el cáncer
EP3609537A1 (en) 2017-04-13 2020-02-19 H. Hoffnabb-La Roche Ag An interleukin-2 immunoconjugate, a cd40 agonist, and optionally a pd-1 axis binding antagonist for use in methods of treating cancer
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
MX2020000604A (es) 2017-07-21 2020-09-10 Genentech Inc Métodos terapéuticos y de diagnóstico para el cáncer.
WO2019033043A2 (en) 2017-08-11 2019-02-14 Genentech, Inc. ANTI-CD8 ANTIBODIES AND USES THEREOF
JP7530829B2 (ja) 2017-09-08 2024-08-08 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト がんの診断及び治療方法
MX2020002502A (es) 2017-09-08 2020-07-20 Amgen Inc Inhibidores de kras g12c y metodos para utilizarlos.
JP7196160B2 (ja) 2017-09-12 2022-12-26 スミトモ ファーマ オンコロジー， インコーポレイテッド Ｍｃｌ－１阻害剤アルボシジブを用いた、ｂｃｌ－２阻害剤に対して非感受性である癌の治療レジメン
WO2019075367A1 (en) 2017-10-13 2019-04-18 Tolero Pharmaceuticals, Inc. PKM2 ACTIVATORS IN COMBINATION WITH OXYGEN REACTIVE SPECIES FOR THE TREATMENT OF CANCER
EP3710001A4 (en) 2017-10-27 2021-07-14 University Of Virginia Patent Foundation COMPOUNDS AND PROCEDURES FOR REGULATING, LIMITING OR INHIBITING AVIL EXPRESSION
EP3707510B1 (en) 2017-11-06 2024-06-26 F. Hoffmann-La Roche AG Diagnostic and therapeutic methods for cancer
TW201930311A (zh) 2017-12-05 2019-08-01 泛德比爾特大學 蕈毒鹼型乙醯膽鹼受體m4之正向別構調節劑
WO2019113174A1 (en) * 2017-12-05 2019-06-13 Vanderbilt University Positive allosteric modulators of the muscarinic acetylcholine receptor m4
JP7391027B2 (ja) 2018-02-26 2023-12-04 ジェネンテック， インコーポレイテッド 抗ｔｉｇｉｔ及び抗ｐｄ－ｌ１アンタゴニスト抗体による治療のための投薬
MX2020010836A (es) 2018-05-04 2021-01-08 Amgen Inc Inhibidores de kras g12c y métodos para su uso.
CA3099118A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
MA52564A (fr) 2018-05-10 2021-03-17 Amgen Inc Inhibiteurs de kras g12c pour le traitement du cancer
CN108676009B (zh) * 2018-05-14 2020-04-21 武汉九州钰民医药科技有限公司 作为her2酪氨酸激酶抑制剂的嘧啶衍生物及其应用
CA3100200A1 (en) 2018-05-21 2019-11-28 Nanostring Technologies, Inc. Molecular gene signatures and methods of using same
WO2019232419A1 (en) 2018-06-01 2019-12-05 Amgen Inc. Kras g12c inhibitors and methods of using the same
EP4268898A3 (en) 2018-06-11 2024-01-17 Amgen Inc. Kras g12c inhibitors for treating cancer
WO2020050890A2 (en) 2018-06-12 2020-03-12 Amgen Inc. Kras g12c inhibitors and methods of using the same
CA3103017A1 (en) 2018-06-23 2019-12-26 Genentech, Inc. Methods of treating lung cancer with a pd-1 axis binding antagonist, a platinum agent, and a topoisomerase ii inhibitor
TW202011991A (zh) 2018-07-18 2020-04-01 美商建南德克公司 用pd-1軸結合拮抗劑、抗代謝劑及鉑劑治療肺癌之方法
MX2021000977A (es) 2018-07-26 2021-04-12 Sumitomo Pharma Oncology Inc Metodos para tratar enfermedades asociadas con expresion anormal de receptor de activina a tipo 1 (acvr1) e inhibidores de acvr1 para uso en los mismos.
