Abstract: The present technology provides methods end medicaments useful for treating prostate cancer and breast cancer. Such methods include administering at least one of cyclo[Phe-D-Pro-Phe-Trp] and cyclo[Phe-D-Pro-Phe-D-Trp] to a subject suffering from prostate cancer or breast cancer.

Abstract: An agent of the present invention comprising poultry feet or a processed product thereof, preferably a hydrolysate of an extract of poultry feet, promotes hyaluronic acid production, thereby exhibiting excellent effects of preventing or treating a joint disorder, improving skin dryness, wrinkles or skin tension, moisturizing the skin, etc. The agent is thus useful as a medicament, a quasi-drug, a cosmetic product, a food product or an animal feed.

Abstract: Abuse-resistant opioid compounds, drug delivery systems, pharmaceutical compositions comprising an opioid covalently bound to a chemical moiety are provided. Methods of delivering an active ingredient to a subject and methods of preventing opioid abuse are also provided.

Abstract: The present invention relates to tripeptide compounds according to the general formula (1) and their use as a medicament, in particular as anti-inflammatory agents.

Abstract: The present invention relates to synthetic analgesic peptides that are analogs of the ?-conotoxin peptide RgIA and their use for treating pain and other disorders.

Abstract: The present invention is directed to a method of producing analgesia in a mammalian subject. The method includes administering to the subject an omega conopeptide, preferably ziconotide, in combination with an analgesic selected from the group consisting of morphine, bupivacaine, clonidine, hydromorphone, baclofen, fentanyl l, buprenorphine, and sufentanil, or its pharmaceutically acceptable salts thereof, wherein the ?-conopeptide retains its potency and is physically and chemically compatible with the analgesic compound. A preferred route of administration is intrathecal administration, particularly continuous intrathecal infusion. The present invention is also directed to a pharmaceutical formulation comprising an omega conopeptide, preferably ziconotide, an antioxidant, in combination with an analgesic selected from the group consisting of morphine, bupivacaine, clonidine, hydromorphone, baclofen, fentanyl, buprenorphine, and sufentanil.

Abstract: The present technology provides methods of generating the peptides, and pharmaceutically acceptable salts of the peptides and intermediates thereof. In some embodiments, the peptide is D-Arg-2?6?-Dmt-Lys-Phe-NH2.

Abstract: The proposed drug relates to medicine and veterinary applications, in particular, as a means for effective control of acute and/or chronic pain, and may be used in emergency medicine for the treatment of acute and/or chronic pain, including the late stages of cancer. The stated means is based on a compound for preventing and/or treating acute or chronic pain in a subject, including an analgesic peptide having an amino acid sequence H-Tyr-D-Arg-Phe-Gly-NH2 or an amino acid sequence H-Tyr-D-Arg-Phe-Sar-OH. Also, a method of use/administration of the compound for the prevention and/or treatment of acute and/or chronic pain is disclosed.

Abstract: The present invention relates to tripeptide compounds according to the general formula (1) and their use as a medicament, in particular as anti-inflammatory agents.

Abstract: Provided are a fluorine-containing amino acid prodrug represented by general formula (I) that makes a fluorine-containing amino acid which is a group 2 metabotropic glutamate receptor agonist into a prodrug, or a pharmaceutically acceptable salt thereof.

Abstract: Compounds of general formula (I): R1-Wn-Xm-AA1-AA2-AA3-AA4-AA5-AA6-AA7-AA8-AA9-Yp-Zq-R2 (I) their stereoisomers, mixtures thereof and/or their cosmetically or pharmaceutically acceptable salts, preparation processes, cosmetic or pharmaceutical compositions which contain them and their use in medicine, particularly in the treatment and/or prevention of pain, inflammation, itching, neurological, compulsive and/or neuropsychiatric diseases and/or disorders and in processes of treatment and/or care of the skin, hair and/or mucous membranes mediated by neuronal exocytosis.

