Astellas Pharma Gmbh

Kotobuki Pharmaceutical Co Ltd

Rational Drug Design Laboratories

Yamanouchi Pharmaceutical Company Ltd.

Mitobridge, Inc.

Akio Kamikawa

Yutaka Kondoh

Hiroshi Tomiyama

Takashi Furutani

Itsuro Shimada

Wataru Hamaguchi

Junji Miyata

Kazuhiko Iikubo

Yoshinori Iwai

Kazuo Kurosawa

Takahiro Matsuya

Takashi Kamikubo

Hiroshi Suzuki

Akio Kakefuda

Yohei Seki

Kentaro Enjo

Masakatsu Kawakami

Toru Kontani

Toru Asano

Kazuyuki Hattori

Tomoaki Kawano

Kenji Sudo

Junko Maeda

Masaaki Hirano

Ryo Sato

Satoshi Aoki

Hiroshi Yamada

Tatsuya Niimi

Junji Sato

Koichi Yonezawa

Satoshi Miyamoto

Ryushi Seo

Kenji Negoro

Minoru Yasuda

Hiroyuki Mano

Nobuaki Shindo

Takatoshi Soga

Sadao Kuromitsu

Hirokazu Kubota

Kazushi Watanabe

Shinya Nagashima

Ryo Naito

Shigeki Kunikawa

Ryosuke Munakata

Kei Ohnuki

Ikumi Kuriwaki

Michinori Akaiwa

Yohei Koganemaru

Shinji Soga

Shimpei Kawakami

Hideyuki Watanabe

Takuya Washio

Masaki Yokota

Kozo Miyasaka

Tomohiko Yamaguchi

Osamu Ikeda

Jeffrey Ciavarri

Yuka Koizumi

Takashi Ogiyama

Kenichi Suzumura

Shuichirou Kakimoto

Yumi Yamashita

Keiichiro Okuyama

Akihiko Nakamura

Javier Ramos Miguelez

Kai Kitamura

Chulwon Kwon

Rika Hoshi

Yinghua Wang

Kenichi Kakefuda

Junichi Shishikura

Yasushi Amano

Keisuke Tamaki

Takashi Chaen

An antibody-drug conjugate of formula (I) or salt thereof of formula I: may have Ab as an anti-CLDN6 antibody or an antigen-binding fragment thereof. The antibody-drug conjugate of formula (I) may be (a) an antibody-drug conjugate comprising Ab bound to 1-{3-[(3S)-4-[(4-{[2-amino-4-(pentylamino)-5H-pyrrolo[3,2-d]pyrimidin-5-yl]methyl}-3-methoxyphenyl)methyl]-3-(fluoromethyl)piperazin-1-yl]-3-oxopropyl}-1H-pyrrole-2,5-dione, (b) an antibody-drug conjugate comprising Ab bound to {(2S)-1-[(4-{[2-amino-7-chloro-4-(pentylamino)-5H-pyrrolo[3,2-d]pyrimidin-5-yl]methyl}-3-methoxyphenyl)methyl]pyrrolidin-2-yl}methyl[2-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)ethyl]carbamate, (c) an antibody-drug conjugate comprising Ab bound to N-[(4-{[2-amino-4-(pentylamino)-5H-pyrrolo[3,2-d]pyrimidin-5-yl]methyl}-3-methoxyphenyl)methyl]-N-cyclopropyl-3-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)propenamide, or (d) an antibody-drug conjugate comprising Ab bound to 1-{3-[(3R)-4-[(4-{[2-amino-4-(pentylamino)-5H-pyrrolo[3,2-d]pyrimidin-5-yl]methyl}-3-methoxyphenyl)methyl]-3-(fluoromethyl)piperazin-1-yl]-3-oxopropyl}-1H-pyrrole-2,5-dione.

Antibody-drug complex containing toll-like receptor 7/8 dual agonist compound

A compound useful as an active ingredient of a pharmaceutical composition for treatment of cancer related to activation of immune cells or cancer resistant to anti-PD-1 antibody/anti-PD-L1 antibody therapy is provided. The present inventors have conducted studies on a compound useful as an active ingredient of a pharmaceutical composition for treatment of cancer related to activation of immune cells or cancer resistant to anti-PD-1 antibody/anti-PD-L1 antibody therapy, and confirmed that a heteroaryl carboxamide compound has DGK ξ (DGKzeta) inhibitory effect, leading to completion of the present invention. The heteroaryl carboxamide compound of the present invention has DGK ξ inhibitory effect, and can be used as a therapeutic agent for treatment of cancer related to activation of immune cells or cancer resistant to anti-PD-1 antibody/anti-PD-L1 antibody therapy.

Heteroaryl carboxamide compound

[Problem] A compound which is useful as a STING inhibitor is provided. [Means for Solution] The present inventors have found aryl alkynamide derivatives having an inhibitory action on STING. The aryl alkynamide derivatives of the present invention have an inhibitory action on STING and can be used as an agent for treating an autoimmune disease, a neurodegenerative disease, a type I interferonopathy and/or other STING-mediated disease.