EP3847154A1 (en) 2018-09-03 2021-07-14 F. Hoffmann-La Roche AG Carboxamide and sulfonamide derivatives useful as tead modulators
AU2019342099A1 (en) 2018-09-19 2021-04-08 Genentech, Inc. Therapeutic and diagnostic methods for bladder cancer
JP7475336B2 (ja) 2018-09-21 2024-04-26 ジェネンテック， インコーポレイテッド トリプルネガティブ乳癌のための診断方法
WO2020070239A1 (en) 2018-10-04 2020-04-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Egfr inhibitors for treating keratodermas
CA3116324A1 (en) 2018-10-18 2020-04-23 Genentech, Inc. Diagnostic and therapeutic methods for sarcomatoid kidney cancer
JP7516029B2 (ja) 2018-11-16 2024-07-16 アムジエン・インコーポレーテツド Ｋｒａｓ ｇ１２ｃ阻害剤化合物の重要な中間体の改良合成法
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法
MA55136A (fr) 2018-11-19 2022-02-23 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
US11034710B2 (en) 2018-12-04 2021-06-15 Sumitomo Dainippon Pharma Oncology, Inc. CDK9 inhibitors and polymorphs thereof for use as agents for treatment of cancer
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
CN113474337A (zh) 2018-12-19 2021-10-01 奥瑞生物药品公司 作为fgfr抑制剂用于治疗癌症的7-((3，5-二甲氧基苯基)氨基)喹喔啉衍生物
ES2953821T3 (es) 2018-12-20 2023-11-16 Amgen Inc Inhibidores de KIF18A
MA54547A (fr) 2018-12-20 2022-03-30 Amgen Inc Amides d'hétéroaryle utiles en tant qu'inhibiteurs de kif18a
WO2020132648A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Kif18a inhibitors
CA3123227A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Heteroaryl amides useful as kif18a inhibitors
JP2022519649A (ja) 2019-02-08 2022-03-24 ジェネンテック， インコーポレイテッド がんの診断および治療方法
US11471456B2 (en) 2019-02-12 2022-10-18 Sumitomo Pharma Oncology, Inc. Formulations comprising heterocyclic protein kinase inhibitors
MX2021010313A (es) 2019-02-27 2021-09-23 Genentech Inc Dosificacion para el tratamiento con anticuerpos anti-tigit y anti-cd20 o anti-cd38.
JP7520389B2 (ja) 2019-02-27 2024-07-23 エピアクシス セラピューティクス プロプライエタリー リミテッド Ｔ細胞機能を評価して治療法に対する応答を予測するための方法および薬剤
KR20210146288A (ko) 2019-03-01 2021-12-03 레볼루션 메디슨즈, 인크. 이환식 헤테로사이클릴 화합물 및 이의 용도
AU2020232242A1 (en) 2019-03-01 2021-09-09 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
JP2022525149A (ja) 2019-03-20 2022-05-11 スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド ベネトクラクスが失敗した急性骨髄性白血病（ａｍｌ）の処置
AU2020245437A1 (en) 2019-03-22 2021-09-30 Sumitomo Pharma Oncology, Inc. Compositions comprising PKM2 modulators and methods of treatment using the same
WO2020223233A1 (en) 2019-04-30 2020-11-05 Genentech, Inc. Prognostic and therapeutic methods for colorectal cancer
CN114269376A (zh) 2019-05-03 2022-04-01 豪夫迈·罗氏有限公司 用抗pd-l1抗体治疗癌症的方法
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
BR112021023277A2 (pt) 2019-05-21 2022-01-04 Amgen Inc Formas em estado sólido
CN110156792A (zh) * 2019-06-28 2019-08-23 广州暨南生物医药研究开发基地有限公司 一种嘧啶并吲哚化合物及其制备方法和应用
CN112300279A (zh) 2019-07-26 2021-02-02 上海复宏汉霖生物技术股份有限公司 针对抗cd73抗体和变体的方法和组合物
MX2022001302A (es) 2019-08-02 2022-03-02 Amgen Inc Inhibidores de kif18a.