Abstract: The present invention relates to a plurality of dosage forms comprising a first dosage form and second dosage form each comprising a therapeutic agent, such as an opioid; wherein the dosage strength of the second dosage form is greater than that of the first dosage form; and wherein the steady state Cave and the steady state AUC of the first and second dosage forms are dose proportional and the single dose Cmax of the second dosage form is less than the minimum level for dose proportionality with respect to the first dosage form. The present invention also relates to methods of administering such dosage forms to a patient, as well as to kits comprising such dosage forms and instructions for administration of the dosage forms to a patient. The inventors believe that the dosage forms and methods of the present invention will lead to improved safety and patient acceptance.

Abstract: The present invention concerns a non-toxic solid pharmaceutical composition for oral administration, containing one or more cysteine compounds from the group of L-cysteine, D-cysteine and N-acetyl cysteine, combined with one or more additional active agents, at least one of which being selected from cystine, glutathione and methionine, the composition further containing one or more pharmaceutical additives. Further, the invention concerns a method for reducing the incidence of severe headaches, particularly migraine and/or cluster headaches.

Abstract: N-type voltage-gated calcium channels (CaV2.2) are critical mediators of neurotransmitter release and are thought to be involved with transmission of nociception. The use of conventional CaV2.2 blockers in pain therapeutics is limited by side effects. Reported herein is a means to suppress both inflammatory and neuropathic pain without directly blocking CaV2.2, but rather by inhibiting the binding of the axonal collapsin response mediator protein 2 (CRMP-2), a protein known to enhance CaV2.2 function. A 15 amino acid peptide of CRMP-2 fused to the protein transduction domain of the HIV tat protein (TAT CBD3) reduced meningeal blood flow induced by activation of the trigeminovascular system, prevented inflammation-induced tactile hypernociception induced by intraplantar formalin and nocifensive behavior following corneal capsaicin application, and reversed neuropathic hypernociception produced by the antiretroviral drug 2?,3?-dideoxycytidine. Preventing CRMP-2—mediated enhancement of CaV2.

Abstract: The present invention features peptides, compositions, and related methods for treating gastrointestinal disorders and conditions, including but not limited to, irritable bowel syndrome (IBS), gastrointestinal motility disorders, functional gastrointestinal disorders, gastroesophageal reflux disease (GERD), duodenogastric reflux, Crohn's disease, ulcerative colitis, inflammatory bowel disease, functional heartburn, dyspepsia, visceral pain, gastroparesis, chronic intestinal pseudo-obstruction (or colonic pseudo-obstruction), disorders and conditions associated with constipation, and other conditions and disorders are described herein. using peptides and other agents that activate the guanylate cyclase C (GC-C) receptor.

Abstract: The present invention relates to Huwentoxin-IV variants, polynucleotides encoding them, methods of making and using the foregoing, and methods of alleviating pain with peptide inhibitors of Nav1.7.

Abstract: Ocular analgesics for topical administration are described. The topical ocular analgesic includes a neo-tryptophan-containing neurotensin analog. The topical ocular analgesic may alternatively include a buffered salt solution, a local anesthetic solution, a tissue penetrating agent, and/or an opiate. The neo-tryptophan-containing neurotensin analog may be present in a dose of about 0.0005 to about 1.2 mg.

Abstract: Surgical implants of the present disclosed include a film comprising a first therapeutic agent and a mesh comprising a second therapeutic agent. The surgical implant includes a film in direct contact with a mesh. The first therapeutic agent may be released at a first rate and the second therapeutic agent may be released at a second rate.

Abstract: Disclosed is a composition of matter comprising an isolated polypeptide, which is a peripherally-restricted Nav1.7 inhibitor. In some disclosed embodiments, the isolated polypeptide is an inhibitor of Nav1.7. Other embodiments are conjugated embodiments of the inventive composition of matter and pharmaceutical compositions containing the inventive composition of matter. Isolated nucleic acids encoding some embodiments of inventive polypeptides and expression vectors, and recombinant host cells containing them are disclosed. A method of treating or preventing pain is also disclosed.

