公开(公告)号：JP2013253089A

公开(公告)日：2013-12-19

申请号：JP2013160858

申请日：2013-08-01

Applicant: PHARMACYCLICS INC

Inventor： HONIGBERG LEE ,  VERNER ERIK ,  BUGGY JOSEPH J ,  LOURY DAVID ,  CHEN WEI

IPC: C07D487/04 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/5377 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D471/04

Abstract: PROBLEM TO BE SOLVED: To provide an irreversible Bruton's kinase inhibitor compound to be used in treatment of diseases.SOLUTION: There is provided a compound illustrated in formulae.

公开(公告)号：JP2004091495A

公开(公告)日：2004-03-25

申请号：JP2003377620

申请日：2003-11-06

Applicant: Pharmacyclics Inc ,  Univ Texas Syst ,  ファーマサイクリクス,インコーポレイテッド ,  ボード オブ リージェンツ, ザ ユニバーシティ オブ テキサス システムBoard Of Regents,The University Of Texas System

Inventor： SESSLER JONATHAN L ,  HARRIMAN ANTHONY M ,  MILLER RICHARD A ,  MODY TARAK D ,  HEMMI GREGORY W ,  KRAAL VLADIMIR A ,  MAGDA DARREN

IPC: A61K31/40 ,  A61K31/407 ,  A61K41/00 ,  A61K47/48 ,  A61K49/00 ,  A61K49/06 ,  A61K49/08 ,  A61K51/00 ,  A61K51/04 ,  A61L2/00 ,  A61P35/02 ,  A61P43/00 ,  B01J31/06 ,  B01J31/16 ,  B01J31/18 ,  C07D487/22 ,  C07H21/00

CPC classification number: A61K51/0485 ,  A61K41/0038 ,  A61K41/0057 ,  A61K41/0076 ,  A61K47/546 ,  A61K49/0021 ,  A61K49/0054 ,  A61K49/085 ,  A61K49/10 ,  A61K49/106 ,  A61K49/126 ,  A61L2/0011 ,  B01J31/061 ,  B01J31/1658 ,  B01J31/1805 ,  B01J31/1815 ,  B01J2531/025 ,  B01J2531/23 ,  B01J2531/26 ,  B01J2531/27 ,  B01J2531/28 ,  B01J2531/36 ,  B01J2531/37 ,  B01J2531/38 ,  B01J2531/72 ,  B01J2531/842 ,  B01J2531/845 ,  B01J2531/847 ,  B01J2531/96 ,  C07D487/22 ,  C07H21/00

Abstract: PROBLEM TO BE SOLVED: To obtain texaphyrin for radiosensitization. SOLUTION: A medicinal composition used for a radiosensitizer is prepared by using the texaphyrin. The texaphyrin is an aromatic 5 position (and heptacyclic) macrocycle (enlarged porphyrin) and, may be due to its inherent lipophilic property, shows larger biolocalization in non-neoplasm organs and non-atheroma plaque in neoplasm organ and atheroma each possible to be a malignant or benign tumor. The texaphyrin improves radiation damage and overcomes many defects of conventional radiosensitizers. COPYRIGHT: (C)2004,JPO

公开(公告)号：JP2012105681A

公开(公告)日：2012-06-07

申请号：JP2012049524

申请日：2012-03-06

Applicant: Pharmacyclics Inc ,  ファーマサイクリクス,インコーポレイテッド

Inventor： HONIGBERG LEE ,  VERNER ERIK ,  PAN ZHENGYING

IPC: C12N9/12 ,  A61K31/519 ,  A61P1/04 ,  A61P1/16 ,  A61P3/02 ,  A61P3/10 ,  A61P5/00 ,  A61P7/06 ,  A61P9/00 ,  A61P13/10 ,  A61P15/00 ,  A61P17/00 ,  A61P17/06 ,  A61P17/14 ,  A61P19/02 ,  A61P21/04 ,  A61P25/00 ,  A61P29/00 ,  A61P37/06 ,  A61P43/00 ,  C07D487/04

