公开(公告)号：US10093696B2

公开(公告)日：2018-10-09

申请号：US15507835

申请日：2015-09-02

申请人： NICOX SCIENCE IRELAND

发明人： Nicoletta Almirante ,  Laura Storoni ,  Elena Bastia ,  Stefania Brambilla ,  Sergio Romeo

IPC分类号： A61K38/00 ,  C07K5/062 ,  A61K38/05 ,  A61K45/06 ,  A61K9/00

摘要： The present invention relates to nitric oxide donor carnosine derivatives having a great efficacy in reducing elevated intraocular pressure, to processes for their preparation and to their use in the treatment and/or prophylaxis of glaucoma and ocular hypertension.

公开(公告)号：US10071183B2

公开(公告)日：2018-09-11

申请号：US14719674

申请日：2015-05-22

申请人： Agency for Science, Technology and Research

发明人： Charlotte A. E. Hauser ,  Ulung Gondo Kusumo Khoe ,  Archana Mishra

IPC分类号： A61K9/00 ,  A01N63/00 ,  A01N65/00 ,  A01N25/00 ,  A61K47/00 ,  C12N5/00 ,  C12N5/02 ,  A61L27/22 ,  A61K8/04 ,  A61K8/64 ,  A61Q19/00 ,  C07K5/062 ,  C07K5/072 ,  C07K5/083 ,  C07K5/103 ,  C07K7/06 ,  A61L27/52 ,  A61L27/54 ,  A61K38/00

CPC分类号： A61L27/22 ,  A61K8/042 ,  A61K8/64 ,  A61K38/00 ,  A61L27/52 ,  A61L27/54 ,  A61L2430/00 ,  A61Q19/00 ,  C07K5/06026 ,  C07K5/06043 ,  C07K5/06052 ,  C07K5/0606 ,  C07K5/06069 ,  C07K5/06104 ,  C07K5/06113 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/1008 ,  C07K5/101 ,  C07K7/06

摘要： The present invention provides an amphiphilic linear peptide and/or peptoid as well as a hy-drogel that includes the amphiphilic linear peptide/peptoid. The amphiphilic linear pep-tide/peptoid is capable of forming, a hydrogel. These peptides/peptoids include short amphi-philic sequences with a hydrophobic portion of aliphatic amino acids and at least one acidic, neutral, or basic polar amino acid. The amphiphilic linear peptide/peptoid is build up of non repetitive aliphatic amino acids, which may be in the L- or D-form. A plurality of such pep-tides/peptoids assembles to supramolecular helical fibers and forms peptide hydrogels after assembly: A corresponding hydrogel is formed in aqueous solutions at physiological pH and is thus useful for inter alia cell culture, tissue engineering, and drug release. Such hydrogels which are rigid, biocompatible and entrapping up to 99.9% of water are also well suited for applications utilizing electronic devices.

公开(公告)号：US10035819B2

公开(公告)日：2018-07-31

申请号：US15482385

申请日：2017-04-07

申请人： The Salk Institute for Biological Studies

发明人： Ronald M. Evans ,  Michael Downes

IPC分类号： A01N43/40 ,  A61K31/4412 ,  C07K5/062 ,  C07C233/75 ,  C07D213/56 ,  C07D231/12 ,  C07D307/54 ,  C07D333/38 ,  C07D295/13 ,  C07D213/40 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

CPC分类号： C07K5/06034 ,  C07C233/73 ,  C07C233/75 ,  C07C233/87 ,  C07C235/42 ,  C07C235/48 ,  C07C235/84 ,  C07C237/32 ,  C07C255/57 ,  C07C259/06 ,  C07C317/44 ,  C07C2601/02 ,  C07C2601/08 ,  C07D205/04 ,  C07D209/34 ,  C07D213/40 ,  C07D213/56 ,  C07D213/64 ,  C07D231/12 ,  C07D271/12 ,  C07D295/13 ,  C07D295/155 ,  C07D305/06 ,  C07D307/54 ,  C07D307/68 ,  C07D307/81 ,  C07D307/83 ,  C07D309/04 ,  C07D309/06 ,  C07D333/24 ,  C07D333/38 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07K5/06026

摘要： Provided herein are deuterated compounds and compositions useful in increasing PPARδ activity. The compounds have a formula where L5 comprises at least one deuterium. Exemplary species include The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).