Abstract: The invention provides agents useful for treating pain. An exemplary agent comprises or consists of the a portion of a retroviral Tat protein. One such agent is the peptide Tat-NR2B9c. This peptide has previously been described as an agent for inhibiting damaging effects of stroke and similar conditions via inhibition of PSD95 interactions with NMDA receptors and/or NOS. The present application provides data showing that the Tat-NR2B9c peptides is effective in alleviation of pain. The alleviation of pain can be obtained at a dose of the peptide below the dose required to inhibit PSD-95 interactions with NMDAR or NOS.

Abstract: Disclosed are compositions and methods related to improving pharmacological properties of bioactive compounds targeting nervous system.

Abstract: Disclosed is a method for treating cancer and/or pain using an intra-patient dose escalation procedure to deliver dosages of crotoxin.

Abstract: The present invention relates to the use of at least one botulinum neurotoxin for the production of a medicament for treating or preventing pain induced by a medicament used for treating the AIDS virus.

Abstract: The present invention is directed to a method of producing analgesia in a mammalian subject. The method includes administering to the subject an omega conopeptide, preferably ziconotide, in combination with an analgesic selected from the group consisting of morphine, bupivacaine, clonidine, hydromorphone, baclofen, fentanyl 1, buprenorphine, and sufentanil, or its pharmaceutically acceptable salts thereof, wherein the ?-conopeptide retains its potency and is physically and chemically compatible with the analgesic compound. A preferred route of administration is intrathecal administration, particularly continuous intrathecal infusion. The present invention is also directed to a pharmaceutical formulation comprising an omega conopeptide, preferably ziconotide, an antioxidant, in combination with an analgesic selected from the group consisting of morphine, bupivacaine, clonidine, hydromorphone, baclofen, fentanyl, buprenorphine, and sufentanil.

Abstract: A first aspect of the invention is a compound (sometimes also referred to herein as an “active agent” or “active compound”) of Formula Ia, or more particularly Formula Ib: or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.

Abstract: The present invention relates to modified opiorphin peptides as new inhibitors of metallo-ectopeptidases.

Abstract: The present invention provides a constant release copolymer composition adapted for use in a controlled release formulation for a bioactive agent, such as a formulation adapted for implantation within a patient's body tissues as a depot to release the agent over a period of time, wherein the copolymer provides a substantially constant rate of release of the bioactive agent over the time period for which the depot persists in the body tissues. The copolymer includes a PLG copolymer and a PLG oligomer of about 5-10 kDa average molecular weight, which can lack free carboxylic acid groups. When the PLG copolymer is a low burst copolymer, the constant release copolymer composition is a low burst, constant release copolymer composition adapted for implantation in the body tissues of a mammal, wherein a substantially constant rate of release of the bioactive agent is achieved.

Abstract: The use of opioid peptides of a novel structure is claimed which, in addition to a pharmacophore, additionally contain structural elements reactive with tachykinin receptors. Due to the synergistic reactivity of the opioid with an additional element, an increased analgesic activity is obtained facilitating protracted effective use due to decreased drug tolerance effects. The drugs may particularly be of use in the treatment of chronic pain as effective analgesics during inflammation caused by rheumatism, gout, neurodegenerative states, post-surgical and post-traumatic inflammations or ones induced by tumors.

Abstract: Provided are fragments of human p97 (melanotransferrin) polypeptides having blood-brain barrier (BBB) transport activity, including variants and combinations thereof, conjugates comprising said p97 fragments, and related methods of use thereof, for instance, to facilitate delivery of therapeutic or diagnostic agents across the BBB.

Abstract: Compounds of the formula I wherein R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a C5-C10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; or R3 is a C2-C4alkyl chain with at least 2 chloro or 3 fluoro substituents; or R3 is C3-C7cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C1-C4alkyl, halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylamino, C1-C6dialkylamino or; R4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R4 is Het, carbocyclyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of ca

Abstract: The present invention provides a method for ameliorating inflammatory and/or neuropathic pain in a subject by modifying the activity of N-methyl-D-aspartate (NMDA) receptors in cells of the subject by inhibition of the interaction of the unique domain of the tyrosine kinase Src enzyme and the NMDA receptor complex.

Abstract: N-acyldipeptide derivatives are described. Compositions comprising the N-acyldipeptide derivatives are therapeutically effective for topical or systemic administration to alleviate or improve conditions, disorders, diseases, symptoms or syndromes associated with a tumor, cancer, immune, nervous, vascular, musculoskeletal or cutaneous system, or other tissue or system in a subject.