CPC classification number: A61K31/52 ,  A61K9/4825 ,  A61K31/00 ,  A61K31/519 ,  A61K39/3955 ,  A61K45/06 ,  C07D487/04 ,  C07K16/2887 ,  C07K2317/24 ,  A61K2300/00

Abstract: PROBLEM TO BE SOLVED: To bring advantages on the therapy of patients having related diseases by inhibiting the activity of tyrosine kinase.SOLUTION: There are provided: compounds that form covalent bonds with Bruton's tyrosine kinase (Btk); irreversible inhibitors of Btk; methods for the preparation of the compounds; pharmaceutical compositions that include the compounds; and also methods of using the Btk inhibitors, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Abstract translation: 要解决的问题：通过抑制酪氨酸激酶的活性，为治疗患有相关疾病的患者带来优势。 提供：与Bruton酪氨酸激酶（Btk）形成共价键的化合物; Btk不可逆抑制剂; 化合物的制备方法; 包括化合物的药物组合物; 以及使用Btk抑制剂单独或与其它治疗剂组合用于治疗自身免疫性疾病或病症，异种免疫疾病或病症，癌症，包括淋巴瘤和炎性疾病或病症的方法。 版权所有（C）2012，JPO＆INPIT

公开(公告)号：JP2011182800A

公开(公告)日：2011-09-22

申请号：JP2011123587

申请日：2011-06-01

Applicant: Pharmacyclics Inc ,  ファーマサイクリクス,インコーポレイテッド

Inventor： BUGGY JOSEPH

IPC: C12N15/09 ,  G01N33/50 ,  A61K38/00 ,  A61K39/395 ,  A61K45/00 ,  A61K48/00 ,  A61P35/00 ,  C07K16/40 ,  C12N1/15 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N9/14 ,  C12N9/18 ,  C12N9/78 ,  C12P21/08 ,  C12Q1/02 ,  C12Q1/34 ,  C12Q1/527 ,  C12Q1/68 ,  G01N33/15 ,  G01N33/566

CPC classification number: C12N9/18 ,  A61K38/00 ,  A61K48/00

Abstract: PROBLEM TO BE SOLVED: To provide novel nucleic acids that encode novel HDAC proteins, which have an affect on chromatin structure and transcription.
SOLUTION: There are provided: vectors and host cells comprising those nucleic acid sequences; chimeric polypeptide molecules comprising the polypeptides fused to heterologous polypeptide sequences; antibodies which bind to the polypeptides; and methods of producing the polypeptides. Further, there are provided methods of identifying novel compositions which mediate HDAC8 and the use of such compositions in diagnosis and treatment of disease.
COPYRIGHT: (C)2011,JPO&INPIT

Abstract translation: 要解决的问题：提供编码新型HDAC蛋白质的新型核酸，其对染色质结构和转录有影响。 提供：提供了包含那些核酸序列的载体和宿主细胞; 包含与异源多肽序列融合的多肽的嵌合多肽分子; 结合多肽的抗体; 以及产生多肽的方法。 此外，提供了鉴定介导HDAC8的新组合物的方法以及这些组合物在疾病诊断和治疗中的用途。 版权所有（C）2011，JPO＆INPIT

公开(公告)号：JP2010235628A

公开(公告)日：2010-10-21

申请号：JP2010155965

申请日：2010-07-08

Applicant: Pharmacyclics Inc ,  ファーマサイクリクス,インコーポレイテッド

Inventor： HONIGBERG LEE ,  VERNER ERIK ,  PAN ZHENGYING

IPC: C07D487/04 ,  A61K31/519 ,  A61P1/04 ,  A61P1/16 ,  A61P3/10 ,  A61P5/14 ,  A61P7/06 ,  A61P9/00 ,  A61P11/06 ,  A61P13/02 ,  A61P15/00 ,  A61P17/00 ,  A61P17/06 ,  A61P17/14 ,  A61P19/02 ,  A61P21/04 ,  A61P35/00 ,  A61P35/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00