公开(公告)号：US10011632B2

公开(公告)日：2018-07-03

申请号：US14917127

申请日：2012-08-21

申请人： Eric Wang ,  Hartmuth C. Kolb ,  Anna Katrin Szardenings ,  Changhui Liu ,  Joseph C. Walsh ,  Gang Chen ,  Anjana Sinha ,  Dhanalakshmi Kasi ,  Chul Yu ,  Umesh B. Gangadharmath ,  Wei Zhang ,  Tieming Zhao ,  Vani P. Mocharla

发明人： Eric Wang ,  Hartmuth C. Kolb ,  Anna Katrin Szardenings ,  Changhui Liu ,  Joseph C. Walsh ,  Gang Chen ,  Anjana Sinha ,  Dhanalakshmi Kasi ,  Chul Yu ,  Umesh B. Gangadharmath ,  Wei Zhang ,  Tieming Zhao ,  Vani P. Mocharla

IPC分类号： C07K5/02 ,  A61K51/04 ,  C07D249/06 ,  C07D249/04 ,  A61K51/08 ,  C07K5/062 ,  C07K5/072 ,  C07D403/12 ,  C07D213/81 ,  C07D213/82 ,  C07D233/78 ,  C07D233/96 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  C07D239/60 ,  C07D251/30 ,  C07D263/34 ,  C07D207/16 ,  C07D277/56 ,  C07D209/48 ,  A61K38/00

CPC分类号： C07K5/0215 ,  A61K38/00 ,  A61K51/0402 ,  A61K51/0453 ,  A61K51/0497 ,  A61K51/088 ,  C07D207/16 ,  C07D209/48 ,  C07D213/81 ,  C07D213/82 ,  C07D233/78 ,  C07D233/96 ,  C07D239/60 ,  C07D249/04 ,  C07D249/06 ,  C07D251/30 ,  C07D263/34 ,  C07D277/56 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07K5/06026 ,  C07K5/06113

摘要： Compounds for targeting and agents for imaging, Prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.

公开(公告)号：US09994613B2

公开(公告)日：2018-06-12

申请号：US15288863

申请日：2016-10-07

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Marion W. Wannamaker ,  Robert J. Davies

IPC分类号： C07K5/062 ,  A61K38/00 ,  A61P17/00 ,  C07K5/06 ,  C07D307/02 ,  C07D477/02 ,  C07D477/20 ,  C07K5/02 ,  C07K5/08 ,  C07D207/16 ,  C07K5/083

CPC分类号： C07K5/06034 ,  A61K38/00 ,  C07D207/16 ,  C07D307/02 ,  C07D477/02 ,  C07D477/20 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06 ,  C07K5/06008 ,  C07K5/06191 ,  C07K5/08 ,  C07K5/0808 ,  Y02A50/385 ,  Y02A50/387 ,  Y02A50/389 ,  Y02A50/475

摘要： This invention describes an ICE inhibitor prodrug (I) having good bioavailability. Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

公开(公告)号：US09975921B2

公开(公告)日：2018-05-22

申请号：US14927669

申请日：2015-10-30

申请人： Helsinn Healthcare SA

发明人： Keith Lorimer ,  Seemon H Pines ,  Bernhard Paul ,  Benjamin Littler

IPC分类号： C07D401/00 ,  C07K5/062 ,  C07D401/06 ,  C07K5/02

CPC分类号： C07K5/06026 ,  C07D401/06 ,  C07K5/0202

摘要： Crystalline forms of anamorelin which are useful as pharmaceutical agents are disclosed. Methods of production and isolation of these polymorphs and pharmaceutical compositions which include these polymorphs and pharmaceutical methods of treatment are also disclosed. The crystalline polymorphs of the present invention are useful as they act directly on the pituitary gland cells to release growth hormone.