CA3146693A1 (en) 2019-08-02 2021-02-11 Amgen Inc. Kif18a inhibitors
AU2020324406A1 (en) 2019-08-02 2022-03-17 Amgen Inc. KIF18A inhibitors
CA3147451A1 (en) 2019-08-02 2021-02-11 Amgen Inc. Kif18a inhibitors
CN110437149B (zh) * 2019-08-20 2021-01-29 大连民族大学 抗肿瘤活性的天然萘基异喹啉类化合物及其组合物、应用
US20230192853A1 (en) 2019-09-04 2023-06-22 Genentech, Inc. Cd8 binding agents and uses thereof
JP2022548978A (ja) 2019-09-27 2022-11-22 ジェネンテック， インコーポレイテッド 薬抗ｔｉｇｉｔ及び抗ｐｄ－ｌ１アンタゴニスト抗体を用いた処置のための投薬
EP4048671A1 (en) 2019-10-24 2022-08-31 Amgen Inc. Pyridopyrimidine derivatives useful as kras g12c and kras g12d inhibitors in the treatment of cancer
US20230024096A1 (en) 2019-10-29 2023-01-26 Hoffmann-La Roche Inc. Bifunctional compounds for the treatment of cancer
CN115873020A (zh) 2019-11-04 2023-03-31 锐新医药公司 Ras抑制剂
CR20220241A (es) 2019-11-04 2022-08-03 Revolution Medicines Inc Inhibidores de ras
CA3160142A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
MX2022005400A (es) 2019-11-06 2022-05-24 Genentech Inc Metodos de diagnostico y terapeuticos para el tratamiento de canceres hematologicos.
WO2021092115A1 (en) 2019-11-08 2021-05-14 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
MX2022005775A (es) 2019-11-13 2022-06-09 Genentech Inc Compuestos terapeuticos y metodos de uso.
CA3161156A1 (en) 2019-11-14 2021-05-20 Amgen Inc. Improved synthesis of kras g12c inhibitor compound
EP4058453A1 (en) 2019-11-14 2022-09-21 Amgen Inc. Improved synthesis of kras g12c inhibitor compound
WO2021108683A1 (en) 2019-11-27 2021-06-03 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
PE20221511A1 (es) 2019-12-13 2022-10-04 Genentech Inc Anticuerpos anti-ly6g6d y metodos de uso
EP4076667A1 (en) 2019-12-20 2022-10-26 Erasca, Inc. Tricyclic pyridones and pyrimidones
CA3163703A1 (en) 2020-01-07 2021-07-15 Steve Kelsey Shp2 inhibitor dosing and methods of treating cancer
WO2021194481A1 (en) 2020-03-24 2021-09-30 Genentech, Inc. Dosing for treatment with anti-tigit and anti-pd-l1 antagonist antibodies
JP2023511595A (ja) 2020-01-27 2023-03-20 ジェネンテック， インコーポレイテッド 抗ｔｉｇｉｔアンタゴニスト抗体を用いたがんを処置するための方法
WO2021155006A1 (en) 2020-01-31 2021-08-05 Les Laboratoires Servier Sas Inhibitors of cyclin-dependent kinases and uses thereof
WO2021177980A1 (en) 2020-03-06 2021-09-10 Genentech, Inc. Combination therapy for cancer comprising pd-1 axis binding antagonist and il6 antagonist
CN115698717A (zh) 2020-04-03 2023-02-03 基因泰克公司 癌症的治疗和诊断方法
CN115885050A (zh) 2020-04-28 2023-03-31 基因泰克公司 用于非小细胞肺癌免疫疗法的方法和组合物
KR20230025691A (ko) 2020-06-16 2023-02-22 제넨테크, 인크. 삼중 음성 유방암을 치료하기 위한 방법과 조성물
KR20230024368A (ko) 2020-06-18 2023-02-20 제넨테크, 인크. 항-tigit 항체 및 pd-1 축 결합 길항제를 사용한 치료
KR20230042600A (ko) 2020-06-18 2023-03-28 레볼루션 메디슨즈, 인크. Ras 억제제에 대한 획득된 저항성을 지연, 예방, 및 치료하는 방법
US11787775B2 (en) 2020-07-24 2023-10-17 Genentech, Inc. Therapeutic compounds and methods of use
CN116568824A (zh) 2020-08-03 2023-08-08 基因泰克公司 淋巴瘤的诊断和治疗方法
EP4196612A1 (en) 2020-08-12 2023-06-21 Genentech, Inc. Diagnostic and therapeutic methods for cancer
CA3187757A1 (en) 2020-09-03 2022-03-24 Ethan AHLER Use of sos1 inhibitors to treat malignancies with shp2 mutations
TW202227460A (zh) 2020-09-15 2022-07-16 美商銳新醫藥公司 Ｒａｓ抑制劑
JP2023544450A (ja) 2020-09-23 2023-10-23 エラスカ・インコーポレイテッド 三環式ピリドン及びピリミドン