CPC classification number: A61K31/52 ,  A61K9/4825 ,  A61K31/00 ,  A61K31/519 ,  A61K39/3955 ,  A61K45/06 ,  C07D487/04 ,  C07K16/2887 ,  C07K2317/24 ,  A61K2300/00

Abstract: PROBLEM TO BE SOLVED: To inhibit the activity of tyrosine kinase and to bring advantages on the therapy of patients of related diseases. SOLUTION: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk), also described are irreversible inhibitors of the Btk, methods for the preparation of the compounds, also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancers including lymphoma, and inflammatory diseases or conditions. COPYRIGHT: (C)2011,JPO&INPIT

Abstract translation: 要解决的问题：抑制酪氨酸激酶的活性，为相关疾病患者的治疗带来好处。 本文公开了与Bruton酪氨酸激酶（Btk）形成共价键的化合物，也描述了Btk的不可逆抑制剂，制备化合物的方法，还公开了包含该化合物的药物组合物。 公开了使用Btk抑制剂的方法，单独或与其它治疗剂组合用于治疗自身免疫性疾病或病症，异种免疫疾病或病症，包括淋巴瘤和炎性疾病或病症的癌症。 版权所有（C）2011，JPO＆INPIT

公开(公告)号：JP2013060466A

公开(公告)日：2013-04-04

申请号：JP2012286719

申请日：2012-12-28

Applicant: Pharmacyclics Inc ,  ファーマサイクリクス,インコーポレイテッド

Inventor： HONIGBERG LEE ,  VERNER ERIK ,  PAN ZHENGYING

IPC: C07D487/04 ,  A61K31/519 ,  A61P35/00

CPC classification number: A61K31/52 ,  A61K9/4825 ,  A61K31/00 ,  A61K31/519 ,  A61K39/3955 ,  A61K45/06 ,  C07D487/04 ,  C07K16/2887 ,  C07K2317/24 ,  A61K2300/00

Abstract: PROBLEM TO BE SOLVED: To provide therapeutic benefit to a patient having relevant diseases by inhibiting tyrosine kinase activity.SOLUTION: There are provided: compounds that form covalent bonds with Bruton's tyrosine kinase (Btk); irreversible inhibitors of Btk; methods for the preparation of the compounds; pharmaceutical compositions that include the compounds; and methods of using the Btk inhibitors, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Abstract translation: 待解决的问题：通过抑制酪氨酸激酶活性为具有相关疾病的患者提供治疗益处。 提供：与Bruton酪氨酸激酶（Btk）形成共价键的化合物; Btk不可逆抑制剂; 化合物的制备方法; 包括化合物的药物组合物; 以及使用Btk抑制剂单独或与其它治疗剂组合用于治疗自身免疫性疾病或病症，异种免疫疾病或病症，癌症，包括淋巴瘤和炎性疾病或病症的方法。 版权所有（C）2013，JPO＆INPIT

公开(公告)号：JP2013014602A

公开(公告)日：2013-01-24

申请号：JP2012196895

申请日：2012-09-07

Applicant: Pharmacyclics Inc ,  ファーマサイクリクス,インコーポレイテッド

Inventor： MADDEN HUGO ,  HEMMI GREG ,  MODY TARAK

IPC: A61K31/409 ,  A61P35/00 ,  A61P35/04 ,  C07D487/22 ,  C07F5/00

Abstract: PROBLEM TO BE SOLVED: To provide a high-purity texaphyrin metal complex, a method for making the complex, and a method for using the complex to treat a disease or the like including cancer and atherosclerosis.SOLUTION: The texaphyrin metal complex has anticancer activity and is represented by formula 1 (wherein: M is a trivalent metal cation such as Gd; each X is OHor the like; Rto Rare independently H, OH or the like; Rand Rare independently H or 1 to 6C alkyl; and each x is independently selected from 2 to 6).