Abstract: The present invention provides peptides capable of sustaining antagonist activity against substance P for long periods of time. A peptide selected from (a) to (d) can sustain antagonist activity against substance P, analgesic activity, and anti-inflammation activity for a long period of time: (SEQ ID NO: 3) (a)?Ala-Tyr-Gln-Leu-Glu-His-Thr-DTrp-Gln-Gly-Leu- Leu-NH2; (b) a peptide consisting of a partial sequence of (a), which consists of 6 to 11 consecutive amino acids comprising at least the C-terminal Thr-DTrp-Gln-Gly-Leu-Leu-NH2 (SEQ ID NO: 18); (c) Ala-Tyr-Gln-Leu-Glu-His-Thr-Phe-Gln-DTrp-Leu-Leu-NH2 (SEQ ID NO: 4); and (d) a peptide consisting of a partial sequence of (c), which consists of 6 to 11 consecutive amino acids comprising at least the C-terminal Thr-Phe-Gln-DTrp-Leu-Leu-NH2 (SEQ ID NO: 8).

Abstract: Botulinum toxin, among other presynaptic neurotoxins is used for the treatment and prevention of migraine and other headaches associated with vascular disorders. Presynaptic neurotoxins are delivered focally, targeting the sphenopalatine ganglion. Exemplary delivery is carried out by way of injection.

Abstract: Novel template-fixed ?-hairpin peptidomimetics of the general formula (I): cyclo[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-P13-P14-T1-T2] wherein the single elements T or P are ?-amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property of antagonizing the biological effect of the receptor FPR1. They can be used as medicaments to treat or prevent diseases or conditions in the areas of inflammatory diseases, allergic conditions, immunological disorders, neuroinflammation, neurological disorders, obstructive airway diseases, infectious diseases, ischemic reperfusion injuries and proliferative disorders such as e.g. cancer. These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

Abstract: Bioavailability of peptide active agents to be administered orally is enhanced by a pharmaceutical composition providing targeted release of the peptide to the intestine by combining the composition with an absorption enhancer. Bioavailability is further significantly increased by administering the composition in an acid-resistant protective vehicle which transports components of the invention through the stomach. The composition may optionally further include a sufficient amount of a pH-lowering agent to lower local intestinal pH. All components are released together into the intestine with the peptide.

Abstract: Oral dosage forms as a biodegradable, water soluble film for delivering pharmaceutically active agents, to patients through insertion into the mouth of patient and methods for administering pharmaceutically active agents to patients by insertion into the mouth to provide selective uptake of said agents through the mucosa and thus avoiding the gastrointestinal tract.

Abstract: The present invention relates to the use of Meteorin for the treatment of allodynia, hyperalgesia, spontaneous pain and phantom pain. In a preferred embodiment the disorder to be treated is allodynia, and hyperalgesia, more preferably allodynia including thermal and tactile allodynia.

Abstract: Compounds of Formula II wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4? is C1-C6alkyl, C1-C6haloalkyl or oxetany-3-yl. for use in the prophylaxis or treatment of a disorder characterized by inappropriate expression or activation of cathepsin S.

Abstract: The present invention provides for silk-derived compositions for treating a wide variety of ocular conditions. The composition is produced by processing the silk cocoon into a water-based solution (i.e., a dissolved silk), which is then cast into a film. The film may be transparent to visible light, and curved in shape for easy application to the ocular surface. The silk film may either self-adhere or be sutured to cover the wound. The degradation time of the film may range from 1 minute to 24 hours, or from 2 hours to 20 hours. The present compositions can help regenerate damaged corneal tissue, thus promoting healing.

Abstract: The present disclosure provides methods of diagnosing painful intervertebral discs. The present disclosure also provides methods of treating a painful intervertebral disc.