Aryl alkynamide derivatives

[Problem] Provided is a compound having a positive allosteric modulating activity (PAM activity) on an &#x3b1;7 nicotinic acetylcholine receptor (&#x3b1;7 nACh receptor). [Means for Solution] The present inventors have studied on a PAM activity on an &#x3b1;7 nACh receptor, and they have found that a tetrahydrooxepinopyridine compound has a PAM activity on an &#x3b1;7 nACh receptor, thereby completing the present invention. The tetrahydrooxepinopyridine compound of the present invention has a PAM activity on an &#x3b1;7 nACh receptor and can be expected as an agent for preventing or treating dementia, cognitive impairment, schizophrenia, Alzheimer's disease, CIAS, negative symptoms of schizophrenia, inflammatory diseases, or pain.

Tetrahydrooxepinopyridine compound

Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.

Diamino heterocyclic carboxamide compound

As a result of studies on compounds having a selective inhibitory activity against 17&#x3b2;HSD type 5, the present inventors have confirmed that a {1-[(indol-2-yl)carbonyl]piperidyl}alkanol derivative has a potent selective inhibitory activity against 17&#x3b2;HSD type 5. The invention has been completed based on these findings. The compound of the present invention can be used as an agent for treating and/or an agent for preventing diseases associated with 17&#x3b2;HSD type 5, such as benign prostatic hyperplasia and prostate cancer, without accompanying adverse effects due to a decrease in testosterone.

Piperidine derivative

The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, lung cancer, non-small cell lung cancer, small cell lung cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive lung cancer, or EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive non-small cell lung cancer, etc.

Di(arylamino)aryl compounds

To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17&#x3b2;HSD type 5. It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17&#x3b2;HSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone, and the present invention has thus been completed.

17&#x3b2;HSD type 5 inhibitor

Provided is a triarylcarboxylic acid derivative, or an isomer, a prodrug, a hydrate, a solvate, a polymorph, or a pharmaceutically acceptable salt thereof, represented by the following general formula (I): wherein A is an optionally substituted aryl or heteroaryl, and B is an optionally substituted monocyclic heteroaryl; and a pharmaceutical composition comprising the same and a pharmaceutically acceptable carrier. The triarylcarboxylic acid derivative (I) exhibits potent xanthine oxidase inhibiting action and is therefore useful as a therapeutic agent for preventing or treating hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy and diabetic retinopathy.

Triarylcarboxylic acid derivative

The present invention relates to a 2-phenylthiophene derivative or a salt thereof, wherein the thiophene ring is substituted with a carboxyl group or the like and the benzene ring has an electron-withdrawing group such as a cyano group and an electron-donating group such as a substituted alkoxy group at the same time. Since the compound of the invention has good xanthine oxidase-inhibitory action and uric acid-lowering action and does not have a structure derived from nucleic acid, the compound has advantages of high safety and excellent effects as compared with conventional compounds and is useful as a therapeutic or preventive agent for hyperuricemia, gout, inflammatory bowel diseases, diabetic kidney diseases, diabetic retinopathy, or the like.

2-phenylthiophene derivative

There is provided a pharmaceutical drug, particularly a novel compound useful for prophylaxis or a therapeutic treatment of various diseases involving infections with viruses of the herpesvirus family, specifically various herpesvirus infections such as varicella (chicken pox) via varicella zoster virus, varicella zoster via recurrent infection with latent varicella zoster virus, herpes labialis and herpes encephalitis via HSV-1 and genital herpes via HSV-2 infection. An N-{2-[(4-substituted phenyl)amino]-2-oxoethyl}tetrahydro-2H-thiopyran-4-carboxamide derivative, of which phenyl group is substituted at position 4 with a specific 5- or 6-membered heteroaryl group, and a salt thereof have an effective anti-virus activity, and the oral administration thereof at a low dose enabled the therapeutic treatment of the above diseases.

Amide derivative

A pharmaceutical drug, particularly a novel compound useful for the prophylaxis or therapeutic treatment of various diseases involving infections with viruses of the Herpesviridae family, specifically various herpesvirus infections such as varicella (chicken pox) via varicella zoster virus, varicella zoster via recurrent infection with latent varicella zoster virus, herpes labialis and herpes encephalitis via HSV-1 and genital herpes via HSV-2 infection. N-{2-[(4-Substituted phenyl)amino]-2-oxoethyl}tetrahydro-2H-thiopyran-4-carboxamide derivative where the phenyl group is substituted at position 4 with a specific five-membered or 6-membered heteroaryl group, has such great anti-virus activity that the oral dosing thereof at a low dose enabled the therapeutic treatment of the diseases.

Tetrahydro-2H-thiopyran-4-carboxamide derivative

Growing community of inventors

Tokyo, Japan

Akio Kamikawa