Abstract translation: 待解决的问题：提供高纯度泰克萨菲瑞金属络合物，制备复合物的方法，以及使用该复合物治疗包括癌症和动脉粥样硬化的疾病等的方法。 泰克萨菲瑞金属络合物具有抗癌活性，由式1表示（其中：M为三价金属阳离子如Gd + 3 ;每个X为OH， SP POS =“POST”> - 等; R 3 至R 8 分别为H，OH 等等; R 1 和R 2 独立地为H或1至6C烷基;并且每个x独立地选自2 至6）。 版权所有（C）2013，JPO＆INPIT

公开(公告)号：JP2001316270A

公开(公告)日：2001-11-13

申请号：JP2001071295

申请日：2001-03-13

Applicant: PHARMACYCLICS INC ,  UNIV TEXAS

Inventor： MAGDA DARREN ,  SESSLER JONATHAN L

IPC: C07D487/22 ,  A61K31/40 ,  A61K31/7125 ,  A61K31/7135 ,  A61K41/00 ,  A61K51/04 ,  A61P35/00 ,  C07H21/00 ,  C07H23/00 ,  C12N15/09

Abstract: PROBLEM TO BE SOLVED: To obtain a photosensitizer having excellent tumor selectivity, not requiring rays with short wavelength which causes photoexcitation essential for photosensitization. SOLUTION: This photo-cleavage of RNA using texaphyrin comprises using photosensitive texaphyrin of [formula 1] in preparation of pharmacological composition useful in a process for photo-cleavage of ribonucleic acid polymer.

公开(公告)号：SA112330827B1

公开(公告)日：2015-07-22

申请号：SA112330827

申请日：2012-09-07

Applicant: PHARMACYCLICS INC ,  SERVIER LAB ,  PHARMACYCLICS LLC ,  PHARMACYCLICS INC

Inventor： ANNE JACQUET-BESCOND ,  IOANA KLOOS ,  RENATA ROBERT ,  STÉPHANE DEPIL ,  SRIRAM BALASUBRAMANIAN ,  SYLVAIN FOULIARD ,  MARYLORE CHENEL

Abstract: يتعلقالاختراعالحاليبـ : N-hydroxy-4-{2-[3-(N,N-dimethylaminomethyl)benzofuran-2-ylcarbonylamino]ethoxy} benzamide لهالصيغة (I): أوملحإضافةمنهمعحمضأوقاعدةمقبولةصيدلانيًا،بمفردهأوبالاشتراكمعجراحة،علاجكيماوي chemotherapy ،علاجهرمونيأوعلاجإشعاعي hormone therapy treatment or radiotherapy،للاستخدامفيعلاجالسرطان treatment of cancer ،حيثيتميزالمركببإعطائهلمدة 4 أياممتتالية،وتتبعهذهالفترةالزمنيةبـ 3 أياممتتاليةدونأيإعطاءللمركبالذيلهالصيغة (I)،بشرطألايكونالعلاجالكيماويهو FOLFOX (oxaliplatin/folinic acid/ 5-fluorouracil). الأدوية. شكل 1.

公开(公告)号：TW201601727A

公开(公告)日：2016-01-16

申请号：TW103126513

申请日：2014-08-01

Applicant: 製藥公司 ,  PHARMACYCLICS, INC.

Inventor： 巴拉蘇羅馬尼恩 司瑞雷門 ,  BALASUBRAMANIAN, SRIRAM

IPC: A61K31/52 ,  A61K31/343 ,  A61P35/00

CPC classification number: A61K31/519 ,  A61K31/343 ,  A61K45/06 ,  A61K2300/00

Abstract: 本文揭示ACK抑制劑與HDAC抑制劑之組合用於治療特徵為存在或發展固態腫瘤之疾病及病症。

Abstract in simplified Chinese: 本文揭示ACK抑制剂与HDAC抑制剂之组合用于治疗特征为存在或发展固态肿瘤之疾病及病症。