Abstract: The present invention is directed to a method of producing analgesia in a mammalian subject. The method includes administering to the subject an omega conopeptide, preferably ziconotide, in combination with an analgesic selected from the group consisting of morphine, bupivacaine, clonidine, hydromorphone, baclofen, fentanyl 1, buprenorphine, and sufentanil, or its pharmaceutically acceptable salts thereof, wherein the ?-conopeptide retains its potency and is physically and chemically compatible with the analgesic compound. A preferred route of administration is intrathecal administration, particularly continuous intrathecal infusion. The present invention is also directed to a pharmaceutical formulation comprising an omega conopeptide, preferably ziconotide, an antioxidant, in combination with an analgesic selected from the group consisting of morphine, bupivacaine, clonidine, hydromorphone, baclofen, fentanyl, buprenorphine, and sufentanil.

Abstract: This invention relates to an isolated, synthetic or recombinant peptide, wherein the peptide comprises the sequence: C K G K G A Xaa1 C R Xaa2 Xaa3 Xaa4 Y Xaa5 C C Xaa6 G Xaa7 C R Xaa8 Xaa9 R C SEQ ID NO: 1 wherein Xaa1, Xaa3, Xaa4, Xaa6, Xaa7 and Xaa8 are independently selected from serine and threonine; Xaa2 is selected from arginine and lysine; Xaa5 is selected from aspartic acid and glutamic acid; and Xaa9 is selected from glycine, alanine, valine, leucine and isoleucine.

Abstract: Transport peptides, alone or attached to a cargo moiety, are capable of targeted axonal import into the spinal cord and other structures of the central nervous system. The transport peptides can be used to deliver therapeutic agents and other molecules of interest from the periphery to the central nervous system, providing a means to detect, treat or prevent neurodegenerative diseases, stroke, chronic pain and other conditions via minimally invasive techniques of administration.

Abstract: A pharmaceutical composition of glutathione and acetaminophen and preparation method thereof. The active ingredients of the composition include glutathione with composition ration of 0.1%˜99.9% and acetaminophen with composition ratio of 99.9%˜0.1%. The further purpose of the invention is to prepare glutathione and acetaminophen composition (raw materials) into various pharmaceutically acceptable dosage forms, such as tablets, sustained/controlled release preparations, capsules, pills, syrups, films, granules, oral solutions, oral suspensions, oral emulsions and oral powders. The beneficial effects of the invention is reflected in that glutathione and acetaminophen combination can effectively prevent the liver cell damage and necrosis caused by acetaminophen overdose and is strongly in favor of cancer pain relief and chemotherapy.

Abstract: Surgical implants are provided which include a film comprising a first therapeutic agent and a mesh comprising a second therapeutic agent. The surgical implant includes a film in direct contact with a mesh. The first therapeutic agent may be released at a first rate and the second therapeutic agent may be released at a second rate.

Abstract: Surgical implants are provided which include a film comprising a first therapeutic agent and a mesh comprising a second therapeutic agent. The surgical implant includes a film in direct contact with a mesh. The first therapeutic agent may be released at a first rate and the second therapeutic agent may be released at a second rate.

Abstract: Surgical implants are provided which include a film comprising a first therapeutic agent and a mesh comprising a second therapeutic agent. The surgical implant includes a film in direct contact with a mesh. The first therapeutic agent may be released at a first rate and the second therapeutic agent may be released at a second rate.

Abstract: Provided is a modified human tumor necrosis factor receptor-1 polypeptide or a fragment thereof that binds to a tumor necrosis factor in vivo or ex vivo. The modified human tumor necrosis factor receptor-1 polypeptide or fragment exhibits improved ability to bind tumor necrosis factor and resistance to proteases.

Abstract: An object of the present invention is to provide a substance which is able to be an active ingredient for the improvement of dysfunction caused by nerve damage. An improving agent for dysfunction due to nerve damage of the present invention as a means for resolution thereof is characterized in that it comprises an endo-?-N-acetylglucosaminidase type enzyme which hydrolyzes an N-acetylglucosamide bond in a keratan sulfate backbone as an active ingredient. When the improving agent of the present invention is administered, clinical improvement is achieved in motor neuron dysfunction and sensory neuron dysfunction such as neuropathic pain represented by a pain caused by allodynia and hyperalgesic reaction of the object to be treated.