公开(公告)号：US09944674B2

公开(公告)日：2018-04-17

申请号：US14111738

申请日：2012-04-15

申请人： Jan-Eric Ahlfors ,  Khalid Mekouar

发明人： Jan-Eric Ahlfors ,  Khalid Mekouar

IPC分类号： C07K5/103 ,  C07K5/02 ,  C07K5/083 ,  C07K5/062 ,  C07K5/065 ,  C07K5/072 ,  C07K5/087 ,  C07K5/093 ,  C07K5/097 ,  C07K14/81 ,  A61K38/06

CPC分类号： C07K5/1008 ,  A61K38/06 ,  C07K5/02 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/06078 ,  C07K5/06095 ,  C07K5/06104 ,  C07K5/06113 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/081 ,  C07K5/0812 ,  C07K5/0819 ,  C07K5/0821 ,  C07K14/8139

摘要： The present invention relates to compounds of Formula I, II, IA-VA, IVA1-IVA5, IIIA1-IIIA5 and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more cysteine proteases. Also described are methods where the compounds of Formula I, II, IA-VA, IVA1-IVA5, IIIA1-IIIA5 are used in the prevention and/or treatment of various diseases and conditions in subjects, including cysteine protease-mediated diseases and/or caspase-mediated diseases such as sepsis, myocardial infarction, cancer, tissue atrophy, ischemia, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative diseases such as multiple sclerosis (MS), amyotrophic lateral sclerosis (ALS), Alzheimer's disease, Parkinson's disease, and Huntington's disease.

公开(公告)号：US20180037581A1

公开(公告)日：2018-02-08

申请号：US15785608

申请日：2017-10-17

申请人： Bristol-Myers Squibb Company

发明人： Ivar M. MCDONALD ,  Naidu S. CHOWDARI ,  Walter Lewis JOHNSON ,  Yong ZHANG ,  Robert M. BORZILLERI ,  Sanjeev GANGWAR

IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  A61K47/68 ,  C07K5/062

CPC分类号： C07D471/04 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6889 ,  C07D487/04 ,  C07D519/00 ,  C07K5/06052

摘要： Benzodiazepine dimers having a structure represented by wherein X comprises a heteroaromatic moiety and is as further defined in the application; R1 is and the other variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).

公开(公告)号：US20180030088A1

公开(公告)日：2018-02-01

申请号：US15726071

申请日：2017-10-05

申请人： Albireo AB

发明人： Per-Göran Gillberg ,  Hans Graffner ,  Ingemar Starke

IPC分类号： C07K5/065 ,  A61K38/05 ,  A61K31/575 ,  C07K5/062 ,  A61K31/554 ,  A61K38/00

CPC分类号： C07K5/06078 ,  A61K31/55 ,  A61K31/554 ,  A61K31/575 ,  A61K38/00 ,  A61K38/05 ,  A61K2121/00 ,  C07K5/06026 ,  C07K5/0606

摘要： The present invention regards specific IBAT inhibitors useful in the prophylaxis and/or treatment of a liver disease. It also relates to compositions comprising these IBAT inhibitors, a method for treatment of the disorders and a kit comprising the substances or the compositions.

公开(公告)号：US09872883B2

公开(公告)日：2018-01-23

申请号：US15135147

申请日：2016-04-21

申请人： HELSINN HEALTHCARE SA ,  ONO PHARMACEUTICAL CO., LTD.

发明人： Shin-itsu Kuwabe ,  Takehiko Yanagimachi ,  Hideyuki Yoshiyama ,  Seemon Pines ,  Eleanor De Groot ,  Silvina Garcia Rubio ,  Peter Manini

IPC分类号： C07D401/06 ,  C07D401/12 ,  A61K31/445 ,  A61K38/05 ,  C07K5/062 ,  A61K9/16

CPC分类号： A61K38/05 ,  A61K9/1682 ,  C07D401/06 ,  C07D401/12 ,  C07K5/06034

摘要： The present invention relates to particulate forms of anamorelin monohydrochloride or a composition comprising anamorelin monohydrochloride having controlled chloride content, preferably isolated in an amorphous and/or fine particulate state, processes for making the particulate forms, and pharmaceutical compositions comprising the particulate forms.