IL301547A (en) 2020-10-05 2023-05-01 Genentech Inc Dosage for treatment with bispecific anti-FCRH5/anti-CD3 antibodies
WO2022121813A1 (zh) * 2020-12-07 2022-06-16 北京泰德制药股份有限公司 Sos1抑制剂、包含其的药物组合物及其用途
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
EP4267250A1 (en) 2020-12-22 2023-11-01 Qilu Regor Therapeutics Inc. Sos1 inhibitors and uses thereof
KR20230146052A (ko) 2021-02-12 2023-10-18 에프. 호프만-라 로슈 아게 암 치료용 비시클릭 테트라히드로아제핀 유도체
TW202309022A (zh) 2021-04-13 2023-03-01 美商努法倫特公司 用於治療具egfr突變之癌症之胺基取代雜環
TWI807787B (zh) * 2021-04-19 2023-07-01 大陸商昆藥集團股份有限公司 苯並嘧啶三環衍生物及製備方法和應用
PE20240089A1 (es) 2021-05-05 2024-01-16 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cancer
JP2024516450A (ja) 2021-05-05 2024-04-15 レボリューション メディシンズ インコーポレイテッド 共有結合性ｒａｓ阻害剤及びその使用
AU2022270116A1 (en) 2021-05-05 2023-12-21 Revolution Medicines, Inc. Ras inhibitors
TW202313633A (zh) 2021-05-25 2023-04-01 美商伊瑞斯卡公司 含硫雜芳族三環ｋｒａｓ抑制劑
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
WO2023018699A1 (en) 2021-08-10 2023-02-16 Erasca, Inc. Selective kras inhibitors
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023097194A2 (en) 2021-11-24 2023-06-01 Genentech, Inc. Therapeutic compounds and methods of use
WO2023097195A1 (en) 2021-11-24 2023-06-01 Genentech, Inc. Therapeutic indazole compounds and methods of use in the treatment of cancer
TW202340214A (zh) 2021-12-17 2023-10-16 美商健臻公司 做為shp2抑制劑之吡唑并吡𠯤化合物
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
WO2023191816A1 (en) 2022-04-01 2023-10-05 Genentech, Inc. Dosing for treatment with anti-fcrh5/anti-cd3 bispecific antibodies
WO2023219613A1 (en) 2022-05-11 2023-11-16 Genentech, Inc. Dosing for treatment with anti-fcrh5/anti-cd3 bispecific antibodies
WO2023240058A2 (en) 2022-06-07 2023-12-14 Genentech, Inc. Prognostic and therapeutic methods for cancer
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
TW202417042A (zh) 2022-07-13 2024-05-01 美商建南德克公司 用抗ｆｃｒｈ５／抗ｃｄ３雙特異性抗體進行治療之給藥
WO2024020432A1 (en) 2022-07-19 2024-01-25 Genentech, Inc. Dosing for treatment with anti-fcrh5/anti-cd3 bispecific antibodies
TW202417439A (zh) 2022-08-11 2024-05-01 瑞士商赫孚孟拉羅股份公司 雙環四氫噻吖呯衍生物
WO2024033458A1 (en) 2022-08-11 2024-02-15 F. Hoffmann-La Roche Ag Bicyclic tetrahydroazepine derivatives
WO2024033389A1 (en) 2022-08-11 2024-02-15 F. Hoffmann-La Roche Ag Bicyclic tetrahydrothiazepine derivatives
WO2024033388A1 (en) 2022-08-11 2024-02-15 F. Hoffmann-La Roche Ag Bicyclic tetrahydrothiazepine derivatives
WO2024081916A1 (en) 2022-10-14 2024-04-18 Black Diamond Therapeutics, Inc. Methods of treating cancers using isoquinoline or 6-aza-quinoline derivatives
WO2024085242A2 (en) 2022-10-21 2024-04-25 Kawasaki Institute Of Industrial Promotion Non-fouling or super stealth vesicle
WO2024091991A1 (en) 2022-10-25 2024-05-02 Genentech, Inc. Therapeutic and diagnostic methods for multiple myeloma
WO2024173842A1 (en) 2023-02-17 2024-08-22 Erasca, Inc. Kras inhibitors

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2949466A (en) 1958-03-04 1960-08-16 Parke Davis & Co Pyrimidine compounds and means of producing the same
US3812127A (en) 1966-10-31 1974-05-21 Pfizer 4-(quinolin-4-yl)piperazine-1-carboxylic acid esters
GB1199768A (en) 1966-10-31 1970-07-22 Pfizer & Co C Nitrogen Heterocycles and process for their preparation
US3517005A (en) 1967-10-26 1970-06-23 Pfizer & Co C Certain 2- and 4-substituted quinazolines
US3702849A (en) 1967-10-26 1972-11-14 Pfizer 4-(isoquinolin-1-yl) piperazine-1-carboxylic acid esters
CH530412A (de) 1968-07-15 1972-11-15 Ciba Geigy Ag Verfahren zur Herstellung von (1)Benzothieno-(2,3-d)pyrimidinen
US3755583A (en) * 1970-06-05 1973-08-28 Chas0!nhx
FR2137271B1 (sv) 1971-05-11 1973-05-11 Progil
GB1417029A (en) 1973-03-07 1975-12-10 Pfizer Ltd Quinazoline-derived amines
US3971783A (en) 1973-03-07 1976-07-27 Pfizer Inc. 4-Aminoquinazoline derivatives as cardiac stimulants
SE435380B (sv) 1976-06-15 1984-09-24 Pfizer Forfarande for framstellning av kinazolinforeningar
US4466965A (en) 1982-07-26 1984-08-21 American Hospital Supply Corporation Phthalazine compounds, compositions and use
WO1984001151A1 (en) 1982-09-24 1984-03-29 Beecham Group Plc Amino-azabicycloalkyl derivatives as dopamine antagonists
IN157280B (sv) 1983-07-15 1986-02-22 Hoechst India
ES8705400A1 (es) 1985-03-14 1987-05-01 Sankyo Co Un procedimiento para la preparacion de nuevos derivados de fenoxialquilaminopirimidina.
US5141941A (en) 1988-11-21 1992-08-25 Ube Industries, Ltd. Aralkylamine derivatives, and fungicides containing the same
GB8912336D0 (en) 1989-05-30 1989-07-12 Smithkline Beckman Intercredit Compounds
US5034393A (en) 1989-07-27 1991-07-23 Dowelanco Fungicidal use of pyridopyrimidine, pteridine, pyrimidopyrimidine, pyrimidopyridazine, and pyrimido-1,2,4-triazine derivatives
JPH03173872A (ja) 1989-09-14 1991-07-29 Ube Ind Ltd アミノピリミジン誘導体、その製造方法及び殺虫・殺菌剤
GB9022644D0 (en) 1990-10-18 1990-11-28 Ici Plc Heterocyclic compounds
SK400992A3 (en) 1990-11-06 1995-08-09 Pfizer Quinazolines derivatives for enhancing antitumor activity
JP2762430B2 (ja) 1991-01-18 1998-06-04 宇部興産株式会社 アラルキルアミノピリミジン類の製法
WO1992014716A1 (en) 1991-02-20 1992-09-03 Pfizer Inc. 2,4-diaminoquinazolines derivatives for enhancing antitumor activity
CA2102780C (en) * 1991-05-10 2007-01-09 Alfred P. Spada Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
DE4131029A1 (de) 1991-09-18 1993-07-29 Basf Ag Substituierte pyrido (2,3-d) pyrimidine als antidots
PT100905A (pt) 1991-09-30 1994-02-28 Eisai Co Ltd Compostos heterociclicos azotados biciclicos contendo aneis de benzeno, ciclo-hexano ou piridina e de pirimidina, piridina ou imidazol substituidos e composicoes farmaceuticas que os contem
US5187168A (en) 1991-10-24 1993-02-16 American Home Products Corporation Substituted quinazolines as angiotensin II antagonists
GB9300059D0 (en) * 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
JP3173872B2 (ja) 1992-05-15 2001-06-04 オリンパス光学工業株式会社 光学素子成形用型および該成形用型を用いた光学素子の成形方法
JPH0641134A (ja) 1992-07-21 1994-02-15 Nippon Soda Co Ltd ピリミドプテリジン誘導体及びその製造方法
GB9323290D0 (en) 1992-12-10 1994-01-05 Zeneca Ltd Quinazoline derivatives
TW444018B (en) 1992-12-17 2001-07-01 Pfizer Pyrazolopyrimidines
JPH06220059A (ja) 1993-01-28 1994-08-09 Tanabe Seiyaku Co Ltd 縮合ピリミジン誘導体及びその製法
DE4308014A1 (de) 1993-03-13 1994-09-15 Hoechst Schering Agrevo Gmbh Kondensierte Stickstoffheterocyclen, Verfahren zu ihrer Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel und Fungizide

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